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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 Rizatriptantablet5 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Act Rizatriptantablet10 mgoralActavis Pharma Company2012-06-14Not applicableCanada
Act Rizatriptan ODTtablet (orally disintegrating)5 mgoralActavis Pharma Company2012-01-30Not applicableCanada
Act Rizatriptan ODTtablet (orally disintegrating)10 mgoralActavis Pharma Company2012-01-30Not applicableCanada
Auro-rizatriptantablet10 mgoralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-rizatriptan ODTtablet (orally disintegrating)5 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-rizatriptan ODTtablet (orally disintegrating)10 mgoralAuro Pharma IncNot applicableNot applicableCanada
Dom-rizatriptan Rdttablet (orally disintegrating)5 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-rizatriptan Rdttablet (orally disintegrating)10 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
Maxalttablet5 mgoralMerck Canada Inc1999-08-312013-07-15Canada
Maxalttablet10 mg/1oralSTAT Rx USA LLC1998-06-29Not applicableUs
Maxalttablet10 mg/1oralRebel Distributors Corp1998-06-29Not applicableUs
Maxalt Rpdtablet (orally disintegrating)10 mgoralMerck Canada Inc1999-08-31Not applicableCanada
Maxalt Rpdtablet (orally disintegrating)5 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 disintegrating)10 mgoralMint Pharmaceuticals Inc2015-06-10Not applicableCanada
Mint-rizatriptan ODTtablet (orally disintegrating)5 mgoralMint Pharmaceuticals Inc2015-06-10Not applicableCanada
Mylan-rizatriptantablet5 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-rizatriptantablet10 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-rizatriptan ODTtablet (orally disintegrating)5 mgoralMylan Pharmaceuticals Ulc2012-01-31Not applicableCanada
Mylan-rizatriptan ODTtablet (orally disintegrating)10 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 disintegrating)5 mgoralNatco Pharma (Canada) Inc2015-02-17Not applicableCanada
Nat-rizatriptan ODTtablet (orally disintegrating)10 mgoralNatco Pharma (Canada) Inc2015-02-17Not applicableCanada
PMS-rizatriptan Rdttablet (orally disintegrating)10 mgoralPharmascience Inc2012-10-30Not applicableCanada
PMS-rizatriptan Rdttablet (orally disintegrating)5 mgoralPharmascience Inc2012-10-30Not applicableCanada
Q-rizatriptan ODTtablet (orally disintegrating)5 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-rizatriptan ODTtablet (orally disintegrating)10 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Riva-rizatriptan ODTtablet (orally disintegrating)5 mgoralLaboratoire Riva Inc2014-06-12Not applicableCanada
Riva-rizatriptan ODTtablet (orally disintegrating)10 mgoralLaboratoire Riva Inc2014-06-12Not applicableCanada
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 disintegrating)5 mgoralSivem Pharmaceuticals Ulc2015-10-07Not applicableCanada
Rizatriptan ODTtablet (orally disintegrating)5 mgoralAbri Pharmaceuticals IncNot applicableNot applicableCanada
Rizatriptan ODTtablet (orally disintegrating)10 mgoralSivem Pharmaceuticals Ulc2015-10-07Not applicableCanada
Rizatriptan ODTtablet (orally disintegrating)10 mgoralSanis Health Inc2015-07-23Not applicableCanada
Rizatriptan ODTtablet (orally disintegrating)10 mgoralAbri Pharmaceuticals IncNot applicableNot applicableCanada
Rizatriptan ODTtablet (orally disintegrating)5 mgoralSanis Health Inc2015-07-23Not applicableCanada
Rizatriptan Rdttablet (orally disintegrating)5 mgoralPro Doc Limitee2013-11-28Not applicableCanada
Rizatriptan Rdttablet (orally disintegrating)10 mgoralPro Doc Limitee2013-11-28Not applicableCanada
Sandoz Rizatriptan ODTtablet (orally disintegrating)5 mgoralSandoz Canada Incorporated2012-01-30Not applicableCanada
Sandoz Rizatriptan ODTtablet (orally disintegrating)10 mgoralSandoz Canada Incorporated2012-01-30Not applicableCanada
Teva-rizatriptantablet5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rizatriptantablet10 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rizatriptan ODTtablet (orally disintegrating)10 mgoralTeva Canada Limited2014-11-04Not applicableCanada
Teva-rizatriptan ODTtablet (orally disintegrating)5 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 disintegrating)5 mgoralVanc Pharmaceuticals IncNot applicableNot applicableCanada
Van-rizatriptan ODTtablet (orally disintegrating)10 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 disintegrating)5 mgoralApotex Inc2013-09-10Not applicableCanada
Apo-rizatriptan Rpdtablet (orally disintegrating)10 mgoralApotex Inc2013-09-10Not applicableCanada
Rizatriptantablet, film coated10 mg/1oralPreferred Pharmaceuticals Inc.2015-08-18Not applicableUs
Rizatriptantablet, film coated10 mg/1oralMacleods Pharmaceuticals Limited2014-03-11Not applicableUs
Rizatriptantablet, film coated10 mg/1oralREMEDYREPACK INC.2015-06-08Not applicableUs
