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Identification
NameRizatriptan
Accession NumberDB00953  (APRD00008)
TypeSmall Molecule
GroupsApproved
DescriptionRizatriptan is a triptan drug used for the treatment of migraine headaches. It is a selective 5-hydroxytryptamine1 receptor subtype agonist.
Structure
Thumb
Synonyms
N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]-ethanamine
N,N-Dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine
Risatriptan
Rizatriptán
Rizatriptan
Rizatriptanum
External Identifiers
  • L-705126
  • MK 462 Free Base
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act RizatriptanTablet10 mgOralActavis Pharma Company2012-06-14Not applicableCanada
Act RizatriptanTablet5 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act Rizatriptan ODTTablet, orally disintegrating5 mgOralActavis Pharma Company2012-01-30Not applicableCanada
Act Rizatriptan ODTTablet, orally disintegrating10 mgOralActavis Pharma Company2012-01-30Not applicableCanada
Auro-rizatriptanTablet10 mgOralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-rizatriptan ODTTablet, orally disintegrating5 mgOralAuro Pharma IncNot applicableNot applicableCanada
Auro-rizatriptan ODTTablet, orally disintegrating10 mgOralAuro Pharma IncNot applicableNot applicableCanada
Dom-rizatriptan RdtTablet, orally disintegrating5 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-rizatriptan RdtTablet, orally disintegrating10 mgOralDominion Pharmacal2013-05-20Not applicableCanada
Ipg-rizatriptanTablet10 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-rizatriptanTablet5 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-rizatriptanTablet5 mgOralJamp Pharma Corporation2012-03-26Not applicableCanada
Jamp-rizatriptanTablet10 mgOralJamp Pharma Corporation2012-03-26Not applicableCanada
Jamp-rizatriptan IrTablet5 mgOralJamp Pharma Corporation2014-09-25Not applicableCanada
Jamp-rizatriptan IrTablet10 mgOralJamp Pharma Corporation2014-09-25Not applicableCanada
Mar-rizatriptanTablet10 mgOralMarcan Pharmaceuticals Inc2012-05-03Not applicableCanada
Mar-rizatriptanTablet5 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
MaxaltTablet10 mg/1OralLake Erie Medical DBA Quality Care Products LLC2007-08-24Not applicableUs
MaxaltTablet5 mg/1OralMerck Sharp & Dohme Corp.1998-06-29Not applicableUs
MaxaltTablet10 mg/1OralPhysicians Total Care, Inc.2007-08-24Not applicableUs
MaxaltTablet10 mg/1OralMerck Sharp & Dohme Corp.1998-06-29Not applicableUs
MaxaltTablet10 mgOralMerck Canada Inc1999-08-31Not applicableCanada
MaxaltTablet10 mg/1OralSTAT Rx USA LLC1998-06-29Not applicableUs
MaxaltTablet5 mgOralMerck Canada Inc1999-08-312013-07-15Canada
MaxaltTablet10 mg/1OralRebel Distributors Corp1998-06-29Not applicableUs
Maxalt RpdTablet, orally disintegrating10 mgOralMerck Canada Inc1999-08-31Not applicableCanada
Maxalt RpdTablet, orally disintegrating5 mgOralMerck Canada Inc2000-05-05Not applicableCanada
Maxalt-mltTablet, orally disintegrating5 mg/1OralSTAT Rx USA LLC1998-06-29Not applicableUs
Maxalt-mltTablet, orally disintegrating10 mg/1OralPhysicians Total Care, Inc.2009-12-29Not applicableUs
Maxalt-mltTablet, orally disintegrating5 mg/1OralMerck Sharp & Dohme Corp.1998-06-29Not applicableUs
Maxalt-mltTablet, orally disintegrating10 mg/1OralMerck Sharp & Dohme Corp.1998-06-29Not applicableUs
Mint-rizatriptan ODTTablet, orally disintegrating10 mgOralMint Pharmaceuticals Inc2015-06-10Not applicableCanada
Mint-rizatriptan ODTTablet, orally disintegrating5 mgOralMint Pharmaceuticals Inc2015-06-10Not applicableCanada
Mylan-rizatriptanTablet5 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-rizatriptanTablet10 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-rizatriptan ODTTablet, orally disintegrating5 mgOralMylan Pharmaceuticals Ulc2012-01-31Not applicableCanada
Mylan-rizatriptan ODTTablet, orally disintegrating10 mgOralMylan Pharmaceuticals Ulc2012-01-31Not applicableCanada
Nat-rizatriptanTablet5 mgOralNatco Pharma (Canada) IncNot applicableNot applicableCanada
Nat-rizatriptanTablet10 mgOralNatco Pharma (Canada) IncNot applicableNot applicableCanada
Nat-rizatriptan ODTTablet, orally disintegrating5 mgOralNatco Pharma (Canada) Inc2015-02-17Not applicableCanada
Nat-rizatriptan ODTTablet, orally disintegrating10 mgOralNatco Pharma (Canada) Inc2015-02-17Not applicableCanada
PMS-rizatriptan RdtTablet, orally disintegrating10 mgOralPharmascience Inc2012-10-30Not applicableCanada
PMS-rizatriptan RdtTablet, orally disintegrating5 mgOralPharmascience Inc2012-10-30Not applicableCanada
