Paracetamol oral solution 25mg / ml, 100ml

Used in children from 3 months to 12 years old as:

Х antipyretic agent - to reduce fever against the background of colds, flu and childhood infectious diseases (including chickenpox, mumps, measles, rubella, scarlet fever);

Х anesthetic - for toothache, including teething, headache, ear pain, otitis media and sore throat.

For children of the 2nd - 3rd month of life, a single dose is possible to lower the temperature after vaccination.

If the temperature does not decrease, a doctor's consultation is necessary.

Inside, in adults and adolescents weighing more than 60 kg, it is used in a single dose of 500 mg, the frequency of administration is up to 4 times / day.

The maximum duration of treatment is 5-7 days.

Maximum doses: single - 1 g, daily - 4 g.

Single doses for oral administration 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.

1 ml of oral solution contains:

active substance: paracetamol - 25.0 mg;

auxiliary substances: sucrose - 300.0 mg, propylene glycol - 400.0 mg, methyl parahydroxybenzoate - 0.8 mg, citric acid - 0.1 mg, vanillin - 1.0 mg, purified water - up to 1.0 ml.

• Chronic alcoholism;

• hypersensitivity to paracetamol;

• age less than 2 months;

• severe impairment of liver and kidney function;

Pharmachologic effect:

Analgesic antipyretic. It has analgesic, antipyretic and weak anti-inflammatory effects.

The mechanism of action is associated with inhibition of the synthesis of prostaglandins, a predominant effect on the center of thermoregulation 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, C max in blood plasma is reached after 10-60 minutes and is about 6 ?g / ml, then gradually decreases and after 6 hours is 11-12 ?g / 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 slightly increases with overdose.

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

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

A negatively acting hydroxylated metabolite, N-acetyl-p-benzoquinone imine, 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 heat up with paracetamol overdose and cause tissue damage.

In adults, most of paracetamol binds to glucuronic acid and to a lesser extent to sulfuric acid.

These conjugated metabolites have no 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 higher.

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.

Clinical pharmacology:

Analgesic antipyretic

Application during pregnancy and children:

Paracetamol crosses the placental barrier.

To date, no negative effects of paracetamol on the fetus in humans have been noted.

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 benefits of therapy for the mother and the potential risk to the fetus or child should be carefully weighed.

In experimental studies, the embryotoxic, teratogenic and mutagenic effects of paracetamol have not been established.

Application in children:

Application is possible according to the dosage regimen.

Side effects:

On the part of 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, itching, urticaria.

Drug interactions:

With simultaneous use with inducers of liver microsomal enzymes, agents with hepatotoxic action, there is a risk of increased hepatotoxic action of paracetamol.

With simultaneous use with anticoagulants, a slight or moderate increase in prothrombin time is possible.

With simultaneous use with anticholinergics, it is possible to reduce the absorption of paracetamol.

With simultaneous use with oral contraceptives, the excretion of paracetamol from the body is accelerated and its analgesic effect may decrease.

When used simultaneously with uricosuric agents, their effectiveness decreases.

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

With simultaneous use with diazepam, it is possible to reduce the excretion of diazepam.

There are reports of the possibility of enhancing the myelodepressant effect of zidovudine when used simultaneously with paracetamol.

A case of severe toxic liver damage is described.

Cases of manifestations of the toxic effect of paracetamol with simultaneous use with isoniazid are described.

With simultaneous use with carbamazepine, phenytoin, phenobarbital, primidone, the effectiveness of paracetamol decreases, which is due to an increase in its metabolism (glucuronization and oxidation processes) and excretion from the body.

Cases of hepatotoxicity with the simultaneous use of paracetamol and phenobarbital have been described.

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

With simultaneous use with lamotrigine, the excretion of lamotrigine from the body is moderately increased.

With simultaneous use with metoclopramide, it is possible to increase the absorption of paracetamol and increase its concentration in the blood plasma.

With simultaneous use with probenecid, it is possible to reduce the clearance of paracetamol; with rifampicin, sulfinpyrazone - it is possible to increase the clearance of paracetamol due to an increase in its metabolism in the liver.

With simultaneous use with ethinyl estradiol, the absorption of paracetamol from the intestine increases.

Dosage:

Inside, in adults and adolescents weighing more than 60 kg, it is used in a single dose of 500 mg, the frequency of administration is up to 4 times / day.

The maximum duration of treatment is 5-7 days.

Maximum doses: single - 1 g, daily - 4 g.

Single doses for oral administration 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.

Precautions:

Use 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 control the picture of peripheral blood and the functional state of the liver.