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.
Phenylephrine
α1-adrenomimetic causes narrowing of arterioles and reduces the permeability of vessels of the nasal mucosa, reduces edema, facilitates breathing, reduces rhinorrhea and lacrimation.Causes dilated pupil without affecting accommodation, lowers intraocular pressure in glaucoma.
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.
Phenylephrine
After ingestion, up to 30% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 3 hours. The connection with plasma proteins is 70%. 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.
X.J00-J06.J00 Acute nasopharyngitis (runny nose)
X.J00-J06.J06 Acute upper respiratory tract infections of multiple and unspecified sites
X.J10-J18.J11 Influenza, virus not identified
XIII.M70-M79.M79.1 Myalgia
XVIII.R50-R69.R50.0 Fever with chills
XVIII.R50-R69.R51 Headache
XVIII.R50-R69.R52.9 Pain, unspecified
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 pregnancy and lactation.
Dosing and Administration:Inside 1 packet 3 times a day after 4 hours.
The highest daily dose: 3 sachets.
The highest single dose: 1 sachet.
Side effects:Central and peripheral nervous system: weakness, 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:Symtomas: nausea, vomiting, pallor of the skin, hepatonecrosis, tubular necrosis.
Necrosis of liver cells, due to the formation of a toxic metabolite of acetaminophen - N-acetyl-p-benzoquinonimine.
Treatment: application of donators SH-groups, precursors of the synthesis of glutathione-methionine and N-acetylcysteine within 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 during treatment are not recommended to drive vehicles and work with moving mechanisms.