Definition
A broad-spectrum antibiotic that is being used as prophylaxis against disseminated Mycobacterium avium complex infection in HIV-positive patients.
Description
Rifabutin is only found in individuals that have used or taken this drug. It is a broad-spectrum antibiotic that is being used as prophylaxis against disseminated Mycobacterium avium complex infection in HIV-positive patients. [PubChem]Rifabutin acts via the inhibition of DNA-dependent RNA polymerase in gram-positive and some gram-negative bacteria, leading to a suppression of RNA synthesis and cell death.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Of the five metabolites that have been identified, 25-O-desacetyl and 31-hydroxy are the most predominant. The former metabolite has an activity equal to the parent drug and contributes up to 10% to the total antimicrobial activity. Route of Elimination: A mass-balance study in three healthy adult volunteers with 14C-labeled rifabutin showed that 53% of the oral dose was excreted in the urine, primarily as metabolites. About 30% of the dose is excreted in the feces. Half Life: 45 (± 17) hours
- Uses/Sources: For the prevention of disseminated Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection. Used in the treatment of tuberculosis. It has also found to be useful in the treatment of (Chlamydia) Chlamydophila pneumoniae (Cpn) Infection.[Wikipedia]
- Symptoms: Symptoms include diarrhea, eructation, abdominal pain, vomitting, nausea, and insomnia.
- Treatment: Clinical experience with rifamycins suggests that gastric lavage to evacuate gastric contents (within a few hours of overdose), followed by instillation of an activated charcoal slurry into the stomach, may help absorb any remaining drug from the gastrointestinal tract. (L1712)
- Route of Exposure: Rifabutin is readily absorbed from the gastrointestinal tract, with an absolute bioavailability averaging 20%.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 4.8 g/kg (male mouse)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Heat shock protein HSP 90-alpha Endoplasmin |
Rifabutin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death. |
9428803 11358819 14660597 11306472 10919672 10759403 10701840 8617772 |
Rifabutin Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
CHOLESTASIS, BENIGN RECURRENT INTRAHEPATIC, 2 | 6.65 |
|
Cholestasis, progressive familial intrahepatic 1 | 5.96 |
|
Afibrinogenemia | 5.84 |
|
Cholestasis, Intrahepatic | 4.28 |
|
Hepatitis C | 4.22 |
|
Osteosarcoma | 4.05 |
|
Liver Cirrhosis, Experimental | 4.0 |
|
Pruritus | 4.0 |
|
Colorectal cancer | 3.76 |
|
Cholestasis | 3.74 |
|
Torsades de pointes | 3.66 |
|
Prostatic Neoplasms | 2.96 |
|
Breast carcinoma | 2.89 |
|