Names and pronunciation
(nair′ah-trip-tan) Amerge
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Drug reference
(nair′ah-trip-tan) Amerge
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Func. class.: Antimigraine agent
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Chem. class.: 5-HT1 receptor agonist
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ACTION: Binds selectively to the vas- cular 5-HT1 B/D receptor subtype; exerts antimigraine effect; causes vasoconstric- tion in cranial arteries
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USES: Acute treatment of migraine with/without aura
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CONTRAINDICATIONS: Hyper- sensitivity, angina pectoris, history of MI, documented silent ischemia, ischemic heart disease, concurrent ergotamine- containing preparations, uncontrolled hypertension, CV syndromes, hemiplegic or basilar migraines, severe renal disease (CCr <15 mL/min); severe hepatic dis- ease (Child-Pugh grade C) Precautions: Pregnancy, breastfeeding, children, geriatric patients, postmeno- pausal women, men >40 yr, CAD risk, hypercholesterolemia, obesity, diabetes, impaired renal/hepatic function, periph- eral vascular disease overuse
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SIDE EFFECTS CNS: Dizziness, sedation, fatigue CV: Increased B/P, palpitations, tachy- dysrhythmias, PR, QTc prolongation, ST/T wave changes, PVCs, atrial flutter/fibrilla- tion, coronary vasospasm EENT: EENT infections, photophobia GI: Nausea, vomiting MISC: Temperature change sensations; tightness, pressure sensations MS: Weakness, neck stiffness, myalgia
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INTERACTIONS Increase: serotonin syndrome, neurolep- tic malignant syndrome—SSRIs (FLUox- etine, fluvoxaMINE, PARoxetine, sertra- line), SNRIs, serotonin receptor agonists, sibutramine, tramadol Increase: QT prolongation—antidys- rhythmics, some phenothiazines, dolase- tron, mefloquine, ziprasidone; monitor QT closely in cardiac patients Increase: vasospastic effects—ergot, ergot derivatives, other 5-HT1 agonists Increase: adverse reactions risk— MAOIs; do not use together Drug/Herb • Serotonin syndrome: SAM-e, St. John’s wort
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DOSAGE AND ROUTES • Adult: PO 1 or 2.5 mg with fluids; if headache returns, repeat 1× after 4 hr; max 5 mg/24 hr Hepatic/renal dose • Adult: PO CCr 15-39 mL/min or mild to moderate hepatic disease max 2.5 mg/24 hr
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Available forms: Tabs 1, 2.5 mg
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Administer: • With fluids as soon as symptoms ap- pear; may take another dose after 4 hr; do not take >5 mg during any 24-hr period • Swallow whole; use without regard to food • Use for >4 headaches/30 days has not been established
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Assess: • Migraine symptoms: aura, duration, effect on lifestyle, aggravating/alleviating factors • Serotonin syndrome, neuroleptic malignant syndrome: increased heart rate, shivering, sweating, dilated pupils, tremors, high B/P, hyperthermia, head- ache, confusion; if these occur, stop product, administer serotonin antagonist if needed; at least 2 wk should elapse between discontinuation of serotonergic agents and start of product • Cardiac status: ECG, increased B/P, dysrhythmias, monitor for PR, QT prolon- gation, ST-T wave changes, PVCs in those with cardiac disease • Stress level, activity, recreation, coping mechanisms • Neurologic status: LOC, blurred vision, nausea, vomiting, tingling in extremities preceding headache • Quiet, calm environment with de- N creased stimulation (noise, bright light, excessive talking) • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; cautious use in breastfeeding
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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: • To report pain, tightness in chest, neck, throat, or jaw; to notify prescriber imme- diately if sudden, severe abdominal pain occurs • Not to use if another 5-HT1 agonist or ergot preparation has been used during past 24 hr; to avoid using >2 days/wk because rebound headache may occur • To notify prescriber if pregnancy is planned or suspected; to avoid breast- feeding • To discuss all OTC, Rx, herbals, sup- plements with health care professional • To take as soon as headache is starting, only use to treat, not prevent, migraine • That drowsiness, dizziness may occur, not to drive or perform other hazardous tasks until response is known
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PHARMACOKINETICS Onset 2-3 hr; peak 2-3 hr; 28%-31% protein binding; half-life 6 hr; metabolized in liver (metabolite); excreted in urine, feces; may be excreted in breast milk
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• Adult: PO 1 or 2.5 mg with fluids; if headache returns, repeat 1× after 4 hr; max 5 mg/24 hr Hepatic/renal dose
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• Adult: PO CCr 15-39 mL/min or mild to moderate hepatic disease max 2.5 mg/24 hr
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