Identification

Summary

Benzocaine is a topical local anesthetic used for the temporary relief of pain and itching associated with minor burns, sunburn, scrapes and insect bites or minor skin irritations.

Brand Names
Anbesol Cold Sore Therapy, Cepacol Sore Throat Plus Cough, Cetacaine, Chloraseptic Sore Throat, Chloraseptic Sore Throat + Cough, Docusol Plus, Enemeez Plus, Medicaine Sting and Bite, One Touch Reformulated Apr 2009, Orasep Reformulated Dec 2013, Rectogel, Salinocaine, Topex, Vagisil Original Formula, Zap, Zilactin-B
Generic Name
Benzocaine
DrugBank Accession Number
DB01086
Background

Benzocaine is an ester local anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.4 It is commonly used for local anesthesia in many over the counter products.13,14,15 Benzocaine was first used for local anesthesia in dentistry.10

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 165.1891
Monoisotopic: 165.078978601
Chemical Formula
C9H11NO2
Synonyms
  • 4-aminobenzoic acid ethyl ester
  • Amben ethyl ester
  • Benzocaina
  • Benzocaine
  • Benzocainum
  • Ethyl aminobenzoate
  • Ethyl p-aminobenzoate
  • Ethyl p-aminophenylcarboxylate
  • p-(Ethoxycarbonyl)aniline
  • p-Carbethoxyaniline
  • p-Ethoxycarboxylic aniline
External IDs
  • AR-01
  • AR01
  • NSC-41531
  • NSC-4688

Pharmacology

Indication

Benzocaine is indicated for local anesthesia in dentistry, minor trauma, and as preparation for infiltrative anesthesia.4 Benzocaine products are indicated for topical anesthesia in a wide variety of conditions including skin irritation,13 oral pain,14 and hemorrhoids.15

Pharmacology
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Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Benzocaine is indicated for use as a topical anesthetic.4 It has a duration of action of approximately 10 minutes9 and a wide therapeutic window.4 Patients should be counselled regarding the risks of methemoglobinemia.4,5,6,8

Mechanism of action

Benzocaine diffuses into nerve cells where it binds to sodium channels, preventing the channels from opening, and blocking the influx of sodium ions.2,3,4 Nerve cells unable to allow sodium into cells cannot depolarize and conduct nerve impulses.3,4

TargetActionsOrganism
ASodium channel protein type 10 subunit alpha
inhibitor
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Benzocaine binds to both serum albumin and alpha-1-acid glycoprotein.7

Metabolism

Benzocaine undergoes ester hydrolysis to form 4-aminobenzoic acid, acetylation to form acetylbenzocaine, or N-hydroxylation to form benzocaine hydroxide.1 4-aminobenzoic acid can be acetylated or acetylbenzocaine can undergo ester hydrolysis to form 4-acetaminobenzoic acid.1

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Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Patients experiencing an overdose may present with local anesthetic systemic toxicity syndrome, decreased cardiovascular function, decreased central nervous system function, cardiac arrest, bradycardia, hypotension, cardiac arrhythmias, syncope, and seizures.4 Patients should be treated with symptomatic and supportive measures which include airway maintenance, controlling seizures, and hemodynamic stabilization.4

Pathways
PathwayCategory
Benzocaine Action PathwayDrug action
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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Benzocaine is combined with 1,2-Benzodiazepine.
AbametapirThe serum concentration of Benzocaine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Benzocaine can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Benzocaine can be increased when it is combined with Abiraterone.
AcebutololThe metabolism of Benzocaine can be decreased when combined with Acebutolol.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Benzocaine.
AcetaminophenBenzocaine may increase the hepatotoxic activities of Acetaminophen.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Benzocaine.
AcetophenazineThe risk or severity of adverse effects can be increased when Acetophenazine is combined with Benzocaine.
AclidiniumBenzocaine may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
Interactions
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Food Interactions
No interactions found.

