Indication: Used to prevent mycobacterial infection in immunocompromised patients, as a therapy in non-tuberculous mycobacterial infection, and as a treatment in pulmonary tuberculous.
Pharmacology: Rifabutin 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. Rifabutin 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: Rifabutin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
Drug Category: Antibiotics; Anti-bacterial Agents; Antituberculosis Agents; ATC:J04AB04
Absorption: Following a single oral dose of 300 mg to nine healthy adult volunteers, rifabutin was readily absorbed from the gastrointestinal tract. Absolute bioavailability averaged 20%.
Interactions:
DrugBank: Interactions for Rifabutin
Interactions for Rifabutin:
Effects on Other Drugs: Rifabutin induces CYP3A enzymes and therefore may reduce the plasma
concentrations of drugs metabolized by those enzymes. This effect may reduce the efficacy of standard doses of such
drugs, which include itraconazole, clarithromycin, and saquinavir.
Effects on Rifabutin: Some drugs that inhibit CYP3A may significantly increase the plasma
concentration of rifabutin. Because high plasma levels of rifabutin may increase the risk of adverse reactions,
carefully monitor patients receiving coadministration of such drugs, which include fluconazole and clarithromycin. In
some cases, the dosage of MYCOBUTIN may need to be reduced when it is coadministered with such a drug.
Antiretrovirals:
Delavirdine: Coadministration of rifabutin and delavirdine is not recommended because rifabutin
substantially decreases the plasma concentrations of delavirdine, and delavirdine increases the plasma concentrations
of rifabutin.
Indinavir: Coadministration of indinavir and rifabutin increases the plasma concentration of
rifabutin. In patients receiving coadministration of indinavir, reduce the dosage of MYCOBUTIN by half.
Nelfinavir: Coadministration of nelfinavir increases the plasma concentration of rifabutin. In
patients receiving nelfinavir, reduce the dosage of MYCOBUTIN by half.
Ritonavir: Coadministration of ritonavir is not recommended because it substantially increases
the plasma concentration of rifabutin. High plasma concentrations of rifabutin may increase the risk of adverse
reactions, including uveitis.
Other Drugs:
Oral contraceptives: Rifabutin may decrease the efficacy of oral contraceptives by inducing drug
metabolism of ethinylestradiol and norethindrone. Women using oral contraceptives should be advised to change to or
supplement with nonhormonal methods of birth control during treatment with MYCOBUTIN.
Other drugs: The structurally similar drug, rifampin, is known to reduce the plasma
concentrations of a number of other drugs. Although rifabutin is a weaker enzyme inducer than rifampin, it may be
expected to have some effect on those drugs as well.
Chemical IUPAC Name: (9S,12E,14S,15R,16S,17R,18R,19R,20S,21S,22E,24Z)-6,16,18,20-Tetrahydroxy-1'-isobutyl-14-methoxy-7,9,15,17,19,21,25-hepta-methyl-spiro[9,4-(epoxypentadeca[1,11,13]trienimino)-2H-furo-[2',3':7,8]-naphth[1,2-d]imidazol-2,4'-piperidin]-5,10,26-(3H,9H)-trione 16-acetate
A Saudi's Hit ListJan 13, 2006 FrontPage magazine.com, ...poet Tawfiq Ziad, Egyptian intellectual Nasr Abu Zayd, Palestinian author Ghassan Kanafani, Palestinian author Emil Habibi, Egyptian intellectual Rifa'a Al ...
‘Doctors’ or palmists?Jan 12, 2006 Lucknow Newsline, One such ‘‘healer’’, Joginder Singh operates his ‘‘Surya Uday Ayurvedic Dawakhana’’ opposite the Rifa-e-Aam club in Golaganj. ...
RIFFA OFF TO A FINE STARTJan 5, 2006 Gulf Daily News, Al Malkiya, under former coach of Egyptian champions Zamalek Ahmed Rifa'at, defended well with their ace Abbas Nesaif proving strong on the backline while ...
The Arab World's Travails: History's BurdenDec 24, 2005 Middle East Forum, One author a Syrian historian, Anwar ar-Rifa‘i, locates an Arab origins for just about all the ancient peoples of the Middle East (Egyptians, Sumerians ...
Once again, region proves its generosityDec 30, 2005 Jackson Sun, ...money. An equally valuable gift is the gift of themselves and their time. Help agencies like ARM and RIFA depend on volunteers. And ...
the Jordanian Muslim Brotherhood Part TwoDec 30, 2005 Asharq Alawsat, 1971 and 1972. In 1973, he was appointed minister of endowments and Islamic affairs in Zaid al-Rifa'i's government. Al-Farhan had ...
Home
Copyright phasechange.org 2006.
All Rights Reserved.
