Page 1 of 30 SCHEDULING STATUS

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1 SCHEDULING STATUS S6 PROPRIETARY NAMES AND DOSAGE FORM OxyContin 5 mg Prolonged Release Tablets OxyContin 10 mg Prolonged Release Tablets OxyContin 20 mg Prolonged Release Tablets OxyContin 40 mg Prolonged Release Tablets OxyContin 80 mg Prolonged Release Tablets COMPOSITION Each OxyContin 5 mg Prolonged Release Tablet contains 5 mg of oxycodone hydrochloride. Each OxyContin 10 mg Prolonged Release Tablet contains 10 mg of oxycodone hydrochloride. Each OxyContin 20 mg Prolonged Release Tablet contains 20 mg of oxycodone hydrochloride. Each OxyContin 40 mg Prolonged Release Tablet contains 40 mg of oxycodone hydrochloride. Each OxyContin 80 mg Prolonged Release Tablet contains 80 mg of oxycodone hydrochloride. Inactive ingredients: Tablet core: ammoniomethacrylate co-polymer, lactose monohydrate, magnesium stearate, povidone, stearyl alcohol, talc, triacetin. Tablet coat: hypromellose, macrogol, talc, titanium dioxide. OxyContin 5 mg contains Brilliant blue FCF aluminium lake. OxyContin 10 mg contains hydroxypropylcellulose and no additional colourant. OxyContin 20 mg contains polysorbate and iron oxide red. OxyContin 40 mg contains polysorbate and iron oxide yellow. OxyContin 80 mg contains hydroxypropylcellulose, iron oxide yellow and indigo carmine. Contains sugar (lactose monohydrate). PHARMACOLOGICAL CLASSIFICATION A 2.9 Other Analgesics PHARMACOLOGICAL ACTION Pharmacodynamic properties: Oxycodone is a full opioid agonist with no antagonist properties. It has affinity for kappa, mu and delta opiate receptors in the brain and spinal cord. Oxycodone is similar to morphine in its action. The therapeutic effect is mainly analgesic, anxiolytic and sedative (see INDICATIONS). Pharmacokinetic properties: Page 1 of 30

2 Oxycodone has an absolute bioavailability of up to 87 % following oral administration. Oxycodone is metabolised principally to noroxycodone via CYP450-3A and oxymorphone via CYP450-2D6. Oxymorphone has some analgesic activity but is present in plasma in low concentrations and is not considered to contribute to oxycodone s pharmacological effect. Oxycodone has an elimination half-life of approximately 3 hours. The release of oxycodone from OxyContin Prolonged Release Tablets is biphasic with an initial relatively fast release providing an early onset of analgesia followed by a more controlled release that determines the 12-hour duration of action. The mean apparent elimination half-life of OxyContin Prolonged Release Tablets is 4,5 hours which leads to steady state being achieved in about one day. OxyContin Prolonged Release Tablets have an oral bioavailability comparable with conventional oral oxycodone, but the former achieve maximal plasma concentrations at about 3 hours rather than about 1 to 1,5 hours. Peak and trough concentrations of oxycodone from OxyContin 10 mg Prolonged Release Tablets administered 12 hourly are equivalent to those achieved from conventional oxycodone 5 mg administered 6 hourly. OxyContin 5 mg, 10 mg, 20 mg, 40 mg and 80 mg Prolonged Release Tablets are bioequivalent in terms of both rate and extent of absorption. Ingestion of a standard high-fat meal does not alter peak oxycodone concentration or the extent of oxycodone absorption from OxyContin Prolonged Release Tablets. Elderly: The AUC in elderly subjects is 15 % greater when compared with younger subjects. Gender: Female subjects have, on average, plasma oxycodone concentrations up to 25 % higher than males on a body weight adjusted basis. The reason for this difference is unknown. Patients with renal impairment: Preliminary data from a study of patients with mild to moderate renal dysfunction show peak plasma oxycodone and noroxycodone concentrations approximately 50 % and 20 % higher, respectively and AUC values of oxycodone, noroxycodone and oxymorphone approximately 60 %, 60 % and 40% higher than normal subjects, respectively. There was an increase in t 1/2 of elimination for oxycodone of only 1 hour. Patients with mild to moderate hepatic impairment: Patients with mild to moderate hepatic dysfunction showed peak plasma oxycodone and noroxycodone concentrations approximately 50 % and 20 % higher, respectively, than normal subjects. AUC values were approximately 95 % and 75 % higher, respectively. Oxymorphone peak plasma concentrations and AUC values were lower by 15 % to 50 %. The t 1/2 elimination for oxycodone increased by 2,3 hours. INDICATIONS OxyContin Prolonged Release Tablets are indicated for the treatment of moderate to severe pain in patients with cancer and post-operative pain after gastrointestinal function has returned. Page 2 of 30

3 OxyContin Prolonged Release Tablets are indicated for the treatment of severe pain requiring the use of a strong opioid analgesic. CONTRAINDICATIONS OxyContin Prolonged Release Tablets are contraindicated in patients with known hypersensitivity to oxycodone or to any of the excipients or in any situation where opioids are contraindicated (see COMPOSITION). OxyContin Prolonged Release Tablets are contraindicated in patients presenting with respiratory depression, with hypoxia and/or hypercapnia from any cause, paralytic ileus, acute abdomen, delayed gastric emptying, chronic obstructive lung disease, cor pulmonale, chronic bronchial asthma, moderate to severe hepatic impairment, severe renal impairment (creatinine clearance < 10 ml/min), chronic constipation. OxyContin Prolonged Release Tablets are contraindicated in patients on concurrent administration of monoamine oxidase inhibitors or within 2 weeks of discontinuation of their use. OxyContin Prolonged Release Tablets must not be used during pregnancy or lactation (see PREGNANCY AND LACTATION). OxyContin Prolonged Release Tablets are not recommended for pre-operative use or for the first hours post-operatively. Patients with rare hereditary problems of galactose intolerance eg. galactosaemia, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. WARNINGS and SPECIAL PRECAUTIONS The major risk is respiratory depression. A reduction in dosage may be advisable in hypothyroidism. OxyContin Prolonged Release Tablets should be used with caution in patients with head injury (due to risk of increased intracranial pressure), hypotension, hypovolaemia, toxic psychosis, disease of the biliary tract, pancreatitis, inflammatory bowel disorders, prostatic hypertrophy, adrenocortical insufficiency, Addison s disease, myxoedema, alcoholism, delirium tremens, impaired renal or hepatic function, debilitated elderly and infirm patients. OxyContin Prolonged Release Tablets should be used with caution in patients taking MAO inhibitors or other CNS depressants, including alcohol or benzodiazepines (see INTERACTIONS). OxyContin Prolonged Release Tablets should not be used where there is a possibility of paralytic ileus occurring. Should paralytic ileus be suspected or occur during use, OxyContin Prolonged Release Tablets should be discontinued immediately. Patients who are to undergo cordotomy or other pain relieving surgical procedures should not receive OxyContin Prolonged Release Tablets for 24 hours before surgery or within the first hours post-operatively. If further treatment with OxyContin Prolonged Release Tablets is then indicated the dosage should be adjusted to the new post-operative requirement. Page 3 of 30

