Formulary
Macitentan: Indications, Dosing, Side Effects and Interactions
Macitentan clinical drug profile including indications, dosing, side effects, cautions and interactions.
MedNext Academy | 3 min read
Macitentan: Indications, Dosing, Side Effects and Interactions
Macitentan clinical drug profile including indications, dosing, side effects, cautions and interactions.
Indications and dose
**Pulmonary arterial hypertension (initiated under specialist supervision)**
- **Adult** (By Mouth): 10 mg daily.
Cautions
Patients over 75 years; pulmonary veno-occlusive disease
Contraindications
Severe anaemia
Side effects
Common or very common Anaemia; fluid retention; flushing; headache; hypotension; increased risk of infection; leucopenia; nasal congestion; oedema; thrombocytopenia
Interactions
**Other interactions (27):**
- In vitro studies The cytochrome P450 CYP3A4 is the main enzyme involved in the metabolism of macitentan and in the formation of its active metabolite, with minor contribution from CYP2C8, CYP2C9,...
- Macitentan and its active metabolite do not have clinically relevant inhibitory or inducing effects on cytochrome P450 enzymes.
- Macitentan and its active metabolite are not inhibitors of hepatic or renal uptake transporters at clinically relevant concentrations, including the organic anion transporting polypeptides (OATP1B1...
- Macitentan and its active metabolite are not relevant substrates of OATP1B1 and OATP1B3 but enter the liver by passive diffusion.
- Macitentan and its active metabolite are not inhibitors of hepatic or renal efflux pumps at clinically relevant concentrations, including the multi-drug resistance protein (P-gp, MDR-1) and...
- Macitentan is not a substrate for P-gp/MDR-1.
Pregnancy
Toxicity in animal studies.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises avoid in severe impairment or if hepatic transaminases are greater than 3 times the upper limit of normal.
Renal impairment
Caution in severe impairment and avoid in patients undergoing dialysis (no information available). M Consider monitoring blood pressure and haemoglobin (risk of hypotension and anaemia). 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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