Rifampicin

General characteristics. Structure:

Active agent: 150 mg of rifampicin.

Excipients: sodium lauryl sulfate, starch corn, magnesium stearate.

Antimicrobic means with the expressed activity against mycobacteria.

Pharmacological properties:

Pharmacodynamics. Rifampitsinaktiven in relation to Micobacteriumtuberculosis. Bactericidal action is connected with suppression of activity of a DNA-dependent RNA polymerase of microorganisms. Enzyme of breast milk does not oppress. Cross resistance to rifampicin is proved only in relation to other Rifamycinums.

Pharmacokinetics. Rifampicin is well soaked up through digestive tract. The peak of concentration in serum can vary from 4 to 32 mg/ml. Absorption of rifampicin worsens at its reception with food.

In an organism of healthy volunteers the rifampicin elimination half-life in plasma makes about 3 hours after acceptance of a dose of 600 mg and increases till 5,1 o'clock after a dose in 900 mg. At regular reception the elimination half-life decreases till 2-3 o'clock. These indicators do not change at patients with a renal failure and, therefore, there is no need for change of a dosage.

After absorption rifampicin is quickly removed in bile what its enterogepatichesky circulation follows. During this process rifampicin is exposed to the progressing deatsetilyation and almost in full is in bile in this form about 6 hours. This intermediate product fully keeps antibacterial activity. Deatsetilyation interferes with a reabsorption through intestines that facilitates a substance conclusion. To 30% of a dose it is removed with urine, and about a half of this quantity represents not modified rifampicin.

Rifampicin well gets into many fabrics and bodies of an organism, and also cerebrospinal fluid. About 80% of rifampicin contact protein. An untied part is not ionized and freely gets into fabrics.

Indications to use:

Pulmonary tuberculosis and other bodies.

Route of administration and doses:

Drug is accepted inside on an empty stomach by 0,5-1 h to food or in 2 h after food.

At treatment of tuberculosis the average daily dose for adults makes 450 mg once a day. At patients (especially in the period of an aggravation) with body weight higher than 50 kg the daily dose can be increased to 600 mg.

Average daily dose for children over 3 years – 10 mg/kg (but no more than 450 mg a day) once a day. At bad portability of rifampicin the daily dose can be divided into two receptions.

At infections of not tubercular nature appoint adult 450-900 mg a day, and to children – 8-10 mg/kg in 2-3 receptions.

At acute gonorrhea appoint inside in a dose 900 mg a day once or within 1-2 days.

Features of use:

At daily reception of rifampicin its portability is better, than at intermittent treatment. At reception of a dose more than 600 mg one or two times a week increase probability of emergence of such side reactions as "an influenzal syndrome" (fever, a fever, an indisposition), a leukopenia, thrombocytopenia, acute hemolitic anemia, skin, gastrointestinal and gepatichesky reactions, an asthma, shock and a renal failure.

In some cases, during the first days of treatment, the hyperbilirubinemia caused by the competition of rifampicin and bilirubin in secretory ways of a liver at the cellular level is possible.

Against the background of use urine, the lacrimal liquid and a phlegm can get a reddish shade that does not represent health hazard. On soft contact lenses emergence of spots is possible.

Pregnancy and lactation. Rifampicin gets into breast milk therefore when using this means it is not necessary to nurse the baby, except cases when, according to the doctor, the expected positive effect prevails over potential risk for the child.

Side effects:

Reactions of a nervous system: headache, drowsiness, exhaustion, ataxy, dizziness, disturbance of concentration of attention, muscular weakness, extremity pains, numbness.

Gastrointestinal frustration: heartburn, anorexia, nausea, vomiting, spasms.

Hematologic reactions: thrombocytopenia, tranzitorny leukopenia, hemolitic anemia. At intermittent therapy or at continuation of reception of rifampicin after emergence of a purpura there were cases of cerebral hemorrhages and death.

Renal reactions: hemolysis, haemoglobinuria, hamaturia, acute renal failure, necrosis of tubules of a kidney.

Hepatic reactions: hepatitis, acute liver failure.

Allergic and immunological reactions: an itch, urticaria, dryness in a throat, an eosinophilia, conjunctivitis.

Ophthalmologic reactions: vision disorder.

Interaction with other medicines:

Rifampicin induces microsomal enzymes of a liver and can weaken action of a number of medicinal substances, including anticoagulants, corticosteroids, cyclosporine, foxglove drugs, theophylline, verapamil, Phenytoinum, quinidine, oral contraceptives, oral hypoglycemic means, chloramphenicol, antifungal means, drugs and analgetics. At reception of the called drugs in parallel with rifampicin correction of their dosages can be required.

At reception of rifampicin in parallel with paraminosalitsilovy acid decrease in level of rifampicin in serum in this connection these means have to be accepted with an interval at least at 4 o'clock is possible. Cases of temporary increase in a bromosulfalein and bilirubin are known.

The women applying oral contraceptives are recommended to pass into treatment time for other, non-hormonal means of prevention of pregnancy.

Pregnancy and lactation. Rifampicin gets into breast milk therefore when using this means it is not necessary to nurse the baby, except cases when, according to the doctor, the expected positive effect prevails over potential risk for the child.

Contraindications:

Drug is contraindicated at hypersensitivity to drug components, diseases of kidneys with decrease in secretory function, infectious hepatitis, heavy reactions to an isoniazid, such as fever, fever and arthritis; to patients with acute gout.

Means should not be appointed in the first trimester of pregnancy, and also at chest feeding. After three months of pregnancy means can be appointed in urgent cases, under direct observation of the doctor and on condition of dominance of the expected positive action over risk for a fruit.

At reception within the last weeks pregnancies means is capable to cause puerperal bleedings in the child and mother, in this case purpose of vitamin K - 1 is possible.

Overdose:

At overdose of rifampicin nausea, vomiting, the increased drowsiness, a loss of consciousness arising within a short period of time after reception are possible. Skin, urine, the lacrimal liquid and a phlegm can get a reddish shade.

At heavy overdose increase in a liver, increase in level of bilirubin and developing of jaundice is possible.

Storage conditions:

List B. To store in densely closed container in the dry, cool, protected from light place at a temperature not above 25 °C. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

Capsules on 150 mg on 10 pieces in the blister, on 2 blisters in a cardboard pack.