4 OxyContin 80 mg Prolonged Release Tablets should not be used in patients not previously exposed to opioids. These tablets strength may cause fatal respiratory depression when administrated to opioid naïve patients. OxyContin Prolonged Release Tablets should be used with caution following abdominal surgery as opioids are known to impair intestinal motility and should not be used until the medical practitioner 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. OxyContin Prolonged Release Tablets has an abuse liability similar to other strong opioids and should be used with caution in opioid dependent patients and in patients with a history of alcohol and drug abuse. Oxycodone may be sought and abused by people with latent or manifest addiction disorders. OxyContin Prolonged Release Tablets should be used with particular care in patients with a history of 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 that provides adequate pain relief with minimum side effects. There must be frequent contact between the medical practitioner and the patient so that the dosage adjustments can be made. It is strongly suggested that the medical practitioner defines treatment outcomes in accordance with pain management guidelines. The medical practitioner and patient can then agree to discontinue treatment if these objectives are not met. Tolerance and dependence: The patient may develop tolerance to OxyContin Prolonged Release Tablets with chronic use and require progressively higher doses to maintain pain control. Prolonged use of OxyContin Prolonged Release 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. For detail on withdrawal symptoms, please see SIDE EFFECTS. Infants who are born to dependent mothers may exhibit withdrawal symptoms and may have respiratory depression at birth. Page 4 of 30

5 OxyContin Prolonged Release Tablets must be swallowed whole and not broken, chewed or crushed. The administration of broken, chewed or crushed OxyContin Prolonged Release Tablets leads to a rapid release and absorption of a potentially fatal dose of oxycodone. 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 that might be fatal. Hyperalgesia that will not respond to a further dose increase of oxycodone may occur, in particular in high doses. An oxycodone dose reduction or change in opioid may be required to re-establish patient analgesia. OxyContin Prolonged Release Tablets should not be pre-soaked, licked or otherwise made wet prior to placing in the mouth, and must be taken one tablet at a time with enough water to ensure complete swallowing immediately after placing in the mouth. Patients with underlying GI disorders such as oesophageal cancer or colon cancer with a small gastrointestinal lumen are at greater risk of developing complications (intestinal obstruction, and exacerbation of diverticulitis, which may require medical intervention to remove the tablet). Caution should be used when prescribing OxyContin Prolonged Release Tablets for patients who have difficulty swallowing or having underlying GI disorders that may predispose them to obstruction. Contains lactose. Patients with the rare hereditary conditions of galactose intolerance e.g. galactosaemia, Lapp lactase deficiency, glucose-galactose malabsorption etc. should not take OxyContin Prolonged Release Tablets. Effect on the ability to drive or use machines: Oxycodone may modify patients reactions to a varying extent depending on the dosage and individual susceptibility. Therefore, patients should not drive or operate machinery if affected. INTERACTIONS OxyContin Prolonged Release Tablets potentiates the effects of tranquillisers, anaesthetics, hypnotics, anti-depressants, sedatives, phenothiazines, neuroleptic medicines, alcohol, other opioids, muscle relaxants and antihypertensives. Concomitant administration of oxycodone with anticholinergics or medications with anticholinergic activity (e.g. tricyclic antidepressants, antihistamines, antipsychotics, muscle relaxants, anti-parkinson medicines) may result in increased anticholinergic adverse effects. Monoamine oxidase inhibitors are known to interact with narcotic analgesics, producing CNS excitation or depression with hypertensive or hypotensive crisis. Page 5 of 30

6 Concurrent administration of quinidine, an inhibitor of cytochrome P450-2D6, resulted in an increase in oxycodone C max by 11 %, AUC by 13 % and t 1/2 elimination by 14 %. Also, an increase in noroxycodone level was observed, (C max by 50 %, AUC by 85 % and t 1/2 elimination by 42 %). The pharmacodynamic effects of oxycodone were not altered. This interaction may be observed for other potent inhibitors of cytochrome P450-2D6 enzyme. Oxycodone is metabolised mainly by cytochrome P450-3A with a contribution from cytochrome P450-2D6. The activities of these metabolic pathways may be inhibited or induced by various coadministered medicines or dietary elements. Oxycodone doses may need to be adjusted accordingly. Cimetidine and inhibitors of cytochrome P450-3A such as azole-antifungal agents (e.g. ketoconazole), macrolide antibiotics (e.g. clarithromycin and erythromycin), protease inhibitors (e.g. ritonavir), and grapefruit juice may inhibit the metabolism of oxycodone, which could lead to an increase in oxycodone plasma concentrations. Cytochrome P450-3A inducers, such as rifampin, carbamazepine, phenytoin and St. John s wort, may induce the metabolism of oxycodone and cause increased clearance of the medicine, resulting in a decrease in oxycodone plasma concentrations. Medicines that inhibit cytochrome P450-2D6 activity, such as paroxetine and quinidine, may cause decreased clearance of oxycodone which could lead to an increase in oxycodone plasma concentrations. PREGNANCY AND LACTATION OxyContin Prolonged Release Tablets are contraindicated for the use in pregnancy and during labour. Infants born to mothers who have received OxyContin Prolonged Release Tablets during pregnancy should be monitored for respiratory depression (see CONTRAINDICATIONS). Prolonged use of oxycodone during pregnancy can result in neonatal opioid withdrawal syndrome. Oxycodone may be secreted in breast milk and may cause respiratory depression in the newborn. OxyContin Prolonged Release Tablets should therefore not be used by breast-feeding mothers. DOSAGE AND DIRECTIONS FOR USE OxyContin Prolonged Release Tablets must be swallowed whole and not chewed. Elderly and adults over 18 years: OxyContin Prolonged Release 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. Increasing severity of pain will require an increased dose of OxyContin Prolonged Release Tablets using the 5 mg, 10 mg, 20 mg, 40 mg or 80 mg tablets 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 medicine Page 6 of 30

