zole-mi-TRIP-tan

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: five ht1 agonists

• Acute treatment of migraine headache.

• Acts as an agonist at specific 5-HT₁ receptor sites in intracranial blood vessels and sensory trigeminal nerves.

• Relief of acute attacks of migraine.

Absorption: Well absorbed (40%) following oral and intranasal administration.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver; some conversion to metabolites that are more active than zolmitriptan. 8% excreted unchanged in urine.

Half-life: 3 hr (for zolmitriptan and active metabolite).

(relief of headache)

*3 hr for orally disintegrating tablets.

Contraindicated in:

• Hypersensitivity
• Significant underlying heart disease (including ischemic heart disease, history of MI, coronary artery vasospasm, uncontrolled hypertension)
• Stroke or transient ischemic attack
• Peripheral vascular disease (including, but not limited to ischemic bowel disease)
• Concurrent (or within 24 hr) use of other 5-HT agonists, ergotamine, or ergot-type medications
• Concurrent (or within 2 wk) use of MAO inhibitors
• Hemiplegic or basilar migraine
• Symptomatic Wolff-Parkinson-White syndrome or other arrhythmias
• Moderate to severe hepatic impairment (nasal spray only).

Use Cautiously in:

• Cardiovascular risk factors (hypertension, hypercholesterolemia, cigarette smoking, obesity, diabetes, strong family history, menopausal females or males >40 yr [use only if cardiovascular status has been evaluated and determined to be safe and 1st dose is administered under supervision])
• Hepatic impairment (use lower doses of oral)
• OB: Safety not established in pregnancy
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Pedi: Safety and effectiveness not established in children <18 yr (oral); children <12 yr (intranasal).

CV: angina, chest pain/pressure/tightness/heaviness, hypertension, MI, palpitations.

Derm: sweating, warm/cold sensation.

EENT: throat pain/tightness/pressure.

GI: dry mouth, dyspepsia, dysphagia, nausea.

MS: myalgia, myasthenia.

Neuro: dizziness, drowsiness, hypesthesia, paresthesia, vertigo, weakness.

Drug-Drug:

• Because of ↑ risk of cerebral vasospasm, avoid concurrent use of other 5-HT agonists (naratriptan, sumatriptan, rizatriptan) and/or ergot-type preparations (dihydroergotamine).
• Concurrent use of MAO inhibitors↑ blood levels and risk of toxicity (avoid use within 2 wk of MAO inhibitors).
• Blood levels may be ↑ by hormonal contraceptives.
• Cimetidine↑ half-life of zolmitriptan and its active metabolite.
• ↑risk of serotonin syndrome with SSRIs, SNRIs, TCAs, triptans, meperidine, bupropion, or buspirone; avoid concurrent use.

Drug-Natural Products:

• ↑risk of serotonergic side effects including serotonin syndrome with St. John’s wort and SAMe.

• PO (Adults): 1.25–2.5 mg initially; if headache returns, dose may be repeated after 2 hr (not to exceed 10 mg/24 hr); Concurrent use of cimetidine: Single dose not to exceed 2.5 mg (not to exceed 5 mg/24 hr).

(Generic available)

• Tablets: 2.5 mg; 5 mg;
• Orally disintegrating tablets: 2.5 mg; 5 mg;
• Nasal spray: 2.5 mg/100 mcL unit-dose spray device (package of 6); 5 mg/100 mcL unit-dose spray device (package of 6);

• Assess pain location, intensity, duration, and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
• Monitor for serotonin syndrome in patients taking SSRIs or SNRIs concurrently with zolmitriptan.

• Do not confuse zolmitriptan with sumatriptan.
• PO: Initial dose is 2.5 mg. Lower doses can be achieved by breaking 2.5-mg tablet.
  • Orally disintegrating tablets should be left in the package until use. Remove from the blister pouch. Do not push tablet through the blister; peel open the blister pack with dry hands and place tablet on tongue. Do not break orally disintegrating tablet. Tablet will dissolve rapidly and be swallowed with saliva. No liquid is needed to take the orally disintegrating tablet.
• Intranasal: Remove cap from nasal spray. Hold upright and block one nostril. Tilt head slightly back, insert device into opposite nostril, and depress plunger. May repeat in 2 hr.

• Inform patient that zolmitriptan should be used only during a migraine attack. It is meant to be used to relieve migraine attack, not to prevent or reduce the number of attacks.
  • Instruct patient to administer zolmitriptan as soon as symptoms appear, but it may be administered any time during an attack. If migraine symptoms return, a 2nd dose may be used. Allow at least 2 hr between doses, and do not use more than 10 mg in any 24-hr period.
  • If dose does not relieve headache, additional zolmitriptan doses are not likely to be effective; notify health care professional.
  • Advise patient that lying down in a darkened room following zolmitriptan administration may further help relieve headache.
  • May cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to notify health care professional prior to next dose of zolmitriptan if pain or tightness in the chest occurs during use. If pain is severe or does not subside, notify health care professional immediately. If wheezing; heart throbbing; swelling of eyelids, face, or lips; skin rash; skin lumps; or hives occur, notify health care professional immediately and do not take more zolmitriptan without approval of health care professional. If feelings of tingling, heat, flushing, heaviness, pressure, drowsiness, dizziness, tiredness, or sickness develop, discuss with health care professional at next visit.
  • Advise patient to avoid alcohol, which aggravates headaches, during zolmitriptan use.
  • Advise patient that overuse (use more than 10 days/mo) 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 zolmitriptan and treatment of symptoms (transient worsening of headache).
  • Advise 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. Patients concurrently taking SSRI or SNRI antidepressants should notify health care professional promptly if signs of serotonin syndrome (mental status changes: agitation, hallucinations, coma; autonomic instability: tachycardia, labile BP, hyperthermia; neuromuscular aberrations: hyper-reflexia, incoordination; and/or gastrointestinal symptoms: nausea, vomiting, diarrhea) occur.
  • Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Holding breastfeeding for 24 hr after the maternal dose will minimize infant exposure via breast milk.

• Relief of migraine attack.

Zomig, Zomig-ZMT

Zomig Rapimelt