Lidocaine

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Identification

Summary

Lidocaine is a local anesthetic used in a wide variety of superficial and invasive procedures.

Brand Names

Agoneaze, Akten, Alivio, Anestacon, Anodyne Lpt, Astero, Cathejell, Curacaine, Depo-medrol With Lidocaine, Dermacinrx Lido V Pak, Dermacinrx Phn Pak, Dermacinrx Prikaan, Diphen, Emla, Fortacin, Glydo, Instillagel, Kenalog, Lido Bdk, Lido-prilo Caine Pack, Lidocan, Lidodan, Lidoderm, Lidopac, Lidopril, Lidopro, Lidosol, Lidothol, Lidotral, Lignospan, Marcaine, Max-freeze, Medi-derm With Lidocaine, Neo-bex, Octocaine, Octocaine With Epinephrine, Oraqix, P-care, P-care X, Pliaglis, Prilolid, Prizotral, Procomycin, Readysharp Anesthetics Plus Ketorolac, Readysharp-A, Readysharp-p40, Readysharp-p80, Relador, Synera, Tridacaine, Triple Antibiotic, Venipuncture Px1, Viadur, Xylocaine, Xylocaine With Epinephrine, Xylocard, Xylonor, Zingo, Ztlido

Generic Name

Lidocaine

DrugBank Accession Number

DB00281

Background

Ever since its discovery and availability for sale and use in the late 1940s, lidocaine has become an exceptionally commonly used medication ⁶. In particular, lidocaine's principal mode of action in acting as a local anesthetic that numbs the sensations of tissues means the agent is indicated for facilitating local anesthesia for a large variety of surgical procedures ^10,7,8. It ultimately elicits its numbing activity by blocking sodium channels so that the neurons of local tissues that have the medication applied on are transiently incapable of signaling the brain regarding sensations ^10,7,8. In doing so, however, it can block or decrease muscle contractile, resulting in effects like vasodilation, hypotension, and irregular heart rate, among others ^10,7,8. As a result, lidocaine is also considered a class Ib anti-arrhythmic agent ^7,8,12. Nevertheless, lidocaine's local anesthetic action sees its use in many medical situations or circumstances that may benefit from its action, including the treatment of premature ejaculation ⁵.

Regardless, lidocaine is currently available as a relatively non-expensive generic medication that is written for in millions of prescriptions internationally on a yearly basis. It is even included in the World Health Organization's List of Essential Medicines ⁹.

Type

Small Molecule

Groups

Approved, Vet approved

Structure

Similar Structures

Weight: Average: 234.3373
Monoisotopic: 234.173213336
Chemical Formula: C₁₄H₂₂N₂O

Synonyms

2-(Diethylamino)-2',6'-acetoxylidide
2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide
alpha-diethylamino-2,6-dimethylacetanilide
Lidocaína
Lidocaina
Lidocaine
Lidocainum
Lignocaine
α-diethylamino-2,6-dimethylacetanilide

External IDs

ALGRX 3268
ALGRX-3268
LSM-3165
NSC-40030

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Pharmacology

Indication

Lidocaine is an anesthetic of the amide group indicated for production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks ^10,7.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Dose Form
Treatment of	Acute otitis media		••••••••••••	•••••••• • •••••
Used in combination for symptomatic treatment of	Anal fissures	Combination Product in combination with: Titanium dioxide (DB09536), Bufexamac (DB13346), Bismuth subgallate (DB13909)	••••••••••••	••••••••• •••••••••••
Used in combination for symptomatic treatment of	Anorectal discomfort	Combination Product in combination with: Glycerin (DB09462)	••• •••
Treatment of	Arrhythmia		••••••••••••	••••••••
Used in combination to treat	Back pain lower back	Combination Product in combination with: Salicylamide O-acetic acid (DB16000), Dexamethasone (DB01234), Kebuzone (DB08940), Cyanocobalamin (DB00115)	••••••••••••	•••••••••• ••••••••

Associated Therapies

Contraindications & Blackbox Warnings

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Pharmacodynamics

Excessive blood levels of lidocaine can cause changes in cardiac output, total peripheral resistance, and mean arterial pressure ^10,7. With central neural blockade these changes may be attributable to the block of autonomic fibers, a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system, and/or the beta-adrenergic receptor stimulating action of epinephrine when present ^10,7. The net effect is normally a modest hypotension when the recommended dosages are not exceeded ^10,7.

In particular, such cardiac effects are likely associated with the principal effect that lidocaine elicits when it binds and blocks sodium channels, inhibiting the ionic fluxes required for the initiation and conduction of electrical action potential impulses necessary to facilitate muscle contraction ^10,7,8. Subsequently, in cardiac myocytes, lidocaine can potentially block or otherwise slow the rise of cardiac action potentials and their associated cardiac myocyte contractions, resulting in possible effects like hypotension, bradycardia, myocardial depression, cardiac arrhythmias, and perhaps cardiac arrest or circulatory collapse ^10,7,8.

Moreover, lidocaine possesses a dissociation constant (pKa) of 7.7 and is considered a weak base ⁸. As a result, about 25% of lidocaine molecules will be un-ionized and available at the physiological pH of 7.4 to translocate inside nerve cells, which means lidocaine elicits an onset of action more rapidly than other local anesthetics that have higher pKa values ⁸. This rapid onset of action is demonstrated in about one minute following intravenous injection and fifteen minutes following intramuscular injection ⁷. The administered lidocaine subsequently spreads rapidly through the surrounding tissues and the anesthetic effect lasts approximately ten to twenty minutes when given intravenously and about sixty to ninety minutes after intramuscular injection ⁷.

Nevertheless, it appears that the efficacy of lidocaine may be minimized in the presence of inflammation ⁸. This effect could be due to acidosis decreasing the amount of un-ionized lidocaine molecules, a more rapid reduction in lidocaine concentration as a result of increased blood flow, or potentially also because of increased production of inflammatory mediators like peroxynitrite that elicit direct actions on sodium channels ⁸.

Mechanism of action

Lidocaine is a local anesthetic of the amide type ^10,7,8. It is used to provide local anesthesia by nerve blockade at various sites in the body ^10,7,8. It does so by stabilizing the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action ^10,7,8. In particular, the lidocaine agent acts on sodium ion channels located on the internal surface of nerve cell membranes ^10,7,8. At these channels, neutral uncharged lidocaine molecules diffuse through neural sheaths into the axoplasm where they are subsequently ionized by joining with hydrogen ions ^10,7,8. The resultant lidocaine cations are then capable of reversibly binding the sodium channels from the inside, keeping them locked in an open state that prevents nerve depolarization ^10,7,8. As a result, with sufficient blockage, the membrane of the postsynaptic neuron will ultimately not depolarize and will thus fail to transmit an action potential ^10,7,8. This facilitates an anesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their generation in the first place ^10,7,8.

In addition to blocking conduction in nerve axons in the peripheral nervous system, lidocaine has important effects on the central nervous system and cardiovascular system ^10,7,8. After absorption, lidocaine may cause stimulation of the CNS followed by depression and in the cardiovascular system, it acts primarily on the myocardium where it may produce decreases in electrical excitability, conduction rate, and force of contraction ^10,7,8.

Target	Actions	Organism
ASodium channel protein type 11 subunit alpha	blocker	Humans
ASodium channel protein type 10 subunit alpha	inhibitor	Humans
ASodium channel protein type 9 subunit alpha	inhibitor	Humans
ASodium channel protein type 5 subunit alpha	inhibitor	Humans
UEpidermal growth factor receptor	antagonist	Humans
USodium channel protein type 4 subunit alpha	Not Available	Humans
UAlpha-1-acid glycoprotein 1	Not Available	Humans
UAlpha-1-acid glycoprotein 2	Not Available	Humans

Absorption

In general, lidocaine is readily absorbed across mucous membranes and damaged skin but poorly through intact skin ¹². The agent is quickly absorbed from the upper airway, tracheobronchial tree, and alveoli into the bloodstream ¹². And although lidocaine is also well absorbed across the gastrointestinal tract the oral bioavailability is only about 35% as a result of a high degree of first-pass metabolism ¹². After injection into tissues, lidocaine is also rapidly absorbed and the absorption rate is affected by both vascularity and the presence of tissue and fat capable of binding lidocaine in the particular tissues ¹².

The concentration of lidocaine in the blood is subsequently affected by a variety of aspects, including its rate of absorption from the site of injection, the rate of tissue distribution, and the rate of metabolism and excretion ^10,7,8. Subsequently, the systemic absorption of lidocaine is determined by the site of injection, the dosage given, and its pharmacological profile ^10,7,8. The maximum blood concentration occurs following intercostal nerve blockade followed in order of decreasing concentration, the lumbar epidural space, brachial plexus site, and subcutaneous tissue ^10,7,8. The total dose injected regardless of the site is the primary determinant of the absorption rate and blood levels achieved ^10,7,8. There is a linear relationship between the amount of lidocaine injected and the resultant peak anesthetic blood levels ^10,7,8.

Nevertheless, it has been observed that lidocaine hydrochloride is completely absorbed following parenteral administration, its rate of absorption depending also on lipid solubility and the presence or absence of a vasoconstrictor agent ^10,7,8. Except for intravascular administration, the highest blood levels are obtained following intercostal nerve block and the lowest after subcutaneous administration ^10,7,8.

Additionally, lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion ¹⁰.

Volume of distribution

The volume of distribution determined for lidocaine is 0.7 to 1.5 L/kg ⁸.

In particular, lidocaine is distributed throughout the total body water ⁷. Its rate of disappearance from the blood can be described by a two or possibly even three-compartment model ⁷. There is a rapid disappearance (alpha phase) which is believed to be related to uptake by rapidly equilibrating tissues (tissues with high vascular perfusion, for example) ⁷. The slower phase is related to distribution to slowly equilibrating tissues (beta phase) and to its metabolism and excretion (gamma phase) ⁷.

Lidocaine's distribution is ultimately throughout all body tissues ⁷. In general, the more highly perfused organs will show higher concentrations of the agent ⁷. The highest percentage of this drug will be found in skeletal muscle, mainly due to the mass of muscle rather than an affinity ⁷.

Protein binding

The protein binding recorded for lidocaine is about 60 to 80% and is dependent upon the plasma concentration of alpha-1-acid glycoprotein ^10,8. Such percentage protein binding bestows lidocaine with a medium duration of action when placed in comparison to other local anesthetic agents ⁸.

Metabolism

Lidocaine is metabolized predominantly and rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys ^10,7. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation ^10,7. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide ^10,7. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine HCl ^10,7. Approximately 90% of lidocaine HCl administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged ^10,7. The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-dimethylaniline ^10,7.

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Lidocaine

Route of elimination

The excretion of unchanged lidocaine and its metabolites occurs predominantly via the kidney with less than 5% in the unchanged form appearing in the urine ^10,7. The renal clearance is inversely related to its protein binding affinity and the pH of the urine ⁷. This suggests by the latter that excretion of lidocaine occurs by non-ionic diffusion ⁷.

Half-life

The elimination half-life of lidocaine hydrochloride following an intravenous bolus injection is typically 1.5 to 2.0 hours ¹⁰. Because of the rapid rate at which lidocaine hydrochloride is metabolized, any condition that affects liver function may alter lidocaine HCl kinetics ¹⁰. The half-life may be prolonged two-fold or more in patients with liver dysfunction ¹⁰.

Clearance

The mean systemic clearance observed for intravenously administered lidocaine in a study of 15 adults was approximately 0.64 +/- 0.18 L/min ¹¹.

Adverse Effects

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Toxicity

Symptoms of overdose and/or acute systemic toxicity involves central nervous system toxicity that presents with symptoms of increasing severity ⁷. Patients may present initially with circumoral paraesthesia, numbness of the tongue, light-headedness, hyperacusis, and tinnitus ⁷. Visual disturbance and muscular tremors or muscle twitching are more serious and precede the onset of generalized convulsions ⁷. These signs must not be mistaken for neurotic behavior ⁷. Unconsciousness and grand mal convulsions may follow, which may last from a few seconds to several minutes ⁷. Hypoxia and hypercapnia occur rapidly following convulsions due to increased muscular activity, together with the interference with normal respiration and loss of the airway ⁷. In severe cases, apnoea may occur. Acidosis increases the toxic effects of local anesthetics ⁷. Effects on the cardiovascular system may be seen in severe cases ⁷. Hypotension, bradycardia, arrhythmia and cardiac arrest may occur as a result of high systemic concentrations, with potentially fatal outcome ⁷.

