Codeine (Codeinum)

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

Antitussives

Opioid narcotic analgesics

Included in the formulation
АТХ:

R.05   Drugs used for cough and colds

Pharmacodynamics:

Opioid activity is due to conversion 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, pronounced antitussive effect.

Pharmacokinetics:

Bioavailability is 50 ± 7%. The volume of distribution is 2.6 ± 0.3 l / kg, it penetrates the placenta and the blood-brain barrier. Relationship with plasma proteins 7%. Biotransformation in the liver, including up 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. The clearance is 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).

Indications:

Cough with bronchial and lung diseases (including bronchopneumonia, bronchitis, emphysema).

ICD-10

X.J00-J06.J06.0   Acute laryngopharyngitis

X.J00-J06.J04.0   Acute laryngitis

X.J00-J06.J04   Acute laryngitis and tracheitis

XVI.P20-P29.P23.6   Congenital pneumonia caused by other bacterial agents

X.J10-J18.J17.0 *   Pneumonia in bacterial diseases classified elsewhere

X.J10-J18.J15.9   Bacterial pneumonia, unspecified

X.J10-J18.J15.8   Other bacterial pneumonia

XVIII.R00-R09.R05   Cough

Contraindications:

Hypersensitivity, bronchial asthma, pneumonia, respiratory failure, alcohol intoxication, craniocerebral trauma, hypotension, collapse, arrhythmia, epilepsy, impaired liver and kidney function, intoxication diarrhea, hypocoagulation conditions, pregnancy, lactation.

Carefully:

In children under 2 years of age, safety and efficacy have not been studied.

Pregnancy and lactation:

The FDA recommendation category is C.

The risk of dependence in the fetus and the development of withdrawal syndrome in a newborn: irritability, convulsions, excessive tearfulness, tremor, lively reflexes, fever, nausea, diarrhea, sneezing and yawning. Adequate and well-controlled studies in humans have not been conducted. Animals did not cause a teratogenic effect in large doses. Penetrates into breast milk in low doses; Apply if the benefits exceed the risk of side effects.

Dosing and Administration:

Inside, adults with pain - 15-60 mg every 3-6 hours, with diarrhea - 30 mg 4 times a day, with cough - 10-20 mg 4 times a day; for children, these doses are respectively 0.5 mg / kg 4-6 times a day, 0.5 mg / kg 4 times a day and 3-10 mg / kg 4-6 times a day. Intramuscularly administered in the same doses as in enteral administration.The highest daily dose is 120 mg.

Side effects:

Addiction, drug dependence, withdrawal syndrome, respiratory depression, hypotension, nausea, vomiting, atony of the intestine and bladder, bradycardia, arrhythmia, allergic reactions.

Overdose:

Symptoms: cold sweating sweat, confusion, dizziness, drowsiness, lowering of arterial pressure, nervousness, fatigue, miosis, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, dry mouth, delirious psychosis, intracranial hypertension (up to cerebral circulatory disturbance) , hallucinations, muscle rigidity, convulsions, in severe cases - loss of consciousness, stopping breathing, coma.

Treatment: gastric lavage, recovery of respiration and maintenance of cardiac activity and blood pressure; intravenous administration of a specific antagonist opioid analgesics - naloxone in a single dose of 0.2-0.4 mg with repeated administration 2-3 minutes before the total dose of 10 mg; the initial dose of naloxone for children is 0.01 mg / kg.

Interaction:

Alcohol, drugs that depress the central nervous system - potentiation of oppressive effects on the central nervous system, including the respiratory center.

Anticholinergics, antidiarrheals - the risk of severe constipation and acute retention of urine.

Antihypertensive drugs, especially ganglion blockers and diuretics - potentiation of the hypotensive effect.

Buprenorphine - a decrease in the therapeutic effect of other λ-receptor agonists, including a reduction in respiratory depression, the emergence of withdrawal syndrome in dependent individuals.

Other drugs that cause drug dependence are an increased risk of developing drug dependence.

Metoclopramide - decreased prokinetic activity of metoclopramide.

Miorelaxants - potentiation of respiratory depression.

Naltrexone, naloxone, nalorfin - antidotes of narcotic analgesics, eliminate all their pharmacological effects, including cause withdrawal syndrome in patients with drug dependence to them.

Narcotic analgesics are different - mutual potentiation of effects.

Phenotiazine neuroleptics - some increase, and some reduce the effect of morphine hydrochloride.

Special instructions:

In patients with impaired renal function, excretion of codeine is slowed, so the intervals between doses should be extended.

With prolonged use, it is possible to develop drug dependence.

Instructions
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