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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for UBRELVY (UBRELVY).
| Breastfeeding | No human data; present in rat milk; M/P ratio unknown. Consider developmental benefits and maternal need. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
["Concomitant use with strong CYP3A4 inducers (e.g., rifampin)","History of hypersensitivity to ubrogepant or any component of the formulation"]
| Precautions | ["May cause hypersensitivity reactions including angioedema and urticaria","Avoid concurrent use with strong CYP3A4 inhibitors (e.g., ketoconazole) due to increased ubrogepant exposure"] |
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| Fertility Effects | No human data; no impairment of fertility in animal studies. |