Pregnancy Category B has been established for the use of lidocaine in pregnancy, although there are no formal, adequate, and well-controlled studies in pregnant women ¹⁰. General consideration should be given to this fact before administering lidocaine to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place ¹⁰. Ultimately, although animal studies have revealed no evidence of harm to the fetus, lidocaine should not be administered during early pregnancy unless the benefits are considered to outweigh the risks ⁷. Lidocaine readily crosses the placental barrier after epidural or intravenous administration to the mother ⁷. The ratio of umbilical to maternal venous concentration is 0.5 to 0.6 ⁷. The fetus appears to be capable of metabolizing lidocaine at term ⁷. The elimination half-life in the newborn of the drug received in utero is about three hours, compared with 100 minutes in the adult ⁷. Elevated lidocaine levels may persist in the newborn for at least 48 hours after delivery ⁷. Fetal bradycardia or tachycardia, neonatal bradycardia, hypotonia or respiratory depression may occur ⁷.

Local anesthetics rapidly cross the placenta and when used for epidural, paracervical, pudendal or caudal block anesthesia, can cause varying degrees of maternal, fetal and neonatal toxicity ¹⁰. The potential for toxicity depends upon the procedure performed, the type and amount of drug used, and the technique of drug administration ¹⁰. Adverse reactions in the parturient, fetus and neonate involve alterations of the central nervous system, peripheral vascular tone, and cardiac function ¹⁰.

Maternal hypotension has resulted from regional anesthesia ¹⁰. Local anesthetics produce vasodilation by blocking sympathetic nerves ¹⁰. Elevating the patient’s legs and positioning her on her left side will help prevent decreases in blood pressure ¹⁰. The fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable ¹⁰.

Epidural, spinal, paracervical, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts ¹⁰. In one study, paracervical block anesthesia was associated with a decrease in the mean duration of first stage labor and facilitation of cervical dilation ¹⁰. However, spinal and epidural anesthesia have also been reported to prolong the second stage of labor by removing the parturient’s reflex urge to bear down or by interfering with motor function ¹⁰. The use of obstetrical anesthesia may increase the need for forceps assistance ¹⁰.

The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life ¹⁰. The long-term significance of these observations is unknown ¹⁰. Fetal bradycardia may occur in 20 to 30 percent of patients receiving paracervical nerve block anesthesia with the amide-type local anesthetics and may be associated with fetal acidosis ¹⁰. Fetal heart rate should always be monitored during paracervical anesthesia ¹⁰. The physician should weigh the possible advantages against risks when considering a paracervical block in prematurity, toxemia of pregnancy, and fetal distress ¹⁰. Careful adherence to the recommended dosage is of the utmost importance in obstetrical paracervical block ¹⁰. Failure to achieve adequate analgesia with recommended doses should arouse suspicion of intravascular or fetal intracranial injection ¹⁰. Cases compatible with unintended fetal intracranial injection of local anesthetic solution have been reported following intended paracervical or pudendal block or both. Babies so affected present with unexplained neonatal depression at birth, which correlates with high local anesthetic serum levels, and often manifest seizures within six hours ¹⁰. Prompt use of supportive measures combined with forced urinary excretion of the local anesthetic has been used successfully to manage this complication ¹⁰.

It is not known whether this drug is excreted in human milk ¹⁰. Because many drugs are excreted in human milk, caution should be exercised when lidocaine is administered to a nursing woman ¹⁰.

Dosages in children should be reduced, commensurate with age, body weight and physical condition ¹⁰.

The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats ¹⁰.

Pathways

Pathway	Category
Lidocaine (Antiarrhythmic) Action Pathway	Drug action
Lidocaine (Local Anaesthetic) Action Pathway	Drug action
Lidocaine (Local Anaesthetic) Metabolism Pathway	Drug metabolism

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of CNS depression can be increased when Lidocaine is combined with 1,2-Benzodiazepine.
Abametapir	The serum concentration of Lidocaine can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Lidocaine can be increased when combined with Abatacept.
Abemaciclib	The risk or severity of methemoglobinemia can be increased when Abemaciclib is combined with Lidocaine.
Abiraterone	The serum concentration of Lidocaine can be increased when it is combined with Abiraterone.

Food Interactions

No interactions found.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Lidocaine hydrochloride	V13007Z41A	6108-05-0	YECIFGHRMFEPJK-UHFFFAOYSA-N
Lidocaine hydrochloride anhydrous	EC2CNF7XFP	73-78-9	IYBQHJMYDGVZRY-UHFFFAOYSA-N

International/Other Brands

After Burn Double Strength Gel / After Burn Double Strength Spray / After Burn Gel / After Burn Spray / Alphacaine / Anestacon Jelly / DermaFlex / Dilocaine / Esracaine / L-Caine / Lidoject-1 / Lidoject-2 / LidoPain SP / Norwood Sunburn Spray / Xilocaina / Xylocaine

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Accucaine	Injection, solution	10 mg/1mL	Infiltration	Advanced Rx Pharmacy of Tennessee, LLC	2023-07-26	Not applicable
Accucaine	Injection, solution	10 mg/1mL	Infiltration	Preferred Pharmaceuticals Inc..	2023-03-01	Not applicable
Accucaine	Injection, solution	10 mg/1mL	Infiltration	Asclemed Usa, Inc.	2016-02-01	Not applicable
Akten	Gel	35 mg/1mL	Ophthalmic	Thea Pharma Inc.	2022-12-01	Not applicable
Akten	Gel	35 mg/1mL	Ophthalmic	Akorn	2008-10-08	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
0.5% LIDOCAINE HCl	Injection, solution	5 mg/1mL	Infiltration; Intravenous	HF Acquisition Co LLC, DBA HealthFirst	2022-08-01	Not applicable
1% Lidocaine Hci	Injection, solution	10 mg/1mL	Infiltration; Perineural	HF Acquisition Co LLC, DBA HealthFirst	2019-12-13	Not applicable
1% Lidocaine Hci	Injection, solution	10 mg/1mL	Infiltration; Perineural	HF Acquisition Co LLC, DBA HealthFirst	2019-12-13	Not applicable
2% Lidocaine Hci	Injection, solution	20 mg/1mL	Infiltration; Perineural	HF Acquisition Co LLC, DBA HealthFirst	2018-10-22	Not applicable
2% Lidocaine Hci	Injection, solution	20 mg/1mL	Infiltration; Perineural	HF Acquisition Co LLC, DBA HealthFirst	2019-12-13	Not applicable

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
4 Lidocaine Topical Anesthetic	Cream	40 mg/1g	Topical	RUGBY LABORATORIES	2020-04-30	Not applicable
4019 First Aid Kit	Kit	2 g/100g	Topical	Honeywell Safety Products USA, Inc.	2018-10-13	Not applicable
4043 First Aid Kit	Kit	2 g/100g	Topical	Honeywell Safety Products USA, Inc	2018-11-21	2019-10-18
7-Select After Sun Lidicaine HCl Pain-Relieving with Aloe Vera	Gel	5 mg/1g	Topical	7-11	2019-02-21	Not applicable
Absorbine jr. Lidocaine	Patch	246 mg/1	Topical	Clarion Brands, Llc	2017-01-01	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
% 0,4 LIDODEKS %5 DEKSTROZ İÇİNDE I.V. İNFÜZYON İÇİN ÇÖZELTİ, 250 ML SETLİ	Lidocaine hydrochloride (0.4 %) + Dextrose, unspecified form (5 %)	Injection, solution	Intravenous	POLİFARMA İLAÇ SAN. VE TİC. A.Ş.	2016-08-05	Not applicable
% 0,4 LIDODEKS %5 DEKSTROZ İÇİNDE I.V. İNFÜZYON İÇİN ÇÖZELTİ, 250 ML SETSİZ	Lidocaine hydrochloride (0.4 %) + Dextrose, unspecified form (5 %)	Injection, solution	Intravenous	POLİFARMA İLAÇ SAN. VE TİC. A.Ş.	2016-08-05	Not applicable
% 0,4 LIDODEKS %5 DEKSTROZ İÇİNDE I.V. İNFÜZYON İÇİN ÇÖZELTİ, 500 ML SETLİ	Lidocaine hydrochloride (0.4 %) + Dextrose, unspecified form (5 %)	Injection, solution	Intravenous	POLİFARMA İLAÇ SAN. VE TİC. A.Ş.	2016-08-05	Not applicable
% 0,4 LIDODEKS %5 DEKSTROZ İÇİNDE I.V. İNFÜZYON İÇİN ÇÖZELTİ, 500 ML SETSİZ	Lidocaine hydrochloride (0.4 %) + Dextrose, unspecified form (5 %)	Injection, solution	Intravenous	POLİFARMA İLAÇ SAN. VE TİC. A.Ş.	2016-08-05	Not applicable
% 0,8 LIDODEKS %5 DEKSTROZ İÇİNDE I.V. İNFÜZYON İÇİN ÇÖZELTİ, 250 ML SETLİ	Lidocaine hydrochloride (0.8 %) + Dextrose, unspecified form (5 %)	Injection, solution	Intravenous	POLİFARMA İLAÇ SAN. VE TİC. A.Ş.	2016-08-05	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
1st Medxpatch With Lidocaine 4%-rx	Lidocaine (4 1/1) + Capsaicin (0.0375 1/1) + Menthol (5 1/1) + Methyl salicylate (20 1/1)	Patch	Topical	Direct Rx	2020-10-14	Not applicable
1st Medxpatch With Lidocaine 4%-rx	Lidocaine (4 g/1) + Capsaicin (0.0375 g/1) + Menthol (5 g/1) + Methyl salicylate (20 g/1)	Patch	Topical	1ST MEDX LLC	2018-03-15	Not applicable
4007 First Aid Kit	Lidocaine hydrochloride (2 g/100mL) + Ethanol (665 mL/1L)	Gel; Kit; Liquid	Topical	Honeywell Safety Products USA, Inc.	2018-09-12	Not applicable
4013 First Aid Kit	Lidocaine hydrochloride (2 g/100mL) + Ethanol (665 mL/1L)	Gel; Kit; Liquid	Topical	Honeywell Safety Products USA, Inc.	2018-09-12	Not applicable
4017 First Aid Kit	Lidocaine hydrochloride (20 mg/1mL) + Lidocaine hydrochloride (0.5 g/100g) + Acetaminophen (325 mg/1) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (1.3 mg/1mL) + Ethanol (0.5 mL/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL)	Cream; Kit; Liquid; Ointment; Swab; Tablet	Ophthalmic; Oral; Topical	Honeywell Safety Products USA, Inc	2018-10-18	Not applicable

Chemical Identifiers

UNII: 98PI200987
CAS number: 137-58-6
InChI Key: NNJVILVZKWQKPM-UHFFFAOYSA-N
InChI: InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)
IUPAC Name: 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
SMILES: CCN(CC)CC(=O)NC1=C(C)C=CC=C1C

References

Synthesis Reference

US2441498A

General References

Khaliq W, Alam S, Puri N: Topical lidocaine for the treatment of postherpetic neuralgia. Cochrane Database Syst Rev. 2007 Apr 18;(2):CD004846. [Article]
Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M: Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973 Apr;78(4):499-508. [Article]
Geha PY, Baliki MN, Chialvo DR, Harden RN, Paice JA, Apkarian AV: Brain activity for spontaneous pain of postherpetic neuralgia and its modulation by lidocaine patch therapy. Pain. 2007 Mar;128(1-2):88-100. Epub 2006 Oct 25. [Article]
Hines R, Keaney D, Moskowitz MH, Prakken S: Use of lidocaine patch 5% for chronic low back pain: a report of four cases. Pain Med. 2002 Dec;3(4):361-5. [Article]
Authors unspecified: Lidocaine/prilocaine spray for premature ejaculation. Drug Ther Bull. 2017 Apr;55(4):45-48. doi: 10.1136/dtb.2017.4.0469. [Article]
Scriabine, Alexander (2017). Pharmaceutical Innovation: Revolutionizing Human Health.. Chemical Heritage Press.. [ISBN:9780941901215]
Electronic Medicines Compendium: Lidocaine 1% w/v solution for injection Monograph [Link]
StatPearls Internet: Lidocaine Profile [Link]
World Health Organization Model Lists of Essential Medicines [Link]
Xylocaine (lidocaine HCl Injection, USP) FDA Label [File]
University of Virginia Children's Hospital: Use of Lidocaine for Analgesia in Children and Adolescents, by Marcia L. Buck, Pharm.D., FCCP, FPPAG [File]
Cytochrome P450-mediated drug interactions affecting lidocaine by Mika Isohanni [File]