7 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 OxyContin Prolonged Release Tablets should be increased. The usual starting dose for opioid naïve 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 daily have been recorded. Patients receiving oral morphine before OxyContin Prolonged Release Tablets 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 OxyContin Prolonged Release 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 medicine reactions were seen based on age, therefore adult doses and dosage intervals are appropriate (see Pharmacokinetic properties). Children under 18 years: The safety and efficacy of OxyContin Prolonged Release Tablets in patients under 18 years of age has 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. Opioid naïve patients should be started on OxyContin 5 mg Prolonged Release Tablets 12 hourly and titrated to pain relief as described (see Pharmacokinetic properties). 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. SIDE EFFECTS Adverse medicine 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. The reactions are listed as MeDRA preferred term by system organ class and absolute frequency. Page 7 of 30

8 Body System Frequency of Occurrence Very Common Uncommon Rare Very Rare Not known Common > 1 % and > 0,1 % and > 0,01 % and < < 0,01 % (cannot be > 10 % < 10 % < 1 % 0,1 % estimated from the available data) Gastrointestinal constipation abdominal mouth melaena, tooth dental disorders, nausea, pain, ulceration, disorder, caries vomiting diarrhoea, stomatitis, gingival dry mouth, flatulence, bleeding hiccups, dysphagia dyspepsia (difficulty swallowing tablet), ileus, eructation, regurgitation, retching Hepato-biliary biliary colic, cholestasis disorders increased hepatic enzymes Metabolism and decreased dehydration, increased nutrition apetite appetite disorders Page 8 of 30

9 Nervous system headache, tremor, impaired hyperalgesi disorders dizziness, lethargy concentration a sedation,, migraine, somnolence dysgeusia, hypertonia, muscle contractions involuntary, hypoaesthesi a, abnormal coordination, syncope, paraesthesia, amnesia, convulsion, speech disorder Page 9 of 30

10 Psychiatric altered perception aggression disorders mood and disturbances personalit (e.g. y change hallucination, (e.g. derealisation) anxiety,, decreased depressio libido, affect n), lability, decreased agitation, activity, euphoric restlessne mood, ss, medicine psycho- dependence motor hyperactivi ty, nervousne ss, insomnia, abnormal thinking, confusion al state Infections and herpes simplex infestations Immune system hypersensitivi anaphylacti disorders ty c reaction, anaphylact oid reaction Eye disorders miosis, visual impairment Ear and impaired labyrinth hearing, disorders vertigo Renal and dysuria,mi urinary urinary cturition retention disorders urgency Page 10 of 30

11 Reproductive system and breast disorders Cardiac disorders Vascular disorders Respiratory, thoracic and mediastinal disorders dyspnoea erectile dysfunction, hypogonadis m tachycardia, palpitations (in the context of withdrawal syndrome) vasodilatatio n dysphonia, cough, respiratory depression, choking Hypotension, orthostatic hypotension amenorrho ea Page 11 of 30

12 Skin and pruritus skin dry skin urticaria subcutaneous reactions / tissue disorders rash, hyperhidro sis Injury, injury from poisoning and accidents, procedural medication complications stuck in throat General asthenia, chills, weight neonatal disorders and fatigue medicine increase, medicine administration withdrawal weight withdrawal site conditions syndrome, decrease syndrome pain (e.g. chest pain), malaise, oedema, peripheral oedema, thirst, medicine tolerance Symptoms of withdrawal: Opioid abstinence or withdrawal syndrome is characterised by some or all of the following: restlessness, lacrimation, rhinorrhoea, yawning, perspiration, chills, myalgia and mydriasis. Other symptoms may also develop, including: irritability, anxiety, backache, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhoea or increased blood pressure, respiratory rate or heart rate. The development of psychological dependence (addiction) to opioid analgesics in properly managed patients with pain has been reported to be rare. However, data are not available to establish the true incidence of psychological dependence (addiction) in chronic pain patients. KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT Signs of oxycodone toxicity and overdosage are miosis, respiratory depression, pulmonary oedema and hypotension. Circulatory failure and somnolence progressing to stupor or deepening coma, hypotonia, bradycardia and death may occur in more severe cases. Page 12 of 30

13 Treatment of oxycodone overdosage: primary attention should be given to the establishment of a patent airway and institution of assisted or controlled ventilation. 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 repeat 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 that 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 overdosage, administer naloxone 0,2 mg intravenously followed by increments of 0,1 mg every 2 minutes if required. Naloxone should be administered in the absence of clinically significant respiratory or circulatory depression secondary to oxycodone overdosage. Naloxone should be administered cautiously to persons who are known, or suspected, to be physically dependant 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, 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. OxyContin Prolonged Release Tablets will continue to release and add to the oxycodone load for up to 12 hours after administration and management of oxycodone overdosage should be modified accordingly. IDENTIFICATION OxyContin 5 mg Prolonged Release Tablets are pale blue, round, bi-convex, film coated tablets, imprinted with OC on one side and 5 on the other side. OxyContin 10 mg Prolonged Release Tablets are white, round, bi-convex, film coated tablets, imprinted with OC on one side and 10 on the other side. OxyContin 20 mg Prolonged Release Tablets are pink, round, bi-convex, film coated tablets, imprinted with OC on one side and 20 on the other side. OxyContin 40 mg Prolonged Release Tablets are yellow, round, bi-convex, film coated tablets, imprinted with OC on one side and 40 on the other side. OxyContin 80 mg Prolonged Release Tablets are green, round, bi-convex, film coated tablets, imprinted with OC on one side and 80 on the other side. Page 13 of 30

