Tolmetin

Tolmetin Should be taken with food.

Hypersensitivity. History of asthma, urticaria or allergic-type reactions following use of aspirin or other NSAIDs. Use in the setting of CABG surgery.

Patient with known CV risk factors or disease (e.g. recent MI, hypertension, heart failure); prior history of peptic ulcer disease or gastrointestinal bleeding, other risk factors for gastrointestinal bleeding (e.g. prolonged NSAID use, smoking, alcohol use, concomitant use of oral corticosteroids or anticoagulants); preexisting asthma without known aspirin sensitivity; coagulation disorder. Debilitated or dehydrated patients. Renal and hepatic impairment. Children and elderly. Avoid use at approx 30 weeks of gestation and later in pregnancy. Lactation.

Significant: New-onset or worsening hypertension; fluid retention and oedema; acute interstitial nephritis with haematuria, proteinuria, nephrotic syndrome; anaphylactoid reactions, elevated ALT or AST levels (≥3 times the ULN), may prolong bleeding time. Rarely, severe blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia).
Cardiac disorders: Chest pain.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbance.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, dyspepsia, gastrointestinal distress, flatulence, constipation, gastritis.
General disorders and administration site conditions: Asthenia.
Investigations: Weight gain or loss; decreased haematocrit or Hb (transient); elevated BUN.
Nervous system disorders: Headache, dizziness, drowsiness.
Psychiatric disorders: Depression.
Renal and urinary disorders: UTI.
Skin and subcutaneous tissue disorders: Skin irritation.
Potentially Fatal: Increased risk of serious CV thrombotic events (e.g. MI, stroke); serious gastrointestinal adverse events (e.g. gastrointestinal bleeding, ulceration and perforation); exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms. Rarely, severe hepatic reactions (e.g. jaundice, fulminant hepatitis, hepatic necrosis, hepatic failure).

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.)

Monitor blood pressure (during initiation and periodically thereafter); CBC and chemistry profile (during prolonged use); renal function (in patients at risk of renal failure). Assess for signs and symptoms of gastrointestinal ulceration and bleeding and hepatic dysfunction. Perform ophthalmologic exam in patients with visual disturbances.

May reduce the therapeutic effects of ACE inhibitors, thiazides or loop diuretics. May increase the plasma levels and reduce the renal clearance of lithium. May increase the risk of adverse effects (particularly bleeding) with aspirin. Increased prothrombin time and bleeding with warfarin.

Decreased peak plasma concentration and total bioavailability with food or milk.

May cause false-positive test results for proteinuria in tests that rely on acid precipitation as an endpoint (e.g. sulfosalicylic acid), urine detection of cannabinoids, and aldosterone/renin ratio.

Description:
Overview: Tolmetin, an NSAID, has antipyretic, analgesic, and anti-inflammatory properties.
Mechanism of Action: Tolmetin reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, leading to reduced formation of prostaglandin precursors.
Pharmacodynamics: Tolmetin does not directly affect hyperalgesia or the pain threshold. The anti-inflammatory effects of tolmetin may be mainly due to the inhibition of COX-2 enzyme.

Inhibition of platelet aggregation observed with tolmetin is due to the dose-dependent COX-1 inhibition in platelets, leading to reduced platelet thromboxane A₂ levels and increased bleeding time.
Onset: Analgesic: 1-2 hours. Anti-inflammatory: May take days to weeks.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Food or milk reduces peak plasma concentration and total bioavailability. Time to peak plasma concentration: Approx 30-60 minutes.
Distribution: Penetrates synovial fluid. Enters breast milk (small amounts). Plasma protein binding: >99%.
Metabolism: Metabolised in the liver via oxidation and conjugation to inactive metabolite.
Excretion: Via urine (as inactive oxidative metabolite or conjugates). Elimination half-life: Biphasic: Approx 1-2 hours (rapid phase); 5 hours (slow phase).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5509, Tolmetin. https://pubchem.ncbi.nlm.nih.gov/compound/Tolmetin. Accessed Jan. 29, 2026.

Store between 20-25°C. Protect from light.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AB03 - tolmetin ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.

Brayfield A, Cadart C (eds). Tolmetin Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/12/2025.

Tolectin Tablet, Film Coated (Poly Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/12/2025.

Tolmetin Sodium Capsule (Atland Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/12/2025.

Tolmetin. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 04/12/2025.

Tolmetin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 04/12/2025.