Bedaquiline


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Pulmonary multidrug-resistant tuberculosis
Adult: In combination with ≥3 other anti-TB agents when an effective treatment regimen cannot otherwise be provided: Weeks 1-2: 400 mg once daily. Weeks 3-24: 200 mg 3 times a week (with at least 48 hours between doses). Administer by directly observed therapy (DOT). Consider local treatment guidelines when choosing the appropriate combination regimen.
Child: 12-<18 years ≥30 kg: Same as adult dose. Treatment recommendations may vary among countries (refer to detailed product or local treatment guidelines).
Cách dùng
tab: Should be taken with food.
Chống chỉ định
Hypersensitivity.
Thận trọng
Patient with heart failure; hypokalaemia, hypocalcaemia, hypomagnesaemia; QTc interval 450-500 milliseconds (derived using Fridericia's formula), personal or family history of congenital QT prolongation; existing or history of hypothyroidism or bradyarrhythmia; history of torsades de pointes. Not intended for use in latent, extrapulmonary (e.g. CNS, bone), or drug-sensitive TB, or infection caused by nontuberculous mycobacteria. Discontinue treatment (including all other QT prolonging drugs) if evidence of QTcF interval is >500 milliseconds (confirmed by repeat ECG) or serious ventricular arrhythmia develops. Moderate to severe hepatic impairment; severe renal impairment (CrCl <30 mL/min) or ESRD requiring haemodialysis or peritoneal dialysis. Children. Pregnancy and lactation. Concomitant use with QT interval prolonging drugs (e.g. ketoconazole, clofazimine).
Tác dụng không mong muốn
Significant: QTc interval prolongation, elevated serum transaminases, increased mortality.
Cardiac disorders: Chest pain.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea.
Investigations: Increased serum amylase.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Haemoptysis.
Skin and subcutaneous tissue disorders: Rash.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Perform culture and susceptibility tests; consult local institutional recommendations before treatment initiation due to risks of antibacterial resistance. Obtain ECG at baseline, after 2 weeks, then monthly during treatment, or more frequently when used concurrently with other QTc interval prolonging drugs or in at-risk patients (e.g. torsades de pointes, congenital long QT syndrome). Monitor serum K, Ca, and Mg (at baseline [correct if necessary] and during treatment); AST, ALT, alkaline phosphatase, and bilirubin (at baseline, monthly during treatment, and as necessary). Monitor for signs and symptoms of hepatic dysfunction. Evaluate sputum specimens every month throughout and at the end of treatment (even if cultures become negative).
Tương tác
May reduce exposure and therapeutic effect with moderate or strong CYP3A4 inducers (e.g. rifampicin, efavirenz, carbamazepine, phenytoin); avoid concomitant use. May increase serum concentration with moderate or strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir, ciprofloxacin, erythromycin); avoid concomitant use for >14 consecutive days unless necessary. Concomitant use with QT interval prolonging drugs including ketoconazole, fluoroquinolones (e.g. moxifloxacin, gatifloxacin), macrolide antibiotics (e.g. clarithromycin), and clofazimine may cause additive or synergistic effects on the QT interval. Hepatotoxic drugs may increase the risk of hepatic-related adverse reactions; avoid concomitant use.
Tương tác với thức ăn
Administration with food increases bioavailability. Avoid concomitant use with alcohol as it may increase the risk of hepatotoxicity. May reduce exposure and therapeutic effect with St. John's wort; avoid concomitant use.
Tác dụng
Description: Bedaquiline is a diarylquinoline antimycobacterial which inhibits the proton transfer chain of mycobacterial ATP synthase, an enzyme necessary for energy generation in Mycobacterium tuberculosis. This action leads to bactericidal effects for both replicating and non-replicating tubercle bacilli.
Pharmacokinetics:
Absorption: Well absorbed. Increased bioavailability with food. Time to peak plasma concentration: Approx 5 hours.
Distribution: Volume of distribution: Approx 164 L. Plasma protein binding: >99.9%.
Metabolism: Metabolised in the liver by CYP3A4 isoenzyme to form less potent N-monodesmethyl metabolite (M2).
Excretion: Mainly via faeces; urine (≤0.001% as unchanged drug). Terminal elimination half-life: Approx 5.5 months (range: 2-8 months).
Đặc tính

Chemical Structure Image
Bedaquiline

Source: National Center for Biotechnology Information. PubChem Database. Bedaquiline, CID=5388906, https://pubchem.ncbi.nlm.nih.gov/compound/Bedaquiline (accessed on Jan. 21, 2020)

Bảo quản
Store between 15-30°C. Protect from light.
Phân loại MIMS
Thuốc kháng lao
Phân loại ATC
J04AK05 - bedaquiline ; Belongs to the class of other drugs used in the systemic treatment of tuberculosis.
Tài liệu tham khảo
Anon. Bedaquiline Fumarate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/10/2021.

Anon. Bedaquiline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/10/2021.

Buckingham R (ed). Bedaquiline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2021.

Janssen-Cilag (New Zealand) Ltd. Sirturo 100 mg Tablets data sheet 31 July 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 05/10/2021.

Joint Formulary Committee. Bedaquiline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2021.

Sirturo (Janssen-Cilag Ltd.). MIMS Thailand. http://www.mims.com/thailand. Accessed 05/10/2021.

Sirturo 100 mg Tablets (Janssen-Cilag Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/10/2021.

Sirturo 100 mg Tablets (Johnson & Johnson Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 05/10/2021.

Sirturo Tablet (Janssen Products, LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 05/10/2021.

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