Caffeine + Paracetamol (Coffeinum + Paracetamolum)

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

Anilides

Included in the formulation
  • Migraine
    pills inwards 
    Promomed Rus, Open Company     Russia
  • Migrenol®
    pills inwards 
    Foor Ventures Enterprise, Inc.     USA
  • Solpadein Fast
    pills inwards 
    GlaxoSmithKline Helsker, ZAO     Russia
  • Solpadein Fast
    pills inwards 
    GlaxoSmithClean Consumer Helscher     United Kingdom
    • АТХ:

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

    Pharmacodynamics:

    Combined drug.

    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. It inhibits cyclooxygenase mainly in the central nervous system, it affects the centers of pain and thermoregulation. Does not have a negative effect on water-salt metabolism and mucous membranes of the gastrointestinal tract,in this regard, has little effect on the synthesis of prostaglandins in peripheral tissues.

    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.

    Indications:

    It is used to relieve the pain syndrome of mild and moderate severity with migraine, headache, ossalgia, neuralgia, myalgia, arthralgia. Used for algodismenorrhea, toothache, febrile syndrome, colds, flu.

    ICD-10

    VI.G40-G47.G43   Migraine

    X.J00-J06.J06.9   Acute upper respiratory tract infection, unspecified

    X.J10-J18.J10   Influenza caused by an identified influenza virus

    XI.K00-K14.K08.8   Other specified changes in teeth and their supporting apparatus

    XIII.M20-M25.M25.5   Pain in the joint

    XIII.M70-M79.M79.1   Myalgia

    XIII.M70-M79.M79.2   Neuralgia and neuritis, unspecified

    XIV.N80-N98.N94.4   Primary dysmenorrhea

    XIV.N80-N98.N94.5   Secondary dysmenorrhea

    XVIII.R50-R69.R50   Fever of unknown origin

    XVIII.R50-R69.R51   Headache

    XVIII.R50-R69.R52.0   Acute pain

    XVIII.R50-R69.R52.2   Another constant pain

    Contraindications:

    Epilepsy, severe renal and hepatic insufficiency, deficiency glucose-6-phosphate dehydrogenase, age up to 12 years, individual intolerance.

    Carefully:

    Pregnancy and lactation, Gilbert's syndrome, viral hepatitis, chronic alcoholism.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. It is used with caution in pregnancy and lactation in cases,when the expected effect exceeds the potential risk to the fetus and newborn.

    Dosing and Administration:

    Inside, 2 tablets 4 times a day with an interval of at least 4 hours.

    The highest daily dose: 8 tablets.

    The highest single dose: 2 tablets.

    Side effects:

    Hemopoietic system: rarely - thrombocytopenia, hemolytic anemia.

    Digestive system: nausea, stomachalgia.

    Allergic reactions.

    Overdose:

    Diarrhea, anorexia - with acute overdose (develops 6-14 hours after exceeding the dose), with chronic (develops 2-4 days after exceeding the dose) - hypocoagulation, disseminated intravascular coagulation 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 ​​for 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.

    Increases the toxicity of paracetamol concurrent use with stimulators of microsomal oxidation in the liver: barbiturates, rifampicin, ethanol, phenylbutazone, phenytoin.

    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
    Up