Morphine (Morphinum)

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
  • Morphine
    solution PC 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Morphine
    solution for injections 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Morphine sulfate
    capsules inwards 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • MST Continus
    pills inwards 
    Mundifarma GmbH, Germany     Germany
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.02.A.A.01   Morphine

    Pharmacodynamics:

    The drug is a complete opioid receptor agonist (μ- and κ-receptor, with activation of μ-receptors 3 times greater than κ-).

    The basic mechanisms of the analgesic effect of opioid analgesics are realized at the level of the spinal cord, subcortical structures and the cerebral cortex:

    I. oppression of pain impulses in the afferent CNS pathways (impaired transmission of impulses from the end of the primary afferents to the intercalary neurons of the spinal cord):

    1) As a result of blocking N-type calcium channels in the presynaptic endings of the axons of the primary afferents, the release of substance P and glutamate decreases, and the transmission of pain impulses to the intercalary neurons of the posterior horns of the spinal cord is impaired.

    2) Due to the stimulation of postsynaptic opioid receptors, the process of depolarization of the postsynaptic membrane and inhibition of activation of intercalary neurons under the action of the mediator. All this leads to a violation of transmission of pain impulses at the level of the spinal cord (spinal action).

    II. Strengthening of the inhibitory effect of the descending antinociceptive system on painful impulses in the afferent CNS pathways:

    When the opioid receptors are stimulated in the gray near-conductor substance and some other parts of the brain stem due to the inhibition of inhibitory GABAergic neurons, activation of the descending antinociceptive system, which inhibits the transmission of pain impulses along the afferent pathways of the spinal cord (supraspinal action), occurs. Descending inhibitory influences at the level of the spinal cord are carried out with the participation of serotonin and norepinephrine.

    III. Changing the emotional assessment of pain: as a result of the action of narcotic analgesics on the higher departments of the central nervous system, the emotional evaluation of pain changes, and its perception decreases (even if the feeling of pain persists, it worries the patient less).

    Pharmacokinetics:

    Quickly and completely absorbed. Metabolized in the liver, half-life is 2-3 hours.Excreted by the kidneys by 90%, the rest is excreted with bile, 10% excreted unchanged. With violations of the liver and kidneys, as well as in elderly patients, the elimination half-life increases.

    Indications:

    Pain syndrome; cough, which can not be stopped with antitussive drugs; Shortness of breath associated with cardiovascular failure.

    ICD-10

    IX.I30-I52.I50   Heart failure

    IX.I30-I52.I50.1   Left ventricular failure

    XVIII.R00-R09.R05   Cough

    XVIII.R00-R09.R07.2   Pain in the region of the heart

    XVIII.R50-R69.R52.0   Acute pain

    XVIII.R50-R69.R52.1   Constant unrestrained pain

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

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:

    Exhaustion.

    Pain in abdomen of unclear etiology.

    Disturbance of breathing (associated with depression of the respiratory center).

    Increased intracranial pressure.

    Trauma of the brain.

    Hepatic-cell failure.

    Simultaneous administration of monoamine oxidase inhibitors.

    Delirium.

    Age to 2 years.

    Acute alcohol intoxication.

    Epileptic status.

    Carefully:

    Elderly age. 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 gastrointestinal tract, urinary system, brain trauma, intracranial hypertension, hepatic or renal failure, hypothyroidism, severe inflammatory bowel disease, hyperplasia of the prostate, urethral stricture, paralytic intestinal obstruction, epileptic syndrome, conditions after surgical intervention on the biliary tract, pulmonary heart failure in the background of chronic lung diseases, pregnancy, breast-feeding.

    Pregnancy and lactation:

    Category FDA - C. In pregnancy, childbirth and the period of breastfeeding, the use of morphine is permissible only for vital indications (it is possible to develop drug dependence in the fetus and the newborn).

    Dosing and Administration:

    The dosage regimen is selected individually.The average dose for oral administration to adults is 10-100 mg twice a day with a break of 12 hours. For children from 12 years, the dose is 1-5 mg.

    For subcutaneous administration, 1 mg. Higher doses for adults: single dose - 0.02 g, daily - 0.05 g.

    Side effects:

    From the genitourinary system: a violation of the outflow of urine, spasm of ureters, decreased libido, decreased potency

    From the side of the central nervous system: sedative or stimulating effect, hallucinations, delirium, increased intracranial pressure, impaired blood circulation of the brain, dizziness, fainting, drowsiness.

    From the cardiovascular system: bradycardia, lowering blood pressure.

    On the part of the digestive system: vomiting, nausea, cholestasis, constipation, dry mouth, anorexia, spasm of bile ducts.

    On the part of the respiratory system: respiratory depression, bronchospasm.

    Allergic reactions: wheezing, facial hyperemia, skin rash, skin rash.

    Local reactions: hyperemia, edema, burning at the injection site.

    Overdose:

    Increased side effects, muscle rigidity, loss of consciousness, coma, hypothermia, cold sticky sweat. Treatment: resuscitation, a specific antagonist - naloxone.

    Interaction:

    The drug enhances the effect of sedatives and hypnotics, anesthesia, anxiolytics.

    With simultaneous admission with barbiturates, narcotic analgesics, CNS depression, arterial hypotension, respiratory depression are observed.

    Barbiturates can reduce the analgesic effect of the drug.

    With simultaneous administration with hormonal contraceptives, the clearance of morphine can increase.

    With simultaneous administration with monoamine oxidase inhibitors, side effects from the cardiovascular system are possible.

    With simultaneous use with phenothiazine derivatives, pain and hypotensive effects increase, and respiratory depression becomes more frequent.

    With simultaneous application with dopamine, the analgesic effect of morphine can be reduced; with ketamine - potentiation of the oppressive effect of morphine on the respiratory center; with ketoprofen - a decrease in respiratory depression due to the action of morphine.

    With simultaneous admission with beta-blockers, it is possible to intensify the inhibitory effect on CNS.

    When administered concomitantly with nalorphine or naloxone, analgesia and respiratory depression that are caused by morphine are inhibited.

    With simultaneous administration with chlorpromazine, potentiation of analgesic, sedative and miotic effects occurs.

    With simultaneous use with mexiletine, a decrease in the absorption of mexiletine is possible; with methylphenidate - enhancing the analgesic effect of morphine and reducing its sedative effect; with metoclopramide - the rate of absorption of morphine increases when ingestion and sedation increases.

    With simultaneous admission with lidocaine, the analgesic effect of morphine increases, with phenylbutazone - morphine cumulation occurs, with cimetidine - increased respiratory depression.

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

    Competitively inhibits hepatic metabolism of zidovudine and reduces its clearance (increased risk of their mutual intoxication). Medicinal products with anticholinergic activity, antidiarrheal medicines (including loperamide) increase the risk of constipation up to intestinal obstruction, urinary retention and oppression CNS.

    Special instructions:

    Use with caution in patients of senile age. Morphine causes pronounced euphoria, with repeated subcutaneous injection, drug dependence develops rapidly; with a regular intake of a therapeutic dose, the dependence can develop after 2-14 days from the start of treatment. The withdrawal syndrome can occur several hours after the cessation of a long course of treatment and reach a maximum after 36-72 hours.

    Do not drink alcohol during use.

    Impact on the ability to drive vehicles and manage mechanisms

    During the period of taking the drug should be abandoned the management of transport and the implementation of potentially dangerous work that requires concentration of attention.

    Instructions
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