Rifapentine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Tuberculosis
Adult: Active pulmonary TB:
Initial phase: 600 mg twice weekly (with an interval of ≥72 hours) for 2 months, in combination with other antimycobacterials.
Continuation phase: 600 mg once weekly for 4 months, in combination with isoniazid or another appropriate antimycobacterial drug.

Latent TB: 25.1-32 kg: 600 mg; 32.1-50 kg: 750 mg; >50 kg: 900 mg. Max: 900 mg. Doses are given once weekly for 3 months, in combination with isoniazid.
Child: Active pulmonary TB (in combination with other antimycobacterials): ≥12 years Same as adult dose.

Latent TB: ≥2-11 years 10-14 kg: 300 mg; 14.1-25 kg: 450 mg; 25.1-32 kg: 600 mg; 32.1-50 kg: 750 mg; >50 kg: 900 mg. Doses are given once weekly for 3 months in combination with isoniazid.
Cách dùng
Film-Coated Tab: Should be taken with food.
Chống chỉ định
Hypersensitivity.
Thận trọng
Patient with porphyria, bilateral pulmonary disease; cavity pulmonary lesions and/or positive sputum cultures after initial phase. HIV-seropositive patients. Hepatic impairment. Children. Pregnancy and lactation. Concomitant use with protease inhibitors and reverse transcriptase inhibitors.
Phản ứng phụ
Significant: Hyperbilirubinaemia, hepatotoxicity, discolouration of body fluids, hyperuricaemia, hypersensitivity including anaphylaxis.
Blood and lymphatic system disorders: Anaemia, lymphonaemia, neutropenia, leukocytosis, thrombocytosis, thrombocytopenia, lymphadenopathy, nonprotein nitrogen increased.
Cardiac disorders: Chest pain, oedema.
Endocrine disorders: Hypoglycaemia, hyperglycaemia, gout, hyperphosphataemia.
Eye disorders: Conjunctivitis.
Gastrointestinal disorders: Dyspepsia, vomiting, nausea, diarrhoea, anorexia, abdominal pain, constipation.
General disorders and administration site conditions: Fever, fatigue.
Infections and infestations: Influenza, herpes zoster.
Musculoskeletal and connective tissue disorders: Back pain, arthralgia.
Nervous system disorders: Headache, dizziness.
Renal and urinary disorders: Pyuria, proteinuria, haematuria, UTI, cystitis.
Respiratory, thoracic and mediastinal disorders: Heamoptysis, cough.
Skin and subcutaneous tissue disorders: Rash, pruritus, diaphoresis.
Potentially Fatal: Clostridium difficile-associated diarrhoea (CDAD), colitis.
Thông tin tư vấn bệnh nhân
This drug may produce red/orange discolouration of urine, faeces, saliva, sweat, tears, skin, teeth, tongue, and CSF. May permanently stain dentures or contact lenses; remove denture and contact lenses during therapy.
MonitoringParameters
Perform culture and sensitivity test prior to therapy. Obtain LFT in patients with pre-existing hepatic impairment prior to therapy and every 2-4 week during therapy. Monitor for signs of hypersensitivity, severe or bloody diarrhoea.
Tương tác
May cause significant decrease in the plasma concentration and loss of therapeutic effect of protease inhibitors or reverse transcriptase inhibitors. May reduce the activity of CYP3A4 substrates (e.g. verapamil, fluconazole, methadone, quinidine, corticosteroids, flouroquinolones, warfarin, tacrolimus). May diminish therapeutic effects of barbiturates, anticonvulsants, benzodiazepines, clofibrate, oral contraceptives.
Food Interaction
Increased absorption with food (particularly high-fat meals).
Lab Interference
May inhibit standard microbiological assays for serum folate and vitamin B12.
Tác dụng
Description: Rifapentine is a long-acting semisynthetic rifamycin derivative. It inhibits DNA-dependent RNA polymerase in susceptible strains of intracellular and extracellular Mycobacterium tuberculosis (MTB) organisms.
Pharmacokinetics:
Absorption: Increased absorption with food (particularly high-fat meals). Bioavailability: 70%. Time to peak serum concentration: 3-10 hours.
Distribution: Volume of distribution: Approx 70 L. Plasma protein binding: Approx 98% primarily to albumin (rifapentine); approx 93% (25-desacetyl rifapentine).
Metabolism: Metabolised in the liver by esterase enzyme to form the active metabolite 25-desacetyl rifapentine.
Excretion: Mainly via faeces (70% as unchanged drug and metabolites); urine (17%, as metabolites). Elimination half-life: Approx 17 hours (rifapentine); approx 24 hours (25-desacetyl rifapentine).
Đặc tính

Chemical Structure Image
Rifapentine

Source: National Center for Biotechnology Information. PubChem Database. Rifapentine, CID=135749824, https://pubchem.ncbi.nlm.nih.gov/compound/Rifapentine (accessed on Jan. 22, 2020)

Bảo quản
Store at 25°C. Protect from excessive heat and humidity.
Phân loại MIMS
Phân loại ATC
J04AB05 - rifapentine ; Belongs to the class of antibiotics. Used in the systemic treatment of tuberculosis.
References
Anon. Rifapentine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 02/05/2018.

Anon. Rifapentine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/05/2018.

Buckingham R (ed). Rifapentine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/05/2018.

Priftin Tablet, Film Coated (Sanofi-Aventis U.S. LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 02/05/2018.

Priftin Tablets (Sanofi-Aventis U.S. LLC). U.S. FDA. https://www.fda.gov/. Accessed 02/05/2018.

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