Identification
- Summary
Promethazine is a first-generation antihistamine used for the treatment of allergic conditions, nausea and vomiting, and motion sickness.
- Brand Names
- Phenadoz, Phenergan, Promethazine DM, Promethegan
- Generic Name
- Promethazine
- DrugBank Accession Number
- DB01069
- Background
Promethazine, originally known as 3,277 R.P., is an N-dimethylaminopropyl derivative of phenothiazine that was developed in France in 1946.1 Promethazine antagonizes a variety of receptors, allowing it to be used for a number of indications including allergic reactions, pain, sedation, nausea, and vomiting.2,8,9,7,10
Promethazine was granted FDA approval before 29 March 1951.11,12
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Promethazine (DB01069)
- Weight
- Average: 284.419
Monoisotopic: 284.13471934 - Chemical Formula
- C17H20N2S
- Synonyms
- (2-dimethylamino-2-methyl)ethyl-N-dibenzoparathiazine
- 10-(2-Dimethylaminopropyl)phenothiazine
- 10-[2-(dimethylamino)propyl]phenothiazine
- N-(2'-dimethylamino-2'-methyl)ethylphenothiazine
- N,N,alpha-trimethyl-10H-phenothiazine-10-ethanamine
- N,N,α-trimethyl-10H-phenothiazine-10-ethanamine
- Proazamine
- Prometazina
- Promethazine
- Promethazinum
- External IDs
- Lilly 1516
Pharmacology
- Indication
Promethazine tablets and suppositories are indicated to treat rhinitis, allergic conjunctivitis, allergic reactions to blood or plasma, dermographism, anaphylactic reactions, sedation, nausea, vomiting, pain, motion sickness, and allergic skin reactions.2,12 Promethazine cough syrup with phenylephrine and codeine is indicated to relieve cough and upper respiratory symptoms, and nasal congestion associated with allergy or the common cold.13
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Allergic conjunctivitis •••••••••••• ••••••••••• Management of Allergic urticaria •••••••••••• •••••••••••• •••••• Adjunct therapy in treatment of Anaphylactic reaction •••••••••••• •••••••••• •••••••••• ••••••••• ••••••••••• Used in combination for symptomatic treatment of Cough Combination Product in combination with: Dextromethorphan (DB00514) •••••••••••• Used in combination for symptomatic treatment of Cough Combination Product in combination with: Codeine (DB00318) •••••••••••• - 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
Promethazine is is a histamine H1 antagonist that can be used for it's ability to induce sedation, reduce pain, and treat allergic reactions.12 Promethazine's effects generally last 4-6h but can last up to 12h.12 Patients should be counselled regarding CNS and respiratory depression, reduce seizure threshold, and bone marrow depression.12
- Mechanism of action
Promethazine is a an antagonist of histamine H1, post-synaptic mesolimbic dopamine, alpha adrenergic, muscarinic, and NMDA receptors.2,8,9 The antihistamine action is used to treat allergic reactions.7 Antagonism of muscarinic and NMDA receptors contribute to its use as a sleep aid, as well as for anxiety and tension.9 Antagonism of histamine H1, muscarinic, and dopamine receptors in the medullary vomiting center make promethazine useful in the treatment of nausea and vomiting.10
Target Actions Organism AHistamine H1 receptor antagonistHumans UDopamine D2 receptor antagonistHumans UMuscarinic acetylcholine receptor M1 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M3 antagonistHumans UMuscarinic acetylcholine receptor M4 antagonistHumans UMuscarinic acetylcholine receptor M5 antagonistHumans UAlpha adrenergic receptor antagonistHumans UCalmodulin inhibitorHumans UHistamine H2 receptor antagonistHumans UP2 Purinoceptors inhibitorUVoltage-gated sodium channel alpha subunit inhibitorHumans UVoltage-gated Potassium Channels inducer- Absorption
