Index of drugs

Moderate to severe pain.

1 ml of solution contains 10 mg of oxycodone hydrochloride.

Opioid analgesic, a pure agonist of opioid receptors (mi, kappa and delta) in the brain, spinal cord and peripheral organs. Opioids may have an effect on the hypothalamic-pituitary-adrenal axis or hypothalamic-pituitary-gonadal axis (increase in prolactin and decrease in blood levels of cortisol and testosterone). Oxycodone is associated with plasma proteins in approximately 45%. It is metabolized in the intestine and liver with the participation of cytochrome P-450 to noroxycodone, oxymorphone and other glucuronide conjugates. Metabolites show little pharmacological activity. Oxycodone and its metabolites are excreted in urine and faeces. The drug penetrates the placenta and into breast milk. In elderly patients, oxycodone blood levels are approximately 15% higher than in young patients. Women have an average of 25% higher blood oxycodone concentrations than men. In patients with mild to severe hepatic impairment, oxycodone and noroxycodone concentrations are higher and oxymorphone concentrations are lower compared to healthy patients, T_0,5 oxycodone can be extended. In patients with mild to severe renal impairment, oxycodone and its metabolites reach higher values ​​compared to healthy subjects, T_0,5 oxycodone can be extended.

Hypersensitivity to the components of the preparation. Severe respiratory depression with hypoxia and / or hypercapnia. Severe chronic obstructive pulmonary disease. Pulmonary heart. Severe bronchial asthma. Intestinal paralysis.

Particularly cautiously use in patients with alcohol and drug misuse. Carefully use in elderly, weakened patients with severe lung, liver or kidney disorders, with mucous edema, hypothyroidism, Addison's disease, benign prostatic hyperplasia, acute organic psychosis after poisoning (eg alcohol), alcohol depilation, found addiction to opioids, pancreatitis, cholelithiasis, obstructive pulmonary disease, inflammatory bowel diseases, increased intracranial pressure and reduced ability to maintain proper blood pressure, epilepsy or prone to convulsions and treated with an MAO inhibitor. In case of occurrence or suspected paralytic ileus, the preparation should be immediately discontinued. Caution should be exercised before surgery, during surgery and within 12-24 hours after surgery. The use of oxycodone as a doping agent is life-threatening. The main risk associated with opioid overdose is respiratory depression, which most often affects elderly or debilitated patients. Respiratory depression caused by oxycodone can lead to the retention of carbon dioxide in the blood and secondary in the cerebrospinal fluid. In susceptible individuals, opioids can cause severe hypotension. During long-term use, the patient may develop tolerance to the drug and it will be necessary to gradually increase the dose to maintain a constant relief of pain. In general, there is also cross-tolerance to other opioids. Chronic use of the preparation may lead to physical and mental dependence, and in the case of a sudden discontinuation of treatment - to the development of withdrawal syndrome. The types and prevalence of oxycodone abuse are similar to those observed with other potent opioids. It is not recommended for use in children under 12 years of age due to insufficient data on safety and efficacy in this age group.

Oxycodone should not be used during pregnancy unless clearly necessary. Prolonged use of oxycodone during pregnancy may lead to withdrawal symptoms in the newborn. When given during delivery, the fetus may develop respiratory depression. Oxycodone is excreted in breast milk.Do not use the product during breast-feeding.

