Phenylephrine
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Identification
- Summary
Phenylephrine is an alpha-1 adrenergic agonist used in the management of hypotension, generally in the surgical setting associated with the use of anesthetics.
- Brand Names
- 4-way, Advil Congestion Relief, Advil Sinus Congestion and Pain, Ala-hist PE, Allerest PE, Benadryl-D Allergy and Sinus, Biorphen, Cyclomydril, Dayquil Sinex, Deconex, Despec Reformulated Jun 2008, Dimetapp Nighttime Cold & Congestion, Diphen, Entex Lq, Gilphex, Histex Ac, Immphentiv, M-end PE, Mydcombi, Mydfrin, Nasopen PE, Neo-synephrine, Omidria, Poly Hist Forte Reformulated Nov 2013, Preparation H Cooling Gel, Preparation H Cream, Preparation H Reformulated Jun 2013, Refenesen PE, Rescon-GG, Rymed-D, Soframycin, Sudafed PE, Sudafed PE Children's Cold & Cough, Sudafed PE Children's Nasal Decongestant, Sudafed PE Head Congestion Plus Pain, Sudafed PE Sinus Headache, Sudo-tab, Sudogest PE, Triaminic Day Time Cold & Cough, Triaminic Night Time Cold & Cough, Vazculep, Wal-profen Congestion Relief and Pain
- Generic Name
- Phenylephrine
- DrugBank Accession Number
- DB00388
- Background
Phenylephrine is an alpha-1 adrenergic receptor agonist used to treat hypotension,6,8 dilate the pupil,7 and induce local vasoconstriction.1 The action of phenylephrine, or neo-synephrine, was first described in literature in the 1930s.2
Phenylephrine was granted FDA approval in 1939.7
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 167.205
Monoisotopic: 167.094628665 - Chemical Formula
- C9H13NO2
- Synonyms
- (−)-m-hydroxy-α-(methylaminomethyl)benzyl alcohol
- Fenilefrina
- l-(3-Hydroxyphenyl)-N-methylethanolamine
- Phenylephrine
- Phenylephrinum
- R(-)-Phenylephrine
- External IDs
- J8.601K
Pharmacology
- Indication
Phenylephrine is available in various drug formulations, which have different indications. Phenylephrine injections are indicated to treat hypotension caused by shock or anesthesia.6,8 The ophthalmic formulation is indicated to induce mydriasis 7,9 and conjunctival vasoconstriction.1 The intranasal formulation is used to treat congestion, and a topical formulation is used to treat hemorrhoids.1 Off-label uses include priapism and induction of local vasoconstriction.1
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for symptomatic treatment of Allergic rhinitis (ar) Combination Product in combination with: Levocetirizine (DB06282) ••• ••• •••••••• •••••• Used in combination for symptomatic treatment of Anorectal discomfort Combination Product in combination with: Pramocaine (DB09345) ••• ••• ••••• Used in combination for symptomatic treatment of Anorectal discomfort Combination Product in combination with: Pramocaine (DB09345) ••• ••• ••••• Used in combination for symptomatic treatment of Cold Combination Product in combination with: Guaifenesin (DB00874), Acetaminophen (DB00316) ••• ••• ••••• Used in combination for symptomatic treatment of Cold Combination Product in combination with: Ascorbic acid (DB00126), Acetaminophen (DB00316) ••• ••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Phenylephrine is an alpha-1 adrenergic agonist that raises blood pressure,6,8 dilates the pupils,7 and causes local vasoconstriction.1 Ophthalmic formulations of phenylephrine act for 3-8 hours7 while intravenous solutions have an effective half life of 5 minutes and an elimination half life of 2.5 hours.3,6 Patients taking ophthalmic formulations of phenylephrine should be counselled about the risk of arrhythmia, hypertension, and rebound miosis.7 Patients taking an intravenous formulation should be counselled regarding the risk of bradycardia, allergic reactions, extravasation causing necrosis or tissue sloughing, and the concomitant use of oxytocic drugs.6,8
- Mechanism of action
Phenylephrine is an alpha-1 adrenergic agonist that mediates vasoconstriction1 and mydriasis7 depending on the route and location of administration. Systemic exposure to phenylephrine also leads to agonism of alpha-1 adrenergic receptors, raising systolic and diastolic pressure as well as peripheral vascular resistance.6,8 Increased blood pressure stimulates the vagus nerve, causing reflex bradycardia.6,8
Target Actions Organism AAlpha-1A adrenergic receptor agonistHumans AD(2) dopamine receptor agonistHumans AAlpha-1B adrenergic receptor agonistHumans AAlpha-1D adrenergic receptor agonistHumans - Absorption
Phenylephrine is 38% orally bioavailable.3 Clinically significant systemic absorption of ophthalmic formulations is possible, especially at higher strengths and when the cornea is damaged.6
- Volume of distribution
- Protein binding
Data regarding the protein binding of phenylephrine in serum is not readily available.6,7,8
- Metabolism
Phenylephrine is mainly metabolized by monoamine oxidase A, monoamine oxidase B, and SULT1A3.4,5,6,8 The major metabolite is the inactive meta-hydroxymandelic acid, followed by sulfate conjugates.5,6,8 Phenylephrine can also be metabolized to phenylephrine glucuronide.5
Hover over products below to view reaction partners
- Route of elimination
86% of a dose of phenylephrine is recovered in the urine3 with 16% as the unmetabolized drug, 57% as the inactive meta-hydroxymendelic acid, and 8% as inactive sulfate conjugates.6,8
- Half-life