Products

Products2
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dosage, form, labeller, route of administration, and marketing period.
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Product Ingredients
IngredientUNIICASInChI Key
Benzocaine hydrochlorideOG625Z9LEO23239-88-5JAADDQHUJDUAKW-UHFFFAOYSA-N
International/Other Brands
Anacaine / Anaesthesin / Anbesol Baby / Dermoplast
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Anal Swabs 20%Stick20 %TopicalEndovations Inc.1988-12-311997-07-15Canada flag
BeeGentle Topical AnestheticGel210 mg/1gTopicalCao Group, Inc.2010-09-012018-10-11US flag
Benzo-JelGel200 mg/1gTopicalHenry Schein, Inc.2015-07-03Not applicableUS flag
Benzo-JelGel200 mg/1gTopicalHenry Schein, Inc.2015-07-03Not applicableUS flag
Benzo-JelGel200 mg/1gTopicalHenry Schein, Inc.2015-07-03Not applicableUS flag
Benzo-Jel BananaGel, dentifrice220 mg/1gDentalHenry Schein1963-02-192015-01-22US flag
Benzo-Jel Bubble GumGel230 mg/1mLDentalHenry Schein1963-02-19Not applicableUS flag
Benzo-Jel CherryGel230 mg/1mLDentalHenry Schein1963-02-19Not applicableUS flag
Benzo-Jel MintGel230 mg/1mLDentalHenry Schein1963-02-19Not applicableUS flag
Benzo-Jel Pina ColadaGel230 mg/1mLDentalHenry Schein1963-02-19Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
20/20 Topical AnestheticStrip10 mg/1DentalAdvanced Dental Anesthetics2012-02-28Not applicableUS flag
7 Select Oral Pain Maximum Strength ReliefGel200 mg/1gTopical7-ELEVEN, INC.2016-12-08Not applicableUS flag
Advance Topical Anesthetic GelGel200 mg/1gDentalThe Atlanta Dental Supply Company Dba Advanced Dental Products2017-03-01Not applicableUS flag
Advance Topical Anesthetic GelGel200 mg/1gDentalThe Atlanta Dental Supply Company Dba Advanced Dental Products2017-03-01Not applicableUS flag
Advance Topical Anesthetic GelGel200 mg/1gDentalThe Atlanta Dental Supply Company Dba Advanced Dental Products2017-03-01Not applicableUS flag
Advance Topical Anesthetic GelGel200 mg/1gDentalThe Atlanta Dental Supply Company Dba Advanced Dental Products2017-03-01Not applicableUS flag
Advance Topical Anesthetic GelGel200 mg/1gDentalThe Atlanta Dental Supply Company Dba Advanced Dental Products2017-03-01Not applicableUS flag
Advance Topical Anesthetic GelGel200 mg/1gDentalThe Atlanta Dental Supply Company Dba Advanced Dental Products2017-03-01Not applicableUS flag
Adventure Medical Kits Dental MedicKit200 mg/1gOral; TopicalTender Corporation2012-09-19Not applicableUS flag
Aftertest Pain ReliefStick100 mg/1mLTopicalDiabetic Supply Of Suncoast, Inc.2017-01-28Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
10 Person ANSIBenzocaine (6 mL/100mL) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Ethanol (60 mL/100mL) + Ibuprofen (200 mg/1) + Lidocaine (0.5 1/100g) + Neomycin sulfate (5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; TopicalGenuine First Aid2010-04-24Not applicableUS flag
25 Person ANSIBenzocaine (6 mL/100mL) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Ethanol (60 mL/100mL) + Ethanol (62 g/100g) + Ibuprofen (200 mg/1) + Isopropyl alcohol (70 mL/100mL) + Lidocaine (0.5 g/100g) + Neomycin sulfate (5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; TopicalGenuine First Aid2010-04-25Not applicableUS flag
2x Med LiqBenzocaine (20 mg/100mL) + Menthol (0.1 mg/100mL)LiquidOralLornamead2021-09-01Not applicableUS flag
2x Med LiqBenzocaine (20 mg/100mL) + Menthol (0.1 mg/100mL)LiquidOralCSR Cosmetic Solutions2021-09-01Not applicableUS flag
3M Nexcare Cold Sore TreatmentBenzocaine (50 mg/1g) + Allantoin (10 mg/1g)OintmentTopical3M Company2008-02-202015-09-30US flag
3x Medicated Mouth Sore GelBenzocaine (20 g/100g) + Menthol (0.1 g/100g) + Zinc chloride (0.15 g/100g)GelOralWalgreens2021-10-20Not applicableUS flag
3x Medicated Mouth Sore GelBenzocaine (20 g/100g) + Menthol (0.1 g/100g) + Zinc chloride (0.15 g/100g)GelOralLornamead2020-06-05Not applicableUS flag
3X Medicated Mouth Sore GelBenzocaine (20 g/100g) + Menthol (0.1 g/100g) + Zinc chloride (0.15 g/100g)GelOralRite Aid2020-06-05Not applicableUS flag
3x Medicated Mouth Sore GelBenzocaine (20 g/100g) + Menthol (0.1 g/100g) + Zinc chloride (0.15 g/100g)GelOralCVS2020-06-05Not applicableUS flag
3x Medicated Mouth Sore GelBenzocaine (20 g/100g) + Menthol (0.1 g/100g) + Zinc chloride (0.15 g/100g)GelOralHEB2020-06-02Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
4125 First Aid KitBenzocaine (10 g/100g) + Benzocaine (10 g/100g) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Benzethonium chloride (0.2 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Menthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4125 First Aid KitBenzocaine (10 g/100g) + Benzocaine (10 g/100g) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Benzethonium chloride (0.2 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Menthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4129 First Aid KitBenzocaine (20 g/100g) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Ethanol (0.5 mL/1mL) + Hydrocortisone acetate (1 g/100g) + Hydrocortisone acetate (1 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (20 mg/1mL) + Povidone-iodine (10 mg/1mL)KitRespiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4142 First Aid KitBenzocaine (10 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Lidocaine hydrochloride (2 g/100g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4209 First Aid KitBenzocaine (20 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4211 First Aid KitBenzocaine (20 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4215 First Aid KitBenzocaine (20 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4217 First Aid KitBenzocaine (10 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4221 First Aid KitBenzocaine (10 g/100g) + Benzocaine (10 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzethonium chloride (0.2 g/100g) + Benzethonium chloride (0.2 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Menthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4221 First Aid KitBenzocaine (10 g/100g) + Benzocaine (10 g/100g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzethonium chloride (0.2 g/100g) + Benzethonium chloride (0.2 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Menthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag

Categories

ATC Codes
C05AD03 — BenzocaineR02AD01 — BenzocaineD04AB04 — BenzocaineN01BA05 — Benzocaine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzoic acid esters. These are ester derivatives of benzoic acid.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzoic acids and derivatives
Direct Parent
Benzoic acid esters
Alternative Parents
Aminobenzoic acids and derivatives / Benzoyl derivatives / Aniline and substituted anilines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Primary amines / Organopnictogen compounds / Organooxygen compounds / Organic oxides
show 1 more
Substituents
Amine / Amino acid or derivatives / Aminobenzoic acid or derivatives / Aniline or substituted anilines / Aromatic homomonocyclic compound / Benzoate ester / Benzoyl / Carboxylic acid derivative / Carboxylic acid ester / Hydrocarbon derivative
show 8 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
substituted aniline, benzoate ester (CHEBI:116735)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
U3RSY48JW5
CAS number
94-09-7
InChI Key
BLFLLBZGZJTVJG-UHFFFAOYSA-N
InChI
InChI=1S/C9H11NO2/c1-2-12-9(11)7-3-5-8(10)6-4-7/h3-6H,2,10H2,1H3
IUPAC Name
ethyl 4-aminobenzoate
SMILES
CCOC(=O)C1=CC=C(N)C=C1

