Rifapentine


Concise Prescribing Info
Indications/Uses
TB.
Dosage/Direction for Use
Adult : PO Active pulmonary TB: Initial phase: 600 mg twice weekly for 2 months. Continuation phase: 600 mg weekly for 4 months. Latent TB: 25.1-32 kg: 600 mg; 32.1-50 kg: 750 mg; >50 kg: 900 mg once weekly for 3 months.
Dosage Details
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.
Administration
Film-Coated Tab: Should be taken with food.
Contraindications
Hypersensitivity.
Special Precautions
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.
Adverse Reactions
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.
Patient Counseling Information
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.
Drug Interactions
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.
Action
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).
Chemical Structure

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)

Storage
Store at 25°C. Protect from excessive heat and humidity.
MIMS Class
ATC Classification
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.

Disclaimer: This information is independently developed by MIMS based on Rifapentine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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