Intravenous phenylephrine has an effective half life of 5 minutes and an elimination half life of 2.5 hours.3,6,8
- Clearance
- Adverse Effects
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- Toxicity
Patients experiencing and overdose may present with headache, hypertension, reflex bradycardia, tingling limbs, cardiac arrhythmias, and a feeling of fullness in the head.6,7,8 Overdose may be treated by supportive care and discontinuing phenylephrine, chronotropic medications, and vasodilators.1 Subcutaneous phentolamine may be used to treat tissue extravasation.1,7
- Pathways
- Not Available
- 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 Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of hypertension can be decreased when 1,2-Benzodiazepine is combined with Phenylephrine. Acebutolol The therapeutic efficacy of Phenylephrine can be decreased when used in combination with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Phenylephrine is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Phenylephrine is combined with Acemetacin. Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Phenylephrine. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Phenylephrine bitartrate 27O3Q5ML57 17162-39-9 NHKOTKKHHYKARN-NDAAPVSOSA-N Phenylephrine hydrochloride 04JA59TNSJ 61-76-7 OCYSGIYOVXAGKQ-FVGYRXGTSA-N Phenylephrine tannate DU5ATO7HYP 1416-03-1 HXLHQWSMCJUVMM-RVLWPPNGSA-N - Active Moieties
Name Kind UNII CAS InChI Key Chloride ion ionic Q32ZN48698 16887-00-6 VEXZGXHMUGYJMC-UHFFFAOYSA-M - Product Images
- International/Other Brands
- AK-Dilate / AK-Nefrin / Alconefrin / Mesatone / Minims Phenylephrine / Neofrin / Ocugestrin / Phenoptic / Phenylephrine Minims / Prefrin / Rhinall / Spersaphrine / Visadron
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Biorphen Injection, solution 0.1 mg/1mL Intravenous Eton Pharmaceuticals, Inc. 2019-11-15 Not applicable US Biorphen Injection, solution 10 mg/1mL Intravenous Eton Pharmaceuticals, Inc. 2021-03-11 2021-04-01 US Biorphen Injection, solution 0.1 mg/1mL Intravenous Dr. Reddy's Laboratories Limited 2022-11-25 Not applicable US Biorphen Injection, solution 0.1 mg/1mL Intravenous Eton Pharmaceuticals, Inc. 2019-11-15 Not applicable US Biorphen Injection, solution 10 mg/1mL Intravenous Dr. Reddy's Laboratories Limited 2022-11-25 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Phenylephrine Hydrochloride Injection 10 mg/1mL Intravenous Sandoz S.P.A. 2020-01-15 Not applicable US Phenylephrine Hydrochloride Injection 10 mg/1mL Intravenous Somerset Therapeutics, Llc 2023-07-17 Not applicable US Phenylephrine Hydrochloride Injection 10 mg/1mL Intravenous Sandoz S.P.A. 2021-02-17 Not applicable US Phenylephrine Hydrochloride Solution 25 mg/1mL Ophthalmic Leading Pharma, Llc 2024-09-05 Not applicable US Phenylephrine Hydrochloride Injection 10 mg/1mL Intravenous Medical Purchasing Solutions, Llc 2021-09-22 Not applicable US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image 4 Way Fast Acting Spray 10 mg/1mL Nasal GlaxoSmithKline Consumer Healthcare Holdings (US) LLC 2010-01-01 Not applicable US 7 Select Nasal Decongestant PE Tablet, film coated 10 mg/1 Oral 7-Eleven 2016-10-07 2020-11-30 US Actifed Tablet 5 mg/1 Oral Belmora LLC 2023-08-01 Not applicable US Anti Hemorrhoidal H Suppository Suppository 0.25 % w/w Rectal Cellchem Pharmaceuticals Inc. Not applicable Not applicable Canada Assured Maximum Strength Nasal Decongestant Tablet 10 mg/1 Oral Spirit Pharmaceuticals LLC 2019-02-26 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 24/7 Life Cold and Flu DayTime Severe Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Dextromethorphan hydrobromide monohydrate (10 mg/1) + Guaifenesin (200 mg/1) Tablet, film coated Oral Lil' Drug Store Products, Inc. 2021-10-27 Not applicable US 4248 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Acetaminophen (110 mg/1) + Acetylsalicylic acid (162 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) + Benzethonium chloride (0.2 g/100g) + Benzocaine (10 g/100g) + Benzocaine (10 g/100g) + Caffeine (32.4 mg/1) + Calcium carbonate (420 mg/1) + 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) + Menthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Salicylamide (152 mg/1) + Tetrahydrozoline hydrochloride (0.05 g/100mL) + Water (98.6 mL/100mL) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US 4356 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + 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) + Benzethonium chloride (0.2 g/100g) + Benzocaine (10 g/100g) + Benzocaine (10 g/100g) + Calcium carbonate (420 mg/1) + 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) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US 4390 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (0.13 g/100mL) + Calcium carbonate (420 mg/1) + Ethanol (62 mL/100mL) + Ibuprofen (200 mg/1) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (24.64 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US 4392 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (0.13 g/100mL) + Calcium carbonate (420 mg/1) + Ethanol (62 mL/100mL) + Ibuprofen (200 mg/1) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (24.64 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 4248 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Acetaminophen (110 mg/1) + Acetylsalicylic acid (162 