External Links

Human Metabolome Database: HMDB0014426
KEGG Drug: D00358
KEGG Compound: C07073
PubChem Compound: 3676
PubChem Substance: 46505060
ChemSpider: 3548
BindingDB: 50017662
RxNav: 6387
ChEBI: 6456
ChEMBL: CHEMBL79
ZINC: ZINC000000020237
Therapeutic Targets Database: DAP000121
PharmGKB: PA450226
Guide to Pharmacology: GtP Drug Page
PDBe Ligand: LQZ
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Lidocaine

PDB Entries

3jqz / 3ttr / 8h6n

FDA label

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MSDS

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Clinical Trials

Clinical Trials Clinical Trial & Rare Diseases Add-on Data Package Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package

Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
Not Available	Active Not Recruiting	Other	Benign facial lentigines	1	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Prevention	Breast Surgery	1	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Prevention	Intraabdominal Infections / Postoperative Pulmonary Complications	1	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Supportive Care	Pain	2	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Supportive Care	Urologic Malignancies	1	somestatus	stop reason	just information to hide

Pharmacoeconomics

Manufacturers

Astrazeneca lp
Noven pharmaceuticals inc
Carlisle laboratories inc
E fougera div altana inc
Graham chemical co
Taro pharmaceuticals usa inc
Teikoku pharma usa inc
Abbott laboratories pharmaceutical products div
Abbott laboratories hosp products div
Abraxis pharmaceutical products
Akorn inc
Baxter healthcare corp anesthesia and critical care
Bel mar laboratories inc
Dell laboratories inc
Elkins sinn div ah robins co inc
Gd searle llc
Hospira inc
International medication systems ltd
International medication system
Luitpold pharmaceuticals inc
Miles laboratories inc
Watson laboratories inc
Wyeth ayerst laboratories
Baxter healthcare corp
B braun medical inc
App pharmaceuticals llc
Meridian medical technologies inc
Dentsply pharmaceutical
Polymedica industries inc
Teva pharmaceuticals usa
Hi tech pharmacal co inc
Wockhardt eu operations (swiss) ag
Actavis mid atlantic llc
Vintage pharmaceuticals llc
Roxane laboratories inc
Kendall co
Paco research corp
Anesiva inc

Packagers

4uOrtho LLC
A. Aarons Inc.
Actavis Group
Aerospace Accessory Service Inc.
Akorn Inc.
Amend
American Dental Cooperative Inc.
American Regent
Amphastar Pharmaceuticals
APP Pharmaceuticals
Aristos Pharmaceuticals
A-S Medication Solutions LLC
AstraZeneca Inc.
Ato Zizine Sarl
Auriga Pharmaceuticals LLC
Avent Inc.
B. Braun Melsungen AG
Baxter International Inc.
Benco Dental Co.
Blairex Labs
Bradley Pharmaceuticals Inc.
Breckenridge Pharmaceuticals
Brookstone Pharmaceuticals
C.O. Truxton Inc.
Cardent International Inc.
Cardinal Health
Carestream Health Inc.
Carlisle Laboratories Inc.
Catalent Pharma Solutions
Codman and Shurtleff Inc.
Covidien LP
Cypress Pharmaceutical Inc.
Darby Dental Supply Co. Inc.
Deltex Pharmaceuticals Inc.
DENTSPLY International
Dispensing Solutions
Diversified Healthcare Services Inc.
Doak Dermatologics
DSC Laboratories
E. Fougera and Co.
Eastman Kodak Co. Dental Products
Endo Pharmaceuticals Inc.
Enterprises Importfab Inc.
F Hoffmann-La Roche Ltd.
Fresca Gourmet Inc.
General Injectables and Vaccines Inc.
Groupe Parima Inc.
H Meer Dental Supply Co.
H.J. Harkins Co. Inc.
Henry Schein Inc.
Hi Tech Pharmacal Co. Inc.
Hospira Inc.
Innoviant Pharmacy Inc.
Keltman Pharmaceuticals Inc.
Kent Dental
Klosterfrau Berlin GmbH
Kylemore Pharmaceuticals
Laboratorios Zeyco SA De CV
Lake Erie Medical and Surgical Supply
Luitpold Pharmaceuticals Inc.
Major Pharmaceuticals
Marlop Pharmaceuticals Inc.
Martica Enterprises Inc.
Mckesson Corp.
Medical Components Inc.
Medical Techniques LLC
Merit Pharmaceuticals
National Pharmaceuticals
NeLLCor Puritan Bennett Mexico SA De CV
Nord Ost Corp.
Noven Pharmaceuticals Inc.
Novocol Pharmaceutical Canada
Nycomed Inc.
Odan Laboratories Ltd.
Palmetto Pharmaceuticals Inc.
Patterson Dental Supply Inc.
Pharmaderm
Pharmedium
Pharmedix
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Primedics Laboratories
Puretek Corp.
Qualitest
Raz Co. Inc.
Rebel Distributors Corp.
Rising Pharmaceuticals
River's Edge Pharmaceuticals
Roxane Labs
S&P Healthcare
Safco Dental Supply Co.
Sandoz
Septodont Inc.
Sheffield Laboratories Div Faria Limited LLC
Smiths Medical ASD Inc.
Sonar Products Inc.
Southwood Pharmaceuticals
Stat Rx Usa
Taro Pharmaceuticals USA
Tech Group Tempe
Teikoku Seiyaku Co. Ltd.
Teva Pharmaceutical Industries Ltd.
Tri State Hospital Supply Corp.
Veratex Corp.
Vintage Pharmaceuticals Inc.
Vyteris Inc.
Wallach Surgical Devices Inc.
Welch Allyn Inc.
Wockhardt Ltd.

