zolmitriptan

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;
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 women, men>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).

Adv. Reactions/Side Effects ⬆ ⬇

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, hypoesthesia, paresthesia, vertigo, weakness

Interactions ⬆ ⬇

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).
MAO inhibitors↑ levels and risk of toxicity; avoid use within 2 wk of MAO inhibitors.
Hormonal contraceptives may ↑ levels and risk of toxicity.
Cimetidine↑ levels and risk of toxicity.
↑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.

Availability ⬆ ⬇

(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)

Route/Dosage ⬆ ⬇

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).

Hepatic Impairment

PO (Adults ): Moderate to severe hepatic impairment (oral tablets only): 1.25 mg initially; if headache returns, dose may be repeated after 2 hr (not to exceed 5 mg/24 hr).
(Adults and Children ≥12 yr): Single 2.5 mg initially (maximum single dose = 5 mg); 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).

US Brand Names ⬆ ⬇

Zomig, ~~Zomig-ZMT~~

Action ⬆ ⬇

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

Therapeutic effects:

Relief of acute attacks of migraine.

Classifications ⬆ ⬇

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: five ht1 agonists

Pharmacokinetics ⬆ ⬇

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).

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

(relief of headache)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.5 hr*	unknown
Intranasal	unknown	3 hr	unknown

*3 hr for orally disintegrating tablets.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Advise 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 ↓ the number of attacks.
- Advise 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 ≥2 hr between doses, and do not use >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 provider.
- 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 provider before 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 provider immediately. If wheezing; heart throbbing; swelling of eyelids, face, or lips; skin rash; skin lumps; or hives occur, notify health care provider immediately and do not take more zolmitriptan without approval of health care provider. If feelings of tingling, heat, flushing, heaviness, pressure, drowsiness, dizziness, tiredness, or sickness develop, discuss with health care provider at next visit.
- Advise patient to avoid alcohol, which aggravates headaches, during zolmitriptan use.
- Advise patient that overuse (>10 days/mo) may lead to exacerbation of headache (migraine-like daily headaches or as a marked ↑ in frequency of migraine attacks). May require gradual withdrawal of zolmitriptan and treatment of symptoms (transient worsening of headache).
- Advise patient taking SSRI or SNRI antidepressants to notify health care provider if signs/symptoms of serotonin syndrome (mental status changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyperreflexia, incoordination], gastrointestinal symptoms [nausea, vomiting, diarrhea]) occur.
- Advise women of reproductive potential to notify health care provider 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.

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Indications ⬇

Contraind./Precautions ⬆ ⬇