References

General References
  1. Hartman NR, Mao JJ, Zhou H, Boyne MT 2nd, Wasserman AM, Taylor K, Racoosin JA, Patel V, Colatsky T: More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems. Regul Toxicol Pharmacol. 2014 Oct;70(1):182-8. doi: 10.1016/j.yrtph.2014.07.002. Epub 2014 Jul 8. [Article]
  2. Becker DE, Reed KL: Essentials of local anesthetic pharmacology. Anesth Prog. 2006 Fall;53(3):98-108; quiz 109-10. doi: 10.2344/0003-3006(2006)53[98:EOLAP]2.0.CO;2. [Article]
  3. Hanck DA, Nikitina E, McNulty MM, Fozzard HA, Lipkind GM, Sheets MF: Using lidocaine and benzocaine to link sodium channel molecular conformations to state-dependent antiarrhythmic drug affinity. Circ Res. 2009 Aug 28;105(5):492-9. doi: 10.1161/CIRCRESAHA.109.198572. Epub 2009 Aug 6. [Article]
  4. Singh R, Al Khalili Y: Benzocaine . [Article]
  5. Moore TJ, Walsh CS, Cohen MR: Reported adverse event cases of methemoglobinemia associated with benzocaine products. Arch Intern Med. 2004 Jun 14;164(11):1192-6. doi: 10.1001/archinte.164.11.1192. [Article]
  6. de Freiras GC, Pozzobon RT, Blaya DS, Moreira CH: Efficacy of Benzocaine 20% Topical Anesthetic Compared to Placebo Prior to Administration of Local Anesthesia in the Oral Cavity: A Randomized Controlled Trial. Anesth Prog. 2015 Summer;62(2):46-50. doi: 10.2344/0003-3006-62.2.46. [Article]
  7. Kitamura K, Omran AA, Takegami S, Tanaka R, Kitade T: (19)F NMR spectroscopic characterization of the interaction of niflumic acid with human serum albumin. Anal Bioanal Chem. 2007 Apr;387(8):2843-8. doi: 10.1007/s00216-007-1162-x. Epub 2007 Feb 14. [Article]
  8. Hieger MA, Afeld JL, Cumpston KL, Wills BK: Topical Benzocaine and Methemoglobinemia. Am J Ther. 2017 Sep/Oct;24(5):e596-e598. doi: 10.1097/MJT.0000000000000521. [Article]
  9. Lee HS: Recent advances in topical anesthesia. J Dent Anesth Pain Med. 2016 Dec;16(4):237-244. doi: 10.17245/jdapm.2016.16.4.237. Epub 2016 Dec 31. [Article]
  10. CORNFELD S: The use of ethyl aminobenzoate. Dent Surv. 1946 Jun;22(6):1101. [Article]
  11. INVIMA Product Authorization: Aldrifress (benzocaine/cetylpyridinium chloride) chewable tablets [Link]
  12. BASG Product Information: Herposicc (benzocaine/zinc oxide) lip ointment [Link]
  13. Dailymed: Dermoplast First Aid (Benzocaine and Benzethonium) Topical Spray [Link]
  14. Dailymed: Rite Aid Maximum Toothache Reliever (Benzocaine and Menthol) Oral Gel [Link]
  15. Dailymed: Americaine (Benzocaine) Topical Ointment [Link]
Human Metabolome Database
HMDB0004992
KEGG Drug
D00552
KEGG Compound
C07527
PubChem Compound
2337
PubChem Substance
46508891
ChemSpider
13854242
BindingDB
197282
RxNav
1399
ChEBI
116735
ChEMBL
CHEMBL278172
ZINC
ZINC000012358719
Therapeutic Targets Database
DAP001234
PharmGKB
PA448576
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Benzocaine
MSDS
Download (73.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionAnesthesia of Mucous Membrane1
4CompletedTreatmentAnalgesia / Pain Relief1
4CompletedTreatmentPharyngitis1
4CompletedTreatmentToothache1
4TerminatedTreatmentNasolabial Folds1
4Unknown StatusTreatmentDental Pain / Postoperative pain1
3CompletedPreventionPeripheral Intravenous Catheterization Application1
3CompletedTreatmentAcute Otitis Media (AOM)1
3CompletedTreatmentAcute Otitis Media (AOM) / Pain1
3CompletedTreatmentAtopic Dermatitis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Aidarex Pharmacuticals LLC
  • Alba Pharmacal
  • American Dental Cooperative Inc.
  • AR Medicom Inc.
  • Assured Packaging Inc.
  • Ballay Pharmaceuticals
  • Bausch & Lomb Inc.
  • Belport Co. Inc.
  • Benco Dental Co.
  • Beutlich Pharmaceuticals LP
  • Bio Pharm Inc.
  • Boca Pharmacal
  • Burkhart Dental Supply Inc.
  • Cao Group Inc.
  • Combe Inc.
  • County Line Pharmaceuticals LLC
  • Cross Country Paper Products Corp.
  • Crosstex International
  • Deepak Products Inc.
  • Dental Resources Inc.