Q-rizatriptan ODTTablet, orally disintegrating5 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-rizatriptan ODTTablet, orally disintegrating10 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Riva-rizatriptan ODTTablet, orally disintegrating5 mgOralLaboratoire Riva Inc2014-06-12Not applicableCanada
Riva-rizatriptan ODTTablet, orally disintegrating10 mgOralLaboratoire Riva Inc2014-06-12Not applicableCanada
RizaportFilm, soluble5 1/1OralRed Hill Biopharma Ltd.2016-08-01Not applicableUs
RizaportFilm, soluble10 1/1OralRed Hill Biopharma Ltd.2016-08-01Not applicableUs
RizatriptanTablet5 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
RizatriptanTablet10 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralPar Pharmaceutical Inc.1998-06-292018-04-30Us
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralPar Pharmaceutical Inc.1998-06-292018-01-31Us
Rizatriptan BenzoateTablet5 mg/1OralPar Pharmaceutical Inc.1998-06-292016-09-30Us
Rizatriptan BenzoateTablet10 mg/1OralPar Pharmaceutical Inc.1998-06-292016-09-30Us
Rizatriptan ODTTablet, orally disintegrating5 mgOralSivem Pharmaceuticals Ulc2015-10-07Not applicableCanada
Rizatriptan ODTTablet, orally disintegrating5 mgOralAbri Pharmaceuticals IncNot applicableNot applicableCanada
Rizatriptan ODTTablet, orally disintegrating10 mgOralSivem Pharmaceuticals Ulc2015-10-07Not applicableCanada
Rizatriptan ODTTablet, orally disintegrating10 mgOralSanis Health Inc2015-07-23Not applicableCanada
Rizatriptan ODTTablet, orally disintegrating10 mgOralAbri Pharmaceuticals IncNot applicableNot applicableCanada
Rizatriptan ODTTablet, orally disintegrating5 mgOralSanis Health Inc2015-07-23Not applicableCanada
Rizatriptan RdtTablet, orally disintegrating5 mgOralPro Doc Limitee2013-11-28Not applicableCanada
Rizatriptan RdtTablet, orally disintegrating10 mgOralPro Doc Limitee2013-11-28Not applicableCanada
Sandoz Rizatriptan ODTTablet, orally disintegrating5 mgOralSandoz Canada Incorporated2012-01-30Not applicableCanada
Sandoz Rizatriptan ODTTablet, orally disintegrating10 mgOralSandoz Canada Incorporated2012-01-30Not applicableCanada
Teva-rizatriptanTablet5 mgOralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rizatriptanTablet10 mgOralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rizatriptan ODTTablet, orally disintegrating10 mgOralTeva Canada Limited2014-11-04Not applicableCanada
Teva-rizatriptan ODTTablet, orally disintegrating5 mgOralTeva Canada Limited2014-11-04Not applicableCanada
Van-rizatriptanTablet10 mgOralVanc Pharmaceuticals Inc2015-07-23Not applicableCanada
Van-rizatriptanTablet5 mgOralVanc Pharmaceuticals Inc2015-07-23Not applicableCanada
Van-rizatriptan ODTTablet, orally disintegrating5 mgOralVanc Pharmaceuticals IncNot applicableNot applicableCanada
Van-rizatriptan ODTTablet, orally disintegrating10 mgOralVanc Pharmaceuticals Inc2016-04-18Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-rizatriptanTablet10 mgOralApotex Inc2012-09-27Not applicableCanada
Apo-rizatriptanTablet5 mgOralApotex Inc2013-03-06Not applicableCanada
Apo-rizatriptan RpdTablet, orally disintegrating5 mgOralApotex Inc2013-09-10Not applicableCanada
Apo-rizatriptan RpdTablet, orally disintegrating10 mgOralApotex Inc2013-09-10Not applicableCanada
RizatriptanTablet, film coated10 mg/1OralREMEDYREPACK INC.2015-06-08Not applicableUs
RizatriptanTablet, film coated10 mg/1OralPreferred Pharmaceuticals Inc.2015-08-18Not applicableUs
RizatriptanTablet, film coated5 mg/1OralMacleods Pharmaceuticals Limited2014-03-11Not applicableUs
RizatriptanTablet, film coated10 mg/1OralMacleods Pharmaceuticals Limited2014-03-11Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralPhysicians Total Care, Inc.2013-01-23Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralAurobindo Pharma Limited2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralSandoz Inc2013-02-11Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralMesource Pharmaceuticals2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralCipla USA Inc.2016-07-22Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralTeva Pharmaceuticals USA Inc2013-02-12Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralJubilant Cadista Pharmaceuticals Inc.2014-03-01Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralCamber Pharmaceuticals, Inc.2015-01-29Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralCitron Pharma LLC2012-12-31Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralAscend Laboratories, LLC2012-06-25Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralSandoz Inc2013-07-02Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralApotex Corp2013-07-01Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralBreckenridge Pharmaceutical, Inc.2012-12-31Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralGlenmark Pharmaceuticals Inc., Usa2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralPhysicians Total Care, Inc.2013-01-29Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralAurobindo Pharma Limited2013-07-01Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralHeritage Pharmaceuticals Inc.2013-12-12Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralProficient Rx LP2013-07-01Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralSun Pharma Global FZE2013-01-12Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralTeva Pharmaceuticals USA Inc2013-02-12Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralJubilant Cadista Pharmaceuticals Inc.2012-03-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralMacleods Pharmaceuticals Limited2014-09-23Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralCipla USA Inc.2013-03-26Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralCitron Pharma LLC2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralAscend Laboratories, LLC2012-06-25Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralSandoz Inc2013-07-02Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralApotex Corp2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralBreckenridge Pharmaceutical, Inc.2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralGlenmark Pharmaceuticals Inc., Usa2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralCitron Pharma LLC2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralAurobindo Pharma Limited2013-07-01Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralHeritage Pharmaceuticals Inc.2013-12-12Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralGlenmark Pharmaceuticals Inc., Usa2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralSun Pharma Global FZE2013-01-12Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating5 mg/1OralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralApotex Corp2012-12-29Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralMacleods Pharmaceuticals Limited2014-09-23Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralCipla USA Inc.2015-03-20Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralJubilant Cadista Pharmaceuticals Inc.2013-03-01Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralA S Medication Solutions2015-01-29Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralAurobindo Pharma Limited2012-12-31Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralSandoz Inc2013-02-11Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralREMEDYREPACK INC.2014-09-092016-04-05Us
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralBreckenridge Pharmaceutical, Inc.2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralCitron Pharma LLC2013-07-01Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralPreferred Pharmaceuuticals, Inc.2013-10-22Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralCamber Pharmaceuticals, Inc.2015-01-29Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralGlenmark Pharmaceuticals Inc., Usa2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralApotex Corp2012-12-29Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralBreckenridge Pharmaceutical, Inc.2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralA S Medication Solutions2013-02-12Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralA S Medication Solutions2012-12-31Not applicableUs
Rizatriptan BenzoateTablet, orally disintegrating10 mg/1OralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan BenzoateTablet5 mg/1OralCipla USA Inc.2016-07-22Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralMedsource Pharmaceuticals2012-12-31Not applicableUs
Rizatriptan BenzoateTablet10 mg/1OralJubilant Cadista Pharmaceuticals Inc.2014-03-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Maxalt MLTNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Rizatriptan benzoate
145202-66-0
Thumb
  • InChI Key: JPRXYLQNJJVCMZ-UHFFFAOYSA-N
  • Monoisotopic Mass: 391.200825065
  • Average Mass: 391.475
DBSALT001798
Categories
UNII51086HBW8G
CAS number144034-80-0
WeightAverage: 269.3449
Monoisotopic: 269.164045633
Chemical FormulaC15H19N5
InChI KeyULFRLSNUDGIQQP-UHFFFAOYSA-N
InChI
InChI=1S/C15H19N5/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3
IUPAC Name
dimethyl({2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethyl})amine
SMILES
CN(C)CCC1=CNC2=C1C=C(CN1C=NC=N1)C=C2
Pharmacology
IndicationFor treatment of acute migraine attacks with or without aura.
