Identification

Name
Almotriptan
Accession Number
DB00918  (APRD00169)
Type
Small Molecule
Groups
Approved, 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 IDs
LAS 31416 / LAS-31416
Product Ingredients
IngredientUNIICASInChI Key
Almotriptan malatePJP312605E181183-52-8QHATUKWEVNMHRY-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlmotriptanTablet12.5 mgOralSanis Health IncNot applicableNot applicableCanada
AlmotriptanTablet12.5 mgOralPro Doc Limitee2014-06-10Not applicableCanada
Almotriptan MalateTablet, coated12.5 mg/1OralPatriot Pharmaceuticals2015-07-07Not applicableUs
Almotriptan MalateTablet, coated6.25 mg/1OralPatriot Pharmaceuticals2015-07-07Not applicableUs
AxertTablet, coated12.5 mg/1OralJanssen Pharmaceuticals2001-05-07Not applicableUs
AxertTablet, coated12.5 mg/1OralPhysicians Total Care, Inc.2006-02-09Not applicableUs00062 2085 12 nlmimage10 06130328
AxertTablet, coated6.25 mg/1OralJanssen Pharmaceuticals2001-05-07Not 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-almotriptanTablet6.25 mgOralMylan Pharmaceuticals2013-07-22Not applicableCanada
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/1OralMylan Pharmaceuticals2015-11-10Not applicableUs
Almotriptan MalateTablet, film coated6.25 mg/1OralTeva2015-07-07Not applicableUs00093 5260 18 nlmimage10 10440850
Almotriptan MalateTablet, film coated12.5 mg/1OralMylan Pharmaceuticals2015-11-10Not applicableUs
Almotriptan MalateTablet, film coated12.5 mg/1OralTeva2015-07-07Not applicableUs00093 5261 29 nlmimage10 15440ac0
Apo-almotriptanTablet12.5 mgOralApotex Corporation2013-10-22Not applicableCanada
Apo-almotriptanTablet6.25 mgOralApotex Corporation2013-12-24Not applicableCanada
International/Other Brands
Almogran
Categories
UNII
1O4XL5SN61
CAS number
154323-57-6
Weight
Average: 335.464
Monoisotopic: 335.166747749
Chemical Formula
C17H25N3O2S
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
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

Pharmacology

Indication

For the treatment of acute migraine headache in adults

Structured Indications
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-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 action

Almotriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction.

TargetActionsOrganism
U5-hydroxytryptamine receptor 1D
agonist
Human
U5-hydroxytryptamine receptor 1B
agonist
Human
Absorption
Not Available
Volume of distribution
  • 180 to 200 L
Protein binding

35%

Metabolism
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)]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3---(T;T) / (C;T)T AlleleEffect Directly StudiedPatients with this genotype have an increased likelihood of responding to almotriptan when treating cluster headache.Details

