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Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: five ht1 agonists

• Acute treatment of migraine headache (for adolescents, migraines should be 4 hr in duration).

• Acts as an agonist at specific 5-HT₁ receptor sites in intracranial blood vessels and sensory trigeminal nerves.

• Cranial vessel vasoconstriction with associated decrease in release of neuropeptides and resultant decrease in migraine headache.

Absorption: Well absorbed following oral administration (70%).

Distribution: Widely distributed to tissues.

Metabolism/Excretion: 27% metabolized by monoamine oxidase-A (MAO-A); 12% metabolized by the CYP3A4 and CYP2D6 isoenzymes; 40% excreted unchanged in urine; 13% excreted in feces as unchanged and metabolized drug.

Half-life: 3–4 hr.

(plasma concentrations)

Contraindicated in:

• Hypersensitivity
• Ischemic cardiovascular, cerebrovascular, or peripheral vascular syndromes (including ischemic bowel disease)
• History of significant cardiovascular disease
• Uncontrolled hypertension
• Should not be used within 24 hr of other 5-HT₁ agonists or ergot-type compounds (dihydroergotamine)
• Basilar or hemiplegic migraine
• Concurrent MAO-A inhibitor therapy or within 2 wk of discontinuing MAO-A inhibitor therapy.

Use Cautiously in:

• Cardiovascular risk factors (hypertension, hypercholesterolemia, cigarette smoking, obesity, diabetes, strong family history, menopausal women, or men >40 yr); use only if cardiovascular status has been evaluated and determined to be safe and first dose is administered under supervision
• Renal impairment
• Hepatic impairment
• Hypersensitivity to sulfonamides (cross-sensitivity may occur)
• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Children <12 yr (safety and effectiveness not established).

CV: CORONARY ARTERY VASOSPASM, MI, myocardial ischemia, VENTRICULAR ARRHYTHMIAS.

GI: dry mouth, nausea.

Neuro: drowsiness, headache, paresthesia.

Drug-Drug:

• Concurrent use with MAO-A inhibitors↑ levels and the risk of toxicity; concurrent use or use within 2 wk or MAO inhibitor contraindicated.
• Concurrent use with other 5-HT₁ agonists or ergot-type compounds (dihydroergotamine) may result in additive vasoactive properties; avoid use within 24 hr of each other.
• ↑serotonin levels and serotonin syndrome may occur when used concurrently with SSRIs or SNRIs.
• CYP3A4 inhibitors, including ketoconazole, itraconazole, ritonavir, and erythromycin, may ↑ levels and risk of toxicity.

• PO (Adults and Children 12 yr): 6.25–12.5 mg initially, may repeat in 2 hr; not to exceed 2 doses per 24-hr period.

(Generic available)

• Tablets: 6.25 mg; 12.5 mg;

• Assess pain location, character, intensity, and duration and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
• Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyperreflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs).

• PO: Tablets should be swallowed whole with liquid.

• Inform patient that almotriptan should only be used during a migraine attack. It is meant to be used for relief of migraine attacks but not to prevent or reduce the number of attacks.
• Instruct patient to administer almotriptan as soon as symptoms of a migraine attack appear, but it may be administered any time during an attack. If migraine symptoms return, a 2nd dose may be used. Allow at least 2 hr between doses, and do not use more than 2 doses in any 24-hr period.
• If first dose does not relieve headache, additional almotriptan doses are not likely to be effective; notify health care professional.
• Caution patient not to take almotriptan within 24 hr of another vascular headache suppressant.
• Advise patient that lying down in a darkened room following almotriptan administration may further help relieve headache.
• Advise patient that overuse (use more than 10 days/month) may lead to exacerbation of headache (migraine-like daily headaches, or as a marked increase in frequency of migraine attacks). May require gradual withdrawal of almotriptan and treatment of symptoms (transient worsening of headache).
• Advise patient to notify health care professional prior to next dose of almotriptan if pain or tightness in the chest occurs during use. If pain is severe or does not subside, notify health care professional immediately. If feelings of tingling, heat, flushing, heaviness, pressure, drowsiness, dizziness, tiredness, or sickness develop discuss with health care professional at next visit.
• May cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
• Advise patient to avoid alcohol, which aggravates headaches, during almotriptan use.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Advise patient to notify health care professional immediately if signs or symptoms of serotonin syndrome occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

• Relief of migraine attack.

Axert