Company: Janssen-Cilag Ltd.
Legal category: Prescription. Hospital. Sport permitted.
Active ingredient: Bedaquiline (as fumarate) 100mg.
Description: White, round, biconvex, uncoated tablet, marked T over 207 on one side and 100 on reverse.
Presentation: 188, price available on request.
Indications: As part of a combination regimen for pulmonary multidrug-resistant tuberculosis when other regimens cannot be used due to resistance or tolerability.
Pharmacology: Bedaquiline is a diarylquinoline. Bedaquiline specifically inhibits mycobacterial adenosine 5’-triphosphate (ATP) synthase, an essential enzyme for the generation of energy in Mycobacterium tuberculosis which leads to bactericidal effects for both replicating and non-replicating tubercle bacilli.
Dosage: Adult: Swallow whole with food. Administer by directly observed therapy. Weeks 1-2: 400mg once daily. Weeks 3-24: 200mg three times per week (at least 48 hours between doses). Consider longer duration individually under close safety surveillance. Elderly: ≥65 years, limited data. Children: <18 years, not recommended.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Pregnancy, lactation; assess risk/benefit.
Special precautions: Caution: Moderate hepatic impairment (not recommended if severe), severe renal impairment, end-stage renal disease requiring haemodialysis or peritoneal dialysis. Obtain an electrocardiogram (ECG) before initiation and at least monthly after. Correct serum potassium, calcium, and magnesium if abnormal at baseline. Follow-up electrolyte monitoring if QT prolongation occurs. Initiation not recommended (assess risk/benefit) in patients with: Heart failure; QT interval as corrected by the Fridericia method (QTcF) >450ms (confirmed by repeat ECG); history of congenital QT prolongation; hypothyroidism/ bradyarrhythmia or history; history of Torsade de Pointes, hypokalemia. Discontinue if significant ventricular arrhythmia or QTcF interval of >500ms (confirmed by repeat ECG) develops. Obtain ECG to detect QT prolongation if syncope occurs. Monitor liver enzymes at baseline, monthly, and as needed; review and discontinue regimen if AST or ALT exceeds 5 times the upper limit of normal. Mortality reported. Driving/using machines. Contains lactose.
Drug interactions: Avoid: Other hepatotoxic drugs, alcohol (especially in patients with diminished hepatic reserve), moderate or strong CYP3A4 inhibitors (used systemically for more than 14 consecutive days), systemic moderate or strong CYP3A4 inducers. Not recommended: Fluoroquinolone antibiotics with potential for significant QT prolongation (i.e. gatifloxacin, moxifloxacin, sparfloxacin), efavirenz. Caution: QTc prolonging drugs, ritonavir-boosted HIV protease inhibitors.
Adverse drug reactions: Headache, dizziness, prolonged QT, gastrointestinal upset, increased transaminases, arthralgia, myalgia.
Full prescribing information and references available from Janssen-Cilag Ltd. Telephone: +44 1 494 567 444.