Interactions

Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe metabolism of Almotriptan can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.Experimental
AbirateroneThe serum concentration of Almotriptan can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Aceprometazine.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Acetophenazine.Approved
AmiodaroneThe serum concentration of Almotriptan can be increased when it is combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Almotriptan.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Almotriptan.Approved
AmperozideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Amperozide.Experimental
AmphetamineThe serum concentration of Almotriptan can be increased when it is combined with Amphetamine.Approved, Illicit
AprepitantThe serum concentration of Almotriptan can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Almotriptan is combined with Aripiprazole.Approved, Investigational
ArmodafinilThe metabolism of Almotriptan can be decreased when combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Almotriptan can be decreased when combined with Artemether.Approved
AsenapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Asenapine.Approved
AtazanavirThe serum concentration of Almotriptan can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Almotriptan can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Azaperone.Investigational, Vet Approved
AzithromycinThe metabolism of Almotriptan can be decreased when combined with Azithromycin.Approved
BenmoxinThe metabolism of Almotriptan can be decreased when combined with Benmoxin.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Benperidol.Investigational
BetaxololThe metabolism of Almotriptan can be decreased when combined with Betaxolol.Approved
BifeprunoxThe risk or severity of adverse effects can be increased when Almotriptan is combined with Bifeprunox.Investigational
BoceprevirThe serum concentration of Almotriptan can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Almotriptan can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Almotriptan can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Almotriptan is combined with Brexpiprazole.Approved
BrofaromineThe serum concentration of Almotriptan can be increased when it is combined with Brofaromine.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Bromocriptine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Bromperidol.Investigational
BupropionThe metabolism of Almotriptan can be decreased when combined with Bupropion.Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Almotriptan.Approved, Investigational
ButaperazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Butaperazine.Experimental
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Almotriptan.Approved
CaffeineThe metabolism of Almotriptan can be decreased when combined with Caffeine.Approved
CarbamazepineThe metabolism of Almotriptan can be increased when combined with Carbamazepine.Approved, Investigational
CariprazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Cariprazine.Approved
CaroxazoneThe metabolism of Almotriptan can be decreased when combined with Caroxazone.Withdrawn
CelecoxibThe metabolism of Almotriptan can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Almotriptan can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Almotriptan can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe metabolism of Almotriptan can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorproethazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Chlorproethazine.Experimental
ChlorpromazineThe metabolism of Almotriptan can be decreased when combined with Chlorpromazine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Chlorprothixene.Approved, Investigational, Withdrawn
CholecalciferolThe metabolism of Almotriptan can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Almotriptan can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Almotriptan can be decreased when combined with Cinacalcet.Approved
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Almotriptan.Approved
ClarithromycinThe serum concentration of Almotriptan can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Almotriptan can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Almotriptan can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Clomipramine.Approved, Vet Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Clopenthixol.Experimental
ClothiapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Almotriptan can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Almotriptan can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Almotriptan can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Almotriptan can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Almotriptan can be increased when it is combined with Conivaptan.Approved, Investigational
CrisaboroleThe metabolism of Almotriptan can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Almotriptan can be decreased when combined with Crizotinib.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Cyamemazine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Cyclobenzaprine.Approved
CyclosporineThe metabolism of Almotriptan can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Almotriptan can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Almotriptan can be decreased when it is combined with Dabrafenib.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Almotriptan is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Almotriptan.Investigational
DarifenacinThe metabolism of Almotriptan can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Almotriptan can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Almotriptan can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Almotriptan can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Almotriptan can be decreased when combined with Delavirdine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Desipramine.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Desvenlafaxine.Approved
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Almotriptan.Approved
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Almotriptan.Approved
DiltiazemThe metabolism of Almotriptan can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Almotriptan can be decreased when combined with Diphenhydramine.Approved
DixyrazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Dixyrazine.Experimental
DolasetronDolasetron may increase the serotonergic activities of Almotriptan.Approved
DosulepinThe metabolism of Almotriptan can be decreased when combined with Dosulepin.Approved
DoxepinThe risk or severity of adverse effects can be increased when Almotriptan is combined with Doxepin.Approved
DoxycyclineThe metabolism of Almotriptan can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Almotriptan can be decreased when combined with Dronedarone.Approved
DroperidolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Droperidol.Approved, Vet Approved
DroxidopaAlmotriptan may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Almotriptan.Approved
EcopipamThe risk or severity of adverse effects can be increased when Almotriptan is combined with Ecopipam.Investigational
EfavirenzThe metabolism of Almotriptan can be decreased when combined with Efavirenz.Approved, Investigational
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Almotriptan.Approved, Investigational
EliglustatThe metabolism of Almotriptan can be decreased when combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Almotriptan can be decreased when it is combined with Enzalutamide.Approved
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Almotriptan is combined with Ergoloid mesylate.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Ergonovine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Almotriptan.Approved
ErythromycinThe metabolism of Almotriptan can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Almotriptan is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Almotriptan can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Almotriptan can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe metabolism of Almotriptan can be decreased when combined with Etravirine.Approved
