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). |
| Molecular Weight | 296.15 |
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 | Avoid: NSAIDs are associated with increased risk of miscarriage and congenital malformations (e.g., cardiac defects) if used in early pregnancy. |
| 2nd trimester | Caution: Use lowest effective dose for shortest duration. NSAIDs may cause oligohydramnios and premature ductus arteriosus constriction, though risk is lower in second trimester. |
| 3rd trimester | Contraindicated: NSAIDs are associated with premature closure of ductus arteriosus, oligohydramnios, and fetal renal impairment. Use after 30 weeks is contraindicated. |
Clinical note
Comprehensive clinical and safety monograph for DYLOJECT (DYLOJECT).
| Placental transfer | Diclofenac crosses the placenta. Fetal concentrations are approximately 30% of maternal plasma concentrations. Evidence from animal and human studies indicates placental transfer. |
| Breastfeeding | Diclofenac (Dyloject) is excreted into breast milk in low amounts (<1% of maternal dose). It is considered compatible with breastfeeding; however, monitor infant for potential adverse effects such as gastrointestinal upset or bleeding. Use the lowest effective dose. |
■ 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 hypersensitivity to diclofenac or any component of the formulationHistory of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDsActive peptic ulcer disease or gastrointestinal bleedingSignificant renal impairment (CrCl <30 mL/min)Severe hepatic impairment (Child-Pugh class C)Treatment of perioperative pain in coronary artery bypass graft (CABG) surgeryThird trimester of pregnancy (after 30 weeks gestation)
| 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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| Lactation Rating | L2 (Safer) |
| 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. |
| 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. |
| Food/Dietary | Avoid alcohol; may increase GI bleeding risk. No specific food restrictions, but taking with food can reduce GI discomfort. |
| Clinical Pearls | DYLOJECT (diclofenac sodium) is an NSAID for IM injection; onset within 30 min. Avoid in patients with CrCl <30 mL/min. Do not administer if patient has received aspirin or other NSAIDs within 24 hours. Rotate injection sites; monitor for anaphylaxis, especially in asthmatics. Contraindicated in setting of coronary artery bypass graft surgery. |
| Patient Advice | Report any signs of bleeding, such as black or bloody stools, or unusual bruising. · Avoid taking aspirin, ibuprofen, naproxen, or other NSAIDs while using this medication. · Do not use alcohol while taking this drug as it increases risk of stomach bleeding. · Seek immediate medical help if you experience chest pain, shortness of breath, slurred speech, or weakness on one side. · Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. · Take with food or milk to reduce stomach upset; do not crush or chew the extended-release tablets. |