Rifabutin: Difference between revisions

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{{Short description|Antibiotic used to treat tuberculosis and Mycobacterium avium complex}}
Rifabutin is a rifamycin [[antibiotic]] that is similar in structure and activity to rifampin and rifapentine and which is used largely in the prevention of Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection. Rifabutin is associated with transient and asymptomatic elevations in serum [[aminotransferase]] and is a likely cause of clinically apparent, acute liver disease.
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'''Rifabutin''' is an [[antibiotic]] that is primarily used to treat [[tuberculosis]] and infections caused by the [[Mycobacterium avium complex]] (MAC). It is a member of the [[rifamycin]] class of antibiotics, which are known for their ability to inhibit bacterial [[RNA polymerase]].
Rifabutin (rif" a bue' tin) is a rifamycin [[antibiotic]] and a synthetic derivative of natural products of the bacterium, Amycolatopsis mediterranei. The rifamycins are complex macrocyclic [[antibiotics]] that have activity against several bacteria, but most prominently M. [[tuberculosis]] and several [[atypical mycobacteria]]l species, probably as a result of inhibition of the DNA-dependent RNA polymerase of mycobacteria. These agents are considered [[bactericidal]] and are active against both intracellular and extracellular organisms. Rifabutin has similar activity and pharmacokinetics as rifampin, but it is less likely to induce hepatic microsomal, drug metabolizing enzymes and, thus, is an appropriate substitute for rifampin in patients on other medications that would be affected by alteration in the P450 system, such as some antiretroviral agents, benzodiazepines, cyclosporine, [[macrolide antibiotics]], oral contraceptives, and warfarin. Rifabutin is available as 150 mg capsules under the trade name of Mycobutin. The current major indication is for prevention of mycobacterium avium complex (MAC) disease in patients with HIV infection, and treatment of [[tuberculosis]] is considered an off-label use. The recommended dose in adults is 300 mg daily in one or two divided doses. Pyridoxine (vitamin B6) is commonly given with rifabutin to prevent [[neuropathy]]. Side effects of rifabutin are uncommon, but include [[rash]], [[fever]], flu-like symptoms, [[gastrointestinal upset]] and orange discoloration of urine and sweat. Rifabutin has some, but far less activity than rifampin as an inducer of the hepatic microsomal drug metabolizing P450 enzymes (CYP 1A2, 2C9, 2C19 and 3A4), the relative potencies being: rifampin (1.0), rifapentine (0.85), and rifabutin (0.4). Nevertheless, use of other medications (such as birth control pills, beta-blockers, benzodiazepines, cyclosporine and oral anticoagulants) with rifabutin should be carefully considered and monitored. Rare but potentially severe adverse events include uveitis, [[hypersensitivity reactions]] and [[C. difficile]] [[diarrhea]].


==Medical uses==
Rifabutin is used in the treatment and prevention of [[Mycobacterium avium complex]] infections, particularly in patients with [[HIV/AIDS]]. It is also used as part of combination therapy for [[tuberculosis]], especially in cases where [[rifampicin]] cannot be used due to drug interactions or resistance.


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===Mycobacterium avium complex===
[[File:Rifabutin_structure.svg|Chemical structure of Rifabutin|thumb|right]]
Rifabutin is effective against the Mycobacterium avium complex, which includes several species of mycobacteria that can cause serious infections in immunocompromised individuals. It is often used in combination with other antibiotics such as [[clarithromycin]] or [[azithromycin]] to prevent or treat these infections.


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===Tuberculosis===
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Rifabutin is used as an alternative to [[rifampicin]] in the treatment of [[tuberculosis]], particularly in patients who are receiving [[antiretroviral therapy]] for [[HIV/AIDS]]. This is because rifabutin has fewer drug interactions compared to rifampicin, making it a preferred choice in these cases.
File:Rifabutin structure.svg|Rifabutin
 
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==Mechanism of action==
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Rifabutin works by inhibiting the bacterial [[DNA-dependent RNA polymerase]], an enzyme that is crucial for the transcription of DNA into RNA. By blocking this enzyme, rifabutin effectively halts the synthesis of bacterial RNA, leading to the death of the bacteria.
File:Rifabutin structure.svg|Rifabutin
 
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==Side effects==
Common side effects of rifabutin include gastrointestinal disturbances such as nausea and vomiting, as well as skin rashes. More serious side effects can include [[neutropenia]], [[uveitis]], and [[hepatitis]]. Patients taking rifabutin may also experience a reddish-orange discoloration of bodily fluids, which is harmless but can be alarming.
 
==Drug interactions==
Rifabutin is known to interact with several other medications, particularly those that are metabolized by the [[cytochrome P450]] enzyme system. It can induce the metabolism of drugs such as [[protease inhibitors]] and [[non-nucleoside reverse transcriptase inhibitors]], which are used in the treatment of [[HIV/AIDS]].
 
==Related pages==
* [[Rifampicin]]
* [[Antibiotic]]
* [[Tuberculosis]]
* [[Mycobacterium avium complex]]
 
[[Category:Antibiotics]]
[[Category:Rifamycins]]
[[Category:World Health Organization essential medicines]]

Latest revision as of 10:54, 23 March 2025

Antibiotic used to treat tuberculosis and Mycobacterium avium complex


Rifabutin
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Rifabutin is an antibiotic that is primarily used to treat tuberculosis and infections caused by the Mycobacterium avium complex (MAC). It is a member of the rifamycin class of antibiotics, which are known for their ability to inhibit bacterial RNA polymerase.

Medical uses[edit]

Rifabutin is used in the treatment and prevention of Mycobacterium avium complex infections, particularly in patients with HIV/AIDS. It is also used as part of combination therapy for tuberculosis, especially in cases where rifampicin cannot be used due to drug interactions or resistance.

Mycobacterium avium complex[edit]

Chemical structure of Rifabutin

Rifabutin is effective against the Mycobacterium avium complex, which includes several species of mycobacteria that can cause serious infections in immunocompromised individuals. It is often used in combination with other antibiotics such as clarithromycin or azithromycin to prevent or treat these infections.

Tuberculosis[edit]

Rifabutin is used as an alternative to rifampicin in the treatment of tuberculosis, particularly in patients who are receiving antiretroviral therapy for HIV/AIDS. This is because rifabutin has fewer drug interactions compared to rifampicin, making it a preferred choice in these cases.

Mechanism of action[edit]

Rifabutin works by inhibiting the bacterial DNA-dependent RNA polymerase, an enzyme that is crucial for the transcription of DNA into RNA. By blocking this enzyme, rifabutin effectively halts the synthesis of bacterial RNA, leading to the death of the bacteria.

Side effects[edit]

Common side effects of rifabutin include gastrointestinal disturbances such as nausea and vomiting, as well as skin rashes. More serious side effects can include neutropenia, uveitis, and hepatitis. Patients taking rifabutin may also experience a reddish-orange discoloration of bodily fluids, which is harmless but can be alarming.

Drug interactions[edit]

Rifabutin is known to interact with several other medications, particularly those that are metabolized by the cytochrome P450 enzyme system. It can induce the metabolism of drugs such as protease inhibitors and non-nucleoside reverse transcriptase inhibitors, which are used in the treatment of HIV/AIDS.

Related pages[edit]