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) + Benzethonium chloride (0.2 g/100g) + Benzocaine (10 g/100g) + Benzocaine (10 g/100g) + Caffeine (32.4 mg/1) + Calcium carbonate (420 mg/1) + 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) + Menthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (5000 [iU]/1g) + Salicylamide (152 mg/1) + Tetrahydrozoline hydrochloride (0.05 g/100mL) + Water (98.6 mL/100mL) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US 4356 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + 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) + Benzethonium chloride (0.2 g/100g) + Benzocaine (10 g/100g) + Benzocaine (10 g/100g) + Calcium carbonate (420 mg/1) + 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) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US 4390 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (0.13 g/100mL) + Calcium carbonate (420 mg/1) + Ethanol (62 mL/100mL) + Ibuprofen (200 mg/1) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (24.64 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US 4392 First Aid Kit Phenylephrine hydrochloride (5 mg/1) + Acetaminophen (325 mg/1) + Ammonia (0.045 g/0.3mL) + Benzalkonium chloride (0.13 g/100mL) + Calcium carbonate (420 mg/1) + Ethanol (62 mL/100mL) + Ibuprofen (200 mg/1) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (24.64 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL) Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Honeywell Safety Products USA, Inc 2018-10-18 Not applicable US A-Tan 12X Suspension Phenylephrine tannate (5 mg/5mL) + Guaifenesin (100 mg/5mL) + Mepyramine tannate (30 mg/5mL) Suspension Oral Amneal Pharmaceuticals LLC 2006-01-06 2008-12-05 US
Categories
- ATC Codes
- S01FB01 — Phenylephrine
- S01FB — Sympathomimetics excl. antiglaucoma preparations
- S01F — MYDRIATICS AND CYCLOPLEGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- R01AB — Sympathomimetics, combinations excl. corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- C01CA — Adrenergic and dopaminergic agents
- C01C — CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
- C01 — CARDIAC THERAPY
- C — CARDIOVASCULAR SYSTEM
- R01AA — Sympathomimetics, plain
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- C05AX — Other agents for treatment of hemorrhoids and anal fissures for topical use
- C05A — AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- S01FB — Sympathomimetics excl. antiglaucoma preparations
- S01F — MYDRIATICS AND CYCLOPLEGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- S01GA — Sympathomimetics used as decongestants
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- R01BA — Sympathomimetics
- R01B — NASAL DECONGESTANTS FOR SYSTEMIC USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- S01GA — Sympathomimetics used as decongestants
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Adrenergic Agents
- Adrenergic Agonists
- Adrenergic alpha-1 Receptor Agonists
- Adrenergic alpha-Agonists
- Adrenergic and Dopaminergic Agents
- Agents for Treatment of Hemorrhoids and Anal Fissures for Topical Use
- Agents producing tachycardia
- Agents that produce hypertension
- Alcohols
- Amines
- Amino Alcohols
- Autonomic Agents
- Cardiac Stimulants Excl. Cardiac Glycosides
- Cardiac Therapy
- Cardiotonic Agents
- Cardiovascular Agents
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Decongestants and Antiallergics
- Ethanolamines
- Monoamine Oxidase A Substrates
- Mydriatics
- Mydriatics and Cycloplegics
- Nasal Decongestants
- Nasal Decongestants for Systemic Use
- Nasal Preparations
- Neurotransmitter Agents
- Ophthalmologicals
- Peripheral Nervous System Agents
- Protective Agents
- Respiratory System Agents
- Sensory Organs
- Sympathomimetic (Adrenergic) Agents
- Sympathomimetics
- Sympathomimetics Excl. Antiglaucoma Preparations
- Sympathomimetics Used as Decongestants
- Sympathomimetics, Plain
- Vasoconstrictor Agents
- Vasoprotectives
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 1-hydroxy-4-unsubstituted benzenoids. These are phenols that are unsubstituted at the 4-position.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenols
- Sub Class
- 1-hydroxy-4-unsubstituted benzenoids
- Direct Parent
- 1-hydroxy-4-unsubstituted benzenoids
- Alternative Parents
- Aralkylamines / 1-hydroxy-2-unsubstituted benzenoids / Benzene and substituted derivatives / Secondary alcohols / 1,2-aminoalcohols / Dialkylamines / Organopnictogen compounds / Hydrocarbon derivatives / Aromatic alcohols
- Substituents
- 1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Alcohol / Amine / Aralkylamine / Aromatic alcohol / Aromatic homomonocyclic compound / Hydrocarbon derivative / Monocyclic benzene moiety
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- phenylethanolamines, secondary amino compound (CHEBI:8093)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1WS297W6MV
- CAS number
- 59-42-7
- InChI Key
- SONNWYBIRXJNDC-VIFPVBQESA-N
- InChI
- InChI=1S/C9H13NO2/c1-10-6-9(12)7-3-2-4-8(11)5-7/h2-5,9-12H,6H2,1H3/t9-/m0/s1
- IUPAC Name
- 3-[(1R)-1-hydroxy-2-(methylamino)ethyl]phenol
- SMILES
- CNC[C@H](O)C1=CC(O)=CC=C1
References
- Synthesis Reference
Franz Dietrich Klinger, Lienhard Wolter, Wolfgang Dietrich, "Method for preparing of L-phenylephrine hydrochloride." U.S. Patent US6187956, issued February, 1976.