A 25mg dose of intramuscular promethazine reaches a Cmax of 22ng/mL.4 Intravenous promethazine reaches a Cmax of 10.0ng/mL, with a Tmax of 4-10h, and an AUC of 14,466ng*h/mL.4 Oral promethazine is only 25% bioavailable due to first pass metabolism.4 Oral promethazine reaches a Cmax of 2.4-18.0ng/mL, with a Tmax of 1.5-3h, and an AUC of 11,511ng*h/mL.4
- Volume of distribution
The volume of distribution of promethazine is approximately 970L or 30L/kg.4
- Protein binding
Promethazine is 93% protein bound in serum,5 mostly to albumin.6
- Metabolism
Promethazine is predominantly metabolized to promethazine sulfoxide, and minorly to desmethylpromethazine and a hydroxy metabolite.3,4 Hydroxylation of promethazine is predominantly mediated by CYP2D6.3
Hover over products below to view reaction partners
- Route of elimination
An intravenous dose of promethazine is 0.64% eliminated in the urine as the unchanged parent drug, 0.02-2.02% in the urine as desmethylpromethazine, 10% in the urine as promethazine sulfoxide.4
- Half-life
The elimination half life of promethazine is approximately 12-15h.4
- Clearance
The intravenous clearance of promethazine is approximately 1.14L/min.4 The renal clearance of promethazine is 5.9mL/min and the renal clearance of promethazine sulfoxide is 90.4mL/min.4
- Adverse Effects
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The intraperitoneal LD50 in rats is 170mg/kg and in mice is 160mg/kg.14 The subcutaneous LD50 in rats is 400mg/kg and in mice is 240mg/kg.14 The oral LD50 in mice is 255mg/kg.14
Patients experiencing an overdose of promethazine may present with mild central nervous system and cardiovascular depression, hypotension, respiratory depression, unconciousness, hyperreflexia, hypertonia, ataxia, athetosis, extensor-plantar reflexes, convulsions, dry mouth, flushing, gastrointestinal symptoms, and fixed, dilated pupils.12 Treat overdoses with symptomatic and supportive treatment, which may include activated charcoal, sodium sulfate, magnesium sulfate, controlled ventilation, diazepam, intravenous fluids, vasopressors, norepinephrine, phenylephrine, anticholinergic antiparkinsonian agents, diphenhydramine, barbiturates, or oxygen.12
- Pathways
Pathway Category Promethazine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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 CNS depression can be increased when Promethazine is combined with 1,2-Benzodiazepine. Abacavir Abacavir may decrease the excretion rate of Promethazine which could result in a higher serum level. Abametapir The serum concentration of Promethazine can be increased when it is combined with Abametapir. Abatacept The metabolism of Promethazine can be increased when combined with Abatacept. Abiraterone The metabolism of Promethazine can be decreased when combined with Abiraterone. - Food Interactions
- Avoid alcohol. Alcohol may increase the sedation caused by promethazine.
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 Promethazine hydrochloride R61ZEH7I1I 58-33-3 XXPDBLUZJRXNNZ-UHFFFAOYSA-N Promethazine teoclate S5PUP23U26 17693-51-5 YCXARMXCESBEDS-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Avomine / Fargan / Farganesse / Lergigan / Prothiazine / Receptozine / Romergan
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Phenergan Suppository 12.5 mg/1 Rectal Wyeth Ltd. 1951-05-01 2008-06-30 US 