Structured Indications
PharmacodynamicsRizatriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists and has 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 Rizatriptan 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 Rizatriptan in humans.
Mechanism of actionThree distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.
TargetKindPharmacological actionActionsOrganismUniProt ID
5-hydroxytryptamine receptor 1DProteinyes
agonist
HumanP28221 details
5-hydroxytryptamine receptor 1BProteinyes
agonist
HumanP28222 details
5-hydroxytryptamine receptor 1FProteinyes
agonist
HumanP30939 details
Related Articles
AbsorptionRapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine attack.
Volume of distribution
  • 140 L [male]
  • 110 L [female]
Protein binding14%
Metabolism

Rizatriptan is metabolized by monoamine oxidase A isoenzyme (MAO-A) to an inactive indole acetic acid metabolite. In addition, several other inactive metabolites are formed. An active metabolite, N-monodesmethyl-rizatriptan, with pharmacological activity similar to that of the parent compound has been identified in small concentrations (14%) in the plasma.

SubstrateEnzymesProduct
Rizatriptan
Not Available
N-monodesmethyl-rizatriptanDetails
Route of eliminationApproximately 14% of an oral dose is excreted in urine as unchanged rizatriptan while 51% is excreted as indole acetic acid metabolite, indicating substantial first pass metabolism.
Half life2-3 hours
ClearanceNot Available
ToxicitySymptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.
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
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe metabolism of Rizatriptan can be decreased when combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.Experimental
AbirateroneThe serum concentration of Rizatriptan can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Aceprometazine.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Acetophenazine.Approved
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Rizatriptan.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Rizatriptan.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Rizatriptan.Approved
AmperozideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Amperozide.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Aripiprazole.Approved, Investigational
AsenapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Asenapine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Azaperone.Vet Approved
AzithromycinThe metabolism of Rizatriptan can be decreased when combined with Azithromycin.Approved
BenmoxinThe metabolism of Rizatriptan can be decreased when combined with Benmoxin.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Benperidol.Investigational
BifeprunoxThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Bifeprunox.Investigational
BortezomibThe metabolism of Rizatriptan can be decreased when combined with Bortezomib.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Brexpiprazole.Approved
BromocriptineBromocriptine may increase the vasoconstricting activities of Rizatriptan.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Bromperidol.Investigational
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Rizatriptan.Approved, Investigational
CabergolineCabergoline may increase the vasoconstricting activities of Rizatriptan.Approved
CaffeineThe metabolism of Rizatriptan can be decreased when combined with Caffeine.Approved
CarbamazepineThe metabolism of Rizatriptan can be increased when combined with Carbamazepine.Approved, Investigational
CariprazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Cariprazine.Approved
CaroxazoneThe metabolism of Rizatriptan can be decreased when combined with Caroxazone.Withdrawn
ChlorpromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Chlorpromazine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Chlorprothixene.Approved, Withdrawn
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Rizatriptan.Approved
ClomipramineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Rizatriptan can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Clozapine.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Cyamemazine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Rizatriptan.Approved
Cyproterone acetateThe serum concentration of Rizatriptan can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DapiprazoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Rizatriptan.Investigational
DeferasiroxThe serum concentration of Rizatriptan can be increased when it is combined with Deferasirox.Approved, Investigational
DesipramineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Desipramine.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Desvenlafaxine.Approved
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Rizatriptan.Approved
