Description

Simple

An antibiotic used to treat several types of bacterial infections, but most commonly for the treatment of tuberculosis.

Clinical

An antibiotic used to treat several types of mycobacterial infections including Mycobacterium avium complex, leprosy, and in combination with other antibacterials to treat latent or active tuberculosis.

Overview

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)

Pharmacology

Indication

For the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections.

Pharmacodynamic

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-neg... Read more

Mechanism of action

Rifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.

Absorption

Well absorbed from gastrointestinal tract.

Protein binding

89%

Volume of distribution

Information currently not available.

Clearance

0.19 +/- 0.06 L/hr/kg [300 mg IV]0.14 +/- 0.03 L/hr/kg [600 mg IV]

Half life

3.35 (+/- 0.66) hours

Route of elimination

Less than 30% of the dose is excreted in the urine as rifampin or metabolites.

Toxicity

LD50=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Shortness of Breath US
Case Reports Varying Reports
Flu syndrome US
Case Reports Varying Reports
Decrease in blood pressure US
Case Reports Varying Reports
Wheezing US
Case Reports Varying Reports
Adrenal Insufficiency US
Varying Reports
Shock US
Case Reports Varying Reports
Cutaneous reactions US
Case Reports Varying Reports
Pruritus US
Case Reports Varying Reports
Urticaria US
Case Reports Varying Reports
Rash US
Case Reports Varying Reports
Pemphigoid reaction US
Case Reports Varying Reports
Erythema multiforme US
Case Reports Varying Reports
Stevens-Johnson Syndrome US
Case Reports Varying Reports
Toxic Epidermal Necrolysis US
Case Reports Varying Reports
Vasculitis US
Case Reports Varying Reports
Eosinophilia US
Case Reports Varying Reports
Sore mouth US
Case Reports Varying Reports
Sore tongue US
Case Reports Varying Reports
Conjunctivitis US
Case Reports Varying Reports
Anaphylaxis US
Case Reports Varying Reports
Edema of the face US
Case Reports Varying Reports
Edema of the extremities US
Case Reports Varying Reports
Nausea US
Case Reports Varying Reports
Anorexia US
Case Reports Varying Reports
Jaundice US
Case Reports Varying Reports
Vomiting US
Case Reports Varying Reports
Epigastric distress US
Case Reports Varying Reports
Heartburn US
Case Reports Varying Reports
Hepatitis US
Case Reports Varying Reports
Transient abnormalities in liver function tests US
Case Reports Varying Reports
Thrombocytopenia US
Case Reports Varying Reports
Shock-like syndrome with hepatic involvement US
Case Reports Varying Reports
Cramps US
Case Reports Varying Reports
Flatulence US
Case Reports Varying Reports
Pseudomembranous Colitis US
Case Reports Varying Reports
Diarrhea US
Case Reports Varying Reports
Elevations in BUN US
Case Reports Varying Reports
Menstrual disturbances US
Case Reports Varying Reports
Visual disturbances US
Case Reports Varying Reports
Myopathy US
Case Reports Varying Reports
Psychosis US
Case Reports Varying Reports
Generalized numbness US
Case Reports Varying Reports
Pain in extremities US
Case Reports Varying Reports
Muscular Weakness US
Case Reports Varying Reports
Acute Renal Failure US
Case Reports Varying Reports
Renal Insufficiency US
Case Reports Varying Reports
Acute tubular necrosis US
Case Reports Varying Reports
Interstitial nephritis US
Case Reports Varying Reports
Hematuria US
Case Reports Varying Reports
Hemoglobinuria US
Case Reports Varying Reports

Contraindications

  • Route:
    • Oral
    • Intravenous
  • Regions: US
  • With Drugs Coadmin:
      • Name: Atazanavir
      • Drugbank Id: DB01072
  • Route:
    • Oral
    • Intravenous
  • Regions: US
  • With Drugs Coadmin:
      • Name: Saquinavir
      • Drugbank Id: DB01232
  • Route:
    • Oral
    • Intravenous
  • Regions: US
  • With Drugs Coadmin:
      • Name: Tipranavir
      • Drugbank Id: DB00932
  • Route:
    • Oral
    • Intravenous
  • Regions: US
  • With Drugs Coadmin:
      • Name: Fosamprenavir
      • Drugbank Id: DB01319
  • Route:
    • Oral
    • Intravenous
  • Regions: US
  • With Drugs Coadmin:
      • Name: Ritonavir
      • Drugbank Id: DB00503

Food Interactions

Avoid alcohol.

Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.

Take with a full glass of water.