Formulary
Rimegepant: Indications, Dosing, Side Effects and Interactions
Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist which inhibits the function of CGRP, thereby preventing migraine attacks.
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Rimegepant: Indications, Dosing, Side Effects and Interactions
Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist which inhibits the function of CGRP, thereby preventing migraine attacks.
Drug action
Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist which inhibits the function of CGRP, thereby preventing migraine attacks.
Indications and dose
**Treatment of acute migraine**
- **Adult** (By Mouth): 75 mg once daily if required.
**Prophylaxis of episodic migraine [in patients who have at least 4 migraine attacks per month]**
- **Adult** (By Mouth): 75 mg once daily on alternate days.
Side effects
Common or very common Nausea Uncommon Hypersensitivity Side-effects, further information Hypersensitivity reactions, including dyspnoea and rash, can occur days after administration. If a hypersensitivity reaction occurs, rimegepant should be discontinued.
Interactions
**Severe interactions:**
- Concomitant administration of rimegepant with itraconazole resulted in a significant increase in rimegepant exposure (AUC by 4-fold and C max 1.5-fold).
- Concomitant administration of rimegepant with rifampicin resulted in a significant decrease (AUC reduced by 80% and C max by 64%) in rimegepant exposure, which may lead to loss of efficacy.
- Concomitant administration of rimegepant with cyclosporine (a potent P-gp and BCRP inhibitor) or with quinidine (a selective P-gp inhibitor) resulted in a significant increase of similar magnitude...
**Other interactions (9):**
- Rimegepant is a substrate of CYP3A4, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) efflux transporters (see section 5.2).
- CYP3A4 inhibitors Inhibitors of CYP3A4 increase plasma concentrations of rimegepant.
- Concomitant administration of rimegepant with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ritonavir) is not recommended (see section 4.4).
- Concomitant administration of rimegepant with medicinal products that moderately inhibit CYP3A4 (e.g., diltiazem, erythromycin, fluconazole) may increase exposure to rimegepant.
- Concomitant administration of rimegepant with fluconazole resulted in increased exposures of rimegepant (AUC by 1.8-fold) with no relevant effect on C max .
- Another dose of rimegepant within 48 hours should be avoided when it is concomitantly administered with moderate inhibitors of CYP3A4 (e.g., fluconazole) (see section 4.2).
Pregnancy
Avoid-limited information available. M
Breast feeding
Specialist sources indicate present in milk but amount probably too small to be harmful. Consider an alternative drug if breast-feeding a neonate (pre or full-term)-limited information available.
Hepatic impairment
Avoid in severe impairment (increased risk of exposure). M
Renal impairment
Caution in severe impairment (increased risk of exposure). M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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