Identification
- Summary
-
Almotriptanis a 5-HT1B/1D receptor agonist used to treat migraines.
- Brand Names
-
Axert
- Generic Name
- Almotriptan
- DrugBank Accession Number
- DB00918
- Background
-
Almotriptan曲普坦药物治疗migraine headaches. Almotriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and stopping the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Almotriptan does not prevent migraine attacks.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
-
Structure for Almotriptan (DB00918)
- Weight
-
Average: 335.464
Monoisotopic: 335.166747749 - Chemical Formula
- C17H25N3O2S
- Synonyms
-
- 1-(((3-(2-(Dimethylamino)ethyl)indol-5-yl)methyl)sulfonyl)pyrrolidine
- Almotriptan
- External IDs
-
- LAS 31416
- LAS-31416
Pharmacology
- Indication
-
For the treatment of acute migraine headache in adults
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with evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets. - Associated Conditions
- Contraindications & Blackbox Warnings
-
Avoid life-threatening adverse drug eventsImprove clinical decision support with information oncontraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support. - Pharmacodynamics
-
Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT1Dfamily) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3or 5-HT4receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT1receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans.
- Mechanism of action
-
Almotriptan binds with high affinity to human 5-HT1Band 5-HT1Dreceptors leading to cranial blood vessel constriction.
Target Actions Organism U5-hydroxytryptamine receptor 1D agonistHumans U5-hydroxytryptamine receptor 1B agonistHumans - Absorption
-
Not Available
- Volume of distribution
-
- 180 to 200 L
- Protein binding
-
35%
- Metabolism
-
Hover over products below to view reaction partners
- Route of elimination
-
Almotriptan is eliminated primarily by renal excretion (about 75% of the oral dose), with approximately 40% of an administered dose excreted unchanged in urine. Approximately 13% of the administered dose is excreted via feces, both unchanged and metabolized.
- Half-life
-
3-4 hours
- Clearance
-
- 57 L/h [healthy]
- 34.2 L/h [moderate renal impairment (creatinine clearance between 31 and 71 mL/min)]
- 9.8 L/h [severe renal impairment (creatinine clearance between 10 and 30 mL/min)]
- Adverse Effects
-
Improve decision support & research outcomesWith structured adverse effects data, including:blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data. - Toxicity
-
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
-
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3 --- (C;T)/(T;T) T Allele EffectDirectly Studied Patients with this genotype have an increased likelihood of responding to almotriptan when treating cluster headache. Details
Interactions
- Drug InteractionsLearn More" title="" 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 adverse effects can be increased when Almotriptan is combined with 1,2-Benzodiazepine. Abacavir Almotriptan may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Almotriptan can be increased when it is combined with Abametapir. Abatacept The metabolism of Almotriptan can be increased when combined with Abatacept. Abiraterone The metabolism of Almotriptan can be decreased when combined with Abiraterone. Acebutolol The metabolism of Almotriptan can be decreased when combined with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Almotriptan is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Almotriptan is combined with Acemetacin. Acenocoumarol The risk or severity of adverse effects can be increased when Almotriptan is combined with Acenocoumarol. Acetaminophen Acetaminophen may decrease the excretion rate of Almotriptan which could result in a higher serum level. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
-
- Take with or without food. The absorption is unaffected by food.
