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Rizatriptan

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. More

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Description

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.

Generic Name

Rizatriptan

Chemical names

Rizatriptan; 144034-80-0; Risatriptan; MK 462 free base; 2-(5-((1H-1,2,4-Triazol-1-yl)methyl)-1H-indol-3-yl)-N,N-dimethylethanamine

Brand names

Maxalt-RPD, Migsun, Ritza, Rizact, Rizatan

IUPAC name

dimethyl({2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethyl})amine

Pharmacokinetics

Rapid following oral administration. 

Actions

Rizatriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors.

Dosage/Dosage form

The recommended initial dose is 5 to 10mg, oral. If symptoms recur after initial response, a further dose of 10 mg may be given. Separate doses by at least 2 hour. Maximum: 30 mg/24 hour.

Therapeutic uses

For treatment of acute migraine attacks with or without aura.

Adverse effects/Side effects

Dry mouth; chest pain, increased BP, palpitation; dyspnoea; skin flushing; nausea, abdominal pain, drowsiness, dizziness, fatigue.

Interaction

  • Increased serum concentrations with propranolol.
  • Increased risk of vasospastic reactions when used with ergotamine and methysergide.
  • Concurrent use with or within 2 wk of stopping MAOI treatment.
  • Concurrent use with St John's wort may increase risk of adverse reactions.
  • Concurrent use with SSRIs may increase risk of serotonin syndrome.

Contraindications

  • History of MI, peripheral vascular disease, transient ishaemic attack, ischaemic heart disease or Prinzmetal's angina; uncontrolled hypertension; basilar or hemiplegic migraine; severe hepatic or renal impairment.
  • Adolescent <18 years.

Storage

Store at 15-30°C

Information

Molecular weight

269.3449

Molecular formula

C15H19N5

CAS number

144034-80-0

Precautions

  • Elderly; mild to moderate hepatic or renal impairment; coronary artery disease; pregnancy, lactation.
  • May cause drowsiness.
  • History of seizures.
  • Ensure an interval of at least 24 hours after stopping an ergotamine compound and starting a serotonin (5-HT1) agonist.