Rifampin active

Inducers (barbiturates, carbamezepine, rifampin) activity ° Inhibitors (cimetidine, macrolides, azole antifungals) —>T activity Protein C deficiency ... 

Ansamacrolides. Antibiotics ia the ansamacroHde family ate also referred to as ansamycias. They are benzenoid or naphthalenoid aromatic compounds ia which nonadjacent positions are bridged by an aliphatic chain to form a cycHc stmcture. One of the aliphatic—aromatic junctions is always an amide bond. Rifampin is a semisyntheticaHy derived member of this family and has clinical importance. It has selective antibacterial activity and inhibits RNA polymerase. 

Most aiititubercular drag s are bacteriostatic (slow or retard the growth of bacteria) against the M. tuberculosis bacillus. These dm usually act to inhibit bacterial cell wall synthesis, which slows the multiplication rate of the bacteria. Only isoniazid is bactericidal, with rifampin and streptomycin having some bactericidal activity. 

Vitamin K is a fat-soluble vitamin cofactor for the activation of factors II, VII, IX, and X in the liver. Almost all neonates are vitamin K-deficient at as a result of (1) insignificant transplacental vitamin K crossover, (2) lack of colonization of the colon by vitamin K-producing bacteria, and (3) inadequate dietary vitamin K intake (especially in breast-fed infants because human milk contains less vitamin K than infant formula or cow s milk). Vitamin K-deficiency bleeding (VKDB) refers to bleeding attributable to vitamin K deficiency within first 6 months of life. It occurs in three general time frames early (0-24 hours), classic (1-7 days), and late (2-12 weeks). Early onset occurs rarely and usually is associated with maternal ingestion of anticonvulsants, rifampin, isoniazid, and warfarin. Classic vitamin K-dependent bleeding usually results from the lack of prophylactic vitamin K administration in... 

Isoniazid is used for treating LTBI.2,6,12,28 Typically, isoniazid 300 mg daily (5-10 mg/kg of body weight) is given alone for 9 months. Lower doses usually are less effective.2,31 The treatment of LTBI reduces a person s lifetime risk of active TB from about 10% to about 1%20 (Table 72-2). Rifampin 600 mg... 

The broad antibacterial activity of rifaximin as well as its topical action make this antibiotic suitable for intrapocket administration in periodontal disease. As a matter of fact, local application of rifaximin compares well with tetracyclines and metronidazole in other extra-GI diseases, i.e. skin infections and BY, respectively (see above). On the other hand, rifampicin (rifampin), another rifamy-cin derivative, has been successfully used in the treatment... 

Tetracycline 500 mg every six hours or doxycycline 100 mg every twelve hours for five to seven days will shorten the duration of illness, and fever usually disappears within one to two days after treatment is begun. Ciprofloxacin and other quinolones are active in vitro and should be considered for victims unable to take tetracycline or doxycycline. Successful treatment of Q fever endocarditis is much more difficult. Tetracycline or doxycycline given in combination with trimethoprim-sulfamethoxazole (TMP-SMX) or rifampin for twelve months or longer has been successful in some cases. However, valve replacement is often required to achieve a cure. 

Tirona, R. G., Leake, B. F., Wolkoff, A. W., and Kim, R. B. (2003) Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. J. Pharmacol. Exp. Ther. 304, 223-228. 

Rifampin. Source, antibacterial activity, and routes of administration are described on p. 274. Albeit mostly well tolerated, this drug may cause several adverse effects including hepatic damage, hypersensitivity with flu-like symptoms, disconcerting but harmless red/orange discoloration of body fluids, and enzyme induction (failure of oral Liillmann, Color Atlas of Pharmacology... 

Drugs that may affect APAP include barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone, ethyl alcohol, and activated charcoal. 

The 4-month regimen According to the MMWR, rifampin given daily for 3 months has resulted in better protection than placebo in treatment of LTBI in non-HIV patients with silicosis in a randomized prospective trial. However, because the patients receiving rifampin had a high rate of active tuberculosis (4%), experts have concluded that a 4-month regimen would be more prudent when using rifampin alone. This option may be useful for patients who cannot tolerate isoniazid or pyrazinamide. 

Pharmacology Rifampin inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase, but does not inhibit the mammalian enzyme. Cross-resistance has only been shown with other rifamycins. Rifampin at therapeutic levels has demonstrated bactericidal activity against intracellular and extracellular Mycobacterium tuberculosis organisms. Pharmacokinetics ... 

Metabolism Rifampin is metabolized in the liver by deacetylation the metabolite is still active against Mycobacterium tuberculosis. About 40% is excreted in bile and undergoes enterohepatic circulation however, the deacetylated metabolite is poorly absorbed. The half-life is approximately 3 hours after a 600 mg oral dose, up to 5.1 after a 900 mg oral dose. With repeated administration, the half-life decreases and averages approximately 2 to 3 hours. 

CYP450 Rifabutin has liver enzyme-inducing properties. The related drug, rifampin, is known to reduce the activity of a number of other drugs. Because of the structural... 

The current CDC recommendation for drug-susceptible initial treatment of active tuberculosis disease is a 6-month regimen consisting of isoniazid, rifampin, and pyrazinamide given for 2 months, followed by isoniazid and rifampin for 4 months. Treatment failure After treatment failure with other primary drugs in any form of active tuberculosis. 

Tuberculosis Treatment of tuberculosis in combination with other active agents. It is most commonly used in patients with multi-drug resistant tuberculosis (MDR-TB) or in situations when therapy with isoniazid and rifampin is not possible because of a combination of resistance and intolerance. 

Recommended for any form of active tuberculosis when treatment with first-line drugs (isoniazid, rifampin) has failed. Use only with other effective antituberculosis... 

Pharmacology Rifapentine is a rifamycin-derivative antibiotic and has a similar profile of microbiological activity to rifampin. 

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