Antibiotics (Properties, Application, Interaction) - Posokhova K.A., Viktorov O.P. 2005

Other Antibiotics
Rifamycins

The rifamycin group of Antibiotics includes rifamycin and its semisynthetic derivatives, such as rifampicin, rifabutin, and rifaximin.

The antibacterial mechanism of rifamycins is based on their ability to bind to the DNA helix, leading to the inhibition of Replication and METABOLISM/31.html">Transcription processes. They are toxic not only to bacterial Cells but also to Eukaryotic cells.

They exhibit a broad spectrum of antibacterial activity.

Rifampicin has a bactericidal effect on Mycobacterium tuberculosis and Mycobacterium leprae. It is active against most cocci (except enterococci). Its activity against staphylococci surpasses that of Tetracyclines, Cephalosporins, and Aminoglycosides. It affects Legionella spp., Brucella spp., Chlamydia spp. (the causative agents of trachoma, psittacosis, and lymphogranuloma venereum), Rickettsia spp., and certain spore-forming bacilli (B. anthracis, C. perfringens). It is also active against some Gram-negative Bacteria, including E. coli, Proteus strains, Klebsiella, and Pseudomonas. Microorganisms develop resistance to rifampicin rapidly; therefore, its use in non-tuberculosis infections is prescribed only when Other Antibiotics prove ineffective.

It is well absorbed when administered orally and penetrates all Organs and Tissues of the body, including across the Blood-Brain barrier. The maximum blood concentration is reached within 2 hours. The average therapeutic concentration is maintained for 12–24 hours. It is excreted from the body via Bile (up to 60%) and urine (up to 15% unchanged and 15% as metabolites).

Rifampicin is primarily used for the Treatment of tuberculosis, leprosy, and Infections caused by multi-resistant pathogens susceptible to rifampicin.

Treatment with rifampicin may cause severe side effects associated with The formation of specific anti-rifampicin Antibodies, including Liver damage, flu-like syndrome (fever, arthralgia, myalgia), thrombocytopenia, and hemolytic anemia. During therapy, the patient's secretions (saliva, sputum, tears, urine) are stained orange-red.

Rifampicin induces the microsomal enzyme system, which can accelerate both its own metabolism and that of other drugs biotransformed in the liver (such as indirect anticoagulants and hormonal contraceptives).