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- Related Diseases
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Overview
| Generic Names: | RFP |
|---|---|
| Trade Names: | Archidyn; L-5103 Lepetit; R/AMP; RAMP; Rfamipicin; Rifa; Rifadin; Rifadin IV; Rifadine; Rifagen; Rifaldazin; Rifaldazine; Rifaldin; Rifampicin; Rifampicin SV; Rifamycin; Rifamycin Amp; Rifaprodin; Rifoldin; Rifoldine; Riforal; Rimactan; Rimactane; Rimactin; Rimazid; Rofact; Tubocin |
| Brand Mixtures: | Rifamate (Rifampin + Isoniazid); Rifater (Isoniazid + Pyrazinaamide + Rifampin) |
| PharmGKB Accession Id: | PA451250 |
Description
A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) (source: Drug Bank)
Indication
For the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections. (source: Drug Bank)
ATC Therapeutic Category
- J04AB:Antibiotics
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Rifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death. (source: Drug Bank)
Pharmacology
Rifampin 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. Rifampin 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
Avoid alcohol.
Take on empty stomach: 1 hour before or 2 hours after meals.
Take with a full glass of water.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Primarily hepatic, rapidly deacetylated. (source: Drug Bank)
Protein Binding
89% (source: Drug Bank)
Absorption
Well absorbed from gastrointestinal tract. (source: Drug Bank)
Toxicity
LD<sub>50</sub>=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness (source: Drug Bank)
Isomeric SMILES Code:
Cc1c(c2c3c4c1O[C@@](C4=O)(OC=C[C@@H]([C@H]([C@H]([C@@H]([C@@H]([C@@H]([C@H]([C@H](C=CC=C(C(=O)Nc(c2O)c(c3O)C=NN5CCN(CC5)C)C)C)O)C)O)C)OC(=O)C)C)OC)C)O (source: Drug Bank)
Curated Annotations (
)
-
rs2472677
at chr3:121001107
in
NR1I2
The CC homozygote of the NR1I2:63396C>T variant is associated with a high level of NR1I2 (PXR) gene induction by rifampicin as measured by increased activity of CYP3A4. This observation was particularly pronounced in livers from male subjects. Samples with the T allele had higher basal levels of NR1I2 mRNA and higher basal activity of CYP3A4. This SNP is predicted to be within a FOXA2 (HNF3beta) transcription factor binding site. This SNP is in LD with 63704G>A (rs12492296), 63813(CAAA)n/(CA)n, and 65104T>C.- Variant Name:
- NR1I2:63396C>T, PXR 63396C>T
- Related Drugs:
- rifampin
- Evidence:
-
PMID:17925385
-
rs72551372
at chr3:121013162
in
NR1I2
cell based studies; enhanced basal activity of cyp3a4 transcription wrt WT- Variant Name:
- V140M
- Related Drugs:
- rifampin
- Evidence:
-
PMID:11602521
-
rs72551374
at chr3:121013232
in
NR1I2
cell based studies; decreased basal activity on cyp3a4 transcription wrt WT; increased fold induction w/ rifampicin- Variant Name:
- D163G
- Related Drugs:
- rifampin
- Evidence:
-
PMID:11602521
-
rs1045642
at chr7:86976581
in
ABCB1
ABCB1 rs2032582 and rs1045642 genotype and peripheral blood lymphocyte efflux of P-gp substrate, rhodamine 123 (Rh123), in vitro, in healthy males: there was no significant difference in Rh123 efflux in CD56+ NK cells after 5, 10, 15, and 30 min efflux, or in CD4+ T-helper cells after 15, 30, 60, and 90 min between individuals with different genotypes. Rh123 efflux was not enhanced by a 10-day administration of P-gp inducer, rifampin, in vivo in 15 individuals before and after rifampin treatment. No genotypic effect was observed for inhibition of Rh123 efflux by P-pg inhibitor, verapamil, in vitro with CD56+ and CD4+.- Variant Name:
- ABCB1:3435C>T, mRNA 3853C>T, Ile1145Ile
- Related Drugs:
- rifampin, verapamil
- Evidence:
-
PMID:12914549
-
rs1045642
at chr7:86976581
in
ABCB1
