Agonist of opioid receptors (mu, kappa, delta). Inhibits the transmission of pain impulses in the central nervous system, reduces the emotional evaluation of pain, causes euphoria, which promotes the formation of drug dependence (mental and physical).
In high doses it has a hypnotic effect. Inhibits conditioned reflexes, reduces the excitability of the cough center, it causes the excitation of the center of the oculomotor nerve (cramps) and n.vagus (bradycardia). Increases the tone of testosterone enanthate vs cypionate smooth muscles of internal organs (including the bronchi, causing bronchospasm), causing spasm of the sphincter of biliary tract and sphincter of Oddi, increases the tone of the sphincter of the bladder weakens peristalsis (leading to the development of constipation). Reduces the secretory activity of the gastrointestinal tract, the basal metabolic rate and body temperature. Depresses the respiratory centers and the gag, so the re-introduction of the use of morphine or emetic drugs on the background to its introduction, do not induce vomiting. It may inhibit the respiratory center, chemoreceptors stimulate the vomiting center and cause nausea and vomiting. The duration of action of about 12 hours.
The ingestion maximum plasma concentration is reached after 4 hours after dosing. It penetrates the blood-brain and placental barriers volume of distribution – 4 l / kg. Metabolized mainly forming glucuronides and sulfates. Excreted by the kidneys (85%) about 9.12% – within 24 hours as unchanged, 80% – in the form of glucuronides; the remaining part (10.7%) – with bile. Small amounts allocated all the glands of external secretion.
Severe pain (especially chronic) syndrome (post-traumatic stress, cancer, post-operative period). Not available for the relief of acute pain.
Hypersensitivity, depression of the respiratory center, pronounced central nervous system depression, paralytic ileus, children up to 7 years, the use of MAO inhibitors in less than 2 weeks before the start of treatment, the use immediately before surgical intervention and the first 24 hours after them, cranio brain injury, broncho-obstructive disease, acute liver disease.
With care .
Older age, prostatic hyperplasia, stenosis of the urethra, liver or kidney failure, lack of adrenal cortex, intracranial hypertension, epileptic syndrome, acute alcohol intoxication, delirium tremens, pulmonary heart disease with chronic lung disease, arrhythmia, a condition after surgery on the biliary or urinary tract, severe inflammatory bowel disease, chronic respiratory disease, hyperthyroidism, abuse of drugs or drug dependence, emotional lability, suicidal thoughts or attempts (including history), general grave condition.
Pregnancy and lactation .
It is not recommended intake during pregnancy. At the time of treatment should stop breastfeeding.
Dosage and administration .
Inside, swallowing whole and not chewed. Used 2 times a day with a 12-hour intervals. In order to reduce persistent pain. Adults Dosage depends on the severity of pain, the patient’s age and previous application of analgesics. With increasing pain, you can use gradually increasing doses of the drug (10, 30, 60 and 100 mg). Patients with intense pain previously untreated narcotic analgesics or pain which is not relieved by the weaker opioids, treatment usually starts with 30 mg every 12 hours increasing the dose to 60 mg every 12 hours if necessary. If necessary, a higher dose, increasing the dose was performed on 25% -50%, while maintaining the 12-hour interval between doses. In malnourished and debilitated patients the initial dose should be reduced. In patients previously treated with conventional dosage forms of morphine or diamorphine. necessary to apply the same daily dose of MST Kontinus with division into 2 doses. Patients transitioning from parenteral administration of morphine to oral MCT Kontinus. The dosage testosterone enanthate vs cypionate should be increased initially to avoid reducing the analgesic effect. Typically, such an increase should be 50-100% of the applied dose. In such patients, the dose should be individualized. Elderly: As with other opioids, it is recommended to reduce the dose. Children from 7 years: a single dose should be 0.2-0.8 mg / kg body weight every 12 hours. The postoperative painAdults:. patients up to 70 kg – 20 mg 2 times a day, patients from 70 kg – 30 mg 2 times a day The drug is not recommended in children.
