Control of moderate and severe relieving pains after analgesics with weaker effects. Control of severe postoperative pain from the second day after surgery.
Opioid analgesic, selective agonist of opioid receptors (strong agonist of mi receptors, weaker kappa and delta receptors). The main therapeutic action of morphine is analgesic and sedative. The special design of the tablet (system of modified release of active substance) reduces the rate of absorption, but does not reduce the bioavailability, so that the drug can be used every 12 hours. Bioavailability shows large individual differences (20-75%). After a single intake, the maximum serum concentration appears after 10-30 minutes. Morphine binds to 40% of plasma proteins, penetrates well into tissues, weakly to o.u.n. (partition coefficient of about 0.4), does not tend to accumulate in the body. In children, penetration to o.u.n. is much more severe than in adults. Morphine is metabolized mainly in the liver to the active metabolite - morphine-6-monoglucuronate (M6G), accumulating on multiple administrations, and morphine-3-monoglucuronate (M3G). The drug is also metabolised in the kidneys and intestinal mucosa. T0,5 serum morphine is 2.5-3 h. The strongest effect occurs between 2 and 8 hours after administration. The duration of action of the drug (in patients who did not tolerate) is about 12 h. The drug is excreted in 85% by the kidneys, in 9-12% in unchanged form, in 7-10% - in the bile.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Abdominal pain syndrome. Intestinal paralysis. Respiratory depression (respiratory depression). Delayed gastric emptying. acute liver disease. Concomitant use of MAO inhibitors and 2 weeks from discontinuation of MAO inhibitors.
Precautions:
It is not recommended to administer the drug: to patients before surgery and for 24 hours after surgery; patients under 12 years of age; children and adolescents over 12 years old in the treatment of postoperative pain. Caution should be exercised and, if necessary, the dose should be reduced if: opioid addiction; addiction to drugs and psychotropic substances in an interview; alcoholism;delirium tremens; the occurrence of disturbances of consciousness; occurrence of respiratory center disorders and lung function or a condition that leads to the occurrence of the above disorders; severe bronchial asthma; severe pulmonary heart; chronic obstructive pulmonary disease; conditions with elevated intracranial pressure when no mechanical ventilation is carried out; hypotension associated with hypovolaemia; hypertrophy of the prostate gland with residual urine in the bladder (risk of bladder rupture due to urinary retention); stenosis of the urethra or renal colic; impaired renal and / or liver function; disorders of bile duct activity; pancreatitis; inflammatory bowel disease; hypothyroidism; adrenal insufficiency; pheochromocytoma; head injury; epilepsy or increased convulsions; administration to elderly patients. Depression of the respiratory system is the most important risk in the case of opioid overdose. Children and the elderly are more sensitive to morphine. Due to the risk of biliary or renal colic seizures, the drug should be used with caution after surgical procedures, especially in the bile ducts and in patients with secondary acute pancreatitis. Exercise caution if you suspect possible paralysis of the gut and discontinue use in the event of paralysis.Patients who are to be subjected to chordotomy or other pain-relieving treatment should not be given 12 hours before the procedure. Long-term use of the drug may lead to the development of tolerance to the drug, causing the need to gradually apply higher doses of morphine to maintain control of the pain. Long-term use of the drug may lead to physical dependence, and withdrawal may occur after a sudden discontinuation of treatment. Morphine may be abused and misused by addicts or addicts. There is a risk of developing psychological dependence on opioid analgesics, including morphine. The drug should be prescribed with extreme caution to patients abusing alcohol or medication. Simultaneous alcohol use and drug use may increase side effects - avoid simultaneous intake. High doses of morphine must not be used immediately at the beginning of the treatment, without prior gradual administration of small doses. In patients with a history of epilepsy, morphine may lower the seizure threshold. In patients with adrenal insufficiency (eg Addison's disease), cortisol levels in the blood plasma should be monitored and if necessary, corticosteroid substitution should be performed. In rare cases, hyperalgesia may occur, which persists after increasing the dose, especially in patients who have been treated with high doses so far. It may be necessary to reduce the dose or change to another opioid. Patients who are to be subjected to chordotomy or other pain-relieving treatment should not be administered 12 hours before the procedure. It is not recommended to administer the drug in the perioperative period or within 24 hours after the operation. Tablets for modifications. release should be swallowed whole, do not break, chew or crumble - giving a broken, cracked or broken tablet with modified release causes a quick release and absorption of potentially lethal dose of morphine. Morphine has a breath-taking effect - at the start of treatment, it is necessary to keep prophylaxis of constipation at the same time. Table. in doses of 10 mg, 30 mg, and 60 mg contain lactose - should not be used in patients with hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose. Table. in doses of 30 mg and 60 mg contain sunset yellow, which may cause allergic reactions.
