Identification
- Summary
Epinastine is an H1 receptor antagonist used to prevent itching in allergic conjunctivitis.
- Brand Names
- Elestat
- Generic Name
- Epinastine
- DrugBank Accession Number
- DB00751
- Background
Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Epinastine (DB00751)
- Weight
- Average: 249.3104
Monoisotopic: 249.126597495 - Chemical Formula
- C16H15N3
- Synonyms
- (±)-epinastine
- 3-amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine
- Epinastin
- Epinastina
- Epinastine
- épinastine
- Epinastinum
- External IDs
- WAL 801 Cl
Pharmacology
- Indication
For the prevention of itching associated with allergic conjunctivitis.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Symptomatic treatment of Allergic conjunctivitis •••••••••••• - Contraindications & Blackbox Warnings
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Epinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT2 -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.
- Mechanism of action
Epinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Target Actions Organism AHistamine H1 receptor antagonistHumans AHistamine H2 receptor antagonistHumans UAlpha-1A adrenergic receptor unknownHumans UAlpha-2A adrenergic receptor unknownHumans U5-hydroxytryptamine receptor 2A antagonistHumans U5-hydroxytryptamine receptor 7 antagonistHumans - Absorption
The absolute bioavailability of epinastine is about 40%.
- Volume of distribution
Not Available
- Protein binding
64%
- Metabolism
Mainly excreted unchanged, less than 10% metabolized.
- Route of elimination
Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.
- Half-life
12 hours
- Clearance
- 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
Pathway Category Epinastine 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 Epinastine is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Epinastine can be increased when it is combined with Abametapir. Abatacept The metabolism of Epinastine can be increased when combined with Abatacept. Abiraterone The metabolism of Epinastine can be decreased when combined with Abiraterone. Acebutolol The metabolism of Epinastine can be decreased when combined with Acebutolol. - 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 Epinastine hydrochloride GFM415S5XL 108929-04-0 VKXSGUIOOQPGAF-UHFFFAOYSA-N - International/Other Brands
- Alegain (Kyorin Rimedio) / Alenapion (Choseido Pharmaceutical) / Alesion (Boehringer Ingelheim) / Alesiotec (Nihon Yakuhin Kogyo) / Alket (Poen) / Allernothin (Morishita Jintan) / Allerstin (Dong Koo) / Alpeed (Daito) / Aplatin (Taiyo Pharmaceutical) / Aresten (Il Sung) / Asmot (Tatsumi Kagaku) / Atergit (Roemmers) / Azusaleon (Shiono Kemikaru) / Elpinan (Towa Yakuhin) / Epinazion (Medisa Shinyaku) / Epioftal (Farmindustria) / Flurinol (Boehringer Ingelheim) / Helvottz (Yoshindo) / Kai lai Zhi (Carelife Pharmaceutical Co Ltd) / Pinasion (Taisho Yakuhin) / Purivist (Allergan) / Relenastine (Lansier) / Relestat (Allergan) / Talerc (Aché) / Timkent (Nisshin Seiyaku) / Yupitel (Iwaki Seiyaku)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Elestat Solution / drops 0.5 mg/1mL Ophthalmic Allergan, Inc. 2004-01-19 Not applicable US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Epinastine Solution / drops 0.5 mg/1mL Ophthalmic Akorn 2017-05-05 Not applicable US Epinastine HCl Solution 0.5 mg/1mL Ophthalmic Av Kare, Inc. 2011-11-15 2015-02-20 US Epinastine HCl Solution 0.5 mg/1mL Ophthalmic Cypress Pharmaceuticals, Inc. 2011-05-02 2013-09-11 US Epinastine Hydrochloride Solution / drops 0.5 mg/1mL Ophthalmic Paddock Laboratories, Inc. 2011-11-01 2014-12-31 US Epinastine Hydrochloride Solution / drops 0.5 mg/1mL Ophthalmic Breckenridge Pharmaceutical, Inc. 2013-11-05 2024-09-30 US
Categories
- ATC Codes
- S01GX10 — Epinastine
- S01GX — Other antiallergics
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Acid Reducers
- Antidepressive Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Decongestants and Antiallergics
- Decreased Histamine Release
- Heterocyclic Compounds, Fused-Ring
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H1 Inhibitors
- Histamine H2 Antagonists
- Neurotransmitter Agents
- Ophthalmics
- Ophthalmologicals
