Generic
Rimegepant
2 brands available in the market
At a glance
Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist used for the acute treatment of migraine with or without aura and preventive treatment of episodic migraine in adults.
Description
Rimegepant is an antagonist of the CGRP receptor, competing with CGRP for occupancy at these receptors. CGRP is a potent vasodilator expressed in primary sensory neurons and implicated in migraine pathogenesis - CGRP levels are elevated during migraine attacks and return to normal after triptan treatment. Rimegepant prevents the actions of CGRP, ultimately terminating migraine headache pain.
Indications
- Acute treatment of migraine (with or without aura)
- Preventive treatment of episodic migraine
Therapeutic class
Other drugs for migraine
Pharmacological class
CGRP Receptor Antagonist (Gepant)
Pharmacology
Rimegepant is a CGRP receptor antagonist that competes with CGRP for receptor occupancy. CGRP is a potent vasodilator expressed in primary sensory neurons and is implicated in migraine pathogenesis - CGRP levels are elevated during migraine attacks and return to normal after treatment. Rimegepant prevents CGRP actions, terminating migraine headache pain.
Mechanism of action
Relieves migraine pain by blocking CGRP receptors.
Dosage
Adult Dose (Oral):
- Acute migraine: 75 mg as needed; max 75 mg in 24 hours
- Episodic migraine prevention: 75 mg every other day
- With strong CYP3A4 inhibitors: Avoid use
- With moderate CYP3A4 inhibitors: Avoid another dose within 48 hours
- With potent P-gp inhibitors: Avoid another dose within 48 hours
Administration
- Take at the same time each day
- Swallow tablet whole
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Nausea
- Stomach pain
- Indigestion
- Allergic reactions (dyspnea, rash)
Precautions & warnings
- Hypersensitivity reactions: Dyspnea, rash; discontinue if occurs
- Avoid use in severe hepatic impairment (Child-Pugh C)
- Avoid use in patients with ESRD (CrCl <15 mL/min)
- Avoid concomitant use with strong CYP3A4 inhibitors/inducers
Contraindications
- History of hypersensitivity reaction to rimegepant or any component
Drug interactions
- Strong CYP3A4 inhibitors: Avoid concomitant use
- Moderate CYP3A4 inhibitors: Avoid another dose within 48 hours
- Strong CYP3A4 inducers: Avoid concomitant use
- Potent P-gp inhibitors (amiodarone, cyclosporine, quinidine): Avoid another dose within 48 hours
Food interactions
It is not known whether it is safe to consume alcohol with Rimegepant.
Use in pregnancy
Use in Pregnancy: No adequate data on use in pregnant women; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No data on presence of rimegepant or metabolites in human milk; consult your doctor.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
No clinically significant pharmacokinetic differences between elderly and younger subjects; sufficient numbers of patients aged 65 and over not studied.
Renal / hepatic impairment
Renal Impairment: No dose adjustment needed in mild, moderate, or severe renal impairment; not studied in ESRD (CrCl <15 mL/min); avoid use in ESRD; consult your doctor.
Hepatic Impairment: No dose adjustment needed in mild (Child-Pugh A) and moderate (Child-Pugh B) hepatic impairment; plasma concentrations significantly higher in severe (Child-Pugh C) hepatic impairment; avoid use in severe hepatic impairment; consult your doctor.
Overdose effects
Limited clinical experience with overdose; treatment: general supportive measures, monitoring of vital signs; no specific antidote; not significantly removed by dialysis (high protein binding).
Storage conditions
Keep below 25°C, away from light and moisture; keep out of reach of children.
Chemical structure
Rimegepant