Rizatriptantablet, film coated5 mg/1oralMacleods Pharmaceuticals Limited2014-03-11Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralSandoz Inc2013-07-02Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralApotex Corp2012-12-29Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralBreckenridge Pharmaceutical, Inc.2012-12-31Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralAscend Laboratories, LLC2016-02-19Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralTeva Pharmaceuticals USA Inc2013-02-12Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralCitron Pharma LLC2012-12-31Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralAurobindo Pharma Limited2013-07-01Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralPhysicians Total Care, Inc.2013-01-23Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralHeritage Pharmaceuticals Inc.2013-12-12Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2013-07-01Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralMesource Pharmaceuticals2012-12-31Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-03-01Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralBreckenridge Pharmaceutical, Inc.2012-12-31Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralSandoz Inc2013-02-11Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralApotex Corp2013-07-01Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralCipla USA Inc.2013-03-26Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralMacleods Pharmaceuticals Limited2014-09-23Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralA S Medication Solutions2013-02-12Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralTeva Pharmaceuticals USA Inc2013-02-12Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralCitron Pharma LLC2012-12-31Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralAurobindo Pharma Limited2013-07-01Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralCamber Pharmaceuticals, Inc.2015-01-29Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralProficient Rx LP2013-07-01Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralPhysicians Total Care, Inc.2013-01-29Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralJubilant Cadista Pharmaceuticals Inc.2012-03-01Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralGlenmark Pharmaceuticals Inc., Usa2013-07-01Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralSun Pharma Global FZE2013-01-12Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralBreckenridge Pharmaceutical, Inc.2013-07-01Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralSandoz Inc2013-02-11Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralApotex Corp2013-07-01Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralCipla USA Inc.2015-03-20Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralMacleods Pharmaceuticals Limited2014-09-23Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralJubilant Cadista Pharmaceuticals Inc.2013-03-01Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2012-12-31Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralCamber Pharmaceuticals, Inc.2015-01-29Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralAurobindo Pharma Limited2012-12-31Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralCitron Pharma LLC2013-07-01Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating5 mg/1oralSandoz Inc2013-07-02Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralApotex Corp2012-12-29Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralPreferred Pharmaceuuticals, Inc.2013-10-22Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralSun Pharma Global FZE2013-01-12Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralBreckenridge Pharmaceutical, Inc.2013-07-01Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralHeritage Pharmaceuticals Inc.2013-12-12Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralREMEDYREPACK INC.2014-09-092016-04-05Us
Rizatriptan Benzoatetablet10 mg/1oralMedsource Pharmaceuticals2012-12-31Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralMylan Pharmaceuticals Inc.2012-12-31Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-03-01Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralGlenmark Pharmaceuticals Inc., Usa2012-12-31Not applicableUs
Rizatriptan Benzoatetablet10 mg/1oralAurobindo Pharma Limited2012-12-31Not applicableUs
Rizatriptan Benzoatetablet5 mg/1oralAscend Laboratories, LLC2016-02-19Not applicableUs
Rizatriptan Benzoatetablet, orally disintegrating10 mg/1oralCitron Pharma LLC2013-07-01Not 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 KeyInChIKey=ULFRLSNUDGIQQP-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
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
Pharmacology
IndicationFor treatment of acute migraine attacks with or without aura.
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.
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
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/1
Tabletoral10 mg
Tabletoral5 mg/1
Tablet (orally disintegrating)oral10 mg
Tablet (orally disintegrating)oral5 mg
Tablet, orally disintegratingoral10 mg/1
Tablet, orally disintegratingoral5 mg/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
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)
Interactions
Drug Interactions
Drug
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.
