e-le-TRIP-tan

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: five ht1 agonists

• Acute treatment of migraine headache.

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

• Cranial vessel vasoconstriction with resultant decrease in migraine headache.

Absorption: 50% absorbed after oral administration.

Distribution: Enters breast milk.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP3A4 enzyme system.

Half-life: 4 hr.

(decreased migraine pain)

Contraindicated in:

• Hypersensitivity
• Hemiplegic or basilar migraine
• Ischemic heart disease or Prinzmetal's angina
• Uncontrolled hypertension
• Wolff-Parkinson-White syndrome or other arrhythmias involving conduction pathways
• Stroke or transient ischemic attack
• Peripheral vascular disease
• Ischemic bowel disease
• Severe hepatic impairment
• Should not be used within 24 hr of other 5-HT₁ agonists or ergot-type compounds (dihydroergotamine)
• Should not be used within 72 hr of potent CYP3A4 inhibitors including ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, and nelfinavir.

Use Cautiously in:

• OB: Use only if potential benefits justify potential risk to fetus
• Lactation: Doses up to 80 mg daily not expected to cause adverse effects in breast-fed infants >2 mo
• Pedi: Safety and effectiveness not established
• Geri: ↑risk of ↑ BP.

Exercise Extreme Caution 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 1st dose is administered under supervision.

CV: ECG changes, angina, chest tightness/pressure, coronary vasospasm, MI, transient hypertension, VENTRICULAR FIBRILLATION, VENTRICULAR TACHYCARDIA.

GI: abdominal pain, dry mouth, dysphagia, nausea.

Neuro: dizziness, drowsiness, paresthesia, weakness.
Misc: ANAPHYLAXIS.

Drug-Drug:

• Blood levels and risk of adverse reactions are ↑ by potent CYP3A4 inhibitors (including ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, and nelfinavir); use within 72 hr is contraindicated.
• Concurrent use (within 24 hr of each other) with ergot-containing drugs (dihydroergotamine) may result in prolonged vasospastic reactions and should be avoided.
• ↑serotonin levels and serotonin syndrome may occur when used concurrently with SSRI and SNRI antidepressants.

• PO (Adults): 20 or 40 mg; may be repeated in 2 hr if initial response is inadequate (not to exceed 80 mg/24 hr or treatment of 3 headaches/mo).

(Generic available)

• Tablets: 20 mg; 40 mg;

• Assess pain location, intensity, character, duration and associated symptoms (photophonia, phonophobia, nausea, vomiting) during migraine attack.

• PO: Administer at the first sign of a headache. If after the initial dose, headache improves but then returns, dose may be repeated at least 2 hr after initial dose. If initial dose is ineffective, second dose is unlikely to be effective.

• Instruct patient that eletriptan should only be used during a migraine attack. Eletriptan is used for treatment of a migraine attack, not for prevention. Advise patient to read the Patient Summary of Information before starting therapy and with each Rx refill in case of changes.
• Instruct patient to take eletriptan at the first sign of a migraine, but may be administered at any time during attack. Allow at least 2 hr between doses and do not use more than 80 mg/day or 3 attacks/mo.
• Caution patient not to take eletriptan within 24 hr of other vascular headache suppressants.
• Advise patient that lying down in a darkened room after eletriptan administration may further help relieve headache.
• Advise patient to notify health care professional if she plans or suspects pregnancy, or if breastfeeding.
• Advise patient to notify health care professional before next dose of eletriptan if pain or tightness in the chest occurs. If chest 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 provider at next visit.
• May cause drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
• Instruct 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 avoid alcohol, which aggravates headaches, during therapy.
• 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 rizatriptan and treatment of symptoms (transient worsening of headache).
• Instruct patient to notify health care professional if signs of serotonin syndrome (mental status changes: agitation, hallucinations, coma; autonomic instability: tachycardia, labile BP, hyperthermia; neuromuscular aberrations: hyperreflexia, incoordination; and/or gastrointestinal symptoms: nausea, vomiting, diarrhea) occur.
• Advise patient to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

• Relief of migraine attack.

Relpax