Phenergan Tablet 12.5 mg/1 Oral Wyeth Ltd. 1951-05-01 2008-06-03 US Phenergan Suppository 50 mg/1 Rectal Wyeth Ltd. 1951-05-01 2008-06-30 US Phenergan Tablet 50 mg/1 Oral Wyeth Ltd. 1951-05-01 2008-06-30 US Phenergan Suppository 25 mg/1 Rectal Wyeth Ltd. 1951-05-01 2008-06-30 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Phenadoz Suppository 25 mg/1 Rectal Actavis Pharma, Inc. 2015-02-17 2022-01-30 US Phenadoz Suppository 25 mg/1 Rectal A-S Medication Solutions 2015-02-17 Not applicable US Phenadoz Suppository 12.5 mg/1 Rectal Paddock Laboratories, Inc. 2003-06-24 2016-11-30 US Phenadoz Suppository 12.5 mg/1 Rectal Actavis Pharma, Inc. 2015-03-16 2021-02-28 US Phenadoz Suppository 12.5 mg/1 Rectal Pd Rx Pharmaceuticals, Inc. 2003-06-24 2018-02-08 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image AXCEL PROMETHAZINE-5 SYRUP 5 mg/5 ml Syrup 5 mg/5ml Oral KOTRA PHARMA MARKETING 1998-11-12 Not applicable Singapore 
Histantil Tab 25mg Tablet 25 mg Oral Pharmascience Inc 1983-12-31 Not applicable Canada 
Histantil Tab 50mg Tablet 50 mg Oral Pharmascience Inc 1983-12-31 Not applicable Canada Phenergan 50 Tablet 50 mg Oral Columbia Laboratories 1996-12-31 2002-07-17 Canada Phenergan Cream 2% Cream 2 % Topical Rhone Poulenc Rorer 1993-12-31 1997-08-13 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ARTU 100 ML SURUP Promethazine hydrochloride (5 mg/5ml) + Sodium benzoate (5 mg/5ml) + Ephedrine hydrochloride (5 mg/5ml) + Potassium guaiacolsulfonate (175 mg/5ml) Syrup Oral GÜNSA GÜNEY İLAÇ VE HAMMADDELER SAN. VE TİC. A.Ş. 1972-03-16 Not applicable Turkey 
BEACODYL LINCTUS Promethazine hydrochloride (3.6 mg/5ml) + Codeine phosphate (9 mg/5ml) Elixir Oral BEACONS PHARMACEUTICALS PTE. LTD. 1994-03-25 Not applicable Singapore BERLIFED Promethazine hydrochloride (5 mg/5mL) + Ammonium chloride (135 mg/5mL) + Pseudoephedrine hydrochloride (15 mg/5mL) + Sodium citrate dihydrate (57 mg/mL) Syrup Oral Berlico Mulia Farma 2017-05-29 2027-02-10 Indonesia 
COPHADYL COUGH LINCTUS Promethazine hydrochloride (3.6 mg/5ml) + Codeine phosphate (9 mg/5ml) Elixir Oral ICM PHARMA PTE. LTD. 1996-12-14 Not applicable Singapore COPHADYL-E COUGH LINCTUS Promethazine hydrochloride (3.6 mg/5ml) + Codeine phosphate (9 mg/5ml) + Ephedrine hydrochloride (6 mg/5ml) Elixir Oral ICM PHARMA PTE. LTD. 1996-12-28 Not applicable Singapore - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Meperidine Hcl and Promethazine Hcl Promethazine hydrochloride (25 mg/1) + Meperidine hydrochloride (50 mg/1) Capsule Oral Physicians Total Care, Inc. 2004-09-03 2013-01-15 US Meperidine Hydrochloride and Promethazine Hydrochloride Promethazine hydrochloride (25 mg/1) + Meperidine hydrochloride (50 mg/1) Capsule Oral Eci Pharmaceuticals Llc 2013-02-19 2018-06-30 US Promethazine HCl Promethazine hydrochloride (0.625 mg/1mL) Injection, solution Intravenous Cantrell Drug Company 2014-05-27 Not applicable US Promethazine HCl Promethazine hydrochloride (1 mg/1mL) Injection, solution Intravenous Cantrell Drug Company 2014-05-27 2017-12-06 US Promethazine HCl Promethazine hydrochloride (0.5 mg/1mL) Injection, solution Intravenous Cantrell Drug Company 2014-05-29 Not applicable US
Categories
- ATC Codes
- R06AD52 — Promethazine, combinations
- R06AD — Phenothiazine derivatives
- R06A — ANTIHISTAMINES FOR SYSTEMIC USE
- R06 — ANTIHISTAMINES FOR SYSTEMIC USE
- R — RESPIRATORY SYSTEM
- D04AA — Antihistamines for topical use
- D04A — ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
- D04 — ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
- D — DERMATOLOGICALS
- V03AB — Antidotes
- V03A — ALL OTHER THERAPEUTIC PRODUCTS
- V03 — ALL OTHER THERAPEUTIC PRODUCTS
- V — VARIOUS
- Drug Categories
- Acid Reducers
- Agents producing tachycardia
- Agents that reduce seizure threshold
- Amines
- Anti-Allergic Agents
- Anticholinergic Agents
- Antidepressive Agents
- Antidotes
- Antihistamines for Systemic Use
- Antihistamines for Topical Use
- Antipruritics
- Antipruritics, Incl. Antihistamines, Anesthetics, Etc.
