ALMOTRIPTAN (al-mo-trip'tan) Axert Classifications: autonomic nervous system agent; adrenergic agonist (sympathomimetic); serotonin 5-ht1-receptor agonist Prototype: Sumatriptan Pregnancy Category: C
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6.25 mg, 12.5 mg tablets
Selective agonist that binds with high affinity to 5-HT1D, 5-HT1B, 5-HT1F serotonin receptors which are found on extracerebral and intracranial blood vessels, and on other structures in the central
nervous system.
Due primarily to agonist effects on 5-HT1D and 5-HT1B serotonin receptors on cranial blood vessels resulting in vasoconstriction and agonist effects on nerve terminals in the
trigeminal system. Activation of these receptors results in constriction of cranial vessels which become dilated during a
migraine attack, inhibition of neuropeptide release, and reduced signal transmission in the pain pathways.
Treatment of migraine headache with or without aura.
Hypersensitivity to almotriptan malate. Significant cardiovascular disease such as ischemic heart disease, coronary artery
vasospasms, MI, angina, arteriosclerosis, cardiac arrhythmias, diabetes mellitus, colitis, history of cerebrovascular events,
or uncontrolled hypertension; stroke, smoking, Wolff-Parkinson-White syndrome, within 24 h of receiving another 5-HT1 agonist or an ergotamine-containing or ergot-type drug; basilar or hemiplegic migraine, pregnancy (category C).
Significant risk factors for coronary artery disease unless a cardiac evaluation has been done; hypertension; risk factors
for cerebrovascular accident; peripheral vascular disease, impaired liver or kidney function, Raynaud's disease, children,
elderly, lactation.
Migraine Headache Adult: PO 6.2512.5 mg. If headache returns, may repeat after at least 2 h (max: 2 tabs/24 h)
Renal Impairment Clcr <10 mL/min: 6.25 mg (max: 12.5 mg/d)
Hepatic Impairment 6.25 mg (max: 12.5 mg/d)
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Oral
- Do not give within 24 h of an ergot-containing drug.
- Administer any time after symptoms of migraine appear.
- Do not administer a second dose without consulting the physician for any attack during which the FIRST dose did NOT work.
- Give a second dose if headache was relieved by first dose but symptoms return; however, wait at least 2 h after the first
dose before giving a second dose.
- Do not give more than two doses in 24 h.
- Store at 15°30° C (59°86° F).
Body as a Whole: Flushing. CNS: Drowsiness, headache, paresthesia. CV: Palpitations, tachycardia, serious cardiac events (including MI) have been reported within a few hours after administration. GI: Nausea, vomiting, dry mouth.
Drug:
Dihydroergotamine,
methysergide, other 5-ht1 agonists may cause prolonged vasospastic reactions; ssris, sibutramine have rarely caused weakness, hyperreflexia, and incoordination; maois should not be used with 5-ht1 agonists.
Absorption: Well absorbed, 70% reaches systemic circulation. Peak: 13 h. Distribution: 35% protein bound. Metabolism: 27% metabolized by monoamine oxidase. Elimination: 75% excreted renally, 13% excreted in feces. Half-Life: 34 h.
Assessment & Drug Effects
- Monitor cardiovascular status carefully following first dose in patients at relatively high risk for coronary artery disease
(e.g., postmenopausal women, men over 40 years old, persons with known CAD risk factors) or who have coronary artery vasospasms.
- Report to physician immediately chest pain or tightness in chest or throat that is severe or does not quickly resolve following
a dose of almotriptan.
- Pain relief usually begins within 10 min of ingestion, with complete relief in approximately 65% of all patients within
2 h.
- Monitor BP, especially in those being treated for hypertension.
Patient & Family Education
- Review patient information leaflet provided by the manufacturer carefully.
- Notify physician immediately if symptoms of severe angina (e.g., severe or persistent pain or tightness in chest, back, neck,
or throat) or hypersensitivity (e.g., wheezing, facial swelling, skin rash, or hives) occur.
- Do not take any other serotonin receptor agonist (e.g., Imitrex, Maxalt, Zomig, Amerge) within 24 h of taking almotriptan.
- Advise physician of any drugs taken within 1 wk of beginning almotriptan.
- Check with physician regarding drug interactions before taking any new OTC or prescription drugs.
- Report any other adverse effects (e.g., tingling, flushing, dizziness) at next physician visit.
- Do not breast feed while taking this drug without consulting physician.