Formulary
Ambrisentan: Indications, Dosing, Side Effects and Interactions
Ambrisentan clinical drug profile including indications, dosing, side effects, cautions and interactions.
MedNext Academy | 3 min read
Ambrisentan: Indications, Dosing, Side Effects and Interactions
Ambrisentan clinical drug profile including indications, dosing, side effects, cautions and interactions.
Indications and dose
**Pulmonary arterial hypertension (initiated by a specialist)**
- **Adult** (By Mouth): 5 mg once daily, increased if necessary to 10 mg once daily.
**Pulmonary arterial hypertension (initiated by a specialist) for ambrisentan**
- **Child 8-17 years (body-weight 20-34 kg)** (By mouth): 2.5 mg once daily, increased if necessary to 5 mg once daily.
- **Child 8-17 years (body-weight 35-49 kg)** (By mouth): 5 mg once daily, increased if necessary to 7.5 mg once daily.
- **Child 8-17 years (body-weight 50 kg and above)** (By mouth): 5 mg once daily, increased if necessary to 10 mg once daily.
Cautions
Not to be initiated in significant anaemia; pulmonary veno-occlusive disease
Contraindications
Idiopathic pulmonary fibrosis
Side effects
Common or very common Abdominal pain; anaemia; asthenia; chest discomfort; constipation; diarrhoea; dizziness; dyspnoea; epistaxis; fluid retention; flushing; headaches; heart failure; hypersensitivity; hypotension; increased risk of infection; nasal congestion; nausea; palpitations; peripheral oedema; skin reactions; syncope; tinnitus; upper respiratory tract congestion; vision disorders; vomiting Uncommon Hepatic disorders; sudden hearing loss
Interactions
**Severe interactions:**
- Phosphodiesterase inhibitors Co-administration of ambrisentan with a phosphodiesterase inhibitor, either sildenafil or tadalafil (both substrates of CYP3A4) in healthy volunteers did not...
- Oral contraceptives In a clinical study in healthy volunteers, steady-state dosing with ambrisentan 10 mg once daily did not significantly affect the single-dose pharmacokinetics of the ethinyl...
- Based on this pharmacokinetic study, ambrisentan would not be expected to significantly affect exposure to oestrogen- or progestogen- based contraceptives.
- Warfarin also had no clinically significant effects on the pharmacokinetics of ambrisentan.
- Ketoconazole Steady-state administration of ketoconazole (a strong inhibitor of CYP3A4) did not result in a clinically significant increase in exposure to ambrisentan (see section 5.2).
**Other interactions (16):**
- Ambrisentan does not inhibit or induce phase I or II drug metabolising enzymes at clinically relevant concentrations in in vitro and in vivo non-clinical studies, suggesting a low potential for...
- Cyclosporine A Steady-state co-administration of ambrisentan and cyclosporine A resulted in a 2-fold increase in ambrisentan exposure in healthy volunteers.
- This may be due to the inhibition by cyclosporine A of transporters and metabolic enzymes involved in the pharmacokinetics of ambrisentan.
- Therefore, when co-administered with cyclosporine A, the dose of ambrisentan in adult patients or paediatric patients weighing 50 kg should be limited to 5 mg once daily (see section 4.2).
- Multiple doses of ambrisentan had no effect on cyclosporine A exposure, and no dose adjustment of cyclosporine A is warranted.
- Rifampicin Co-administration of rifampicin (an inhibitor of Organic Anion Transporting Polypeptide [OATP], a strong inducer of CYP3A and 2C19, and inducer of P-gp and...
Pregnancy
Avoid (teratogenic in animal studies).
Breast feeding
Manufacturer advises avoid-no information available.
Hepatic impairment
Manufacturer advises avoid in severe impairment or if baseline serum transaminases exceed 3 times the upper limit of normal.
Renal impairment
Use with caution if creatinine clearance less than 30 mL/minute. M See Prescribing in renal impairment .
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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