Rizatriptan Benzoate is indicated for the acute treatment of migraine attacks with or without aura in adults.

Migraine pathophysiology involves multiple physiological and molecular mechanisms. Dilation of intracranial extracerebral blood vessels, especially those supplying the dura mater, is associated with migraine pain. Activation of the trigeminovascular system leads to release of vasoactive neuropeptides from trigeminal nerves, causing neurogenic inflammation and vasodilation. Migraine-related nausea and vomiting are believed to result from activation of central and nociceptive pathways projecting to brainstem and cortical pain centers. Serotonin (5-HT) imbalance is also involved, where 5-HT interacts with 5-HT1B and 5-HT1D receptors to influence vascular tone and trigeminal nerve activity.

Rizatriptan is a selective agonist of 5-HT1B and 5-HT1D receptors located on cranial blood vessels and trigeminal sensory nerves. It binds with high affinity to these receptors. Although the exact mechanism is not fully understood, its antimigraine effect is thought to involve: Vasoconstriction of intracranial blood vessels via 5-HT1B receptors, Inhibition of trigeminal nociceptive transmission, Reduction of vasoactive neuropeptide release via 5-HT1D receptors Animal studies also show inhibition of dural vasodilation and plasma protein leakage.

Single doses of 5 or 10 mg of Rizatriptan Tablets is indicated for the acute treatment of migraines in adults. Doses should be separated by at least 2 hours; no more than 30 mg should be taken in any 24-hour period.

Dosage adjustment for special case: The choice of dose should therefore be made on an individual basis, weighing the possible benefit of the 10-mg dose with the potential risk for increased adverse events. The safety of treating, on average, more than four headaches in a 30-day period has not been established. Patients receiving propranolol: In patients receiving propranolol, the 5-mg dose of Rizatriptan should be used, up to a maximum of 3 doses in any 24-hour period.

Administration of Rizatriptan Benzoate Tablets, administration with liquid is not necessary. Orally disintegrating tablets are packaged in a blister within an outer aluminum pouch and patients should not remove the blister from the outer pouch until just prior to dosing. The blister pack should then be peeled open with dry hands and the orally disintegrating tablet placed on the tongue, where it will dissolve and be swallowed with the saliva.

Rizatriptan 5 mg should be used in patients taking propranolol. Concomitant use of ergotamine-containing or ergot-type drugs (e.g., dihydroergotamine or methysergide) within 24 hours of rizatriptan is contraindicated. Co-administration of rizatriptan with other 5-HT1 agonists within 24 hours is not recommended. Rizatriptan should not be used in patients receiving MAO-A inhibitors or non-selective MAO inhibitors.

Rizatriptan Benzoate is contraindicated in patients with ischemic heart disease (e.g., angina, history of myocardial infarction, or silent ischemia) or symptoms suggestive of coronary artery disease, coronary vasospasm including Prinzmetal’s angina, or other significant cardiovascular disease. It is also contraindicated in uncontrolled hypertension. Hypersensitivity to rizatriptan or any excipients is another contraindication.

Cardiac events are rare but may occur, especially in patients with cardiovascular risk factors. Reported events include coronary vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation. Other uncommon effects include chills, heat sensitivity, facial edema, abdominal distension, fever, orthostatic effects, syncope, and swelling.

There are no adequate controlled studies in pregnant women. Rizatriptan should be used only if clearly needed. It is unknown whether it is excreted in human milk; therefore caution is advised in nursing mothers.

Rizatriptan Benzoate should be used only when a clear diagnosis of migraine has been established. It should not be administered to patients with documented ischemic or vasospastic coronary artery disease. Drugs in this class may cause coronary artery vasospasm; therefore, patients who develop signs or symptoms suggestive of angina after dosing should be evaluated for coronary artery disease or a predisposition to Prinzmetal’s variant angina before receiving further doses, and should be monitored with electrocardiography. Rizatriptan should be used with caution in patients with moderate hepatic impairment.

If there is no response to the first dose during a migraine attack, the diagnosis of migraine should be reconsidered before administering a second dose.

Pediatric Use: Safety and effectiveness of rizatriptan in pediatric patients have not been established; therefore, it is not recommended for use in patients under 18 years of age.

Use in the Elderly: The pharmacokinetics of rizatriptan are similar in elderly patients (≥65 years) and younger adults. However, clinical experience is limited in the elderly because migraine is less common in this population. In clinical studies, no significant differences were observed in efficacy or overall adverse event rates between patients under 65 years and those 65 years and older.

No serious overdoses were reported in trials. Doses up to 40 mg were generally tolerated, with dizziness and somnolence being most common. Hypertension and cardiovascular symptoms may occur in overdose. Gastric lavage and activated charcoal may be considered.

5-HT Agonists

Store in a cool and dry place below 30°C. Protect from light. Keep out of reach of children.