Rifampicin

When ATH:
J04AB02

Rifampicin – Characteristic

Semi-synthetic derivative of the natural rifamycin. Crystalline powder brick or brick-red color, without smell. Practically insoluble in water, it is soluble in formamide, slightly soluble in ethanol, soluble in ethyl acetate and methanol, freely soluble in chloroform. It is sensitive to oxygen, light and air moisture.

Pharmacological action.
Broad-spectrum antibacterial, bactericide, TB, protivoleproznoe.

Application.

Tuberculosis (all forms) is in combination therapy. Leprosy (in combination with dapsonom-multibacilljarnye types of disease). Infectious diseases, caused by susceptible microorganisms (in case of resistance to other antibiotics, and in a combination antimicrobial therapy). Brucellosis is in combination therapy with tetracycline antibiotic (doxycycline). Meningococcal meningitis (prevention in humans, were in close contact with sick meningococcal meningitis; in batsyllonosyteley Neisseria meningitidis).

Contraindications.

Hypersensitivity, incl. to other drugs of rifamycin, the liver and kidneys, transferred less 1 years ago, infectious hepatitis, jaundice, incl. mechanical.

In / in the introduction: cardio-pulmonary insufficiency II-III degree, phlebitis, childhood.

Restrictions apply.

Age to 1 year, alcoholism (the risk of hepatotoxicity).

Pregnancy and breast-feeding.

It contraindicated in I trimester of pregnancy. In II and III trimesters is possible only under strict indications, After comparing the expected benefits to the mother and the potential risk to the fetus.

Rifampin passes through the blood-placenta barrier (concentration in the serum is fetal birth 33% the concentration in maternal serum). In animal studies, teratogenicity installed. Rabbits, dosed, to 20 times the usual daily human dose, osteopenia and marked toxic effect on the embryo. In experiments in rodents, rifampicin at a dose of 150-250 mg / kg / day induced congenital malformations, primarily cleft lip and palate, Spina Bifida. When used in the last weeks of pregnancy can cause postnatal haemorrhage in the mother and the newborn bleeding.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Provided with breast milk, while the child receives less 1% adopted mother dose. Although adverse reactions in humans has not been registered, at the time of treatment should abandon breastfeeding.

Women of childbearing age during treatment requires reliable contraception (incl. non-hormonal).

Side effects.

From the nervous system and sensory organs: headache, blurred vision, ataxia, disorientation.

Cardio-vascular system and blood (hematopoiesis, hemostasis): low blood pressure (With the rapid on / in a), phlebitis (at long on / in), trombotsitopenicheskaya purpura, trombo- and leukopenia, bleeding, acute hemolytic anemia.

From the digestive tract: oral candidiasis, decreased appetite, nausea, vomiting, erosive gastritis, indigestion, abdominal pain, diarrhea, psevdomembranoznыy colitis, increased liver transaminases and bilirubin in the blood, jaundice (1–3%), hepatitis, the defeat of the pancreas.

With the genitourinary system: tubular necrosis, interstitial nephritis, acute renal failure, menstrual irregularities.

Allergic reactions: skin rash, itch, hives, fever, angioedema, bronchospasm, lacrimation, eozinofilija.

Other: arthralgia, muscular weakness, herpes, induction of porphyria, flu-like symptoms (when intermittent or irregular therapy).

Cooperation.

As a potent inducer of cytochrome P450, can cause potentially dangerous interactions.

Reduces the activity of anticoagulants, corticosteroids, oral hypoglycemic agents, Digitalis preparations, antiarrhythmics (incl. disopyramide, quinidine, mexiletine), antiepileptics, dapsone, metadona, gidantoinov (phenytoin), geksoʙarʙitala, nortriptyline, haloperidol, benzodiazepines, drugs hormones, incl. oral contraceptives, tiroksina, teofillina, chloramphenicol, doxycycline, ketoconazole, itraconazole, Terbinafine, Cyclosporin A, azathioprine, beta-blockers, BCC, fluvastatin, Enalapril, cimetidine (due to the induction of hepatic microsomal enzymes and accelerate the metabolism of these drugs). It should not be taken with indinavir sulfate, nelfinavir and, tk. their plasma concentrations due to the acceleration of metabolism are greatly reduced. Preparations Pasco, soderzhashtie bentonite (hydrous aluminum), and antacids while taking violate the absorption of rifampicin. Together with the admission of opiates, anticholinergics and ketoconazole decreased bioavailability of rifampicin; probenecid and co-trimoxazole increase its concentration in blood. Simultaneous treatment with isoniazid and pyrazinamide increases the frequency and severity of liver dysfunction (amid liver disease) and the likelihood of developing neutropenia.

