eletriptan hydrobromide


eletriptan hydrobromide

Relpax

Pharmacologic class: 5-hydroxytryptamine-1 (5-HT1) receptor agonist

Therapeutic class: Antimigraine agent

Pregnancy risk category C

Action

Binds with serotonin 5-HT1B receptors on intracranial blood vessels and serotonin 5-HT1D receptors on sensory nerve endings, constricting cranial arteries and thereby relieving migraine

Availability

Tablets: 20 mg, 40 mg

Indications and dosages

Migraine with or without aura

Adults: Initially, 20 to 40 mg P.O.; may repeat in 2 hours if headache returns after initial improvement. Maximum recommended single dosage is 40 mg.

Contraindications

• Hypersensitivity to drug

• Basilar and hemiplegic migraine

• Severe hepatic disease

• Ischemic heart disease

• Peripheral vascular disease

• Cerebrovascular syndromes

• Uncontrolled hypertension

• Ischemic bowel disease

• Within 24 hours of another serotonin agonist or ergot-type drug

Precautions

Use cautiously in:

• hepatic or renal impairment, diabetes mellitus, hypercholesterolemia, cardiac disorders

• pregnant or breastfeeding patients

• children.

Administration

• Give first dose as soon as migraine symptoms arise.

See Be aware that first dose should be given under close supervision to patients with coronary artery disease.

• If headache improves but then recurs, give second dose at least 2 hours after first.

• Be aware that drug's safety in treating an average of more than three headaches within a 30-day period has not been established.

Adverse reactions

CNS: dizziness, insomnia, drowsiness, headache, fatigue, anxiety, paresthesia, asthenia,cerebrovascular ischemia

CV: chest pain, palpitations, hypertension,cardiovascular ischemia

GI: nausea, vomiting, diarrhea, dry mouth

Musculoskeletal: muscle weakness

Respiratory: chest tightness or pressure

Skin: flushing

Other: hot or cold sensation

Interactions

Drug-drug. Antihistamines, ergotamine, ergot derivatives: increased vasospastic effects

CYP450-3A4 inhibitors (such as clarithromycin, ketoconazole, propranolol): increased eletriptan blood level

MAO inhibitors: increased eletriptan effects

Patient monitoring

• Monitor vital signs and assess for chest pain, tightness, or pressure.

Patient teaching

• Instruct patient to take first dose as soon as migraine symptoms occur. If headache improves but then recurs, advise him to take second dose at least 2 hours after first.

• Caution patient to avoid driving and other hazardous activities until drug no longer affects concentration and alertness.

• Tell patient to report chest pain, pressure, or tightness.

• Inform patient that drug won't prevent migraines and isn't effective against other headache types.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.