Caffeine + Paracetamol + Chlorfenamine + Ascorbic acid (Coffeinum + Paracetamolum + Chlorpheniraminum + Acidum ascorbinicum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Anilides

Included in the formulation
  • Grippostad® C
    capsules inwards 
    SHTADA Artznajmittel AG     Germany
    • АТХ:

    N.02.B.E.71   Paracetamol in combination with psycholeptics

    Pharmacodynamics:

    Combined drug.

    Has analgesic, antipyretic, antihistamine, vasoconstrictive, sedative, bronchodilating and antitussive action.

    Caffeine

    The alkaloid contained in coffee seeds, tea leaves, cola nuts, cocoa, affects the content of intracellular calcium, adenosine receptors and phosphodiesterase, which destroys cAMP.

    It inhibits the phosphodiesterase of cAMP, increasing its concentration in the brain tissues. Has psychostimulant activity, increasing mental and physical performance, reducing the need for sleep and removing the feeling of fatigue.

    It stimulates the respiratory and vasomotor centers, having an analeptic effect. It inhibits the production of prolactin and the secretion of milk.

    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 H1receptors. 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.

    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:

    Caffeine

    After ingestion, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached in 30-75 minutes. The connection with plasma proteins is 35%.

    Metabolism in the liver to paraxanthin (80%), theobromine (10%), theophylline (4%).

    Slows the clearance of paracetamol

    The half-life is 5 hours. Elimination by the kidneys.

    Paracetamol

    After oral administration, it is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached in 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 the blood plasma is achieved after 2.5 hours. The connection with plasma proteins is 70%. The therapeutic effect develops 1 hour after admission and lasts for 24 hours. Penetrates through the blood-brain barrier.

    Metabolism in the liver.

    Half-life is 2 hours. Elimination by the kidneys.

    Ascorbic acid

    Completely absorbed from the gastrointestinal tract after ingestion. Connection with plasma proteins - 25%. Normally, the concentration of ascorbic acid in the blood: 15-20 mcg / 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 to 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 to treat influenza and colds accompanied by headache, fever, rhinitis. Used for allergic rhinitis.

    ICD-10

    X.J00-J06.J00   Acute nasopharyngitis (runny nose)

    X.J00-J06.J06.8   Other acute upper respiratory tract infections of multiple localization

    X.J10-J18.J11   Influenza, virus not identified

    X.J30-J39.J34.8   Other specified diseases of nose and nasal sinuses

    XVIII.R00-R09.R07.0   A sore throat

    XVIII.R50-R69.R50.0   Fever with chills

    XVIII.R50-R69.R51   Headache

    Contraindications:

    Bleeding in the gastrointestinal tract, phenylketonuria, deficiency of glucose-6-phosphate dehydrogenase, portal hypertension, anemia, leukopenia, thrombocytopenia, age up to 15 years, pregnancy and lactation, 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, 2 capsules per reception, 3-4 times a day. Re-reception if necessary in 4-6 hours.

    The highest daily dose: 12 capsules.

    The highest single dose: 2 capsules.

    Side effects:

    Central and peripheral nervous system: weakness, drowsiness, hallucinations, impaired coordination of movements.

    Hemopoietic system: rarely - aplastic anemia, pancytopenia.

    Digestive system: dry mouth, constipation.

    Dermatological reactions: exfoliative dermatitis.

    Sense organs: diplopia.

    urinary system: difficulty urinating.

    Allergic reactions.

    Overdose:

    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, phenytoin) 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.

    Instructions
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