Paracetamol pills 500mg, 20pcs – Ozon

Composition

of 1 tab. : paracetamol 500 mg

Pharmacological action

Analgesic-antipyretic. It has analgesic, antipyretic and weak anti-inflammatory effects. The mechanism of action is associated with inhibition of prostaglandin synthesis, a predominant effect on the center of thermoregulation in the hypothalamus.

Pharmacokinetics

After oral use, paracetamol is rapidly absorbed from the gastrointestinal tract, mainly in the small intestine, mainly by passive transport. After a single dose of 500 mg_{, cmax} in blood plasma is reached in 10-60 minutes and is about 6 mcg / ml, then gradually decreases and after 6 hours is 11-12 mcg/ml.

It is widely distributed in tissues and mainly in body fluids, with the exception of adipose tissue and cerebrospinal fluid.

Protein binding is less than 10% and increases slightly with overdose. The sulfate and glucuronide metabolites do not bind to plasma proteins even in relatively high concentrations.

Paracetamol is mainly metabolized in the liver by conjugation with glucuronide, conjugation with sulfate, and oxidation with the participation of mixed liver oxidases and cytochrome P450.

The hydroxylated negative metabolite N-acetyl-p-benzoquinonymine, which is formed in very small amounts in the liver and kidneys under the influence of mixed oxidases and is usually detoxified by binding to glutathione, can accumulate in an overdose of paracetamol and cause tissue damage.

In adults, most paracetamol binds to glucuronic acid and to a lesser extent to sulfuric acid. These conjugated metabolites have no biological activity. In premature infants, newborns, and in the first year of life, the sulfate metabolite predominates.

T_1/2 is 1-3 hours. In patients with cirrhosis of the liver, T_1/2 is slightly larger. The renal clearance of paracetamol is 5%.

It is excreted in the urine mainly in the form of glucuronide and sulfate conjugates. Less than 5% is excreted as unchanged paracetamol.

Indications

Pain syndrome of mild and moderate intensity of various genesis (including headache, migraine, toothache, neuralgia, myalgia, algodismenorrhea; pain from injuries, burns). Fever in infectious and inflammatory diseases.

Use during pregnancy and lactation

Paracetamol penetrates the placental barrier. To date, no negative effects of paracetamol on the fetus in humans have been observed.

Paracetamol is excreted in breast milk: the content in milk is 0.04-0.23% of the dose taken by the mother.

If it is necessary to use paracetamol during pregnancy and lactation (breastfeeding), the expected benefit of therapy for the mother and the potential risk to the fetus or child should be carefully weighed.

The embryotoxic, teratogenic, and mutagenic effects of paracetamol have not been established in experimental studies.

Contraindications

Chronic alcoholism, hypersensitivity to paracetamol.

Side effects

From the digestive system:  rarely-dyspeptic phenomena, with prolonged use in high doses – hepatotoxic effect.

From the hematopoietic system:  rarely-thrombocytopenia, leukopenia, pancytopenia, neutropenia, agranulocytosis.

Allergic reactions:  rarely – skin rash, pruritus, urticaria.

Interaction

When used concomitantly with inducers of microsomal liver enzymes, drugs that have a hepatotoxic effect, there is a risk of increasing the hepatotoxic effect of paracetamol.

When used concomitantly with anticoagulants, a slight or moderate increase in prothrombin time is possible.

When used concomitantly with anticholinergic agents, it is possible to reduce the absorption of paracetamol.

When used concomitantly with oral contraceptives, the elimination of paracetamol from the body accelerates and its analgesic effect may decrease.

When used concomitantly with uricosuric agents, their effectiveness decreases.

With the simultaneous use of activated carbon, the bioavailability of paracetamol decreases.

When used concomitantly with diazepam, it is possible to reduce the excretion of diazepam.

There are reports of the possibility of enhancing the myelodepressive effect of zidovudine when used concomitantly with paracetamol. A case of severe toxic liver damage is described.

Cases of toxic effects of paracetamol when used concomitantly with isoniazid are described.

When used concomitantly with carbamazepine, phenytoin, phenobarbital, primidone, the effectiveness of paracetamol decreases, which is due to an increase in its metabolism (processes of glucuronidation and oxidation) and excretion from the body. Cases of hepatotoxicity with concomitant use of paracetamol and phenobarbital have been described.

When using colestyramine for a period of less than 1 hour after taking paracetamol, it is possible to reduce the absorption of the latter.

When used concomitantly with lamotrigine, the elimination of lamotrigine from the body is moderately increased.

When used concomitantly with metoclopramide, it is possible to increase the absorption of paracetamol and increase its concentration in blood plasma.

When used concomitantly with probenecid, paracetamol clearance may decrease; with rifampicin, sulfinpyrazone, paracetamol clearance may increase due to an increase in its metabolism in the liver.

When used concomitantly with ethinyl estradiol, the absorption of paracetamol from the intestine increases.

How to take, course of use and dosage

Inside or rectally in adults and adolescents with a body weight of more than 60 kg, a single dose of 500 mg is used, the frequency of use is up to 4 times/day. The maximum duration of treatment is 5-7 days.

Maximum doses:  one – time-1 g, daily-4 g.

Single oral doses for children aged 6-12 years – 250-500 mg,1-5 years-120-250 mg, from 3 months to 1 year-60-120 mg, up to 3 months-10 mg/kg. Single doses for rectal use in children aged 6-12 years – 250-500 mg,1-5 years-125-250 mg.

The frequency of application is 4 times / day with an interval of at least 4 hours. The maximum duration of treatment is 3 days.

Maximum dose:  4 single doses per day.

Special instructions

It is used with caution in patients with impaired liver and kidney function, with benign hyperbilirubinemia, as well as in elderly patients.

With prolonged use of paracetamol, it is necessary to monitor the picture of peripheral blood and the functional state of the liver.

Active ingredient

Paracetamol

Dosage form

Tablets

Description

Pregnant women as prescribed by a doctor, Children over 6 years of age, Nursing mothers as prescribed by a doctor, For adults

Indications

Myositis, Osteoarthritis, Neuritis, Migraines, Burns, Sciatica, Flu, Colds, Infectious Diseases, Sciatica, Otitis Media, Osteoarthritis and Arthritis