Rifampin drug data and news

Rifampin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Rifampin
Brand Names/Synonyms Archidyn; L-5103 Lepetit; R/AMP; RAMP; RFP; Ramp; Rfamipicin; Rifa; Rifadin; Rifadin Iv; Rifadine; Rifagen; Rifaldazin; Rifaldazine; Rifaldin; Rifamate; Rifampicin; Rifampicin Sv; Rifampin; Rifamycin; Rifamycin Amp; Rifaprodin; Rifater; Rifoldin; Rifoldine; Riforal; Rimactan; Rimactane; Rimactin; Rimazid; Rofact; Tubocin
Indication For the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections
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Description Not Available
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 Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. 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.
Mechanism Of Action Rifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
Rifampin News
(When available)

Trends in Tuberculosis—United States, 2005  16 May 2006
...all non-Hispanic. Persons identified as Hispanic might be of any race. Defined as resistant to at least isoniazid and rifampin. - Journal of American Medical Association (subscription),

New Study Shows Initial Treatment With 800 mg/day Imatinib ...  May 15, 2006
...least 50% and clinical response should be carefully monitored in patients receiving Gleevec tablets with a potent CYP3A4 inducer such as rifampin or phenytoin. ... - DG News

Leaders call for countries to tackle tough TB  May 10, 2006
For more than a decade, health officials have worried about "multidrug-resistant" TB, which can withstand the mainline antibiotics isoniazid and rifampin. ... - Columbus Ledger-Enquirer,

View larger version (35K):  May 3, 2006
The patient was treated with ethambutol, isoniazid, pyrazinamide, and rifampin for six months, with an excellent clinical response. ... - New England Journal of Medicine (subscription),

Inmate dies from infection; rest given antibiotics  May 1, 2006
...passed it on. The state health department was informed and sent 1,440 doses of the antibiotic rifampin to the jail. Inmates and ... - Atlanta Journal Constitution (subscription),

Fatal illness stirs concern at jail  May 2, 2006
...passed it on. The state Health Department was informed and sent 1,440 doses of the antibiotic Rifampin to the jail. Inmates and ... - Atlanta Journal Constitution (subscription),

Drug-resistant strain emerges  Apr 17, 2006
The term refers to bacteria that are resistant to the two first-line therapies normally used to treat the disease, the antibiotics - isoniazid and rifampin. ... - Deccan Herald,

Dosage Forms CAPSULE
Drug_Category Leprostatic Agents; Antibiotics; Antituberculosis Agents; ATC:J04AB
Absorption Well absorbed from gastrointestinal tract
Interactions Interactions for Rifampin:

ENZYME INDUCTION: Rifampin is known to induce certain cytochrome P-450 enzymes. Administration of rifampin with drugs that undergo biotransformation through these metabolic pathways may accelerate elimination of coadministered drugs. To maintain optimum therapeutic blood levels, dosages of drugs metabolized by these enzymes may require adjustment when starting or stopping concomitantly administered rifampin.

Rifampin has been reported to accelerate the metabolism of the following drugs: anticonvulsants (eg, phenytoin), antiarrhythmics (eg, disopyramide, mexiletine, quinidine, tocainide), oral anticoagulants, antifungals (eg, fluconazole, itraconazole, ketoconazole), barbiturates, beta-blockers, calcium channel blockers (eg, diltiazem, nifedipine, verapamil), chloramphenicol, clarithromycin, corticosteroids, cyclosporine, cardiac glycoside preparations, clofibrate, oral or other systemic hormone contraceptives, dapsone, diazepam, doxycycline, fluoroquinolones (eg ciprofloxacin), haloperidol, oral hypoglycemic agents (sulfonylureas), levothyroxine, methadone, narcotic analgesics, nortriptyline, progestins, quinine, tacrolimus, theophylline tricyclic antidepressants (eg, amitriptyline, nortriptyline), and zidovudine. It may be necessary to adjust the dosages of these drugs if they are given concurrently with rifampin.

Patients using oral or other systemic hormonal contraceptives should be advised to change to nonhormonal methods of birth control during rifampin therapy.

Rifampin has been observed to increase the requirements for anticoagulant drugs of the coumarin type. In patients receiving anticoagulants and rifampin concurrently, it is recommended that the prothrombin time be performed daily or as frequently as necessary to establish and maintain the required dose of anticoagulant.

Diabetes may become more difficult to control.

OTHER INTERACTIONS: When the two drugs were taken concomitantly, decreased concentrations of atovaquone and increased concentrations of rifampin were observed.

Concurrent use of ketoconazole and rifampin has resulted in decreased serum concentrations of both drugs. Concurrent use of rifampin and enalapril has resulted in decreased concentrations of enalaprilat, the active metabolite of enalapril. Dosage adjustments should be made if indicated by the patient's clinical condition.

Concomitant antacid administration may reduce the absorption of rifampin. Daily doses of rifampin should be given at least 1 hour before the ingestion of antacids.

Probenecid and cotrimoxazole have been reported to increase the blood level of rifampin.

When rifampin is given concomitantly with either halothane or isoniazid, the potential for hepatotoxicity is increased. The concomitant use of rifampin and halothane should be avoided. Patients receiving both rifampin and isoniazid should be monitored close for hepatotoxicity.

Plasma concentrations of sulfapyridine may be reduced following the concomitant administration of sulfasalazine and rifampin. This finding may be the result of alteration in the colonic bacteria responsible for the reduction of sulfasalazine to sulfapyridine and mesalamine.

Toxicity LD50=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness
Organisms Affected Mycobacteria and a variety of other gram negative and gram postivie bacteria
Chemical IUPAC Name {2,7-(Epoxypentadeca[1,11,13]trienimino)naphtho[2,} 1-b\]furan-1,11(2H)-dione, {22-heptamethyl-8-[N-(4-methyl-1-piperazinyl)formimidoyl]-,} 21-acetate
Chemical Formula C43H58N4O12
Molecular Weight 822.94 g/mol
Smiles String CC1C=CC=C(C(=O)N=C2C(=CNN3CCN(CC3)C)C(=C4C(=C2O)C(=C(C5=C4C(=O)C(O5)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)C)O)O)C
Melting Point 183 °C
Water Solubility 1.4 mg/mL
State Solid
LogP/Hphobicity 3.719
Isoelectric Point Not Available
Biotransformation Primarily hepatic, rapidly deacetylated.
Half Life 3.35 (+/- 0.66) hours
Protein Binding [%] 89%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Rifampin.html
http://www.rxlist.com/cgi/generic2/rifampin.htm
http://www.mpfinechemicals.com/PDF/msds/195490.pdf
Drug Type Approved Drug
Accession No APRD00207
CAS Registry Number 13292-46-1
KEGG Compound ID C06688
PubChem ID SID:168608
PharmGKB ID PA451250
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 393444

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