Index of drugs

Severe pain that requires treatment with opioid analgesics.

1 tabl about release contains 5 mg, 10 mg, 20 mg, 40 mg or 80 mg of oxycodone hydrochloride (and a maximum of 15 mg, 30 mg, 12 mg, 24 mg and 48 mg of sucrose respectively).

Opioid analgesic. Oxycodone has affinity for kappa, mi and delta opioid receptors in the brain and spinal cord. It has no antagonistic effect. The therapeutic effect is mainly to remove pain and calm down. Compared to oxycodone in a rapid-release form, administered alone or in combination with other substances, sustained-release tablets provide pain relief over a clearly longer period without an increased incidence of side effects. Oxycodone reaches C_max after about 3 hours. It binds with proteins in 38-45%. T_0,5 is 4-6 h. The main metabolic pathways of oxycodone are N-demethylation (CYP3A4) to inactive noroxycodone and O-demethylation (CYP2D6) to active oxymorphone. Oxycodone and its metabolites are excreted in urine and faeces.

Hypersensitivity to the active substance or any of the excipients. Severe respiratory failure with hypoxia of organs and tissues and / or hypercapnia. Severe chronic obstructive disease of the lungs. Pulmonary heart syndrome. Severe bronchial asthma. Paralytic intestinal obstruction. acute abdomen syndrome, delayed gastric emptying. Any situation where opioid drugs are contraindicated. Moderate to severe hepatic impairment. Severe renal impairment (creatinine clearance <10 ml / min). Chronic constipation. It is not recommended to use before planned surgery and within 24 hours after surgery. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

There are no studies on the use of the product in children <12 yrs., Therefore, use in this age group is not recommended. Dose reduction may be indicated if the patient has hypothyroidism. Special care should be taken when using the medicine in elderly patients or in frail and infirm patients, in patients with severe lung, liver or kidney disorders, mucous edema, hypothyroidism, Addison's disease (adrenal insufficiency), intoxication psychosis (e.g. alcoholic), hypertrophy of the prostate gland, alcoholism, diagnosed with opioid addiction, alcohol depilation (delirium tremens), pancreatitis, biliary tract diseases, biliary colic or urinary tract colitis, increased intracranial pressure, hypotension, hypovolaemia, psychosis after intoxication, intestinal inflammatory diseases, adrenocortical insufficiency, alcohol addicts, circulatory disorders, epilepsy or a tendency to convulsions, patients taking MAO inhibitors. In the case of patients with head injuries, the doses should be carefully selected and closely monitored. The preparation should not be used in patients who may experience paralytic ileus. If there is a suspicion of a paralytic intestinal obstruction or it occurs while taking the drug, stop using the drug immediately. Patients undergoing additional pain management procedures (eg surgery, blockage of nerve plexuses) should not take the medicine within 12 h before the planned procedure. If postoperative therapy is indicated, the dose should be adjusted accordingly. 80 mg prolonged-release tablets should not be used by patients who have not been treated with opioids before, the dose may cause them to have respiratory depression leading to death. Particular care should be taken when oxycodone is used in patients undergoing bowel surgery. Opioids should be given during the postoperative period only if the bowel function has been restored. Patients with severe hepatic impairment should be closely monitored.In patients suffering from chronic non-cancer pain, opioids should be used as part of a comprehensive treatment program using other medications and therapies. The key element determining the way of treating a patient with chronic non-neoplastic pain is to analyze the history of patient addiction and substance abuse. There is a risk of developing mental addiction. Avoid using the drug in patients who are currently or have been past addicted to alcohol or drugs. If it is appropriate to treat the patient with opioids, the main goal is not to reduce the dose of opioid, but to set the optimal dose to relieve pain, minimizing side effects. The patient should be in constant contact with the treating physician so that the dose can be adjusted accordingly. It is strongly recommended that the doctor evaluate the results of treatment in accordance with the applicable guidelines for the treatment of pain. The doctor, together with the patient, may decide to stop treatment if the expected goals are not achieved. Oxycodone is an addictive drug and can be abused by people with latent or manifest addictive disorders. Respiratory depression is the most important risk caused by opioids and the risk of developing it is greatest in elderly or debilitated patients. Respiratory depression caused by oxycodone can lead to an increase in the concentration of carbon dioxide in the blood and thus in the cerebrospinal fluid. In patients with congenital tendencies, opioids can cause a significant reduction in blood pressure. Long-term use of oxycodone may lead to the development of tolerance, resulting in higher doses to achieve anesthetic effect. There is cross-tolerance to other opioids. Chronic use of the drug may cause physical dependence. Discontinuation symptoms may occur after abrupt cessation of treatment. If therapy with oxycodone is no longer necessary, the daily dose should be gradually reduced to avoid withdrawal symptoms. Hyperalgesia that do not respond to an increase in the dose of oxycodone are very rare, especially when high doses are used. It may be necessary to reduce the dose of oxycodone or to use another opioid medicine. The drug has addictive potential. When used as recommended in patients with chronic pain, the risk of physical or mental addiction is clearly limited. There are no data on the incidence of psychological dependence in patients with chronic pain. In patients with alcohol addiction or substance abuse, the drug should be prescribed with extreme caution. It is not recommended to use the drug in the pre-operative period and within the first 12-24 hours after surgery. In the event of an unlawful intravenous injection, the tablet aids may cause tissue necrosis at the injection site, infection, increased risk of endocarditis and damage, heart valve disease that can lead to death, pulmonary granuloma or other serious life-threatening events. In order to ensure the proper action of the drug, the tablets should not be chewed or crushed; taking crushed tablets or chewing them leads to the rapid release and absorption of a potentially lethal dose of oxycodone. Concomitant use of alcohol and oxycodone may increase the side effects - avoid simultaneous use. Using the drug as a doping agent may pose a health risk. The product contains sucrose, therefore it should not be used in patients with rare hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency.

