Codeine + Morphine + Noscapine + Papaverine hydrochloride + Tebain (Codeinum + Morphinum + Noscapinum + Papaverini hydrochloridum + Tebainum)

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

Opioid narcotic analgesics

Included in the formulation
  • Omnompon
    solution PC 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
    • АТХ:

    N.02.A.A.51   Morphine in combination with other drugs

    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.

    Morphine - an agonist of opioid μ- and κ-receptors (3: 1 - activation of μ-receptors is 3 times stronger than κ): suppression of interneuronal transmission of pain impulses in the afferent ways of the CNS, a decrease in the emotional evaluation of pain and reaction to it.

    Noscapine, thebaine - complete natural agonists of opioid receptors - the mechanism of action is similar to that of morphine, papaverine hydrochloride is an antispasmodic.

    Pharmacokinetics:

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

    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).

    Bioavailability of morphine - 75% (with food).The volume of distribution - 3,3 ± 0,9 l / kg, a decrease in chronic renal failure. Penetrates through the placenta and the blood-brain barrier. The connection with plasma proteins is 35 ± 2%. Biotransformation in the liver, including up to morphine-6-glucuronide (2 times more active than morphine), in part - in the mucosa of the intestine. Half-life is 2-2.5 hours, an increase in newborns. Clearance 24 ± 10 ml / min / kg, decreased in newborns, with chronic renal failure and burns. Elimination by the kidneys (85%, 9-12% unchanged) and with feces (7-10%) in unchanged form and metabolites (intestinal-hepatic circulation).

    Absorption of papaverine is variable. Bioavailability - 54%. The connection with plasma proteins is 90%. Biotransformation in the liver. The half-life is 0.5-2 hours (up to 24 hours). Elimination by the kidneys in the form of metabolites. Removed during hemodialysis.

    Indications:

    Pain syndrome (of various etiology), intestinal colic, biliary colic, renal colic.

    ICD-10

    IX.I20-I25.I23   Some current complications of acute myocardial infarction

    IX.I20-I25.I22.90   Repeated myocardial infarction of unspecified site with hypertension

    IX.I20-I25.I22.9   Secondary myocardial infarction, unspecified

    IX.I20-I25.I22.80   Secondary myocardial infarction of other specified localization with hypertension

    IX.I20-I25.I22.8   Secondary myocardial infarction of other specified location

    IX.I20-I25.I22.10   Secondary myocardial infarction with hypertension

    IX.I20-I25.I22.1   Repeated myocardial infarction of the inferior wall

    IX.I20-I25.I22.00   Secondary myocardial infarction with hypertension

    IX.I20-I25.I22.0   Repeated myocardial anterior wall infarction

    IX.I20-I25.I22   Repeated myocardial infarction

    IX.I20-I25.I21.90   Acute myocardial infarction, unspecified with hypertension

    IX.I20-I25.I21.9   Acute myocardial infarction, unspecified

    IX.I20-I25.I21.40   Acute subendocardial myocardial infarction with hypertension

    IX.I20-I25.I21.4   Acute subendocardial myocardial infarction

    IX.I20-I25.I21.30   Acute transmural myocardial infarction of unspecified site with hypertension

    IX.I20-I25.I21.3   Acute transmural myocardial infarction, unspecified

    IX.I20-I25.I21.20   Acute transmural myocardial infarction of other specified localizations with hypertension

    IX.I20-I25.I21.2   Acute transmural myocardial infarction of other specified locations

    IX.I20-I25.I21.10   Acute transmural myocardial infarction of the lower wall of the myocardium with hypertension

    IX.I20-I25.I21.1   Acute transmural myocardial infarction of the inferior wall

    IX.I20-I25.I21.00   Acute transmural myocardial infarction of the anterior wall of the myocardium with hypertension

    IX.I20-I25.I21.0   Acute transmural myocardial infarction of anterior wall

    IX.I20-I25.I21   Acute myocardial infarction

    XIV.N20-N23.N23   Renal colic, unspecified

    XVIII.R10-R19.R10.4   Other and unspecified abdominal pain

    XVIII.R10-R19.R10.3   Pain localized in other areas of the lower abdomen

    XVIII.R10-R19.R10.2   Pain in the pelvis and perineum

    XVIII.R10-R19.R10.1   Pain localized in the upper abdomen

    XVIII.R10-R19.R10   Pain in the abdomen and pelvis

    XIX.T08-T14.T14.9   Injury, unspecified

    Contraindications:

    Hypersensitivity, respiratory insufficiency, elderly age, cachexia, trauma of the skull, hemorrhagic stroke, acute diseases of the internal organs until diagnosis, pregnancy.

    Carefully:

    Abdominal pain of unclear etiology, asthma attack, chronic obstructive pulmonary disease, arrhythmias, convulsions, drug dependence (including history), alcoholism, suicidal tendencies, emotional lability, cholelithiasis, surgical interventions on the digestive tract, urinary system, head injury brain, intracranial hypertension, hepatic or renal failure, hypothyroidism, severe inflammatory bowel disease, prostatic hyperplasia, urinary stricture about the channel,paralytic intestinal obstruction, epileptic syndrome, conditions after surgery on the biliary tract, pulmonary heart failure in the background of chronic lung diseases, pregnancy, breast-feeding, simultaneous treatment with MAO inhibitors. In children, efficacy and safety have not been studied.

