rizatriptan (Maxalt, Maxalt-MLT)

Introduction

Tradenames: Maxalt, Maxalt-MLT. Rizatriptan benzoate.

Indications

migraine headache

Contraindications

• concurrent use of MAO inhibitor (use 2 week washout)

Dosage

• 5-10 mg PO, may repeat in 2 hours
• maximum: 30 mg QD

Tabs: 5, 10 mg

Sublingual: Maxalt MLT

Pharmacokinetics

• onset of action faster than other triptans
• metabolized via monoamine oxidase

elimination via liver

1/2life = 2-3 hours

protein binding = 14 %

Adverse effects

• most common (1-10%)
  • paresthesia, chest pressure, neck, throat or jaw pain, dry mouth, nausea, dizziness, somnolence, asthenia, fatigue, tachycardia, hypertension, diarrhea, palpitations, constipation, flatulence, tongue edema, decreased mental accuity, euphoria, tremor, dyspnea, flushing, hot flashes
• uncommon (< 1%)
  • myalgia, arthralgia, muscle spasm, nasal congestion, epistaxis, blurred vision, tinnitus, dry eyes, pruritus, rash, urticaria, polyuria
• rare
  • coronary artery vasospasm
  • transient myocardial ischemia
  • myocardial infarction
  • ventricular tachycardia
  • ventricular fibrillation
• overdose
  • syncope
  • bradycardia
  • vomiting
  • 3rd degree AV block
• frequent use may exacerbate migraines

• drug adverse effects of triptan(s)

Drug interactions

• concurrent use of propranolol may increase levels of rizatriptan: reduce dose of rizatriptan

• drug interaction(s) of triptans with SNRIs
• drug interaction(s) of triptans with SSRIs
• drug interaction(s) of methylene blue with serotonin agonists
• drug interaction(s) of linezolid with serotonin agonists

More general terms

• serotonin agonist (5-HT receptor agonist, triptan)
• indole
• amine

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5078
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=77997
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3038519