Generic
Rizatriptan
5 brands available in the market
At a glance
Rizatriptan is a prescription medicine used for the acute treatment of migraine attacks with or without aura. It relieves migraine headache, nausea, and sensitivity to light and sound by constricting blood vessels in the brain.
Description
Rizatriptan is a selective 5-HT1B/1D receptor agonist. It causes vasoconstriction of intracranial extracerebral blood vessels and inhibits nociceptive neurotransmission in trigeminal pain pathways, reducing migraine pain and associated inflammation.
Indications
- Acute migraine attacks (with or without aura)
Therapeutic class
5-HT Agonists
Pharmacological class
Selective Serotonin Receptor Agonist (5-HT1B/1D)
Pharmacology
Rizatriptan binds with high affinity to 5-HT1B receptors on intracranial blood vessels and 5-HT1D receptors on trigeminal sensory nerves. It constricts dilated intracranial vessels and inhibits the release of vasoactive neuropeptides, reducing neurogenic inflammation and migraine pain.
Mechanism of action
Agonist at 5-HT1B/1D receptors causing vasoconstriction and reducing neurogenic inflammation.
Dosage
Adult Dose (Oral):
- Initial: 10 mg (for a single attack); if ineffective, do not take a second dose for the same attack
- Recurrence: 10 mg if symptoms return (at least 2 hours apart)
- Maximum: 30 mg/24 hours (or 20 mg/24 hours if taking propranolol)
- With propranolol: 5 mg (max 3 doses/24 hours)
- Mild-moderate hepatic/renal impairment: Start with 5 mg (may repeat 5 mg after 2 hours); max 10 mg/24 hours
Administration
- Swallow tablets whole; do not chew, crush, or break
- May take with or without food (fixed time is better)
- Orally disintegrating tablet: Place on tongue; it dissolves and is swallowed with saliva
Missed dose
If you miss a dose, take it as soon as you remember; if it's almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Dizziness and somnolence
- Dry mouth
- Throat, jaw, and neck pain
- Paresthesia (tingling or pricking sensation)
- Weakness and heaviness
- Nausea
Precautions & warnings
- Do not use in patients with history of MI, ischemic heart disease, or Prinzmetal's angina
- Do not use in uncontrolled hypertension
- Do not use in basilar or hemiplegic migraine
- May affect driving ability (drowsiness and dizziness)
- Risk of serotonin syndrome (caution with SSRIs)
Contraindications
- Ischemic heart disease or coronary artery vasospasm
- Uncontrolled hypertension
- Hypersensitivity to rizatriptan or any component
- Severe hepatic or renal impairment
- Age <18 years
- Use of or within 2 weeks of stopping MAOI therapy
Drug interactions
- Propranolol: Increases serum concentration of rizatriptan (use 5 mg dose)
- Ergotamine and methysergide: Increased risk of vasospastic reactions
- SSRIs: Increased risk of serotonin syndrome
- MAOIs: Potentially fatal interaction (avoid)
Food interactions
Caution is advised when consuming alcohol with Rizatriptan; consult your doctor.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; use only if clearly needed; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited data suggests no significant risk to the baby; caution advised; consult your doctor.
Pediatric use
Safety and efficacy not established in patients <18 years; use not recommended.
Geriatric use
Elderly (≥65 years) have similar pharmacokinetics to younger adults; clinical experience is limited as migraine is infrequent in elderly.
Renal / hepatic impairment
Renal Impairment: Caution in severe kidney disease; dose adjustment may be needed; avoid in severe impairment; consult your doctor.
Hepatic Impairment: Start with 5 mg in mild-moderate liver disease; avoid in severe impairment; consult your doctor.
Overdose effects
Overdose may cause dizziness and somnolence; severe cases may cause hypertension and cardiovascular symptoms; consider gastrointestinal decontamination and activated charcoal.
Storage conditions
Store in a cool and dry place below 30°C, protected from light; keep out of reach of children.
Chemical structure
Rizatriptan