US6187956- General References
- Richards E, Maani CV: Phenylephrine . [Article]
- Prescott F: CLINICAL EVALUATION OF THE PRESSOR ACTIVITY OF METHEDRINE, NEO-SYNEPHRINE, PAREDRINE, AND PHOLEDRINE. Br Heart J. 1944 Oct;6(4):214-20. doi: 10.1136/hrt.6.4.214. [Article]
- Kanfer I, Dowse R, Vuma V: Pharmacokinetics of oral decongestants. Pharmacotherapy. 1993 Nov-Dec;13(6 Pt 2):116S-128S; discussion 143S-146S. [Article]
- Bairam AF, Rasool MI, Alherz FA, Abunnaja MS, El Daibani AA, Gohal SA, Alatwi ES, Kurogi K, Liu MC: Impact of SULT1A3/SULT1A4 genetic polymorphisms on the sulfation of phenylephrine and salbutamol by human SULT1A3 allozymes. Pharmacogenet Genomics. 2019 Jul;29(5):99-105. doi: 10.1097/FPC.0000000000000371. [Article]
- Gelotte CK, Zimmerman BA: Pharmacokinetics, safety, and cardiovascular tolerability of phenylephrine HCl 10, 20, and 30 mg after a single oral administration in healthy volunteers. Clin Drug Investig. 2015 Sep;35(9):547-58. doi: 10.1007/s40261-015-0311-9. [Article]
- FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [Link]
- FDA Approved Drug Products: Phenylephrine Ophthalmic Solution [Link]
- FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [Link]
- FDA Approved Drug Products: MYDCOMBI (tropicamide and phenylephrine hydrochloride ophthalmic spray) 1%/2.5%, for topical ophthalmic use [Link]
- External Links
- Human Metabolome Database
- HMDB0002182
- KEGG Drug
- D08365
- KEGG Compound
- C07441
- PubChem Compound
- 6041
- PubChem Substance
- 46506961
- ChemSpider
- 5818
- BindingDB
- 50067212
- 8163
- ChEBI
- 8093
- ChEMBL
- CHEMBL1215
- ZINC
- ZINC000000113355
- Therapeutic Targets Database
- DAP000224
- PharmGKB
- PA450935
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Phenylephrine
- MSDS
- Download (74.7 KB)
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 dataNot Available Active Not Recruiting Treatment Anesthesia therapy / Hypotension 1 somestatus stop reason just information to hide Not Available Completed Not Available Healthy Volunteers (HV) 1 somestatus stop reason just information to hide Not Available Completed Not Available Uterine Fibroids (Leiomyomas) 1 somestatus stop reason just information to hide Not Available Completed Basic Science Assess Phenylephrine on EVP and IOP 1 somestatus stop reason just information to hide Not Available Completed Basic Science Cardiovascular Disease (CVD) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Accutome Inc.
- Advanced Pharmaceutical Services Inc.
- Advent Pharmaceuticals Inc.
- Aero Pharmaceuticals Inc.
- AG Marin Pharmaceuticals
- Akorn Inc.
- Alba Pharmacal
- Alcon Laboratories
- Allegis Pharmaceuticals
- Allergy Laboratories Inc.
- Altaire Pharmaceuticals
- Ambi Pharmaceuticals Inc.
- Amend
- American Regent
- Amneal Pharmaceuticals
- Anip Acquisition Co.
- A-S Medication Solutions LLC
- Athlon Pharmaceuticals Inc.
- Auriga Pharmaceuticals LLC
- Baroli
- Bausch & Lomb Inc.
- Baxter International Inc.
- Bayer Healthcare
- Bio Pharm Inc.
- Blansett Pharmacal Co. Inc.
- Boca Pharmacal
- Breckenridge Pharmaceuticals
- Brookstone Pharmaceuticals
- Bryant Ranch Prepack
- BTA Pharmaceuticals
- Burel Pharmaceuticals Inc.
- Capellon Pharmaceuticals LLC
- Cardinal Health
- Centurion Labs
- Chain Drug
- Chemins Co. Inc.
- Claris Lifesciences Inc.
- Conta Care Ophthalmics and Diagnostics
- Contract Pharm
- Cornerstone Pharmacy
- Cypress Pharmaceutical Inc.
- Deca Pharmaceuticals LLC
- Deltex Pharmaceuticals Inc.
- Deston Therapeutics
- Dexo LLC
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- DSC Laboratories
- Ebewe Pharma
- Econolab Inc.
- Edwards Pharmaceuticals
- Emerson Labs
- Endo Pharmaceuticals Inc.
- Everett Laboratories Inc.
- Eye Care and Cure Corp.
- Eye Supply Usa Inc.
- Falcon Pharmaceuticals Ltd.
- Gayheart Pharmaceutical Inc.
- Gentex Pharma LLC
- Gil Pharmaceutical Corp.
- Gm Pharmaceuticals Inc.
- Great Southern Laboratories
- Hawthorn Pharmaceuticals
- Hi Tech Pharmacal Co. Inc.
