Oxaprozin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Juvenile rheumatoid arthritis
Child: ≥6 yr 22-31 kg: 600 mg once daily; 32-54 kg: 900 mg once daily; ≥55 kg: 1,200 mg once daily.

Oral
Osteoarthritis, Rheumatoid arthritis
Adult: 1,200 mg once daily. Max: 1,800 mg or 26 mg/kg, whichever is lower, given in divided doses.
Special Patient Group
Patient w/ low body wt: Osteoarthritis; Rheumatoid arthritis: Initially, 600 mg once daily.
Renal Impairment
Osteoarthritis; Rheumatoid arthritis: Severe or on dialysis: Initially, 600 mg once daily, may be increased to 1,200 mg once daily if necessary.
Chống chỉ định
Hypersensitivity. History of bronchospasm, asthma, urticaria, or other allergic-type reactions w/ NSAIDs; active GI bleeding, severe heart failure, recent MI. CABG surgery.
Thận trọng
Patient w/ history of peptic ulcer disease and/or GI bleeding, coagulopathy, HTN, oedema, known or risk factors for CV disease, on dialysis, DM, other forms of asthma. Smokers. Severe renal and hepatic impairment. Childn. Pregnancy and lactation.
Phản ứng phụ
Significant: Drowsiness, dizziness, blurred vision, HTN, fluid retention, oedema, decreased platelet adhesion and aggregation, prolonged bleeding time, anaemia, increased risk of hyperkalaemia, photosensitivity reactions, renal papillary necrosis (long term use). Rarely, blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia).
Nervous: Headache, CNS inhibition (e.g. depression, sedation, confusion), sleep disturbance, sedation.
GI: Abdominal pain/distress, anorexia, constipation, diarrhoea, dyspepsia, flatulence, heartburn, nausea, vomiting.
Hepatic: Increased ALT/AST.
Genitourinary: Abnormal renal function, dysuria, urinary frequency.
Otic: Tinnitus.
Dermatologic: Pruritus, rash.
Potentially Fatal: Increased risk of CV thrombotic events (e.g. MI, heart failure, stroke); GI adverse events (e.g. inflammation, bleeding, ulceration and perforation of the stomach or intestines); anaphylactoid reactions (e.g. severe bronchospasm); serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis). Rarely, hepatic injury (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure).
PO: C (Avoid during 3rd trimester or near delivery)
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness, dizziness and blurred vision, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor BP, CBC, K levels, renal function, and LFT. Monitor signs and symptoms of GI bleeding.
Quá liều
Symptoms: Lethargy, drowsiness, nausea, vomiting, abdominal pain, GI bleeding, HTN, acute renal failure, resp depression, coma. Management: Symptomatic and supportive treatment. May consider emesis and/or activated charcoal admin.
Tương tác
Increased risk of renal toxicity w/ diuretics, ACE inhibitors, angiotensin II receptor blockers (ARBs). Increased risk of bleeding w/ anticoagulants, antiplatelets, SSRIs, serotonin norepinephrine reuptake inhibitors. Increased risk of hyperkalaemia w/ ACE inhibitors. May increase serum conc of lithium. May increase serum concentration and prolong the half-life of digoxin. May increase the risk of methotrexate and ciclosporin toxicity. Increased risk of myelosuppression, renal and GI toxicity w/ pemetrexed. May decrease antihypertensive effect of diuretics, ACE inhibitors, ARBs, β-blockers. May decrease natriuretic effect of furosemide.
Potentially Fatal: Increased risk of GI adverse events w/ oral corticosteroids, aspirin, anticoagulants, SSRIs.
Food Interaction
Increased risk of GI adverse events w/ alcohol.
Lab Interference
False positive result for benzodiazepines in urine immunoassay screening test.
Tác dụng
Description: Oxaprozin is a propionic acid derivative NSAID w/ analgesic, and antipyretic properties. It inhibits the enzyme cyclooxygenase-1 and 2 (COX-1 and 2) resulting in the blockage of prostaglandin synthesis.
Pharmacokinetics:
Absorption: Slowly but extensively absorbed from the GI tract. Time to peak plasma concentration: Approx 2-3 hr.
Distribution: Volume of distribution: 11-17 L/70 kg. Plasma protein binding: 99%, mainly to albumin.
Metabolism: Metabolised in the liver via oxidation and glucuronidation into ester and ether inactive glucuronide metabolites and active phenolic metabolite (small amount).
Excretion: Mainly via urine (5%, as unchanged drug; 65%, as metabolites); faeces (35%, as metabolites). Elimination half-life: 41-55 hr.
Đặc tính

Chemical Structure Image
Oxaprozin

Source: National Center for Biotechnology Information. PubChem Database. Oxaprozin, CID=4614, https://pubchem.ncbi.nlm.nih.gov/compound/Oxaprozin (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại ATC
M01AE12 - oxaprozin ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.
References
Anon. Oxaprozin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/09/2017.

Buckingham R (ed). Oxaprozin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com/. Accessed 19/09/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Oxaprozin. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 19/09/2017.

Oxaprozin Tablet, Film Coated (PD-Rx Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/09/2017.

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