  • Dental Technologies Inc.
  • DENTSPLY International
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • DSHealthcare Inc.
  • Essence Dental LLC
  • Foremost Dental LLC
  • Germiphene Corp.
  • Great Southern Laboratories
  • Henry Schein Inc.
  • Hi Tech Pharmacal Co. Inc.
  • Irisys Inc.
  • Laboratorios Zeyco SA De CV
  • Major Pharmaceuticals
  • Mallinckrodt Inc.
  • Marlop Pharmaceuticals Inc.
  • Medical Products Laboratories Inc.
  • Medtech Labs
  • Palmetto Pharmaceuticals Inc.
  • Patterson Dental Supply Inc.
  • Perrigo Co.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prescript Pharmaceuticals
  • PruGen Inc. Pharmaceuticals
  • Puretek Corp.
  • Qualitest
  • Rebel Distributors Corp.
  • Redpharm Drug
  • River's Edge Pharmaceuticals
  • Sciarra Laboratories Inc.
  • SDA Laboratories Inc.
  • Sonar Products Inc.
  • Sunstar Pharmaceutical Inc.
  • Taro Pharmaceuticals USA
  • Taylor Pharmaceuticals
  • Trigen Laboratories Inc.
  • UCB Pharma
  • Vintage Pharmaceuticals Inc.
  • Wyeth Pharmaceuticals
Dosage Forms
FormRouteStrength
StripDental10 mg/1
KitRespiratory (inhalation); Topical
KitOphthalmic; Oral; Respiratory (inhalation); Topical
KitOphthalmic; Topical
KitOphthalmic; Respiratory (inhalation); Topical
CreamOral
KitOral; Topical
KitTopical
KitOral; Topical200 mg/1g
StickTopical100 mg/1mL
SwabTopical
Tablet, chewableOral
Tablet, chewableOral10 mg
CreamTopical7.5 g/100g
GelDental; Periodontal200 mg/1g
Aerosol, sprayTopical11.4 g/57g
OintmentTopical5.6 g/28g
OintmentTopical
Powder, for solutionTopical
GelTopical2833 mg/60mL
StickTopical20 %
GelOral7.5 %
GelTopical20 %
SolutionTopical200 mg/1mL
LiquidOral
SolutionTopical100 mg/1mL
GelOral0.2 g/100g
LiquidTopical0.2 mg/2mL
Solution / dropsAuricular (otic)
CreamCutaneous
LiquidTopical
LiquidTopical20 g/100mL
GelOral10 g/100g
SolutionAuricular (otic)0.02 g
GelDental6.4 g/100g
GelBuccal; Topical7.5 g
GelBuccal; Topical7.5 %
LiquidTopical2.1 mg/30mL
GelTopical75 mg/1g
GelTopical100 mg/1g
LiquidTopical.075 mL/1mL
SwabTopical.075 mL/1mL
GelBuccal; Oral7.5 g
GelTopical10 g/100g
GelTopical7.5 g/100g
LozengeOral15 mg/1
GelTopical210 mg/1g
SprayTopical11.8 g/59mL
SprayTopical20 mL/100mL
GelDental230 mg/1mL
GelDental200 mg/1g
Tablet, chewableOral10 mg
GelTopical200 mg/1mL
PowderNot applicable1 g/1g
SwabTopical0.12 mL/1
SwabTopical60 mg/1mL
CreamTopical
OintmentTopical
CreamTopical0.2 g/1g
LiquidTopical5 g/100g
CreamTopical5 g/100g
SprayTopical5 g/100g
CreamTopical5 g/100mL
BeadOral3 mg/1
GelBuccal10 g/100g
LiquidBuccal
GelBuccal20 g/100mL
OintmentTopical20 %
CreamTopical71.9395789 mg/1mL
CreamTopical73.9395789 mg/1mL
CreamTopical34.05 g/454g
GelOral9 mg/1mL
TabletOral
TabletBuccal; Oral10 mg
GelTopical0.2 g/1g
KitElectro-osmosis
LotionTopical
LiquidOral20 g/100mL
CreamTopical10 g/100g
SprayOral
Tablet, orally disintegratingOral6 mg/1
LozengeOral3 mg/1
LozengeOral4 mg/1
LozengeOral
SwabTopical0.06 mL/1mL
AerosolTopical
LotionTopical50 mg/1mL
CreamTopical0.1 g/1g
OintmentTopical10 g/100g
LiquidAuricular (otic)
GelTopical0.075 g/1g
SpongeTopical
Paste, dentifriceTopical200 mg/1g
Solution
PasteDental
GelOral75 mg/1g
Paste, dentifriceTopical20 g/100g
LiquidOral200 mg/1mL
Gel, dentifriceDental20 g/100g
Gel, dentifriceOral20 g/100g
LiquidDental20 g/100g
Gel, dentifriceDental10 g/100g
Gel, dentifriceDental
SwabOral
StripTopical10 g/100g
LiquidDental
LiquidDental; Topical200 mg/1mL
GelDental
OintmentDental0.2 g/1mL
GelBuccal; Topical
OintmentTopical1.27 g/100g
LotionTopical0.05 g/1g
GelTopical7.5 %
SolutionBuccal; Oral
OintmentRectal
SuppositoryRectal
LozengeOral1.0 mg
GelTopical2410 mg/50mL
GelTopical50 mg/1mL
SprayBuccal; Oral20 %
Aerosol, meteredTopical
LiquidRectal
Aerosol, sprayTopical
LiquidOral7.5 mg/100mg
SprayOral7.5 mg/100mL
PatchTopical6 g/100g
SolutionCutaneous
SprayTopical20 G
GelTopical20 % w/w
PatchTopical
GelDental2.4 g/12g
GelDental6 g/30g
Spray, meteredDental11.4 g/57g