- Hospira Inc.
- HUB Pharmaceuticals
- International Ethical Labs Inc.
- Invision Pharmaceuticals
- Iopharm Laboratories Inc.
- Irisys Inc.
- Jaymac Pharmaceuticals LLC
- Kowa Pharmaceuticals America Inc.
- Kylemore Pharmaceuticals
- Lark Pharmaceuticals Inc.
- Larken Laboratories Inc.
- Laser Pharmaceuticals
- Luitpold Pharmaceuticals Inc.
- Lunsco Inc.
- Macoven Pharmaceuticals LLC
- Major Pharmaceuticals
- Marnel Pharmaceuticals Inc.
- MCR American Pharmaceuticals Inc.
- Med Tek Pharmaceuticals Inc.
- Meda AB
- Medique Products
- Midland Healthcare LLC
- Midland Pharmaceutical LLC
- Midlothian Labs
- Monte Sano Pharmaceuticals Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Nadin Co.
- Neilgen Pharma Inc.
- Nephron Pharmaceuticals Corp.
- Nexgen Pharma Inc.
- Nolco Pharmaceuticals Inc.
- Norega Laboratories Inc.
- Novis PR Inc.
- Nucare Pharmaceuticals Inc.
- Numark Laboratories Inc.
- Ocusoft
- Optopics
- Palm Pharmaceuticals LLC
- Palmetto Pharmaceuticals Inc.
- Pamlab LLC
- Pfizer Inc.
- Pharmaceutical Association
- Pharmaceutical Generic Developers Inc.
- Pharmedium
- Physicians Total Care Inc.
- Poly Pharmaceuticals Inc.
- Portal Inc.
- Prasco Labs
- Preferred Pharmaceuticals Inc.
- Prescript Pharmaceuticals
- Provident Pharmaceuticals LLC
- Qualitest
- Quality Home Products
- Quality Research Pharmaceutical Inc.
- Rebel Distributors Corp.
- Respa Pharmaceuticals Inc.
- Rico Pharmacal
- River's Edge Pharmaceuticals
- Rugby Laboratories
- Rx Formulations Corp.
- Sanofi-Aventis Inc.
- Scherer Labs
- Schwarz Pharma Inc.
- Scientific Laboratories Inc.
- Seatrace Pharmaceuticals Inc.
- Seyer Pharmatec Inc.
- Silarx Pharmaceuticals
- Sonar Products Inc.
- Sorter Labs
- Southwood Pharmaceuticals
- Sovereign Pharmaceuticals Ltd.
- Stesso Pharmaceuticals LLC
- Summa Rx Laboratories Inc.
- Teral Laboratories
- Teva Pharmaceutical Industries Ltd.
- TG United Inc.
- Tiber Pharmaceuticals LLC
- Tri Med Laboratories Inc.
- Trigen Laboratories Inc.
- United Research Laboratories Inc.
- US Pharmaceutical Corp.
- Varsity Laboratories
- Vertical Pharmaceuticals Inc.
- Vetco Pharma
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- Vision Pharma LLC
- Walgreen Co.
- Wilson Ophthalmic Corp.
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- Dosage Forms
Form Route Strength Kit Ophthalmic; Oral; Respiratory (inhalation); Topical Solution Oral Tablet Oral 4.000 mg Solution Nasal 0.500 g Capsule, liquid filled Not applicable Tablet, effervescent Oral Granule, effervescent Oral Capsule, gelatin coated Oral Kit Oral Tablet, coated Oral Solution Intramuscular; Intravenous; Subcutaneous 10 mg Tablet Oral 500.00 mg Syrup Oral 10 mg/5mL Solution / drops Ophthalmic 1.2 mg/15mL Strip Oral 10 mg Solution Oral 1.25 mg / 0.8 mL Capsule Capsule Nasal Suspension / drops Oral Injection, solution Intravenous 0.1 mg/1mL Injection, solution Parenteral 0.1 mg/ml Injection, solution Parenteral 10 mg/ml Tablet 10 mg Tablet; tablet, multilayer Oral 500 mg Tablet 400 mg Tablet; tablet, multilayer Oral Solution Oral 500.000 mg Tablet Oral 5.000 mg Syrup Oral 2 mg/5ml Liquid Topical Capsule Oral 250.0000 mg Solution / drops Ophthalmic 10 % Elixir Oral Solution Oral 2.5 mg/5mL Liquid Auricular (otic) Solution Oral 2.500 g Spray Nasal 50 mg/ml Kit; tablet, coated Oral Suspension Kit; tablet Oral Capsule, coated pellets Oral Tablet Oral 4.00 mg Solution Nasal 1.25 mg/1mL Gel Rectal Cream Topical Solution Ophthalmic 0.2 % Kit; liquid; solution Oral Kit; tablet; tablet, coated Oral Capsule; kit Oral Kit; liquid Oral Capsule, gelatin coated; capsule, liquid filled; kit Oral Tablet Oral 300 mg Tablet Oral 5 1/1 Tablet, chewable Oral Liquid Oral 2.5 mg/5mL Syrup Not applicable Elixir; kit; solution Oral Cream; kit; liquid; ointment; tablet; tablet, chewable; tablet, film coated Oral; Topical Syrup Oral 5 mg/5mL Aerosol, metered Respiratory (inhalation) Spray Nasal 21.73 mg/15mL Spray Nasal 10 mg/1mL Granule Oral 650.00 mg Tablet Oral 500.000 mg Injection, solution Solution Conjunctival; Ophthalmic 100 mg Solution Intravenous 10 mg Solution Ophthalmic 25 mg Solution / drops Nasal; Topical Injection, solution 100 MICROGRAMMI/ML Cloth Topical Powder, for suspension Oral Capsule Oral 15 mg Solution Oral 55.000 mg Solution / drops Ophthalmic 1.2 mg/1mL Solution / drops Nasal Cream Rectal; Topical Tablet Oral 50000000 mg Gel Topical Ointment Topical 0.25 % Spray Topical Tablet Oral 325.000 mg Kit; powder Oral Spray Nasal Injectable, liposomal Intravenous 100 ug/1mL Injection Intravenous 100 ug/1mL Tablet, orally disintegrating Oral Liquid Nasal 1 g/100mL Solution Nasal 0.250 g Capsule Oral 25 mg Powder, for solution Oral 1000 mg Solution Oral 0.400 g Tablet, multilayer Oral Liquid Nasal 0.125 % Liquid Nasal 1.25 mg/1mL Liquid Nasal 0.00125 mg/1mL Solution Nasal 2.500 mg Solution / drops Oral Tablet, film coated Oral 5 mg/1 Ointment Rectal; Topical Solution Ophthalmic 2.5 % w/v Solution Ophthalmic 10 % w/v Kit; solution; suspension Oral Kit; tablet, film coated Oral Kit; tablet, coated; tablet, film coated Oral Capsule, liquid filled; kit; solution Nasal; Oral Capsule Oral Capsule, liquid filled Oral Spray, metered Ophthalmic Solution / drops Ophthalmic 2.5 % Injection, solution Intraocular Insert Ophthalmic Tablet, coated Oral 10 mg/1 Tablet Oral 25 mg/1 Solution / drops Topical 0.25 g/100mL Spray Topical 0.25 g/100mL Syrup Oral 40 mg/5mL Solution / drops Nasal 1 % Solution Intramuscular; Intravenous; Subcutaneous 10 mg / mL Solution / drops Nasal Spray Nasal 0.25 g/100mL Spray Nasal 0.5 g/100mL Liquid Intramuscular; Intravenous; Subcutaneous 10 mg / mL Liquid Intramuscular; Intravenous; Subcutaneous 1 % Strip Oral Solution Oral 12.5 mg/5ml Solution / drops; suspension / drops Capsule, coated Oral Solution / drops Nasal 1 g/100mL Liquid Oral 5 mg / 5 mL Capsule, coated Oral 500 mg Spray Nasal Tablet, film coated Lotion Ophthalmic Solution Ophthalmic 2.5 % Solution Ophthalmic Injection, solution, concentrate Intraocular Solution, concentrate Ophthalmic Solution, concentrate Intraocular; Irrigation Solution Conjunctival; Ophthalmic 25 mg Powder Oral 10 mg Tablet 150 mg Tablet 1 mg Syrup Oral 1 mg/5mL Tablet 12 mg Granule, for solution Oral Granule Oral Injection, solution Intraocular; Ophthalmic Injection, solution Intravenous 50 mcg/ml Injection, solution Intravenous; Intravenous bolus 50 mcg/ml Injection, solution Parenteral 100 Mikrogramm/ml Injection, solution Parenteral 50 Mikrogramm/ml Tablet Oral 10 mg/1 Injection, solution 50 mcg/ml Liquid Oral Injection, solution Intravenous 0.08 mg/1mL Injection, solution Intravenous 1 mg/1mL Injection, solution Intravenous 100 ug/1mL Injection, solution Intravenous 160 ug/1mL Injection, solution Intravenous 300 ug/1mL Injection, solution Intravenous 40 ug/1mL Injection, solution Intravenous 50 ug/1mL Injection Intramuscular; Intravenous; Subcutaneous 10 mg/1 mL Injection Intramuscular; Intravenous; Subcutaneous 10 mg/1mL Injection Intravenous 100 mg/10mL Injection Intravenous 50 mg/5mL Injection, solution Intramuscular; Intravenous; Subcutaneous 10 mg/1mL Injection, solution Intravenous 10 mg/1mL Powder Not applicable 1 g/1g Solution Ophthalmic 100 mg/1mL Solution Ophthalmic 25 mg/1mL Solution / drops Ophthalmic 100 mg/1mL Solution / drops Ophthalmic 25 mg/1mL Suppository Rectal Solution Intramuscular; Intravenous; Subcutaneous 0.1 mg / mL Solution Intravenous 50 mcg / mL Solution Intramuscular; Intravenous; Subcutaneous 10 mg / 1 mL Tablet Oral Solution Ophthalmic 100.000 mg Solution Conjunctival; Ophthalmic 1.2 mg Liquid Ophthalmic .12 % Solution Ophthalmic 1.2 mg/ml Cloth; kit; suppository Rectal; Topical Suppository Rectal 6.25 mg/1 Ointment Topical 14 % Gel Rectal 0.25 % w/w Suppository Rectal 85.5 % Gel Rectal; Topical Solution Oral 0.1000 g Tablet Oral 15.000 mg Suspension Oral Syrup Oral Suppository Rectal 0.25 % w/w Cloth; cream; kit Topical Solution / drops Ophthalmic Tablet, multilayer, extended release Oral Capsule, liquid filled; kit Oral Solution Nasal; Respiratory (inhalation) 2 mg Syrup Oral 100 mg/5ml Syrup Oral 62.5 mg/5mL Cream Rectal Tablet Oral 750 mg/1 Ointment Topical Spray Nasal 1 g/100mL Kit; tablet; tablet, film coated Oral Tablet Oral 12.5 mg Tablet Oral 10 mg Tablet Oral 5 mg Tablet Oral 5 mg/1 Tablet, film coated Oral 10 mg/1 Suspension Ophthalmic Solution Conjunctival; Ophthalmic Tablet Oral 162.00 mg Tablet Oral 400.000 mg Liquid Oral 2.5 mg/15mL Powder Oral Kit; solution Oral Kit; powder, for solution Oral Ointment Rectal Liquid Nasal 1 mg/100mL Suspension