Morphine (Morphine)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceMorphineMorphine
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  • 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
    • Dosage form: & nbsphypodermic solution
    Composition:

    1 ml of the solution contains:

    active substance - morphine hydrochloride in terms of anhydrous substance - 8.56 mg;

    Excipients - disodium edetate (disodium ethylenediaminetetraacetic acid), glycerol (glycerin distilled), solution of hydrochloric acid 0.1 M, water for injection.

    Description:Transparent colorless or yellowish liquid.
    Pharmacotherapeutic group:Analgesic narcotic drug
    ATX: & nbsp

    N.02.A.A.01   Morphine

    Pharmacodynamics:

    It is an agonist of opioid receptors (mu, kappa, delta). Activates the endogenous antinociceptive system and thus disrupts the interneuronal transmission of painful impulses at various levels of the central nervous system, and also changes the emotional color of the pain, affecting the higher parts of the brain.

    Morphine increases the threshold of pain sensitivity with stimuli of different modalities,inhibits conditioned reflexes has euphoric and mild hypnotic effect, increases the tone of the center of the vagus nerve, inhibits center emesis may stimulate chemoreceptors trigger zone emetic center, depresses the respiratory center, causing constriction of the pupil due to the activation center oculomotor nerve increases bronchial tone and smooth muscle sphincters internal organs (intestine, biliary tract, urinary bladder), enhances the contractile activity of myo-metry, attenuates intestinal peristalsis, inhibits secre activity of the glands of the gastrointestinal tract. Somewhat reduces the basal metabolic rate and body temperature, stimulates the release of antidiuretic hormone. It causes the expansion of peripheral blood vessels and the release of histamine, which can result in reduced blood pressure, skin redness, increased sweating, eye reddening membrane protein. With subcutaneous injection, the effect develops after 10-20 minutes and lasts for 3-5 hours.

    Addictive and drug (opioid) dependence (morphinism).

    Pharmacokinetics:

    The volume of distribution is 4 l / kg.With blood plasma proteins binds 30-35% of the drug. Cmax 50-90 min. Half-life is 2-4 hours.

    About 10% of the parenterally administered drug is excreted in the urine within 24 hours unchanged, 80% - in the form of glucuronide metabolites, the rest is excreted with bile and excreted by the intestine. It penetrates the blood-brain barrier and the placental barrier and is found in breast milk.

    Indications:Morphine it is used as an anesthetic for severe pain syndrome of traumatic origin, in preoperative, operative and postoperative periods, with myocardial infarction, severe attacks of angina, pain in malignant formations and other conditions accompanied by severe pain.
    Contraindications:

    Hypersensitivity to opiates.

    Conditions accompanied by respiratory depression or severe depression of the central nervous system. Convulsive conditions. Increased intracranial pressure. Head injuries. Acute alcoholic conditions and alcoholic psychosis. Bronchial asthma. Paralytic intestinal obstruction.Heart failure due to chronic lung diseases. Cardiac arrhythmias.

    Acute surgical diseases of the abdominal cavity before diagnosis. Conditions after surgical interventions on the biliary tract.

    Do not use morphine on the background of treatment with monoamine oxidase (MAO) inhibitors and for another 14 days after their withdrawal.

    Carefully:

    Chronic obstructive pulmonary disease, drug dependence (including history), alcoholism, suicidal tendencies, emotional lability, cholelithiasis, surgical interventions on the gastrointestinal tract, urinary system, hepatic or renal insufficiency, hypothyroidism, severe inflammatory bowel disease , prostatic hyperplasia, urethral stricture, epileptic syndrome.

    The general severe condition of the patient, the elderly age, children's age.

    Pregnancy and lactation: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:

    Morphine is administered subcutaneously. Doses are selected individually depending on the age and condition of the patient.

    Adults: usual doses for adults under the skin - 1 ml of a solution of 10 mg / ml. The analgesic effect develops in 10-15 minutes, reaches a maximum after 1-2 hours and persists for 8 to 12 hours or more.

