Names and pronunciation
R (rye-zah-trip′tan) Maxalt, Maxalt-MLT
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Drug reference
R (rye-zah-trip′tan) Maxalt, Maxalt-MLT
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Func. class.: Migraine agent
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Chem. class.: 5-HT1D receptor ago- nist, abortive agent-triptan
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ACTION: Binds selectively to the vascu- lar 5-HT1B/1D receptor subtype; exerts anti- migraine effect; causes vasoconstriction of the cranial arteries
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USES: Acute treatment of migraine
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CONTRAINDICATIONS: Angina pectoris, history of MI, documented silent ischemia, Prinzmetal’s angina, ischemic heart disease, concurrent ergotamine- containing preparations, uncontrolled hypertension, hypersensitivity, basilar or hemiplegic migraine Precautions: Pregnancy, breastfeeding, children, geriatric patients, postmeno- pausal women, men >40 yr, risk factors for CAD, hypercholesterolemia, obesity, diabetes, impaired renal/hepatic function
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SIDE EFFECTS CNS: Dizziness, drowsiness, headache, fatigue, warm/cold sensations, flushing CV: MI, ventricular fibrillation, ventricular tachycardia, coronary artery vasospasm, palpitations, hypertension, peripheral vascular ischemia, ECG changes ENDO: Hot flashes, mild increase in growth hormone GI: Nausea, dry mouth, diarrhea, abdominal pain, ischemic colitis RESP: Chest tightness, pressure, dyspnea
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INTERACTIONS Weakness, hyperreflexia, incoordina- tion: SSRIs Increase: levels of sibutramine Increase: rizatriptan action—cimetidine, oral contraceptives, MAOIs, nonselective MAOI (type A and B), isocarboxazid, pargyline, phenelzine, propranolol, tranylcypromine Increase: vasospastic effects—ergot, ergot derivatives, other 5-HT receptor agonists Drug/Herb Serotonin syndrome: St. John’s wort
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DOSAGE AND ROUTES Acute migraine • Adult: PO 5-10 mg single dose, redos- ing separated by ≥2 hr, max 30 mg/24 hr Acute migraine in those using propranolol • Adult: PO 5 mg daily, max 10 mg/day given in 2 doses separated by ≥2 hr
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Available forms: Tabs (Maxalt) 5, 10 mg; orally disintegrating tabs (Maxalt- MLT) 5, 10 mg
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Administer: • Orally disintegrating tab: do not open blister until use; peel blister open with dry hands; place tab on patient’s tongue, where it will dissolve, and have patient swallow with saliva (contains phenylalanine) • Not to be used for more than 3-4 times per month
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Assess: • Migraine symptoms: visual distur- bances, aura, intensity, nausea, vomiting, photophobia • Stress level, activity, recreation, coping mechanisms • Neurologic status: LOC, blurring vi- sion, nausea, vomiting, tingling in ex- tremities preceding headache • Ingestion of tyramine foods (pickled products, beer, wine, aged cheese), food additives, preservatives, colorings, artifi- cial sweeteners, chocolate, caffeine, which may precipitate these types of headaches • Renal status: urine output • Quiet, calm environment with de- creased stimulation: noise, bright light, excessive talking • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; enroll in the registry, 1-800-986-8999; cautious use in breastfeeding, excretion unknown
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Evaluate: • Therapeutic response: decrease in fre- quency, severity of headache
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • About use of orally disintegrating tab: instruct patient not to open blister until use, to peel blister open with dry hands, to place tab on tongue, where it will dis- solve, and to swallow with saliva (con- tains phenylalanine) • To report any side effects to prescriber • To use alternative contraception while taking product if oral contraceptives are being used • That product does not prevent or reduce number of migraines; if 1st dose does not relieve pain, do not use more, notify pre- scriber; to avoid use in acute headache, use of agent >10 days a month due to the risk of medication overuse headaches
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PHARMACOKINETICS Onset of pain relief 10 min-2 hr; peak 1-11⁄2 hr; duration 14-16 hr; 14% plasma protein binding; metabolized in liver (metabolite); excreted in urine (82%), feces (12%); half-life 2-3 hr
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• Adult: PO 5-10 mg single dose, redos- ing separated by ≥2 hr, max 30 mg/24 hr Acute migraine in those using propranolol
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• Adult: PO 5 mg daily, max 10 mg/day given in 2 doses separated by ≥2 hr
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