Dosage Forms

Form	Route	Strength
Solution	Intravenous
Gel; kit; liquid	Topical
Kit	Topical	2 g/100g
Inhalant; kit; liquid; ointment; spray; tablet	Ophthalmic; Oral; Respiratory (inhalation); Topical
Cream; kit; swab	Topical
Cream; kit; liquid; tablet	Ophthalmic; Oral; Topical
Kit; liquid; swab	Ophthalmic; Topical
Gel; kit; liquid; swab	Topical
Cream; kit; liquid	Topical
Kit	Oral; Respiratory (inhalation); Topical
Gel; inhalant; kit; liquid; ointment	Ophthalmic; Respiratory (inhalation); Topical
Cream; gel; kit; liquid; ointment; swab	Ophthalmic; Topical
Cream; kit; liquid; swab	Ophthalmic; Topical
Gel; kit; liquid; swab	Ophthalmic; Topical
Cream; kit; liquid; swab	Topical
Kit	Ophthalmic; Oral; Respiratory (inhalation); Topical
Kit	Respiratory (inhalation); Topical
Kit; liquid; ointment; swab	Ophthalmic; Topical
Cream; kit; liquid; ointment; swab; tablet	Ophthalmic; Oral; Topical
Cream; kit; liquid; ointment; swab	Ophthalmic; Topical
Kit; liquid; ointment; spray; swab; tablet	Ophthalmic; Oral; Topical
Kit; liquid; lozenge; ointment; spray; swab; tablet	Ophthalmic; Oral; Topical
Kit	Ophthalmic; Respiratory (inhalation); Topical
Gel; inhalant; kit; liquid; ointment; swab	Ophthalmic; Respiratory (inhalation); Topical
Gel; kit; liquid; ointment; swab	Ophthalmic; Topical
Cream; inhalant; kit; swab; tablet	Oral; Respiratory (inhalation); Topical
Gel; kit; swab	Topical
Cream; inhalant; kit; liquid	Ophthalmic; Respiratory (inhalation); Topical
Cream; kit; liquid; ointment; spray; tablet	Ophthalmic; Oral; Topical
Cream; kit; liquid; ointment; swab; tablet	Oral; Topical
Inhalant; kit; liquid; ointment; spray; swab; tablet	Ophthalmic; Oral; Respiratory (inhalation); Topical
Cream; kit; liquid; ointment; swab	Topical
Inhalant; kit; swab	Respiratory (inhalation); Topical
Gel; kit; ointment; swab	Topical
Cream; kit; ointment; swab	Topical
Gel; kit; liquid; ointment	Ophthalmic; Topical
Gel; kit; liquid; ointment; solution; swab	Ophthalmic; Topical
Gel; kit; liquid; ointment	Topical
Gel; kit; liquid; ointment; swab	Topical
Kit; liquid; ointment; swab; tablet	Ophthalmic; Oral; Topical
Cream; kit; liquid	Ophthalmic; Topical
Gel; kit; liquid	Ophthalmic; Topical
Cream; kit; liquid; ointment	Topical
Kit; liquid; ointment; swab; tablet	Oral; Topical
Kit; liquid; ointment; spray; tablet	Ophthalmic; Oral; Topical
Cream; gel; kit; liquid; ointment; spray; swab	Ophthalmic; Topical
Cream; kit; liquid; ointment; spray; swab	Ophthalmic; Topical
Gel; kit; liquid; ointment; swab; tablet	Oral; Topical
Cream; kit; liquid; swab; tablet	Oral; Topical
Kit; liquid; ointment; swab	Topical
Liquid	Subarachnoid
Solution	Intravenous	1.00 g
Patch	Topical	246 mg/1
Injection, solution; kit	Infiltration; Intramuscular; Intravenous; Perineural; Topical
Injection, solution; kit	Infiltration; Intramuscular; Perineural; Topical
Gel	Topical	70 mg/3.5g
Gel	Topical	25 mg/1mL
Solution	Topical
Spray	Topical	1 % w/w
Gel	Topical	1 % w/w
Liquid; spray	Topical	0.5 %
Gel	Topical	0.5 %
Gel	Topical	2.5 g/100g
Gel	Ophthalmic	35 mg/1mL
Gel	Topical	5 mg/1mL
Patch	Transdermal	4 g/1
Gel	Topical	4 %
Ointment	Topical	4 g/100mL
Swab	Topical	4 g/100mL
Gel	Topical	0.5 g/100mL
Gel	Topical	2.5 g/1g
Solution	Other
Patch	Topical	1 g/10g
Solution	Parenteral	596.487 mg
Liquid	Infiltration; Subcutaneous	1 % / kit
Cream	Topical	4 mg/100g
Injection	Infiltration; Perineural
Gel	Cutaneous
Gel	Topical	2 g/1mL
Solution / drops	Oral
Cream	Topical	4 % w/w
Injection	Percutaneous
Aerosol, foam	Topical	4 g/100g
Cream	Topical	5 g/100mL
Liquid	Epidural	1 % / kit
Solution / drops	Ophthalmic
Ointment	Topical	0.05 g/1g
Cream; kit	Topical
Solution	Intramuscular; Intravenous	500 mg/5ml
Solution	Intramuscular; Intravenous; Subcutaneous	20 mg/ml
Kit; liquid	Intravenous
Liquid	Intravenous
Liquid	Intra-articular	1 % / kit
Ointment	Rectal	0.250 g
Cream	Topical	40 MG/G
Patch	Topical	411.4 mg/1
Lotion	Topical	4 g/100g
Patch	Topical	422 mg/1
Kit	Topical	4 g/100g
Solution	Parenteral	500.00 mg
Implant	Intradermal	.3 %
Gel	Topical	4.1 mg/1mL
Gel	Topical	4.81 mg/1mL
Gel	Topical	5.05 mg/1mL
Kit	Oral; Topical
Patch	Topical; Transdermal
Solution	Intramuscular
Spray	Topical	5 g/100mL
Gel	Topical	0.7 %
Liquid	Topical	2 %
Kit; patch	Percutaneous; Topical; Transdermal
Patch	Percutaneous; Topical; Transdermal	960 mg/1
Lozenge	Oral	5 mg
Kit	Infiltration
Kit	Infiltration; Intra-articular; Intralesional; Intramuscular; Perineural; Topical
Injection, solution; injection, suspension; kit; solution; swab	Infiltration; Intra-articular; Intralesional; Intramuscular; Intrathecal; Intravascular; Intravenous; Topical
Cream	Topical	2 %
Cream	Topical	2 g/100g
Cream	Topical	2.8 g/56g
Kit	Epidural; Infiltration; Topical
Kit	Infiltration; Intra-articular; Intralesional; Intramuscular; Intrathecal; Intravascular; Intravenous; Perineural; Topical
Spray	Topical	5 % w/w
Spray	Topical	5 mg/100mL
Kit	Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Topical
Patch	Topical	22 mg/1
Cream	Topical	40 mg/1
Spray	Topical	10 mg/1mg
Oil	Topical
Liquid	Topical	3.4 g/68mL
Cream	Topical	20 mg/1mL
Spray	Topical	20 mg/1L
Cream	Topical	2.25 %
Gel	Topical	0.02 g/1g
Gel	Topical	2 g/100g
Jelly	Topical	20 mg / g
Gel	Topical	2.5 g/100mL
Aerosol, spray	Topical	0.64 g/127g
Lotion	Topical	3 g/100g
Cream	Topical	3.9 g/100mL
Cream	Topical	3.9 g/100g
Gel	Topical	2.4123 g/482.46g
Gel	Topical	0.72 %
Spray	Topical	.05 g/100g
Spray	Topical	0.5 g/100g
Gel	Topical	.5 g/100mL
Spray	Topical	200 g/1L
Spray	Topical	2.4 %
Gel	Topical	0.025 g/1g
Cream	Topical	10 mg/1g
Kit	Electro-osmosis
Cream	Topical	0.04 mg/1mg
Gel	Topical	3.5 mg/100mL
Liquid	Topical	1.5 g/50mL
Solution	Parenteral	0.036 g
Gel	Topical	1.0 %
Gel	Topical	20 mg / g
Gel	Transmucosal
Gel		2 %
Gel
Patch	Topical	23 mg/1
Injection, powder, for solution	Intramuscular
Solution	Parenteral	35.000 mg
Liquid	Subcutaneous
Liquid; ointment	Intravenous; Topical
Kit; liquid; ointment	Infiltration; Parenteral; Subcutaneous; Topical
Solution	Buccal; Oral	5.5 mg
Kit	Intravenous
Spray	Nasal
Spray	Nasal	50 mg/ml
Solution	Intravenous	500.000 mg
Solution	Intramuscular	75.000 mg
Liquid	Epidural; Infiltration; Subcutaneous
Patch	Topical	560 mg/1
Patch	Topical	40 mg/1g
Cream	Topical	4 g/100mL
Aerosol, spray	Topical	5 g/100g
Cream	Topical	40 mg/1g
Cream	Topical	50 mg/1g
Liquid	Topical
Gel	Topical	5 mg/1g
Rinse	Topical
Patch	Transdermal	567 mg/1
Kit	Transdermal
Patch	Transdermal	858 mg/1
Patch	Transdermal	40 mg/1
Cream; kit; tablet, film coated	Oral; Topical
Injection, solution; kit; solution	Epidural; Infiltration; Intracaudal; Perineural; Topical
Spray	Topical	5 g/100g
Gel	Topical	0.2 g
Gel	Buccal
Gel	Oral
Patch	Buccal	46.1 mg/1
Suspension	Intra-articular; Intrabursal; Intrasynovial; Periarticular
Solution	Topical	10 mg/1mL
Spray	Topical	50 mg/1g
Cream; injection, suspension; kit	Intra-articular; Intramuscular; Topical
Kit	Topical	50 mg/1g
Cream	Topical	38.8 mg/1g
Solution	Cutaneous
Emulsion	Topical
Kit	Cutaneous; Topical
Kit	Infiltration; Intramuscular; Intravenous; Topical
Injection, solution; kit; solution; swab	Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Intrathecal; Intravascular; Intravenous; Perineural; Topical
Kit	Epidural; Infiltration; Intramuscular; Intravenous; Topical
Solution	Intramuscular	100.000 mg
Lozenge	Oral	1.2 mg
Injection, solution, concentrate	Intramuscular
Gel	Buccal; Oral	2 g
Solution	Parenteral	100 mg
Cream; kit; liquid; ointment; tablet; tablet, chewable; tablet, film coated	Oral; Topical
Kit	Epidural; Infiltration; Intracaudal; Subcutaneous; Topical
Solution	Intramuscular	1.000 mg
Cream	Topical	5 g
Solution
Cream		25 mg/g
Suppository	Rectal
Cream; gel; kit	Topical
Patch	Topical	84 mg/1
Cream	Topical	0.5 g/10g
Cream	Topical	1.2 g/30g
Cream	Topical	1.5 g/30g
Cream	Topical	5 % w/w
Cream	Topical	5 g/100g
Solution	Intramuscular	20.000 mg
Liquid	Topical	40 mg/1g
Spray	Topical	9.6 %
Capsule, delayed release; cream; kit	Oral; Topical
Injection	Retrobulbar
Kit; liquid; solution; swab	Oral; Topical
Spray	Topical	10 mg/0.08mL
Gel	Oral	20 mg/g
Kit	Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
Injection, solution; injection, suspension; kit; solution; swab	Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intrathecal; Intravascular; Intravenous; Perineural; Soft tissue; Topical
Kit	Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; Topical
Kit	Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
Injection, solution; injection, suspension; kit; solution; swab	Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intrasynovial; Intrathecal; Intravascular; Intravenous; Perineural; Soft tissue; Topical
Solution / drops	Topical	4 g/100mL
Liquid	Auricular (otic)	4 g/100mL
Kit	Topical	2 g/100mL
Cream	Topical	40 mg/1mL
Injection, solution
Injection, solution	Intragingival
Spray	Oral
Spray	Topical	20 mg/1mL
Lotion	Topical	4 g/1mL
Spray	Topical	4.48 g/112g
Soap	Topical	1.92 g/48mL
Cream	Cutaneous
Cream	Occlusive dressing technique
Plaster	Topical
Gel	Topical	0.8 %
Liquid	Topical	4 mg/100mL
Patch	Topical; Transdermal	0.04 g/1g
Patch	Topical; Transdermal	344 mg/1
Gel	Topical	8 mg/1g
Tablet	Vaginal
Kit; ointment; solution	Infiltration; Intravenous; Topical
Gel	Topical	40 mg/1000mg
Spray	Topical	40 mg/1000mg
Cream	Topical	50 mg/1000mg
Gel	Topical	50 mg/1000mg
Spray	Topical	50 mg/1000mg
Cream	Topical	4 mg/1mL
Kit	Ophthalmic; Topical
Liquid; spray	Topical
Spray	Topical	40 mg/1mL
Ointment	Rectal	5.000 g
Spray	Topical	20 g/1000mL
Ointment	Topical
Kit	Oral
Solution	Auricular (otic); Topical
Spray	Cutaneous
Injection, solution; kit	Infiltration; Perineural; Topical
Injection, solution; kit	Perineural; Retrobulbar; Topical
Gel	Topical	10 mg/1g
Spray	Topical	10 mg/1g
Kit	Cutaneous; Oral
Gel	Topical	2 %
Patch	Topical	490 mg/1
Lotion	Topical	3.5 g/100g
Kit	Intra-amniotic