    Higher doses for adults under the skin: single 0.02 g, daily -0.05 g.

    Children from birth to 2 years

    Subcutaneously 100-200 μg / kg of body weight (0.1-0.2 mg / kg) if necessary every 4-6 hours, so that the total dose does not exceed 15 mg.

    Children over 2 years old

    Subcutaneously 100-200 μg / kg of body weight (0.1-0.2 mg / kg) if necessary every 4-6 hours, so that the total dose does not exceed 1.5 mg / kg body weight.

    Side effects:

    From the digestive system: more often - nausea and vomiting (often at the beginning of therapy), constipation; less often - dry mouth, anorexia, biliary tract spasm, cholestasis (in the main bile duct), gastralgia, stomach cramps; rarely - hepatotoxicity (dark urine, pale stool, icteric sclera and skin), with severe inflammatory bowel diseases - intestinal atony, paralytic intestinal obstruction, toxic megacolon (constipation, flatulence, nausea, stomach cramps, vomiting).

    From the cardiovascular system: more often - lowering blood pressure, tachycardia, less often - bradycardia, the frequency is unknown - increased blood pressure

    From the respiratory system: more often - oppression of the respiratory center, less often - bronchospasm, atelectasis.

    From the nervous system: more often - dizziness, fainting, drowsiness, unusual fatigue, general weakness; less often - headache, tremor, involuntary muscle twitching, discoordination of muscle movements, paresthesia, nervousness, depression, confusion (hallucinations, depersonalization), increased intracranial pressure with the probability of subsequent cerebral circulatory disorders, insomnia; rarely - restless sleep, depression of the central nervous system, against a background of large doses - rigidity of muscles (especially respiratory), in children - paradoxical agitation, anxiety; frequency unknown - convulsions, nightmares, sedative or stimulating effect (especially in elderly patients), delirium, decreased ability to concentrate.

    From the genitourinary system: less often - a decrease in diuresis, spasm of ureters (difficulty and pain when urinating, frequent urge to urinate), decreased libido, decreased potency; frequency unknown - 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.

    Allergic reactions: more often - wheezing, facial hyperemia, skin rash of the face; less often - skin rash, hives, itching, face swelling, edema of the trachea, laryngeospasm, chills.

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

    Other: more often - increased sweating, dysphonia; less often - a violation of the clarity of visual perception (including diplopia), miosis, nystagmus, imaginary feeling of well-being, a feeling of discomfort; frequency is unknown - tinnitus, drug dependence, tolerance, withdrawal syndrome (muscle pain, diarrhea, tachycardia, mydriasis, hyperthermia, rhinitis, sneezing, sweating, yawning, anorexia, nausea, vomiting, nervousness, fatigue, irritability, tremor, spasms in the stomach, general weakness, hypoxia, muscle contractions, headache, increased blood pressure and other vegetative symptoms).

    With the repeated use of morphine in the course of 1-2 weeks (sometimes within 2-3 days), it is possible to develop addiction (weakening of the analgesic effect) and opioid drug dependence.

    Overdose:

    When poisoning or overdose develops stuporous or comatose state, hypothermia, lowering of arterial pressure, respiratory depression is observed. A characteristic feature is a pronounced narrowing of the pupils (with significant hypoxia the pupils can be enlarged).

    First aid for poisoning - maintenance of adequate pulmonary ventilation Intravenous administration of a specific opinoid naloxone antagonist at a dose of 0.4 to 2 mg quickly restores breathing. In the absence of effect after 2-3 minutes, the administration of naloxone is repeated. The initial dose of naloxone for children is 0.01 mg / kg. It is possible to use yalorfina: 5 - 10 mg intramuscularly or intravenously every 15 minutes to a total dose of 40 mg. Consideration should be given to the possibility of developing a withdrawal syndrome when naloxone and nalorphine are administered to patients with morphine dependence - in such cases, the doses of antagonists should be increased gradually.

