Codeine + Caffeine + Metamizol sodium + Paracetamol + Phenobarbital (Codeinum + Coffeinum + Methamizolum natrium + Paracetamolum + Phenobarbitalum)

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

Opioid narcotic analgesics

Opioid non-narcotic analgesics and opioid antagonists

Psychostimulants

Included in the formulation
  • Quintalgin®
    pills inwards 
    Interchim Joint Stock Company Ukrainian-Belgian Chemical Enterprise    
  • Santopolalgin
    pills inwards 
    HIMFARM, JSC     Kazakhstan
  • Sedal-M®
    pills inwards 
    Sopharma, AO     Bulgaria
  • Sedalgin-Neo®
    pills inwards 
    Balkanfarma - Dupnitsa AD     Bulgaria
    • АТХ:

    N.02.B.B.72   Metamizole sodium in combination with psycholeptics

    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.

    Analgesic and antipyretic effects due to a nonselective blockade cyclooxygenases and a decrease in the synthesis of prostaglandins and their precursors from arachidonic acid.

    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.

    The sedative-hypnotic effect of phenobarbital is due to the enhancement and / or imitation of inhibitory effects γ-aminobutyric acid, a 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 electrical stimulation of the motor cortex of the cerebral cortex.

    Pharmacokinetics:

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

    Metamizole sodium in the intestinal wall is hydrolyzed to form an active metabolite, 4-methyl-amino-antipyrine,which in turn is metabolized to 4-formyl-amino-antipyrine and other metabolites. The binding of the active metabolite with proteins is 50-60%. Metabolites are excreted by the kidneys and excreted in breast milk.

    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:

    Pain syndrome of various etiology: headache and toothache, migraine, neuralgia, arthralgia, febrile syndrome.

    ICD-10

    VI.G40-G47.G43.1   Migraine with aura [classic migraine]

    VI.G40-G47.G43.0   Migraine without aura [simple migraine]

    VI.G40-G47.G43.9   Migraine, unspecified

    VI.G40-G47.G43.8   Another migraine

    VI.G40-G47.G43   Migraine

    XVIII.R50-R69.R52.9   Pain, unspecified

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

    XVIII.R50-R69.R52.0   Acute pain

    XVIII.R50-R69.R52   Pain, not elsewhere classified

    XVIII.R50-R69.R51   Headache

    XIII.M70-M79.M70.6   Bursitis of large trochanter (femur)

    XIII.M50-M54.M54.1   Radiculopathy

    XIII.M45-M49.M47.2   Other spondylosis with radiculopathy

    XIII.M70-M79.M79.1   Myalgia

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

    XVIII.R50-R69.R50   Fever of unknown origin

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

    VI.G50-G59.G50.0   Neuralgia of the trigeminal nerve

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

    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.

    Carefully:

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

    Pregnancy and lactation:

    The category of FDA recommendations is not defined.

    Contraindicated during pregnancy and during breastfeeding.

    Dosing and Administration:

    Inside - 1 tablet 1-3 times a day.The course of treatment depends on the effectiveness of therapy and, as a rule, does not exceed 5 days.

    Side effects:

    From the nervous system and sensory organs: drowsiness, lethargy, decreased concentration of attention.

    From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): granulocytopenia, agranulocytosis.

    On the part of the digestive system: Dyspeptic phenomena, pain in the epigastric region, erosive-ulcerative lesions of the gastrointestinal tract.

    Allergic reactions: skin rash.

    Overdose:

    Symptoms: pale skin, anorexia (lack of appetite), abdominal pain, nausea, vomiting, gastrointestinal bleeding, agitation, restlessness, confusion, tachycardia, arrhythmia, hyperthermia (increased body temperature), 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; while concurrent administration of caffeine and cimetidine, oral contraceptives,disulfiram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increase in blood concentrations).

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

    Stimulants of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which makes it possible to develop a hepatotoxic effect with small overdoses. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxic effects. When taken together with salicylates, the nephrotoxic effect of paracetamol increases. The combination with chloramphenicol leads to an increase in the toxic properties of the latter. Strengthens the effect of anticoagulants of indirect action and reduces the effectiveness of uricosuric drugs.

    Special instructions:

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

    Instructions
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