Overview
| Generic Names: | Ansatipin; Ansatipine; Antibiotic LM 427; RBT; Rifabutina [Spanish]; Rifabutine [French]; Rifabutinum [Latin] |
|---|---|
| Trade Names: | Alfacid; Ansamycin; Mycobutin |
| PharmGKB Accession Id: | PA451249 |
Description
A broad-spectrum antibiotic that is being used as prophylaxis against disseminated Mycobacterium avium complex infection in HIV-positive patients. PubChem (source: Drug Bank)
Indication
For the prevention of disseminated <i>Mycobacterium avium</i> complex (MAC) disease in patients with advanced HIV infection. (source: Drug Bank)
ATC Therapeutic Category
- J04AB:Antibiotics
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Rifabutin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death. (source: Drug Bank)
Pharmacology
Rifabutin is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including <i>Pseudomonas aeruginosa</i>) and specifically <i>Mycobacterium tuberculosis</i>. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifabutin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency. (source: Drug Bank)
Food Interactions
High-fat meals slow the rate of absorption.
Take with food to reduce irritation.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
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. (source: Drug Bank)
Protein Binding
85% (source: Drug Bank)
Absorption
Rifabutin is readily absorbed from the gastrointestinal tract, with an absolute bioavailability averaging 20%. (source: Drug Bank)
Toxicity
LD<sub>50</sub> = 4.8 g/kg (mouse, male) (source: Drug Bank)
Isomeric SMILES Code:
C[C@H]\1[C@H]([C@@H]([C@@H]([C@@H]([C@@H]([C@@H]([C@@H](/C=C\O[C@]2(OC3=C(C2=O)C4=C(C(=O)C(=C5C4=N[C@]6(N5)CCN(CC6)CC(C)C)NC(=O)/C(=C\C=C1)/C)C(=C3C)O)C)OC)C)OC(=O)C)C)O)C)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
NR1I2 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| HSP90AA1 |
|
(source: Drug Bank) |
| HSP90B1 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
The rifamycin decreases the anticoagulant effect (source: Drug Bank) |
| amitriptyline |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| amoxapine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| amprenavir |
|
Amprenavir increases the effect and toxicity of rifabutin (source: Drug Bank) |
| atazanavir |
|
Atazanavir increases levels/toxicity of rifabutin (source: Drug Bank) |
| atorvastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| atovaquone |
|
Rifabutin decreases the effect of atovaquone (source: Drug Bank) |
| bupropion |
|
Rifampin reduces bupropion levels (source: Drug Bank) |
| buspirone |
|
Rifabutin decreases the effect of buspirone (source: Drug Bank) |
| cerivastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| clarithromycin |
|
The rifamycin decreases the effect of the macrolide (source: Drug Bank) |
| clomipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| clozapine |
|
Rifabutin decreases the effect of clozapine (source: Drug Bank) |
| cyclosporine |
|
The rifamycin decreases the effect of cyclosporine (source: Drug Bank) |
| dapsone |
|
Decreased levels of dapsone (source: Drug Bank) |
| delavirdine |
|
Rifabutin decreases the effect of delavirdine (source: Drug Bank) |
| desipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| dicumarol |
|
The rifamycin decreases the anticoagulant effect (source: Drug Bank) |
| doxepin |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| doxycycline |
|
The rifamycin decreases the effect of doxycycline (source: Drug Bank) |
| erlotinib |
|
Decreased levels/effect of erlotinib (source: Drug Bank) |
| erythromycin |
|
The rifamycin decreases the effect of the macrolide (source: Drug Bank) |
| ethinyl estradiol |
|
This product may cause a slight decrease of the contraceptive effect (source: Drug Bank) |
| fluconazole |
|
Fluconazole increases levels/toxicity of rifabutin (source: Drug Bank) |
| fluvastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| fosamprenavir |
|
Amprenavir increases the effect and toxicity of rifabutin (source: Drug Bank) |
| haloperidol |
|
The rifamycin decreases the effect of haloperidol (source: Drug Bank) |
| imipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| indinavir |
|
Rifabutin decreases the effect of indinavir (source: Drug Bank) |
| itraconazole |
|
Rifabutin decreases the effect of itraconazole (source: Drug Bank) |
| lovastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| mestranol |
|
This product may cause a slight decrease of the contraceptive effect (source: Drug Bank) |
| methadone |
|
The rifamycin decreases the effect of methadone (source: Drug Bank) |
| norethindrone |
|
This product may cause a slight decrease of the contraceptive effect (source: Drug Bank) |
| nortriptyline |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| posaconazole |
|
Modification of drug levels for both agents (source: Drug Bank) |
| propafenone |
|
Rifampin decreases the effect of propafenone (source: Drug Bank) |
| protriptyline |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| ritonavir |
|
Rifabutin decreases the effect of ritonavir (source: Drug Bank) |
| saquinavir |
|
Rifabutin decreases the effect of saquinavir (source: Drug Bank) |
| simvastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| sirolimus |
|
The rifamycin decreases the effect of sirolimus (source: Drug Bank) |
| sunitinib |
|
Possible decrease in sunitinib levels (source: Drug Bank) |
| tacrolimus |
|
The rifamycin decreases the effect of tacrolimus (source: Drug Bank) |
| tamoxifen |
|
The rifamycin decreases the effect of anti-estrogen (source: Drug Bank) |
| toremifene |
|
The rifamycin decreases the effect of anti-estrogen (source: Drug Bank) |
| trimipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| voriconazole |
|
Rifabutin decreases the effect of voriconazole (source: Drug Bank) |
| warfarin |
|
The rifamycin decreases the anticoagulant effect (source: Drug Bank) |
| zidovudine |
|
The rifamycin decreases levels of zidovudine (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.