Rifapentine: Difference between revisions

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{{intro}}
{{Short description|Antibiotic used to treat tuberculosis}}
Rifampin (also referred to as rifampicin) is a macrocyclic [[antibiotic]] with major activity against mycobacteria, commonly used in combination with other agents as therapy of [[tuberculosis]]. Rifampin is associated with transient and asymptomatic elevations in serum [[aminotransferase]] and bilirubin levels and is a well known cause of clinically apparent, acute liver disease that can be severe and even fatal.
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{{moa}}
'''Rifapentine''' is an [[antibiotic]] used in the treatment of [[tuberculosis]] (TB). It is a member of the [[rifamycin]] class of antibiotics, which are known for their ability to inhibit bacterial [[RNA polymerase]], thereby preventing the synthesis of bacterial [[RNA]] and [[protein]].
Rifampin (rif am' pin) belongs to a class of medications know as rifamycins and is a synthetic derivative of natural products of the bacterium, S. mediterranei. Rifampin is a complex macrocyclic [[antibiotic]] that has activity against several bacteria, but most prominently inhibits growth of M. [[tuberculosis]] and several [[atypical mycobacteria]]l species, probably as a result of inhibition of the DNA-dependent RNA polymerase of mycobacteria. Rifampin was approved for use in therapy of [[tuberculosis]] in the United States in 1971. Rifampin remains a mainstay of therapy of [[tuberculosis]] and [[atypical mycobacteria]] [[infections]] and is usually used in conjunction with isoniazid and/or pyrazinamide. Other approved uses of rifampin include chemoprophylaxis of meningococcal disease and meningitis due to H. influenza. Rifampin is used off-label as therapy of [[itching]] due to liver disease. Rifampin is available in multiple generic forms and under the trade names of Rimactane and Rifadin in capsules of 150 and 300 mg. Pediatric formulations are available as well, as are powdered preparations for parenteral administration. The recommended dose for therapy of [[tuberculosis]] in adults is 600 mg (~10 mg/kg) daily and in children 10-20 mg/kg, but no more than 600 mg daily. Fixed combinations of rifampin (300 mg) with isoniazid (150 mg) are available under the brand name Rifamate, and combinations of rifampin (120 mg) with both isoniazid (50 mg) and pyrazinamide (300 mg) under the brand name Rifater. Side effects of rifampin are uncommon, but include [[rash]], [[fever]], flu-like symptoms, [[gastrointestinal upset]] and orange discoloration of urine and sweat. Rifampin is a potent inducer of many hepatic enzymes including the drug metabolizing enzymes, CYP 1A2, 2C9, 2C19 and 3A4 for which reason use of concurrent medications (such as oral contraceptives, anticoagulants, some antiretroviral agents, cyclosporine, benzodiazepines, and [[macrolide antibiotics]]) should be carefully chosen and monitored. Rifabutin and rifapentine are two other rifamycins that can be used in place of rifampin, rifabutin being useful if drug-interactions are an issue and rifapentine if once weekly dosing is preferred.


==Medical uses==
Rifapentine is primarily used in the treatment of [[active tuberculosis]] and [[latent tuberculosis infection]]. It is often used in combination with other antitubercular drugs such as [[isoniazid]] and [[pyrazinamide]] to enhance efficacy and prevent the development of drug resistance.


{{tb drugs}}
===Active tuberculosis===
In the treatment of active tuberculosis, rifapentine is used as part of a combination therapy. It is typically administered once or twice weekly, depending on the phase of treatment. The use of rifapentine in combination with other drugs helps to shorten the duration of therapy and improve patient adherence.


{{coststubd}}
===Latent tuberculosis infection===
For latent tuberculosis infection, rifapentine is used in combination with isoniazid in a regimen known as the "3HP" regimen, which involves once-weekly dosing for 12 weeks. This regimen has been shown to be as effective as longer regimens and is associated with better patient compliance.


{{intro}}
==Mechanism of action==
Rifapentine is a rifamycin [[antibiotic]] that is similar in structure and activity to rifampin and rifabutin and that is used in combination with other agents as therapy of [[tuberculosis]], particularly in once or twice weekly regimens. Rifapentine is associated with transient and asymptomatic elevations in serum [[aminotransferase]] and is a likely cause of clinically apparent acute [[liver injury]].
Rifapentine works by inhibiting the bacterial [[DNA-dependent RNA polymerase]], an enzyme essential for the transcription of DNA into RNA. By blocking this enzyme, rifapentine effectively halts the production of bacterial proteins, leading to the death of the bacteria.


