Paracetamol for children, 120mg/5ml suspension 100 g

Pharmacotherapeutic group: analgesic non-narcotic drug

ATX code: [N02BE01]

Pharmacological properties

Pharmacodynamics. Non-narcotic analgesic, has analgesic and antipyretic effects.

The drug blocks cyclooxygenase 1 and 2 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 lack of a significant anti-inflammatory effect. The drug has no adverse effect on water-salt metabolism and mucosa of the gastrointestinal tract.

Pharmacokinetics. Absorption is high, time to reach maximum concentration is 0.5-2 hours, maximum concentration is 5-20 µg/ml. Binding with plasma proteins is 15%. It penetrates through the blood-brain barrier. Less than 2% of the dose taken by a nursing mother penetrates into breast milk. Therapeutically effective plasma concentrations of paracetamol are achieved when administered at a dose of 10-15 mg/kg.

It is metabolized in liver: 80% reacts in conjugation with glucuronic acid and sulfates to form inactive metabolites, 17% reacts in hydroxylation to form 8 active metabolites, which conjugate with glutathione and then with cysteine and mercapturic acid to form inactive metabolites. The main cytochrome P450 isoenzymes for this metabolic pathway are CYP2E1 (predominantly), CYP1A2 and CYP3A4 (secondary role).

In glutathione deficiency, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. Additional metabolic pathways are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronic and sulfuric acids.

In adults, glucuronidation predominates; in newborns (including premature infants) and young children, sulfation predominates. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

The elimination half-life is 2-3 hours. Within 24 hours, 85-95% of paracetamol is excreted by the kidneys as glucuronides and sulfates, 3% – unchanged. In elderly patients the clearance of paracetamol is decreased and the elimination half-life is increased.

Indications

It is used for rapid relief of headache, including migraine pain, toothache, neuralgia, muscle and rheumatic pain, as well as algodysmenorrhea, pain from injuries, burns; to reduce fever in colds and the flu.

Active ingredient

Composition

Active ingredient:

Paracetamol 24 mg;

Associates:

sugar,

sorbitol,

citric acid,

How to take, the dosage

For children aged 3-12 months 2.5-5 ml syrup (60-120 mg of paracetamol).

For children aged 1-5 years – 5-10 ml syrup (120-240 mg of paracetamol).

For children aged 5-12 years – 10-20 ml syrup (240-480 mg of paracetamol).

Adults and children with body weight over 60 kg – 20-40 ml of syrup (480-960 mg of paracetamol).

The frequency of paracetamol syrup administration is 3-4 times a day.

Interaction

The drug when taken for a long time increases the effect of indirect anticoagulants (warfarin and other coumarins), which increases the risk of bleeding. Inducers of microsomal oxidation enzymes in the liver (barbiturates, diphenine, carbamazepine, rifampicin, zidovudine, phenytoin, ethanol, flumecinol, phenylbutazone and tricyclic antidepressants) increase the risk of hepatotoxic effects in overdose.

Long-term use of barbiturates reduces the effectiveness of paracetamol.

Ethanol promotes acute pancreatitis.

Microsomal oxidation inhibitors (cimetidine) reduce the risk of hepatotoxic effects. Concomitant use with other non-steroidal anti-inflammatory drugs increases the nephrotoxic effect.

The concomitant use of paracetamol in high doses and salicylates increases the risk of kidney and bladder cancer. Diflunisal increases the plasma concentration of paracetamol by 50% – risk of hepatotoxicity.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug. Metoclopramide and domperidone increase and cholestyramine decreases the absorption rate of paracetamol. The drug may decrease the activity of uricosuric drugs.

Special Instructions

Consult your doctor before you take this medicine:

to avoid anti-toxic liver damage, do not take paracetamol with alcoholic drinks, or with people who have a tendency to drink alcohol spirits chronically.

Peripheral blood count and liver function should be monitored during long-term treatment.

Contraindications

– Individual hypersensitivity to the components of the drug;

– diseases of the blood system;

– genetic absence of glucose-6-phosphate dehydrogenase;

– Sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;

– period of newborn (age less than 1 month).

With caution

– hepatic and renal failure;

– benign hyperbilirubinemia (including Gilbert syndrome);

– alcoholic liver damage, alcoholism;

– diabetes mellitus;

– pregnancy, lactation period;

– old age;

– early infant age (1 – 3 months).

Side effects

In the recommended doses, the drug is usually well tolerated. Paracetamol rarely causes side effects. Allergic reactions (skin rash, pruritus, urticaria, Quincke’s edema), erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), dizziness, nausea, epigastric pain; anemia, thrombocytopenia, agranulocytosis; insomnia may sometimes be observed. When prolonged use in high doses – increased likelihood of impairment of liver and kidney function, as well as hematopoietic system.

Digestive system disorders: nausea, epigastric pain, increased liver enzymes activity, hepatonecrosis. Endocrine system: hypoglycemia. If unusual symptoms occur, it is necessary to consult a doctor.

Overdose

The signs of paracetamol overdose are nausea, vomiting, stomach pain, pale skin, anorexia. After a day or two, signs of liver damage are determined. In severe cases liver failure and coma develop. Specific antidote in paracetamol poisoning is N-acetylcysteine.

Symptoms: pale skin, anorexia, nausea, vomiting; hepatonecrosis (severity of necrosis depends directly on the degree of overdose). If overdose is suspected, it is necessary to seek medical attention immediately.

The toxic effects of the drug in adults may be observed after taking more than 10-15 g of paracetamol: increase of “hepatic” transaminases activity, increase of prothrombin time (12-48 hours after intake); the full clinical picture of liver damage becomes apparent after 1-6 days. Rarely, liver dysfunction develops fulminantly and may be complicated by renal failure (tubular necrosis).

Treatment: the victim should undergo gastric lavage during the first 4 hours of poisoning, take adsorbents (activated charcoal) and consult a physician, the administration of SH-group donators and precursors of glutathione synthesis – methionine in 8-9 hours after overdose and N-acetylcysteine – in 12 hours. The need for additional therapeutic measures (further methionine administration, intravenous N-acetylcysteine administration) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Pregnancy use

Use with caution in pregnancy, breastfeeding and children under 3 months of age.

Similarities