- Antipsychotic Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dermatologicals
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs causing inadvertant photosensitivity
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H2 Antagonists
- Miscellaneous Anxiolytics Sedatives and Hypnotics
- Muscarinic Antagonists
- Neurotoxic agents
- Neurotransmitter Agents
- P-glycoprotein inhibitors
- Phenothiazine Derivatives
- Phenothiazines
- Photosensitizing Agents
- Potential QTc-Prolonging Agents
- Propylamines
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin Agents
- Serotonin Modulators
- Sulfur Compounds
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzothiazines
- Sub Class
- Phenothiazines
- Direct Parent
- Phenothiazines
- Alternative Parents
- Alkyldiarylamines / Diarylthioethers / Benzenoids / 1,4-thiazines / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Alkyldiarylamine / Amine / Aromatic heteropolycyclic compound / Aryl thioether / Azacycle / Benzenoid / Diarylthioether / Hydrocarbon derivative / Organic nitrogen compound / Organonitrogen compound
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- phenothiazines, tertiary amine (CHEBI:8461)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- FF28EJQ494
- CAS number
- 60-87-7
- InChI Key
- PWWVAXIEGOYWEE-UHFFFAOYSA-N
- InChI
- InChI=1S/C17H20N2S/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3
- IUPAC Name
- dimethyl[1-(10H-phenothiazin-10-yl)propan-2-yl]amine
- SMILES
- CC(CN1C2=CC=CC=C2SC2=CC=CC=C12)N(C)C
References
- Synthesis Reference
- US2530451
- General References
- HALPERN BN, HAMBURGER J: A new synthetic anti-histamine substance derived from phenothiazine; phenergan, 3,277 R.P. Can Med Assoc J. 1948 Oct;59(4):322-6. [Article]
- Southard BT, Al Khalili Y: Promethazine . [Article]
- Nakamura K, Yokoi T, Inoue K, Shimada N, Ohashi N, Kume T, Kamataki T: CYP2D6 is the principal cytochrome P450 responsible for metabolism of the histamine H1 antagonist promethazine in human liver microsomes. Pharmacogenetics. 1996 Oct;6(5):449-57. [Article]
- Taylor G, Houston JB, Shaffer J, Mawer G: Pharmacokinetics of promethazine and its sulphoxide metabolite after intravenous and oral administration to man. Br J Clin Pharmacol. 1983 Mar;15(3):287-93. doi: 10.1111/j.1365-2125.1983.tb01501.x. [Article]
- Cantisani C, Ricci S, Grieco T, Paolino G, Faina V, Silvestri E, Calvieri S: Topical promethazine side effects: our experience and review of the literature. Biomed Res Int. 2013;2013:151509. doi: 10.1155/2013/151509. Epub 2013 Nov 19. [Article]
- He LL, Wang ZX, Wang YX, Liu XP, Yang YJ, Gao YP, Wang X, Liu B, Wang X: Studies on the interaction between promethazine and human serum albumin in the presence of flavonoids by spectroscopic and molecular modeling techniques. Colloids Surf B Biointerfaces. 2016 Sep 1;145:820-829. doi: 10.1016/j.colsurfb.2016.06.001. Epub 2016 Jun 2. [Article]
- Authors unspecified: Promethazine . [Article]
- Smith HS, Cox LR, Smith BR: Dopamine receptor antagonists. Ann Palliat Med. 2012 Jul;1(2):137-42. doi: 10.3978/j.issn.2224-5820.2012.07.09. [Article]
- Adolph O, Koster S, Georgieff M, Georgieff EM, Moulig W, Fohr KJ: Promethazine inhibits NMDA-induced currents - new pharmacological aspects of an old drug. Neuropharmacology. 2012 Aug;63(2):280-91. doi: 10.1016/j.neuropharm.2012.03.006. Epub 2012 Apr 7. [Article]
- Flake ZA, Linn BS, Hornecker JR: Practical selection of antiemetics in the ambulatory setting. Am Fam Physician. 2015 Mar 1;91(5):293-6. [Article]
- AVERY JL: Treatment of enterobiasis with one oral dose of promethazine hydrochloride. J Am Med Assoc. 1956 Jun 23;161(8):681-3. doi: 10.1001/jama.1956.02970080011004. [Article]
- FDA Approved Drug Products: Phenergran Promethazine Oral Tablets (Discontinued) [Link]
- FDA Approved Drug Products: Promethazine with Phenylephrine and Codeine Oral Syrup [Link]
- Cayman Chemical: Promethazine MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0015202
- KEGG Drug
- D00494
- KEGG Compound
- C07404
- PubChem Compound
- 4927
- PubChem Substance
- 46507798
- ChemSpider
- 4758
- BindingDB
- 50017696
- 8745
- ChEBI
- 8461
- ChEMBL
- CHEMBL643
- Therapeutic Targets Database
- DAP000334
- PharmGKB
- PA451128
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Promethazine
- FDA label
- Download (93.4 KB)
- MSDS
- Download (74.8 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Basic Science Vestibular 1 4 Completed Prevention Nausea / Post Operative Nausea and Vomiting (PONV) 1 4 Completed Prevention Post Operative Nausea and Vomiting (PONV) 1 4 Completed Treatment Aggression / Agitation / Psychiatric Emergency 1 4 Completed Treatment Chronic Hepatitis C Infection With Hepatic Coma / Hepatic Failure / Hepatic Impairment 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Aidarex Pharmacuticals LLC
- Amerisource Health Services Corp.
- Apotheca Inc.
- A-S Medication Solutions LLC
- Atlantic Biologicals Corporation
- Baxter International Inc.
- Bioniche Pharma
- Blenheim Pharmacal
- Bryant Ranch Prepack
- C.O. Truxton Inc.
- Cadila Healthcare Ltd.
- Caraco Pharmaceutical Labs
- Cardinal Health
- Carlisle Laboratories Inc.
- Century Pharmaceuticals Inc.
- Clint Pharmaceutical Inc.
- Comprehensive Consultant Services Inc.
- Consolidated Midland Corp.
- Corepharma LLC
- Dee Stevens and Son Feeder
- DHHS Program Support Center Supply Service Center
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Ebewe Pharma
- G & W Labs
- General Injectables and Vaccines Inc.
- Global Pharmaceuticals
- Goldline Laboratories Inc.
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Hi Tech Pharmacal Co. Inc.
- Hikma Pharmaceuticals
- Hospira Inc.
- Impax Laboratories Inc.
- Innoviant Pharmacy Inc.
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Keltman Pharmaceuticals Inc.
- KVK-Tech Inc.
- Lake Erie Medical and Surgical Supply
- Lark Pharmaceuticals Inc.
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Mallinckrodt Inc.
- Martica Enterprises Inc.
- Martin Surgical Supply
- Mckesson Corp.
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Neuman Distributors Inc.
- Nubenco Enterprises Inc.
- Nucare Pharmaceuticals Inc.
- Paddock Labs
- Palmetto Pharmaceuticals Inc.
- Patient First Corp.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Perrigo Co.
- Pharmaceutical Association
- Pharmacy Service Center
- Pharmedix
- Pharmpak Inc.
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Prescript Pharmaceuticals
- Qualitest
- Rebel Distributors Corp.
- Redpharm Drug
- Remedy Repack
- Resource Optimization and Innovation LLC
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- St Mary's Medical Park Pharmacy
- Stat Rx Usa
- Sun Pharmaceutical Industries Ltd.
- Taro Pharmaceuticals USA
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- United Research Laboratories Inc.
- Vangard Labs Inc.
- Vintage Pharmaceuticals Inc.
- Watson Pharmaceuticals
- West-Ward Pharmaceuticals
- Wockhardt Ltd.
- Zydus Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral Cream Topical 2 % Solution Oral 20 mg/mL Elixir Oral 9 mg/5ml Injection Intramuscular; Intravenous 50 mg Syrup Oral 9 mg/5ml Cream Topical Injection, solution Parenteral 50 MG/2ML Syrup Oral 100 mg/100ml Tablet, coated 25 MG Ointment Topical Stick Extracorporeal Capsule Oral Syrup Oral 5 mg/5ml Injection, solution Intramuscular 50 mg/1mL Suppository Rectal 50 mg/1 Tablet Oral 50 mg Solution Intramuscular; Intravenous 25 mg / mL Syrup Oral 10 mg / 5 mL Tablet Oral 10 mg / tab Tablet Oral 25 mg / tab Tablet Oral 50 mg / tab Tablet, film coated Oral Syrup Oral 10 mg/5ml Tablet, coated Solution Oral 100 ml Solution Oral 30 ml Solution Oral 50 ml Tablet, film coated Oral 10 MG Tablet, film coated Oral 100 MG Tablet, film coated Oral 25 MG Tablet, film coated Oral 50 MG Tablet, film coated Oral 75 MG Injection Intramuscular 50 mg/1mL Injection Intramuscular; Intravenous 25 mg/1mL Injection Intramuscular; Intravenous 50 mg/1mL Injection, solution Intravenous 0.5 mg/1mL Injection, solution Intravenous 0.625 mg/1mL Injection, solution Intravenous 1 mg/1mL Liquid Intramuscular; Intravenous 28.2 mg / mL Injection Intramuscular Solution Oral Injection Intramuscular 25 mg/1mL Injection, solution Intramuscular 25 mg/1 Injection, solution Intramuscular; Intravenous 25 mg/1mL Injection, solution Intramuscular; Intravenous 50 mg/1mL Powder Not applicable 1 g/1g Solution Oral 6.25 mg/5mL Suppository Rectal 12.5 mg/1 Suppository Rectal 25 mg/1 Syrup Oral 6.25 mg/5mL Tablet Oral 12.5 mg/1 Tablet Oral 25 mg/1 Tablet Oral 25 mg/301 Tablet Oral 50 mg/1 Liquid Intramuscular; Intravenous 25 mg / mL Liquid Oral Syrup Oral Syrup Oral 1 mg/ml Tablet, sugar coated Oral 25 MG Emulsion Topical Pill Syrup Oral Elixir Oral Elixir Oral 10.0 mg/5ml Elixir Oral 10 mg/5ml Tablet Oral 25 mg Elixir Oral 10 mg/5ml Elixir Oral 5.0 MG/5ml Elixir Oral 5 mg/5ml Solution 5 mg/5ml - Prices