Patch	Topical	40 mg/1mL
Aerosol	Topical	40 mg/1g
Gel	Topical	500 g/100000mg
Spray	Cutaneous	.50 g/100g
Kit	Ophthalmic; Oral; Topical
Suppository	Vaginal
Injection, solution; injection, suspension; kit	Infiltration; Intra-articular; Intralesional; Intramuscular; Perineural; Topical
Cream	Topical	4 g/1mL
Gel	Topical	3402 mg/85.05g
Lotion	Topical	9068 mg/226.7g
Gel	Topical	2832 mg/70.8g
Spray	Topical	4 g/100g
Cream	Topical	5.0 % w/w
Cream	Topical	100 g/100g
Gel	Topical	0.8 g/100g
Gel	Topical	0.8 % w/w
Patch	Percutaneous; Topical; Transdermal	4 g/100g
Cream	Topical	45 mg/1mL
Cream	Topical	1.4 g/28g
Cream	Rectal	2.000 g
Gel	Topical	3.4 mg
Soap	Topical
Soap	Topical	50 mg/1g
Injection, solution	Intra-articular
Liquid; ointment	Epidural; Topical
Kit	Epidural; Infiltration; Intra-articular; Topical
Gel	Topical	0.5 % w/w
Injection		2 %
Solution	Intravenous	20.000 mg
Injection	Parenteral	2 % w/v
Spray	Topical	.50 g/100g
Lotion	Topical	.5 g/100mL
Gel	Urethral
Kit	Infiltration; Intra-articular; Intramuscular; Respiratory (inhalation); Topical
Kit	Intravenous; Topical
Solution	Topical	2 % w/v
Injection, solution		10 %
Spray		100 mg/ml
Injection
Spray	Topical	10 mg/10mg
Inhalant; injection, solution; injection, suspension; kit; solution	Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Respiratory (inhalation); Topical
Solution	Parenteral	2 g
Injection, suspension, extended release
Gel; injection
Kit	Intra-articular; Intralesional
Kit	Intra-articular; Intramuscular
Lotion	Topical	15 mg/1mL
Injection		20 mg/ml
Gel	Topical	4 g/50g
Ointment	Topical	30 gr
Spray, metered	Topical	96 mg/1mL
Injection	Subcutaneous	1 %
Injection	Epidural; Intramuscular; Intraspinal; Intravenous; Parenteral	1 %
Injection	Subcutaneous	2 %
Injection	Epidural; Intramuscular; Intraspinal; Intravenous; Parenteral	2 %
Cream	Cutaneous	4 g
Cloth; cream; gel; kit; ointment; solution	Ophthalmic; Topical
Kit	Ophthalmic
Liquid	Endotracheal	40 mg / mL
Solution	Intramuscular	200.000 mg
Gel	Topical	30 gr
Ointment	Topical	30 g
Gel	Topical	4 g/4g
Gel	Topical	4 mg/100mg
Lotion	Topical	30 mg/1mL
Lotion	Topical	30 mg/177mL
Injection, solution	Parenteral
Spray	Topical	100 mg/ml
Injection	Parenteral	50 mg
Injection	Parenteral	10 mg
Solution	Dental
Solution	Intradermal; Perineural; Subcutaneous
Solution	Parenteral
Solution	Epidural; Intravenous	400 mg
Injection, solution		10 MG/ML
Solution	Infiltration	20 mg
Solution	Infiltration	36 mg
Solution	Parenteral	500 mg
Solution	Intravenous	2 g
Solution	Intradermal; Intravenous; Perineural; Subcutaneous	20 mg
Cream
Injection, solution	Parenteral	10 MG/ML
Injection, solution	Parenteral	20 MG/ML
Solution / drops	Ophthalmic
Solution / drops	Ophthalmic	40 MG/ML
Gel	Topical
Ointment	Topical
Cream	Buccal; Topical	5 g
Gel	Topical	2 % w/v
Gel	Topical	4 g/100mL
Injection, solution	Subcutaneous
Ointment	Topical	10 1/1
Ointment	Topical	2.5 g/50g
Ointment	Topical	35.44 g/1g
Ointment	Topical	4 g/1
Ointment	Topical	5 g/100g
Ointment	Topical	50 mg/1g
Patch	Cutaneous	140 mg/1
Patch	Cutaneous	50 mg/1
Patch	Percutaneous; Topical; Transdermal	4 mg/1
Patch	Topical	3.5 g/1
Patch	Topical	4 g/4g
Patch	Topical	4 g/1g
Patch	Topical	50 mg/1g
Suppository	Rectal	50 mg/1
Ointment	Topical	15 g/100g
Solution	Infiltration
Cream	Topical	0.03 g/1g
Ointment	Topical	30 g/100g
Cream	Topical	4.27 g/100g
Cream	Rectal; Topical	5 g/100g
Patch	Topical	700 mg/1
Cream	Rectal; Topical	5.25 g/100g
Cream	Topical
Cream	Rectal	50 mg/1g
Spray	Topical	5 %
Cream	Topical	0.4 g/1g
Gel	Topical	20 mg/g
Cream	Topical	3 mg/1g
Cream	Topical	30 mg/1g
Injection		20 mg
Injection, solution	Parenteral	10 mg/1mL
Injection, solution	Parenteral	20 mg/1mL
Injection, solution	Retrobulbar; Topical; Transtracheal	40 mg/1mL
Cream	Rectal; Topical
Ointment	Topical	4 g/100g
Injection	Epidural; Infiltration; Intracaudal; Perineural
Lotion	Topical
Liquid	Epidural; Infiltration	10 mg / mL
Liquid	Infiltration	10 mg / mL
Liquid	Intravenous	20 mg / mL
Solution	Infiltration	10 mg / mL
Injection		21.3 mg
Injection		5 %
Gel	Topical	18 mg/1g
Gel	Topical	30 mg/1g
Injection	Epidural; Infiltration; Intracaudal	10 mg/1mL
Injection	Infiltration; Intravenous	10 mg/1mL
Injection	Infiltration; Intravenous	20 mg/1mL
Injection	Infiltration; Intravenous	5 mg/1mL
Injection	Infiltration; Perineural	10 mg/1mL
Injection	Parenteral	20 mg/1mL
Injection, solution	Dental; Infiltration	20 mg/1mL
Injection, solution	Epidural; Infiltration	10 mg/1mL
Injection, solution	Epidural; Infiltration	20 mg/1mL
Injection, solution	Epidural; Infiltration; Intracaudal	10 mg/1mL
Injection, solution	Epidural; Infiltration; Intracaudal	20 mg/1mL
Injection, solution	Epidural; Infiltration; Intracaudal; Perineural	10 mg/1mL
Injection, solution	Epidural; Infiltration; Perineural	20 mg/1mL
Injection, solution	Infiltration	10 mg/1mL
Injection, solution	Infiltration	15 mg/1mL
Injection, solution	Infiltration	20 mg/1mL
Injection, solution	Infiltration	5 mg/1mL
Injection, solution	Infiltration; Intravenous	5 mg/1mL
Injection, solution	Intravenous	10 mg/1mL
Injection, solution	Intravenous	100 mg/1mL
Injection, solution	Intravenous	20 mg/1mL
Injection, solution	Intravenous	200 mg/1mL
Injection, solution	Retrobulbar; Topical	40 mg/1mL
Liquid	Topical	18 g/1L
Liquid	Topical	20 mg/1mL
Liquid	Topical	200 mL/1L
Lotion	Topical	3 g/100mL
Lotion	Topical	5.31 mL/177mL
Powder	Not applicable	1 g/1g
Solution	Intravenous	10 mg/1mL
Solution	Intravenous	20 mg/1mL
Solution	Oral	20 mg/1mL
Solution	Oral	40 mg/1mL
Solution	Oral; Topical	20 mg/1mL
Solution	Oropharyngeal	20 mg/1mL
Solution	Topical	20 mg/1mL
Solution	Topical	40 mg/1mL
Spray	Laryngeal; Transtracheal	20 mg/1mL
Spray	Laryngeal; Transtracheal	40 mg/1mL
Spray	Topical	123.6 mg
Cream	Rectal
Solution	Epidural; Infiltration
Injection, solution	Infiltration	2 %
Solution	Parenteral	2 %
Injection	Intravenous
Injection	Intravenous	4 mg/1mL
Injection, solution	Intraspinal
Injection, solution	Intravenous
Injection, solution	Intravenous	4 mg/1mL
Injection, solution	Intravenous	400 mg/100mL
Injection, solution	Intravenous	8 mg/1mL
Injection, solution	Intravenous	800 mg/100mL
Injection, solution	Dental; Infiltration
Injection, solution	Epidural
Injection, solution	Epidural; Infiltration
Injection, solution	Infiltration
Gel	Rectal
Solution	Epidural; Infiltration	10 mg / mL
Solution	Epidural; Infiltration	20 mg / mL
Solution	Infiltration	20 mg / mL
Solution	Intravenous	20 mg / mL
Solution	Infiltration	5 mg / mL
Liquid	Infiltration	2 %
Injection		21.33 mg
Injection		21.9 mg
Solution	Topical	4 % w/v
Gel	Oral	2 g/100mL
Solution	Infiltration	1 % w/v
Solution	Infiltration	2 % w/v
Ointment	Topical	5 % w/w
Ointment	Topical	5 g / 100 g
Patch	Topical	40 mg/1000mg
Aerosol	Topical	4 % w/w
Liquid	Topical	38 mg/1mL
Patch	Topical	344 mg/1
Patch	Topical	0.4 g/1
Patch	Transdermal	700 mg/1
Cream	Topical	39.2 mg/1mL
Patch	Topical	50 mg/1
Patch	Topical	4 g/1
Patch	Topical	11 mg/1
Gel	Topical	0.9 g/30g
Spray	Topical	4.6 g/115g
Injection, solution	Intravenous	2 %
Cream	Topical	10 g/100g
Solution	Topical	4 %
Jelly	Topical	20 mg / mL
Jelly	Topical	2 %
Ointment	Topical	5 %
Solution	Buccal	2 %
Injection, suspension	Parenteral
Patch	Cutaneous	50 mg/1g
Patch	Cutaneous	700 mg/1
Patch	Cutaneous	700 mg/12h
Liquid	Cutaneous	700 mg/1000mg
Gel	Topical	3 mg/100mL
Injection, solution
Patch	Topical	22.7 mg/0.24mg
Patch	Topical	25.3 mg/0.24mg
Patch	Topical	25.8 mg/0.24mg
Patch	Topical	28.1 mg/0.24mg
Patch	Topical	29 mg/0.24mg
Patch	Topical	21.5 mg/0.24mg
Gel	Topical	28 mg/1g
Kit	Epidural; Infiltration; Intracaudal; Perineural	10 mg/1mL
Kit	Epidural; Infiltration; Intracaudal	20 mg/1mL
Cream	Topical	4 g
Solution	Oral	10 g
Injection, solution	Intramuscular; Intravenous; Subcutaneous	100 mg/5ml
Injection, solution	Intramuscular; Intravenous; Subcutaneous	40 mg/2ml
Injection, solution	Intramuscular; Intravenous; Subcutaneous	500 mg/5ml
Patch	Transdermal
Injection	Intramuscular	300 mg/3mL
Cream	Topical	32.5 mg/1g
Kit	Topical	5 g/100g
Patch	Iontophoresis
Kit; liquid; ointment	Topical
Patch	Topical
Gel	Topical	38.8 mg/1g
Spray	Topical	50 mg/1mL
Patch	Topical	683 mg/1
Cream	Topical	37.5 mg/1g
Cream	Topical	39.5 mg/1g
Kit	Not applicable
Gel	Topical	40 mg/1g
Solution	Intramuscular	20 mg
Solution	Intramuscular	10 mg
Kit; patch	Cutaneous	50 mg/1g
Spray	Topical	10 mg/0.1mL
Solution	Parenteral	100.00 mg
Injection	Intravenous
Injection	Intravenous	10 mg/ml
Injection	Intravenous	20 mg/ml
Plaster	Transdermal	5 % w/w
Plaster	Topical	0.700 g/plaster
Spray	Oral	10 %W/V
Injection, solution	Submucosal
Liquid	Infiltration
Solution	Intramuscular; Intravenous	600 mg
Solution	Intramuscular; Intravenous	300 mg
Capsule, coated	Oral	500 mg
Solution	Intramuscular; Intravenous	60000000 mg
Injection	Intramuscular
Gel	Topical	2.36 g/118mL
Spray, metered	Topical	10 mg/100mL
Insert	Vaginal
Gel; kit; patch	Topical
Injection	Intravascular; Intravenous
Patch	Percutaneous; Topical; Transdermal	4 mg/100mg
Cream		5 %
Kit	Epidural; Infiltration; Intra-articular; Intramuscular; Topical
Gel	Topical	5 g/100g
Liquid	Subcutaneous	1 % / kit
Injection	Parenteral	1 % w/v
Injection, solution	Subcutaneous	200 mg/10ml
Spray, metered	Topical	9.6 mg/100mL
Kit	Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Topical
Spray	Topical	2 g/100mL
Cream	Topical	4 %
Cream	Topical	5 %
Patch	Topical	40 mg/1
Tablet	Buccal; Oral
Spray	Topical	40 mg/1g
Gel	Topical	5 %
Kit	Oral	20 mg/1mL
Kit	Oral; Topical	20 mg/1mL
Solution	Oral; Topical	5 g/100g
Spray	Topical	20 g/1L
Gel	Oral; Topical
Gel	Submucosal	0.05 % w/w
Gel	Topical	0.04 g/1g
Lotion	Topical	40 mg/1mL
Gel	Topical	10 mg/1mL
Solution / drops	Ophthalmic; Topical
Suspension / drops	Auricular (otic)
Kit	Epidural; Infiltration; Intra-articular; Intramuscular
Injection, solution; injection, suspension; kit; solution; swab	Epidural; Infiltration; Intra-articular; Intramuscular; Intrathecal; Intravascular; Intravenous; Perineural; Topical
