Clinical and pharmacological group: & nbsp
Anilides
Included in the formulation
АТХ:N.02.B.E Anilides
N.02.B.E.51 Paracetamol in combination with other drugs, excluding psycholeptics
Pharmacodynamics:Combined drug.
Has analgesic, antipyretic, antihistamine, vasoconstrictive, sedative, bronchodilator and antitussive action.
Paracetamol
Has antipyretic, analgesic and anti-inflammatory effect. Inhibits cyclooxygenase, mainly in the central nervous system, affects the centers of pain and thermoregulation. It does not have a negative effect on water-salt metabolism and mucous membranes of the gastrointestinal tract, and therefore has little effect on the synthesis of prostaglandins in peripheral tissues.
Chlorphenamine
Block H1-receptor has antihistamine, antiserotonin, anticholinergic, sedative effect. Narrows the vessels of the nasal cavity, depresses the symptoms of allergic rhinitis: rhinorrhea, sneezing, itching of the nose and eyes.
Pharmacokinetics:Paracetamol
After oral administration, it is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 20-30 minutes. The connection with plasma proteins is 15%.Penetrates through the blood-brain barrier, enters the breast milk.
Metabolism in the liver by glucuronation and sulfation (80%) with the formation of inactive metabolites, about 17% is hydroxylated to active metabolites, which are subsequently deactivated after conjugation with sulfates and glutathione. With a lack of glutathione, these metabolites block the enzyme systems of the liver, causing necrosis of hepatocytes.
Half-life is 2-3 hours. Elimination by the kidneys, about 3% unchanged.
Chlorphenamine
After ingestion, up to 30% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is achieved after 2.5 hours. The connection with plasma proteins is 70%. The therapeutic effect develops 1 hour after taking and continues for 24 hours. Penetrates through the blood-brain barrier.
Metabolism in the liver.
Half-life is 2 hours. Elimination by the kidneys.
Indications:It is used to treat influenza and colds accompanied by headache, fever, rhinitis. Used for allergic rhinitis.
X.J10-J18.J11 Influenza, virus not identified
X.J20-J22.J22 Acute respiratory infection of lower respiratory tract, unspecified
X.J30-J39.J39 Other diseases of the upper respiratory tract
Contraindications: Bleeding in the gastrointestinal tract, phenylketonuria, deficiency of glucose-6-phosphate dehydrogenase, portal hypertension, anemia, leukopenia, thrombocytopenia, individual intolerance.
Carefully:Gilbert's syndrome, viral hepatitis, old age, alcoholism.
Pregnancy and lactation:Recommendations for FDA - category is not defined. Contraindicated in I trimester of pregnancy. It is used with caution in pregnancy and lactation, when the expected effect overcomes possible complications.
Dosing and Administration:Children
6-12 years: 1/2 bags every 6-8 hours, not more than 6 packets per day.
Adults and children over 12 years.
Inside for 1 packet 2-3 every 6-8 hours.
The highest daily dose: 6 packets.
The highest single dose: 1 sachet.
Side effects:Central and peripheral nervous system: weakness of drowsiness, hallucinations, impaired coordination of movements.
The system of hematopoiesis: rarely aplastic anemia, pancytopenia.
Digestive system: dry mouth, constipation.
Dermatological reactions: exfoliative dermatitis.
Sense organs: diplopia.
Urinary system: difficulty urinating.
Allergic reactions.
Overdose:Symptoms: nausea, vomiting, pallor of the skin, hepatonecrosis, tubular necrosis.
Treatment: application of donators SH-groups, precursors of the synthesis of glutathione-methionine after 8 hours and N-acetylcysteine after 12 hours after an overdose.
Interaction:Strengthens the effect of indirect coagulants and toxicity of chloramphenicol.
The intake of ethanol in the treatment of the drug leads to the development of acute pancreatitis.
Simultaneous use with stimulators of microsomal oxidation in the liver - barbiturates, rifampicin, ethanol, phenylbutazone, phenothionine, increases the toxicity of paracetamol.
Reduces the risk of hepatotoxic effects of microsomal oxidation inhibitors (cimetidine).
Special instructions:Monitoring of glucose and uric acid in the plasma, the composition of peripheral blood, the functional state of the liver.
Patients are not allowed to drink alcohol during treatment and it is not recommended to drive vehicles and work with moving mechanisms.