- P-glycoprotein substrates
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Sensory Organs
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dibenzazepines. These are compounds with two benzene rings connected by an azepine ring. Azepine is an unsaturated seven-member heterocycle with one nitrogen atom replacing a carbon atom.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzazepines
- Sub Class
- Dibenzazepines
- Direct Parent
- Dibenzazepines
- Alternative Parents
- Azepines / Benzenoids / Imidazolines / Guanidines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- 2-imidazoline / Aromatic heteropolycyclic compound / Azacycle / Azepine / Benzenoid / Carboximidamide / Dibenzazepine / Guanidine / Hydrocarbon derivative / Organic 1,3-dipolar compound
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- guanidines, benzazepine (CHEBI:51032)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- Q13WX941EF
- CAS number
- 80012-43-7
- InChI Key
- WHWZLSFABNNENI-UHFFFAOYSA-N
- InChI
- InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)
- IUPAC Name
- 2,4-diazatetracyclo[12.4.0.0^{2,6}.0^{7,12}]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine
- SMILES
- NC1=NCC2N1C1=CC=CC=C1CC1=CC=CC=C21
References
- Synthesis Reference
Akiharu Isowaki, Tomoko Nakajima, Akira Ohtori, "Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine." U.S. Patent US20090143359, issued June 04, 2009.
US20090143359- General References
- Walther G, Daniel H, Bechtel WD, Brandt K: New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneimittelforschung. 1990 Apr;40(4):440-6. [Article]
- Schilling JC, Adamus WS, Kuthan H: Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1990 Dec;28(12):493-7. [Article]
- External Links
- Human Metabolome Database
- HMDB0014889
- KEGG Drug
- D01713
- PubChem Compound
- 3241
- PubChem Substance
- 46509056
- ChemSpider
- 3128
- BindingDB
- 50131441
- 39684
- ChEBI
- 51032
- ChEMBL
- CHEMBL1106
- Therapeutic Targets Database
- DAP001074
- PharmGKB
- PA164764489
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Epinastine
- FDA label
- Download (113 KB)
- MSDS
- Download (57 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 Treatment Allergic Conjunctivitis (AC) 2 4 Completed Treatment Allergic Reaction 1 4 Withdrawn Treatment Allergic Conjunctivitis (AC) 1 3 Completed Not Available Allergic Conjunctivitis (AC) 1 3 Completed Treatment Atopic Dermatitis 2
Pharmacoeconomics
- Manufacturers
- Allergan inc
- Packagers
- Allergan Inc.
- Dosage Forms
Form Route Strength Solution Ophthalmic 0.500 mg Solution Intraocular; Ophthalmic 0.5 mg Tablet Oral 20 mg Solution Ophthalmic 0.5 mg/1mL Solution / drops Ophthalmic 0.5 mg/1mL Solution Ophthalmic 0.5 mg Syrup Oral 0.2 g Tablet Oral 10 mg Tablet, extended release Oral Tablet, coated Oral 20 mg Tablet Oral 20.00 mg Tablet Oral 20.000 mg Solution / drops Conjunctival 0.5 mg/ml Liquid Ophthalmic 0.5 mg/1ml Solution 0.5 mg/ml Solution / drops Ophthalmic 0.5 mg/ml Solution / drops Ophthalmic 0.05 % Solution Ophthalmic 0.05 % w/v - Prices
Unit description Cost Unit Elestat 0.05% Solution 5ml Bottle 116.58USD bottle Elestat 0.05% eye drops 22.94USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7429602 No 2008-09-30 2020-11-29 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 205-208 °C Not Available logP 3.51 BIOBYTE (1995) - Predicted Properties
Property Value Source Water Solubility 0.163 mg/mL ALOGPS logP 2.53 ALOGPS logP 3.07 Chemaxon logS -3.2 ALOGPS pKa (Strongest Basic) 8.77 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 41.62 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 76.9 m3·mol-1 Chemaxon Polarizability 27.33 Å3 Chemaxon Number of Rings 4 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 + 0.9923 Blood Brain Barrier + 0.9787 Caco-2 permeable + 0.5766 P-glycoprotein substrate Substrate 0.5665 P-glycoprotein inhibitor I Non-inhibitor 0.8193 P-glycoprotein inhibitor II Non-inhibitor 0.5736 Renal organic cation transporter Inhibitor 0.7994 CYP450 2C9 substrate Non-substrate 0.8676 CYP450 2D6 substrate Substrate 0.8919 CYP450 3A4 substrate Non-substrate 0.5422 CYP450 1A2 substrate Non-inhibitor 0.5686 CYP450 2C9 inhibitor Non-inhibitor 0.9243 CYP450 2D6 inhibitor Non-inhibitor 0.5228 CYP450 2C19 inhibitor Non-inhibitor 0.8702 CYP450 3A4 inhibitor Non-inhibitor 0.6566 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.726 Ames test AMES toxic 0.5689 Carcinogenicity Non-carcinogens 0.9144 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.7509 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9353 hERG inhibition (predictor II) Non-inhibitor 0.8419