14 PRESENTATION OxyContin 5 mg Prolonged Release Tablets are supplied in clear PVC and aluminium foil blister packs of 28. OxyContin 10 mg Prolonged Release Tablets are supplied in clear PVC and aluminium foil blister packs of 28. OxyContin 20 mg Prolonged Release Tablets are supplied in clear PVC and aluminium foil blister packs of 28. OxyContin 40 mg Prolonged Release Tablets are supplied in clear PVC and aluminium foil blister packs of 28. OxyContin 80 mg Prolonged Release Tablets are supplied in clear PVC and aluminium foil blister packs of 28. STORAGE INSTRUCTIONS Store at or below 25 ⁰ C. Store in original package in the outer carton in order to protect from light. Store this medicine out of the reach of children. REGISTRATION NUMBERS South Africa: S6 OxyContin 5 mg Prolonged Release Tablets: 41/2.9/1098 OxyContin 10 mg Prolonged Release Tablets: 41/2.9/1099 OxyContin 20 mg Prolonged Release Tablets: 41/2.9/1100 OxyContin 40 mg Prolonged Release Tablets: 41/2.9/1101 OxyContin 80 mg Prolonged Release Tablets: 41/2.9/1102 Namibia: NS4 OxyContin 5 mg Prolonged Release Tablets: 12/2.9/0259 OxyContin 10 mg Prolonged Release Tablets: 12/2.9/0260 OxyContin 20 mg Prolonged Release Tablets: 12/2.9/0261 OxyContin 40 mg Prolonged Release Tablets: 12/2.9/0262 OxyContin 80 mg Prolonged Release Tablets: 12/2.9/0263 Botswana: S1A OxyContin 5 mg Prolonged Release Tablets: BOT OxyContin 10 mg Prolonged Release Tablets: BOT OxyContin 20 mg Prolonged Release Tablets: BOT OxyContin 40 mg Prolonged Release Tablets: BOT Page 14 of 30

15 OxyContin 80 mg Prolonged Release Tablets: BOT NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION Mundipharma (Pty) Ltd 2 nd floor Mariendahl House Newlands on Main Claremont DATE OF PUBLICATION OF THIS PACKAGE INSERT Date of registration: 9 October 2009 Date of this revision: 29 September 2017 = OxyContin is a registered trademark. Page 15 of 30

16 SKEDULERINGSTATUS S6 EIENDOMSNAAM EN DOSEERVORM OxyContin 5 mg Verlengde Vrystellings Tablette OxyContin 10 mg Verlengde Vrystellings Tablette OxyContin 20 mg Verlengde Vrystellings Tablette OxyContin 40 mg Verlengde Vrystellings Tablette OxyContin 80 mg Verlengde Vrystellings Tablette SAMESTELLING Elke OxyContin 5 mg tablet bevat 5 mg oksikodoonhidrochloried. Elke OxyContin 10 mg tablet bevat 10 mg oksikodoonhidrochloried. Elke OxyContin 20 mg tablet bevat 20 mg oksikodoonhidrochloried. Elke OxyContin 40 mg tablet bevat 40 mg oksikodoonhidrochloried. Elke OxyContin 80 mg tablet bevat 80 mg oksikodoonhidrochloried. Onaktiewe bestanddele: Tablet kern: ammoniometakrilaat ko-polimeer, laktosemonohidraat, magnesiumstearaat, povidoon, stearielalkohol, talk en triasetaat. Tablet bedekking: hipromellose, makrogol, talk, titaandioksied. OxyContin 5 mg bevat skitterende blou FCF aluminiumlak kleurstof. OxyContin 10 mg bevat hidroksipropielsellulose en geen addisionele kleurstowwe. OxyContin 20 mg bevat polysorbaat en ysteroksied rooi kleurstof. OxyContin 40 mg bevat polysorbaat en ysteroksied geel kleurstof. OxyContin 80 mg bevat hidroksipropielsellulose, ysteroksied geel en indigo karmyn as kleurstowwe. Bevat suiker: (laktosemonohidraat). FARMAKOLOGIESE KLASSIFIKASIE A 2.9 Ander Analgetika FARMAKOLOGIESE WERKING Farmakodinamiese eienskappe: Oksikodoon is 'n vol opioïed agonis met geen antagonistiese eienskappe nie. Dit het affiniteit vir kappa-, mu- en delta-opiaatreseptore in die brein en rugmurg. Oksikodoon is soortgelyk aan morfien in sy werking. Die terapeutiese effek is hoofsaaklik analgeties, angsiolities en sederend (sien INDIKASIES). Farmakokinetiese eienskappe: Page 16 of 30

17 Oksikodoon het 'n absolute biobeskikbaarheid tot 87 % na orale toediening. Oksikodoon word hoofsaaklik na noroksikodoon via CYP450-3A en oksimorfoon via CYP450-2D6, gemetaboliseer. Oksimorfoon het geringe analgetiese werking en is in lae konsentrasies in plasma teenwoordig, maar word nie beskou om tot die farmakologiese effek by te dra nie. Oksikodoon het 'n eliminasie halfleeftyd van ongeveer 3 uur. Die vrystelling van oksikodoon vanuit OxyContin tablette is bifasies met 'n aanvanklike relatiewe vinnige vrystelling wat 'n vroeë aanvang van analgesie verskaf, gevolg deur 'n meer beheerde vrystelling wat die 12-uur duur van werking bepaal. Die gemiddelde skynbare eliminasie halfleeftyd van OxyContin tablette is 4,5 uur en lei tot konstante bloedvlakke binne een dag. OxyContin tablette het 'n orale biobeskikbaarheid wat vergelykbaar is met konvensionele orale oksikodoon, maar die eersgenoemde bereik maksimale plasmakonsentrasies na ongeveer 3 uur eerder as ongeveer na 1 tot 1,5 uur. Piek- en trog- konsentrasies van oksikodoon vanaf OxyContin 10 mg wat 12 uurliks toegedien word, is ekwivalent aan konvensionele orale oksikodoon waar 5 mg 6 uurliks toegedien word. OxyContin 5 mg, 10 mg, 20 mg, 40 mg and 80 mg is bio-ekwivalent in terme van beide tempo en omvang van absorpsie. Inname van n standaard, hoë-vet maaltyd verander nie die piek oksikodoon konsentrasie of die omvang van die absorpsie daarvan vanuit OxyContin tablette, nie. Bejaardes: Die AOK by bejaarde persone is 15 % groter wanneer vergelyk word met jonger persone. Geslag: Op 'n liggaamsgewig aangepaste basis het vroulike persone, gemiddeld tot 25 % hoër oksikodoon plasmakonsentrasies as mans. Die rede vir die verskil is onbekend. Pasiënte met renale inkorting: Voorlopige data van 'n studie het getoon dat pasiënte met ligte tot matige renale inperking, piek plasma oksikodoon- en noroksikodoon konsentrasies van ongeveer 50 % en 20 %, en AOK waardes van oksikodoon, noroksikodoon en oksimorfoon ongeveer 60 %, 60 % and 40% onderskeidelik hoër as normale persone het. Daar was 'n verhoging van slegs een uur in t 1/2 van eliminasie vir oksikodoon. Pasiënte met ligte tot matige hepatiese inkorting: Pasiënte met ligte tot matige hepatiese disfunksie wys piek plasma oksikodoon- en noroksikodoonkonsentrasies van onderskeidelik ongeveer 50 % en 20 % hoër as normale persone. AOK waardes was onderskeidelik ongeveer 95 % en 75 % hoër, respektiewelik. Oksimorfoon piek plasmakonsentrasies en AOK waardes was met 15 % tot 50 % laer. Die t 1/2 eliminasie vir oksikodoon het met 2,3 uur verhoog. INDIKASIES OxyContin tablette is aangedui vir die behandeling van matige tot erge pyn by pasiënte met kanker en post-operatiewe pyn nadat gastroïntestinale funksie teruggekeer het. Page 17 of 30