Side effects . From the digestive system: nausea and vomiting (usually at the beginning of therapy), constipation, dry mouth, anorexia, spasm of the biliary tract, cholestasis, gastralgia, hepatotoxicity (dark urine, pale stools, ikterichnost sclera and skin), with severe inflammatory bowel disease – intestinal, paralytic ileus, toxic megacolon. cardio-vascular system: decrease or increase in blood pressure, tachycardia or bradycardia. respiratory system: depression of the respiratory center, bronchospasm, atelectasis. From the nervous system: dizziness, fainting, drowsiness, unusual tiredness, weakness, headache, tremor, involuntary muscle twitching, discoordination, paresthesia, confusion (hallucinations, depersonalization), increased intracranial pressure with a probability of subsequent ischemic attacks, insomnia, restless sleep. Against the background of high doses – muscle stiffness (especially respiratory), in children – paradoxical excitement, restlessness, seizures, nightmares, sedative or stimulating effect (especially in elderly patients), delirium, decreased ability to concentrate. With the genitourinary system: decrease diuresis, spasm of the ureters, decreased libido, reduced potency, spasm of the sphincter of the bladder, a violation of the outflow of urine, or aggravation of the condition in prostatic hyperplasia and stenosis of the urethra. Allergic reactions: facial flushing, skin rash, face edema, tracheal edema, laryngospasm, chills . Other: increased sweating, hoarseness; violation of clarity of vision (including diplopia), miosis, nystagmus, an imaginary feeling of well-being, a sense of discomfort; tinnitus, drug dependence and tolerance, “lifting” syndrome (muscle pain, diarrhea, tachycardia, mydriasis, pyrexia, rhinitis, sneezing, sweating, yawning, anorexia, nausea, vomiting, nervousness, fatigue, irritability, tremors, stomach cramps , dilated pupils, fatigue, hypoxia, muscle contraction, headache, increased blood pressure, and others. vegetative symptoms). Drug dependence, tolerance, “cancellation” syndrome.
Symptoms: bradycardia, decreased blood pressure, hypothermia, anxiety, dry mouth, delirium, increased intracranial pressure (with a probability of subsequent ischemic attacks), hallucinations, cramps, muscle stiffness, cramps, in severe cases – respiratory arrest, coma.
Treatment: gastric lavage, respiratory rehabilitation and maintenance of heart activity. Intravenous administration of a specific antagonist of opioid analgesics – paloksona a single dose of 0.2-0.4 mg, with the re-introduction of 2-3 minutes to a total dose of 10 mg, symptomatic therapy.
Enhances the effect of hypnotics, sedatives, society and Valium drugs, anxiolytics.
The systematic admission of barbiturates, especially phenobarbital, likely reducing the analgesic effect of narcotic analgesics, stimulates the development of tolerance crosshairs.
When concomitantly with monoamine oxidase inhibitors (due to possible overstimulation or braking testosterone enanthate vs cypionate with the occurrence of hyper- or hypotensive crises), the dosage should be reduced to% of the original.
When concomitantly with beta-blockers may increase the inhibitory action on the central nervous system with dopamine – a decrease in analgesic effect of morphine, cimetidine – increased respiratory depression.
Chlorpromazine strengthens myotic, sedative and analgesic effects of morphine.
phenothiazines and barbiturates increase the hypotensive effect and increases the risk of respiratory depression.
Naloxone restores breathing, eliminating analgesia after administration of morphine.
Nalorfin eliminates the respiratory depression caused by morphine.
The drugs with anticholinergic activity, antidiarrheal agents ( including loperamide) increase the risk of constipation (up to intestinal obstruction), urinary retention, and depression of the central nervous system.
Ethanol, miorelaksany and drugs that suppress the central nervous system, enhance deprimiruyuschie effects and respiratory depression.
Buprenorphine (including prior therapy) reduces the effect of dr.opioidnyh analgesics; during treatment with high doses of agonists of the mu-opioid receptor reduces respiratory depression, and treatment with low-dose agonist-mu or kappa opioid receptor – strengthens; accelerates the emergence of drug dependence on the background of the symptoms of “withdrawal” upon discontinuance of the agonists of mu-opioid receptor, with their sudden abolition partially reduces the severity of symptoms.
Naloxone reduces the effect of opioid analgesics, as well as they cause respiratory depression and central nervous system; may require higher doses to the leveling effects of butorphanol, nalbuphine and pentazocine, who were appointed to eliminate the adverse effects dr.opioidov; can accelerate the emergence of symptoms of “withdrawal” on the background of drug addiction.
Naltrexone accelerates the appearance of symptoms of “withdrawal” on the background of drug dependence (symptoms may appear within 5 minutes after administration, continued for 48 hours, characterized by stability and the difficulty of their elimination) ; reduces the effect of opioid analgesics (analgesic, antidiarrheal, antitussive); no effect on symptoms caused by histamine response.
Enhances the hypotensive effect of drugs that lower blood pressure (including ganglioblokatorov, diuretics).
Competitive Zidovudine inhibits hepatic metabolism and reduces its clearance (increased risk of their mutual intoxication).
Decreases effect metoclopramide.
Special instructions .
In the period of treatment testosterone enanthate vs cypionate should refrain from driving motor vehicles and other classes of potentially hazardous activities that require high concentration and psychomotor speed reactions, avoid drinking beverages alkogolsoderzhashih.