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Rifapentine

Catalog No. DB01201 Name DrugBank
CAS Number 61379-65-5 Website http://www.ualberta.ca/
M. F. C47H64N4O12 Telephone (780) 492-3111
M. W. 877.03066 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 1071

SYNONYMS

IUPAC name
(7S,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-26-[(E)-N-(4-cyclopentylpiperazin-1-yl)carboximidoyl]-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1^{4,7}.0^{5,28}]triaconta-1,3,5(28),9,19,21,25(29),26-octaen-13-yl acetate
IUPAC Traditional name
@rifapentine
Brand Name
Priftin
Synonyms
Cyclopentyl rifampin

DATABASE IDS

PubChem SID 46507322
PubChem CID 6323497
CAS Number 61379-65-5

PROPERTIES

Hydrophobicity(logP) 4

DETAILS

Description (English)
Item Information
Drug Groups 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.
Indication For the treatment of pulmonary tuberculosis.
Pharmacology 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.
Affected Organisms
Mycobacterium
Biotransformation Hepatic
Absorption Rapidly and well absorbed from the gastrointestinal tract.
Protein Binding 97.7% (bound to plasma proteins)
Elimination Following a single 600 mg oral dose of radiolabeled rifapentine to healthy volunteers (n=4), 87% of the total 14C rifapentine was recovered in the urine (17%) and feces (70%).
Distribution * 70.2 ± 9.1 L
Clearance * Apparent Oral cl=2.51 +/- 0.14 L/h [Male tuberculosis patients who received 600 mg rifapentine in combination with isoniazid, pyrazinamide and ethambutol]
* Apparent Oral cl=1.69 +/- 0.41 L/h [Female tuberculosis patients who received 600 mg rifapentine in combination with isoniazid, pyrazinamide and ethambutol]
External Links
Wikipedia
RxList
Drugs.com

REFERENCES