Index of drugs

Treatment of opioid withdrawal syndrome. Substitution treatment of addiction to heroin and morphine (as part of special substitution therapy programs). In addition, for a 1 mg / ml dose: a second-line drug in the fight against severe pain, especially in cancer and post-surgical procedures.

1 ml of syrup contains 1 mg or 5 mg of methadone hydrochloride; the syrup contains sucrose.

Opioid analgesic - opioid receptor agonist. Works on o.u.n. and on the smooth intestinal muscles in a manner similar to morphine. It causes a withdrawal syndrome similar to that of morphine, but with a more graded pre-stage, moderately longer course and less clear symptoms. The drug is quickly absorbed from the digestive tract, reaching C_max after 3-4 h. Approximately 85% is bound to plasma proteins. It is metabolized in the liver. It is excreted in urine and bile, mainly in the form of metabolites. Apparent average T_0,5 after a single dose is about 15 hours, in the case of long-term use - 22 hours.

Hypersensitivity to methadone or auxiliary substances of the preparation. Organic heart disease. Severe liver or kidney problems. Unsatisfied diabetes. Porphyria. Hypotension. Damage o.u.n. and increasing intracranial pressure. Increased attacks of bronchial asthma. Respiratory failure and chronic obstructive pulmonary disease. Pulmonary heart. Oligemia. Pregnancy and breastfeeding. Methadone is not indicated for anesthesia in obstetrics (due to the long half-life may cause inhibition of respiratory center function in the newborn). The use of methadone as an analgesic in children is not recommended (existing clinical trials are not sufficient to determine the appropriate dosing regimen).

Due to the risk of prolonged QT interval and ventricular tachycardiatorsades de pointes, especially the adjustment of high doses (> 100 mg / day), the preparation should be used with extreme caution in patients with a history of conduction, advanced cardiac disease (including ischemic heart disease), liver disease, history of sudden deaths in the family, with electrolyte disturbances (hypokalemia, hypomagnesemia), concomitantly treated with QT prolonging drugs, concomitantly treated with drugs that may cause electrolyte disturbances, simultaneously treated with drugs that inhibit CYP3A4 activity - ECG examination is recommended in these groups before methadone therapy is started and then reaching the maintenance dose. ECG monitoring is recommended for all patients who increase their dose> 100 mg / day and for 7 days after adjusting the dose. Carefully (in reduced doses) use in patients with: hypothyroidism, with Addison's disease, with prostatic hyperplasia, with urethral stricture, with severe constipation, in weakened and elderly people. Methadone should be administered with extreme caution and in reduced doses to patients who receive simultaneously: other opioid analgesics, anesthetics for general anesthesia, phenothiazine, other hypnotics, tricyclic antidepressants and other drugs inhibiting the activity o.u.n. and alcohol (depression, deep sedation or coma may occur). The inhibitory effect of methadone on respiration and the ability to raise the pressure of the cerebrospinal fluid can be significantly increased in the case of an existing increase in intracranial pressure; moreover, drugs produce undesirable effects that can mask neurological symptoms in patients with pathological changes within o.u.n. In patients with acute attacks of asthma, with COPD or with the pulmonary heart and in people with markedly reduced respiratory reserve preceded by pre-existing respiratory depression, organ and tissue hypoxia or hypercapnia, even commonly used therapeutic doses of the drug can reduce respiratory flow and increase airway resistance until to stop breathing.Methadone or other drugs can interfere with the diagnosis or management of patients with acute abdominal symptoms. Methadone administration may result in severe reductions in blood pressure in people with oligemia or when concomitant medications such as phenothiazine or some anesthetics are used. Methadone does not have an anxiolytic effect, so the symptoms of anxiety that occur during treatment can not be treated by increasing its dose. Methadone can cause addiction similar to morphine dependence. Following repeated administration of methadone, psychological dependence, physical dependence and tolerance may occur, so it must be prescribed and administered with the same care as with morphine. In patients with physical dependence on the drug, administration of the usual dose of opioid antagonist may result in an acute withdrawal syndrome. The severity of this syndrome will depend on the degree of physical dependence and the dose of the antagonist given. The use of an opioid antagonist should, if possible, be avoided in this case. When it has to be used to treat severe respiratory depression in a physically addicted patient, the antagonist must be administered with extreme caution and gradually in doses than those normally used. Due to the sucrose content, syrup should not be used in patients with hereditary fructose intolerance, sucrase-isomaltase deficiency or impaired glucose-galactose absorption. The syrup contains small amounts of ethanol (<100 mg / 100 ml).

Do not use during pregnancy unless the clinical condition of the woman requires methadone administration. Methadone crosses the placental barrier. Methadone administration during pregnancy may result in fetal death, low birth weight, respiratory failure, withdrawal syndrome and developmental disorders in the child. Methadone is excreted in human milk - the drug is contraindicated in breast-feeding women because it can cause the child's addiction.

The most important side effects of methadone are: respiratory depression, respiratory arrest, circulatory collapse, shock and cardiac arrest. The most commonly observed adverse reactions are headache, dizziness, sedation, nausea, vomiting, hyperhidrosis and orthostatic hypotension. Very often: vomiting, nausea. Common: weakness, euphoria, dysphoria, insomnia, agitation, disorientation, miosis, visual disturbances, constipation. Uncommon: headache, brief loss of consciousness, decreased libido, respiratory depression, decreased blood pressure, dry mouth, pruritus, urticaria, other skin reactions, edema and less often haemorrhagic haemorrhage, urinary retention, difficulty urinating, anti-diuretic effect , bile duct contractions, impotence. Rare: tachycardia or bradycardia, additional cramps, arrhythmias. Frequency unknown: anorexia. At high doses, you may experience tachycardia typetorsade de pointes.

Orally.Addiction - an initial dose of 15-20 mg is usually sufficient for the abolition of withdrawal symptoms. For patients addicted to high doses of drugs, higher doses may be necessary. In the treatment of addiction to heroin and morphine, the dosage should be correlated with the detoxification program and adjusted to the degree of addiction of the patient.Ache (only a dose of 1 mg / ml) - the usual dose in an adult is 2.5-10 mg, repeated if necessary every 3-8 h. Dosage methadone as a painkiller should be regulated depending on the severity of pain and the response of the patient's body .