Pyrazinamidum

General characteristics. Structure:

Active ingredient: 500,0 mg of Pyrazinamidum.

Excipients: potato starch, gelatin, sodium carboxymethylstarch (примогель), silicon dioxide colloid (aerosil A 300 brand), magnesium stearate.

The synthetic antituberculous remedy having active bacteriostatic and bactericidal action.

Pharmacological properties:

Pharmacodynamics. Antitubercular, antibacterial drug. Affects intracellularly located mycobacteria, well gets into the centers of tubercular defeat. Its activity does not decrease in acid medium of caseous masses, in communication with what it is appointed at caseous and necrotic processes, caseous lymphadenites, tuberkuloma. Depending on a dose renders bactericidal or bacteriostatic effect. During treatment by one Pyrazinamidum resistance development is possible, the probability decreases at a combination to other antitubercular drugs.

Pharmacokinetics. It is quickly and completely soaked up in a GIT. In plasma contacts proteins for 10-20%. Cmax is reached in 1-2 h. Well gets into fabrics and bodies, including through a blood-brain barrier. It is metabolized in a liver, at the same time the intermediate active metabolite having mikobakteriostatichesky activity is formed. Biological half-life makes 8-9 hours. It is removed by kidneys: in not changed look — 3%, in the form of pirazinoyevy acid — 33%, in the form of other metabolites — 36%.

Indications to use:

Tuberculosis (all forms and localizations) of adults and children, as a part of a combination therapy.

Route of administration and doses:

Inside, in time or after food, once a day, it is more preferable during a breakfast with a small amount of water, in a daily dose of 20-30 mg/kg. About 90 mg/kg once a week, or on 2-2.5 g 3 times a week, or on 3-3.5 g 2 times a week can be appointed. The maximum daily dose — 2.5 g. A course of treatment — 3 months and more. In case of unsatisfactory portability drug is appointed in 2-3 receptions. At persons of advanced and senile age the daily dose should not exceed 15 mg/kg. In these cases it is reasonable to appoint drug every other day. To children — on 15-20 mg/kg once a day; the maximum daily dose — 1.5 g.

Features of use:

At prolonged treatment it is necessary to control activity of ALT, nuclear heating plant and concentration of uric acid in blood once a month.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, abnormal liver function (anorexia, morbidity of a liver, hepatomegalia, jaundice, yellow atrophy), aggravation of a round ulcer.

From TsNS: dizziness, headache, sleep disorders, hyperexcitability, depressions; in some cases — hallucinations, spasms, confusion of consciousness.

From bodies of a hemopoiesis and system of a hemostasis: thrombocytopenia, sideroblastny anemia, vacuolation of erythrocytes, porphyria, hypercoagulation, splenomegaly.

From an urinary system: dysuria, intersticial nephrite. A delay in an organism of uric acid and emergence in joints of pains of gouty character. Allergic reactions: skin rash, small tortoiseshell.

Interaction with other medicines:

Let's combine with all antitubercular drugs, except PASK. Strengthens antitubercular action of an ofloksatsin and lomefloksatsin. At chronic destructive forms Pyrazinamidum is recommended to be combined with rifampicin or Ethambutolum (portability is better, than at a combination to rifampicin, but the effect is weaker). Reduces efficiency of antigouty means.

Contraindications:

Liver diseases, hyperuricemia, gout, hypersensitivity. At pregnancy it is appointed only in emergency.

Overdose:

Symptoms: an abnormal liver function, strengthening of expressiveness of side effects from TsNS. Treatment: symptomatic.

Storage conditions:

List B. At a temperature not over 30 ºС in the places not available to children.

Issue conditions:

According to the recipe

Packaging:

On 100 tablets weighing 500 mg in a plastic jar.