AbirateroneThe serum concentration of Rizatriptan can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Aceprometazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Acetophenazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Rizatriptan.
AmisulprideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Rizatriptan.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Rizatriptan.
AmperozideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Amperozide.
AripiprazoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Aripiprazole.
AsenapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Asenapine.
AzaperoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Azaperone.
AzithromycinThe metabolism of Rizatriptan can be decreased when combined with Azithromycin.
BenmoxinThe metabolism of Rizatriptan can be decreased when combined with Benmoxin.
BifeprunoxThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Bifeprunox.
BortezomibThe metabolism of Rizatriptan can be decreased when combined with Bortezomib.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Brexpiprazole.
BromocriptineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Bromocriptine.
BromocriptineBromocriptine may increase the vasoconstricting activities of Rizatriptan.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Rizatriptan.
CabergolineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Cabergoline.
CabergolineCabergoline may increase the vasoconstricting activities of Rizatriptan.
CaffeineThe metabolism of Rizatriptan can be decreased when combined with Caffeine.
CarbamazepineThe metabolism of Rizatriptan can be increased when combined with Carbamazepine.
CariprazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Cariprazine.
CaroxazoneThe metabolism of Rizatriptan can be decreased when combined with Caroxazone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Chlorprothixene.
CitalopramThe metabolism of Rizatriptan can be decreased when combined with Citalopram.
CitalopramThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Citalopram.
ClomipramineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Clomipramine.
ClotrimazoleThe metabolism of Rizatriptan can be decreased when combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Clozapine.
CyamemazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Cyamemazine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Rizatriptan.
Cyproterone acetateThe serum concentration of Rizatriptan can be decreased when it is combined with Cyproterone acetate.
DapiprazoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Dapiprazole.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Rizatriptan.
DeferasiroxThe serum concentration of Rizatriptan can be increased when it is combined with Deferasirox.
DesipramineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Desipramine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Desvenlafaxine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Rizatriptan.
DihydroergotamineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Dihydroergotamine.
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Rizatriptan.
DolasetronDolasetron may increase the serotonergic activities of Rizatriptan.
DoxepinThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Doxepin.
DroperidolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Droperidol.
DroxidopaRizatriptan may increase the hypertensive activities of Droxidopa.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Rizatriptan.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Rizatriptan.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ergoloid mesylate.
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Rizatriptan.
ErgonovineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ergonovine.
ErgonovineErgonovine may increase the vasoconstricting activities of Rizatriptan.
ErgotamineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ergotamine.
ErgotamineErgotamine may increase the vasoconstricting activities of Rizatriptan.
EscitalopramThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Escitalopram.
FencamfamineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fencamfamine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Rizatriptan.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Rizatriptan.
FlupentixolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fluspirilene.
FluvoxamineThe metabolism of Rizatriptan can be decreased when combined with Fluvoxamine.
FluvoxamineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Fluvoxamine.
FrovatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Frovatriptan.
FurazolidoneThe metabolism of Rizatriptan can be decreased when combined with Furazolidone.
GranisetronGranisetron may increase the serotonergic activities of Rizatriptan.
HaloperidolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Haloperidol.
HydracarbazineThe metabolism of Rizatriptan can be decreased when combined with Hydracarbazine.
IloperidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Rizatriptan.
IproclozideThe metabolism of Rizatriptan can be decreased when combined with Iproclozide.
IproniazidThe metabolism of Rizatriptan can be decreased when combined with Iproniazid.
IsocarboxazidThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Isocarboxazid.
IsocarboxazidThe metabolism of Rizatriptan can be decreased when combined with Isocarboxazid.
LevomilnacipranThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Levomilnacipran.
LidocaineThe metabolism of Rizatriptan can be decreased when combined with Lidocaine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Rizatriptan.
LithiumThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lithium.
LorcaserinThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lorcaserin.
LoxapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Loxapine.
LurasidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lurasidone.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Rizatriptan.
MebanazineThe metabolism of Rizatriptan can be decreased when combined with Mebanazine.
MelperoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Melperone.
MesoridazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Mesoridazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Rizatriptan.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Methotrimeprazine.
Methylene blueThe metabolism of Rizatriptan can be decreased when combined with Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Metoclopramide.
MexiletineThe metabolism of Rizatriptan can be decreased when combined with Mexiletine.
MilnacipranThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Milnacipran.