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Rizatriptan.Approved
DolasetronDolasetron may increase the serotonergic activities of Rizatriptan.Approved
DoxepinThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Doxepin.Approved
DroperidolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Droperidol.Approved, Vet Approved
DroxidopaRizatriptan may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Rizatriptan.Approved
EcopipamThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ecopipam.Investigational
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Rizatriptan.Approved, Investigational
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Rizatriptan.Approved
ErgonovineErgonovine may increase the vasoconstricting activities of Rizatriptan.Approved
ErgotamineErgotamine may increase the vasoconstricting activities of Rizatriptan.Approved
EscitalopramThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Escitalopram.Approved, Investigational
FencamfamineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Rizatriptan.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Rizatriptan.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fluphenazine.Approved
FluspirileneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fluspirilene.Approved
FluvoxamineThe metabolism of Rizatriptan can be decreased when combined with Fluvoxamine.Approved, Investigational
FrovatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Frovatriptan.Approved, Investigational
FurazolidoneThe metabolism of Rizatriptan can be decreased when combined with Furazolidone.Approved, Vet Approved
GranisetronGranisetron may increase the serotonergic activities of Rizatriptan.Approved, Investigational
HaloperidolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Haloperidol.Approved
HydracarbazineThe metabolism of Rizatriptan can be decreased when combined with Hydracarbazine.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Rizatriptan.Approved
IproclozideThe metabolism of Rizatriptan can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Rizatriptan can be decreased when combined with Iproniazid.Withdrawn
IsocarboxazidThe metabolism of Rizatriptan can be decreased when combined with Isocarboxazid.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Levomilnacipran.Approved
LidocaineThe metabolism of Rizatriptan 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 Rizatriptan.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lithium.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lorcaserin.Approved
LoxapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Loxapine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lurasidone.Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Rizatriptan.Approved
MebanazineThe metabolism of Rizatriptan can be decreased when combined with Mebanazine.Withdrawn
MelperoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Melperone.Approved
MesoridazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Mesoridazine.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Rizatriptan.Approved
MethotrimeprazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Methotrimeprazine.Approved
Methylene blueThe metabolism of Rizatriptan can be decreased when combined with Methylene blue.Investigational
MetoclopramideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Metoclopramide.Approved, Investigational
MexiletineThe metabolism of Rizatriptan can be decreased when combined with Mexiletine.Approved
MilnacipranThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Milnacipran.Approved
MinaprineThe metabolism of Rizatriptan can be decreased when combined with Minaprine.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Rizatriptan.Approved
MoclobemideThe metabolism of Rizatriptan can be decreased when combined with Moclobemide.Approved
MolindoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Molindone.Approved
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Rizatriptan.Approved, Investigational
NefazodoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Nefazodone.Approved, Withdrawn
NevirapineThe metabolism of Rizatriptan can be decreased when combined with Nevirapine.Approved
NialamideThe metabolism of Rizatriptan can be decreased when combined with Nialamide.Withdrawn
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Rizatriptan.Approved
OctamoxinThe metabolism of Rizatriptan can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Olanzapine.Approved, Investigational
OndansetronOndansetron may increase the serotonergic activities of Rizatriptan.Approved
OsanetantThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Rizatriptan can be decreased when it is combined with Osimertinib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Rizatriptan.Approved, Investigational
