• Home
  • A-B index
  • Pharmacological Index
  • Drug Classes
  • Active Ingredients
  • Companies
  • News
  • Oxycontin
    / Rafa


    Active Ingredient
    Oxycodone HCl 10, 20, 40, 80 mg

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Controlled-Release Tablets

    20 X 10 mg

    partial basket chart 9404 15028

    Controlled-Release Tablets

    20 X 20 mg

    partial basket chart 9405 15029

    Controlled-Release Tablets

    20 X 40 mg

    partial basket chart 35562 15102

    Controlled-Release Tablets

    20 X 80 mg

    partial basket chart 35563 15103

    Related information


    Dosage

    Elderly and adults over 18 years: Tablets should be taken at 12-hourly intervals. The dosage is dependent on the severity of the pain, and the patient’s previous history of analgesic requirements. It is not intended for use as a prn analgesic. Increasing severity of pain will require an increased dosage of tablets using the 5 mg, 10 mg, 20 mg, 40 mg or 80 mg tablet strengths, either alone or in combination, to achieve pain relief. The correct dosage for any individual patient is that which controls the pain and is well tolerated for a full 12 hours. Patients should be titrated to pain relief unless unmanageable adverse drug reactions prevent this. If higher doses are necessary increases should be made, where possible, in 25% – 50% increments. The need for escape medication more than twice a day indicates that the dosage of tablets should be increased. The usual starting dose for opioid naïve patients or patients presenting with severe pain uncontrolled by weaker opioids is 10 mg, 12-hourly. Some patients may benefit from a starting dose of 5 mg to minimise the incidence of side effects. The dose should then be carefully titrated, as frequently as once a day if necessary, to achieve pain relief. For the majority of patients, the maximum dose is 200 mg 12- hourly. However, a few patients may require higher doses. Doses in excess of 1000 mg have been recorded. Patients receiving oral morphine before therapy should have their daily dose based on the following ratio: 10 mg of oral oxycodone is equivalent to 20 mg of oral morphine. It must be emphasised that this is a guide to the dose of tablets required. Inter-patient variability requires that each patient is carefully titrated to the appropriate dose. Controlled pharmacokinetic studies in elderly patients (aged over 65 years) have shown that, compared with younger adults, the clearance of oxycodone is only slightly reduced. No untoward adverse drug reactions were seen based on age, therefore adult doses and dosage intervals are appropriate.
    Pediatric use: OxyContin 10, 20, 40, 80: should not be used in patients under 18 years of age. OxyContin 5: Safety and effectiveness in pediatric patients below the age of 18 years have not been established.
    Adults with mild to moderate renal impairment and mild hepatic impairment: The plasma concentration in this population may be increased. Therefore dose initiation should follow a conservative approach. Patients should be started on OxyContin 5 mg 12-hourly or oxycodone HCl liquid 2.5 mg 6-hourly and titrated to pain relief as described above.
    Use in non-malignant pain: Opioids are not first line therapy for chronic non-malignant pain, nor are they recommended as the only treatment. Types of chronic pain which have been shown to be alleviated by strong opioids include chronic osteoarthritic pain and intervertebral disc disease. The need for continued treatment in non-malignant pain should be assessed at regular intervals.
    Cessation of therapy: When a patient no longer requires therapy with oxycodone, it may be advisable to taper the dose gradually to prevent symptoms of withdrawal.


    Indications

    Moderate to severe chronic pain.


    Contra-Indications

    Hypersensitivity to any of the constituents, respiratory depression, head injury, known or suspected paralytic ileus and GI obstruction, acute abdomen, delayed gastric emptying, chronic obstructive airways disease, cor pulmonale, severe bronchial asthma, hypercarbia, known oxycodone sensitivity or in any situation where opioids are contra-indicated, moderate to severe hepatic impairment, severe renal impairment (creatinine clearance <10 ml/min), chronic constipation, concurrent administration of monoamine oxidase inhibitors or within 2 weeks of discontinuation of their use. Not recommended for pre-operative use or for the first 24 hours post-operatively. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take the 5 mg strength. Pregnancy.


