section name header

Pronunciation

al-moe-TRIP-tan

Classifications

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: five ht1 agonists

Indications

REMS


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: 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.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown1–3 hrunknown





Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

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

GI: dry mouth, nausea

Neuro: drowsiness, headache, paresthesia

Interactions

Drug-drug:

Route/Dosage

Availability

(Generic available)

Assessment

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Axert