DOLOBID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DOLOBID (DOLOBID).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis.
| Metabolism | Primarily hepatic via glucuronidation; minor metabolism via CYP2C9. Metabolites include diflunisal glucuronides. |
| Excretion | Renal: ~90% as glucuronide conjugates (diflunisal acyl glucuronide, diflunisal phenolic glucuronide); <5% unchanged. Biliary/fecal: minimal, <10%. |
| Half-life | Terminal elimination half-life: 8-12 hours (dose-dependent; prolonged up to 15 hours with higher doses). Clinical context: allows twice-daily dosing; extended half-life in renal impairment. |
| Protein binding | >99% bound, primarily to albumin (saturable at high concentrations). |
| Volume of Distribution | 0.1-0.15 L/kg. Small Vd indicates extensive plasma protein binding and limited tissue distribution. |
| Bioavailability | Oral: ~80-90% (absolute bioavailability not fully established; high due to minimal first-pass metabolism). |
| Onset of Action | Oral: analgesic effect within 1 hour; anti-inflammatory effect within 2-3 days (due to steady-state accumulation). |
| Duration of Action | Analgesic: 6-12 hours (dose-dependent). Max anti-inflammatory effect may take up to 1 week. Long duration due to slow elimination. |
| Brand Substitutes | Jasdase 50mg/15mg Tablet, Ugflam S 50mg/15mg Tablet, Difzol-S Tablet, Nacflam S 50mg/15mg Tablet, Defcon S 50mg/15mg Tablet |
250-500 mg orally twice daily. Maximum 1500 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 50%. GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid use. |
| Pediatric use | Not recommended for pediatric patients. |
| Geriatric use | Start at lowest effective dose; maximum 1000 mg/day. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DOLOBID (DOLOBID).
| Breastfeeding | Diflunisal is excreted into breast milk in low amounts; M/P ratio is approximately 0.1-0.2. Based on limited data, risk to infant is considered low, but avoid if possible due to potential adverse effects on platelet function and renal function. Use with caution and monitor infant for adverse effects. |
| Teratogenic Risk | First trimester: NSAIDs are associated with a slightly increased risk of miscarriage and congenital malformations, particularly cardiac defects. Second trimester: No major teratogenic effects reported; however, use with caution due to potential for oligohydramnios and fetal renal impairment. Third trimester: Avoid due to risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal dysfunction. NSAIDs also increase risk of periventricular hemorrhage in preterm infants. |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use. DOLOBID is contraindicated in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
["Hypersensitivity to diflunisal or any NSAID","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs","Perioperative pain in the setting of coronary artery bypass graft (CABG) surgery","Advanced renal disease","Active peptic ulcer disease or gastrointestinal bleeding"]
| Precautions | ["Cardiovascular thrombotic events","Gastrointestinal bleeding, ulceration, and perforation","Renal toxicity","Hepatic effects","Hypertension","Fluid retention and edema","Anaphylactoid reactions","Serious skin reactions (e.g., Stevens-Johnson syndrome)"] |
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| Fetal Monitoring | Monitor maternal renal function, blood pressure, and signs of gastrointestinal bleeding. Fetal monitoring includes ultrasound assessment of amniotic fluid volume (to detect oligohydramnios) and ductus arteriosus patency in third trimester. Assess neonatal platelet function and renal function if exposed near term. |
| Fertility Effects | NSAIDs including diflunisal may reversibly impair female fertility by inhibiting prostaglandin synthesis, affecting ovulation and implantation. Consider discontinuation if pregnancy is planned. |