almotriptan, Axert Classification

 Indications

Acute treatment of migraine headache (for adolescents,

migraines should be 4 hr in duration).

Action

Acts as an agonist at specific 5-HT1 receptor sites in intracranial

blood vessels and sensory trigeminal nerves.

Therapeutic Effects: Cranial vessel vasoconstriction

with associated decrease in release of neuropeptides

and resultant decrease in migraine headache.

Pharmacokinetics

Absorption: Well absorbed following oral administration

(70%).

Distribution: Unknown.

Metabolism and Excretion: 40% excreted unchanged

in urine; 27% metabolized by monoamine

oxidase-A (MAO-A); 12% metabolized by CYP3A4 and

CYP2D6; 13% excreted in feces as unchanged and metabolized

drug.

Half-life: 3–4 hr.

TIME/ACTION PROFILE (Blood levels)

ROUTE ONSET PEAK DURATION

PO unknown 1–3 hr unknown 

Contraindications/Precautions

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; Impaired

hepatic or renal function; Hypersensitivity to sulfonamides

(cross-sensitivity may occur); OB, Lactation:

Safety not established; Pedi: Children 12 yr (safety not

established).

Adverse Reactions/Side Effects

CNS: drowsiness, headache. CV: CORONARY ARTERY

VASOSPASM, MI, VENTRICULAR ARRHYTHMIAS, myocardial

ischemia. GI: dry mouth, nausea. Neuro: paresthesia.

Interactions

Drug-Drug: Concurrent use with MAO-A inhibitorsqblood

levels and the risk of adverse reactions

(concurrent use or use within 2 wk or MAO inhibitor is

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).qserotonin levels

and serotonin syndrome may occur when used concurrently

with SSRI and SNRI antidepressants.

Blood levels and effects may beqby ketoconazole,

itraconazole, ritonavir, and erythromycin (inhibitors

of CYP3A4 enzymes).

Route/Dosage

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.

Hepatic/Renal Impairment

PO (Adults): 6.25 mg initially, may repeat in 2 hr; not

to exceed 2 doses per 24-hr period.

Availability (generic available)

Tablets: 6.25 mg, 12.5 mg.