Unit description Cost Unit Promethegan 12 50 mg Suppository Box 101.64USD box Phenergan 12 50 mg Suppository Box 80.16USD box Phenergan 12 25 mg Suppository Box 62.59USD box Promethegan 12 25 mg Suppository Box 62.27USD box Promethazine HCl 12 50 mg Suppository Box 60.94USD box Phenergan 12 12.5 mg Suppository Box 54.58USD box Phenergan 25 mg suppository 8.32USD suppository Promethegan 50 mg suppository 8.14USD suppository Phenergan 12.5 mg suppository 7.94USD suppository Phenergan 50 mg suppository 7.39USD suppository Promethazine 50 mg suppository 4.88USD suppository Promethegan 25 mg suppository 4.62USD suppository Phenadoz 25 mg suppository 4.45USD suppository Promethazine 25 mg suppository 4.32USD suppository Promethegan 12.5 mg suppository 4.02USD suppository Promethazine HCl 12.5 mg Suppository 4.0USD suppository Phenadoz 12.5 mg suppository 3.89USD suppository Phenergan 25 mg/ml ampul 3.84USD ml Promethazine 12.5 mg suppository 3.82USD suppository Phenergan 50 mg/ml ampul 3.68USD ml Promethazine HCl 50 mg/ml Solution 1ml Ampule 2.8USD ampule Promethazine 50 mg/ml ampul 2.25USD ml Promethazine hcl powder 2.14USD g Promethazine 25 mg/ml ampul 1.1USD ml Promethazine 25 mg/ml 1.06USD ml Promethazine HCl 50 mg tablet 0.81USD tablet Promethazine 50 mg tablet 0.78USD tablet Promethazine HCl 25 mg tablet 0.73USD tablet Phenergan 25 mg tablet 0.62USD tablet Promethazine 25 mg tablet 0.51USD tablet Promethazine 12.5 mg tablet 0.49USD tablet Promethazine-DM 6.25-15 mg/5ml Syrup 0.18USD ml Promethazine HCl 6.25 mg/5ml Syrup 0.11USD ml Promethazine VC Plain 6.25-5 mg/5ml Syrup 0.09USD ml Promethazine-Codeine 6.25-10 mg/5ml Syrup 0.06USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 60 °C PhysProp boiling point (°C) 190-192 °C at 3.00E+00 mm Hg PhysProp water solubility 15.6 mg/L (at 24 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 4.81 HANSCH,C ET AL. (1995) logS -4.26 ADME Research, USCD pKa 9.1 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 0.0245 mg/mL ALOGPS logP 4.52 ALOGPS logP 4.29 Chemaxon logS -4.1 ALOGPS pKa (Strongest Basic) 9.05 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 6.48 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 88.5 m3·mol-1 Chemaxon Polarizability 32.38 Å3 Chemaxon Number of Rings 3 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
Property Value Probability Human Intestinal Absorption + 0.9832 Blood Brain Barrier + 0.9855 Caco-2 permeable + 0.8867 P-glycoprotein substrate Substrate 0.8157 P-glycoprotein inhibitor I Inhibitor 0.8408 P-glycoprotein inhibitor II Non-inhibitor 0.6473 Renal organic cation transporter Inhibitor 0.5156 CYP450 2C9 substrate Non-substrate 0.7736 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.5338 CYP450 1A2 substrate Inhibitor 0.9107 CYP450 2C9 inhibitor Non-inhibitor 0.9341 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8308 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.567 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.9088 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6959 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9786 hERG inhibition (predictor II) Inhibitor 0.7661
Spectra
- Mass Spec (NIST)
- Download (7.88 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 170.6447147 predictedDarkChem Lite v0.1.0 [M-H]- 157.82068 predictedDeepCCS 1.0 (2019) [M+H]+ 170.6102147 predictedDarkChem Lite v0.1.0 [M+H]+ 160.1787 predictedDeepCCS 1.0 (2019) [M+Na]+ 170.5799147 predictedDarkChem Lite v0.1.0 [M+Na]+ 166.27182 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Suzuki A, Yasui-Furukori N, Mihara K, Kondo T, Furukori H, Inoue Y, Kaneko S, Otani K: Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol. Ther Drug Monit. 2003 Apr;25(2):192-6. [Article]
- Smith BN, Armstrong WE: Histamine enhances the depolarizing afterpotential of immunohistochemically identified vasopressin neurons in the rat supraoptic nucleus via H1-receptor activation. Neuroscience. 1993 Apr;53(3):855-64. [Article]
