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| Clinical data | |
|---|---|
| Trade names | Mycobutin[1] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a693009 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | 85% |
| Protein binding | 85% |
| Metabolism | Liver |
| Eliminationhalf-life | 28 to 62 hours (mean) |
| Excretion | Kidney and fecal |
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| UNII | |
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| ChEBI | |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.133.627 |
| Chemical and physical data | |
| Formula | C46H62N4O11 |
| Molar mass | 847.019 g·mol−1 |
| 3D model (JSmol) | |
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Rifabutin (Rfb) is anantibiotic used to treattuberculosis and prevent and treatMycobacterium avium complex.[1] It is typically only used in those who cannot toleraterifampin such as people withHIV/AIDS onantiretrovirals.[1] For active tuberculosis it is used with otherantimycobacterial medications.[1] For latent tuberculosis it may be used by itself when the exposure was withdrug-resistant TB.[1]
Rifabutin was approved for medical use in the United States in 1992.[1] It is on theWorld Health Organization's List of Essential Medicines.[3]
Rifabutin is now recommended as first-line treatment fortuberculosis (TB),[4] butrifampicin was used more widely because of its cheaper cost. However, due to the expiration of patents, prices are now similar.
Common side effects includeabdominal pain,nausea, rash,headache, andlow blood neutrophil levels.[1] Other side effects include muscles pains anduveitis.,[1] especially when hitting Bartonella and Babesia colonies in the capillaries of the ciliary body in the eye anterior chamber. While no harms have been found duringpregnancy it has not been well studied in this population.[1] Rifabutin is in therifamycin family of medications.[1] It works by blockingRNA production in bacteria.[5]
Scientists at the Italian drug company Achifar discovered rifabutin in 1975. (Eventually Archifar became part ofFarmitalia Carlo Erba, a unit of the conglomerate Montedison which was subsequently bought byPharmacia) This company's Adria Laboratories subsidiary filed forFood and Drug Administration (FDA) approval of rifabutin under the brand name Mycobutin in the early 1990s and the drug gained FDA approval in December 1992.[citation needed]
Rifabutin is primarily bactericidal antibiotic drug used to treat tuberculosis. Its effect on bacteria is based on the DNA-dependent RNA polymerase blocking drug rifamycin S, a semi-synthetic derivative. It is effective, for example, in highly resistant mycobacteria, Gram-positive bacteria (and some are effective against Gram-negative bacteria), but also againstMycobacterium tuberculosis,M. leprae, andM. avium intracellulare.[citation needed]
Rifabutin is a rifamycin, which like rifampicin, works via inhibition of DNA‐dependent RNA synthesis in prokaryotes.