    Pregnancy and lactation:

    The FDA recommendation category is C.

    The risk of dependence in the fetus and the development of the phenomenon of cancellation in the 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 concentrations; Apply if the benefits exceed the risk of side effects.

    Dosing and Administration:

    Subcutaneously to 1 ml of 1-2% solution. Higher doses: single dose - 0.03 g, daily - 0.1 g.

    Side effects:

    From the nervous system and sensory organs: dizziness, headache, asthenia, anxiety, irritability, insomnia, nightmarish dreams, confusion,hallucinations, delirium, increased intracranial pressure, paresthesia, involuntary muscle twitching, convulsions, discoordination of movements, blurred vision, nystagmus, diplopia, miosis, ringing in the ears, change in taste; against a background of large doses - stiff muscles (especially respiratory); in children, paradoxical agitation; physical and mental dependence (after 1-2 weeks of regular admission), withdrawal syndrome.

    From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia / bradycardia, palpitation, decrease / increase in blood pressure, fainting.

    On the part of the respiratory system: oppression of the respiratory center, bronchospasm, atelectasis.

    On the part of the digestive system: nausea, vomiting, constipation / diarrhea, dry mouth, anorexia, gastralgia, biliary tract spasm, cholestasis; with severe inflammatory bowel diseases - intestinal atony, paralytic intestinal obstruction, toxic megacolon (constipation, flatulence, nausea, stomach cramps, vomiting).

    From the genitourinary system: decreased diuresis, spasm of ureters (difficulty and pain when urinating, frequent urge to urinate),spasm of the sphincter of the bladder, a violation of the outflow of urine or aggravation of this condition with prostatic hyperplasia and stenosis of the urethra, a decrease in libido and / or potency.

    Allergic reactions: wheezing, face hyperemia, edema of the face, edema of the trachea, laryngospasm, chills, itching, rash, urticaria.

    Others: increased sweating, dysphonia, weight loss, dehydration, pain in the limbs; local reactions - hyperemia, swelling, burning at the injection site.

    Overdose:

    Symptoms of acute and chronic overdose: cold sticky sweat, confusion, dizziness, drowsiness, lowering of blood pressure, nervousness, fatigue, miosis, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, dryness of oral mucosa, delirious psychosis, intracranial hypertension (up to the violation of cerebral circulation), hallucinations, muscle rigidity, convulsions, in severe cases - loss of consciousness, respiratory arrest, coma.

    Treatment: resuscitation, intravenous administration of a specific antagonist opioid analgesics - naloxone.

    Interaction:

    Extends and enhances the effect of drugs that depress the central nervous system, including hypnotics, sedatives, drugs for general anesthesia, anxiolytics, antipsychotics and local anesthetics medicines.

    Medicinal products, depressing the central nervous system, including ethanol, intensify the depressive effect and respiratory depression (so do the muscle relaxants).

    With the systematic administration of barbiturates, especially phenobarbital, there is a possibility of reducing the severity of analgesic effects.

    With caution should be used simultaneously with MAO inhibitors because of possible overexcitation or inhibition with the emergence of hyper- or hypotensive crises (first to assess the effect of interaction, the dose should be reduced to 1/4 of the recommended).

    With simultaneous admission with beta-blockers, it is possible to increase the inhibitory effect on the central nervous system, with dopamine - decrease the analgesic effect of morphine, with cimetidine - increase respiratory depression, with other opioid analgesics - increase of CNS depression, respiration, hypotension.

    Chlorpromazine enhances the sedative and analgesic effects of morphine.

    The derivatives of phenothiazine and barbiturates increase the hypotensive effect and increase the risk of respiratory depression.

    Naloxone reduces the effect of opioid analgesics, as well as the respiratory depression and central nervous system caused by them.

    Nalorphine eliminates the respiratory depression caused by morphine.

    Strengthens the hypotensive effect medicines, reducing blood pressure (including ganglioblokatorov, diuretikov).

    Competitively inhibits hepatic metabolism of zidovudine and reduces its clearance (increased risk of their mutual intoxication).

    Medicinal productsbut with anticholinergic activity, antidiarrheal medicines (including loperamide) increase the risk of constipation up to intestinal obstruction, urinary retention and CNS depression.

    Reduces the effect of metoclopramide.

    Morphine can increase the anticoagulant activity of coumarin and other anticoagulants.

    Special instructions:

    Do not use morphine in situations where paralytic ileus is possible. If there is a risk of paralytic ileus, use morphine immediately.

    In patients with presumed heart surgery or another operation with intensive pain syndrome, the use of morphine should be discontinued 24 hours before the operation. If the therapy is subsequently shown, then the dosing regimen is chosen taking into account the severity of the operation.

    If there is nausea and vomiting, you can use a combination with phenothiazine.

    During the treatment period, take care when driving vehicles and engage in other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions, avoid the use of ethanol. Concomitant use of other drugs acting on the central nervous system (antihistamines, sleeping pills, psychotropic drugs, other pain medications) is allowed only with the permission and under the supervision of a physician.

    It should be borne in mind that children under 2 years of age are more sensitive to the effects of opioid analgesics and paradoxical reactions may occur.

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