Codeine + Caffeine + Paracetamol + Propyphenazone + Phenobarbital (Codeinum + Coffeinum + Paracetamolum + Propyphenazonum + Phenobarbitalum)

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

Opioid narcotic analgesics

Psychostimulants

Opioid non-narcotic analgesics and opioid antagonists

Included in the formulation
АТХ:

N.02.B.E   Anilides

Pharmacodynamics:

The opioid activity of codeine is due to the transformation into morphine. Weak agonist opioidnyh λ- and φ-receptors (activation of λ-receptors is 3 times stronger than φ): suppression of interneuronal transmission of pain impulses in the afferent ways of the central nervous system, a decrease in the emotional evaluation of pain and reaction to it.

Caffeine inhibits cAMP phosphodiesterase by increasing the concentration of cAMP in the tissues of the brain, heart, and other organs.

Exciting the centers of the vagus nerve, caffeine causes bradycardia (central action), relaxes the smooth muscles of other organs, including bronchi, slightly increases diuresis due to inhibition of reabsorption of electrolytes in the renal tubules.

Analeptic action is due to the direct excitation of the respiratory and vasomotor center.

Paracetamol is a non-narcotic analgesic, a derivative of para-aminophenol, an active metabolite of phenacetin. It has analgesic and antipyretic action. Anti-inflammatory activity is absent.The analgesic effect is associated with the inhibition of cyclooxygenase in the central nervous system. The effect on the serotonergic and cannabinoid systems of the brain is not excluded.

Propifenazone - a non-steroidal anti-inflammatory agent - inhibits cyclooxygenase, thereby disrupting the formation of prostaglandins E2 and I2, which determines the main pharmacological effects of the drug - anti-inflammatory, analgesic and antipyretic.

The sedative-hypnotic effect of phenobarbital is due to the enhancement and / or imitation of inhibitory effects of GABA, the violation of the permeability of cell membranes, the processes of monosynaptic and polysynaptic transmission in the central nervous system, an increase in the threshold of electric stimulation of the motor cortex of the cerebral cortex.

Pharmacokinetics:

The components of the drug are well absorbed into the digestive tract.

Paracetamol penetrates the blood-brain barrier. Metabolised in the liver. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged.

Caffeine is well absorbed in the intestines. It is excreted mainly by kidneys in the form of metabolites, about 10% - in unchanged form.

Codeine slightly binds to plasma proteins.It is subject to biotransformation in the liver (10% by demethylation passes into morphine). It is excreted by the kidneys (5-15% - unchanged).

Phenobarbital well penetrates the placental barrier. Biotransformatsya in the liver. The main metabolite does not have pharmacological activity. It is excreted by the kidneys, including 20-25% - unchanged.

Indications:Headache, neuralgia, feverish conditions.
ICD-10

XVIII.R50-R69.R51   Headache

XIII.M50-M54.M54.5   Lower back pain

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

VI.G40-G47.G44.2   Headache of intense type

VI.G40-G47.G44.1   Vascular headache, not elsewhere classified

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

XVIII.R50-R69.R50.1   Persistent fever

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

Contraindications:

Hypersensitivity (including to individual components), pulmonary insufficiency, acute attack of bronchial asthma, respiratory failure due to respiratory center depression, impaired liver and / or kidney function, deficiency glucose-6-phosphate dehydrogenase, anemia, leukopenia, pregnancy, lactation, children's age (up to 12 years).

Carefully:

Stomach ulcer and duodenal ulcer (remission stage), elderly age.

Pregnancy and lactation:

The category of FDA recommendations is not defined.

Adequate and well-controlled studies of the components of the drug in humans have not been conducted. Do not apply. The components of the drug penetrate into breast milk. Do not use during breastfeeding.

Dosing and Administration:

Inside 1 tablet 1-3 times a day; the maximum daily dose of 4 tablets. The course of treatment as an analgesic agent is not more than 5 days, as an antipyretic agent - no more than 3 days.

Side effects:

Allergic reactions (rash, itching, urticaria), dizziness, drowsiness, tachycardia, nausea, vomiting, constipation, leukopenia, granulocytopenia, agranulocytosis. With prolonged uncontrolled admission in high doses - addiction (weakening analgesic effect) and drug dependence, due to the presence of codeine; hepatic and / or renal failure.

Overdose:

Symptoms: pallor of the skin, anorexia (lack of appetite), abdominal pain, nausea, vomiting, gastrointestinal bleeding, agitation, motor anxiety, confusion, tachycardia, arrhythmia, hyperthermia (fever), frequent urination,headache, tremor or muscle twitching, epileptic seizures, increased hepatic transaminase activity, hepatonecrosis, increased prothrombin time. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdosage hepatic insufficiency develops with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis, arrhythmia, pancreatitis. If you suspect an overdose, seek medical help immediately.

Treatment: gastric lavage followed by administration of activated charcoal. Specific antidote for paracetamol poisoning is acetylcysteine. The introduction of acetylcysteine ​​is topical within 8 hours after taking paracetamol. With gastrointestinal bleeding it is necessary to administer antacids and rinse the stomach with an ice-cold 0.9% solution of sodium chloride; maintenance of ventilation and oxygenation; with epileptic seizures - intravenous diazepam; maintaining the balance of liquid and salts.

Interaction:

When concomitantly with barbiturates, tricyclic antidepressants, rifampicin, ethanol increases the risk of hepatotoxicity (these combinations should be avoided).

Long-term use of barbiturates reduces the effectiveness of paracetamol.

With the joint use of caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin) it is possible to increase metabolism and increase caffeine clearance; with the simultaneous administration of caffeine and cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increasing blood concentrations).

Simultaneous use of caffeine-containing beverages and other CNS stimulating agents may lead to excessive stimulation of the CNS.

Special instructions:

It is possible to reduce the concentration and speed of psychomotor reactions, therefore, during the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Instructions
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