calcitonin gene-related peptide receptor antagonists
Acute treatment of migraine with or without aura.
Binds to and antagonizes the calcitonin gene-related peptide (CGRP) receptor, which reduces the neuroinflammatory and vasodilatory effects of CGRP.
Relief of pain associated with acute migraine attacks.
Absorption: Rapidly absorbed. Absorption delayed by high-fat food.
Distribution: Widely distributed to extravascular tissues.
Metabolism and Excretion: Primarily metabolized by the liver via CYP3A4 enzyme to inactive metabolites. Eliminated in bile/feces (42% as unchanged drugs) and urine (6% as unchanged drug).
Half-life: 5–7 hr.
TIME/ACTION PROFILE (pain relief)
|PO||30–60 min||2 hr||24 hr|
- Concurrent use of strong CYP3A4 inhibitors;
- End-stage renal disease (CCr <15 mL/min).
Use Cautiously in:
- Severe hepatic impairment (↓ dose);
- Severe renal impairment (CCr 15–29 mL/min);
- OB: Safety not established in pregnancy;
- Lactation: Safety not established in breast feeding;
- Pedi: Safety and effectiveness in children not established.
Adverse Reactions/Side Effects
GI: dry mouth, nausea
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, or ketoconazole may significantly ↑ levels and risk of toxicity; concurrent use contraindicated.
- Moderate CYP3A4 inhibitors as well as weak CYP3A4 inhibitors, including ciprofloxacin, cyclosporine, fluconazole, fluvoxamine, or verapamil may ↑ levels and risk of toxicity; ↓ ubrogepant dose.
- Strong CYP3A4 inducers, including phenobarbital, phenytoin, or rifampin may significantly ↓ levels and effectiveness; avoid concurrent use.
- Moderate CYP3A4 inducers or weak CYP3A4 inducers may ↓ levels and effectiveness; ↑ ubrogepant dose.
- P-glycoprotein (P-gp) inhibitors as well as breast cancer resistant protein (BCRP) inhibitors, including carvedilol, eltrombopag, or quinidine , may ↑ levels and risk of toxicity; ↓ ubrogepant dose.
St. John's wort may ↓ levels and effectiveness; avoid concurrent use.
Grapefruit juice may ↑ levels and risk of toxicity; ↓ ubrogepant dose.
PO (Adults): 50 mg or 100 mg initially; if response is inadequate at 2 hr, may repeat dose (not to exceed 200 mg/24 hr). Concurrent use of moderate CYP3A4 inhibitor– 50 mg initially (not to exceed 50 mg/24 hr). Concurrent use of weak CYP3A4 inhibitor– 50 mg initially; if response is inadequate at 2 hr, may repeat dose (not to exceed 100 mg/24 hr). Concurrent use of weak or moderate CYP3A4 inducer– 100 mg initially; if response is inadequate at 2 hr, may repeat dose (not to exceed 200 mg/24 hr). Concurrent use of P-gp or BCRP inhibitor– 50 mg initially; if response is inadequate at 2 hr, may repeat dose (not to exceed 100 mg/24 hr).
PO (Adults): CCr 15–29 mL/min– 50 mg initially; if response is inadequate at 2 hr, may repeat dose (not to exceed 100 mg/24 hr).
PO (Adults): Severe hepatic impairment (Child–Pugh Class C)– 50 mg initially; if response is inadequate at 2 hr, may repeat dose (not to exceed 100 mg/24 hr).
Tablets: 50 mg, 100 mg
- Assess pain location, character, intensity, and duration and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
- PO Administer without regard to food. If needed, a second dose may be taken at least 2 hr after initial dose.
- Instruct patient to take ubrogepant as soon as symptoms of a migraine attack appear, but it may be administered any time during an attack. If migraine symptoms return, a second dose may be used. Allow at least 2 hr between doses, and do not use more than 100 mg in any 24-hr period. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
- Inform patient that ubrogepant should only be used 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.
- Advise patient to avoid grapefruit and grapefruit juice during therapy. Instruct patient not take a second tablet within 24 hr if grapefruit or grapefruit juice was consumed.
- May cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient to avoid alcohol, which aggravates headaches, during ubrogepant use.
- Advise patient that lying down in a darkened room following ubrogepant administration may further help relieve 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, especially St. John's wort.
- Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breast feeding.
Relief of migraine attack.
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