PargylineThe metabolism of Rizatriptan can be decreased when combined with Pargyline.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Rizatriptan.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Rizatriptan can be increased when it is combined with Peginterferon alfa-2b.Approved
PerazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Rizatriptan.Approved
PhenelzineThe metabolism of Rizatriptan can be decreased when combined with Phenelzine.Approved
PheniprazineThe metabolism of Rizatriptan can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe metabolism of Rizatriptan can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe metabolism of Rizatriptan can be decreased when combined with Phenoxypropazine.Withdrawn
PimozideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pimozide.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pipotiazine.Approved
PirlindoleThe metabolism of Rizatriptan can be decreased when combined with Pirlindole.Approved
PivhydrazineThe metabolism of Rizatriptan can be decreased when combined with Pivhydrazine.Withdrawn
PrimidoneThe metabolism of Rizatriptan can be increased when combined with Primidone.Approved, Vet Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Procarbazine.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Prochlorperazine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Promethazine.Approved
PropericiazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Propericiazine.Approved
PropranololThe serum concentration of Rizatriptan can be increased when it is combined with Propranolol.Approved, Investigational
ProthipendylThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Prothipendyl.Investigational
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Rizatriptan.Approved
QuetiapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Quetiapine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Raclopride.Investigational
RasagilineThe metabolism of Rizatriptan can be decreased when combined with Rasagiline.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Reserpine.Approved
RifampicinThe metabolism of Rizatriptan can be increased when combined with Rifampicin.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ritanserin.Investigational
RopiniroleThe metabolism of Rizatriptan can be decreased when combined with Ropinirole.Approved, Investigational
SafrazineThe metabolism of Rizatriptan can be decreased when combined with Safrazine.Withdrawn
SelegilineThe metabolism of Rizatriptan can be decreased when combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Sertindole.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Sertraline.Approved
SimeprevirThe metabolism of Rizatriptan can be decreased when combined with Simeprevir.Approved
SulpirideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Sulpiride.Approved
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Rizatriptan.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Tapentadol.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Rizatriptan.Approved
TenofovirThe metabolism of Rizatriptan can be decreased when combined with Tenofovir.Approved, Investigational
TeriflunomideThe serum concentration of Rizatriptan can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Rizatriptan can be decreased when combined with Theophylline.Approved
ThioproperazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thioproperazine.Approved
ThioridazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thioridazine.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Tiapride.Investigational
TiclopidineThe metabolism of Rizatriptan can be decreased when combined with Ticlopidine.Approved
ToloxatoneThe metabolism of Rizatriptan can be decreased when combined with Toloxatone.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Rizatriptan.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe metabolism of Rizatriptan can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe metabolism of Rizatriptan can be decreased when combined with Tranylcypromine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Rizatriptan.Approved, Investigational
TrifluoperazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Rizatriptan.Approved
TropisetronTropisetron may increase the serotonergic activities of Rizatriptan.Investigational
VemurafenibThe serum concentration of Rizatriptan 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 Rizatriptan.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Vilazodone.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Vortioxetine.Approved
ZiprasidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ziprasidone.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Rizatriptan.Approved, Investigational
ZotepineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Montserrat Armengol Asparo, Pere Dalmases Barjoan, “Process for preparing a rizatriptan.” U.S. Patent US20050148778, issued July 07, 2005.

