DYLOJECT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DYLOJECT (DYLOJECT).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), thereby reducing prostaglandin synthesis, which mediates inflammation, pain, and fever.
| Metabolism | Hepatic metabolism primarily via CYP2C9 isoenzyme; also undergoes glucuronidation and oxidation. |
| Excretion | Renal: ~50% as unchanged drug and metabolites (glucuronide conjugates); Biliary/fecal: ~40% as metabolites; <5% unchanged in feces. |
| Half-life | 2-4 hours (terminal) in adults; prolonged in elderly (up to 6-8 hours) and hepatic impairment (up to 12 hours). |
| Protein binding | 99.7% bound primarily to albumin. |
| Volume of Distribution | 0.1-0.2 L/kg (low Vd, indicating limited tissue distribution and high plasma protein binding). |
| Bioavailability | Oral: ~90% (with food slightly decreases rate but extent unchanged); IM: 100% (complete). |
| Onset of Action | Oral: 30-60 minutes; Intramuscular: 20-30 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Analgesic: 4-6 hours (oral/IM); Anti-inflammatory: up to 8 hours; shorter duration with IV bolus (due to rapid redistribution). |
50 mg intramuscularly every 6 hours as needed for pain; maximum 150 mg per day.
| Dosage form | SOLUTION |
| Renal impairment | CrCl 30-60 mL/min: 50 mg every 8 hours; CrCl <30 mL/min: 50 mg every 12 hours; not recommended in dialysis. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50 mg every 8 hours; Child-Pugh C: avoid use. |
| Pediatric use | 1 mg/kg intramuscularly every 6-8 hours; maximum 5 mg/kg per day; not for children <6 months. |
| Geriatric use | Initiate at 50 mg intramuscularly every 8 hours; maximum 100 mg per day due to increased risk of CNS effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DYLOJECT (DYLOJECT).
| Breastfeeding | Contraindicated: Diclofenac (active component) is excreted into breast milk at low levels (M/P ratio ~0.03). However, due to risk of adverse effects in infant (e.g., platelet dysfunction, renal impairment), use is not recommended. |
| Teratogenic Risk | Category D: Known to cause fetal harm in first and third trimesters. First trimester: increased risk of cardiovascular and neural tube defects. Third trimester: premature closure of ductus arteriosus, oligohydramnios, and necrotizing enterocolitis. Avoid in second trimester unless absolutely necessary. |
■ 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 increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. DYLOJECT is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery. NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients and patients with a prior history of peptic ulcer disease and/or GI bleeding are at greater risk.
| Serious Effects |
["History of asthma, urticaria, or allergic-type reactions to aspirin or other NSAIDs","Perioperative pain setting of coronary artery bypass graft (CABG) surgery","Active gastrointestinal bleeding or peptic ulcer disease","Advanced renal disease","Third trimester of pregnancy"]
| Precautions | ["Cardiovascular thrombotic events (including MI and stroke)","Gastrointestinal bleeding, ulceration, and perforation","Hypertension and fluid retention","Renal toxicity including papillary necrosis and renal failure","Hepatic effects including elevated liver enzymes and severe hepatic reactions","Anaphylactoid reactions and asthma exacerbation","Serious skin reactions (e.g., Stevens-Johnson syndrome, exfoliative dermatitis)","Hematologic effects (e.g., prolonged bleeding time)","NSAID use during late pregnancy should be avoided (risk of premature closure of ductus arteriosus)","Ophthalmologic effects with prolonged use"] |
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| Fetal Monitoring |
| Monitor maternal renal function, blood pressure, and amniotic fluid index. Perform fetal echocardiography in second trimester if exposed. Monitor for oligohydramnios and ductus arteriosus constriction via ultrasound. |
| Fertility Effects | Reversible impairment: Diclofenac may inhibit ovulation by interfering with prostaglandin synthesis. Effects on spermatogenesis are not well established but potential for decreased fertility in males. |