Trade Names:Maxalt- Tablets 5 mg- Tablets 10 mg
Trade Names:Maxalt-MLT- Tablets, orally disintegrating 5 mg- Tablets, orally disintegrating 10 mgMaxalt RPD (Canada)
Binds to serotonin 1 B and 1 D receptors in intracranial arteries leading to vasoconstriction and subsequent relief of migraine headache.
Completely absorbed orally. Bioavailability is about 45%. T max is about 1 to 1.5 h. C max is about 19.8 mg/L.
Vd is 140 L in men and 110 L in women. Protein binding is 14%.
Extensive first pass metabolism via oxidative deamination by monoamine oxidase-A (MAO-A) to the indole acetic acid metabolite (inactive) and N-monodesmethyl-rizatriptan (active metabolite).
Eliminated in urine (82%; 14% excreted as unchanged, 51% excreted as indole acetic acid metabolite) and feces (12%). Plasma t ½ is 2 to 3 h.
AUC is about 30% higher and C max is 11% higher in women than in men.Hemodialysis patients
Ccr is less than 2 mL/min per 1.73 m 2 ; AUC was 44% greater.
Treatment of acute migraine attacks with or without aura.
Patients with ischemic heart disease (eg, angina, MI history, silent ischemia, coronary artery vasospastic disease, uncontrolled hypertension, basal or hemiplegic migraine). Rizatriptan is contraindicated within 24 h of use with other serotonin agonists, ergotamine compounds, or methysergide, or concurrent treatment with MAO inhibitors or within 14 days following discontinuation of an MAO inhibitor.
PO 5 or 10 mg tablet with the onset of migraine headache. Individualize dose based on response and side effects. Doses may be repeated after a minimum of 2 h as needed with a max dose of 30 mg in a 24-h period. Patients taking propanolol should receive the 5 mg dose with a max of 3 doses (15 mg) in a 24-h period. The MLT formulation is a rapidly disintegrating tablet that may be taken without water. It is placed on the tongue where it rapidly breaks apart and can then be swallowed with normal saliva production.
Store tablets and orally disintegrating tablets at ambient room temperature (59° to 86°F).
Increased risk of vasospastic reactions; therefore, coadministration of two 5-HT 1 agonists within 24 h of each other is contraindicated.Ergot-containing drugs
Additive and prolonged vasospasm.MAO inhibitors
Use of rizatriptan with MAO inhibitors or within 14 days following discontinuation of an MAO inhibitor is contraindicated.Propranolol
Increased rizatriptan plasma concentrations.Selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, fluvoxamine, sertraline)
Weakness, hyperreflexia, and incoordination have been rarely reported.Sibutramine
Serotonin syndrome, including CNS irritability, motor weakness, shivering, myoclonus, and altered consciousness may occur.
None well documented.
Palpitation (at least 1%); coronary artery vasospasm, transient myocardial ischemia, ventricular tachycardia, ventricular fibrillation (rare); MI, myocardial ischemia, stroke (postmarketing).
Dizziness (9%); somnolence (8%); paresthesia (4%); headache (2%); hypesthesia, decreased mental acuity, euphoria, tremor (at least 1%).
Flushing (at least 1%).
Nausea (6%); dry mouth (3%); diarrhea, vomiting (at least 1%); dysgeusia (postmarketing).
Hot flashes (at least 1%).
Dyspnea (at least 1%).
Asthenia, fatigue (7%); atypical sensations (5%); pain, tightness, pressure, or heaviness of chest, localized pain (3%); tightness, pain, or pressure of neck, throat, or jaw, regional tightness, pressure, or heaviness (2%); warm or cold sensations (at least 1%); hypersensitivity (including angioedema), wheezing, or toxic epidermal necrolysis (postmarketing).
Category C .
Safety and efficacy not established.
Cl is decreased; use with caution.
Cl is decreased; use with caution.
May cause coronary vasospasm in patients with CAD. Administer first dose in health care provider's office or similarly staffed and equipped facility to patients at possible risk of unrecognized coronary disease.
Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists.
Elevation in BP, including hypertensive crisis, have been reported with administration of 5-HT 1 agonists.
The MLT formulation contains phenylalanine.
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