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Identification
NameAlmotriptan
Accession NumberDB00918  (APRD00169)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Almotriptan is a triptan drug for the treatment of 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.

Structure
Thumb
Synonyms
1-(((3-(2-(Dimethylamino)ethyl)indol-5-yl)methyl)sulfonyl)pyrrolidine
External Identifiers
  • LAS 31416
  • LAS-31416
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Almotriptantablet12.5 mgoralPro Doc Limitee2014-06-10Not applicableCanada
Almotriptan Malatetablet, coated12.5 mg/1oralPatriot Pharmaceuticals, LLC2015-07-07Not applicableUs
Almotriptan Malatetablet, coated6.25 mg/1oralPatriot Pharmaceuticals, LLC2015-07-07Not applicableUs
Axerttablet, coated12.5 mg/1oralPhysicians Total Care, Inc.2006-02-09Not applicableUs
Axerttablet, coated6.25 mg/1oralJanssen Pharmaceuticals, Inc.2001-05-07Not applicableUs
Axerttablet, coated12.5 mg/1oralJanssen Pharmaceuticals, Inc.2001-05-07Not applicableUs
Axert 12.5mgtablet12.5 mgoralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc2003-12-08Not applicableCanada
Axert 6.25mgtablet6.25 mgoralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc2003-12-08Not applicableCanada
Mylan-almotriptantablet12.5 mgoralMylan Pharmaceuticals Ulc2013-07-22Not applicableCanada
Mylan-almotriptantablet6.25 mgoralMylan Pharmaceuticals Ulc2013-07-22Not applicableCanada
PMS-almotriptantablet12.5 mgoralPharmascience IncNot applicableNot applicableCanada
Sandoz Almotriptantablet12.5 mgoralSandoz Canada Incorporated2013-07-22Not applicableCanada
Teva-almotriptantablet12.5 mgoralTeva Canada Limited2014-12-12Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Almotriptantablet, film coated6.25 mg/1oralAjanta Pharma Limited2015-10-07Not applicableUs
Almotriptantablet, film coated12.5 mg/1oralAjanta Pharma Limited2015-10-07Not applicableUs
Almotriptan Malatetablet, film coated6.25 mg/1oralTeva Pharmaceuticals USA Inc2015-07-07Not applicableUs
Almotriptan Malatetablet, film coated12.5 mg/1oralMylan Pharmaceuticals Inc.2015-11-10Not applicableUs
Almotriptan Malatetablet, film coated6.25 mg/1oralMylan Pharmaceuticals Inc.2015-11-10Not applicableUs
Almotriptan Malatetablet, film coated12.5 mg/1oralTeva Pharmaceuticals USA Inc2015-07-07Not applicableUs
Apo-almotriptantablet12.5 mgoralApotex Inc2013-10-22Not applicableCanada
Apo-almotriptantablet6.25 mgoralApotex Inc2013-12-24Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlmogranNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Almotriptan malate
181183-52-8
ThumbNot applicableDBSALT001204
Categories
UNII1O4XL5SN61
CAS number154323-57-6
WeightAverage: 335.464
Monoisotopic: 335.166747749
Chemical FormulaC17H25N3O2S
InChI KeyInChIKey=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
dimethyl(2-{5-[(pyrrolidine-1-sulfonyl)methyl]-1H-indol-3-yl}ethyl)amine
SMILES
CN(C)CCC1=CNC2=C1C=C(CS(=O)(=O)N1CCCC1)C=C2
Taxonomy
DescriptionThis 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 subsituted at the 3-position by an ethanamine.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassTryptamines and derivatives
Direct ParentTryptamines and derivatives
Alternative Parents
Substituents
  • Tryptamine
  • Indole
  • Aralkylamine
  • Benzenoid
  • Substituted pyrrole
  • Heteroaromatic compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Pyrrolidine
  • Pyrrole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of acute migraine headache in adults
PharmacodynamicsAlmotriptan 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-HT1D family) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor 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-HT1 receptors 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 actionAlmotriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 180 to 200 L
Protein binding35%
Metabolism
SubstrateEnzymesProduct
Almotriptan
N-desmethylalmotriptanDetails
Almotriptan
2-{5-[(pyrrolidine-1-sulfonyl)methyl]-1H-indol-3-yl}acetic acidDetails
Almotriptan
2-{5-[(pyrrolidine-1-sulfonyl)methyl]-1H-indol-3-yl}ethan-1-olDetails
Almotriptan
1-[({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methane)sulfonyl]pyrrolidin-2-olDetails
Route of eliminationAlmotriptan 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 life3-4 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)]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3
Gene symbol: GNB3
UniProt: P16520
rs5443 Not AvailableT AlleleBetter response to drug treatment17361120
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9781
Caco-2 permeable-0.7421
P-glycoprotein substrateSubstrate0.5636
P-glycoprotein inhibitor INon-inhibitor0.8282
P-glycoprotein inhibitor IINon-inhibitor0.8679
Renal organic cation transporterNon-inhibitor0.553
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.6292
CYP450 1A2 substrateNon-inhibitor0.605
CYP450 2C9 inhibitorNon-inhibitor0.8089
CYP450 2D6 inhibitorNon-inhibitor0.6273
CYP450 2C19 inhibitorNon-inhibitor0.8581
CYP450 3A4 inhibitorNon-inhibitor0.8929
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8486
Ames testNon AMES toxic0.6532
CarcinogenicityNon-carcinogens0.8588
BiodegradationNot ready biodegradable0.9508
Rat acute toxicity2.5976 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5255
hERG inhibition (predictor II)Non-inhibitor0.6008
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Ortho mcneil janssen pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tablet, coatedoral12.5 mg/1
Tablet, coatedoral6.25 mg/1
Tablet, film coatedoral12.5 mg/1
Tablet, film coatedoral6.25 mg/1
Tabletoral12.5 mg
Tabletoral6.25 mg
Prices
Unit descriptionCostUnit
Axert 12 12.5 mg tablet Box300.14USD box
Axert 6 6.25 mg tablet Box150.05USD box
Axert 12.5 mg tablet24.05USD tablet
Axert 6.25 mg tablet24.05USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2120028 No1999-03-232013-07-19Canada
US5565447 Yes1995-11-072015-11-07Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.121 mg/mLALOGPS
logP2.04ALOGPS
logP1.52ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)17.14ChemAxon
pKa (Strongest Basic)9.55ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area56.41 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity94.52 m3·mol-1ChemAxon
Polarizability37.01 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
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 ReferencesNot Available
External Links
ATC CodesN02CC05
AHFS Codes
  • 28:32.28
PDB EntriesNot Available
FDA labelDownload (778 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcepromazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Amisulpride.
AripiprazoleThe risk or severity of adverse effects can be increased when Almotriptan is combined with Aripiprazole.
AtazanavirThe serum concentration of Almotriptan can be increased when it is combined with Atazanavir.
BenzquinamideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Benzquinamide.
BoceprevirThe serum concentration of Almotriptan can be increased when it is combined with Boceprevir.
CabergolineCabergoline may increase the vasoconstricting activities of Almotriptan.
CarphenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Carphenazine.
CeritinibThe serum concentration of Almotriptan can be increased when it is combined with Ceritinib.
ChlormezanoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Chlorprothixene.
ClarithromycinThe serum concentration of Almotriptan can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Clozapine.
CobicistatThe serum concentration of Almotriptan can be increased when it is combined with Cobicistat.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Almotriptan.
DarunavirThe serum concentration of Almotriptan can be increased when it is combined with Darunavir.
DroperidolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Droperidol.
DroxidopaAlmotriptan may increase the hypertensive activities of Droxidopa.
FencamfamineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Almotriptan.
GranisetronGranisetron may increase the serotonergic activities of Almotriptan.
HaloperidolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Haloperidol.
IdelalisibThe serum concentration of Almotriptan can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Almotriptan can be increased when it is combined with Indinavir.
ItraconazoleThe serum concentration of Almotriptan can be increased when it is combined with Itraconazole.
KetoconazoleThe serum concentration of Almotriptan can be increased when it is combined with Ketoconazole.
LoxapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Loxapine.
MesoridazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Methotrimeprazine.
MetoclopramideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Metoclopramide.
MolindoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Molindone.
NefazodoneThe serum concentration of Almotriptan can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Almotriptan can be increased when it is combined with Nelfinavir.
OlanzapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Almotriptan is combined with Ondansetron.
PaliperidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Paliperidone.
PerphenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Perphenazine.
PhenelzineThe metabolism of Almotriptan can be decreased when combined with Phenelzine.
PimozideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Piperacetazine.
PosaconazoleThe serum concentration of Almotriptan can be increased when it is combined with Posaconazole.
ProchlorperazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Risperidone.
RitonavirThe serum concentration of Almotriptan can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Almotriptan can be increased when it is combined with Saquinavir.
SertindoleThe risk or severity of adverse effects can be increased when Almotriptan is combined with Sertindole.
SulpirideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Sulpiride.
TelaprevirThe serum concentration of Almotriptan can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Almotriptan can be increased when it is combined with Telithromycin.
ThioridazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thiothixene.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Almotriptan.
TranylcypromineThe metabolism of Almotriptan can be decreased when combined with Tranylcypromine.
TrifluoperazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Triflupromazine.
VoriconazoleThe serum concentration of Almotriptan can be increased when it is combined with Voriconazole.
ZiprasidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Zuclopenthixol.
Food Interactions
  • Take without regard to meals.
  • The absorption is unaffected by food.