Ophthalmic 1.2 mg Kit; powder; syrup Oral Strip Oral 2.5 mg Tablet, extended release Oral Kit; syrup Oral Tablet, film coated Oral Tablet Oral 30 mg Suspension Oral 1000 mg/1 Kit; suspension Oral Powder, for solution Oral Suspension Conjunctival; Ophthalmic Suspension Intraocular; Ophthalmic Solution Parenteral 10 mg Injection Intravenous 10 mg/1mL Solution / drops; suspension / drops Nasal Spray Nasal 0.0005 g/1mL Spray Nasal 0.004975 g/1mL Solution / drops Ophthalmic Capsule Oral 10.00 mg Tablet, sugar coated Oral 30 mg Capsule Oral 250.000 mg Liquid Ophthalmic Liquid Ophthalmic 100 mg/1ml Tablet Syrup Nasal Tablet, sugar coated Oral Lozenge Oral Solution Nasal Syrup Liquid Ophthalmic 0.9 mg/1ml Elixir Tablet, film coated Nasal - Prices
Unit description Cost Unit Mydfrin 2.5% Solution 5ml Bottle 37.1USD bottle Neo-synephrine 10 mg/ml amp 5.68USD ml Mydfrin 2.5% eye drops 5.28USD ml Phenylephrine 10 mg/ml vial 3.0USD ml Phenylephrine 2.5% eye drop 2.09USD ml Neofrin 10% eye drops 1.93USD ml Ak-dilate 10% eye drops 1.34USD ml Phenylephrine hcl crystals 1.34USD g Phenylephrine 10% eye drops 1.25USD ml Phenylephrine-ns 0.8 mg/10 ml 1.2USD ml Phenylephrine-ns 0.4 mg/10 ml 1.17USD ml Mydfrin 2.5 % Solution 1.09USD ml Neofrin 2.5% eye drops 0.6USD ml Ak-dilate 2.5% eye drops 0.45USD ml Neo-synephrine 0.25% drops 0.36USD ml Hemorrhoidal suppository 0.28USD suppository Neo-synephrine 12 hour spray 0.28USD ml Neo-synephrine 1% drops 0.26USD ml Sudafed pe 10 mg tablet 0.25USD tablet Neo-synephrine 0.5% drops 0.23USD ml Little noses decon nose drp 0.22USD ml Wal-phed pe 10 mg tablet 0.22USD tablet Tur-bi-kal nose drops 0.21USD ml Industrial 0.12% eye drops 0.17USD ml Ephrine 1% nose drops 0.15USD ml Phenylephrine 10 mg tablet 0.08USD tablet Rhinall 0.25% nose drops 0.07USD ml Non-pseudo sinus decongest tablet 0.05USD tablet Pv nasal decongestant 5 mg tablet 0.03USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8173707 Yes 2012-05-08 2024-01-30 US US9278101 Yes 2016-03-08 2024-01-30 US US8586633 Yes 2013-11-19 2024-01-30 US US9066856 Yes 2015-06-30 2034-04-23 US US8859623 No 2014-10-14 2033-11-14 US US9399040 Yes 2016-07-26 2024-01-30 US US9486406 Yes 2016-11-08 2034-04-23 US US9855246 No 2018-01-02 2033-10-23 US US11213480 No 2016-09-26 2036-09-26 US US11471400 No 2016-08-05 2036-08-05 US US11398306 No 2011-07-15 2031-07-15 US US10839960 No 2020-11-17 2031-07-15 US US11839487 No 2011-07-15 2031-07-15 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 140-145 °C Not Available water solubility Freely soluble in water Not Available logP -0.31 HANSCH,C ET AL. (1995) pKa 8.97 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 22.0 mg/mL ALOGPS logP -0.69 ALOGPS logP -0.07 Chemaxon logS -0.88 ALOGPS pKa (Strongest Acidic) 9.07 Chemaxon pKa (Strongest Basic) 9.69 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 52.49 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 47.25 m3·mol-1 Chemaxon Polarizability 18.2 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9943 Blood Brain Barrier - 0.9115 Caco-2 permeable - 0.7294 P-glycoprotein substrate Substrate 0.5308 P-glycoprotein inhibitor I Non-inhibitor 0.9527 P-glycoprotein inhibitor II Non-inhibitor 0.9109 Renal organic cation transporter Non-inhibitor 0.856 CYP450 2C9 substrate Non-substrate 0.7882 CYP450 2D6 substrate Non-substrate 0.7756 CYP450 3A4 substrate Non-substrate 0.6946 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9646 CYP450 2D6 inhibitor Non-inhibitor 0.923 CYP450 2C19 inhibitor Non-inhibitor 0.9088 CYP450 3A4 inhibitor Non-inhibitor 0.858 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9594 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.8841 Biodegradation Ready biodegradable 0.7647 Rat acute toxicity 2.6480 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.5164 hERG inhibition (predictor II) Non-inhibitor 0.8717
Spectra
- Mass Spec (NIST)
- Download (8.12 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 141.2056449 predictedDarkChem Lite v0.1.0 [M-H]- 134.06697 predictedDeepCCS 1.0 (2019) [M+H]+ 142.1971449 predictedDarkChem Lite v0.1.0 [M+H]+ 136.6397 predictedDeepCCS 1.0 (2019) [M+Na]+ 141.4022449 predictedDarkChem Lite v0.1.0 [M+Na]+ 145.42511 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Martinez-Salas SG, Campos-Peralta JM, Pares-Hipolito J, Gallardo-Ortiz IA, Ibarra M, Villalobos-Molina R: Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. Auton Autacoid Pharmacol. 2007 Jul;27(3):137-42. [Article]