FelodipineThe metabolism of Almotriptan can be decreased when combined with Felodipine.Approved, Investigational
FencamfamineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Almotriptan.Approved, Illicit, Investigational, Vet Approved
FluanisoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fluanisone.Experimental
FluconazoleThe metabolism of Almotriptan can be decreased when combined with Fluconazole.Approved
FluoxetineThe metabolism of Almotriptan can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fluphenazine.Approved
FluspirileneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Fluspirilene.Approved, Investigational
FluvoxamineThe metabolism of Almotriptan can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Almotriptan can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Almotriptan can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Almotriptan can be increased when combined with Fosphenytoin.Approved
FrovatriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Frovatriptan.Approved, Investigational
FurazolidoneThe metabolism of Almotriptan can be decreased when combined with Furazolidone.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Almotriptan can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Almotriptan can be decreased when combined with Gemfibrozil.Approved
GranisetronGranisetron may increase the serotonergic activities of Almotriptan.Approved, Investigational
HaloperidolThe metabolism of Almotriptan can be decreased when combined with Haloperidol.Approved
HarmalineThe serum concentration of Almotriptan can be increased when it is combined with Harmaline.Experimental
HydracarbazineThe metabolism of Almotriptan can be decreased when combined with Hydracarbazine.Experimental
IdelalisibThe serum concentration of Almotriptan can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Iloperidone.Approved
ImatinibThe metabolism of Almotriptan can be decreased when combined with Imatinib.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Almotriptan.Approved
IndinavirThe serum concentration of Almotriptan can be increased when it is combined with Indinavir.Approved
IproclozideThe metabolism of Almotriptan can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Almotriptan can be decreased when combined with Iproniazid.Withdrawn
IrbesartanThe metabolism of Almotriptan can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Almotriptan can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Almotriptan is combined with Isocarboxazid.Approved
IsoniazidThe metabolism of Almotriptan can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Almotriptan can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Almotriptan can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Almotriptan can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe serum concentration of Almotriptan can be increased when it is combined with Ketoconazole.Approved, Investigational
LapatinibThe metabolism of Almotriptan can be decreased when combined with Lapatinib.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Almotriptan is combined with Levomilnacipran.Approved
LidocaineThe metabolism of Almotriptan can be decreased when combined with Lidocaine.Approved, Vet Approved
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Almotriptan.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Almotriptan is combined with Lithium.Approved
LobeglitazoneThe metabolism of Almotriptan can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe serum concentration of Almotriptan can be increased when it is combined with Lopinavir.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Almotriptan is combined with Lorcaserin.Approved
LosartanThe metabolism of Almotriptan can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Almotriptan can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Loxapine.Approved
LuliconazoleThe serum concentration of Almotriptan can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Almotriptan can be increased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Almotriptan can be decreased when combined with Lumefantrine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Lurasidone.Approved
ManidipineThe metabolism of Almotriptan can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Maprotiline.Approved
MebanazineThe metabolism of Almotriptan can be decreased when combined with Mebanazine.Withdrawn
MelperoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Melperone.Approved, Investigational
MesoridazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Mesoridazine.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Almotriptan.Approved
MethotrimeprazineThe metabolism of Almotriptan can be decreased when combined with Methotrimeprazine.Approved
Methylene blueThe metabolism of Almotriptan can be decreased when combined with Methylene blue.Approved, Investigational
MethylergometrineMethylergometrine may increase the vasoconstricting activities of Almotriptan.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Metoclopramide.Approved, Investigational
MetoprololThe metabolism of Almotriptan can be decreased when combined with Metoprolol.Approved, Investigational
MexiletineThe metabolism of Almotriptan can be decreased when combined with Mexiletine.Approved
MidostaurinThe metabolism of Almotriptan can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Almotriptan can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Almotriptan is combined with Milnacipran.Approved
MinaprineThe metabolism of Almotriptan can be decreased when combined with Minaprine.Approved
MirabegronThe metabolism of Almotriptan can be decreased when combined with Mirabegron.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Almotriptan.Approved
MitotaneThe serum concentration of Almotriptan can be decreased when it is combined with Mitotane.Approved
MoclobemideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Moclobemide.Approved
ModafinilThe metabolism of Almotriptan can be decreased when combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Molindone.Approved
MoperoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Moperone.Experimental
MosapramineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Mosapramine.Experimental
NaratriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Naratriptan.Approved, Investigational
NefazodoneThe serum concentration of Almotriptan can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Almotriptan can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Almotriptan can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Almotriptan can be increased when combined with Nevirapine.Approved
NialamideThe metabolism of Almotriptan can be decreased when combined with Nialamide.Withdrawn
NicardipineThe metabolism of Almotriptan can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Almotriptan can be decreased when combined with Nicotine.Approved
NilotinibThe metabolism of Almotriptan can be decreased when combined with Nilotinib.Approved, Investigational
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Almotriptan.Approved
OctamoxinThe metabolism of Almotriptan can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Almotriptan can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Almotriptan can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronOndansetron may increase the serotonergic activities of Almotriptan.Approved
OsanetantThe risk or severity of adverse effects can be increased when Almotriptan is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Almotriptan can be increased when it is combined with Osimertinib.Approved
OxypertineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Oxypertine.Experimental
PalbociclibThe serum concentration of Almotriptan can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Almotriptan.Approved, Investigational
PanobinostatThe serum concentration of Almotriptan can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Almotriptan can be decreased when combined with Pantoprazole.Approved