Avoid taking the drug during pregnancy or breast-feeding. Newborns born to mothers who received opioids during the last 3-4 weeks before childbirth should be monitored for respiratory disorders. In newborns of mothers treated with oxycodone, withdrawal symptoms can be observed. Oxycodone can be excreted into breast milk and cause respiratory depression in the newborn.

Very common: drowsiness, pain and dizziness, constipation, nausea, vomiting, pruritus. Common: reduced appetite, various psychological side effects, including mood changes (e.g.anxiety), changes in activity (most often suppression, sometimes related to lethargy, nervousness and insomnia) unusual dreams, depression and cognitive impairment (abnormal thinking, confusion, amnesia), tremors, asthenia, sedation, low blood pressure (which may be accompanied by the occurrence of secondary symptoms, such as palpitations), weakness of cough, bronchospasm, dyspnoea, dry mouth, which may be accompanied by thirst and difficulty swallowing, abdominal pain, diarrhea, bouncing back with stomach contents, indigestion, loss of appetite, disorder skin (including rash), excessive sweating, weakness. Uncommon: hypersensitivity, syndrome of abnormal secretion of antidiuretic hormone, changes in perception, such as depersonalization, hallucinations, agitation, mood changes, anxiety, confusion, dysphoria, euphoria, decreased libido, emotional instability, changes in taste, visual disturbances, hyperaural sensitivity, addiction drug, increased or decreased muscle tone, involuntary muscle contractions, hypoaesthesia, paresthesia, impaired coordination, malaise, dizziness, amnesia, taste disturbances, syncope, speech disorders, convulsions, lacrimation, miosis, blurred vision, dizziness , ventricular tachycardia, palpitations (in the context of withdrawal syndrome), vasodilation, facial flushing, increased cough, breathing disorders, pharyngitis, rhinitis, voice changes, hiccups, mouth ulcers, gingivitis, tooth discoloration, dysfunction phagia, belching, gastritis, gastrointestinal disorders, intestinal obstruction, stomatitis, flatulence, increased liver enzymes, dry skin, exfoliative dermatitis, muscle stiffness, urinary disorders (urinary retention, increased need to urinate), contraction ureters, decreased libido, impotence, accidental injury, tolerance to the drug, pain (e.g. chest pain), swelling, migraine, physical dependence with withdrawal symptoms, allergic reactions, peripheral edema, malaise, thirst, fever, chills. Rare: lymphadenopathy, dehydration, seizures, especially in patients with epilepsy or in patients with a tendency to convulsions, muscle spasms, hypotension, orthostatic hypotension, bleeding gums, increased appetite, tarry stools, urticaria, symptoms of herpes simplex, increased sensitivity to light, hematuria, weight gain or loss, connective tissue inflammation. Frequency unknown: anaphylactic reaction, anaphylactoid reaction, increased pain sensation, caries, biliary colic, cholestasis, amenorrhea. It can develop tolerance and addiction. Long-term use of the drug may lead to physical dependence and withdrawal syndrome after abrupt cessation of treatment. Symptoms of abstinence from opioids (or withdrawal syndrome) are characterized by the occurrence of some or all of the following symptoms: anxiety, tearing, rhinorrhea, yawning, excessive sweating, chills, muscle pain, mydriasis and palpitation. There may also be other symptoms, including: irritability, anxiety, back pain, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhea or high blood pressure, increased respiratory rate and pulse rate.