Risk or phenotype-associated allele: none. Phenotype: No genetic association with dicloxacillin pharmacokinetics given 1g dicloxacillin prior to or after 600 mg rifampin (ABCB1 (P-gp) inducer). Study size: 18 (13 male). Study population/ethnicity: Healthy volunteers (12 Caucasian, 5 Asian, 1 African American, 1 subject undetermined) from San Francisco, California, USA. Significance metric(s): not significant. Type of association: GN; PK.- Variant Name:
- ABCB1:3435T>C, Ile1145Ile
- Related Drugs:
- dicloxacillin, rifampin
- Evidence:
-
PMID:15778422
-
rs1045642
at chr7:86976581
in
ABCB1
Risk or phenotype-associated allele: none. Phenotype: No association with dicloxacillan pharmacokinetics given 1g dicloxacillan prior to or after 600 mg rifampin (ABCB1 (P-gp) inducer). Study size: 18 (13 male). Study population/ethnicity: Healthy volunteers (12 Caucasian, 5 Asian, 1 African American, 1 subject undetermined) from San Francisco, California, USA. Significance metric(s): not significant. Type of association: GN; PK.- Variant Name:
- ABCB1:3435T>C, Ile1145Ile
- Related Drugs:
- dicloxacillin, rifampin
- Evidence:
-
PMID:15778422
-
rs2032582
at chr7:86998554
in
ABCB1
ABCB1 rs2032582 and rs1045642 genotype and peripheral blood lymphocyte efflux of P-gp substrate, rhodamine 123 (Rh123), in vitro, in healthy males: there was no significant difference in Rh123 efflux in CD56+ NK cells after 5, 10, 15, and 30 min efflux, or in CD4+ T-helper cells after 15, 30, 60, and 90 min between individuals with different genotypes. Rh123 efflux was not enhanced by a 10-day administration of P-gp inducer, rifampin, in vivo in 15 individuals before and after rifampin treatment. No genotypic effect was observed for inhibition of Rh123 efflux by P-pg inhibitor, verapamil, in vitro with CD56+ and CD4+.- Variant Name:
- ABCB1:2677G>T/A, mRNA 3095G>T/A, Ala893Ser/Thr
- Related Drugs:
- rhodamine 123, rifampin, verapamil
- Evidence:
-
PMID:12914549
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
ABCB1 |
|
Publications, Variants |
|
|
ABCC2 |
|
Publications |
|
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CYP1A2 |
|
Publications |
|
|
CYP24A1 |
|
Publications |
|
|
CYP2A6 |
|
Publications |
|
|
CYP2B6 |
|
Publications |
|
|
CYP2C19 |
|
Publications |
|
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CYP2C8 |
|
Publications |
|
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CYP2C9 |
|
Publications |
|
|
CYP2D6 |
|
Publications |
|
|
CYP2E1 |
|
Publications |
|
|
CYP3A |
|
Publications |
|
|
CYP3A4 |
|
Publications |
|
|
DRD2 |
|
Publications |
|
|
NR1I2 |
|
Publications, Variants |
|
|
NR1I3 |
|
Publications |
|
|
SLCO1B1 |
|
Publications |
|
|
SLCO1B3 |
|
Publications |
|
|
SLCO2B1 |
|
Publications |
|
|
UGT1A1 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ABCB1 |
|
(source: Drug Bank) |
| NR1I2 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
atorvastatin |
|
Publications |
|
|
donepezil |
|
Publications |
|
|
efavirenz |
|
Publications |
|
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losartan |
|
Publications |
|
|
nevirapine |
|
Publications |
|
|
risperidone |
|
Publications |
|
|
sorafenib |
|
Publications |
|
|
warfarin |
|
Publications |
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) |
| alfentanil |
|
Rifampin reduces levels and efficacy of alfentanil (source: Drug Bank) |
| amiodarone |
|
Rifampin decreases the effect of amiodarone (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 |
|
In presence of rifampin, anticipate decrease of amprenavir (source: Drug Bank) |
| atazanavir |
|
Rifampin reduces levels and efficacy of atazanavir (source: Drug Bank) |
| atorvastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| atovaquone |
|
The agent decreases the effect of atovaquone (source: Drug Bank) |
| bisoprolol |
|
Rifampin decreases the effect of the metabolized beta-blocker (source: Drug Bank) |
| bupropion |
|
Rifampin reduces bupropion levels (source: Drug Bank) |
| buspirone |
|
