Paracetamol-LekT - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Non-narcotic analgesic, blocks the structural enzyme (COX-1) and inducible enzyme (COX-2) mainly in the central nervous system, affecting the pain centers and thermoregulation.In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on the activity of cyclooxygenase (COX), which explains the almost complete absence of anti-inflammatory effect. Absence of blocking influence on the synthesis of prostaglandins (Pg) in peripheral tissues determines the absence of a negative influence on water-salt metabolism (retention of sodium and water ions) and mucous membrane of the gastrointestinal tract.

Pharmacokinetics:

The mechanism of analgesic effect of paracetamol is associated with the suppression of biosynthesis of prostaglandins. Inhibiting cyclooxygenase, it prevents the formation of mainly prostaglandins E2 and F₂, which play an important role in the perception of pain stimuli by nociceptors and the transmission of induced excitation to the central nervous system. Paracetamol more actively inhibits cyclooxygenase in the cells of the central nervous system, and is much weaker in peripheral tissues. The antipyretic effect of paracetamol is due to the inhibition of the biosynthesis of prostaglandins, directly in the hypothalamus, in particular the prostaglandins Ej and E₂, which are mediators of the thermoregulatory center.Pharmacokinetics Paracetamol is characterized by rapid and complete absorption from the gastrointestinal tract, a uniform distribution in tissues, a relatively short half-life.

The maximum concentration in the plasma is usually formed 30-60 minutes after ingestion. Detected for 5 hours after a single dose. The bioavailability of the drug is very high, approaching 90%. The degree of binding to proteins is 25-50%. Metabolized Paracetamol (up to 80%) by microsomal enzymes of the liver by conjugation with the formation of glucuronides and sulfates, only 3 % is excreted by the kidneys in an unchanged form.

Indications:

Feverish syndrome on the background of infectious diseases; pain syndrome (mild to moderate): arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea.

Contraindications:

Hypersensitivity to the components of the drug, children's age (up to 3 years).

Carefully:

Renal and hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, alcoholic liver damage, alcoholism, pregnancy, lactation, elderly age.

Pregnancy and lactation:

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

The use of paracetamol during pregnancy and during breastfeeding is not contraindicated, but if necessary, the expected benefit of therapy for the mother and the potential risk to the fetus or the child should be carefully weighed.

You should also consult your doctor!

Dosing and Administration:

Inside, with a lot of liquid, 1-2 hours after eating (taking immediately after a meal leads to a delay in the onset of action). Adults and adolescents older than 12 years (body weight over 40 kg) single dose - 500 mg; the maximum single dose is 1000 mg. Multiplicity of destination - up to 4 times a day. The maximum daily dose is 4000 mg.

For children, depending on age: the maximum single dose of 10-15 mg / kg, the maximum daily dose - up to 60 mg / kg.

The maximum daily dose for children older than 3-6 years is 1000 mg, 6-9 years - 1500 mg, 9-12 years - 2000 mg. Multiplicity of destination - 3-4 times a day. The interval between each reception is at least 4 hours.

The maximum duration of treatment without consulting a doctor is 3 days (when taken as an antipyretic drug) and 5 days (as analgesic).

Side effects:

Allergic reactions (including skin rash).

Rarely - hematopoiesis.

Overdose:

Overdose Paracetamol: acute overdose develops 6-14 hours after admission, chronic - after 2-4 days.

Symptoms of acute overdose: diarrhea, decreased appetite.

Symptoms of chronic overdose: cerebral edema,

hypocoagulation, the development of the syndrome of disseminated intravascular coagulation, hypoglycemia, metabolic acidosis, arrhythmia, collapse, rarely a violation of liver function develops with lightning speed and can be complicated by renal failure (renal tubular necrosis), prolonged use of the drug in large doses.

Treatment: introduction of donators SH-groups and precursors of glutathione synthesis - methionine and acetylcysteine must be administered within 8-9 and 12 hours, respectively. The need for additional therapeutic measures (further introduction of methionine, iv injection of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction:

Reduces the effectiveness of uricosuric medicines. The concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (a decrease in the synthesis of procoagulant factors in the liver).

Inductors of microsomal liver enzymes (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication even with a slight overdose. Long-term use of barbiturates reduces the effectiveness of paracetamol.

Ethanol promotes the development of acute pancreatitis.

Inhibitors of microsomal liver enzymes (incl. cimetidine) reduce the risk of hepatotoxic effects.

Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer.Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

With continued febrile syndrome in the presence of paracetamol for more than 3 days and pain syndrome for more than 5 days, a doctor's consultation is required.

The risk of liver damage increases in patients with alcoholic liver disease.

Distorts the indicators of laboratory studies in the quantitative determination of glucose and uric acid in plasma.

During long-term treatment, monitoring of the peripheral blood pattern and the functional state of the liver is necessary.

Simultaneous reception with ethanol is not recommended.

Effect on the ability to drive transp. cf. and fur:

Patients who administer vehicles are advised to use the drug with extreme caution.

Form release / dosage:Tablets 200 mg or 500 mg.

Packaging:

10 tablets per contour cell pack.

For 10 tablets in a contour non-jawed package.

For 1, 2, 5 contour mesh or contour non-jawed packages with instructions for use are placed in a bundle.

It is allowed to place contour non-cellular packages in a group package with the appropriate number of instructions for use.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-001777

Date of registration:19.07.2012

The owner of the registration certificate:Tyumen Chemical - Pharmaceutical Plant, OJSC Tyumen Chemical - Pharmaceutical Plant, OJSC Russia

Manufacturer: & nbsp

Tyumen Chemical - Pharmaceutical Plant, OJSC Russia

Information update date: & nbsp02.10.2015

Illustrated instructions

Instructions

Paracetamol-Lect (Paracetamol-LekT)