.Pharmacolibrary.Drugs.J_AntiinfectivesForSystemicUse.J04A_DrugsForTreatmentOfTuberculosis.J04AM06_RifampicinPyrazinamideEt.RifampicinPyrazinamideEt

Information

This combination drug is used for the treatment of active tuberculosis infection and is composed of rifampicin, pyrazinamide, ethambutol, and isoniazid. It is an essential, approved regimen in first-line tuberculosis therapy recommended by the WHO and many national tuberculosis programs. It targets Mycobacterium tuberculosis through multiple mechanisms: rifampicin inhibits RNA synthesis, isoniazid inhibits mycolic acid synthesis, pyrazinamide disrupts membrane energetics, and ethambutol interferes with cell wall synthesis.

Pharmacokinetics

Population pharmacokinetics in adult patients with pulmonary tuberculosis receiving fixed-dose combination tablets under directly observed therapy; mixed male and female, mean age around 38 years.

References

1. Chen, C, et al., & Simonsson, US (2016). Population pharmacokinetics, optimised design and sample size determination for rifampicin, isoniazid, ethambutol and pyrazinamide in the mouse. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 93 319–333. DOI:10.1016/j.ejps.2016.07.017 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27473307

2. Denti, P, et al., & Andersen, AB (2015). Pharmacokinetics of Isoniazid, Pyrazinamide, and Ethambutol in Newly Diagnosed Pulmonary TB Patients in Tanzania. PloS one 10(10) e0141002–None. DOI:10.1371/journal.pone.0141002 PUBMED:https://pubmed.ncbi.nlm.nih.gov/26501782

3. Langdon, G, et al., & Simonsson, US (2005). Population pharmacokinetics of rifapentine and its primary desacetyl metabolite in South African tuberculosis patients. Antimicrobial agents and chemotherapy 49(11) 4429–4436. DOI:10.1128/AAC.49.11.4429-4436.2005 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16251279

Revisions

• 06/2025 initial generated model