PargylineThe metabolism of Almotriptan can be decreased when combined with Pargyline.Approved
ParoxetineThe metabolism of Almotriptan can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Almotriptan can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Penfluridol.Experimental
PentobarbitalThe metabolism of Almotriptan can be increased when combined with Pentobarbital.Approved, Vet Approved
PerazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Almotriptan is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Almotriptan.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Almotriptan.Approved
PheniprazineThe metabolism of Almotriptan can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe metabolism of Almotriptan can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe metabolism of Almotriptan can be decreased when combined with Phenoxypropazine.Withdrawn
PhenytoinThe metabolism of Almotriptan can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Pimozide.Approved
PioglitazoneThe metabolism of Almotriptan can be decreased when combined with Pioglitazone.Approved, Investigational
PipamperoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Pipamperone.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Pipotiazine.Approved, Investigational
PirlindoleThe metabolism of Almotriptan can be decreased when combined with Pirlindole.Approved
PivhydrazineThe metabolism of Almotriptan can be decreased when combined with Pivhydrazine.Withdrawn
PosaconazoleThe serum concentration of Almotriptan can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Almotriptan can be increased when combined with Primidone.Approved, Vet Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Procarbazine.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Prochlorperazine.Approved, Vet Approved
PromazineThe metabolism of Almotriptan can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Promethazine.Approved
PropericiazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Propericiazine.Approved
ProthipendylThe risk or severity of adverse effects can be increased when Almotriptan is combined with Prothipendyl.Investigational
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Almotriptan.Approved
QuetiapineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Quetiapine.Approved
QuinidineThe metabolism of Almotriptan can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Almotriptan can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Almotriptan can be decreased when combined with Rabeprazole.Approved, Investigational
RacloprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Raclopride.Investigational
RanolazineThe metabolism of Almotriptan can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Rasagiline.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Reserpine.Approved, Investigational
RifabutinThe metabolism of Almotriptan can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Almotriptan can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Almotriptan can be increased when combined with Rifapentine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Almotriptan is combined with Ritanserin.Investigational
RitonavirThe metabolism of Almotriptan can be decreased when combined with Ritonavir.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Rizatriptan.Approved
RolapitantThe metabolism of Almotriptan can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Almotriptan can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneThe metabolism of Almotriptan can be decreased when combined with Rosiglitazone.Approved, Investigational
SafrazineThe metabolism of Almotriptan can be decreased when combined with Safrazine.Withdrawn
SaquinavirThe serum concentration of Almotriptan can be increased when it is combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Almotriptan can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Almotriptan is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Sertraline.Approved
SildenafilThe metabolism of Almotriptan can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Almotriptan can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Almotriptan can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Almotriptan can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Almotriptan can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleThe metabolism of Almotriptan can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Almotriptan can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Sultopride.Experimental
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Almotriptan.Approved, Investigational
TamoxifenThe metabolism of Almotriptan can be decreased when combined with Tamoxifen.Approved
TapentadolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Tapentadol.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Almotriptan.Approved
TelaprevirThe serum concentration of Almotriptan can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Almotriptan can be increased when it is combined with Telithromycin.Approved
Tenofovir disoproxilThe metabolism of Almotriptan can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Almotriptan can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TeriflunomideThe serum concentration of Almotriptan can be decreased when it is combined with Teriflunomide.Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Tetrahydropalmatine.Investigational
TheophyllineThe metabolism of Almotriptan can be decreased when combined with Theophylline.Approved
ThiopropazateThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thiopropazate.Experimental
ThioproperazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thioproperazine.Approved
ThioridazineThe metabolism of Almotriptan can be decreased when combined with Thioridazine.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Tiapride.Approved, Investigational
TiclopidineThe metabolism of Almotriptan can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Almotriptan can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Almotriptan can be decreased when it is combined with Tocilizumab.Approved
ToloxatoneThe metabolism of Almotriptan can be decreased when combined with Toloxatone.Approved
TopiramateThe metabolism of Almotriptan can be decreased when combined with Topiramate.Approved
TopiroxostatThe metabolism of Almotriptan can be decreased when combined with Topiroxostat.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Almotriptan.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe metabolism of Almotriptan can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Almotriptan.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Almotriptan.Approved, Investigational
TrifluoperazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Trifluoperazine.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe metabolism of Almotriptan can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Almotriptan.Approved
TropisetronTropisetron may increase the serotonergic activities of Almotriptan.Approved, Investigational
VemurafenibThe serum concentration of Almotriptan can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Almotriptan.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Almotriptan is combined with Veralipride.Experimental
VerapamilThe metabolism of Almotriptan can be decreased when combined with Verapamil.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Almotriptan.Approved
VoriconazoleThe serum concentration of Almotriptan can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Almotriptan.Approved
ZiprasidoneThe metabolism of Almotriptan can be decreased when combined with Ziprasidone.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Almotriptan.Approved, Investigational
ZotepineThe risk or severity of adverse effects can be increased when Almotriptan is combined with Zotepine.Approved, Investigational
ZucapsaicinThe metabolism of Almotriptan can be decreased when combined with Zucapsaicin.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Almotriptan is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Take without regard to meals.
  • The absorption is unaffected by food.