- Miller RA, Tu AT: Factors in snake venoms that increase capillary permeability. J Pharm Pharmacol. 1989 Nov;41(11):792-4. [Article]
- Claro E, Arbones L, Garcia A, Picatoste F: Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex. Eur J Pharmacol. 1986 Apr 16;123(2):187-96. [Article]
- Ikeda H, Kubo N, Nakamura A, Harada N, Minamino M, Yamashita T: Histamine-induced calcium released from cultured human mucosal microvascular endothelial cells from nasal inferior turbinate. Acta Otolaryngol. 1997 Nov;117(6):864-70. [Article]
- Paton DM, Webster DR: Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Golembiewski JA, O'Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Golembiewski JA, O'Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Golembiewski JA, O'Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Golembiewski JA, O'Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM4
- Uniprot ID
- P08173
- Uniprot Name
- Muscarinic acetylcholine receptor M4
- Molecular Weight
- 53048.65 Da
References
- Golembiewski JA, O'Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM5
- Uniprot ID
- P08912
- Uniprot Name
- Muscarinic acetylcholine receptor M5
- Molecular Weight
- 60073.205 Da
References
- Golembiewski JA, O'Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific 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) prot...
Components:
References
- Southard BT, Al Khalili Y: Promethazine . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Titin binding
- Specific Function
- Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
- Gene Name
- CALM1
- Uniprot ID
- P0DP23
- Uniprot Name
- Calmodulin
- Molecular Weight
- 16837.47 Da
References
- Cohen ME, Sharp GW, Donowitz M: Suggestion of a role for calmodulin and phosphorylation in regulation of rabbit ileal electrolyte transport: effects of promethazine. Am J Physiol. 1986 Nov;251(5 Pt 1):G710-7. [Article]
- Scott JA, Khaw BA, Fallon JT, Locke E, Rabito CA, Peto CA, Homcy CJ: The effect of phenothiazines upon maintenance of membrane integrity in the cultured myocardial cell. J Mol Cell Cardiol. 1986 Dec;18(12):1243-54. [Article]
- Lohr KM, Feix JB, Kurth C: Chlorpromazine inhibits neutrophil chemotaxis beyond the chemotactic receptor-ligand interaction. J Infect Dis. 1984 Nov;150(5):643-52. [Article]
- DiPaola M, Keith CH, Feldman D, Tycko B, Maxfield FR: Loss of alpha 2-macroglobulin and epidermal growth factor surface binding induced by phenothiazines and naphthalene sulfonamides. J Cell Physiol. 1984 Feb;118(2):193-202. [Article]
- Luchowski EM, Yousif F, Triggle DJ, Maurer SC, Sarmiento JG, Janis RA: Effects of metal cations and calmodulin antagonists on [3H] nitrendipine binding in smooth and cardiac muscle. J Pharmacol Exp Ther. 1984 Sep;230(3):607-13. [Article]
- Baig AM, Katyara P, Rajabali MN, Khaleeq A, Nazim F, Lalani S: Neuroleptic Drug Targets a Brain-Eating Amoeba: Effects of Promethazine on Neurotropic Acanthamoeba castellanii. ACS Chem Neurosci. 2019 Jun 19;10(6):2868-2876. doi: 10.1021/acschemneuro.9b00100. Epub 2019 May 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and diff...
- Gene Name
- HRH2
- Uniprot ID
- P25021
- Uniprot Name
- Histamine H2 receptor
- Molecular Weight
- 40097.65 Da
References
- Dick W, Lorenz W, Heintz D, Sitter H, Doenicke A: [Histamine release during induction of combination anesthesia using nalbuphine or fentanyl. Modulation of the reaction by premedication with promethazine/pethidine]. Anaesthesist. 1992;41(5):239-47. [Article]
- Kind
- Protein group
- Organism
- Not Available
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities. Transduces a signal by increasing the intracellular calcium ions and by stimulating adenylyl cyclase activity. The rank order of potency for agonists of this receptor is 1-oleoyl- > 1-stearoyl- > 1-palmitoyl- > 1-myristoyl- > 1-alkyl- > 1-alkenyl-LPA.