Liquid	Buccal
Kit	Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
Injection, powder, for solution	Intramuscular; Intravenous
Injection, solution	Intraocular
Liquid	Infiltration; Intraspinal; Subcutaneous	1 % / kit
Injection, solution	Retrobulbar	40 mg/1mL
Liquid	Topical	40 mg/1000mg
Cream	Topical	0.04 g/28g
Liquid	Topical	10 mg/1mL
Solution / drops	Auricular (otic)	1 mg/ml
Solution	Buccal; Oral	0.55 g
Solution	Buccal; Oral	5.55 mg
Solution	Intramuscular; Intravenous
Solution	Parenteral	200 mg
Solution	Subcutaneous	0.0180 mg
Gel	Topical	2 g/100mL
Spray	Topical	24.64 mg/1mL
Cream	Topical	5 mg/1g
Gel	Topical	1.12 g/28g
Cream	Topical	4 g/100g
Gel	Topical	50 mg/1mL
Cream	Topical	5 mg/30g
Cream	Topical	4 mg/100mL
Cream	Topical	5 mg/100mL
Spray	Topical	0.04 mg/1mg
Stick	Topical
Patch		700 MG
Gel	Topical	.5 g/100g
Injection	Dental	0.01 mg/mL
Liquid	Dental; Subcutaneous
Ointment	Rectal	50 MG/G
Injection	Intramuscular	75 mg/2ml
Oil	Topical	8 mg/1mL
Injection, solution; injection, suspension; kit	Infiltration; Intra-articular; Intramuscular; Perineural; Topical
Gel	Ophthalmic	20 MG/G
Paste	Submucosal	3 % w/w
Lotion	Topical	0.5 % w/v
Gel	Dental
Gel	Periodontal
Solution / drops	Auricular (otic)	10000 IU/ml
Solution / drops	Auricular (otic)	1 %
Solution	Auricular (otic)
Suspension	Auricular (otic)
Injection, solution; kit; solution	Epidural; Infiltration; Intracaudal; Intravenous; Perineural; Topical
Injection, solution; injection, suspension; kit; solution	Epidural; Infiltration; Intra-articular; Intracaudal; Intralesional; Intramuscular; Intravenous; Perineural; Soft tissue; Topical
Injection, solution; injection, suspension; kit; solution	Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Intravenous; Perineural; Topical
Liquid; ointment	Subcutaneous; Topical
Spray	Oral
Lozenge	Oral	5 mg/1mg
Cream	Topical	0.04 g/40g
Lotion	Topical	40 mg/4mL
Cream	Topical	50 mg/1mL
Cream	Topical	3.86 g/100g
Liquid	Topical	4 g/100mL
Patch	Topical	4 g/100g
Patch	Topical	0.04 g/1g
Patch	Topical	0.3 g/1
Gel	Topical	7.128 mg/1mL
Gel	Topical	7.13 mg/1mL
Cream	Topical	2.5 g/50g
Liquid	Infiltration; Subcutaneous; Topical
Gel	Topical	2 mg/1g
Injection		0.0125 mg/ml
Liquid	Intravenous	1 %
Kit; ointment; solution	Infiltration; Subcutaneous; Topical
Injection	Epidural; Infiltration	1 %
Solution	Topical	10.000 g
Injection	Infiltration; Perineural	2 % w/v
Cream	Topical	41.2 mg/1g
Injection, solution	Intraocular; Ophthalmic
Kit	Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Respiratory (inhalation); Topical
Cloth; injection, solution; injection, suspension; kit	Infiltration; Intra-articular; Intramuscular; Topical
Solution		10.00 g
Solution	Parenteral	35 mg
Solution	Parenteral	200.000 mg
Solution	Parenteral	1 g
Liquid	Epidural; Intravenous
Liquid	Dental	2 %
Kit	Infiltration; Soft tissue; Topical
Kit	Epidural; Infiltration; Intracaudal
Cream; kit; powder, for solution; tablet, coated	Oral; Rectal
Solution / drops	Auricular (otic)
Spray	Topical	2.6 %
Spray	Topical	4 %
Solution	Topical	40 mg / mL
Gel	Buccal; Dental; Topical
Cream	Topical	400 mg/1mg
Patch	Topical	.005 mg/1g
Ointment	Topical	.005 mg/1g
Spray, metered	Topical	9.6 g/100mL
Cream; kit; patch	Cutaneous; Topical
Capsule; cream; kit	Oral; Topical
Ointment	Topical	10 mg/1mL
Spray	Topical	10 g/100g
Cream
Gel	Topical	0.5 g/100g
Patch	Topical	240 mg/1
Liquid	Topical	0.5 g/100g
Injection, solution; kit; solution	Infiltration; Perineural; Topical
Cream	Cutaneous	2.000 g
Packing	Dental
Cream	Topical	2.5 %w/w
Lotion	Topical	10 mg/1g
Lotion	Topical	2 g/100mL
Plaster	Transdermal
Patch	Topical	18 mg/116cm2
Patch	Topical	4 mg/100mg
Lotion	Oral
Kit	Intra-articular; Intralesional; Intramuscular
Kit	Intramuscular; Intravenous
Kit	Epidural; Infiltration
Cream	Topical	0.04 g/1g
Cream	Topical	0.05 g/1g
Spray	Topical	5.9 g/118mL
Cloth	Topical
Cloth; cream; kit	Topical
Gel	Topical	20 mg/1mL
Gel	Topical	20 mg/1g
Liquid	Topical	40 mg/1mL
Spray	Topical	4 % w/w
Gel	Topical	4 g/100g
Gel	Topical	4 % w/w
Cream	Topical	2.24 g/56g
Injection, solution	Intramuscular
Solution	Parenteral	10 mg
Solution	Epidural; Infiltration	400 mg
Solution	Epidural	200 mg
Solution	Topical	10 g
Ointment	Topical	5 g
Solution	Parenteral	0.2 g
Spray	Topical	2 %
Solution	Topical	2 %
Cream	Percutaneous; Topical; Transdermal
Liquid	Percutaneous; Topical; Transdermal
Patch	Percutaneous; Topical; Transdermal	42 mg/1
Spray	Topical	1.1 g/12g
Patch	Topical	4 g/100mL
Lotion	Topical	4 g/100mL
Gel	Topical	30 mg/1mL
Gel	Topical	11.9 g/234.6g
Solution		2 %W/V
Gel	Topical	2.0 %
Gel	Topical	40 mg/1mL
Solution	Other	10.000 mg
Patch	Cutaneous; Topical; Transdermal	560 mg/14g
Liquid	Topical	125 mg/1mL
Kit	Topical
Gel	Topical	1 %
Spray	Topical	5 mg/1g
Aerosol	Topical	0.5 %
Lotion	Topical	0.5 %
Spray	Topical	4 g/100mL
Gel	Topical	0.057 mg/1mL
Gel	Topical	7.1258 mg/1mL
Gel	Topical	0.50 % w/w
Cream	Topical	0.5 g/100g
Ointment	Rectal
Kit	Infiltration; Topical
Liquid	Parenteral; Topical
Liquid	Infiltration; Subcutaneous
Kit	Infiltration	1 %
Spray	Topical	10 g/100mL
Spray, metered	Topical	9.6 %
Spray	Topical	96 mg/1mL
Gel	Topical
Swab	Topical
Spray, metered	Topical	9.6 % w/w
Aerosol	Topical	0.5 % w/w
Gel	Topical	5.00 mg/1g
Gel	Topical	2 % w/w
Gel	Topical	5.05 g/1g
Gel	Topical	1 g/100g
Swab	Topical	1 %
Spray	Topical	10 mg/1mL
Jelly; kit; ointment	Topical
Patch	Cutaneous
Patch	Topical
Powder	Intravenous	30 mg
Ointment	Topical	1.0 g/100g
Ointment	Topical	0.5 g/100g
Patch	Topical	4 mg/1
Liquid	Intrathoracic; Subcutaneous	1 % / kit
Liniment	Topical
Spray	Topical	10 mg/100mL
Gel	Topical	2.36 g/59g
Spray	Topical	2.36 g/59g
Gel	Topical	5 % w/w
Gel	Topical	15 mg/1mL
Lozenge	Buccal	8 mg
Lozenge	Oral	8 mg
Solution	Parenteral	100.000 mg
Insert	Vaginal	800.00 mg
Cream; kit; solution	Topical
Patch
Liquid	Topical	50 mg/1mL
Spray	Topical	2.5 g/100mL
Gel	Topical	2.5 %
Ointment	Topical	5.000 g
Solution	Parenteral	20.000 mg
Solution	Parenteral	0.0225 mg
Solution	Parenteral	36.000 mg
Patch	Percutaneous; Topical; Transdermal	560 mg/1
Emulsion	Urethral
Solution	Auricular (otic)	1.00 g
Kit	Topical	40 mg/1mL
Cream	Topical
Cream	Topical	2 % w/w
Injection	Parenteral
Injection	Infiltration; Perineural	2 %
Patch	Topical	5 %
Patch	Topical	700.00 mg
Plaster	Transdermal	700 mg
Patch	Topical; Transdermal	0.7 g
Kit	Subcutaneous; Topical
Solution	Topical
Lotion	Cutaneous; Rectal; Topical; Vaginal	4 g/100g
Solution	Intramuscular	100.00 mg
Spray	Topical	100 mg/1mL
Spray	Topical	0.5 mg/100mg
Liquid	Topical	4 g/100g
Spray	Topical
Aerosol, spray	Topical	4 g/100g
Cream	Topical	1 %
Aerosol, spray	Topical	4.52 g/113g
Lotion	Topical	3.4 g/85g
Gel	Topical	3.2 g/88mL
Solution	Topical	2 % w/w
Solution	Topical	0.5 % w/w
Spray	Topical	0.5 % w/w
Gel	Rectal	2.35 g/100mL
Gel	Topical	4.625 g/100mL
Gel	Rectal	4.625 g/100mL
Cream	Topical	2 g/1mL
Spray	Topical	2 mg/100mL
Kit	Cutaneous	50 mg/1g
Injection	Parenteral
Injection, solution	Interstitial
Injection	Parenteral	0.5 %
Injection	Parenteral	1 %
Injection, solution	Interstitial	2 %
Injection	Parenteral	2 %
Injection	Submucosal
Kit; patch; swab	Topical
Spray		10 %
Injection, solution	Epidural; Intravenous; Subcutaneous	2 %
Injection, solution		2 %
Injection, solution		20 MG/ML
Spray	Oral	10 %
Solution	Parenteral	20 mg
Solution	Topical	100 mg
Gel
Gel		20 MG/G
Injection
Injection	Dental	20 mg/1mL
Injection	Infiltration
Injection	Infiltration	10 mg/1mL
Injection	Infiltration	15 mg/1mL
Injection	Infiltration	20 mg/1mL
Injection	Infiltration	5 mg/1mL
Injection	Infiltration	50 mg/1mL
Injection	Intravenous	20 mg/1mL
Injection, solution	Infiltration; Perineural
Injection, solution	Infiltration; Perineural	10 mg/1mL
Injection, solution	Infiltration; Perineural	20 mg/1mL
Injection, solution	Infiltration; Perineural	5 mg/1mL
Jelly	Topical	20 mg/1mL
Spray	Topical	10 %
Liquid	Intraspinal
Liquid	Infiltration	5 mg / mL
Solution	Epidural	15 mg / mL
Liquid	Infiltration	20 mg / mL
Solution	Epidural	20 mg / mL
Injection	Epidural; Perineural	2 %
Solution	Epidural
Injection	Dental	0.0125 mg/ml
Liquid	Subarachnoid	50 mg / mL
Solution	Epidural; Infiltration	17.3 mg / mL
Injection	Intradermal	50 mg/5ml
Gel	Topical	20 mg / mL
Injection, solution	Epidural; Infiltration; Intracaudal; Perineural
Injection, solution	Epidural; Infiltration; Intracaudal; Perineural	15 mg/1mL
Injection, solution	Epidural; Infiltration; Intracaudal; Perineural	20 mg/1mL
Liquid	Intraspinal; Percutaneous	1 %
Liquid	Percutaneous	1 %
Solution	Retrobulbar; Topical	40 mg/1mL
Liquid	Epidural
Liquid	Infiltration	1 %
Ointment	Topical	50 mg/g
Aerosol	Oral; Topical
Spray	Topical	10 mg
Spray, metered	Topical	10 mg / act
Spray	Topical	40 mg / mL
Liquid	Topical	50 mg / mL
Solution	Oral; Topical	20 mg / mL
Injection	Dental
Liquid	Epidural; Intracaudal	20 mg / mL
Solution	Intravenous	100 mg / 5 mL
Liquid	Intravenous	200 mg / mL
Injection, solution	Intra-articular; Intramuscular; Periarticular; Perineural; Subcutaneous; Submucosal	10 mg/ml
Injection	Parenteral	10 mg/ml
Spray, metered	Buccal
Aerosol	Topical
Aerosol, metered	Buccal
Spray	Topical	0.15 g/100g
Spray
Ointment
Injection, solution	Intravenous	300 mg/30ml
Injection, solution	Intravenous	50 mg/5ml
Solution	Subcutaneous
Aerosol, spray	Topical
Spray, metered	Topical
Cream	Topical	40 mg/1000mg
Cream	Topical	20 mg/1000mg
Liquid	Topical	2.5 %
Solution	Topical	4.0 %
Powder	Intradermal	0.5 mg/1
Ointment	Rectal	50 mg
Solution	Topical	10.00 g
Gel	Topical	50 mg/1g
Patch	Topical	36 mg/1
Solution
Liquid	Dental
Solution		40 mg/1ml
Plaster	Transdermal	5 %w/w
Solution		20 mg/1ml
Solution		10 mg/1ml
Lozenge	Oral
Liquid	Auricular (otic)
Suppository	Topical
Powder
Cream	Topical	10 %w/w
Gel		2 %w/w
Injection, solution		20 mg/1ml
Injection, solution		10 mg/1ml