US20050148778
General References
  1. Wellington K, Plosker GL: Rizatriptan: an update of its use in the management of migraine. Drugs. 2002;62(10):1539-74. [PubMed:12093318 ]
  2. Wellington K, Jarvis B: Spotlight on rizatriptan in migraine. CNS Drugs. 2002;16(10):715-20. [PubMed:12269863 ]
  3. Ikemoto F, Toru T, Aijima H, Natsumeda Y: [Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance]. Nihon Yakurigaku Zasshi. 2004 Apr;123(4):295-302. [PubMed:15056946 ]
  4. Villalon CM, Centurion D, Valdivia LF, De Vries P, Saxena PR: An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. [PubMed:12434581 ]
  5. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [PubMed:11152011 ]
External Links
ATC CodesN02CC04
AHFS Codes
  • 28:32.28
PDB EntriesNot Available
FDA labelDownload (873 KB)
MSDSDownload (57.7 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9406
Caco-2 permeable+0.5547
P-glycoprotein substrateSubstrate0.7478
P-glycoprotein inhibitor INon-inhibitor0.8752
P-glycoprotein inhibitor IINon-inhibitor0.7244
Renal organic cation transporterInhibitor0.7394
CYP450 2C9 substrateNon-substrate0.8572
CYP450 2D6 substrateNon-substrate0.6765
CYP450 3A4 substrateSubstrate0.5574
CYP450 1A2 substrateNon-inhibitor0.9149
CYP450 2C9 inhibitorNon-inhibitor0.9063
CYP450 2D6 inhibitorNon-inhibitor0.8913
CYP450 2C19 inhibitorNon-inhibitor0.9515
CYP450 3A4 inhibitorNon-inhibitor0.9688
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.956
Ames testAMES toxic0.5644
CarcinogenicityNon-carcinogens0.9133
BiodegradationNot ready biodegradable0.9439
Rat acute toxicity2.5433 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7051
hERG inhibition (predictor II)Non-inhibitor0.7265
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Merck and co inc
Packagers
Dosage forms
FormRouteStrength
TabletOral5 mg
TabletOral10 mg
TabletOral10 mg/1
TabletOral5 mg/1
Tablet, orally disintegratingOral10 mg
Tablet, orally disintegratingOral5 mg
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral5 mg/1
Film, solubleOral10 1/1
Film, solubleOral5 1/1
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
Prices
Unit descriptionCostUnit
Maxalt 12 10 mg tablet Box333.27USD box
Maxalt 12 5 mg tablet Box333.27USD box
Maxalt-MLT 3 5 mg Dispersible Tablet Box286.96USD box
Maxalt 9 5 mg tablet Box203.46USD box
Maxalt 6 5 mg tablet Box107.44USD box
Maxalt-MLT 3 10 mg Dispersible Tablet Box83.32USD box
Maxalt mlt 10 mg tablet26.7USD tablet
Maxalt mlt 5 mg tablet26.7USD tablet
Maxalt 10 mg tablet25.31USD tablet
Maxalt 5 mg tablet22.98USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2060139 No1998-12-012012-01-28Canada
US5298520 No1995-06-292012-06-29Us
US5602162 No1994-02-112014-02-11Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point178-180 °CNot Available
water solubility42 mg/mL (for free base)Not Available
logP1.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.338 mg/mLALOGPS
logP1.67ALOGPS
logP1.77ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)17.24ChemAxon
pKa (Strongest Basic)9.56ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area49.74 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity93.13 m3·mol-1ChemAxon
Polarizability30 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
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
  • 1,2,4-triazole
  • Pyrrole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Longmore J, Hargreaves RJ, Boulanger CM, Brown MJ, Desta B, Ferro A, Schofield WN, Taylor AA, Hill RG: Comparison of the vasoconstrictor properties of the 5-HT1D-receptor agonists rizatriptan (MK-462) and sumatriptan in human isolated coronary artery: outcome of two independent studies using different experimental protocols. Funct Neurol. 1997 Jan-Feb;12(1):3-9. [PubMed:9127118 ]
  3. Longmore J, Boulanger CM, Desta B, Hill RG, Schofield WN, Taylor AA: 5-HT1D receptor agonists and human coronary artery reactivity in vitro: crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519. Br J Clin Pharmacol. 1996 Oct;42(4):431-41. [PubMed:8904614 ]
  4. Sciberras DG, Polvino WJ, Gertz BJ, Cheng H, Stepanavage M, Wittreich J, Olah T, Edwards M, Mant T: Initial human experience with MK-462 (rizatriptan): a novel 5-HT1D agonist. Br J Clin Pharmacol. 1997 Jan;43(1):49-54. [PubMed:9056052 ]
