Clinical and pharmacological group: & nbsp

Anilides

Included in the formulation
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  • 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, vasoconstrictive effect.

    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.

    Ascorbic acid

    Regulates the transport of hydrogen ions in oxidation-reduction reactions, including in the process at any stage of the Krebs cycle. Participates in the regulation of carbohydrate metabolism.Provides absorption of iron in the intestine, transferring it from trivalent into a divalent form, facilitating its incorporation into heme. Participates in the formation of tetrahydrofolic acid, the synthesis of steroid hormones, norepinephrine and adrenaline, collagen, prothrombin, glycogen. Inactivates hyaluronidase, activating the regeneration of tissues and normalizing the permeability of capillaries. Disinfects toxins and has an antioxidant effect, catching free radicals. He takes an active part in the regulation of immune processes: enhances the formation of antibodies, phagocytic activity and the synthesis of interferon. It inhibits the release of histamine and strengthens its degeneration, suppresses the release of mediators of inflammation and allergic reactions.

    Lengthens the action of paracetamol by slowing its excretion and improves its tolerability.

    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 oral administration, it is poorly absorbed in the gastrointestinal tract. The therapeutic effect develops in 30-90 s after the beginning of admission and lasts for 2-6 hours. Metabolism in the intestine and in the liver before the formation of sulfate conjugates.

    The half-life is 21-32 hours. Elimination by the kidneys.

    Ascorbic acid

    Completely absorbed from the gastrointestinal tract after ingestion. The connection with plasma proteins is 25%. Normally, the concentration of ascorbic acid in the blood is 15-20 μg / ml. The concentration of ascorbic acid in erythrocytes and plasma is lower than in platelets and leukocytes.

    Ascorbic acid is oxidized to dehydroascorbic acid,metabolized into inactive ascorbate-2-sulfate and oxalic acid, then excreted in the urine. In cases of exceeding the dose (more than 200 mg.) ascorbic acid is eliminated by the kidneys in an unchanged form.

    Indications:

    It is used for symptomatic treatment of influenza and colds accompanied by hyperthermia, chills, headache, nasal congestion, pain in the nasal sinuses and throat.

    X.J00-J06.J06   Acute upper respiratory tract infections of multiple and unspecified sites

    Contraindications:

    Renal and hepatic insufficiency of severe degree, hyperthyroidism, prostatic hyperplasia, gastrointestinal bleeding, phenylketonuria, glucose-6-phosphate dehydrogenase deficiency, portal hypertension, anemia, leukopenia, thrombocytopenia, individual intolerance.

    Carefully:

    Gilbert's syndrome, viral hepatitis, old age, alcoholism.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. It is used with caution in pregnancy and lactation, when the expected effect exceeds the risk of complications.

    Dosing and Administration:

    Children 12-18 years: inside by 1 sachet through every 6 hours, not more than 3 bags per day.

    Adults

    Inside for 1 sachet every 4-6 hours, no more than 4 sachets a day, treatment course up to 5 days.

    The highest daily dose: 1 sachet (capsule).

    The highest single dose: 4 sachets (capsules).

    Side effects:

    Central and peripheral nervous system: headache.

    The system of hematopoiesis: anemia, pancytopenia, thrombocytopenia.

    The cardiovascular system: arterial hypertension, tachycardia.

    Digestive system: nausea, decreased appetite.

    Allergic reactions.

    Overdose:

    Symtomas: diarrhea, anorexia - with acute overdose (develops 6-14 hours after exceeding the dose), with chronic (develops 2-4 days after exceeding the dose) - hypocoagulation, DIC syndrome, cerebral edema, rarely - fulminant renal failure due to 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.

    Instructions
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