Paracetamol suspension for oral use Strawberry 120mg/5ml, 100g

Composition

Active ingredient:  

paracetamol 24 mg;

Auxiliary substances:  

sugar,

sorbitol,

citric acid,

three-substituted sodium citric acid,

propylene glycol,

ethyl alcohol,

riboflavin,

aromatic additives,

sodium benzoate,

water.

Pharmacological action

Pharmacotherapeutic group: non-narcotic analgesic agent

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 absence of a significant anti-inflammatory effect. The drug does not adversely affect the water-salt metabolism and the mucous membrane of the gastrointestinal tract.

Pharmacokinetics. Absorption is high, the time to reach the maximum concentration is 0.5-2 hours, the maximum concentration is 5-20 mcg / ml. Binding to plasma proteins -15%. Penetrates the blood-brain barrier. Less than 2% of

the dose of the drug taken by a nursing mother passes into breast milk. A therapeutically effective plasma concentration of paracetamol is achieved when it is administered at a dose of 10-15 mg / kg. It is metabolized in the liver: 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites,17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione, and then with cysteine and mercapturic acid and form inactive metabolites. The main cytochrome P 450 isoenzymes for this pathway of metabolism are CYP2E1 (mainly), CYP1A2 and CYP3A4 (secondary role). When glutathione is deficient, 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 acid and sulfuric acid.

In adults, glucuronidation prevails, in newborns (including premature babies) and young children – sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates, and glutathione conjugates) 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 in the form of glucuronides and sulfates,3% – unchanged. In elderly patients, the clearance of paracetamol decreases and the elimination half-life increases.

Indications

It is used to quickly relieve headaches, including migraine pain, toothache, neuralgia, muscle and rheumatic pain, as well as for algodismenorrhea, pain from injuries, burns; to reduce fever in colds and flu.

Use during pregnancy and lactation

Use with caution during pregnancy, lactation and children under 3 months of age.

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;

– neonatal period (up to 1 month of age).

With caution

– hepatic and renal insufficiency;

– benign hyperbilirubinemia (including Gilbert’s syndrome);

– alcoholic liver damage, alcoholism;

– diabetes mellitus;

– pregnancy, lactation;

– the elderly;

– early infancy (1-3 months).

Side effects

At the recommended doses, the drug is usually well tolerated. Paracetamol rarely causes side effects. Sometimes allergic reactions (skin rash, pruritus, urticaria, Quincke’s edema), erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), dizziness, nausea, epigastric pain; anemia, thrombocytopenia, agranulocytosis; insomnia may occur. Long-term use in large doses increases the likelihood of impaired liver and kidney function, as well as the hematopoietic system.

From the digestive system:  nausea, epigastric pain, increased activity of liver enzymes, hepatonecrosis. Endocrine system disorders: hypoglycemia. If you experience unusual symptoms, you should consult a doctor.

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 overdoses.

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

Ethanol contributes to the development of acute pancreatitis.

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

Concomitant long-term use of high-dose paracetamol and salicylates increases the risk of kidney and bladder cancer. Diflunisal increases the plasma concentration of paracetamol by 50% – the risk of developing hepatotoxicity.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. Metoclopramide and domperidone increase, and cholestyramine reduces the rate of absorption of paracetamol. The drug may reduce the activity of uricosuric drugs.

How to take, course of use and dosage

For children aged 3 to 12 months,2.5-5 ml of syrup (60-120 mg of paracetamol). For children from 1 year to 5 years – 5-10 ml of syrup (120-240 mg of paracetamol). For children aged 5-12 years – 10-20 ml of syrup (240-480 mg of paracetamol). Adults and children weighing more than 60 kg – 20-40 ml of syrup (480-960 mg of paracetamol). The frequency of taking paracetamol syrup is 3-4 times a day.

Overdose

Signs of paracetamol overdose include nausea, vomiting, stomach pain, pallor of the skin, and anorexia. After a day or two, signs of liver damage are detected. In severe cases, liver failure and a comatose state develop. A specific antidote for paracetamol poisoning is N-acetylcysteine.

Symptoms:  pallor of the skin, anorexia, nausea, vomiting; hepatonecrosis (the severity of necrosis directly depends on the degree of overdose). If an overdose is suspected, seek immediate medical attention. The toxic effect of the drug in adults is possible after taking more than 10-15 g of paracetamol: an increase in the activity of “liver” transaminases, an increase in prothrombin time (12-48 hours after use); a detailed clinical picture of liver damage is manifested in 1-6 days. Rarely, liver dysfunction develops rapidly and can be complicated by renal failure (tubular necrosis).

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

Special instructions

Please consult your doctor before taking this medicine if: :

• You have severe liver or kidney disease.
• You are taking anti-nausea and vomiting medications (metoclopramide, domperidone), as well as cholesterol-lowering medications (cholestyramine).
• You are taking anticoagulants and need painkillers every day for an extended period of time. Paracetamol in this case can be taken occasionally;

IN ORDER TO AVOID TOXIC LIVER DAMAGE, PARACETAMOL SHOULD NOT BE COMBINED WITH THE INTAKE OF ALCOHOLIC BEVERAGES, AS WELL AS TAKEN BY PEOPLE WHO ARE PRONE TO CHRONIC ALCOHOL CONSUMPTION.

During long-term treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver.

Form of production

syrup

Storage conditions

Store in a dry place, protected from light and out of reach of children, at a temperature not exceeding + 25 ° C.

Shelf life

3 years

Active ingredient

Paracetamol

Dosage form

Oral suspension