Rifampicin

Rifampicin or rifampin (USAN) is a bacteriostatic antibiotic drug of the rifamycin group. It is a semisynthetic compound derived from Streptomyces mediterranei. Rifampicin may be abbreviated RIF, RMP, RD or R.

Indications

It is typically used to treat Mycobacterium infections, including tuberculosis and leprosy; and also has a role in the treatment of methicillin-resistant Staphylococcus aureus (MRSA) in combination with fusidic acid. It is used in prophylactic therapy against Neisseria meningitidis (meningococcal) infection.

It is also used to treat Listeria species, Neisseria gonorrhoeae, Haemophilus influenzae and Legionella pneumophila For these non-standard indications, sensitivity testing should be done (if possible) before starting rifampicin therapy. Rifampicin resistance develops quickly during treatment and rifampicin monotherapy should not be used to treat these infections – it should be used in combination with other antibiotics.

Enterobacteriaceae, Acinetobacter and Pseudomonas species are intrinsically resistant to rifampicin.

Mechanism of action

Rifampicin inhibits DNA-dependent RNA polymerase in bacterial cells by binding its beta subunit, thus preventing transcription of messenger RNA (mRNA) and subsequent translation to proteins.

Adverse effects

Adverse effects are chiefly related to the drug's hepatotoxicity, and patients receiving rifampicin often undergo liver function tests including aspartate aminotransferase (AST).

The most common unwanted effects are fever, gastrointestinal disturbances, rashes and immunological reactions. Liver damage, associated with jaundice, has also been reported and in some rare cases has led to death.

Taking rifampicin can cause certain bodily fluids, such as urine, tears and semen, to become orange-red in colour. This may permanently stain soft contact lenses. It also may be excreted in breast milk, therefore breast feeding should be avoided.

Rifampicin is an inducer of hepatic cytochrome P450 enzymes (such as CYP2D6 and CYP3A4) and will increase the metabolism of a many drugs that are cleared by the liver through this enzyme system. This results in numerous drug interactions such as reduced efficacy of the oral contraceptive pill.

Preparations

In the US, rifampin is marketed as

  • Rifadin® (Aventis),
  • Rifater® (in combination with isoniazid and pyrazinamide) (Aventis),
  • Rimactane® (Novartis).
  • In the UK, rifampicin is marketed as

  • Rifadin® (Aventis),
  • Rimactane® (Sandoz),
  • Rifater® (in combination with isoniazid and pyrazinamide) (Aventis),
  • Rifinah® (in combination with isoniazid) (Aventis)
  • Rimactazid® (in combination with isoniazid) (Sandoz)
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