Rifabutin

Products

Rifabutin is commercially available in capsule form (mycobutin). It has been approved in many countries since 1994.

Structure and properties

Rifabutin (C46H62N4O11, Mr = 847 g/mol ) is a semisynthetic ansamycin antibiotic. It exists as a reddish purple amorphous powder that is sparingly soluble in water.

Effects

Rifabutin (ATC J04AB04) has antibacterial properties against mycobacteria. The effects are due to inhibition of DNA-dependent bacterial RNA polymerase.

Indications

  • For combination treatment of pulmonary tuberculosis (Mycobacterium tuberculosis).
  • For prevention and combination treatment of Mycobacterium avium intracellulare complex (MAC) infections in HIV.

Dosage

According to the professional information. The capsules are taken once a day and independently of meals.

Contraindications

  • Hypersensitivity, including to rifamycin.
  • Combination with ritonavir

Full precautions can be found in the drug label.

Interactions

Rifabutin is a known inducer of CYP3A4 and thus can reduce the concentrations and efficacy of numerous drugs to a relevant extent. It is itself also metabolized by this enzyme. Other drug interactions are possible with HIV protease inhibitors (CYP inhibitors) and antacids, among others.

Adverse effects

The most common possible adverse effects include a rash, neutropenia, and leukopenia. Other common adverse reactions include fever, hypersensitivity reactions, shock, headache, insomnia, muscle pain, indigestion, bad taste, weakness, chest pain, pain, thrombocytopenia, anemia, eosinophilia, urine discoloration, and an increase in liver enzymes.