rizatriptan

Absorption: Completely absorbed after oral administration, but first-pass metabolism results in 45% bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized by monoamine oxidase-A (MAO-A); minor conversion to an active compound; 14% excreted unchanged in urine.

Half-Life: 2–3 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	30 min	1–1.5 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Ischemic or vasospastic cardiovascular, cerebrovascular, or peripheral vascular syndromes;
History of significant cardiovascular disease;
Uncontrolled hypertension;
Should not be used within 24 hr of other 5-HT₁ agonists or ergot-type compounds (dihydroergotamine);
Basilar or hemiplegic migraine;
Concurrent MAO-A inhibitor therapy or within 2 wk of discontinuing MAO-A inhibitor therapy;
Phenylketonuria (orally disintegrating tablet [ODT] contains aspartame).

Use Cautiously in:

Severe renal impairment, especially in patients on dialysis;
Moderate hepatic impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children 12 yr (oral films) or 6 yr (tablets and ODTs).

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.

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, CORONARY ARTERY VASOSPASM, MI, myocardial ischemia, VENTRICULAR ARRHYTHMIAS

Derm: TOXIC EPIDERMAL NECROLYSIS

GI: dry mouth, nausea

Neuro: dizziness, drowsiness, weakness

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with MAO-A inhibitors↑ levels and adverse reactions (concurrent use or use within 2 wk of MAO inhibitor is contraindicated).
Concurrent use with other 5-HT agonists or ergot-type compounds (dihydroergotamine) may result in ↑ vasoactive properties (avoid use within 24 hr of each other).
Propranolol↑ levels and risk of adverse reactions (↓ dose of rizatriptan; rizatriptan not recommended in children <40 kg).
↑risk of serotonin syndrome when used with SSRIs or SNRIs.

Drug-Natural Products:

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

Route/Dosage ⬆ ⬇

PO (Adults ): Tablet or ODT: 5–10 mg (use 5-mg dose in patients receiving propranolol); may be repeated in 2 hr; not to exceed 3 doses/24 hr. Oral film: 10 mg administered on the tongue; may be repeated in 2 hr; not to exceed 3 doses/24 hr.
PO (Children 6–17 yr and ≥40 kg): Tablet or ODT: 10 mg single dose (use 5-mg dose in patients receiving propranolol).
PO (Children 6–17 yr and <40 kg): Tablet or ODT: 5 mg single dose (do NOT use in patients receiving propranolol).
PO (Children 12–17 yr and ≥40 kg): Oral film: 10 mg administered on the tongue as single dose.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 10 mg
ODTs (Maxalt-MLT)peppermint flavor: 5 mg; 10 mg
Oral films: 10 mg

Assessment ⬆ ⬇

Assess pain location, character, intensity, and duration and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyper reflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs).
Assess cardiovascular status in triptan-naive patients with multiple cardiovascular risk factors (increased age, diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) before receiving rizatriptan. For patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation, consider administering the 1st dose of rizatriptan in a medically supervised setting and performing an ECG immediately following administration. Periodic cardiovascular evaluation in intermittent long-term users of rizatriptan may be used.

Implementation ⬆ ⬇

If migraine headache returns, a second dose may be administered 2 hr after first dose. Maximum daily dose should not exceed 30 mg in any 24-hr period.
PO: DNC: Tablets should be swallowed whole with liquid.
- ODTs 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. Tablet will dissolve rapidly and be swallowed with saliva. No liquid is needed to take the ODT.
- Place the oral film on tongue, where it will disintegrate within approximately 2 min and can be swallowed with saliva. No liquid is needed.

Patient/Family Teaching ⬆ ⬇

Inform patient that rizatriptan should be used only during a migraine attack. It is meant to be used for relief of migraine attacks but not to prevent or reduce the number of attacks.
Instruct patient to administer rizatriptan as soon as symptoms of a migraine attack appear, but it may be administered at 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 30 mg in any 24-hr period.
If patient has no response to first dose of rizatriptan, reconsider diagnosis of migraine before rizatriptan is administered to treat any subsequent attacks.
Caution patient not to take rizatriptan within 24 hr of other vascular headache suppressants.
Advise patient that lying down in a darkened room after rizatriptan administration may further help relieve headache.
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 rizatriptan and treatment of symptoms (transient worsening of headache).
Advise patient to notify health care professional before next dose of rizatriptan if pain or tightness in the chest occurs during use. If 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 professional at next visit.
May cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Caution patient to avoid alcohol, which aggravates headaches, during rizatriptan use.
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.
Advise patient to notify health care professional immediately if signs or symptoms of serotonin syndrome occur.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