    Interaction:

    Strengthens the effect of hypnotics, sedatives, local anesthetics, preparations for general anesthesia and anxiolytics.

    Ethanol, muscle relaxants and drugs that depress the central system, enhance the depressant effect and respiratory depression.

    Buprenorphine (including previous therapy) reduces the effect of other opioid analgesics; against the background of the application of high doses of agonists of mu-opioid receptors reduces respiratory depression, and on the background of the use of low doses of agonists of mu or kappa-opioid receptors - enhances; accelerates the appearance of the symptoms of "withdrawal syndrome" when discontinuing the admission of agonists of mu-opioid receptors against the background of drug dependence, with a sudden withdrawal of them partially reduces the severity of these symptoms. With the systematic administration of barbiturates, especially phenobarbital, there is a possibility of reducing the expression of the analgesic effect of narcotic analgesics, stimulating the development of cross tolerance.

    With simultaneous admission with beta-blockers, it is possible to intensify the inhibitory effect on the central nervous system, with dopamine - decrease the analgesic effect of morphine,cimetidine - increased respiratory depression, other opioid-tion analgesics - central nervous system depression, respiratory depression, blood pressure lowering.

    Chlorpromazine enhances the myotonic, 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 and central nervous system caused by them; higher doses may be required to level the effects of butorphanol, nalbuphine and pentazocine, which have been prescribed to eliminate the undesirable effects of other opioids; can accelerate the appearance of symptoms of "withdrawal syndrome" against the background of drug dependence.

    Naltrexone accelerates the appearance of symptoms of "withdrawal syndrome" against the background of drug dependence (symptoms can appear only 5 minutes after drug administration, continue for 48 hours, are characterized by persistence and difficulty of their elimination); reduces the effect of opioid analgesics (analgesic, antidiarrheal, anti-cough); does not affect the symptoms caused by the histamine reaction.

    Nalorphine eliminates the respiratory depression caused by morphine.

    Strengthens the hypotensive effect of drugs that reduce blood pressure (including ganglioblocators, diuretics).

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

    Medicines with anticholinergic activity, antidiarrhoeal drugs (including loperamide) increase the risk of constipation up to intestinal obstruction, urinary retention and central nervous system depression. Reduces the effect of metoclopramide.

    Special instructions:

    Use with caution morphine in elderly patients, with general exhaustion, with liver and kidney diseases, insufficiency of the cortical layer of the adrenal glands. Under careful supervision and in reduced doses should be used morphine against the background of drugs acting on the central nervous system (drugs for anesthesia, hypnotics, anxiolytics, antidepressants, antipsychotics, anti-histamine, other non-narcotic analgesics) to avoid excessive central nervous system depression and inhibition of respiratory center activity.

    The drug should not be combined with narcotic analgesics from the group of partial agonists (buprenorphine) and agonists - antagonists (nalboufine, butorphanol, tramadol) opioid receptors due to the danger of weakening analgesia and the possibility of provoking withdrawal syndrome in patients with opioid dependence.

    The analgesic effect and undesirable effects of opioid agonists (trimeperidin, fentanyl) in the therapeutic dose range are summarized with the effects of morphine.

    Do not use in situations where paralytic ileus may occur. When the threat of paralytic ileus emergence, the use of morphine should be stopped immediately.

    In patients with a presumed heart operation 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.

    Sometimes there may be tolerance and dependence on the drug.

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

    To reduce the side effects of morphine preparations on the intestine, laxatives should be used.

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

    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions, avoiding the use of ethanol.
    Form release / dosage:Solution for subcutaneous administration of 10 mg / ml in syringe tubes of 1 ml (1 cm3).
    Packaging:For 20, 50 or 100 syringes with instructions for use in a cardboard box.
    Storage conditions:In the dark place at a temperature of no higher than 15 ° C. List II "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation". Keep out of the reach of children.
    Shelf life:2 years. Use the product later than the date specified on the packaging is prohibited.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001645 / 02
    Date of registration:17.09.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp01.06.2018
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