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 Almotriptan malate PJP312605E 181183-52-8 QHATUKWEVNMHRY-UHFFFAOYSA-N - Product Images
-
- International/Other Brands
- Almogran
- Brand Name Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Almotriptan Tablet 12.5 mg Oral Pro Doc Limitee 2014-06-10 Not applicable Canada 
Almotriptan Tablet 12.5 mg Oral Sanis Health Inc 2018-03-06 Not applicable Canada Almotriptan Malate Tablet, coated 6.25 mg/1 Oral Patriot Pharmaceuticals, LLC 2015-07-07 2018-04-30 US 
Almotriptan Malate Tablet, coated 12.5 mg/1 Oral Patriot Pharmaceuticals, LLC 2015-07-07 2018-07-31 US Axert Tablet, coated 6.25 mg/1 Oral Ortho-McNeil Pharmaceuticals, Inc. 2001-05-07 2014-09-30 US Axert Tablet, coated 6.25 mg/1 Oral Janssen Pharmaceuticals, Inc. 2001-05-07 2020-06-15 US Axert Tablet, coated 12.5 mg/1 Oral Physicians Total Care, Inc. 2006-02-09 Not applicable US 
Axert Tablet, coated 12.5 mg/1 Oral Janssen Pharmaceuticals, Inc. 2001-05-07 2020-06-15 US Axert Tablet, coated 12.5 mg/1 Oral Ortho-McNeil Pharmaceuticals, Inc. 2001-05-07 2014-09-30 US 
Axert 12.5mg Tablet 12.5 mg Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc 2003-12-08 2017-10-27 Canada - Generic Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Almotriptan Tablet, film coated 12.5 mg/1 Oral Ajanta Pharma USA Inc. 2015-10-07 Not applicable US Almotriptan Tablet, film coated 6.25 mg/1 Oral Ajanta Pharma USA Inc. 2015-10-07 Not applicable US Almotriptan Malate Tablet, film coated 12.5 mg/1 Oral Mylan Pharmaceuticals Inc. 2015-11-10 Not applicable US Almotriptan Malate Tablet, film coated 12.5 mg/1 Oral Teva Pharmaceuticals USA, Inc. 2015-07-07 Not applicable US 
Almotriptan Malate Tablet, film coated 6.25 mg/1 Oral Mylan Pharmaceuticals Inc. 2015-11-10 Not applicable US Almotriptan Malate Tablet, film coated 6.25 mg/1 Oral Teva Pharmaceuticals USA, Inc. 2015-07-07 Not applicable US 
Apo-almotriptan Tablet 12.5 mg Oral Apotex Corporation 2013-10-22 Not applicable Canada Apo-almotriptan Tablet 6.25 mg Oral Apotex Corporation 2013-12-24 Not applicable Canada Mylan-almotriptan Tablet 12.5 mg Oral Mylan Pharmaceuticals 2013-07-22 Not applicable Canada Mylan-almotriptan Tablet 6.25 mg Oral Mylan Pharmaceuticals 2013-07-22 Not applicable Canada
Categories
- ATC Codes
- N02CC05 — Almotriptan
- Drug Categories
-
- Agents that produce hypertension
- Amines
- Analgesics
- Antidepressive Agents
- Antimigraine Preparations
- Biogenic Amines
- Biogenic Monoamines
- Central Nervous System Depressants
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Indoles
- Migraine Disorders
- Monoamine Oxidase A Substrates
- Nervous System
- Neurotransmitter Agents
- Selective Serotonin 5-HT1 Receptor Agonists
- Selective Serotonin Agonists
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 1b Receptor Agonists
- Serotonin 1d Receptor Agonists
- Serotonin 5-HT1 Receptor Agonists
- Serotonin Agents
- Serotonin Modulators
- Serotonin Receptor Agonists
- Serotonin-1b and Serotonin-1d Receptor Agonist
- Triptans
- Chemical TaxonomyProvided byClassyfire
-
- Description
- This compound belongs to the class of organic compounds known as tryptamines and derivatives. These are compounds containing the tryptamine backbone, which is structurally characterized by an indole ring substituted at the 3-position by an ethanamine.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Indoles and derivatives
- Sub Class
- Tryptamines and derivatives
- Direct Parent
- Tryptamines and derivatives
- Alternative Parents
- 3-alkylindoles/Aralkylamines/Substituted pyrroles/Organosulfonamides/Organic sulfonamides/Benzenoids/Sulfonyls/Pyrrolidines/Heteroaromatic compounds/Trialkylamines show 4 more
- Substituents
- 3-alkylindole/Amine/Aralkylamine/芳香heteropolycyclic compound/Azacycle/Benzenoid/Heteroaromatic compound/Hydrocarbon derivative/Indole/Organic nitrogen compound show 16 more
- Molecular Framework
- 芳香heteropolycyclic compounds
- External Descriptors
- tertiary amine, sulfonamide, indoles (CHEBI:520985)
- Affected organisms
-
- Humans and other mammals
Chemical Identifiers
- UNII
- 1O4XL5SN61
- CAS number
- 154323-57-6
- InChI Key
- WKEMJKQOLOHJLZ-UHFFFAOYSA-N
- InChI
-
InChI=1S/C17H25N3O2S/c1-19(2)10-7-15-12-18-17-6-5-14(11-16(15)17)13-23(21,22)20-8-3-4-9-20/h5-6,11-12,18H,3-4,7-10,13H2,1-2H3
- IUPAC Name
-
二甲基(2 - {5 - [(pyrrolidine-1-sulfonyl)甲基]1 h -indol-3-yl}ethyl)amine
- SMILES
-
CN(C)CCC1=CNC2=C1C=C(CS(=O)(=O)N1CCCC1)C=C2
References
- Synthesis Reference
-
Ramasubramanian Sridharan, Vandanapu Purushotham, Kori Algooram, Nitin Pradhan, "Crystalline forms of almotriptan and processes for their preparation." U.S. Patent US20070112055, issued May 17, 2007.
