Rizat

• Acute Treatment of Migraine: Approved for the acute treatment of migraine attacks with or without aura in adults and pediatric patients aged 6 years and older.
• Off-Label Uses: Occasionally used off-label for acute cluster headache attacks, although not officially approved for this indication.
• Note: Not indicated for migraine prevention or for hemiplegic or basilar migraine.

• Adults:
• Initial dose: 5 mg or 10 mg orally at onset of migraine.
• If symptoms persist or return, a second dose may be administered at least 2 hours after the first.
• Maximum dose: 30 mg within 24 hours.
• Pediatrics (6 to 17 years):
• Dose depends on body weight.
• ≥40 kg: 10 mg dose.
• <40 kg: 5 mg dose.
• Elderly:
• No specific dose adjustment; monitor for cardiovascular risks.
• Renal/Hepatic Impairment:
• Use caution; no formal dose adjustment but close monitoring advised.
• Administration Route: Oral tablets.
• Frequency: Single doses as needed; maximum 3 doses/day.
• Duration: Use as needed for migraine attacks; not for continuous use.

Rizatriptan Benzoate acts as a selective agonist at serotonin (5-HT1B/1D) receptors located on intracranial blood vessels and sensory nerves of the trigeminal system. Activation of 5-HT1B receptors causes vasoconstriction of dilated cranial blood vessels, while activation of 5-HT1D receptors inhibits release of pro-inflammatory neuropeptides such as calcitonin gene-related peptide (CGRP). These effects reduce neurogenic inflammation and vascular dilation, thereby relieving migraine pain and associated symptoms.

• Absorption: Rapid oral absorption; peak plasma concentration within 1 to 1.5 hours.
• Bioavailability: Approximately 40%.
• Distribution: Moderate volume of distribution; crosses blood-brain barrier.
• Metabolism: Primarily metabolized by monoamine oxidase A (MAO-A) in the liver.
• Metabolites: No active metabolites of clinical significance.
• Elimination: Mainly excreted in urine.
• Half-Life: Approximately 2 to 3 hours.
• Onset of Action: Therapeutic effects typically begin within 30 minutes to 1 hour.

• Pregnancy: Classified as FDA Pregnancy Category C. Animal studies indicate potential risks; use only if benefits outweigh risks. Limited human data.
• Lactation: Excreted in breast milk in small amounts. Caution advised; breastfeeding not recommended for 24 hours post-dose.

• Primary Class: Antimigraine agent.
• Subclass: Selective serotonin 5-HT1 receptor agonist (Triptan class).

• Known hypersensitivity to rizatriptan or any formulation component.
• History of ischemic heart disease, angina, or other significant cardiovascular disorders.
• Cerebrovascular disease or peripheral vascular disease.
• Uncontrolled hypertension.
• Use within 24 hours of another 5-HT1 agonist or ergotamine derivatives.
• Concurrent or recent (within 14 days) use of monoamine oxidase inhibitors (MAOIs).

• Use with caution in patients with cardiovascular risk factors.
• Risk of serotonin syndrome when combined with other serotonergic drugs.
• Monitor for signs of medication-overuse headache in patients using frequently.
• Possible transient increases in blood pressure; monitor hypertensive patients.
• Discontinue immediately if chest pain or symptoms suggestive of myocardial ischemia occur.
• Not recommended for hemiplegic or basilar migraine due to cerebrovascular risk.

• Common:
• Central nervous system: dizziness, fatigue, somnolence.
• Gastrointestinal: nausea.
• Sensory: paresthesia, flushing.
• Throat discomfort or tightness.
• Serious/Rare:
• Chest pain or ischemia.
• Serotonin syndrome (especially with serotonergic co-medications).
• Hypersensitivity reactions including rash or anaphylaxis.
• Transient hypertension.
• Side effects usually appear shortly after dosing and may be dose-dependent.

• MAO Inhibitors: Contraindicated; increase rizatriptan levels.
• Other Triptans or Ergot Derivatives: Risk of additive vasospasm; avoid co-administration.
• SSRIs/SNRIs: Increased risk of serotonin syndrome.
• Propranolol: May increase rizatriptan plasma concentrations; dose adjustment may be needed.
• Alcohol: May worsen CNS effects; caution advised.

• FDA approval expanded to include pediatric patients aged 6 and above.
• Enhanced warnings regarding serotonin syndrome risks.
• Emphasis on avoiding overuse to prevent medication-overuse headache.
• No major changes in dosing or approved indications recently.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep container tightly closed.
• No refrigeration or special reconstitution required.