Rifampin decreases the effect of buspirone (source: Drug Bank) |
| celecoxib |
|
Decreased levels/effect of the NSAID (source: Drug Bank) |
| cerivastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| chloramphenicol |
|
Rifampin decreases the effect of chloramphenicol (source: Drug Bank) |
| chlorpropamide |
|
Rifampin decreases the effect of sulfonylurea (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 |
|
Rifampin decreases the effect of clozapine (source: Drug Bank) |
| cortisone acetate |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| cyclosporine |
|
The rifamycin decreases the effect of cyclosporine (source: Drug Bank) |
| dapsone |
|
Decreased levels of dapsone (source: Drug Bank) |
| dasatinib |
|
Decreased levels/efficacy of dasatinib (source: Drug Bank) |
| delavirdine |
|
Rifampin decreases the effect of delavirdine (source: Drug Bank) |
| desipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| dexamethasone |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| diazepam |
|
Rifampin decreases the effect of benzodiazepine (source: Drug Bank) |
| diclofenac |
|
Decreased levels/effect of the NSAID (source: Drug Bank) |
| dicumarol |
|
The rifamycin decreases the anticoagulant effect (source: Drug Bank) |
| diltiazem |
|
Rifampin decreases levels of diltiazem (source: Drug Bank) |
| disopyramide |
|
Rifampin decreases the effect of disopyramide (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) |
| enalapril |
|
Rifampin decreases the effect of enalapril (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 contraceptive effect (source: Drug Bank) |
| fentanyl |
|
Rifampin reduces levels and efficacy of alfentanil (source: Drug Bank) |
| fluconazole |
|
Fluconazole decreases the effect of imidazole (source: Drug Bank) |
| fluvastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| fosamprenavir |
|
In presence of rifampin, anticipate decrease of amprenavir (source: Drug Bank) |
| gefitinib |
|
Rifampin reduces levels and efficacy of gefitinib (source: Drug Bank) |
| glibenclamide |
|
Rifampin decreases the effect of sulfonylurea (source: Drug Bank) |
| gliclazide |
|
Rifampin decreases the effect of sulfonylurea (source: Drug Bank) |
| glimepiride |
|
Rifampin decreases the effect of sulfonylurea (source: Drug Bank) |
| glipizide |
|
Rifampin decreases the effect of sulfonylurea (source: Drug Bank) |
| haloperidol |
|
The rifamycin decreases the effect of haloperidol (source: Drug Bank) |
| hydrocortisone |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| imatinib |
|
Rifampin decreases levels of imatinib (source: Drug Bank) |
| imipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| indinavir |
|
Rifampin decreases the effect of indinavir (source: Drug Bank) |
| itraconazole |
|
Rifampin decreases the effect of the imidazole (source: Drug Bank) |
| ketoconazole |
|
Rifampin decreases the effect of the imidazole (source: Drug Bank) |
| lamotrigine |
|
Rifampin decreases levels of lamotrigine (source: Drug Bank) |
| leflunomide |
|
Rifampin increases the effect of leflunomide (source: Drug Bank) |
| losartan |
|
Rifampin decreases the effect of losartan (source: Drug Bank) |
| lovastatin |
|
The rifamycin decreases the effect of the statin drug (source: Drug Bank) |
| mefloquine |
|
Rifampin lowers mefloquine levels (source: Drug Bank) |
| mephenytoin |
|
Rifampin decreases the effect of the hydantoin (source: Drug Bank) |
| mestranol |
|
This product may cause a slight decrease of contraceptive effect (source: Drug Bank) |
| methadone |
|
The rifamycin decreases the effect of methadone (source: Drug Bank) |
| methylprednisolone |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| metoprolol |
|
Rifampin decreases the effect of the metabolized beta-blocker (source: Drug Bank) |
| mexiletine |
|
Rifampin decreases the effect of mexiletine (source: Drug Bank) |