US20070112055 - General References
-
- FDA Approved Drug Products: Almotriptan Oral Tablets [Link]
- External Links
-
- Human Metabolome Database
- HMDB0015054
- PubChem Compound
- 123606
- PubChem Substance
- 46505165
- ChemSpider
- 110198
- 279645
- ChEBI
- 520985
- ChEMBL
- CHEMBL1505
- ZINC
- ZINC000000018087
- Therapeutic Targets Database
- DAP001345
- PharmGKB
- PA10246
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Almotriptan
- FDA label
-
Download (778 KB)
Clinical Trials
- Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
-
Phase Status Purpose Conditions Count 4 Completed Other Workplace Migraine Treatment 1 4 Completed Treatment Classical migraine/Migraine/Migraine Without Aura 1 4 Completed Treatment Migraine 2 4 Completed Treatment Migraine/Sinusitis 1 4 Recruiting Treatment Migraine With Aura/Migraine Without Aura 1 4 Unknown Status Prevention Medication Overuse Headache 1 3 Completed Treatment Migraine 2 Not Available Completed Not Available Migraine 3
Pharmacoeconomics
- Manufacturers
-
- Ortho mcneil janssen pharmaceuticals inc
- Packagers
-
- Janssen-Ortho Inc.
- McNeil Laboratories
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Ortho-McNeil-Janssen Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Dosage Forms
-
Form Route Strength Tablet, film coated Oral 12.5 MG Tablet, film coated Oral 12.5 mg/1 Tablet, film coated Oral 6.25 mg/1 Tablet, coated Oral 12.5 mg/1 Tablet, coated Oral 6.25 mg/1 Tablet Oral 12.5 mg Tablet Oral 6.25 mg - Prices
-
Unit description Cost Unit Axert 12 12.5 mg tablet Box 300.14USD box Axert 6 6.25 mg tablet Box 150.05USD box Axert 12.5 mg tablet 24.05USD tablet Axert 6.25毫克的平板电脑 24.05USD 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 CA2120028 No 1999-03-23 2013-07-19 Canada US5565447 Yes 1996-10-15 2015-11-07 US
Properties
- State
- Solid
- Experimental Properties
-
Property Value Source logP 1.6 Not Available - Predicted Properties
-
Property Value Source Water Solubility 0.121 mg/mL ALOGPS logP 2.04 ALOGPS logP 1.52 Chemaxon logS -3.4 ALOGPS pKa (Strongest Acidic) 17.14 Chemaxon pKa (Strongest Basic) 9.55 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 56.41 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 94.52 m3·mol-1 Chemaxon Polarizability 37.01 Å3 Chemaxon Number of Rings 3 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 + 1.0 Blood Brain Barrier + 0.9781 Caco-2 permeable - 0.7421 P-glycoprotein substrate Substrate 0.5636 P-glycoprotein inhibitor I Non-inhibitor 0.8282 P-glycoprotein inhibitor II Non-inhibitor 0.8679 Renal organic cation transporter Non-inhibitor 0.553 CYP450 2C9 substrate Non-substrate 0.7898 CYP450 2D6 substrate Substrate 0.8919 CYP450 3A4 substrate Substrate 0.6292 CYP450 1A2 substrate Non-inhibitor 0.605 CYP450 2C9 inhibitor Non-inhibitor 0.8089 CYP450 2D6 inhibitor Non-inhibitor 0.6273 CYP450 2C19 inhibitor Non-inhibitor 0.8581 CYP450 3A4 inhibitor Non-inhibitor 0.8929 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8486 Ames test Non AMES toxic 0.6532 Carcinogenicity Non-carcinogens 0.8588 Biodegradation Not ready biodegradable 0.9508 Rat acute toxicity 2.5976 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5255 hERG inhibition (predictor II) Non-inhibitor 0.6008
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
-
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
Build, predict & validate machine-learning models
使用我们的结构化和以证据为基础的数据集unlock new
insights and accelerate drug research.
insights and accelerate drug research.