MinaprineThe metabolism of Rizatriptan can be decreased when combined with Minaprine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Rizatriptan.
MoclobemideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Moclobemide.
MoclobemideThe metabolism of Rizatriptan can be decreased when combined with Moclobemide.
MolindoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Molindone.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Rizatriptan.
NefazodoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Nefazodone.
NevirapineThe metabolism of Rizatriptan can be decreased when combined with Nevirapine.
NialamideThe metabolism of Rizatriptan can be decreased when combined with Nialamide.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Rizatriptan.
OctamoxinThe metabolism of Rizatriptan can be decreased when combined with Octamoxin.
OlanzapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ondansetron.
OndansetronOndansetron may increase the serotonergic activities of Rizatriptan.
OsanetantThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Osanetant.
OsimertinibThe serum concentration of Rizatriptan can be decreased when it is combined with Osimertinib.
PaliperidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Paliperidone.
PalonosetronPalonosetron may increase the serotonergic activities of Rizatriptan.
PargylineThe metabolism of Rizatriptan can be decreased when combined with Pargyline.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Rizatriptan.
Peginterferon alfa-2bThe serum concentration of Rizatriptan can be increased when it is combined with Peginterferon alfa-2b.
PerospironeThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Perospirone.
PerphenazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Perphenazine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Rizatriptan.
PhenelzineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Phenelzine.
PhenelzineThe metabolism of Rizatriptan can be decreased when combined with Phenelzine.
PheniprazineThe metabolism of Rizatriptan can be decreased when combined with Pheniprazine.
PhenobarbitalThe metabolism of Rizatriptan can be increased when combined with Phenobarbital.
PhenoxypropazineThe metabolism of Rizatriptan can be decreased when combined with Phenoxypropazine.
PimozideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pimozide.
PipamperoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pipamperone.
PipotiazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pipotiazine.
PirlindoleThe metabolism of Rizatriptan can be decreased when combined with Pirlindole.
PivhydrazineThe metabolism of Rizatriptan can be decreased when combined with Pivhydrazine.
PrimidoneThe metabolism of Rizatriptan can be increased when combined with Primidone.
ProcarbazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Procarbazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Promazine.
PromethazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Promethazine.
PropericiazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Propericiazine.
PropranololThe serum concentration of Rizatriptan can be increased when it is combined with Propranolol.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Rizatriptan.
QuetiapineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Quetiapine.
RasagilineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Rasagiline.
RasagilineThe metabolism of Rizatriptan can be decreased when combined with Rasagiline.
RemoxiprideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Reserpine.
RifampicinThe metabolism of Rizatriptan can be increased when combined with Rifampicin.
RisperidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Risperidone.
RopiniroleThe metabolism of Rizatriptan can be decreased when combined with Ropinirole.
SafrazineThe metabolism of Rizatriptan can be decreased when combined with Safrazine.
SelegilineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Selegiline.
SelegilineThe metabolism of Rizatriptan can be decreased when combined with Selegiline.
SertindoleThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Sertraline.
SimeprevirThe metabolism of Rizatriptan can be decreased when combined with Simeprevir.
SulpirideThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Rizatriptan.
TapentadolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Tapentadol.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Rizatriptan.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Tedizolid Phosphate.
TenofovirThe metabolism of Rizatriptan can be decreased when combined with Tenofovir.
TeriflunomideThe serum concentration of Rizatriptan can be decreased when it is combined with Teriflunomide.
TheophyllineThe metabolism of Rizatriptan can be decreased when combined with Theophylline.
ThioproperazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thioproperazine.
ThioridazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thiothixene.
TiclopidineThe metabolism of Rizatriptan can be decreased when combined with Ticlopidine.
ToloxatoneThe metabolism of Rizatriptan can be decreased when combined with Toloxatone.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Rizatriptan.
Trans-2-PhenylcyclopropylamineThe metabolism of Rizatriptan can be decreased when combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Tranylcypromine.
TranylcypromineThe metabolism of Rizatriptan can be decreased when combined with Tranylcypromine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Rizatriptan.
TrifluoperazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Triflupromazine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Rizatriptan.
VemurafenibThe serum concentration of Rizatriptan can be increased when it is combined with Vemurafenib.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Rizatriptan.
VilazodoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Vortioxetine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Ziprasidone.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Rizatriptan.
ZotepineThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Zotepine.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Zuclopenthixol.
Food InteractionsNot Available

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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23