18 OxyContin tablette is aangedui vir die behandeling van erge pyn wat die gebruik van 'n sterk opioïed analgetikum vereis. KONTRA-INDIKASIES OxyContin tablette is teenaangedui by pasiënte met bekende hipersensitiwiteit teenoor oksikodoon of teenoor enige van die ander bestanddele of in enige situasie waar opioïede teenaangedui is (sien SAMESTELLING). OxyContin tablette is teenaangedui by pasiënte wat aan respiratoriese onderdrukking ly, met hipoksie en/of hiperkapnie van enige oorsaak, of pasiënte wat ly aan paralitiese ileus, akute buik, vertraagde gastriese lediging, kroniese obstruktiewe lugwegsiekte, cor pulmonale, kroniese brongiale asma, matige tot erge hepatiese inkorting, erge renale inkorting (kreatinienopruiming < 10 ml/min) of kroniese hardlywigheid. OxyContin tablette is teenaangedui by pasiënte wat gelyktydige toediening van monoamienoksidaseïnhibeerders ontvang of binne 2 weke van staking van hul gebruik. OxyContin tablette moet nie deur swanger of borsvoedende vrouens gebruik word nie (sien SWANGERSKAP en LAKTASIE). OxyContin tablette word nie aanbeveel vir pre-operatiewe gebruik of vir die eerste uur post-operatief nie. Pasiënte met seldsame, oorerflike probleme van galaktose intoleransie, bv. galaktosemie, die Lapp laktase tekort of glukose-galaktose wanabsorpsie moet nie hierdie medisyne neem nie. WAARSKUWINGS en SPESIALE VOORSORGMAATREËLS Die groot risiko is respiratoriese onderdrukking. 'n Verlaging in dosis mag nodig wees by hipotiroïedisme. OxyContin tablette moet versigtig gebruik word by pasiënte met hoof beserings (as gevolg van die risiko van verhoogde intrakraniale druk), hipotensie, hipovolemie, toksiese psigose, siekte van die biliêre kanaal, pankreatitis, inflammatoriese ingewandsafwykings, prostaat hipertrofie, adrenokortikale ontoereikendheid, Addison se siekte, miksedeem, alkoholisme, delirium tremens, verswakte renale of hepatiese funksie en verswakte bejaardes en sieklike pasiënte. OxyContin tablette moet met omsigtigheid gebruik word in pasiënte wat MAO-inhibeerders of SSSonderdrukkers gebruik, insluitende alkohol of bensodiasepiene (sien INTERAKSIES). OxyContin tablette moet nie gebruik word as daar 'n moontlikheid is dat paralitiese ileus kan ontwikkel nie. Indien paralitiese ileus vermoed word of voorkom tydens gebruik van OxyContin tablette, moet dit onmiddellik gestaak word. Pasiënte wat kordotomie of ander pynverligtende chirurgiese prosedures ondergaan moet nie OxyContin tablette vir 24 uur voor chirurgie of binne die eerste uur na chirurgie gebruik nie. Indien verdere behandeling met OxyContin tablette dan aangedui is, moet die dosis na die nuwe post-operatiewe vereistes aangepas word. Page 18 of 30

