Rizatriptan

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Rizatriptan
Rizatriptan.svg
Systematic (IUPAC) name
N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
Clinical data
Trade namesMaxalt
AHFS/Drugs.commonograph
MedlinePlusa601109
Pregnancy cat.
Legal status
  • Prescription only
RoutesOral
Pharmacokinetic data
Bioavailability45%
Protein binding14%
Metabolismby monoamine oxidase
Half-life2–3 hours
Excretion82% urine; 12% faeces
Identifiers
CAS number145202-66-0 YesY
ATC codeN02CC04
PubChemCID 5078
IUPHAR ligand51
DrugBankDB00953
ChemSpider4900 YesY
UNIIWR978S7QHH YesY
KEGGD00675 N
ChEBICHEBI:48273 YesY
ChEMBLCHEMBL905 YesY
Chemical data
FormulaC15H19N5 
Mol. mass269.345 g/mol
 N (what is this?)  (verify)
 
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Rizatriptan
Rizatriptan.svg
Systematic (IUPAC) name
N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
Clinical data
Trade namesMaxalt
AHFS/Drugs.commonograph
MedlinePlusa601109
Pregnancy cat.
Legal status
  • Prescription only
RoutesOral
Pharmacokinetic data
Bioavailability45%
Protein binding14%
Metabolismby monoamine oxidase
Half-life2–3 hours
Excretion82% urine; 12% faeces
Identifiers
CAS number145202-66-0 YesY
ATC codeN02CC04
PubChemCID 5078
IUPHAR ligand51
DrugBankDB00953
ChemSpider4900 YesY
UNIIWR978S7QHH YesY
KEGGD00675 N
ChEBICHEBI:48273 YesY
ChEMBLCHEMBL905 YesY
Chemical data
FormulaC15H19N5 
Mol. mass269.345 g/mol
 N (what is this?)  (verify)

Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the treatment of migraine headaches.[1] It is available in strengths of 5 and 10 mg as tablets and orally disintegrating tablets (Maxalt-MLT).

Maxalt obtained approval by the United States Food and Drug Administration (FDA) on June 29, 1998. It is a second-generation triptan.

Rizatriptan is available only by prescription in Australia, Finland, the United States, Canada and New Zealand. Similarly, it is classed as a POM (Prescription Only Medicine) in the United Kingdom, Italy (as Rizaliv), Israel (as Rizalt), The Netherlands, Croatia and Spain (as Maxalt).

Indications[edit]

Rizatriptan is FDA-approved to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks.[1] Rizatriptan is also used off-label to treat cluster headaches.

Contraindications[edit]

Adverse effects[edit]

Mechanism of action[edit]

Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors.[2] Like the other triptans sumatriptan and zolmitriptan, rizatriptan induces vasoconstriction—possibly by inhibiting the release of calcitonin gene-related peptide from sensory neurons in the trigeminal nerve.[2]

References[edit]

  1. ^ a b "Rizatriptan". MedlinePlus. U.S. National Library of Medicine. 
  2. ^ a b Wellington, K; Plosker, G. L. (2002). "Rizatriptan: An update of its use in the management of migraine". Drugs 62 (10): 1539–74. doi:10.2165/00003495-200262100-00007. PMID 12093318.  edit

External links[edit]