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

Non-narcotic analgesic, blocks activity of both cyclooxygenase isoforms COX1 and COX2 predominantly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of anti-inflammatory effect.The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (retention of sodium and water ions) and the mucous membrane of the gastrointestinal tract.

Pharmacokinetics:

Absorption is high, the time to reach the maximum concentration (TCmax) is 0.5-2 h; the maximum concentration (Cmax) is 5-20 μg / ml. Connection with plasma proteins - 15%.

Penetrates through the blood-brain barrier. Less than 1% of accepted lactating mother dose of paracetamol penetrates into the breast milk.

Metabolized in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation with microsomal enzymes of the liver. AT In the latter case, toxic intermediate metabolites are formed which subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for a given pathway of metabolism is isoenzyme CYP2E1 (predominantly), CYP1A2 and CYP3A4 (secondary role). With a deficiency of glutathione, these metabolites can cause damage and necrosis hepatocytes. Additional ways metabolism are the hydroxylation of up to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which subsequently conjugated to glucuronides or sulfates.

In adults, glucuronation predominates, in newborns (including premature) and small children - sulfation. Conjugated metabolites paracetamol (glucuronides, sulfates and conjugates with glutathione) have a low pharmacological (including toxic) activity.

The half-life (T1 / 2) is 1-4 hours. It is excreted by the kidneys in the form of metabolites, predominantly conjugates, only 3% unchanged. In elderly patients the clearance of the drug decreases and T1 / 2 increases.

Indications:

Moderate or mild pain syndrome (headache, toothache, migraine, arthralgia, neuralgia, myalgia), algodismenorea.

Feverish syndrome on the background of infectious diseases.

Contraindications:

Hypersensitivity to paracetamol.

Children up to 8 years.

Carefully:

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

Pregnancy and lactation:The drug should be used only if the expected benefit to the mother exceeds the possible risk to the fetus and the baby.

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 over 12 years (body weight more than 40 kg) single dose - 500 mg; the maximum single dose - 1 g. The frequency of admission - up to 4 times a day. The maximum daily dose is 4 g.

In patients with impaired liver or kidney function, with Gilbert syndrome, in elderly patients the daily dose should be reduced (the interval between doses is increased).

Children: the maximum daily dose for children 8-9 years (before 30 kg) - 1.5 g, 9-12 years (up to 40 kg) - 2 g. The frequency of admission - 4 times a day; interval between eachReception - not less than 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 (rash, itching, angioedema, hives), rarely disorders of hematopoiesis (anemia, thrombocytopenia, methemoglobinemia).

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:Symptoms: during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, abdominal pain; metabolic disorder of glucose acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose hepatic insufficiency with progressive encephalopathy, coma, death, acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis.

With prolonged admission in high doses may be hepatotoxic and nephrotoxic action (renal colic, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia).

Hepatotoxic effect in adults is manifested when taking 10 g or more

Treatment: introduction of donators SHgroups andof fusion glutathione - methionine for 8-9 hours after an overdose and acetylcysteine for 8 hours.

The need for additional therapeutic measures (further introduction of methionine, intravenous injection of acetylcysteine) is determined in 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 of sedimentation).

Inductors of microsomal enzymes in the liver (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 Barbiturates reduce the effectiveness of paracetamol.

Ethanol promotes the development of acute pancreatitis.

Inhibitors of microsomal oxidation (including 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 use of paracetamol in high doses and sapicylates increases the risk of developing kidney or bladder cancer.

Diflunisal increases the plasma concentration of paracetamol by 50%; risk of hepatotoxicity.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

With the ongoing febrile syndrome in the background of the use of paracetamol more than 3 days and a painful syndrome more than 5 days, consultation of the doctor is required.

Use with caution in patients with impaired liver or kidney function.

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.

To avoid toxic damage to the liver paracetamol should not be combined with reception of alcoholic beverages, and also to receive persons prone to chronic alcohol consumption. The risk of liver damage increases in patients with alcoholic hepatosis.

Effect on the ability to drive transp. cf. and fur:Data on the effect on the ability to drive vehicles and perform work that requires concentration and speed of psychomotor reactions is not.

Form release / dosage:Tablets, 500 mg.

Packaging:For 10 tablets in a contour non-cellular package of paper with a polymer coating.

For 10 tablets in a contour mesh package made of a polyvinylchloride film and aluminum foil or paper with a polymeric coating.

By 10,20,25,30,40,50,60 tablets in cans of polymeric.

1, 2, 3, 4, 5 contour non-jammed packages or contour mesh packages together with the instruction for use are placed in a bundle.

Banks polymer, or contour non-cellular packages, or contoured cells with an equal number of instructions for use are placed in a bag of plastic film or a box of cardboard.

Storage conditions:

In dry, 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 the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:P N002526 / 01

Date of registration:22.07.2008

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Paracetamol-UBF (Paracetamol-UBF)