TOLECTIN DS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TOLECTIN DS (TOLECTIN DS).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis.
| Metabolism | Hepatic metabolism primarily via oxidation and conjugation (glucuronidation); minor involvement of CYP450 enzymes. |
| Excretion | Primarily renal, 95% of a dose excreted in urine as glucuronide conjugates and oxidative metabolites; less than 5% fecal. |
| Half-life | Terminal elimination half-life approximately 1 hour; clinical context: requires frequent dosing every 6-8 hours due to short half-life. |
| Protein binding | Approximately 99% bound to plasma albumin. |
| Volume of Distribution | 0.1-0.2 L/kg; indicates distribution primarily in extracellular fluid and plasma. |
| Bioavailability | Oral: approximately 100% (well absorbed). |
| Onset of Action | Oral: 30-60 minutes to analgesia; anti-inflammatory effect within a few days to 2 weeks. |
| Duration of Action | Oral: 4-6 hours for analgesia; anti-inflammatory effect may persist longer with regular dosing. |
400 mg orally three times daily; maximum dose 1800 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | GFR 30-89 mL/min: no adjustment needed. GFR < 30 mL/min: caution, reduce dose by 50% or increase interval to every 12 hours. Not recommended in severe renal failure. |
| Liver impairment | Child-Pugh class A: no adjustment needed. Child-Pugh class B or C: avoid use due to increased risk of hepatotoxicity. |
| Pediatric use | Children >=2 years: starting dose 20 mg/kg/day orally in 3-4 divided doses; maintenance dose 15-30 mg/kg/day. Maximum 30 mg/kg/day or 1800 mg/day, whichever is less. |
| Geriatric use | Initiate at lowest effective dose; monitor renal function and adjust accordingly. Consider dose reduction by 25-50% in elderly due to increased risk of GI bleeding and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TOLECTIN DS (TOLECTIN DS).
| Breastfeeding | Excreted into breast milk in low amounts; M/P ratio 0.3; consider risks of infant NSAID exposure; avoid if possible, especially with prolonged use. |
| Teratogenic Risk | First trimester: increased risk of cardiac defects and gastroschisis; third trimester: risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment; avoid in pregnancy especially after 30 weeks. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cardiovascular thrombotic events, including myocardial infarction and stroke, can occur with NSAIDs. Increased risk of serious gastrointestinal adverse events such as bleeding, ulceration, and perforation.
| Serious Effects |
Hypersensitivity to tolmetin or other NSAIDs, history of asthma, urticaria, or allergic-type reactions after aspirin/NSAIDs, perioperative pain in coronary artery bypass graft (CABG) surgery.
| Precautions | Cardiovascular risk, gastrointestinal risk, renal toxicity, hepatic effects, anaphylactoid reactions, skin reactions (including Stevens-Johnson syndrome), hematologic effects, and use in pregnancy (avoid in third trimester). |
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| Monitor renal function, amniotic fluid volume, and ductal patency via fetal echocardiography if used after 20 weeks' gestation. |
| Fertility Effects | May impair female fertility via inhibition of prostaglandin synthesis affecting ovulation; reversible upon discontinuation. |