Targets

Kind
Protein
Organism
Human
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 substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 Da
References
  1. 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. [PubMed:10193663 ]
  2. 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. [PubMed:11134654 ]
  3. 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. [PubMed:11642004 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
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 substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. 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. [PubMed:10193663 ]
  2. 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. [PubMed:10824628 ]
  3. 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. [PubMed:11050304 ]
  4. 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. [PubMed:11069595 ]
  5. 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. [PubMed:11134654 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. 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. [PubMed:12642466 ]
  3. 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. [PubMed:15762767 ]
Kind
Protein
Organism
Human
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. 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. [PubMed:15762767 ]
Kind
Protein
Organism
Human
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 tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine.
Gene Name:
MAOA
Uniprot ID:
P21397
Molecular Weight:
59681.27 Da
References
  1. 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. [PubMed:15762767 ]
  2. 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. [PubMed:12353056 ]
  3. 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. [PubMed:12642466 ]
Kind
Protein
Organism
Human
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 important role in the metabolism of trimethylamine (TMA), via the production of TMA N-oxide (TMAO). Is also able to perform S-oxidation when acting on sulfide compounds (PubMed:9224773).
Gene Name:
FMO3
Uniprot ID:
P31513
Molecular Weight:
60032.975 Da
References
  1. 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. [PubMed:12642466 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. 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. [PubMed:12642466 ]
Kind
Protein
Organism
Human
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. 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. [PubMed:12642466 ]
Kind
Protein
Organism
Human
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. 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. [PubMed:12642466 ]
Kind
Protein
Organism
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. 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. [PubMed:12642466 ]
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Drug created on June 13, 2005 07:24 / Updated on August 24, 2016 01:53