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-00di-0590000000-b39e6b7f0c2561681ad3 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0udi-0090000000-91653437d5b0b0635ca0 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0090000000-b52e77f2fd1806d2c197 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0udi-0090000000-218336f95f740dc28172 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-3090000000-f89534d25c65cbe24be6 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0a4l-2590000000-ba87d707561f4d2a7a1b Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-9430000000-7bb1414fdc204d44f849 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 161.6319906 predictedDarkChem Lite v0.1.0 [M-H]- 152.09908 predictedDeepCCS 1.0 (2019) [M+H]+ 161.9375906 predictedDarkChem Lite v0.1.0 [M+H]+ 154.45709 predictedDeepCCS 1.0 (2019) [M+Na]+ 162.2060906 predictedDarkChem Lite v0.1.0 [M+Na]+ 160.55035 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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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
- Tsujii T, Yamamoto E, Ohira T, Saito N, Watanabe S: Effects of sedative and non-sedative H1 antagonists on cognitive tasks: behavioral and near-infrared spectroscopy (NIRS) examinations. Psychopharmacology (Berl). 2007 Sep;194(1):83-91. Epub 2007 May 30. [Article]
- Walther G, Daniel H, Bechtel WD, Brandt K: New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneimittelforschung. 1990 Apr;40(4):440-6. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- 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
- Bielory L, Ghafoor S: Histamine receptors and the conjunctiva. Curr Opin Allergy Clin Immunol. 2005 Oct;5(5):437-40. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Unknown
- 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...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Dupont LJ, Meade CJ, Demedts MG, Verleden GM: Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor. Eur Respir J. 1996 Jul;9(7):1433-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Unknown
- General Function
- Thioesterase binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 48956.275 Da
References
- Dupont LJ, Meade CJ, Demedts MG, Verleden GM: Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor. Eur Respir J. 1996 Jul;9(7):1433-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Dupont LJ, Pype JL, Meade CJ, DeLeyn P, Deneffe G, Demedts MG, Verleden GM: Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro. Eur Respir J. 1999 Nov;14(5):1068-75. [Article]
- Dupont LJ, Meade CJ, Demedts MG, Verleden GM: Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor. Eur Respir J. 1996 Jul;9(7):1433-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Dupont LJ, Pype JL, Meade CJ, DeLeyn P, Deneffe G, Demedts MG, Verleden GM: Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro. Eur Respir J. 1999 Nov;14(5):1068-75. [Article]
Enzymes
- 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
- Kishimoto W, Hiroi T, Sakai K, Funae Y, Igarashi T: Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92. [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
- Kishimoto W, Hiroi T, Sakai K, Funae Y, Igarashi T: Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-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 performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Kishimoto W, Hiroi T, Sakai K, Funae Y, Igarashi T: Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Ishiguro N, Nozawa T, Tsujihata A, Saito A, Kishimoto W, Yokoyama K, Yotsumoto T, Sakai K, Igarashi T, Tamai I: Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier. Drug Metab Dispos. 2004 May;32(5):519-24. [Article]
Drug created at June 13, 2005 13:24 / Updated at December 02, 2023 06:59