19 OxyContin 80 mg moet nie deur pasiënte wat nie voorheen aan opioïede blootgestel is, gebruik word nie. Die sterkte van die tablette kan noodlottige respiratoriese onderdrukking veroorsaak wanneer dit aan opioïed naïewe pasiënte toegedien word. OxyContin tablette moet versigtig gebruik word na abdominale chirurgie. Aangesien opioïede bekend is daarvoor om intestinale motiliteit in te kort, moet dit nie gebruik word totdat die geneesheer seker is dat normale ingewandsfunksie herstel is nie. Vir geskikte pasiënte wat aan kroniese, nie-kwaadaardige pyn ly, moet opioïede gebruik word as deel van 'n omvattende behandelingsprogram wat ander medisyne en behandelingsmodaliteite insluit. Dit is baie belangrik om gedurende die evaluering van n pasiënt met kroniese, nie-kwaadaardige pyn, die geskiedenis van verslawing en misbruik te oorweeg. OxyContin tablette het n potensiaal vir misbruik wat soortgelyk is aan ander sterk opioïede, en moet daarom met sorg gebruik word by opioïedafhanklike pasiënte, of indien die geneesheer of apteker bekommerd is oor die risiko van misbruik. Oksikodoon kan gesoek en misbruik word deur persone met latente of duidelike verslawingstoornisse. OxyContin tablette moet met spesifieke sorg by pasiënte met 'n geskiedenis van alkoholen dwelmmisbruik, gebruik word. Indien opioïedbehandeling as geskik beskou word vir die pasiënt, is die hoof doel van behandeling nie om die dosis van die opioïed te verminder nie, maar eerder om 'n dosis te bereik wat genoegsame pynverligting met die minimum newe-effekte verskaf. Daar moet gereelde kontak tussen die geneesheer en pasiënt wees sodat dosisaanpassings gemaak kan word. Dit word sterk aanbeveel dat die geneesheer die uitkoms vir die behandeling bepaal soos dit in die pynbeheer riglyne voorgeskryf word. Die geneesheer en pasiënt kan dan ooreenkom om behandeling te staak as hierdie doelwitte nie bereik word nie. Toleransie en afhanklikheid: Die pasiënt kan toleransie ontwikkel teenoor OxyContin tablette wanneer dit kronies gebruik word en mag aanhoudende hoër dosisse vereis om die pyn te beheer. Langdurige gebruik van OxyContin tablette kan tot fisiese afhanklikheid lei en 'n onttrekkingsindroom kan ontwikkel na skielike staking van die behandeling. Wanneer die pasiënt nie verdere behandeling met oksikodoon benodig nie, mag dit raadsaam wees om die dosis geleidelik te verminder om onttrekkingsimptome te voorkom. Vir meer inligting oor onttrekkingsindroom, sien NEWE EFFEKTE. Babas van afhanklike moeders, kan onttrekkingsimptome toon en respiratoriese onderdrukking by geboorte hê. Page 19 of 30

20 OxyContin tablette moet heel ingesluk word en nie gebreek, gekou of fyngedruk word nie. Die gebruik van gebreekte, gekoude of fyngedrukte OxyContin tablette lei tot vinnige vrystelling en absorpsie van 'n potensieel noodlottige dosis van oksikodoon. Dit is te verwagte dat die misbruik van die tablette deur parenterale toediening, ander ernstige nadelige effekte soos lokale weefsel nekrose, infeksie, pulmonale granulomas, verhoogde risiko van endokarditis en hartbesering, wat noodlottig mag wees, tot gevolg kan hê. Hiperalgesie wat nie reageer op n verdere verhoging in dosis nie kan voorkom, veral in hoë dosisse. n Verminderde dosis van oksikodoon of n ander opioied mag nodig wees om pynverligting te bewerkstellig. OxyContin tablette moet nie opgelos, gelek of enigsins nat gemaak word voor orale gebruik nie. Een tablet moet op n slag geneem word met genoeg water om te verseker dat die tablet heeltemal ingesluk word, onmiddelik nadat dit geneem is. Pasiënte met onderliggende gastro-intestinale probleme, soos esofageale kanker of kolon kanker met n klein gastro-intestinale lumen het n groter risiko om komplikasies op te tel (intestinale obstruksie, en verergerde divertikulitis, wat moontlik mediese ingryping kan noodsaak om die tablet te verwyder). OxyContin tablette moet met omsigtigheid gebruik word by pasiënte wat sukkel om te sluk of wat onderliggende gastro-intestinale probleme het wat moonlik tot obstruksie kan ly. Bevat Laktose. Pasiënte met n rare oorerflike kondisie van galaktose intoleransie, soos galaksosemie, Lapp se laktase afwyking, glukose-galaktose malabsopsie ens. moet nie OxyContin tablette neem nie. Effek op die vermoë om te betuur of masjienerie te gebruik: Oksikodoon kan die pasiënt se reaksie tot 'n afwisselende omvang verander, afhangend van die dosis en die individuele vatbaarheid. Daarom moet pasiënte nie bestuur of met masjienerie werk indien hul geaffekteer word nie. INTERAKSIES OxyContin tablette versterk die effek van kalmeermiddels, anestetika, hipnotika, antidepressante, sedeermiddels, fenotiasiene, neuroleptiese geneesmiddels, alkohol, ander opioïede, spierverslappers en antihipertensiewe middels. Gesamentlike gebruik van oksikodoon en anticholinergiese medisyne of medisyne met anticholinerge effek (bv. trisikliese antidepressante, antihistamiene, antipsigotiese middels, spierverslappers, anti-parkinson medisyne) kan anticholinerge newe effekte vererger. Monoamienoksidaseïnhibeerders is bekend om n interaksie te hê met narkotiese analgetika, wat SSS prikkeling of onderdrukking met hipertensiewe of hipotensiewe krisis veroorsaak. Page 20 of 30

21 Gelyktydige toediening van kinidien, 'n inhibeerder van sitochroom P450-2D6, lei tot 'n verhoging in oksikodoon C maks van 11 %, AOK van 13 % en t 1/2 eliminasie van 14 %. Daar is ook 'n verhoging in noroksikodoonvlak opgemerk, (C maks van 50 %, AOK van 85 % en t 1/2 eliminasie van 42 %). Die farmakodinamiese effekte van oksikodoon was onveranderd. Hierdie interaksie kan ook verwag word wanneer ander kragtige inhibeerders van sitochroom P450-2D6 ensiem gelyktydig toegedien word. Oksikodoon word hoofsaaklik deur sitochroom P450-3A met n bydrae van sitochroom P450-2D6 gemetaboliseer. Die aktiwiteite van hierdie metaboliese roetes mag geinhibeer of versterk word deur verskeie medisyne of voedsel wat daarmee saam gebruik word. n Dosis aanpassing van oksikodoon mag nodig wees. Simetidien en inhibeerders van sitochroom P450-3A, soos asool-antifungale middels (bv. ketokonasool), makroliede antibiotika (bv. klaritromisien en eritromisien), protease inhibeerders (bv. ritonavier), en pomelosap kan die metabolisme van oksikodoon inhibeer, wat n toename in oksikodoon plasma konsentrasies kan veroorsaak. Sitochroom P450-3A induseerders, soos rifampisien, karbamasepien, fenitoïen en St. John s wort, kan die metabolisme van oksikodoon induseer en verhoogde uitskeiding veroorsaak, wat verlaagde oksikodoon plasmakonsentrasies teweegbring. Medisyne wat sitochroom P450-2D6 aktiwiteit inhibeer, soos paroksetien en kinidien, kan verlaagde uitskeiding van oksikodoon veroorsaak wat kan lei tot n verhoging in oksikodoon plasmakonsentrasies. SWANGERSKAP EN LAKTASIE OxyContin tablette word teenaangedui gedurende swangerskap of kraam. Babas, gebore aan moeders wat opioïede tydens swangerskap ontvang het, moet gemoniteer word vir respiratoriese onderdrukking (sien KONTRA-INDIKASIES). Langtermyn gebruik van oksikodoon gedurende swangerskap kan lei to neonatale opioied onttrekkingsindroom. Oksikodoon kan in borsmelk uitgeskei word en kan respiratoriese onderdrukking by pasgeborenes veroorsaak. OxyContin tablette moet daarom nie deur borsvoedende moeders gebruik word nie. DOSIS EN GEBRUIKSAANWYSINGS OxyContin tablette moet heel ingesluk word en nie gekou word nie. Bejaardes en volwassenes ouer as 18 jaar: OxyContin tablette moet in 12-uurlikse intervalle geneem word. Die dosis is afhanklik van die pynvlak en die pasiënt se geskiedenis van analgetiese vereistes. n Verhoging in die pynvlak sal 'n verhoging in dosis van OxyContin tablette vereis, met gebruik van die 5 mg, 10 mg, 20 mg, 40 mg of 80 mg tablet sterktes òf alleen òf in kombinasie, om pynverligting te bereik. Page 21 of 30