    Special Precautions

    The major risk of opioid excess is respiratory depression. Closely monitor patients for respiratory depression when initiating therapy with this drug and following dose increases. Instruct patients on proper administration of tablets to reduce the risk As with all narcotics, a reduction in dosage may be advisable in hypothyroidism. Use with caution in patients with raised intracranial pressure, hypotension, hypovolaemia, toxic psychosis, diseases of the biliary tract, pancreatitis, inflammatory bowel disorders, prostatic hypertrophy, adrenocortical insufficiency, alcoholism, delirium tremens, chronic renal and hepatic disease or severe pulmonary disease, and debilitated, elderly patients. The oxycodone may aggravate convulsions in patients with convulsive disorders, and may induce or aggravate seizures in some clinical settings. Monitor patients with a history of seizure disorders for worsened seizure control during therapy.
    Tablets should not be used where there is a possibility of paralytic ileus occurring. Should paralytic ileus be suspected or occur during use, tablets should be discontinued immediately. As with all opioid preparations, patients about to undergo additional pain relieving procedures (e.g. surgery, plexus blockade) should not receive tablets for 12 hours prior to the intervention. If further treatment with tablets is indicated then the dosage should be adjusted to the new post-operative requirement.
    80 mg should not be used in patients not previously exposed to opioids. This tablet strength may cause fatal respiratory depression when administered to opioid naïve patients. As with all opioid preparations, tablets should be used with caution following abdominal surgery as opioids are known to impair intestinal motility and should not be used until the physician is assured of normal bowel function. For appropriate patients who suffer with chronic non-malignant pain, opioids should be used as part of a comprehensive treatment programme involving other medications and treatment modalities. A crucial part of the assessment of a patient with chronic non-malignant pain is the patient’s addiction and substance abuse history. There is potential for development of psychological dependence (addiction) to opioid analgesics, including oxycodone.  Tablets, like all opioids, should be avoided in patients with a history of, or present alcohol and drug abuse. If opioid treatment is considered appropriate for the patient, then the main aim of treatment is not to minimise the dose of opioid but rather to achieve a dose which provides adequate pain relief with a minimum of side effects. There must be frequent contact between physician and patient so that dosage adjustments can be made. It is strongly recommended that the physician defines treatment outcomes in accordance with pain management guidelines. The physician and patient can then agree to discontinue treatment if these objectives are not met. Hyperalgesia that will not respond to a further dose increase  may very rarely occur in particular in high doses. A dose reduction or change in opioid may be required. This drug has an abuse profile similar to other strong opioids. It may be sought and abused by people with latent or manifest addiction disorders. As with other opioids, infants who are born to dependent mothers may exhibit withdrawal symptoms and may have respiratory depression at birth. Tablets must be swallowed whole, and not broken, chewed or crushed. The administration of broken, chewed or crushed tablets leads to a rapid release and absorption of a potentially fatal dose of oxycodone.
    OxyContin 10, 20, 40, 80: There have been post-marketing reports of difficulty in swallowing tablets. These reports included choking, gagging, regurgitation and tablets stuck in the throat. Instruct patients not to pre-soak, lick or otherwise wet tablets prior to placing in the mouth, and to take one tablet at a time with enough water to ensure complete swallowing immediately after placing in the mouth. There have been rare post-marketing reports of cases of intestinal obstruction, and exacerbation of diverticulitis, some of which have required medical intervention to remove the tablet. Patients with underlying GI disorders such as esophageal cancer or colon cancer with a small gastrointestinal lumen are at greater risk of developing these complications. Use caution when prescribing for patients who have difficulty swallowing or have underlying GI disorders that may predispose them to obstruction. Consider use of an alternative analgesic in patients who have difficulty swallowing and patients at risk for underlying GI disorders resulting in a small gastrointestinal lumen. Concomitant use of alcohol and may increase the undesirable effects; concomitant use should be avoided. Abuse of the tablets by parenteral administration can be expected to result in other serious adverse events, such as local tissue necrosis, infection, pulmonary granulomas, increased risk of endocarditis, and valvular heart injury, which may be fatal.
    For full details see prescribing information.


    Side Effects

    Adverse drug reactions are typical of full opioid agonists. Tolerance and dependence may occur. Constipation may be prevented with an appropriate laxative. If nausea and vomiting are troublesome, oxycodone may be combined with an anti-emetic.
    Metabolism and nutritional disorders: Decreased appetite, Anorexia.
    Respiratory, thoracic and mediastinal disorders: Bronchospasm Dyspnoea Cough decreased.
    Psychiatric disorders: Anxiety, Confusional state, Insomnia, Nervousness, Thinking abnormal, Abnormal dreams, Depression.
    Nervous system disorders: Headache, Dizziness, Sedation, Somnolence, Tremor.
    Gastrointestinal disorders: Constipation, Nausea, Vomiting, Dry mouth, Dyspepsia, Abdominal Pain, Diarrhoea.
    Skin and subcutaneous tissue disorders: Hyperhidrosis, Pruritus, Rash.
    General disorders and administration site conditions: Asthenic conditions.
    Tolerance and Dependence: The patient may develop tolerance to the drug with chronic use and require progressively higher doses to maintain pain control. Prolonged use tablets may lead to physical dependence and a withdrawal syndrome may occur upon abrupt cessation of therapy. When a patient no longer requires therapy with oxycodone, it may be advisable to taper the dose gradually to prevent symptoms of withdrawal. The opioid abstinence or withdrawal syndrome is characterised by some or all of the following: restlessness, lacrimation, rhinorrhea, yawning, perspiration, chills, myalgia, mydriasis and palpitations. Other symptoms also may develop, including: irritability, anxiety, backache, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhoea, or increased blood pressure, respiratory rate or heart rate.
    For full details see prescribing information.


