Rizat5 mg

Established / FDA-Approved Use

Rizat is indicated for the acute treatment of migraine with or without aura in adults and in pediatric patients 6 to 17 years of age.

• Rizat is intended to treat a migraine attack that has already started, not to reduce the number of attacks.
• Rizat is not indicated for the preventive (prophylactic) treatment of migraine and is not indicated for the treatment of cluster headache, tension-type headache, or other headache disorders.

Not Established / Not Recommended

Rizat has not been shown to be effective for hemiplegic or basilar migraine and should not be used in these subtypes because of the overlap with stroke-like presentations. There is no established role for Rizat as an off-label agent outside acute migraine treatment.

Each tablet contains Rizatriptan Benzoate equivalent to 5 mg or 10 mg of rizatriptan (base). Rizatriptan Benzoate is available as conventional (swallowable) tablets and as orally disintegrating tablets (ODT/MLT), the latter of which may contain aspartame (a source of phenylalanine).

Rizat is a selective serotonin 5-HT1B/1D receptor agonist belonging to the triptan class of anti-migraine medicines. It is used to relieve the pain and associated symptoms (nausea, photophobia, phonophobia) of an acute migraine attack in adults and adolescents.

Rizat works by binding to 5-HT1B/1D receptors on intracranial blood vessels and trigeminal sensory nerves, producing cranial vasoconstriction and inhibiting the release of pro-inflammatory neuropeptides that mediate migraine pain.

Anti-migraine preparations; Selective serotonin 5-HT1B/1D receptor agonist (Triptan)

Rizatriptan Benzoate is a selective agonist at serotonin 5-HT1B and 5-HT1D receptors. Activation of these receptors on intracranial (extracerebral) blood vessels causes vasoconstriction, and activation of presynaptic 5-HT1D receptors on trigeminal sensory nerve terminals inhibits the release of vasoactive neuropeptides (such as CGRP), reducing neurogenic inflammation and interrupting pain transmission in the trigeminovascular system.

Pharmacokinetics

• Absorption: Oral bioavailability is approximately 40-45%; peak plasma concentration is reached in about 1-1.5 hours (may be delayed with the orally disintegrating formulation or when taken with food).
• Metabolism: Primarily metabolized by monoamine oxidase-A (MAO-A) to an inactive indole acetic acid metabolite.
• Elimination half-life: Approximately 2-3 hours.
• Excretion: Mainly renal, as metabolites and a small fraction of unchanged drug.

Rizat tablets are taken orally, with or without food, at the first sign of a migraine attack. Orally disintegrating tablets dissolve on the tongue without the need for water; conventional tablets should be swallowed whole with water. Do not use Rizat to treat a headache that is different from your usual migraine pattern without consulting a physician.

Clinically Significant Interactions

• MAOIs (e.g., moclobemide, phenelzine): Concurrent use or use within 2 weeks of discontinuing an MAOI is contraindicated; MAOIs markedly increase Rizat plasma concentrations by inhibiting its metabolism (MAO-A).
• Other triptans or ergotamine-type medications (ergotamine, dihydroergotamine, methysergide): Concurrent use or use within 24 hours of Rizat is contraindicated due to additive, prolonged vasospastic/vasoconstrictive effects.
• SSRIs, SNRIs, and other serotonergic drugs: Concomitant use may increase the risk of serotonin syndrome (agitation, hallucinations, tachycardia, hyperreflexia, incoordination, diarrhea); monitor closely, especially at treatment initiation.
• Propranolol: Increases Rizat plasma levels by roughly 70%; use the reduced 5 mg dose regimen (see Dosage and Administration).

Most adverse effects of Rizat are mild and transient. Common reactions (occurring in more than 2% of patients) include:

• Dizziness
• Drowsiness/somnolence
• Fatigue or asthenia
• Paresthesia (tingling/numbness)
• Nausea
• Dry mouth
• Chest pain, tightness, or pressure (usually non-cardiac in origin but see Precautions and Warnings for evaluation of cardiac risk)

Serious but uncommon reactions include serotonin syndrome, cardiac arrhythmias, myocardial ischemia/infarction, and cerebrovascular events (see Precautions and Warnings).