- Tomiyama Y, Kobayashi K, Tadachi M, Kobayashi S, Inada Y, Kobayashi M, Yamazaki Y: Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter. Eur J Pharmacol. 2007 Nov 14;573(1-3):201-5. Epub 2007 Jul 6. [Article]
- Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328]
- FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [Link]
- FDA Approved Drug Products: Phenylephrine Ophthalmic Solution [Link]
- FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
- Specific Function
- dopamine binding
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328]
- FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [Link]
- FDA Approved Drug Products: Phenylephrine Ophthalmic Solution [Link]
- FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1D
- Uniprot ID
- P25100
- Uniprot Name
- Alpha-1D adrenergic receptor
- Molecular Weight
- 60462.205 Da
References
- Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328]
- FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [Link]
- FDA Approved Drug Products: Phenylephrine Ophthalmic Solution [Link]
- FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:18391214, PubMed:20493079, PubMed:24169519, PubMed:8316221). Preferentially oxidizes serotonin (PubMed:20493079, PubMed:24169519). Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline (By similarity)
- Specific Function
- aliphatic amine oxidase activity
- Gene Name
- MAOA
- Uniprot ID
- P21397
- Uniprot Name
- Amine oxidase [flavin-containing] A
- Molecular Weight
- 59681.27 Da
References
- Raffel DM, Corbett JR, del Rosario RB, Gildersleeve DL, Chiao PC, Schwaiger M, Wieland DM: Clinical evaluation of carbon-11-phenylephrine: MAO-sensitive marker of cardiac sympathetic neurons. J Nucl Med. 1996 Dec;37(12):1923-31. [Article]
- Raffel DM, Corbett JR, del Rosario RB, Mukhopadhyay SK, Gildersleeve DL, Rose P, Wieland DM: Sensitivity of [11C]phenylephrine kinetics to monoamine oxidase activity in normal human heart. J Nucl Med. 1999 Feb;40(2):232-8. [Article]
- FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [Link]
- FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amines such as neurotransmitters, and exogenous amines including the tertiary amine, neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), with concomitant reduction of oxygen to hydrogen peroxide and participates in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924). Preferentially degrades benzylamine and phenylethylamine (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924)
- Specific Function
- aliphatic amine oxidase activity
- Gene Name
- MAOB
- Uniprot ID
- P27338
- Uniprot Name
- Amine oxidase [flavin-containing] B
- Molecular Weight
- 58762.475 Da
References
- Gelotte CK, Zimmerman BA: Pharmacokinetics, safety, and cardiovascular tolerability of phenylephrine HCl 10, 20, and 30 mg after a single oral administration in healthy volunteers. Clin Drug Investig. 2015 Sep;35(9):547-58. doi: 10.1007/s40261-015-0311-9. [Article]
- FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [Link]
- FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic monoamines (neurotransmitters such as dopamine, norepinephrine and serotonin) and phenolic and catechol drugs
- Specific Function
- amine sulfotransferase activity
- Gene Name
- SULT1A3
- Uniprot ID
- P0DMM9
- Uniprot Name
- Sulfotransferase 1A3
- Molecular Weight
- 34195.96 Da
References
- Bairam AF, Rasool MI, Alherz FA, Abunnaja MS, El Daibani AA, Gohal SA, Alatwi ES, Kurogi K, Liu MC: Impact of SULT1A3/SULT1A4 genetic polymorphisms on the sulfation of phenylephrine and salbutamol by human SULT1A3 allozymes. Pharmacogenet Genomics. 2019 Jul;29(5):99-105. doi: 10.1097/FPC.0000000000000371. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- Konstandi M, Kostakis D, Harkitis P, Johnson EO, Marselos M, Adamidis K, Lang MA: Benzo(alpha)pyrene-induced up-regulation of CYP1A2 gene expression: role of adrenoceptor-linked signaling pathways. Life Sci. 2006 Jun 20;79(4):331-41. Epub 2006 Feb 28. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 13, 2024 03:58