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Drugs reference index «Rizatriptan Benzoate»

Rizatriptan Benzoate

Pronunciation: (rye-zah-TRIP-tan)Class: Serotonin 5-HT 1 receptor agonist

Trade Names:Maxalt- Tablets 5 mg- Tablets 10 mg

Trade Names:Maxalt-MLT- Tablets, orally disintegrating 5 mg- Tablets, orally disintegrating 10 mg

Maxalt RPD (Canada)

Pharmacology

Binds to serotonin 1 B and 1 D receptors in intracranial arteries leading to vasoconstriction and subsequent relief of migraine headache.

Pharmacokinetics

Absorption

Completely absorbed orally. Bioavailability is about 45%. T max is about 1 to 1.5 h. C max is about 19.8 mg/L.

Distribution

Vd is 140 L in men and 110 L in women. Protein binding is 14%.

Metabolism

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).

Elimination

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.

Special Populations

Gender

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.

Indications and Usage

Treatment of acute migraine attacks with or without aura.

Contraindications

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.

Dosage and Administration

Adults

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.

Storage/Stability

Store tablets and orally disintegrating tablets at ambient room temperature (59° to 86°F).

Drug Interactions

5-HT 1 agonists (eg, sumatriptan)

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.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitation (at least 1%); coronary artery vasospasm, transient myocardial ischemia, ventricular tachycardia, ventricular fibrillation (rare); MI, myocardial ischemia, stroke (postmarketing).

CNS

Dizziness (9%); somnolence (8%); paresthesia (4%); headache (2%); hypesthesia, decreased mental acuity, euphoria, tremor (at least 1%).

Dermatologic

Flushing (at least 1%).

GI

Nausea (6%); dry mouth (3%); diarrhea, vomiting (at least 1%); dysgeusia (postmarketing).

Genitourinary

Hot flashes (at least 1%).

Respiratory

Dyspnea (at least 1%).

Miscellaneous

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).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Cl is decreased; use with caution.

Hepatic Function

Cl is decreased; use with caution.

Cardiac

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.

Cerebrovascular events

Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists.

Hypertensive crisis

Elevation in BP, including hypertensive crisis, have been reported with administration of 5-HT 1 agonists.

Phenylketonurics

The MLT formulation contains phenylalanine.

Overdosage

Symptoms

Hypertension.

Patient Information

  • Advise patient to read the patient information leaflet before starting therapy and again with each refill.
  • Caution patient using disintegrating tablet not to open the blister until ready to take the dose.
  • Explain that drug is to be used only during migraine and does not prevent or reduce the number of attacks. Emphasize that drug is used only to treat actual migraine attack and should not be used to prevent migraine headaches or treat headaches caused by other conditions.
  • Advise patient that drug is to be taken as soon as symptoms of migraine appear. A second dose may be taken if symptoms return, but no sooner than 2 h following the first dose. For a given attack, if there is no response to the first tablet, do not take a second tablet without first consulting with health care provider. Do not take more than 30 mg in any 24-h period.
  • Advise patient that safety of treating more than 4 headaches in a 30-day period has not been established and to inform health care provider if headaches are occurring more frequently.
  • Advise patient to immediately notify health care provider if any of the following occur after taking a dose of rizatriptan: severe chest pain or chest pain that does not go away; sudden and/or severe stomach pain; shortness of breath; wheezing; swelling of eyelids, face, or lips.
  • Advise patient that if tightness, pain, pressure, or heaviness in chest, throat, neck, or jaw occurs when using sumatriptan, to discuss these symptoms with health care provider before using again.
  • Advise patient to notify health care provider if feelings of tingling, heat, flushing, tiredness, dizziness, heaviness, or pressure occur after treatment.
  • Advise patient that drug may cause fatigue or dizziness and to use caution while driving or performing other activities requiring mental alertness.
  • Advise patient to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreen and wear protective clothing to avoid photosensitivity reactions.
  • Instruct patient to continue taking prescribed migraine prophylactic medications daily as directed.
  • Advise patient not currently taking a migraine prophylactic drug to discuss the use of such drugs with health care provider.

Copyright © 2009 Wolters Kluwer Health.

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