Rifapentine: Difference between revisions
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'''| [[Rifapentine labels and packages|Labels and Packages]]''' | '''| [[Rifapentine labels and packages|Labels and Packages]]''' | ||
Revision as of 17:12, 6 January 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]
Overview
Rifapentine is an antibiotic which is similar to rifampin and rifabutin in structure and activity. It is a rifamycin antibiotic. It is used in combination with other antimycobacterial drugs . It can be used once or twice per week .
Category
Antimycobacterial
US Brand Names
PRIFTIN®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Dosage and Administration | How Supplied | Labels and Packages
Mechanisms of Action
Rifapentine is a rifamycin antiobiotic. The antibacterial activity of rifapentine relies on the inhibition of bacterial DNA-dependent RNA synthesis.[1] This is due to the high affinity of rifapentine to prokaryotic RNA polymerase. Crystal structure data of the antibiotic bound to RNA polymerase indicates that rifapentine blocks synthesis by causing strong steric clashes with the growing oligonucleotide ("steric-occlusion" mechanism).[2][3] If rifapentine binds the polymerase after the chain extension process has started, no inhibition is observed on the biosynthesis, consistent with a steric-occlusion mechanism.
References
- ↑ Calvori, C.; Frontali, L.; Leoni, L.; Tecce, G. (1965). "Effect of rifamycin on protein synthesis". Nature. 207 (995): 417–8. doi:10.1038/207417a0. PMID 4957347.
- ↑ Campbell, E.A., Korzheva, N., Mustaev, A., Murakami, K., Nair, S., Goldfarb, A., Darst, S.A. (2001). "Structural mechanism for rifampicin inhibition of bacterial RNA polymerase". Cell. 104 (6): 901–12. doi:10.1016/S0092-8674(01)00286-0. PMID 11290327.
- ↑ Feklistov, A., Mekler, V., Jiang, Q., Westblade, L.F., Irschik, H., Jansen, R., Mustaev, A., Darst, S.A., Ebright, R.H. (2008). "Rifamycins do not function by allosteric modulation of binding of Mg2+ to the RNA polymerase active center". Proc Natl Acad Sci USA. 105 (39): 14820–5. doi:10.1073/pnas.0802822105. PMID 18787125.