Tolmetin sodium

Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Juvenile idiopathic arthritis
Child: ≥2 years Initially, 20 mg/kg daily in 3 or 4 divided doses. Maintenance: 15-30 mg/kg daily in 3 or 4 divided doses.

Topical/Cutaneous
Osteoarthritis, Rheumatoid arthritis
Adult: Initially, 400 mg tid, then adjust after 1-2 weeks according to response. Maintenance: 600-1,800 mg daily in 3 divided doses.
Cách dùng
Should be taken with food.
Chống chỉ định
Hypersensitivity to salicylates (e.g. aspirin) or other NSAIDs. Aspirin-sensitive asthma. Treatment of peri-operative pain in CABG surgery. Pregnancy (late stage).
Thận trọng
Patient with CV disease, history of gastrointestinal disease (e.g. bleeding or ulcer), fluid retention, dehydration, pre-existing asthma, coagulation disorders, hypertension. Smokers or alcoholic patient. Hepatic and severe renal impairment. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Hyperkalaemia, elevated ALT/AST levels, hypertension, oedema, peptic ulcer, jaundice, weight changes (gain/loss); renal papillary necrosis, acute interstitial nephritis, nephrotic syndrome (long-term use).
Cardiac disorders: Chest pain.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbance.
Gastrointestinal disorders: Abdominal pain, diarrhoea, dyspepsia, flatulence, gastrointestinal distress, nausea, vomiting, constipation, gastritis.
General disorders and administration site conditions: Asthenia, fever.
Nervous system disorders: Dizziness, headache.
Psychiatric disorders: Depression, drowsiness.
Renal and urinary disorders: UTI, increased BUN.
Skin and subcutaneous tissue disorders: Irritation.
Potentially Fatal: Anaphylactoid reactions (e.g. swelling of the face or throat, breathing difficulty), exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, MI, stroke, gastrointestinal bleeding, ulceration, and perforation, severe blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia), hepatic failure, liver necrosis, fulminant hepatitis.
PO: Z (NSAIDs caused foetal ductus arteriosus premature closure, foetal renal impairment and persistent pulmonary hypertension. Avoid near term, else use lowest dose for shortest time.)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, drowsiness, and blurred vision, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor blood pressure and K levels closely during initiation and throughout the course of treatment. Perform CBC, chemistry profile, hepatic and renal function tests regularly, especially for patients with prolonged use. Monitor for signs and symptoms of gastrointestinal bleeding and hepatic dysfunction.
Tương tác
Increased risk of bleeding with anticoagulants, corticosteroids, salicylates (e.g. aspirin) and other NSAIDs. May decrease the antihypertensive effect of ACE inhibitors or angiotensin receptor blockers. Increases the plasma concentration of lithium. May reduce the natriuretic effects of furosemide or thiazide diuretics. May enhance methotrexate toxicity.
Tương tác với thức ăn
Avoid alcohol.
Ảnh hưởng đến kết quả xét nghiệm
False-positive result for proteinuria test using acid precipitation method.
Tác dụng
Description:
Mechanism of Action: Tolmetin, a pyrrole acetic acid derivative blocks prostaglandin synthesis by inhibiting cyclooxygenase isoenzymes COX-1 and COX-2.
Onset: Analgesic: 1-2 hours. Anti-inflammatory: Days to weeks.
Pharmacokinetics:
Absorption: Rapidly and well absorbed from the gastrointestinal tract. Food and milk decreases bioavailability. Time to peak plasma concentration: Approx 30-60 minutes.
Distribution: Penetrates synovial fluid and enters breast milk (very small amounts). Plasma protein binding: >99%, to albumin.
Metabolism: Metabolised in the liver via oxidation and conjugation.
Excretion: Mainly via urine (as inactive metabolites/conjugates and unchanged drug). Elimination half-life: Biphasic 1-2 hours (rapid); approx 5 hours (slow).
Đặc tính

Chemical Structure Image
Tolmetin sodium

Source: National Center for Biotechnology Information. PubChem Database. Tolmetin sodium, CID=23665411, https://pubchem.ncbi.nlm.nih.gov/compound/Tolmetin-sodium (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
Thuốc kháng viêm không steroid
Phân loại ATC
M01AB03 - tolmetin ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.
Tài liệu tham khảo
Anon. Tolmetin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/11/2017.

Buckingham R (ed). Tolmetin Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/11/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Tolmetin Sodium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 08/11/2017.

Tolectin DS Capsules/Tolectin 600 Tablets (Ortho-Mcneil Pharmaceutical, Inc.). U.S. FDA. https://www.fda.gov/. Accessed 09/11/2017.

Tolmetin Sodium Tablet, Film Coated (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/11/2017.

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