Zolmitriptan
Zolmitriptan (Zomig)
Zolmitriptan
(zohl-mih- TRIP-tin)
Pregnancy Category: C Zomig (Rx)

Classification: Antimigraine drug

Action/Kinetics: Binds to serotonin 5-HT _1B/1D receptors on intracranial blood vessels and in sensory nerves of trigeminal system. This results in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Well absorbed after PO use. Peak plasma levels: 2 hr. t 1/2, elimination: 3 hr (for zolmitriptan and active metabolite). Excreted in feces and urine.

Uses: Treatment of acute migraine in adults with or without aura. Use only when there is clear diagnosis of migraine.

Contraindications: Prophylaxis of migraine or management of hemiplegic or basilar migraine. Use in angina pectoris, history of MI, documented or silent ischemia, ischemic heart disease, coronary artery vasospasm (including Prinzmetal's variant angina), other significant underlying CV disease. Also use in uncontrolled hypertension, within 24 hr of treatment with another serotonin HT ₁ agonist or an ergotamine-containing or ergot-type drug (e.g., dihydroergotamine, methysergide). Concurrent use with MAO inhibitor or within 2 weeks of discontinuing MAO inhibitor.

Special Concerns: Use with caution in liver disease and during lactation. A significant increase in BP may occur in those with moderate-to-severe hepatic impairment. Safety and efficacy have not been determined for cluster headache.

Side Effects: GI:
Dry mouth, dyspepsia, dysphagia, nausea, increased appetite, tongue edema, esophagitis, gastroenteritis, abnormal liver function, thirst. CV: Palpitations, arrhythmias, hypertension, syncope. Atypical sensations: Hypesthesia, paresthesia, warm/cold sensation. CNS: Dizziness, somnolence, vertigo, agitation, anxiety, depression, emotional lability, insomnia. Pain pressure sensations: Chest pain, tightness, pressure and/or heaviness. Pain, tightness, or heaviness in the neck, throat, or jaw. Heaviness, pressure, tightness other than in the chest or neck. Musculoskeletal: Myalgia, myasthenia, back pain, leg cramps, tenosynovitis. Respiratory: Bronchitis, bronchospasm epistaxis, hiccup, laryngitis, yawn. Dermatologic: Sweating, pruritus, rash, urticaria, ecchymosis, photosensitivity. GU: Hematuria, cystitis, polyuria, urinary frequency or urgency. Body as a whole: Asthenia, allergic reaction, chills, facial edema, edema, fever, malaise. Miscellaneous: Dry eye, eye pain, hyperacusis, ear pain, parosmia, tinnitus.

Drug Interactions: Cimetidine / t 1/2 of zolmitriptan is doubled Ergot-containing drugs / Prolonged vasospastic reactions MAO Inhibitors / Zolmitriptan levels Oral contraceptives / Zolmitriptan plasma levels Selective serotonin reuptake inhibitors / Rarely, weakness, hyperreflexia, and incoordination

How Supplied: Tablets: 2.5 mg, 5 mg

Dosage
?Tablets Migraine headaches.
Adults, initial: 2.5 mg or lower. Dose of 5 mg may be required. If headache returns, repeat dose after 2 hr, not to exceed 10 mg in 24-hr period.