Orally. Dosage depends on the intensity of pain and the individual sensitivity of the patient to treatment.Adults and youth> 12 y. Dose adjustment. The usual starting dose for non-opioid patients is 10 mg every 12 hours. Some patients may respond to a starting dose of 5 mg, which reduces the incidence of side effects. In patients who have been taking opioids in the past, treatment may be started with higher doses, taking into account their previous experience with opioid therapy. According to clinical trials, 10-13 mg oxycodone hydrochloride in sustained release form corresponds to approximately 20 mg of morphine sulphate in sustained release form. In the event of a change in therapy with other opioids, it is recommended to start treatment with prolonged-release tablets, giving 50% -75% of the calculated dose of oxycodone.Some patients taking oxycodone prolonged-release tablets according to an established schedule need analgesics in a rapid-release form to suppress breakthrough pain. The drug is not recommended for the treatment of acute and / or breakthrough pain. A single dose of fast-relief formulation should be 1/6 of the daily dose of oxycodone in the form of prolonged-release tablets. Using a quick relief formulation more than twice daily means that the oxycodone prolonged-release tablet dose should be increased. The dose should not be increased more frequently than every 1-2 days until a fixed dose administered twice a day is fixed. Increasing the dose from 10 mg to 20 mg administered every 12 hours should be done gradually, by about 1/3 of the daily dose. The aim is to establish a patient-specific dosage that, in a double daily dose, allows adequate relief of pain with tolerable side effects and the use of such a small dose of a pain relief agent as soon as possible throughout the treatment. For most patients, it is effective to administer the same dose in the morning and evening (every 12 hours). For some patients, uneven distribution of doses over a 24-hour period may be beneficial. The lowest effective dose should be administered. In the treatment of non-cancer pain, a dose of 40 mg / day is usually sufficient, but a higher dose may be necessary. Patients with cancer pain may require a dose of 80-120 mg, which can be increased to 400 mg in individual cases. If higher doses are required, this should be considered individually taking into account the patient's effectiveness, tolerability and the risk of side effects. The drug should not be used longer than necessary. If long-term therapy is needed due to the type and severity of the disease, careful and regular monitoring is recommended to determine if and to what extent treatment should be continued.Discontinuation of treatment. If therapy is no longer indicated, it is recommended to gradually reduce the daily dose to prevent symptoms of withdrawal syndrome.Special groups of patients. In patients> 65 years, there is usually no need to adjust the dose. However, in malnourished, elderly patients who have not previously used opioids, the usual starting dose is 5 mg every 12 hours. Patients at risk, for example, kidney or liver failure, low body weight or slowed drug metabolism, not previously taking opioids, should receive half the initial dose for adults. Therefore, the lowest recommended dose, i.e. 10 mg, may not be adequate as the starting dose. The increase in dose should be carried out in accordance with the individual clinical condition of the patient. The drug is not recommended for use in children <12 y.Method of administration. The drug should be administered twice a day, with meals or regardless of meals with enough liquid. 5 mg prolonged-release tablets: swallow whole, do not chew. 10 mg, 20 mg, 40 mg, 80 mg prolonged-release tablets: swallow whole or break the tablet into two parts, do not chew.