Prices

Unit description	Cost	Unit
Rocephin 10 gm vial	478.32USD	each
Lidocaine HCl 3% Lotion 177ml Bottle	230.3USD	bottle
Rocephin 2 gm vial	97.5USD	each
Rocephin 1 gm vial	62.02USD	each
EMLA 2.5-2.5% Cream 30 gm Tube	58.4USD	tube
Lidocaine-Prilocaine 2.5-2.5% Cream 30 gm Tube	47.79USD	tube
Lidocaine HCl 2% Gel 10ml Syringe	17.99USD	syringe
Lidocaine HCl 2% Gel 30ml Tube	17.99USD	tube
Lidocaine HCl 4% Solution 50ml Bottle	16.99USD	bottle
Lidocaine Viscous 2% Solution 100ml Bottle	13.99USD	bottle
Lidocaine hcl 1% syringe	9.76USD	ml
Lidocaine HCl 4% Solution 4ml Bottle	9.42USD	bottle
Lidoderm 1 Box = 30 Patches	8.03USD	patch
Akten 3.5% drops	7.5USD	ml
Lidocaine 5% in d7.5w ampul	3.06USD	ml
Lidocaine 3% cream	2.91USD	g
Lidamantle 3% cream	2.03USD	g
Zilactin-l cold sore liquid	0.99USD	ml
Xylocaine 2% jelly	0.68USD	ml
Lidocaine hcl 10% vial	0.55USD	ml
Xylocaine 5% ointment	0.42USD	g
Xylocaine Jelly 2 % Jelly	0.41USD	g
Xylocaine 2% Solution	0.34USD	ml
Xylocaine 5 % Ointment	0.29USD	g
Lidocaine HCl 1% Solution	0.24USD	ml
Lidocaine hcl powder	0.24USD	g
Lidocaine base powder	0.22USD	g
Lidocaine hcl 4% solution	0.18USD	ml
Xylocaine 0.5% vial	0.18USD	ml
Lidodan 5 % Ointment	0.16USD	g
Xylocaine Viscous 2 % Liquid	0.1USD	ml
Lidocaine hcl 0.5% vial	0.08USD	ml
Solarcaine aerosol	0.06USD	g
Lidodan Viscous 2 % Liquid	0.06USD	ml
Lidocaine 2% viscous solution	0.03USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5234957	No	1993-08-10	2011-02-27
US5827529	No	1998-10-27	2015-10-27
US8540665	No	2013-09-24	2029-10-22
US6881200	No	2005-04-19	2016-06-11
US6004286	No	1999-12-21	2017-03-17
US5899880	No	1999-05-04	2016-05-04
US6031007	No	2000-02-29	2017-04-01
US6629968	No	2003-10-07	2020-06-30
US6635045	No	2003-10-21	2021-06-29
US6546281	No	2003-04-08	2015-07-28
US5658583	No	1997-08-19	2015-07-28
US6465006	No	2002-10-15	2015-07-28
US6465709	No	2002-10-15	2020-07-07
US6780426	No	2004-08-24	2015-07-28
US6306431	No	2001-10-23	2015-07-28
US5919479	No	1999-07-06	2015-07-28
US6528086	No	2003-03-04	2019-09-28
US8759401	No	2014-06-24	2026-07-24
US9370622	No	2016-06-21	2035-09-28
US9358338	No	2016-06-07	2035-04-27
US9283174	No	2016-03-15	2031-05-10
US9925264	No	2018-03-27	2031-05-10
US9931403	No	2018-04-03	2031-05-10
US10350180	No	2019-07-16	2031-01-14
US10603293	No	2020-03-31	2031-01-14
US10765640	No	2020-09-08	2031-05-10
US10765749	No	2020-09-08	2031-05-10
US10751305	No	2020-08-25	2031-01-14
US11278623	No	2011-05-10	2031-05-10
US11786455	No	2011-05-10	2031-05-10
US11793766	No	2011-05-10	2031-05-10

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	68.5 °C	PhysProp
boiling point (°C)	159-160 °C at 2.00E+00 mm Hg	PhysProp
water solubility	4100 mg/L (at 30 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	2.44	AVDEEF,A (1997)
logS	-1.76	ADME Research, USCD
Caco2 permeability	-4.21	ADME Research, USCD
pKa	8.01	SANGSTER (1994)

Predicted Properties

Property	Value	Source
Water Solubility	0.593 mg/mL	ALOGPS
logP	1.81	ALOGPS
logP	2.84	Chemaxon
logS	-2.6	ALOGPS
pKa (Strongest Acidic)	13.78	Chemaxon
pKa (Strongest Basic)	7.75	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	2	Chemaxon
Hydrogen Donor Count	1	Chemaxon
Polar Surface Area	32.34 Å²	Chemaxon
Rotatable Bond Count	5	Chemaxon
Refractivity	73.93 m³·mol^-1	Chemaxon
Polarizability	27.77 Å³	Chemaxon
Number of Rings	1	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	Yes	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST)

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Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-00xr-7900000000-a9354c2fae02587e1a3f
Mass Spectrum (Electron Ionization)	MS	splash10-000i-9000000000-38a47958df650b972703
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-000i-0090000000-7a90fe8d9b35b745cfce
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-001i-0920000000-f9f648594c0f1642cc4c
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0089-0900000000-5716ccc63e48696473bc
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-9d18ae1cd0a81ee63d35
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-0090000000-83bc5908a67b3ba4b826
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-8090000000-e305bfb01d615662d8a1
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-eab27554002663b2d3fd
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-1b684e31ff74300b808f
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-b39af34b526d79a4b07b
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-9466a1403df493f5b6e9
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-0090000000-c773b8e10c70518882c1
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-8090000000-00b6d0139ebe20cdb189
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-0b33ce49934844438e43
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-502494c9626d1dca25d1
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-b39af34b526d79a4b07b
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-86c007695ec40849f993
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-7f630b7fa4e36c59e0d2
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-000i-9060000000-b5aef137d8e488097fc4
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-000i-9000000000-b21ee69ce889ba36b5e5
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-000i-9000000000-9d7555c18e41a90508a5
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-000i-0090000000-3dd6e01da50ad1a66b2f
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-000i-9230000000-577ea8a290877187b518
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-000i-9000000000-3f33ed4d35a979dbd732
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-000i-9000000000-343e9e6a26be64016b15
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-000i-9000000000-c1923c77757d099538dd
LC-MS/MS Spectrum - LC-ESI-IT , positive	LC-MS/MS	splash10-000i-9000000000-9ff21e9bcf3f87f70774
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-eaebad6c7c4ce7832c9c
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-2e21612ecf5a40923bb5
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9050000000-930a3c8f94fdb363cc0f
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-000i-9000000000-bc7800eef651a1a0ee2c
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-000i-9000000000-a658a8aeac537602e1a7
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-000i-9000000000-5a056c9766b47a19f0a2
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-000i-9000000000-d649b0b05937216241a6
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-000i-6090000000-31a60a2cff302fde1ad8
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-000i-9020000000-da68f84a1fd4a905c98c
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-000i-6090000000-d9a64c8f059ab3d59aae
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-02n9-0930000000-717832365aea61d0a552
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-059i-9610000000-3d96ac1d932ac0dd2944
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-00xu-4900000000-f4829c9c0c8952f2e3cc
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0ab9-9200000000-92910513008e2d7b7a37
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0006-9200000000-e60d3a47d4c7a821e6a2
1H NMR Spectrum	1D NMR	Not Applicable
13C NMR Spectrum	1D NMR	Not Applicable
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	163.2898453	predicted	DarkChem Lite v0.1.0
[M-H]-	164.1867453	predicted	DarkChem Lite v0.1.0
[M-H]-	156.24376	predicted	DeepCCS 1.0 (2019)
[M+H]+	164.2454453	predicted	DarkChem Lite v0.1.0
[M+H]+	165.0721453	predicted	DarkChem Lite v0.1.0
[M+H]+	158.60176	predicted	DeepCCS 1.0 (2019)
[M+Na]+	163.3885453	predicted	DarkChem Lite v0.1.0
[M+Na]+	164.6412453	predicted	DarkChem Lite v0.1.0
[M+Na]+	164.76459	predicted	DeepCCS 1.0 (2019)

Targets

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Details1. Sodium channel protein type 11 subunit alpha

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Blocker

General Function: Sodium channel mediating the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient (PubMed:10580103, PubMed:12384689, PubMed:24036948, PubMed:24776970, PubMed:25791876, PubMed:26645915). Involved in membrane depolarization during action potential in nociceptors which function as key relay stations for the electrical transmission of pain signals from the periphery to the central nervous system (PubMed:24036948, PubMed:24776970, PubMed:25791876, PubMed:26645915). Also involved in rapid BDNF-evoked neuronal depolarization (PubMed:12384689)
Specific Function: voltage-gated sodium channel activity
Gene Name: SCN11A
Uniprot ID: Q9UI33
Uniprot Name: Sodium channel protein type 11 subunit alpha
Molecular Weight: 204919.66 Da

References

Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Details2. Sodium channel protein type 10 subunit alpha

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms
Specific Function: transmembrane transporter binding
Gene Name: SCN10A
Uniprot ID: Q9Y5Y9
Uniprot Name: Sodium channel protein type 10 subunit alpha
Molecular Weight: 220623.605 Da

References

Ekberg J, Jayamanne A, Vaughan CW, Aslan S, Thomas L, Mould J, Drinkwater R, Baker MD, Abrahamsen B, Wood JN, Adams DJ, Christie MJ, Lewis RJ: muO-conotoxin MrVIB selectively blocks Nav1.8 sensory neuron specific sodium channels and chronic pain behavior without motor deficits. Proc Natl Acad Sci U S A. 2006 Nov 7;103(45):17030-5. Epub 2006 Oct 31. [Article]
Muroi Y, Chanda B: Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol. 2009 Jan;133(1):1-15. doi: 10.1085/jgp.200810103. Epub 2008 Dec 15. [Article]
Karoly R, Lenkey N, Juhasz AO, Vizi ES, Mike A: Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study. PLoS Comput Biol. 2010 Jun 17;6(6):e1000818. doi: 10.1371/journal.pcbi.1000818. [Article]

Details3. Sodium channel protein type 9 subunit alpha

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:15385606, PubMed:16988069, PubMed:17145499, PubMed:17167479, PubMed:19369487, PubMed:24311784, PubMed:25240195, PubMed:26680203, PubMed:7720699). It is a tetrodotoxin-sensitive Na(+) channel isoform (PubMed:7720699). Plays a role in pain mechanisms, especially in the development of inflammatory pain (PubMed:17145499, PubMed:17167479, PubMed:19369487, PubMed:24311784)
Specific Function: voltage-gated sodium channel activity
Gene Name: SCN9A
Uniprot ID: Q15858
Uniprot Name: Sodium channel protein type 9 subunit alpha
Molecular Weight: 226370.175 Da

References

Sheets PL, Jackson JO 2nd, Waxman SG, Dib-Hajj SD, Cummins TR: A Nav1.7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity. J Physiol. 2007 Jun 15;581(Pt 3):1019-31. Epub 2007 Apr 12. [Article]
Muroi Y, Chanda B: Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol. 2009 Jan;133(1):1-15. doi: 10.1085/jgp.200810103. Epub 2008 Dec 15. [Article]
Karoly R, Lenkey N, Juhasz AO, Vizi ES, Mike A: Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study. PLoS Comput Biol. 2010 Jun 17;6(6):e1000818. doi: 10.1371/journal.pcbi.1000818. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	108000	N/A	N/A	A29539

Details4. Sodium channel protein type 5 subunit alpha

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:1309946, PubMed:21447824, PubMed:23085483, PubMed:23420830, PubMed:25370050, PubMed:26279430, PubMed:26392562, PubMed:26776555). It is a tetrodotoxin-resistant Na(+) channel isoform (PubMed:1309946). This channel is responsible for the initial upstroke of the action potential. Channel inactivation is regulated by intracellular calcium levels (PubMed:19074138). Required for normal electrical conduction including formation of the infranodal ventricular conduction system and normal action potential configuration, as a result of its interaction with XIRP2 (By similarity)
Specific Function: ankyrin binding
Gene Name: SCN5A
Uniprot ID: Q14524
Uniprot Name: Sodium channel protein type 5 subunit alpha
Molecular Weight: 226937.475 Da

