Bosentan Monohydrate
Cardiac Therapy · Endothelin receptor antagonist
Indications
Pulmonary arterial hypertension to improve exercise capacity and symptoms in patients with grade II and III functional status. Systemic sclerosis with ongoing digital ulcer disease to reduce the number of new digital ulcers.
Dosage
Hypertension: Adults: Initially 62.5 mg twice daily for 4 wk, increasing to maintenance of 125 mg twice daily. Some patients may benefit from 250 mg twice daily. Max: 500 mg/day. Children: Not recommended. Systemic sclerosis: Adults: Initially 62.5 mg twice daily for 4 wk, increasing to maintenance of 125 mg twice daily. Children: Not recommended.
Adverse Effects
Headache, flushing, abnormal hepatic function, anaemia, infected skin ulcer, urinary tract infection, dyspnoea, GI upset, erythema, dermatitis, pain in extremity, back pain, peripheral oedema, hepatic disorders, syncope, palpitations, hypotension, GORD, erythema, nasal congestion.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Moderate to severe hepatic impairment, hepatic aminotransferase levels >3x upper limit. Precautions: Severe pulmonary arterial hypertension. Raised liver enzymes; monitor prior to and at monthly intervals during therapy and two weeks after any increase in dose. Advise patients to report any signs suggestive of liver damage. Monitor haemoglobin prior to and at monthly intervals during therapy for first 4 months and quarterly thereafter. Monitor for signs of fluid retention. Women of childbearing potential should use non-hormonal contraception during treatment; perform monthly pregnancy test where appropriate. Withdraw gradually.
Interactions
CYP3A4 inhibitors (particularly potent inhibitors e.g. ketoconazole, itraconazole, ritonavir) or CYP3A4 inducers, CYP2C9 inhibitors (voriconazole, fluconazole), contraceptives, cyclosporin, rifampicin, glibenclamide, tacrolimus, sirolimus, sildenafil, tadalafil, simvastatin, immunosuppressants, warfarin, protease inhibitors, nevirapine.
Advice to Patient
Take with or without meals. Contact prescriber immediately if there is hepatic dysfunction, including yellow skin or eyes, fever, nausea, vomiting, fatigue or abdominal pain. Do not miss follow-up tests.
Pharmacokinetics
Metabolism: Hepatic. Bioavailability: Approx. 50%. Half-life elimination: Approx. 5 hrs. Time to peak, plasma: 3-5 hrs. Excretion: Faeces, urine.
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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