Index of drugs

Fever, in the course of colds and flu-like conditions. Headaches. Muscle, bone and joint pain of various origins. Menstrual cramps. Pain after surgical and dental procedures. Pain associated with teething in children (applies to the preparation in doses of 125 mg and 250 mg).

1 suppository contains 125 mg, 250 mg or 500 mg of paracetamol.

Paracetamol has an analgesic and antipyretic effect as well as a low anti-inflammatory activity. It is an active metabolite of phenacetin with much lower toxicity. Paracetamol by inhibiting arachidonic acid cyclooxygenase, inhibits the synthesis of prostaglandins in the central nervous system (o.u.n.). It reduces the sensitivity o.u.n. for kinin and serotonin, which increases the pain threshold. The reduction in the concentration of prostaglandins in the hypothalamus is responsible for the antipyretic effect. Paracetamol does not affect platelet aggregation. After rectal administration, the bioavailability of paracetamol is lower, determined to be about 2/3 after oral administration. The time necessary to achieve the therapeutic concentration for suppositories is 120-240 min, which means that the analgesic effect appears 2-4 hours after application. Bioavailability and the rate of absorption of paracetamol in the form of suppositories depends on many factors: the dose of the drug, the size of the suppository (the lower the dose and its size, the greater the bioavailability), the type of substrate (the greater the lipophilicity of the substrate the greater the bioavailability and faster effect, but shorter duration of action) and the degree of rectal vascularization. Paracetamol binds to 25-50% of blood proteins. It passes through the placenta as well as into breast milk of women who are breastfeeding, T_0,5 in milk it is 1.35-3.5 h. Metabolism takes place in the liver, where as a result of conjugation with glucuronic acid (on average about 60%) and sulfuric acid (about 35%), non-toxic metabolites are formed. The remaining amount of Paracetamol, with the participation of cytochrome P450 isoenzymes (mainly 1A2, 2E1, 3A) is transformed into the hepatotoxic metabolite - N-acetyl-p-benzoquinone. This metabolite detoxifies as a result of hepatic glutathione. Paracetamol, in the form of inactive metabolites, is excreted mainly via the kidneys and (to a lesser extent) with bile.

Hypersensitivity to the active substance or any of the preparation's originals. Severe hepatic or renal failure. Viral hepatitis. Alcoholic disease.

Because of the risk of overdose before use, check that other medicines do not contain paracetamol. During the use of the drug should not drink alcohol because of the risk of toxic liver damage. There is a special risk of liver damage in people who are starved and regularly consuming alcohol. Paracetamol should be used with caution in patients allergic to Acetylsalicylic acid (less than 5% of patients sensitized to acetylsalicylic acid also exhibits signs of hypersensitivity to paracetamol), in patients with renal or hepatic impairment. Paracetamol may cause haemolysis in people who are deficient in glucose-6-phosphate dehydrogenase.

Paracetamol crosses the placenta; in previous studies, no adverse effects of paracetamol (at the recommended doses) on the fetus were found. Paracetamol is excreted in breast milk in small amounts. Paracetamol can be used during pregnancy and breastfeeding in case of extreme necessity.

The following may occur: pruritus, urticaria, rash and erythema, angioneurotic edema, dyspnea, sweating, low blood pressure, up to shock symptoms, asthma attack; granulocytopenia, arganulocytosis, thrombocytopenia, methemoglobinemia; nausea, vomiting, symptoms of liver damage; renal colic, renal papillary necrosis, acute renal failure.

Rectally. Children from 3 months to 1 year: 10 mg / kg at intervals of not less than 6 hours. Children from 1 to 6 years: 125 mg - 250 mg paracetamol (1 suppository 125 mg, 2 suppositories 125 mg or 1 suppository 250 mg).The maximum daily dose of paracetamol for children is 65 mg / kg. Children from 7 to 12 years: 1 suppository (250 mg paracatamol) up to 4 times, not more often than every 4 hours. Adults and children> 12 years: 1 suppository (500 mg paracetamol) 4-6 times a day, not more often than 4 h. The maximum daily dose of paracetamol for adults is 4 g.