References

Itoh H, Tsuji K, Sakaguchi T, Nagaoka I, Oka Y, Nakazawa Y, Yao T, Jo H, Ashihara T, Ito M, Horie M, Imoto K: A paradoxical effect of lidocaine for the N406S mutation of SCN5A associated with Brugada syndrome. Int J Cardiol. 2007 Oct 18;121(3):239-48. Epub 2007 Apr 18. [Article]
Fedida D, Orth PM, Hesketh JC, Ezrin AM: The role of late I and antiarrhythmic drugs in EAD formation and termination in Purkinje fibers. J Cardiovasc Electrophysiol. 2006 May;17 Suppl 1:S71-S78. [Article]
Wallace CH, Baczko I, Jones L, Fercho M, Light PE: Inhibition of cardiac voltage-gated sodium channels by grape polyphenols. Br J Pharmacol. 2006 Nov;149(6):657-65. Epub 2006 Oct 3. [Article]
Cerne A, Bergh C, Borg K, Ek I, Gejervall AL, Hillensjo T, Olofsson JI, Stener-Victorin E, Wood M, Westlander G: Pre-ovarian block versus paracervical block for oocyte retrieval. Hum Reprod. 2006 Nov;21(11):2916-21. Epub 2006 Jul 13. [Article]
Muroi Y, Chanda B: Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol. 2009 Jan;133(1):1-15. doi: 10.1085/jgp.200810103. Epub 2008 Dec 15. [Article]
Karoly R, Lenkey N, Juhasz AO, Vizi ES, Mike A: Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study. PLoS Comput Biol. 2010 Jun 17;6(6):e1000818. doi: 10.1371/journal.pcbi.1000818. [Article]

Details5. Epidermal growth factor receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses (PubMed:10805725, PubMed:27153536, PubMed:2790960, PubMed:35538033). Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF (PubMed:12297049, PubMed:15611079, PubMed:17909029, PubMed:20837704, PubMed:27153536, PubMed:2790960, PubMed:7679104, PubMed:8144591, PubMed:9419975). Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules (PubMed:27153536). May also activate the NF-kappa-B signaling cascade (PubMed:11116146). Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling (PubMed:11602604). Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin (PubMed:11483589). Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration (PubMed:20462955). Plays a role in enhancing learning and memory performance (By similarity). Plays a role in mammalian pain signaling (long-lasting hypersensitivity) (By similarity)
Specific Function: actin filament binding
Gene Name: EGFR
Uniprot ID: P00533
Uniprot Name: Epidermal growth factor receptor
Molecular Weight: 134276.185 Da

References

Sakaguchi M, Kuroda Y, Hirose M: The antiproliferative effect of lidocaine on human tongue cancer cells with inhibition of the activity of epidermal growth factor receptor. Anesth Analg. 2006 Apr;102(4):1103-7. [Article]

Details6. Sodium channel protein type 4 subunit alpha

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Pore-forming subunit of a voltage-gated sodium channel complex through which Na(+) ions pass in accordance with their electrochemical gradient. Alternates between resting, activated and inactivated states (PubMed:12766226, PubMed:15318338, PubMed:16890191, PubMed:17898326, PubMed:18690054, PubMed:19347921, PubMed:25707578, PubMed:26700687, PubMed:29992740, PubMed:30190309). Required for normal muscle fiber excitability, normal muscle contraction and relaxation cycles, and constant muscle strength in the presence of fluctuating K(+) levels (PubMed:12766226, PubMed:15318338, PubMed:16890191, PubMed:19347921, PubMed:25707578, PubMed:26659129, PubMed:26700687)
Specific Function: voltage-gated sodium channel activity
Gene Name: SCN4A
Uniprot ID: P35499
Uniprot Name: Sodium channel protein type 4 subunit alpha
Molecular Weight: 208059.175 Da

References

Leuwer M, Haeseler G, Hecker H, Bufler J, Dengler R, Aronson JK: An improved model for the binding of lidocaine and structurally related local anaesthetics to fast-inactivated voltage-operated sodium channels, showing evidence of cooperativity. Br J Pharmacol. 2004 Jan;141(1):47-54. Epub 2003 Dec 8. [Article]

Details7. Alpha-1-acid glycoprotein 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Functions as a transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction
Specific Function: Not Available
Gene Name: ORM1
Uniprot ID: P02763
Uniprot Name: Alpha-1-acid glycoprotein 1
Molecular Weight: 23539.43 Da

References

Herve F, Duche JC, d'Athis P, Marche C, Barre J, Tillement JP: Binding of disopyramide, methadone, dipyridamole, chlorpromazine, lignocaine and progesterone to the two main genetic variants of human alpha 1-acid glycoprotein: evidence for drug-binding differences between the variants and for the presence of two separate drug-binding sites on alpha 1-acid glycoprotein. Pharmacogenetics. 1996 Oct;6(5):403-15. [Article]

Details8. Alpha-1-acid glycoprotein 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Functions as a transport protein in the blood stream. Binds various hydrophobic ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability. Appears to function in modulating the activity of the immune system during the acute-phase reaction
Specific Function: Not Available
Gene Name: ORM2
Uniprot ID: P19652
Uniprot Name: Alpha-1-acid glycoprotein 2
Molecular Weight: 23602.43 Da

References

Herve F, Duche JC, d'Athis P, Marche C, Barre J, Tillement JP: Binding of disopyramide, methadone, dipyridamole, chlorpromazine, lignocaine and progesterone to the two main genetic variants of human alpha 1-acid glycoprotein: evidence for drug-binding differences between the variants and for the presence of two separate drug-binding sites on alpha 1-acid glycoprotein. Pharmacogenetics. 1996 Oct;6(5):403-15. [Article]

Enzymes

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
Specific Function: 1,8-cineole 2-exo-monooxygenase activity
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT: Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65. [Article]
Zhang J, Zhu J, Yao X, Duan Y, Zhou X, Yang M, Li X: Pharmacokinetics of Lidocaine Hydrochloride Metabolized by CYP3A4 in Chinese Han Volunteers Living at Low Altitude and in Native Han and Tibetan Chinese Volunteers Living at High Altitude. Pharmacology. 2016;97(3-4):107-13. doi: 10.1159/000443332. Epub 2016 Jan 6. [Article]
Mustajoki P, Mustajoki S, Rautio A, Arvela P, Pelkonen O: Effects of heme arginate on cytochrome P450-mediated metabolism of drugs in patients with variegate porphyria and in healthy men. Clin Pharmacol Ther. 1994 Jul;56(1):9-13. doi: 10.1038/clpt.1994.94. [Article]
Flockhart Table of Drug Interactions [Link]

Details2. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
Specific Function: anandamide 11,12 epoxidase activity
Gene Name: CYP2D6
Uniprot ID: P10635
Uniprot Name: Cytochrome P450 2D6
Molecular Weight: 55768.94 Da

References

Masubuchi Y, Takahashii C, Fujio N, Horie T, Suzuki T, Imaoka S, Funae Y, Narimatsu S: Inhibition and induction of cytochrome P450 isozymes after repetitive administration of imipramine in rats. Drug Metab Dispos. 1995 Sep;23(9):999-1003. [Article]
Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT: Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65. [Article]
Flockhart Table of Drug Interactions [Link]

Details3. Cytochrome P450 3A5

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
Specific Function: aromatase activity
Gene Name: CYP3A5
Uniprot ID: P20815
Uniprot Name: Cytochrome P450 3A5
Molecular Weight: 57108.065 Da

References

Flockhart Table of Drug Interactions [Link]

Details4. Cytochrome P450 3A7

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones (PubMed:17178770, PubMed:9555064). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position (PubMed:12865317, PubMed:14559847). Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics including anticonvulsants (PubMed:9555064)
Specific Function: all-trans retinoic acid 18-hydroxylase activity
Gene Name: CYP3A7
Uniprot ID: P24462
Uniprot Name: Cytochrome P450 3A7
Molecular Weight: 57469.95 Da

References

Flockhart Table of Drug Interactions [Link]

Details5. Cytochrome P450 1A2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable)
Specific Function: aromatase activity
Gene Name: CYP1A2
Uniprot ID: P05177
Uniprot Name: Cytochrome P450 1A2
Molecular Weight: 58406.915 Da

References

Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [Article]
Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT: Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65. [Article]
Wei X, Dai R, Zhai S, Thummel KE, Friedman FK, Vestal RE: Inhibition of human liver cytochrome P-450 1A2 by the class IB antiarrhythmics mexiletine, lidocaine, and tocainide. J Pharmacol Exp Ther. 1999 May;289(2):853-8. [Article]
Orlando R, Piccoli P, De Martin S, Padrini R, Floreani M, Palatini P: Cytochrome P450 1A2 is a major determinant of lidocaine metabolism in vivo: effects of liver function. Clin Pharmacol Ther. 2004 Jan;75(1):80-8. doi: 10.1016/j.clpt.2003.09.007. [Article]

Details6. Cytochrome P450 2C9

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids and steroids (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:15766564, PubMed:19965576, PubMed:7574697, PubMed:9866708). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Exhibits low catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes bisallylic hydroxylation and hydroxylation with double-bond migration of polyunsaturated fatty acids (PUFA) (PubMed:9435160, PubMed:9866708). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan (PubMed:25994031)
Specific Function: (R)-limonene 6-monooxygenase activity
Gene Name: CYP2C9
Uniprot ID: P11712
Uniprot Name: Cytochrome P450 2C9
Molecular Weight: 55627.365 Da

References

Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT: Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65. [Article]

Details7. Cytochrome P450 2C8

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond (PubMed:15766564, PubMed:19965576, PubMed:7574697). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form (PubMed:11093772). Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1) (PubMed:14559847). Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol) (PubMed:26427316)
Specific Function: arachidonic acid epoxygenase activity
Gene Name: CYP2C8
Uniprot ID: P10632
Uniprot Name: Cytochrome P450 2C8
Molecular Weight: 55824.275 Da

References

Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]

Details8. Cytochrome P450 2A6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity
Specific Function: arachidonic acid epoxygenase activity
Gene Name: CYP2A6
Uniprot ID: P11509
Uniprot Name: Cytochrome P450 2A6
Molecular Weight: 56517.005 Da

References

Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]

Details9. Cytochrome P450 2B6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of endocannabinoids and steroids (PubMed:12865317, PubMed:21289075). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the epoxidation of double bonds of arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:21289075). Hydroxylates steroid hormones, including testosterone at C-16 and estrogens at C-2 (PubMed:12865317, PubMed:21289075). Plays a role in the oxidative metabolism of xenobiotics, including plant lipids and drugs (PubMed:11695850, PubMed:22909231). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850)
Specific Function: anandamide 11,12 epoxidase activity
Gene Name: CYP2B6
Uniprot ID: P20813
Uniprot Name: Cytochrome P450 2B6
Molecular Weight: 56277.81 Da

References

Hedrich WD, Hassan HE, Wang H: Insights into CYP2B6-mediated drug-drug interactions. Acta Pharm Sin B. 2016 Sep;6(5):413-425. doi: 10.1016/j.apsb.2016.07.016. Epub 2016 Aug 9. [Article]

Transporters

Details1. Organic cation/carnitine transporter 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine (PubMed:10454528, PubMed:10525100, PubMed:10966938, PubMed:17509700, PubMed:20722056, PubMed:33124720). Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 11.3 (PubMed:10454528, PubMed:10525100, PubMed:10966938). In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from Bacillus Subtilis wich induces cytoprotective heat shock proteins contributing to intestinal homeostasis (PubMed:18005709). May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Specific Function: (R)-carnitine transmembrane transporter activity
Gene Name: SLC22A5
Uniprot ID: O76082
Uniprot Name: Organic cation/carnitine transporter 2
Molecular Weight: 62751.08 Da

References

Ohashi R, Tamai I, Nezu Ji J, Nikaido H, Hashimoto N, Oku A, Sai Y, Shimane M, Tsuji A: Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2. Mol Pharmacol. 2001 Feb;59(2):358-66. [Article]

Details2. ATP-dependent translocase ABCB1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
Specific Function: ABC-type xenobiotic transporter activity
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: ATP-dependent translocase ABCB1
Molecular Weight: 141477.255 Da

References

Wang E, Lew K, Barecki M, Casciano CN, Clement RP, Johnson WW: Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. Chem Res Toxicol. 2001 Dec;14(12):1596-603. [Article]
Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [Article]
Hu Y, Qin X, Cao H, Yu S, Feng J: Reversal effects of local anesthetics on P-glycoprotein-mediated cancer multidrug resistance. Anticancer Drugs. 2017 Mar;28(3):243-249. doi: 10.1097/CAD.0000000000000455. [Article]

Drug created at June 13, 2005 13:24 / Updated at October 08, 2024 09:29

Lidocaine

Identification

Structure for Lidocaine (DB00281)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

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Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)

Targets

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Enzymes

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Transporters

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