    Drug interactions

    Like other opioids, potentiates the effects of tranquillisers, anaesthetics, hypnotics, anti-depressants, sedatives, phenothiazines, neuroleptic drugs, other opioids, muscle relaxants and antihypertensives. Monoamine oxidase inhibitors are known to interact with narcotic analgesics, producing CNS excitation or depression with hypertensive or hypotensive crisis. Concurrent use  and other central nervous system (CNS) depressants including sedatives or hypnotics, general anesthetics, phenothiazines, tranquilizers, and alcohol can increase the risk of respiratory depression, hypotension, profound sedation or coma. Monitor patients receiving CNS depressants and  for signs of respiratory depression and hypotension. When such combined therapy is contemplated, reduce the initial dose  and consider using a lower dose of the concomitant CNS depressant. Alcohol may enhance the pharmacodynamic effects; concomitant use should be avoided. Mixed Agonist/Antagonist Opioid Analgesics (i.e., pentazocine, nalbuphine, and butorphanol) – should generally not be administered to a patient who has received or is receiving a course of therapy with a pure opioid agonist analgesic such as this drug. In this situation, mixed agonist/antagonist analgesics may reduce the analgesic effect of oxycodone and may precipitate withdrawal symptoms in these patients.
    Diuretics – opioids can reduce the efficacy of diuretics by inducing the release of antidiuretic hormone. opioids may also lead to acute retention of urine by causing spasm of the sphincter of the bladder, particularly in men with enlarged prostates. Anticholinergics or other medications with anticholinergic activity – when used concurrently with opioid analgesics may result in increased risk of urinary retention and/or severe constipation, which may lead to paralytic ileus. Monitor patients for signs of urinary retention or reduced gastric motility when its is used concurrently with anticholinergic drugs. this drug is metabolized in part via the CYP2D6 and CYP3A4 pathways. The activities of these metabolic pathways may be inhibited or induced by various co-administered drugs or dietary elements. Oxycodone doses may need to be adjusted accordingly.
    Cimetidine and CYP3A4 inhibitors, such as macrolide antibiotics (e.g., clarithromycin, erythromycin), azole-antifungal agents (e.g., ketoconazole, voriconazole), and protease inhibitors (e.g., ritonavir), may cause decreased clearance of oxycodone which could lead to an increase in oxycodone plasma concentrations.
    CYP3A4 inducers, such as rifampin, carbamazepine, and phenytoin, may induce the metabolism of oxycodone and cause increased clearance of the drug, resulting in a decrease in oxycodone plasma concentrations.Drugs that inhibit CYP2D6 activity, such as paroxetine and quinidine, may cause decreased clearance of oxycodone which could lead to an increase in oxycodone plasma concentrations.
    For full details see prescribing information.


    Pregnancy and Lactation

    Tablets are not recommended for use in pregnancy nor during labour. Infants born to mothers who have received opioids during pregnancy should be monitored for respiratory depression. Oxycodone may be secreted in breast milk and may cause respiratory depression in the newborn. Tablets should, therefore, not be used in breast-feeding mothers.


    Overdose

    Signs of oxycodone toxicity and overdose: miosis, respiratory depression, hypotension and hallucinations. Circulatory failure and somnolence progressing to stupor or deepening coma, hypotonia, bradycardia, and death may occur in more severe cases.
    The effects of overdose will be potentiated by the simultaneous ingestion of alcohol or other psychotropic drugs.
    Treatment of oxycodone overdose: Primary attention should be given to the establishment of a patent airway and institution of assisted or controlled ventilation. In the case of massive overdose, administer naloxone intravenously (0.4 to 2 mg for an adult and 0.01 mg/kg body weight for children), if the patient is in a coma or respiratory depression is present. Repeat the dose at 2 minute intervals if there is no response. If repeated doses are required then an infusion of 60% of the initial dose per hour is a useful starting point. A solution of 10 mg made up in 50 ml dextrose will produce 200 micrograms/ml for infusion using an IV pump (dose adjusted to the clinical response). Infusions are not a substitute for frequent review of the patient’s clinical state. Intramuscular naloxone is an alternative in the event IV access is not possible. As the duration of action of naloxone is relatively short, the patient must be carefully monitored until spontaneous respiration is reliably re-established. Naloxone is a competitive antagonist and large doses (4 mg) may be required in seriously poisoned patients.
    For less severe overdose, administer naloxone 0.2 mg intravenously followed by increments of 0.1 mg every 2 minutes if required. The patient should be observed for at least 6 hours after the last dose of naloxone. Naloxone should not be administered in the absence of clinically significant respiratory or circulatory depression secondary to oxycodone overdose. Naloxone should be administered cautiously to persons who are known, or suspected, to be physically dependent on oxycodone. In such cases, an abrupt or complete reversal of opioid effects may precipitate pain and an acute withdrawal syndrome. Additional/other considerations:
    – Consider activated charcoal (50 g for adults, 10 -15 g for children), if a substantial amount has been ingested within 1 hour, provided the airway can be protected. It may be reasonable to assume that late administration of activated charcoal may be beneficial for prolonged release preparations; however there is no evidence to support this.
    – Tablets will continue to release and add to the oxycodone load for up to 12 hours after administration and management of oxycodone overdose should be modified accordingly. Gastric contents may need to be emptied as this can be useful in removing unabsorbed drug, particularly when a prolonged release formulation has been taken.


    Manufacturer
    Rafa Laboratories Ltd.
    CLOSE