| midazolam |
|
Rifampin decreases the effect of benzodiazepine (source: Drug Bank) |
| morphine |
|
Rifampin decreases the effect of morphine/codeine (source: Drug Bank) |
| mycophenolate mofetil |
|
Significant decrease in immunosuppressant levels (source: Drug Bank) |
| nelfinavir |
|
Rifampin decreases the effect of nelfinavir (source: Drug Bank) |
| nifedipine |
|
Rifampin decreases the effect of the calcium channel blocker (source: Drug Bank) |
| norethindrone |
|
This product may cause a slight decrease of contraceptive effect (source: Drug Bank) |
| nortriptyline |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| phenytoin |
|
Rifampin decreases the effect of the hydantoin (source: Drug Bank) |
| prednisolone |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| prednisone |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| propafenone |
|
Rifampin decreases the effect of propafenone (source: Drug Bank) |
| propranolol |
|
Rifampin decreases the effect of the metabolized beta-blocker (source: Drug Bank) |
| protriptyline |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| quinidine |
|
Rifampin decreases the effect of quinidine (source: Drug Bank) |
| repaglinide |
|
Rifampin decreases the effect of repaglinide (source: Drug Bank) |
| ritonavir |
|
Rifampin decreases the effect of ritonavir (source: Drug Bank) |
| rofecoxib |
|
Decreased levels/effect of the NSAID (source: Drug Bank) |
| rosiglitazone |
|
Rifampin reduces levels and efficacy of rosiglitazone (source: Drug Bank) |
| saquinavir |
|
Rifampin 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) |
| tadalafil |
|
Rifampin reduces levels and efficacy of tadalafil (source: Drug Bank) |
| tamoxifen |
|
The rifamycin decreases the effect of anti-estrogen (source: Drug Bank) |
| telithromycin |
|
Rifampin decreases the effect of telithromycin (source: Drug Bank) |
| terbinafine |
|
Rifampin decreases the effect of terbinafine (source: Drug Bank) |
| theophylline |
|
Rifampin decreases the effect of theophylline (source: Drug Bank) |
| tocainide |
|
Rifampin lowers tocainide levels/effects (source: Drug Bank) |
| tolbutamide |
|
Rifampin decreases the effect of sulfonylurea (source: Drug Bank) |
| toremifene |
|
The rifamycin decreases the effect of anti-estrogen (source: Drug Bank) |
| triamcinolone |
|
The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank) |
| triazolam |
|
Rifampin decreases the effect of benzodiazepine (source: Drug Bank) |
| trimethoprim |
|
Rifampin decreases the effect of trimethoprim (source: Drug Bank) |
| trimipramine |
|
The rifamycin decreases the effect of tricyclics (source: Drug Bank) |
| verapamil |
|
Rifampin decreases the effect of the calcium channel blocker (source: Drug Bank) |
| voriconazole |
|
Rifampin decreases the effect of voriconazole (source: Drug Bank) |
| warfarin |
|
The rifamycin decreases the anticoagulant effect (source: Drug Bank) |
| zaleplon |
|
Rifampin decreases the effect of zaleplon (source: Drug Bank) |
| zidovudine |
|
The rifamycin decreases levels of zidovudine (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
HIV |
|
Publications |
|
|
Leukemia |
|
Publications |
|
|
Meningitis, Bacterial |
|
Publications |
|
|
Mycobacterium Infections |
|
Publications |
|
|
Osteomalacia |
|
Publications |
|
|
Osteosarcoma |
|
Publications |
|
|
Toxic liver disease |
|
Publications |
|
|
Tuberculosis |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
- In vivo and in vitro characterization of variants




- PD
- PK
- FA
Submitted by Mary Relling, PharmD involving CYP3A, CYP3A4, CYP3A5, NR1I2, , midazolam, nifedipine, rifampin and troleandomycin
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
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LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
