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Rifapentine


ACCESSION NB: DB01201 (APRD01217)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
Rifapentine is an antibiotic drug used in the treatment of tuberculosis. It inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme.

VOLUME OF DISTRIBUTION: 70.2 ± 9.1 L

CATEGORIES:
Leprostatic Agents Antimycobacterials Antibiotics, Antitubercular

ABSORPTION: Rapidly and well absorbed from the gastrointestinal tract.

INDICATION:
For the treatment of pulmonary tuberculosis.

PHARMACODYNAMICS:
Rifapentine is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifampin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency.

MECHANISM OF ACTION:
Rifapentine has shown higher bacteriostatic and bactericidal activities especially against intracellular bacteria growing in human monocyte-derived macrophages. Rifapentine inhibits DNA-dependent RNA polymerase in susceptible strains of M. tuberculosis. Rifapentine acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.

PROTEIN BINDING:
97.7% (bound to plasma proteins)

METABOLISM:
Hepatic

AFECTED ORGANISMS:
Mycobacterium