Products
Rifampicin is commercially available as film-coated tablets, coated tablets, capsules, and injectables (Rimactan, generics). In addition to mono, various combination preparations are also available. Rifampicin has been approved in many countries since 1968. This article refers to peroral monotherapy.
Structure and properties
Rifampicin (C43H58N4O12, Mr = 823 g/mol) exists as a reddish brown to brownish red crystalline powder that is sparingly soluble in water. It is semisynthetically derived from rifamycin SV. It was developed in the 1950s by Sensi and Timbal at the Dow-Lepetit research laboratories in Milan, Italy. Rifampicin is also known as rifampin.
Effects
Rifampicin (ATC J04AB02) has bactericidal properties against and as well as other Gram-positive and Gram-negative bacteria. The effects are due to selective inhibition of bacterial DNA-dependent RNA polymerase. The half-life is short, ranging from 1 to 5 hours. Rifampicin distributes well and also has intracellular effects.
Indications
For the treatment of bacterial infectious diseases with susceptible pathogens:
- Tuberculosis (combination therapy).
- Leprosy (combination therapy)
- Non-mycobacterial infections: Brucellosis, meningococcal meningitis prophylaxis.
Dosage
According to the professional information. Medicines must be taken fasting, at least half an hour before eating.
Contraindications
- Hypersensitivity
- Liver disease, cirrhosis, peripheral neuritis, porphyria.
- Combination with voriconazole
- Combination with protease inhibitors
- Combination with telaprevir
- Combination with saquinavir + ritonavir (liver toxicity).
- Combination with halothane (liver toxicity).
Full precautions can be found in the drug label.
Interactions
Rifampicin has a high potential for drug-drug interactions. It is a known inducer of CYP450 isoenzymes. This may increase the metabolism of CYP substrates and lead to a decrease in efficacy. Furthermore, rifampicin also induces drug transporters such as P-glycoprotein.
Adverse effects
The most common potential adverse effects include:
- Fatigue, drowsiness, headache, drowsiness, dizziness.
- Eye redness
- Lack of appetite, nausea, abdominal pain, flatulence.
- Heat sensation, itching with or without rash, urticaria.
Rifampicin can turn the skin, urine, sweat, saliva, tears, and stools orange-red. It has liver-toxic properties and can rarely cause hepatitis, jaundice, and in the worst cases, liver failure and fulminant hepatitis.