22 Die korrekte dosis vir enige individuele pasiënt is dit wat die pyn beheer en goed verdra word vir die volle 12 uur. Pasiënte moet getitreer word tot pynverligting, tensy onbeheerde ongewensde geneesmiddelreaksies dit verhoed. Indien hoër dosisse nodig is, moet verhogings, waar moontlik, in 25 % - 50 % inkremente gemaak word. Die behoefte aan reddings-medisyne meer as twee keer per dag wys daarop dat die dosis OxyContin tablette verhoog moet word. Die gewone aanvangsdosis vir opioïed naïewe pasiënte wat erge pyn vertoon, wat nie met swakker opioïede beheer word nie, is 10 mg 12-uurliks. Sommige pasiënte kan voordeel trek daaruit om 'n aanvangsdosis van 5 mg te gebruik om sodoende die kanse van newe-effekte te verminder. Die dosis moet daarna sorgvuldig getitreer word, so dikwels as een keer per dag, indien nodig om pynverligting te bereik. Vir die meerderheid van pasiënte is die maksimum dosis 200 mg 12-uurliks. Nogtans, kan 'n klein hoeveelheid pasiënte hoër dosisse benodig. Dosisse groter as 1000 mg daagliks is al aangeteken. Pasiënte wat orale morfien ontvang het voor die behandeling met OxyContin tablette, moet hul daaglikse dosis op die volgende verhouding baseer: 10 mg orale oksikodoon is ekwivalent aan 20 mg orale morfien. Dit moet beklemtoon word dat dit slegs 'n riglyn is tot die dosis van OxyContin tablette wat benodig word. Inter-pasiënt wisselvalligheid vereis dat elke pasiënt sorgvuldig getitreer moet word tot die geskikte dosis. Gekontroleerde farmakokinetiese studies by bejaarde pasiënte (ouer as 65 jaar) het aangetoon dat die opruiming van oksikodoon slegs effens verlaag is in vergelyking met jonger volwassenes. Geen onverwagse reaksies is waargeneem gebaseer op die ouderdom nie, daarom is volwasse dosisse en dosisintervalle geskik (sien Farmakokinetiese eienskappe). Kinders jonger as 18 jaar: Die veiligheid en doeltreffendheid van OxyContin tablette by pasiënte jonger as 18 jaar is nog nie vasgestel nie. Volwassenes met ligte tot matige renale inkorting en matige hepatiese inkorting: Die plasmakonsentrasie in hierdie populasie kan verhoog wees. Daarom moet die inisiasie dosis 'n konserwatiewe benadering volg. Opioïed naïewe pasiënte moet met 12 uurlikse OxyContin 5 mg begin word en getitreer word tot pynverligting soos beskryf, bereik word. (sien Farmakokinetiese eienskappe). Staking van behandeling: Wanneer 'n pasiënt nie langer behandeling met oksikodoon benodig nie, is dit raadsaam om die dosis geleidelik te verminder om onttrekkingsimptome te verhoed. NEWE EFFEKTE Newe effekte is tipies met vol opioïed agoniste. Toleransies en afhanklikheid kan voorkom. Hardlywigheid kan met 'n geskikte purgeermiddel voorkom word. Oksikodoon kan met anti-emetika Page 22 of 30

23 gekombineer word indien naarheid en braking n probleem is. Die reaksies word as MeDRA voorkeurterme in orgaanklas en absolute frekwensie gelys Liggaamstelsel Frekwensie van voorkoms Baie Algemeen Nie Seldsaam Baie Onbekend Algemeen > 1 % en < algemeen > 0,01 % Seldsaam (kan nie > 10 % 10 % > 0,1 % en < en < 0,1 % < 0,01 % beraam 1 % word uit beskikbare data) Gastroïntestinale konstipasie, abdominale mond melaena, tandbederf afwykings naarheid, pyn, ulserasie, tandafwyki braking diarree, stomatitis, ng, droë mond, winderigheid, tandvleis- hik, disfagie bloeding dispepsie (moeilik om tablet te sluk), ileus, wind opbreek, opbraking, braak geluide Hepatobiliêre biliêre koliek, cholestasie afwykings verhoogde hepatiese ensieme Metabolisme en verminderd dehidrasie verhoogde voedings- e aptyt aptyt afwykings Page 23 of 30

24 Senuweestelsel hoofpyn, bewing, ingekorte hiperalgesie afwykings duiseligheid lustelooshei konsentrasie,, sedasie, d migraine, slaperigheid dysgeusie, onwillekeurig e spiersametre kkings, hipoastesie, abnormale koördinasie, sinkopee, parestesie, amnesie, konvulsies, spraak afwyking Page 24 of 30