Overdose.

Symptoms: nausea, vomiting, abdominal pain, enlargement of the liver, jaundice, periorbital edema, or swelling of the face, pulmonary edema, clouding of consciousness, convulsions, mental disorders, lethargy, "Red man syndrome" (red-orange color of the skin, mucous membranes and sclera).

Treatment: gastric lavage, administration of activated charcoal, diurez, simptomaticheskaya therapy.

Dosing and Administration.

Inside, / drip. Inside, fasting (30-60 minutes before meals or 2 hours after meals), with a full glass of water. B / drip (introduction rate of 60-80 drops per minute). When poor tolerability daily dose can be divided into 2 reception / administration.

Tuberculosis: PO / in (with subsequent transition to oral), adults weighing less than 50 kg - for 450 mg, 50 kg and more-on 600 mg 1 once a day, every day or 3 times a week. The maximum daily dose - 600 mg. Children over 3 years and a newborn is 10-20 mg/kg/day, no more 450 mg / day. The duration of the course is 6-9-12 months or more.

Leprosy: inside, adults - 600 mg, Children - 10 mg / kg 1 once a month, in combination with dapsone and clofazimine, during 2 years or more.

Infections nontuberculous etiology: inside, adults-450-900 mg/day, children — 8-10 mg/kg/day in 2-3 reception. B /, 300-900 Mg / day for 7-10 days.

Brucellosis: inside, adults - 900 mg / day for 45 days (in combination with doxycycline).

Prevention of meningococcal meningitis: inside, every 12 no, adults - 600 mg, children — in one dose 10 mg / kg, the newborn is 5 mg / kg for 2 days.

Precautions.

When non-tuberculous diseases prescribed only after failure of other antibiotics (the rapid development of resistance). Patients with impaired renal function Dosage adjustment, if it exceeds 600 mg / day. To use caution in newborns, premature children (due to age immaturity of enzyme systems of the liver) and malnourished patients. Newborns should be administered simultaneously with vitamin K (prevention of bleeding). To use caution in HIV-infected patients, receiving HIV protease inhibitor. The on / in the introduction of rifampicin diabetics should enter 2 IU insulin per 4-5 g glucose (Solvent). If you have flu-like syndrome in intermittent regimen should be possible to move to a daily intake; At the same time, increase the dose gradually. When possible, move from / in the introduction to oral admission (the risk of phlebitis). During treatment should monitor blood count, the function of the kidneys and liver, first 1 once every 2 Sun, then monthly; possible supplementation or increased doses of glucocorticoids. In the case of prophylactic use in bacilli carrier Neisseria meningitidis must be strict medical supervision of the patient for early detection of disease symptoms (the development of resistant pathogens). Preparations Pasco, soderzhashtie bentonite (hydrous aluminum), It should be taken no earlier than, than 4 h after administration of rifampicin. During treatment should avoid alcohol (It increases the risk of hepatotoxicity).

Cautions.

Standing rifampicin better tolerated, than intermittent (2-3 Times a week). To prepare the solution for i / v infusion every 0,15 g is dissolved in 2,5 ml water for injection, vigorously shaken until complete dissolution and then mixed with 125 ml 5% glucose solution.

When applied in patients, unable to swallow the capsule whole, and children is acceptable capsule contents mixed with applesauce or jelly.

Urine stains, mud, sputum, lacrimal fluid, sweat, nasal secretion skin and orange-red. Can bravely painted soft contact lenses. During treatment should not be used microbiological methods for determining the concentration of folic acid and vitamin B₁₂ serum.

Cooperation