UBRELVY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for UBRELVY (UBRELVY).
Calcitonin gene-related peptide (CGRP) receptor antagonist; blocks CGRP-mediated vasodilation and nociception.
| Metabolism | Primarily metabolized by CYP3A4; minor contribution from CYP2C9. |
| Excretion | Primarily hepatic metabolism via CYP3A4, with 42% of dose excreted in feces (6% unchanged) and 26% in urine (1% unchanged). |
| Half-life | Terminal elimination half-life is approximately 50 hours, supporting once-daily dosing. |
| Protein binding | High (approx. 96%) bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 120 L (1.7 L/kg for a 70 kg individual), indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is approximately 50% (range 42-60%). |
| Onset of Action | Oral: Onset of clinically meaningful headache relief occurs as early as 2 hours post-dose. |
| Duration of Action | Duration of action is approximately 24 hours per dose, consistent with once-daily administration; maximal effect may take up to 8 weeks. |
| Molecular Weight | 497.46 |
100 mg orally once, may repeat once after at least 2 hours if needed; maximum 200 mg per 24 hours.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min). Not studied in severe renal impairment (eGFR <30 mL/min) or ESRD; use with caution. |
| Liver impairment | Mild hepatic impairment (Child-Pugh A): no dose adjustment. Moderate (Child-Pugh B): 50 mg orally initially, may repeat once after at least 2 hours if needed; maximum 100 mg per 24 hours. Severe (Child-Pugh C): not recommended. |
| Pediatric use | Not indicated for pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; pharmacokinetics similar to younger adults. Consider renal and hepatic function. |
| 1st trimester | Limited human data; animal studies show no evidence of harm, but there is insufficient human data to rule out risk. |
| 2nd trimester | Limited human data; animal studies show no evidence of harm, but there is insufficient human data to rule out risk. |
| 3rd trimester | Limited human data; animal studies show no evidence of harm, but there is insufficient human data to rule out risk. |
Clinical note
Comprehensive clinical and safety monograph for UBRELVY (UBRELVY).
| Placental transfer | Expected to cross placenta due to molecular weight <500 Da; specific data in humans are lacking. |
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Weigh risk versus benefit. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to ubrogepant or any excipient
| Precautions | May cause hypersensitivity reactions including angioedema and urticaria, Avoid concurrent use with strong CYP3A4 inhibitors (e.g., ketoconazole) due to increased ubrogepant exposure |
| Food/Dietary | Grapefruit and grapefruit juice may increase ubrogepant concentrations (CYP3A4 inhibition); avoid concomitant consumption. No other significant food interactions reported. |
| Clinical Pearls | Ubrogepant is a CGRP receptor antagonist indicated for acute treatment of migraine with or without aura. Onset of efficacy is typically within 2 hours. Do not use for migraine prophylaxis. Maximum dose is 200 mg per 24 hours (one 100 mg tablet, may repeat after 2 hours if needed). Avoid use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) as they increase ubrogepant exposure. Dose adjustment required with moderate CYP3A4 inhibitors (e.g., verapamil, fluconazole): initial dose 50 mg, max single dose 50 mg, max daily dose 100 mg. Contraindicated with strong CYP3A4 inducers (e.g., rifampin) due to potential for subtherapeutic levels. Monitor for hypersensitivity reactions, including dyspnea and rash. Not recommended in patients with severe hepatic impairment (Child-Pugh C) or end-stage renal disease. Safety in pregnancy not established; avoid if possible. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | No adequate human data; animal studies show no teratogenicity at exposures up to 19 times human AUC at 200 mg/day. Risk cannot be excluded; use only if benefit outweighs risk. |
| Fetal Monitoring | No specific monitoring required beyond routine prenatal care. |
| Fertility Effects | No human data; no impairment of fertility in animal studies. |
| Patient Advice | Take UBRELVY only when you have a migraine headache, not to prevent them. · The usual dose is one 50 mg or 100 mg tablet at the first sign of migraine. You may take a second dose if needed, at least 2 hours after the first, but do not exceed 200 mg in 24 hours. · Do not take UBRELVY if you are taking certain medications (e.g., for fungal infections, antibiotics, or HIV) without consulting your doctor. · Common side effects include nausea, fatigue, and dizziness. Serious allergic reactions (rash, hoarseness, difficulty breathing) require immediate medical care. · Store at room temperature, away from moisture and heat. Keep out of reach of children. |