Paracetamol, tablets 500 mg 20 pcs

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

Pharmacokinetics

After oral administration, paracetamol is rapidly absorbed from the gastrointestinal tract, mainly in the small intestine, mainly by passive transport. After a single dose of 500 mg, the C_max in plasma is reached after 10-60 min and is about 6 µg/ml, then gradually decreases and is 11-12 µg/ml after 6 h.

Widely distributed in tissues and mainly in the fluid media of the body, with the exception of adipose tissue and cerebrospinal fluid.

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

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

The hydroxylated metabolite with negative effects, N-acetyl-p-benzoquinonimine, 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 paracetamol overdose 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 h. In patients with cirrhosis, the T_1/2 is slightly longer. Renal clearance of paracetamol is 5%.

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

Indications

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

Pharmacological effect

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

Pharmacokinetics

After oral administration, 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 after 10-60 minutes and is about 6 mcg/ml, then gradually decreases and after 6 hours it is 11-12 mcg/ml.

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. Sulfate and glucuronide metabolites do not bind to plasma proteins even at relatively high concentrations.

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

A hydroxylated metabolite with a negative effect, N-acetyl-p-benzoquinoneimine, which is formed in very small quantities in the liver and kidneys under the influence of mixed oxidases and is usually detoxified by binding to glutathione, can accumulate during an overdose of paracetamol and cause tissue damage.

In adults, most paracetamol is bound to glucuronic acid and to a lesser extent to sulfuric acid. These conjugated metabolites do not have biological activity. In premature babies, newborns and in the first year of life, the sulfate metabolite predominates.

T1/2 is 1-3 hours. In patients with liver cirrhosis, T1/2 is slightly longer. 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.

Special instructions

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

With long-term use of paracetamol, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

Active ingredient

Paracetamol

Composition

For one tablet

active substance: paracetamol – 500 mg;

excipients:

potato starch,

croscarmellose sodium (croscarmellose sodium),

povidone (low molecular weight medical polyvinylpyrrolidone),

stearic acid,

talc.

Pregnancy

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

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), you should carefully weigh the expected benefits of therapy for the mother and the potential risk to the fetus or child.

Experimental studies have not established the embryotoxic, teratogenic and mutagenic effects of paracetamol.

Contraindications

Chronic alcoholism, hypersensitivity to paracetamol.

Side Effects

From the digestive system: rarely – dyspeptic symptoms, with long-term use in high doses – hepatotoxic effect.

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

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

Interaction

When used simultaneously with inducers of microsomal liver enzymes and agents with hepatotoxic effects, there is a risk of increasing the hepatotoxic effect of paracetamol.

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

When used simultaneously with anticholinergic drugs, the absorption of paracetamol may be reduced.

When used simultaneously with oral contraceptives, the elimination of paracetamol from the body is accelerated and its analgesic effect may be reduced.

When used simultaneously with uricosuric drugs, their effectiveness decreases.

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

When used simultaneously with diazepam, the excretion of diazepam may be reduced.

There are reports of the possibility of enhancing the myelosuppressive effect of zidovudine when used simultaneously with paracetamol. A case of severe toxic liver damage has been described.

Cases of toxic effects of paracetamol have been described when used simultaneously with isoniazid.

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

When using cholestyramine for a period of less than 1 hour after taking paracetamol, the absorption of the latter may be reduced.

When used simultaneously with lamotrigine, the excretion of lamotrigine from the body moderately increases.

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

When used simultaneously with probenecid, the clearance of paracetamol may be reduced; with rifampicin, sulfinpyrazone – it is possible to increase the clearance of paracetamol due to an increase in its metabolism in the liver.

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

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf life

4 years. Do not use after the expiration date indicated on the package.

Manufacturer

Ozon, Russia