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
Not Available
External Links
Human Metabolome Database
HMDB15054
PubChem Compound
123606
PubChem Substance
46505165
ChemSpider
110198
ChEBI
520985
ChEMBL
CHEMBL1505
Therapeutic Targets Database
DAP001345
PharmGKB
PA10246
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Almotriptan
ATC Codes
N02CC05 — Almotriptan
AHFS Codes
  • 28:32.28 — Selective Serotonin Agonists
FDA label
Download (778 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentMigraines2
4CompletedTreatmentMigraines2
4Unknown StatusPreventionAnalgesic Rebound Headache1

Pharmacoeconomics

Manufacturers
  • Ortho mcneil janssen pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedOral12.5 mg/1
Tablet, film coatedOral6.25 mg/1
Tablet, coatedOral12.5 mg/1
Tablet, 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)
CA2120028No1999-03-232013-07-19Canada
US5565447Yes1995-11-072015-11-07Us

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

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
Tryptamine / 3-alkylindole / Indole / Aralkylamine / Substituted pyrrole / Organic sulfonic acid amide / Benzenoid / Organosulfonic acid amide / Pyrrole / Pyrrolidine
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tertiary amine, sulfonamide, indoles (CHEBI:520985)

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 subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
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 subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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...
Gene Name
MAOA
Uniprot ID
P21397
Uniprot Name
Amine oxidase [flavin-containing] A
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 impor...
Gene Name
FMO3
Uniprot ID
P31513
Uniprot Name
Dimethylaniline monooxygenase [N-oxide-forming] 3
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34