Pregnancy: Data on Rizat use in pregnant women are limited and have not established a clear drug-associated risk of major birth defects or miscarriage. Migraine itself and untreated attacks can also affect pregnancy. Rizat should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus; consult a physician before use.

Lactation: Rizat is excreted into breast milk in small amounts. There is no data on its effects on the breastfed infant or on milk production. Caution should be exercised, and a physician should be consulted to weigh the benefits of treatment against potential infant exposure; minimizing infant exposure (e.g., waiting several hours after a dose before breastfeeding) may be advised by the treating physician.

• Cardiovascular risk: Rarely, Rizat has been associated with serious cardiac events including myocardial infarction, arrhythmias, and coronary artery vasospasm, even in patients without known coronary artery disease. Cardiovascular evaluation is recommended before starting Rizat in patients with multiple cardiovascular risk factors (e.g., hypertension, diabetes, smoking, obesity, strong family history, postmenopausal women, men over 40).
• Cerebrovascular events: Stroke and other cerebrovascular events have been reported rarely; discontinue and evaluate if signs of stroke occur.
• Serotonin syndrome: Risk increases with concomitant SSRIs, SNRIs, or MAOIs (see Interactions); watch for agitation, hallucinations, tachycardia, hyperreflexia, and incoordination.
• Medication-overuse headache: Frequent use (more than 10 days per month) can lead to worsening headache; limit treatment days per standard triptan-class guidance and consult a physician if headaches increase in frequency.
• Peripheral vasospastic reactions: Use with caution in patients at risk for peripheral vascular ischemia.
• Hemiplegic/basilar migraine: Not to be used, as clinical presentation may overlap with stroke and the vasoconstrictive mechanism raises theoretical concern.
• Phenylketonuria: Orally disintegrating tablets may contain aspartame (a source of phenylalanine); use caution in patients with phenylketonuria.

Overdose with Rizat may cause exaggeration of known effects such as elevated blood pressure, cardiovascular events, seizures, tremor, and extremity discoloration. There is no specific antidote. In case of suspected overdose, seek immediate medical attention or contact a poison control center/emergency services. Treatment is supportive, with continuous cardiovascular monitoring for at least 12 hours or until symptoms resolve; do not attempt unsupervised home treatment.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

• Pediatric patients: Approved for acute migraine treatment in patients 6-17 years using weight-based single dosing (see Dosage and Administration); safety and efficacy of a second dose within 24 hours have not been established in this age group.
• Elderly (>65 years): Limited clinical experience; use with caution given the higher likelihood of underlying cardiovascular disease. Rizat is generally not recommended for routine use in the elderly without prior cardiovascular assessment.
• Hepatic impairment: No dose adjustment needed in mild-to-moderate impairment; not studied in severe impairment (see Dosage and Administration).
• Renal impairment: Not specifically studied in severe renal impairment; use with caution.
• Pregnancy and lactation: See Pregnancy and Lactation section.

Rizat is intended for short-term, as-needed (acute) treatment of an individual migraine attack — typically one dose, with a possible second dose if needed after 2 hours, and not for continuous or prophylactic daily use. To reduce the risk of medication-overuse headache, treatment should generally be limited to no more than about 10 days per month; consult a physician if more frequent use is required.

Triptans (Selective Serotonin 5-HT1B/1D Receptor Agonists)

Rizatriptan Benzoate selectively binds to and activates 5-HT1B and 5-HT1D serotonin receptors. Stimulation of 5-HT1B receptors on intracranial extracerebral blood vessels produces vasoconstriction, reversing the vasodilation thought to occur during a migraine attack. Stimulation of presynaptic 5-HT1D receptors on trigeminal nerve terminals inhibits the release of vasoactive and pro-inflammatory neuropeptides (including calcitonin gene-related peptide, CGRP), reducing neurogenic inflammation around cranial vessels and decreasing transmission of pain signals through the trigeminocervical complex.

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Rizat is approved for the acute treatment of migraine in pediatric patients 6 to 17 years of age, using weight-based single dosing: 5 mg for children weighing less than 40 kg and 10 mg for those weighing 40 kg or more. Safety and efficacy of a second dose within 24 hours, and use for migraine prevention, have not been established in this age group. Rizat is not recommended in children under 6 years of age, as safety and efficacy have not been established.