- Specific Function
- G protein-coupled receptor activity
Components:
References
- Cantisani C, Ricci S, Grieco T, Paolino G, Faina V, Silvestri E, Calvieri S: Topical promethazine side effects: our experience and review of the literature. Biomed Res Int. 2013;2013:151509. doi: 10.1155/2013/151509. Epub 2013 Nov 19. [Article]
- Horvat A, Orlic T, Banjac A, Momic T, Petrovic S, Demajo M: Inhibition of rat brain ecto-atpase activity by various drugs. Gen Physiol Biophys. 2006 Mar;25(1):91-105. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity
- Specific 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...
Components:
References
- Cantisani C, Ricci S, Grieco T, Paolino G, Faina V, Silvestri E, Calvieri S: Topical promethazine side effects: our experience and review of the literature. Biomed Res Int. 2013;2013:151509. doi: 10.1155/2013/151509. Epub 2013 Nov 19. [Article]
- Tanaka H, Habuchi Y, Nishimura M, Sato N, Watanabe Y: Blockade of Na+ current by promethazine in guinea-pig ventricular myocytes. Br J Pharmacol. 1992 Aug;106(4):900-5. doi: 10.1111/j.1476-5381.1992.tb14432.x. [Article]
- Kind
- Protein group
- Organism
- Not Available
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney (PubMed:1990381...
Components:
References
- Cantisani C, Ricci S, Grieco T, Paolino G, Faina V, Silvestri E, Calvieri S: Topical promethazine side effects: our experience and review of the literature. Biomed Res Int. 2013;2013:151509. doi: 10.1155/2013/151509. Epub 2013 Nov 19. [Article]
- Galeotti N, Ghelardini C, Bartolini A: The role of potassium channels in antihistamine analgesia. Neuropharmacology. 1999 Dec;38(12):1893-901. doi: 10.1016/s0028-3908(99)00068-4. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Only exerts an inhibitory effect at high concentrations not normally observed in plasma.
- 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
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- He N, Zhang WQ, Shockley D, Edeki T: Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes. Eur J Clin Pharmacol. 2002 Feb;57(12):847-51. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Platts SH, Shi SJ, Meck JV: Akathisia with combined use of midodrine and promethazine. JAMA. 2006 May 3;295(17):2000-1. [Article]
- Nakamura K, Yokoi T, Inoue K, Shimada N, Ohashi N, Kume T, Kamataki T: CYP2D6 is the principal cytochrome P450 responsible for metabolism of the histamine H1 antagonist promethazine in human liver microsomes. Pharmacogenetics. 1996 Oct;6(5):449-57. [Article]
- He N, Zhang WQ, Shockley D, Edeki T: Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes. Eur J Clin Pharmacol. 2002 Feb;57(12):847-51. [Article]
- Flockhart Table of Drug Interactions [Link]
- 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
- Potential CYP2B6 Substrates, Inhibitors, Inudcers (https://ctep.cancer.gov/protocoldevelopment/docs/cyp2b6.doc) [File]
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
- He LL, Wang ZX, Wang YX, Liu XP, Yang YJ, Gao YP, Wang X, Liu B, Wang X: Studies on the interaction between promethazine and human serum albumin in the presence of flavonoids by spectroscopic and molecular modeling techniques. Colloids Surf B Biointerfaces. 2016 Sep 1;145:820-829. doi: 10.1016/j.colsurfb.2016.06.001. Epub 2016 Jun 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
- Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocyte...
- Gene Name
- ABCC3
- Uniprot ID
- O15438
- Uniprot Name
- Canalicular multispecific organic anion transporter 2
- Molecular Weight
- 169341.14 Da
References
- Kock K, Ferslew BC, Netterberg I, Yang K, Urban TJ, Swaan PW, Stewart PW, Brouwer KL: Risk factors for development of cholestatic drug-induced liver injury: inhibition of hepatic basolateral bile acid transporters multidrug resistance-associated proteins 3 and 4. Drug Metab Dispos. 2014 Apr;42(4):665-74. doi: 10.1124/dmd.113.054304. Epub 2013 Oct 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Atpase activity, coupled to transmembrane movement of substances
- Specific Function
- May be an organic anion pump relevant to cellular detoxification.
- Gene Name
- ABCC4
- Uniprot ID
- O15439
- Uniprot Name
- Multidrug resistance-associated protein 4
- Molecular Weight
- 149525.33 Da
References
- Kock K, Ferslew BC, Netterberg I, Yang K, Urban TJ, Swaan PW, Stewart PW, Brouwer KL: Risk factors for development of cholestatic drug-induced liver injury: inhibition of hepatic basolateral bile acid transporters multidrug resistance-associated proteins 3 and 4. Drug Metab Dispos. 2014 Apr;42(4):665-74. doi: 10.1124/dmd.113.054304. Epub 2013 Oct 23. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54