ALMOTRIPTAN
(al-mo-trip'tan)
Axert
Classifications: autonomic nervous system agent; adrenergic agonist (sympathomimetic); serotonin 5-ht1-receptor agonist
Prototype: Sumatriptan
Pregnancy Category: C

Availability

6.25 mg, 12.5 mg tablets

Actions

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.

Therapeutic Effects

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.

Uses

Treatment of migraine headache with or without aura.

Contraindications

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).

Cautious Use

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.

Route & Dosage

Migraine Headache
Adult: PO 6.25–12.5 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)

Administration

Oral

Adverse Effects (1%)

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.

Interactions

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.

Pharmacokinetics

Absorption: Well absorbed, 70% reaches systemic circulation. Peak: 1–3 h. Distribution: 35% protein bound. Metabolism: 27% metabolized by monoamine oxidase. Elimination: 75% excreted renally, 13% excreted in feces. Half-Life: 3–4 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug