Acetylsalicylic acid + Codeine + Caffeine + Paracetamol (Acidum acetylsalicylicum + Codeinum + Coffeinum + Paracetamolum)

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

NSAIDs - Salicylic acid derivatives

Included in the formulation
АТХ:

N.02.B.A.01   Acetylsalicylic acid

Pharmacodynamics:

The effect of the drug is due to its constituent components; has analgesic, antipyretic, psychostimulating, antitussive and anti-inflammatory effects. Eliminates the symptoms of "colds" and flu.

Acetylsalicylic acid and paracetamol by reducing the synthesis of prostaglandins have antipyretic and analgesic effect.

Codeine has a central antitussive effect (by suppressing the excitability of the cough center), and an analgesic effect caused by the excitation of opiate receptors in various parts of the central nervous system, leading to stimulation of the antinociceptive system and a change in the emotional perception of pain. Codeine to a lesser extent than morphine, depresses breathing, rarely causes miosis, nausea, vomiting and constipation (activation of opioid receptors in the intestine causes relaxation of smooth muscles, decreased peristalsis and spasm of all sphincters).

Caffeine exerts an exciting effect on the central nervous system, enhancing excitation in the cerebral cortex,respiratory and vascular-motor centers, activates conditioned reflexes and physical working capacity, reduces drowsiness and fatigue.

Pharmacokinetics:

Acetylsalicylic acid

Absorption is complete, fast. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The connection with plasma proteins is high. PThe half-elimination period (half-life) - 15-20 minutes, quickly hydrolyzed to salicylates (in the gastrointestinal tract, liver and blood). In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. The maximum concentration in the blood plasma is reached after about 2 hours. When biotransformation in the liver formed metabolites, found in many tissues and urine. Excretion of salicylates is carried out mainly by active secretion in the tubules of the kidneys in unmodified form and in the form of metabolites. Excretion of unchanged substance and metabolites depends on the hydrogen index of urine (with alkalinization of urine ionization of salicylates increases, their reabsorption worsens and excretion increases significantly).

Codeine

After oral administration, it is rapidly absorbed.Connection with plasma proteins - 30%. Time of maximum concentration in blood plasma - in 2-4 hours. Metabolised in the liver to active metabolites; The isozyme CYP2D6 participates in the metabolism of the drug. 10% by demethylation is converted into morphine. It is excreted by the kidneys (5-15% unchanged and 10% in the form of morphine and its metabolites) and with bile.

F - 50 ± 7%. Vd - 2.6 ± 0.3 l / kg, penetrates the placenta and the blood-brain barrier. Relationship with plasma proteins 7%. Biotransformation in the liver, incl. to morphine, and then to morphine-6-glucuronide (2 times more active than morphine) under the action of CYP2D6. The half-life is 2.2-4 hours. Cl 11 ± 2 ml / kg per minute. Elimination mainly with feces, kidneys - 5-15% (10% unchanged in the form or in the form of morphine-6-glucuronide).

Caffeine

Caffeine and its water-soluble salts are well absorbed in the intestine (including fat). PThe half-elimination period (half-life) is about 5 hours, some people - up to 10 hours. The main part is demethylated and oxidized. About 10% is excreted by the kidneys unchanged.

Paracetamol

Paracetamol is quickly and almost completely absorbed from the gastrointestinal tract (maximum concentration 5-20 μg / ml, time to reach a maximum concentration of 0.5-2 hours). It binds to plasma proteins by 15%. Paracetamol penetrates the blood-brain barrier. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg body weight. The half-life is 1-4 hours. Paracetamol is metabolized in the liver and excreted in the urine, mainly in the form of glucuronides and sulfonated conjugates, less than 5% is excreted unchanged in urine.

Indications:

Pain syndrome: headache, toothache (except for cases of extraction of teeth), pharyngitis, myalgia, arthralgia, neuralgia, ishialgia, lumbago, algodismenorea, febrile syndrome.


ICD-10

XIII.M50-M54.M54.3   Sciatica

XIII.M70-M79.M79.1   Myalgia

XIV.N80-N98.N94.6   Dysmenorrhea, unspecified

XVIII.R50-R69.R50   Fever of unknown origin

XVIII.R50-R69.R51   Headache

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

Contraindications:

Hypersensitivity, hepatic and / or renal failure, peptic ulcer of the stomach and duodenum (in the stage of exacerbation); diarrhea with pseudomembranous colitis, toxic dyspepsia, hypocoagulation, pregnancy (I term), breast-feeding, child age (up to 15 years - the risk of Reye's syndrome in children with hyperthermia on a background of viral diseases), acute depression of the respiratory center.Allergic diseases, bronchial asthma.

Caffeine, like other stimulants of the central nervous system, is contraindicated in cases of increased excitability, insomnia, severe hypertension and atherosclerosis, with organic diseases of the cardiovascular system, in old age, with glaucoma. The intake of caffeine accelerates the growth of cysts in patients with polycystosis.

Carefully:

Caution should be given to the drug with concomitant therapy with anticoagulants, gout, peptic ulcer and / or duodenal ulcer (in the anamnesis), erosive gastritis, susceptibility to gastrointestinal bleeding, gout, liver disease, hypoprothrombinemia, hypovitaminosis K, anemia, conditions predisposing to fluid retention in the body (including - in case of violation of heart function, arterial hypertension), thyrotoxicosis, with bronchial asthma. During the drug should refrain from drinking alcohol.

Pregnancy and lactation:

Category Food and Drug Administration (US Food and Drug Administration) - not installed.

The drug is contraindicated in the first trimester of pregnancy. Acetylsalicylic acid has a teratogenic effect; when applied in the first trimester leads to a developmental defect - splitting of the upper palate; in the third trimester - to inhibition of labor (inhibition of Pg synthesis), to the closure of the arterial duct in the fetus, which causes hyperplasia of the pulmonary vessels and hypertension in the vessels of the small circle of blood circulation. Isolated with breast milk, which increases the risk of bleeding in the child due to impaired platelet function. Not applicable during pregnancy and lactation.

Dosing and Administration:

Inside, adults in a daily dose - 1-2 tablets (1 tablet contains: Acetylsalicylic acid - 0.2 g, paracetamol - 0.2 g, caffeine - 0.05 g, codeine - 0.008 g) 2-3 times a day; children over 6 years - 1/2 tablets up to 4 times a day. The interval between repeated receptions is not less than 4 hours.

Duration of treatment without consulting a doctor is no more than 5 days when taken as an analgesic drug and 3 days as an antipyretic drug.

Side effects:

Nausea, abdominal pain, erosive gastritis, constipation, respiratory depression, hyperventilation, skin rash, itching (in rare cases).

Overdose:

Not described.

Interaction:

Inductors of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites of the drug.

The drug reduces the effectiveness of uricosuric and hypotensive drugs and diuretics; It enhances the effect of anticoagulants, antiplatelet agents, fibrinolytic agents, hypoglycemic effect of sulfonylurea derivatives, as well as side effects of glucocorticoids, estrogens. Antacids and colestramine reduce absorption.

The drug increases the concentration in the blood of drugs Li +, methotrexate.

Special instructions:

Children should not be prescribed medications containing acetylsalicylic acid, since in the case of a viral infection they can increase the risk of developing Reye's syndrome. Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver.

With continued use of the drug, control of peripheral blood and the functional state of the liver is necessary. Because the acetylsalicylic acid slows the clotting of the blood, the patient, if he is to undergo surgery, must warn the doctor in advance about taking the drug.

Patients with hypersensitivity or with asthmatic reactions to salicylates or their derivatives acetylsalicylic acid can be prescribed only with special precautions (in emergency care settings). Acetylsalicylic acid in low doses reduces the excretion of uric acid.

In patients with a corresponding predisposition, this can in some cases provoke a gout attack.

During treatment should be discarded from the use of ethanol (increased risk of gastrointestinal bleeding and development of hepatotoxicity) and from employment by potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Instructions
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