SprayOral; Topical
GelDental; Topical20 g/100g
GelDental20 %
GelDental; Oral; Periodontal200 mg/1
LiquidDental20 %
LiquidDental; Oral; Periodontal200 mg/1
SprayTransmucosal
KitOphthalmic; Oral; Topical
LiquidOral50 mg/1mL
LozengeOral10 mg
SolutionOral
CreamTopical4.5 g/100g
LozengeOral2 mg
SprayDental; Periodontal200 mg/1g
GelDental; Periodontal
SprayDental; Periodontal
LiquidTopical20 %
GelOral; Topical20 %
SprayTopical20 %
GelDental; Oral; Periodontal200 mg/1g
SprayDental; Oral; Periodontal200 mg/1g
LiquidDental; Oral; Periodontal200 mg/1g
AerosolDental; Topical21.9 %
LiquidTopical15 mg/1mL
SolutionTopical150 mg/1mL
GelDental; Oral6.4 g/100g
LiquidTopical6 g/100g
CreamTopical5 %
LiquidBuccal; Topical
LiquidBuccal200 mg/1mL
GelOral
CreamDental
GelTopical7 g/100mL
LozengeBuccal
GelOral20 g/100g
GelOral200 mg/1g
CreamTopical; Vaginal
GranuleOral6 mg/1
Gel, dentifriceDental200 mg/1g
LiquidTopical1417 mg/30mL
LiquidTopical50 mg/1mL
GelTopical3.00 g/100mL
GelTopical2.13 g/28.35g
GelDental; Oral6.4 g/32g
GelTopical7 g/100g
GelTopical5 g/100g
SwabTopical0.12 g/0.6mL
SwabTopical0.12 g/1g
ClothTopical
LiquidTopical5 g/100mL
SprayTopical11.4 g/57g
LiquidTopical200 mg/1g
LiquidOral200 mg/1g
GelDental
CreamTopical20 mg/100mg
CreamTopical200 mg/1mL
Powder, for solutionOral90 mg/1
GelBuccal; Topical20 g
Tablet, solubleOral6 mg
TabletBuccal
TabletBuccal; Oral
SprayTopical
GelDental; Topical
GelBuccal
Spray, meteredDental; Oral; Topical12 g/60g
Paste, dentifriceDental19.8 mg/1g
LiquidDental205 mg / g
StripDental
GelDental200 mg / g
SwabTopical0.2 g/1mL
SwabTopical0.2 mL/1mL
GelTopical
SwabTopical75 mg/1g
GelTopical10 g
Film, solubleOral
GelTopical200 mg/1g
LiquidTopical0.2 mL/1mL
PasteTopical
GelOral0.2 mL/1mL
GelTopical20 g/100g
OintmentTopical5.00 mg/1g
GelBuccal; Oral20 g
SolutionAuricular (otic)
SolutionAuricular (otic)20 mg
LiquidTopical.009 mg/1mL
LiquidTopical18.6 g/100mL
GelOral; Topical
Solution / dropsAuricular (otic)200 mg/1mL
GelTopical5 g/100mL
LiquidTopical4 g/100mL
SolutionTopical4 g/100mL
GelDental221 mg/1g
GelDental; Oral; Periodontal0.2 g/1g
GelDental; Topical20 %
CreamRectal
SuppositoryRectal5 MG
GelTopical20 1/100g
CreamTopical4.2 g/56g
DressingTopical70 g/1000g
LiquidAuricular (otic)200 mg/1mL
OintmentTopical200 mg/1g
LiquidTopical200 mg/1mL
Gel, dentifriceOral7.5 g/100g
GelOral200 mg/1mL
Gel, dentifriceOral
SwabTopical15 %
Powder, for solutionOral150 mg/3000mg
KitTopical0.05 g/1g
ClothTopical0.0543 g/1
KitTopical0.0543 g/1
KitTopical6 g/1
GelDental; Oral20 g/100g
Aerosol, sprayTopical1.125 g/15g
GelTopical5.06 g/67.50g
GelTopical5.07 g/67.5g
GelTopical5.07 g/67.50g
SyrupDental1.8 %
Gum, chewingOral
SolutionTopical
SwabTopical0.06 mg/1
SolutionTopical10 g/100g
SwabTopical6 g/100mL
SwabOral20 %
PatchCutaneous
LiquidOral1.3 mg/13mL
LiquidOral10 g/100mL
OintmentTopical3.5 g/100g
DressingOral
Gel, dentifriceDental220 mg/1g
Spray, meteredPeriodontal220 mg/1g
GelOral; Topical200 mg / g
GelDental220 mg/1g
GelTopical18 g
GelTopical20 mg
GelTopical180 mg/g
SprayTopical4.5 g/60mL
GelDental200 mg/1mL
EnemaRectal
SprayTopical7.5 g/100mL
Spray
OintmentTopical20 g/100g
LiquidOral20 g/100g
SwabTopical6 g/1001
Spray, meteredTopical
AerosolOral
GelTopical10 %
SwabTopical20 %
GelTopical0.1 g/1g
GelDental20 g/100g
Gel7.5 %w/w
Prices
Unit descriptionCostUnit
Americaine Anesthetic 20% Gel 28 gm Tube22.99USD tube
Americaine 20% ear drops1.26USD ml
Oticaine 20% ear drops0.83USD ml
Americaine lubricant0.71USD g
Hurricaine 20% liquid swab0.6USD swab
Hurricaine 20% spray0.52USD ml
Anbesol baby 7.5% gel0.41USD g
Cepacol 6 mg fizzlers tablet0.39USD tablet
Benzocaine powder0.09USD g
Dermoplast pain relieving spry0.07USD ml
Dermoplast spray0.07USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)92 °CPhysProp
boiling point (°C)310 °CPhysProp
water solubility1310 mg/L (at 30 °C)YALKOWSKY,SH & HE,Y (2003)
logP1.86HANSCH,C ET AL. (1995)
pKa2.51 (at 25 °C)PERRIN,DD (1965)