  5. Williamson DJ, Hill RG, Shepheard SL, Hargreaves RJ: The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs. Br J Pharmacol. 2001 Aug;133(7):1029-34. [PubMed:11487512 ]
  6. Wackenfors A, Jarvius M, Ingemansson R, Edvinsson L, Malmsjo M: Triptans induce vasoconstriction of human arteries and veins from the thoracic wall. J Cardiovasc Pharmacol. 2005 May;45(5):476-84. [PubMed:15821444 ]
  7. Wellington K, Plosker GL: Rizatriptan: an update of its use in the management of migraine. Drugs. 2002;62(10):1539-74. [PubMed:12093318 ]
  8. Wellington K, Jarvis B: Spotlight on rizatriptan in migraine. CNS Drugs. 2002;16(10):715-20. [PubMed:12269863 ]
  9. Ikemoto F, Toru T, Aijima H, Natsumeda Y: [Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance]. Nihon Yakurigaku Zasshi. 2004 Apr;123(4):295-302. [PubMed:15056946 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. Wellington K, Plosker GL: Rizatriptan: an update of its use in the management of migraine. Drugs. 2002;62(10):1539-74. [PubMed:12093318 ]
  2. Wellington K, Jarvis B: Spotlight on rizatriptan in migraine. CNS Drugs. 2002;16(10):715-20. [PubMed:12269863 ]
  3. Ikemoto F, Toru T, Aijima H, Natsumeda Y: [Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance]. Nihon Yakurigaku Zasshi. 2004 Apr;123(4):295-302. [PubMed:15056946 ]
  4. Pauwels PJ, Palmier C, Dupuis DS, Colpaert FC: Interaction of 5-HT1B/D ligands with recombinant h 5-HT1A receptors: intrinsic activity and modulation by G-protein activation state. Naunyn Schmiedebergs Arch Pharmacol. 1998 May;357(5):490-9. [PubMed:9650800 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  6. Williamson DJ, Hill RG, Shepheard SL, Hargreaves RJ: The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs. Br J Pharmacol. 2001 Aug;133(7):1029-34. [PubMed:11487512 ]
  7. Wackenfors A, Jarvius M, Ingemansson R, Edvinsson L, Malmsjo M: Triptans induce vasoconstriction of human arteries and veins from the thoracic wall. J Cardiovasc Pharmacol. 2005 May;45(5):476-84. [PubMed:15821444 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and 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 cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1F
Uniprot ID:
P30939
Molecular Weight:
41708.505 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Villalon CM, Centurion D, Valdivia LF, de Vries P, Saxena PR: Migraine: pathophysiology, pharmacology, treatment and future trends. Curr Vasc Pharmacol. 2003 Mar;1(1):71-84. [PubMed:15320857 ]
  3. Villalon CM, Centurion D, Valdivia LF, De Vries P, Saxena PR: An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. [PubMed:12434581 ]
  4. Wainscott DB, Johnson KW, Phebus LA, Schaus JM, Nelson DL: Human 5-HT1F receptor-stimulated [35S]GTPgammaS binding: correlation with inhibition of guinea pig dural plasma protein extravasation. Eur J Pharmacol. 1998 Jul 3;352(1):117-24. [PubMed:9718276 ]
  5. Goadsby PJ, Classey JD: Evidence for serotonin (5-HT)1B, 5-HT1D and 5-HT1F receptor inhibitory effects on trigeminal neurons with craniovascular input. Neuroscience. 2003;122(2):491-8. [PubMed:14614913 ]

Enzymes

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. Iwasa T, Sano H, Sugiura A, Uchiyama N, Hara K, Okochi H, Nakagawa K, Yasumori T, Ishizaki T: An in vitro interethnic comparison of monoamine oxidase activities between Japanese and Caucasian livers using rizatriptan, a serotonin receptor 1B/1D agonist, as a model drug. Br J Clin Pharmacol. 2003 Nov;56(5):537-44. [PubMed:14651728 ]
  2. Van Haarst AD, Van Gerven JM, Cohen AF, De Smet M, Sterrett A, Birk KL, Fisher AL, De Puy ME, Goldberg MR, Musson DG: The effects of moclobemide on the pharmacokinetics of the 5-HT1B/1D agonist rizatriptan in healthy volunteers. Br J Clin Pharmacol. 1999 Aug;48(2):190-6. [PubMed:10417495 ]
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. Sternieri E, Coccia CP, Pinetti D, Ferrari A: Pharmacokinetics and interactions of headache medications, part I: introduction, pharmacokinetics, metabolism and acute treatments. Expert Opin Drug Metab Toxicol. 2006 Dec;2(6):961-79. [PubMed:17125411 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23