{{moa}}
==Side effects==
Rifapentine (rif" a pen' teen) 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. Rifapentine has a longer half-life than rifampin and rifabutin, which allows for once or twice weekly dosing, which is its major advantage. Rifapentine was approved for use in treating active as well as latent [[tuberculosis]] in 1998. It is available as 150 mg film coated tablets under the trade names of Priftin. The recommended dose for active [[tuberculosis]] in adults is 600 mg twice weekly for 2 months, followed by 600 mg (~10 mg/kg) once weekly for 4 months as a part of directly observed therapy and in combination with isoniazid or other [[antituberculosis]] agents. The recommended regimen for latent tuberculsosis is a 12 week regimen of 600 mg once weekly in combination with isoniazid as directly observed therapy. Pyridoxine (vitamin B6) is commonly given with rifapentine and isoniazid to prevent [[neuropathy]]. Side effects of rifapentine are uncommon, but include [[rash]], [[fever]], flu-like symptoms, [[gastrointestinal upset]] and orange discoloration of urine and sweat. Rifapentine is intermediate between rifabutin and rifampin in activity 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). For this reason, use of other medications (such as many antiretroviral agents, oral contraceptives, beta-blockers, benzodiazepines, cyclosporine, [[macrolide antibiotics]] and oral anticoagulants) with rifapentine should be carefully considered and monitored.
Common side effects of rifapentine include [[nausea]], [[vomiting]], and [[diarrhea]]. It can also cause [[hepatotoxicity]], which is a concern with all rifamycin antibiotics. Patients taking rifapentine may experience [[orange discoloration]] of bodily fluids, such as urine and tears, which is a harmless but notable side effect.


==Drug interactions==
Rifapentine is a potent inducer of [[cytochrome P450]] enzymes, which can lead to significant drug interactions. It can decrease the effectiveness of other medications metabolized by these enzymes, such as [[oral contraceptives]], [[anticoagulants]], and certain [[antiretroviral drugs]].


{{tb drugs}}
==Pharmacokinetics==
Rifapentine is well absorbed from the gastrointestinal tract and has a long half-life, which allows for less frequent dosing compared to other rifamycins. It is metabolized in the liver and excreted primarily in the bile.


{{coststubd}}
==History==
<gallery>
Rifapentine was developed as a derivative of [[rifampicin]] with a longer half-life, allowing for less frequent dosing. It was approved for medical use in the United States in 1998.
File:Rifapentine.svg|Rifapentine
 
</gallery>
==Related pages==
<gallery>
* [[Tuberculosis]]
File:Rifapentine.svg|Rifapentine
* [[Antibiotic]]
</gallery>
* [[Rifampicin]]
* [[Isoniazid]]
 
[[Category:Antibiotics]]
[[Category:Tuberculosis]]
[[Category:Rifamycins]]

Latest revision as of 11:08, 23 March 2025

Antibiotic used to treat tuberculosis


Rifapentine
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Rifapentine is an antibiotic used in the treatment of tuberculosis (TB). It is a member of the rifamycin class of antibiotics, which are known for their ability to inhibit bacterial RNA polymerase, thereby preventing the synthesis of bacterial RNA and protein.

Medical uses[edit]

Rifapentine is primarily used in the treatment of active tuberculosis and latent tuberculosis infection. It is often used in combination with other antitubercular drugs such as isoniazid and pyrazinamide to enhance efficacy and prevent the development of drug resistance.

Active tuberculosis[edit]

In the treatment of active tuberculosis, rifapentine is used as part of a combination therapy. It is typically administered once or twice weekly, depending on the phase of treatment. The use of rifapentine in combination with other drugs helps to shorten the duration of therapy and improve patient adherence.

Latent tuberculosis infection[edit]

For latent tuberculosis infection, rifapentine is used in combination with isoniazid in a regimen known as the "3HP" regimen, which involves once-weekly dosing for 12 weeks. This regimen has been shown to be as effective as longer regimens and is associated with better patient compliance.

Mechanism of action[edit]

Rifapentine works by inhibiting the bacterial DNA-dependent RNA polymerase, an enzyme essential for the transcription of DNA into RNA. By blocking this enzyme, rifapentine effectively halts the production of bacterial proteins, leading to the death of the bacteria.

Side effects[edit]

Common side effects of rifapentine include nausea, vomiting, and diarrhea. It can also cause hepatotoxicity, which is a concern with all rifamycin antibiotics. Patients taking rifapentine may experience orange discoloration of bodily fluids, such as urine and tears, which is a harmless but notable side effect.

Drug interactions[edit]

Rifapentine is a potent inducer of cytochrome P450 enzymes, which can lead to significant drug interactions. It can decrease the effectiveness of other medications metabolized by these enzymes, such as oral contraceptives, anticoagulants, and certain antiretroviral drugs.

Pharmacokinetics[edit]

Rifapentine is well absorbed from the gastrointestinal tract and has a long half-life, which allows for less frequent dosing compared to other rifamycins. It is metabolized in the liver and excreted primarily in the bile.

History[edit]

Rifapentine was developed as a derivative of rifampicin with a longer half-life, allowing for less frequent dosing. It was approved for medical use in the United States in 1998.

Related pages[edit]

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