25 Psigiatriese veranderde persepsie aggressie afwykings gemoed en steurnisse persoonlik- (bv. heidsverand hallusinasies, ering (bv. derealisering) angs,, verlaagde depressie), libido, verlaagde beïnvloed aktiwiteit, labiele affek, rustelooshei geïrriteerdhei d, psigo- d, euforiese motoriese gemoed, hiperaktiwit medisyne eit, afhanklikheid senuweeagt igheid, insomnie, abnormale denke, verwarring Infeksies en herpes infestasies simplex Immuunstelsel hipersensitiwi anafilakties afwykings teit e reaksie, anafilaktoïe d-reaksie Oogafwykings miose, visuele steurnisse Oor en Labarint- gehoor afwykings inkorting, vertigo Renale en urinêre disurie, urinêre afwykings mikturasie retensie dringendhei d Page 25 of 30

26 Voortplantingstel sel en borsafwykings Kardiale afwykings Vaskulêre afwykings Respiratoriese en torakale en mediastinale afwykings dispnee erektiele disfunksie, hipogonadis me tagikardie, palpitasies (in die konteks van onttrekkingsi ndroom) vasodilatasie disfonie, hoes, respiratoriese onderdrukkin g, verstikking hipotensie, ortostaties e hipotensie amenorree Page 26 of 30

27 Vel en pruritus velreaksies/ droë vel urtikarie subkutaneuse uitslag, weefsel hiperhidros afwykings e Besering, besering na vergiftiging en ongelukke, prosedure medikasie komplikasies wat vassit in die keel Algemene astenie, koudheid, gewigs- neonatale afwykings en moegheid geneesmid- toename, medisyne toedieningsplek delonttrekking gewigs- onttrekkings toestande sindroom, pyn afname indroom (bv. borspyn), malaise, edeem, perifere edeem, dors, medisyne verdraagsaamheid Simptome geassosieer met onttrekkingsindroom: Die opioïed onthouding- of onttrekkingsindroom word gekarakteriseer deur sommige van die volgende: rusteloosheid, lakrimasie, rinorree, gaap, sweet, koue rillings, mialgie en midriase. Ander simptome mag ook ontwikkel wat die volgende insluit: geïrriteerdheid, angs, rugpyn, gewrigspyn, swakheid, abdominale krampe, slapeloosheid, naarheid, anoreksie, braking, diarree of verhoogde bloeddruk, - respiratoriese snelheid of - hartsnelheid. Die ontwikkeling van psigologiese afhanklikheid (verslawing) aan opioïed analgetika by pasiënte waarvan pyn behoorlik beheer word, is as seldsaam aangemeld. Data om die ware insidensie van psigologiese afhanlikheid by kroniese pasiënte vas te stel, is egter nie beskikbaar nie. BEKENDE SIMPTOME VAN OORDOSERING EN DIE BESONDERHEDE VAN BEHANDELING DAARVAN Tekens van oksikodoontoksisiteit en -oordosering is: klein pupille, respiratoriese onderdrukking, pulmonale edeem en hipotensie. Sirkulatoriese versaking en slaperigheid wat tot stupor of verdiepte koma vorder, hipotonie, bradikardie en dood kan voorkom in meer ernstige gevalle. Page 27 of 30

28 Behandeling van oksikodoon oordosis: primêre aandag moet geskenk word aan die vestiging van 'n patente lugweg en die instelling van bygestaande of beheerde ventilasie. Dien naloksoon (0,4 tot 2 mg vir 'n volwassene en 0,01 mg/kg liggaamsgewig vir kinders) intraveneus toe, indien die pasiënt in 'n koma is of respiratoriese onderdrukking teenwoordig is. Herhaal die dosis met 2 minuut intervalle indien daar geen reaksie is nie. Indien herhaaldosisse nodig is, is 'n infusie van 60 % van die aanvanklike dosis per uur 'n bruikbare beginpunt. 'n Oplossing van 10 mg opgemaak in 50 ml dekstrose sal 200 mikrogram/ml vir infusie lewer met gebruik van 'n IV pomp (dosis aangepas tot die kliniese respons). Infusies is nie 'n plaasvervanger vir gereelde hersiening van die pasiënt se kliniese toestand nie. Intramuskulêre naloksoon is 'n alternatief in die geval waar IV toegang nie moontlik is nie. Aangesien die werkingsduur van naloksoon relatief kort is, moet die pasiënt noukeurig gemonitor word totdat spontane asemhaling betroubaar herstel het. Naloksoon is 'n mededingende antagonis en groot doserings (4 mg) mag by ernstig vergiftigde pasiënte nodig wees. Vir n minder ernstige oordosis, dien 0,2 mg naloksoon intraveneus toe, gevolg deur inkremente van 0,1 mg elke 2 minute, indien nodig. In die afwesigheid van kliniese beduidende respiratoriese of sirkulatoriese onderdrukking tot oksikodoon oordosis, moet naloksoon sekondêr toegedien word. Naloksoon moet versigtig toegedien word aan persone wat bekend is of verdink word van fisiese afhanklikheid van oksikodoon. In sulke gevalle kan 'n skielike of volledige omkering van opioïed effekte, pyn en 'n akute onttrekkingsindroom voorkom. Addisionele/ander oorwegings: Oorweeg geaktiveerde steenkool (50 g vir volwassenes, g vir kinders), indien 'n aansienlike hoeveelheid binne 1 uur ingeneem is, mits die lugweg beskerm kan word. Die aanname dat die laat toediening van geaktiveerde steenkool voordelig kan wees vir verlengde vrystellingspreparate kan geregverdig word, alhoewel daar nie bewyse is om dit te ondersteun nie. OxyContin tablette sal voortgaan om vry te stel en by die oksikodoonlading te voeg tot en met 12 uur na toediening, en die hantering van die oksikodoon-oordosis moet daarvolgens aangepas word. IDENTIFIKASIE OxyContin 5 mg tablette is ligblou, ronde, bi-konvekse, filmbedekte tablette, met OC op een kant gedruk en 5 op die ander kant. OxyContin 10 mg tablette is wit, ronde, bi-konvekse, filmbedekte tablette, met OC op een kant gedruk en 10 op die ander kant. OxyContin 20 mg tablette is pienk, ronde, bi-konvekse, filmbedekte tablette, met OC op een kant gedruk en 20 op die ander kant. OxyContin 40 mg tablette is geel, ronde, bi-konvekse, filmbedekte tablette, met OC op een kant gedruk en 40 op die ander kant. Page 28 of 30