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

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 empty stomach: 1 hour before or 2 hours after meals.
  • Take with a full glass of water.

Interactions

Type in a drug name to check for interaction with Rifampicin
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be increased when combined with Rifampicin.
(S)-Warfarin
The metabolism of (S)-Warfarin can be increased when combined with Rifampicin.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be increased when combined with Rifampicin.
8-azaguanine
The metabolism of 8-azaguanine can be increased when combined with Rifampicin.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be increased when combined with Rifampicin.
9-aminocamptothecin
The metabolism of Rifampicin can be increased when combined with 9-aminocamptothecin.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be increased when combined with Rifampicin.
9-Methylguanine
The metabolism of 9-Methylguanine can be increased when combined with Rifampicin.
Abacavir
The metabolism of Abacavir can be increased when combined with Rifampicin.
Abemaciclib
The serum concentration of Rifampicin can be increased when it is combined with Abemaciclib.
Abiraterone
The metabolism of Abiraterone can be increased when combined with Rifampicin.
Acebutolol
The metabolism of Acebutolol can be increased when combined with Rifampicin.
Acefylline
The metabolism of Acefylline can be increased when combined with Rifampicin.
Acenocoumarol
The metabolism of Acenocoumarol can be increased when combined with Rifampicin.
Acetaminophen
Rifampicin may increase the hepatotoxic activities of Acetaminophen.
Acetohexamide
The serum concentration of Acetohexamide can be decreased when it is combined with Rifampicin.
Acetyldigoxin
The serum concentration of Acetyldigoxin can be decreased when it is combined with Rifampicin.
Acetylsalicylic acid
The serum concentration of Rifampicin can be decreased when it is combined with Acetylsalicylic acid.
Acyclovir
The metabolism of Acyclovir can be increased when combined with Rifampicin.
Adefovir dipivoxil
The excretion of Adefovir dipivoxil can be decreased when combined with Rifampicin.
1 References
  1. 1 . Baysarowich J, Koteva K, Hughes DW, Ejim L, Griffiths E, Zhang K, Junop M, Wright GD: Rifamycin antibiotic resistance by ADP-ribosylation: Structure and diversity of Arr. Proc Natl Acad Sci U S A. 2008 Mar 25;105(12):4886-91. doi: 10.1073/pnas.0711939105. Epub 2008 Mar 18.PubMed: 18349144