Pregnancy and lactation:
It is not recommended for pregnant women, unless in the doctor's opinion the benefit for the mother outweighs the potential risk to the fetus. Morphine sulphate crosses the placenta, inhibits uterine systolic function. In newborns whose mothers have been receiving opioid analgesics for a longer period of time, symptoms of withdrawal syndrome may occur. Morphine may prolong or shorten the duration of labor. Newborns whose mothers received opioid analgesics during labor should be monitored for symptoms of respiratory depression or withdrawal syndrome and, if necessary, the appropriate opioid antagonist should be used. Morphine is excreted in milk, where it reaches concentrations higher than in maternal plasma - breast-feeding is not recommended during treatment. Due to the mutagenic properties, morphine should be given to women and men of childbearing age only if they use effective contraception.
Side effects:
Very often: nausea, constipation. Common: changes in activity level (usually lowering, but also increased level of activity), insomnia, changes in cognitive and sensory functions (eg perceptual disorders, confusion), headache and dizziness, involuntary muscle contractions, drowsiness, abdominal pain, anorexia, dryness oral cavity, vomiting (especially at the beginning of treatment), loss of appetite, excessive sweating, rash, impaired urination, weakness, pruritus. Uncommon: hypersensitivity reactions, agitation, euphoria, hallucinations, mood swings, fits, increased tension, paresthesia, syncope, blurred vision, dizziness, redness on the face, clinically significant reduction or increase in blood pressure, non-cardiac edema, depression respiratory center, bronchospasm, intestinal obstruction, taste disturbances, indigestion, increased liver enzymes, urticaria, urinary retention, peripheral edema (transient after completion of morphine use), tachycardia.Rare: increased pancreatic enzymes or pancreatitis, renal colic. Very rare: drug addiction, decreased libido, tremor, hyperesthesia or allodynia, blurred vision, diplopia and nystagmus, shortness of breath, other rashes such as rash, muscle spasms, muscle stiffness, malabsorption syndrome of ADH (SIADH syndrome; : hyponatremia). Not known: anaphylactic reactions, anaphylactoid reactions, thinking disorders, dysphoria, pupil constriction, decreased coughing reflex, bile colic, amenorrhea, decreased libido, erectile dysfunction, tolerance to the drug, withdrawal syndrome, changes in the teeth (the exact relationship with morphine treatment has not been determined). In addition, palpitations, decreased heart rate and heart failure may occur.
Dosage:
Orally. The drug is administered at regular intervals every 12 hours.Adults. Dose should be determined individually depending on the intensity of pain and including medical history (pain intensity, patient's age and response to previous analgesics) so as to bring the pain down and maintain analgesia until the Next dose (in 12 hours). Recurrence or severity of pain between doses requires increasing the dose, not shortening the interval between doses. Treatment should begin with the lowest effective dose that should be increased during treatment. In patients with low body weight, the starting dose is 10 mg every 12 h, in the remaining patients 30 mg every 12 h, increasing the subsequent doses by 30-50% until adequate pain control. It is recommended to start treatment with a rapid-release morphine drug to set the dose, as dose adjustment with a modified-release form may be difficult. When converting morphine in a rapidly released form to MST Continus, the existing dose of morphine should be maintained, but administered in two divided doses every 12 hours. When converting morphine used parenterally to MST Continus, the current daily dose should be increased by 50-100% and administered in two divided doses every 12 h. For the treatment of postoperative pain (no earlier than one day after surgery): in patients with b. less than 70 kg - 2 tables after 10 mg every 12 h, in patients with bw over 70 kg - 1 tablet 30 mg every 12 hours. Tabl. 200 mg can be used in patients who require a daily dose of 400 mg or more. If necessary, the patient may be given an additional dose of parenteral morphine with particular caution in determining the daily amount of morphine, taking into account the effect of morphine administered in the form of about modifications. release.Youth over 12 years. In the treatment of severe cancer pain dosage is strictly dependent on the doctor's decision; 0.2-0.8 mg / kg is recommended as the initial dose. every 12 hours. Dose adjustment should be performed as described for adult patients. Table. 100 mg and 200 mg are not recommended for use in adolescents. It is not recommended for the treatment of post-operative pain in children.Special groups of patients. Elderly patients (aged 75 years and over) and patients with generally poor health may be more susceptible to morphine - greater caution and / or longer intervals should be used when adjusting the dose; if necessary, reduce the dose. It is not recommended for children under 12 years of age.Method of administration. The drug is used at regular intervals, every 12 hours. The tablets should be swallowed whole; they must not be divided, bitten or crushed because immediate release of morphine and potentially toxic dose can occur. The drug can be taken regardless of meals.
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