Predicted Properties
PropertyValueSource
Water Solubility2.85 mg/mLALOGPS
logP2.2ALOGPS
logP1.5ChemAxon
logS-1.8ALOGPS
pKa (Strongest Basic)2.78ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area52.32 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity47.53 m3·mol-1ChemAxon
Polarizability17.46 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9963
Blood Brain Barrier+0.9609
Caco-2 permeable+0.7814
P-glycoprotein substrateNon-substrate0.8329
P-glycoprotein inhibitor INon-inhibitor0.9589
P-glycoprotein inhibitor IINon-inhibitor0.9612
Renal organic cation transporterNon-inhibitor0.8818
CYP450 2C9 substrateNon-substrate0.8426
CYP450 2D6 substrateNon-substrate0.7934
CYP450 3A4 substrateNon-substrate0.7513
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.937
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7883
Ames testNon AMES toxic0.8825
CarcinogenicityCarcinogens 0.513
BiodegradationReady biodegradable0.7718
Rat acute toxicity1.7665 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9721
hERG inhibition (predictor II)Non-inhibitor0.9668
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.74 KB)
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (1 TMS)GC-MSsplash10-00dl-0980000000-9bd6d020be04ce49bd3e
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-00di-4900000000-9341302295e361a20bfd
GC-MS Spectrum - EI-BGC-MSsplash10-0109-9400000000-8e31c925b871e0f0299e
GC-MS Spectrum - EI-BGC-MSsplash10-0109-9400000000-c755b4e5336a2867357e
GC-MS Spectrum - EI-BGC-MSsplash10-01b9-1900000000-a811093acfd0672fece6
GC-MS Spectrum - CI-BGC-MSsplash10-014i-0900000000-49302e8e4fd5158a36da
GC-MS Spectrum - EI-BGC-MSsplash10-00di-5900000000-dcd2847110af7c87bf18
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00dl-0980000000-9bd6d020be04ce49bd3e
Mass Spectrum (Electron Ionization)MSsplash10-00xr-6900000000-0594451f3b181ab3c883
MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)LC-MS/MSsplash10-00kr-0900000000-b54aebb77e7a69ada07c
MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)LC-MS/MSsplash10-014i-5900000000-ce90658bd0fc66df820d
MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)LC-MS/MSsplash10-03xu-9100000000-5179b7804d2c59e71aa4
MS/MS Spectrum - EI-B (HITACHI RMU-7M) , PositiveLC-MS/MSsplash10-00di-4900000000-9341302295e361a20bfd
MS/MS Spectrum - EI-B (HITACHI RMU-7) , PositiveLC-MS/MSsplash10-0109-9400000000-8e31c925b871e0f0299e
MS/MS Spectrum - EI-B (HITACHI RMU-6D) , PositiveLC-MS/MSsplash10-0109-9400000000-c755b4e5336a2867357e
MS/MS Spectrum - EI-B (HITACHI M-60) , PositiveLC-MS/MSsplash10-01b9-1900000000-57d39b512bc5bdbb4987
MS/MS Spectrum - CI-B (HITACHI M-60) , PositiveLC-MS/MSsplash10-014i-0900000000-49302e8e4fd5158a36da
MS/MS Spectrum - EI-B (JEOL JMS-DX-300) , PositiveLC-MS/MSsplash10-00di-5900000000-dcd2847110af7c87bf18
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, PositiveLC-MS/MSsplash10-014i-0900000000-a0f10abbe67842c2c958
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, PositiveLC-MS/MSsplash10-00du-5900000000-43a89461a4d9cc5d1409
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, PositiveLC-MS/MSsplash10-00dl-9600000000-049e2653cbbf24aaf010
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, PositiveLC-MS/MSsplash10-002f-9100000000-6fbc7720b326773643af
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, PositiveLC-MS/MSsplash10-00ou-9000000000-d7f7622c3a270c5ffcbb
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-0900000000-e061a0f4172b47a8bd22
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00du-5900000000-54757e57c91d3eaa1976
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00dl-9600000000-049e2653cbbf24aaf010
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-002f-9100000000-e16fc2db7a632fc6f4da
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00ou-9000000000-d7f7622c3a270c5ffcbb
