Rifampicin: Effect, Applications, Side Effects

How rifampicin works

The antibiotic rifampicin is effective against various strains of bacteria. It blocks a bacterial enzyme (RNA polymerase) that the germs need to produce vital proteins. As a result, they die. The antibiotic therefore has a bactericidal (bactericidal) effect.

Because it is well distributed in the body – rifampicin also has a good intracellular effect – it is usually used to treat sensitive pathogens that reside inside body cells, such as various mycobacteria.

Absorption, breakdown and excretion

Rifampicin is easily absorbed from the intestine into the bloodstream after being taken by mouth. There it binds to about 80 percent of plasma proteins and is distributed evenly throughout the body. Particularly high concentrations can be found in the lungs and bile.

Approximately two to five hours after ingestion, half of the antibiotic has left the body, mainly in the bile (and therefore in the stool). This elimination half-life is shortened with longer treatment periods.

Rifampicin is used for

  • Treatment of tuberculosis (in combination with other medicines)
  • Treatment of infections with non-tuberculous mycobacteria (in combination with other medicines)
  • Treatment of leprosy (in combination with other medicines)
  • Treatment of certain non-mycobacterial infections (in combination with other medicines)
  • Treatment of brucellosis (in combination with a tetracycline antibiotic)
  • Prevention (prophylaxis) of meningococcal meningitis (meningococcal meningitis)

How long rifampicin must be taken (and possibly with which other medications) depends on the infection in question.

How rifampicin is used

The active ingredient is usually taken orally. Tuberculosis patients are usually given ten milligrams of rifampicin per kilogram of body weight once a day. For other infections, the dosage is usually six to eight milligrams per kilogram of body weight twice a day.

What are the side effects of rifampicin?

Since severe side effects in the liver occur primarily in a previously damaged organ, liver function is checked before starting therapy. Liver values (such as liver enzymes) should be checked regularly during treatment.

Other possible rifampicin side effects include gastrointestinal complaints, menstrual cycle disorders, skin reactions (such as redness, itching) and a temporary lack of certain blood cells (neutrophil granulocytes and thrombocytes). Fatigue, headaches, dizziness and loss of appetite may also occur.

Some patients develop flu-like symptoms (especially if they take the antibiotic irregularly or if they start taking it again after an interruption).

Rifampicin can turn all body fluids (urine, saliva, sweat, tears, stool, etc.) orange-red.

If you suffer from severe side effects or develop symptoms other than those mentioned during treatment, please consult your doctor.

What should I bear in mind when taking rifampicin?

Contraindications

Rifampicin must not be taken if:

  • severe liver dysfunction
  • concomitant treatment with certain active substances against HIV (with protease inhibitors, non-nucleoside reverse transcriptase inhibitors or integrase inhibitors)
  • concomitant treatment with certain active substances against hepatitis C (with non-structural protein 5A inhibitors or the polymerase inhibitors dasabuvir and sofosbuvir)
  • concomitant treatment with voriconazole (antifungal agent)
  • concomitant treatment with cobicistat (booster for some antibiotics)

Interactions

The combination with other liver-damaging medications and the use of rifampicin with regular alcohol consumption can also be dangerous.

The antibiotic strongly stimulates the formation of liver enzymes. This affects CYP enzymes (such as CYP3A4, CYP2, CYP2B, CYP2C), UDP-glucuronosyl transferase 1A (UGT1A) and P-glycoproteins. Among other things, these enzymes ensure the breakdown of various drugs – including rifampicin itself. The antibiotic can therefore accelerate its own degradation and that of other drugs.

Your doctor will therefore ask you very carefully about other medicines you are taking before starting rifampicin treatment in order to avoid interactions as far as possible from the outset.

During treatment with rifampicin, you should first ask your doctor or pharmacist before taking any new medication (including over-the-counter and herbal preparations) whether the medication in question is suitable for simultaneous use.

Age restriction

Rifampicin can, if necessary, be administered to infants in an adjusted dosage.

Pregnancy and breastfeeding

Acute tuberculosis during pregnancy can be treated with rifampicin. In the case of other infections, however, its use should be examined critically – it is advisable to switch to other and better proven antibiotics if possible.

Rifampicin is also one of the drugs of choice for tuberculosis during breastfeeding. According to previous reports, there is no risk to the breastfed infant if the mother is treated with the antibiotic. In individual cases, babies have thinner stools and rarely diarrhea.

How to obtain medication with rifampicin

Rifampicin is available in oral form (e.g. as a tablet) and as an infusion solution. In Germany, Austria and Switzerland, the active ingredient is only available on prescription in all dosage forms.

How long has rifampicin been known?

In 1957, antibacterial substances were isolated from the fungus Streptomyces mediterranei and named rifamycins. Their best-known representative is rifampicin.