Very common: sedation (drowsiness up to consciousness disorders), dizziness and headache, constipation, nausea, vomiting, pruritus. Common: loss or loss of appetite, changes in mood and personality (including anxiety, depression, euphoria), reduced activity, anxiety, excessive psychomotor activity, agitation, nervousness, insomnia, abnormal thinking, confusion, fainting, paresthesia, hypotension, dyspnoea, abdominal pain, diarrhea, dry mouth, hiccups, indigestion, skin reactions / rash, urinary retention, painful urination, sudden urge to blisters, excessive sweating (also with chills), weakness. Uncommon: perceptual disorders (eg hallucinations, lack of consciousness), hypersensitivity reactions, decreased sex drive, concentration disorders, migraine, dysgeusia, increased muscle tone, muscle tremors, uncontrolled muscle movements, hypoesthesia, concentration disorders, visual disturbances, hearing disorders dizziness, tachycardia, vasodilation, voice changes, cough, mouth ulcers, oral mucositis, flatulence, belching, biliary colic, erectile dysfunction, physical dependence including withdrawal symptoms, pain (including pain in the chest), malaise, edema, accidental injuries. Rare: herpes, dehydration, increased appetite, seizures (especially in patients with epilepsy or prone to seizures), amnesia, palpitations, tarry stools, tooth diseases, bleeding gums, dysphagia, dry skin, atrophy of menses, increase or decrease weight, thirst. Very rare: anaphylactic reactions, speech disorders, intestinal obstruction, increased liver enzymes, urticaria. Frequency unknown: psychological dependence, tachyphylaxis. Due to its pharmacological properties, oxycodone may cause: respiratory depression, miosis, bronchospasm and smooth muscle contraction, and may suppress the cough reflex.

Adults and children over 12 years.intravenous (after dilution in 0.9% NaCl, 5% Glucose or water for injections).Intravenous bolus: 1-10 mg for 1-2 min, in the case of acute pain, the dose should be increased until the optimal analgesic effect is obtained; if the pain relieves, the dose may be repeated, usually every 4 hours.Infusion: 2 mg / h as the starting dose.Patient-controlled analgesia0.03 mg / kg in the form of a bolus, with a refraction time of at least 5 minutes.subcutaneous (if necessary, the preparation can be diluted with 0.9% NaCl solution, 5% glucose or water for injections).Subcutaneous bolus: 5 mg as the starting dose, in case of acute pain the dose should be increased until the optimal analgesic effect is obtained; if the pain relieves, the dose may be repeated, usually every 4 hours.Subcutaneous infusion: 7.5 mg daily as the starting dose, the dose should be gradually increased depending on the symptoms.Change from oral to parenteral: 2 mg oral oxycodone corresponds to approximately 1 mg of oxycodone in the parenteral form. Due to the high individual variability among patients, the dose should be increased with caution. Patients with pain in the course of a neoplastic disease in whom oral administration is changed to parenteral administration may require significantly higher doses.Change from the parenteral form of morphine to oxycodone. The basis for the gradual increase in the dose in each patient is the dose ratio of the equivalent intravenous form of morphine relative to oxycodone level 1: 0.7. This factor should be applied by gradually increasing the dose in each patient. Then the dose of the drug may be gradually increased depending on the severity of pain and the individual sensitivity of the patient. Of particular importance for dose adaptation is consideration of previous patient's responses to treatment with both opioid and other medications, as well as current patient's needs for analgesia (dynamic changes in pain intensity, e.g. in post-operative pain; organ and system function disorders, e.g. metabolism, interaction with other medicines used simultaneously, e.g.affecting o.u.n .; possible partial cross-tolerance to other opioids, previously administered in high doses).
The preparation should not be administered for longer than absolutely necessary. If it is necessary to treat pain for a long time due to the nature and severity of the disease, the patient should be carefully monitored to determine if further treatment is needed, and if so, to what extent. The lowest effective analgesic dose should be used. The initial dose in patients previously treated with opioids may be higher. In the case of acute pain after surgical procedures, a correspondingly higher dose should be applied, depending on previous experience. The gradual increase in dose over time may be necessary if the relief of pain is not sufficient or the intensity of pain increases. In the event of symptoms of overdose, e.g. sedation, the dose should be reduced.
Elderly patients who do not have clinically apparent liver or kidney problems are generally not required to adjust their dosage. Patients at high risk, such as those with renal or hepatic impairment, low body weight or slow metabolic drugs who have not been treated with opioids before, should receive an initial dose that is half the amount normally recommended in adults.