使用我们的结构化和以证据为基础的数据集unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1D
- Uniprot ID
- P28221
- Uniprot Name
- 5-hydroxytryptamine receptor 1D
- 分子量
- 41906.38 Da
References
- Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [Article]
- Bou J, Domenech T, Puig J, Heredia A, Gras J, Fernandez-Forner D, Beleta J, Palacios JM: Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol. 2000 Dec 20;410(1):33-41. [Article]
- Gras J, Llupia J, Llenas J, Palacios JM: Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Arzneimittelforschung. 2001 Sep;51(9):726-32. [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
-
Unknown
- Actions
-
Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1B
- Uniprot ID
- P28222
- Uniprot Name
- 5-hydroxytryptamine receptor 1B
- 分子量
- 43567.535 Da
References
- Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R: Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. [Article]
- Fleishaker JC, Sisson TA, Carel BJ, Azie NE: Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers. Clin Pharmacol Ther. 2000 May;67(5):498-503. [Article]
- van den Broek RW, MaassenVanDenBrink A, de Vries R, Bogers AJ, Stegmann AP, Avezaat CJ, Saxena PR: Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels. Eur J Pharmacol. 2000 Oct 27;407(1-2):165-73. [Article]
- Knyihar-Csillik E, Tajti J, Csillik AE, Chadaide Z, Mihaly A, Vecsei L: Effects of eletriptan on the peptidergic innervation of the cerebral dura mater and trigeminal ganglion, and on the expression of c-fos and c-jun in the trigeminal complex of the rat in an experimental migraine model. Eur J Neurosci. 2000 Nov;12(11):3991-4002. [Article]
- Bou J, Domenech T, Puig J, Heredia A, Gras J, Fernandez-Forner D, Beleta J, Palacios JM: Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol. 2000 Dec 20;410(1):33-41. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Enzymes
- 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
- 分子量
- 57342.67 Da
References
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
- McEnroe JD, Fleishaker JC: Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine. Clin Pharmacokinet. 2005;44(3):237-46. [Article]
- FDA Approved Drug Products: Almotriptan Oral Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- 分子量
- 55768.94 Da
References
- McEnroe JD, Fleishaker JC: Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine. Clin Pharmacokinet. 2005;44(3):237-46. [Article]
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
- FDA Approved Drug Products: Almotriptan Oral Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Serotonin binding
- Specific Function
- Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral...
- Gene Name
- MAOA
- Uniprot ID
- P21397
- Uniprot Name
- Amine oxidase [flavin-containing] A
- 分子量
- 59681.27 Da
References
- McEnroe JD, Fleishaker JC: Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine. Clin Pharmacokinet. 2005;44(3):237-46. [Article]
- Gras J, Llenas J, Jansat JM, Jauregui J, Cabarrocas X, Palacios JM: Almotriptan, a new anti-migraine agent: a review. CNS Drug Rev. 2002 Fall;8(3):217-34. [Article]
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
- FDA Approved Drug Products: Almotriptan Oral Tablets [Link]
- Med-Psych Review: Triptans [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Trimethylamine monooxygenase activity
- Specific Function
- Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an impor...
- Gene Name
- FMO3
- Uniprot ID
- P31513
- Uniprot Name
- Dimethylaniline monooxygenase [N-oxide-forming] 3
- 分子量
- 60032.975 Da
References
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- 分子量
- 55930.545 Da
References
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- 分子量
- 56848.42 Da
References
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- 分子量
- 55824.275 Da
References
- Salva M, Jansat JM, Martinez-Tobed A, Palacios JM: Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Drug Metab Dispos. 2003 Apr;31(4):404-11. [Article]
Drug created at June 13, 2005 13:24 / Updated at March 02, 2023 12:22