Oxycodone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Moderate to severe pain
Adult: As inj: 1-10 mg over 1-2 min, repeated not more often than 4 hrly. As infusion: Initially, 2 mg/hr, increased as necessary. Patient-controlled analgesia (PCA): 0.03 mg/kg, admin w/ a minimum lock-out time of 5 min.
Elderly: Give the lowest dose w/ careful titration to pain control.

Oral
Moderate to severe pain
Adult: Initially, 5 mg 4-6 hrly may increase as necessary. Extended-release tab: 5-10 mg 12 hrly. Max: 400 mg/day.

Subcutaneous
Moderate to severe pain
Adult: As inj: Initially, 5 mg 4 hrly. As infusion: Initially, 7.5 mg daily adjusted according to response.
Elderly: Give the lowest dose w/ careful titration to pain control.
Renal Impairment
Oral:
Mild to moderate: Initial: 2.5 mg 6 hrly. Severe: Contraindicated.
Intravenous/Subcutaneous:
Mild to moderate: Give the lowest dose w/ careful titration to pain control. Severe: Contraindicated.
Hepatic Impairment
Oral:
Mild: Initial: 2.5 mg 6 hrly. Moderate to severe: Contraindicated.
Intravenous/Subcutaneous:
Mild: Give the lowest dose w/ careful titration to pain control. Moderate to severe: Contraindicated.
Cách dùng
Prolonged-Release: May be taken with or without food. 160 mg tab must be taken on an empty stomach. Do not take w/ high fat meals. All strengths: Swallow whole, do not break/chew/crush. Taking broken, chewed or crushed tab leads to rapid release & absorption of a potentially fatal dose of oxycodone.
Hướng dẫn pha thuốc
Dilute to 1 mg/mL in 0.9% saline, 5% dextrose or water for inj.
Tương kỵ
Prochlorperazine, cyclizine in concentrations greater than 3 mg/mL or when diluted in 0.9% saline.
Chống chỉ định
Resp depression, known or suspected paralytic ileus, acute abdomen, delayed gastric emptying, COPD, cor pulmonale, acute or chronic bronchial asthma, hypercarbia, chronic constipation. Concurrent admin of MAOIs or w/in 2 wk of discontinuation of use. Moderate to severe hepatic and severe renal impairment. Lactation.
Thận trọng
Patient w/ raised intracranial pressure, hypotension, hypovolaemia, toxic psychosis, biliary tract diseases, pancreatitis, inflammatory bowel disorders, prostatic hypertrophy, adrenocortical insufficiency, history of drug abuse or acute alcoholism, delirium tremens, thyroid dysfunction. Mild to moderate renal and mild hepatic impairment. Pregnancy.
Phản ứng phụ
Nausea, constipation, vomiting, resp depression, headache, pruritus, insomnia, dizziness, asthenia, somnolence, abdominal pain, chills and fever, hypotension, anorexia, diarrhoea, dyspepsia, dysphagia, anxiety, nervousness, tremor, vasodilation, cough, dyspnoea, rash.
PO: B (Prolonged use may cause neonatal opioid withdrawal syndrome (NOWS).)
Thông tin tư vấn bệnh nhân
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor pain relief, resp and mental status, BP; signs of misuse, abuse, and addiction; signs or symptoms of hypogonadism or hypoadrenalism.
Quá liều
Symptoms: Pin-point pupils, resp depression, hypotension. Circulatory failure and somnolence progressing to stupor or deepening coma, skeletal muscle flaccidity, bradycardia and death may occur in more severe cases. Management: Maintain adequate respiration and employ supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary oedema. Cardiac arrest or arrhythmias may require cardiac massage or defibrillation. Naloxone may be used as an antidote.
Tương tác
Potentiates the effects of tranquilisers, anaesth, hypnotics, anti-depressants, sedatives, phenothiazines, neuroleptic drugs, other opioids, muscle relaxants and antihypertensives. Concurrent admin of quinidine, a CYP2D6 inhibitor may cause an increase in serum levels and elimination half-life of oxycodone. Cimetidine and CYP3A inhibitors (e.g. ketoconazole, erythromycin) may inhibit the metabolism of oxycodone.
Potentially Fatal: Concurrent admin of MAOIs may result to CNS excitation or depression w/ hypertensive or hypotensive crisis.
Food Interaction
May potentiate the CNS depressant effect of alcohol.
Tác dụng
Description: Oxycodone is a synthetic phenanthrene-derivative opiate agonist. It binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain. It produces generalised CNS depression.
Onset: 10-15 min (immediate-release).
Duration: 3-6 hr (immediate-release); ≤12 hr (extended-release).
Pharmacokinetics:
Absorption: Absorbed from the GI tract. Bioavailability: Approx 60-87%.
Distribution: Crosses the placenta and enters breast milk. Volume of distribution: 2.6 L/kg. Plasma protein binding: Approx 45%.
Metabolism: Metabolised via glucuronidation to noroxycodone by CYP3A isoenzymes and to a lesser extent, to oxymorphone by CYP2D6.
Excretion: Via urine as unchanged drug. Elimination half-life: 2-4 hr.
Bảo quản
Store between 15-30°C. Protect from light.
Phân loại MIMS
References
Anon. Oxycodone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/07/2014.

Buckingham R (ed). Oxycodone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/07/2014.

Joint Formulary Committee. Oxycodone Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/07/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Oxycodone, Oxycodone HCl, Oxycodone Terephthalate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 30/07/2014.

Oxecta Tablet (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/07/2014.

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