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-5900100000-72ac4bcb64db0d25261e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-000i-2900000000-89639c79865df34d7081
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-000i-2900000000-2132ea2de3c0db3e47fa
1H NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity
Specific 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 acro...
Gene Name
SCN10A
Uniprot ID
Q9Y5Y9
Uniprot Name
Sodium channel protein type 10 subunit alpha
Molecular Weight
220623.605 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Ahern CA, Eastwood AL, Dougherty DA, Horn R: Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels. Circ Res. 2008 Jan 4;102(1):86-94. Epub 2007 Oct 25. [Article]
  4. Hanck DA, Nikitina E, McNulty MM, Fozzard HA, Lipkind GM, Sheets MF: Using lidocaine and benzocaine to link sodium channel molecular conformations to state-dependent antiarrhythmic drug affinity. Circ Res. 2009 Aug 28;105(5):492-9. doi: 10.1161/CIRCRESAHA.109.198572. Epub 2009 Aug 6. [Article]
  5. Lipkind GM, Fozzard HA: Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels. Mol Pharmacol. 2005 Dec;68(6):1611-22. Epub 2005 Sep 20. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Hartman NR, Mao JJ, Zhou H, Boyne MT 2nd, Wasserman AM, Taylor K, Racoosin JA, Patel V, Colatsky T: More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems. Regul Toxicol Pharmacol. 2014 Oct;70(1):182-8. doi: 10.1016/j.yrtph.2014.07.002. Epub 2014 Jul 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Hartman NR, Mao JJ, Zhou H, Boyne MT 2nd, Wasserman AM, Taylor K, Racoosin JA, Patel V, Colatsky T: More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems. Regul Toxicol Pharmacol. 2014 Oct;70(1):182-8. doi: 10.1016/j.yrtph.2014.07.002. Epub 2014 Jul 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Hartman NR, Mao JJ, Zhou H, Boyne MT 2nd, Wasserman AM, Taylor K, Racoosin JA, Patel V, Colatsky T: More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems. Regul Toxicol Pharmacol. 2014 Oct;70(1):182-8. doi: 10.1016/j.yrtph.2014.07.002. Epub 2014 Jul 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Hartman NR, Mao JJ, Zhou H, Boyne MT 2nd, Wasserman AM, Taylor K, Racoosin JA, Patel V, Colatsky T: More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems. Regul Toxicol Pharmacol. 2014 Oct;70(1):182-8. doi: 10.1016/j.yrtph.2014.07.002. Epub 2014 Jul 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Hartman NR, Mao JJ, Zhou H, Boyne MT 2nd, Wasserman AM, Taylor K, Racoosin JA, Patel V, Colatsky T: More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems. Regul Toxicol Pharmacol. 2014 Oct;70(1):182-8. doi: 10.1016/j.yrtph.2014.07.002. Epub 2014 Jul 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Triglyceride lipase activity
Specific Function
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acy...
Gene Name
CES1
Uniprot ID
P23141
Uniprot Name
Liver carboxylesterase 1
Molecular Weight
62520.62 Da
References
  1. Bell FP: The effect of local anesthetics on arterial lipid metabolism. Inhibition of sterol esterification in vitro. Atherosclerosis. 1981 Jan-Feb;38(1-2):81-8. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Kitamura K, Omran AA, Takegami S, Tanaka R, Kitade T: (19)F NMR spectroscopic characterization of the interaction of niflumic acid with human serum albumin. Anal Bioanal Chem. 2007 Apr;387(8):2843-8. doi: 10.1007/s00216-007-1162-x. Epub 2007 Feb 14. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as 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...

Components:
References
  1. Becker DE, Reed KL: Essentials of local anesthetic pharmacology. Anesth Prog. 2006 Fall;53(3):98-108; quiz 109-10. doi: 10.2344/0003-3006(2006)53[98:EOLAP]2.0.CO;2. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. 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]

Drug created at June 13, 2005 13:24 / Updated at November 28, 2021 11:56