Introduction
Dyloject (diclofenac sodium) is an intravenous nonsteroidal anti-inflammatory drug (NSAID) specifically formulated for hospital use. It provides rapid onset of analgesic and anti-inflammatory effects for patients who cannot take oral medications. Dyloject offers the therapeutic benefits of diclofenac with the advantage of parenteral administration, making it particularly valuable in postoperative pain management and other acute care settings.
Mechanism of Action
Dyloject exerts its pharmacological effects through inhibition of prostaglandin synthesis by competitive inhibition of cyclooxygenase (COX) isoenzymes, primarily COX-1 and COX-2. This inhibition reduces the conversion of arachidonic acid to prostaglandin precursors, thereby decreasing inflammation, pain, and fever. The intravenous formulation provides more rapid achievement of therapeutic concentrations compared to oral administration.
Indications
Dyloject is indicated for:
- Management of mild to moderate pain
- Management of moderate to severe pain as an adjunct to opioid analgesics
- Treatment of primary dysmenorrhea
It is specifically approved for use in hospitalized patients who require analgesic therapy but cannot take oral medications.
Dosage and Administration
Standard dosing: 37.5 mg administered by IV injection over no less than 15 seconds every 6 hours as needed Maximum daily dose: 150 mg (four doses) Special populations:- Elderly: Use the lowest effective dose; consider reduced frequency
- Renal impairment: Not recommended in patients with advanced renal disease
- Hepatic impairment: Use with caution in patients with hepatic impairment
- Pediatric: Safety and effectiveness not established
- For IV use only
- Administer undiluted
- Inject slowly over at least 15 seconds
- Do not mix with other medications
- Use aseptic technique
Pharmacokinetics
Absorption: Complete and immediate bioavailability following IV administration Distribution: Volume of distribution approximately 1.4 L/kg; >99% bound to plasma proteins Metabolism: Extensive first-pass metabolism primarily via CYP2C9, with minor contributions from CYP2C8 and CYP3A4. Forms multiple metabolites including 4'-hydroxy-, 3'-hydroxy-, and 5-hydroxy-diclofenac Elimination: Terminal half-life of approximately 2 hours; excreted primarily in urine (65%) and bile (35%) as metabolitesContraindications
- Hypersensitivity to diclofenac or other NSAIDs
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
- Perioperative pain in coronary artery bypass graft (CABG) surgery
- Third trimester of pregnancy
Warnings and Precautions
Cardiovascular risk: NSAIDs may increase risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke GI risk: Risk of GI bleeding, ulceration, and perforation Hepatotoxicity: Severe hepatic reactions, including liver failure, have been reported Hypertension: New onset or exacerbation of existing hypertension Heart failure: Fluid retention and edema have been observed Renal effects: Renal toxicity including papillary necrosis; risk increased in patients with renal impairment, heart failure, or liver dysfunction Anaphylactoid reactions: May occur even without prior exposure Hematologic effects: Anemia may occur; monitor hemoglobin periodicallyDrug Interactions
Anticoagulants: Increased risk of bleeding with warfarin, heparin, and other anticoagulants Aspirin: Concomitant use may increase GI toxicity ACE inhibitors/ARBs: Reduced antihypertensive effect; increased risk of renal impairment Diuretics: Reduced diuretic and antihypertensive efficacy Lithium: Increased lithium plasma levels Methotrexate: Increased methotrexate toxicity Cyclosporine: Increased nephrotoxicity risk SSRIs/SNRIs: Increased risk of GI bleedingAdverse Effects
Common (≥2%):- Nausea (8%)
- Headache (7%)
- Vomiting (4%)
- Dizziness (3%)
- Somnolence (3%)
- Injection site pain (2%)
- GI bleeding, ulceration, perforation
- Cardiovascular thrombotic events
- Hepatotoxicity
- Hypertension
- Acute renal failure
- Anaphylactoid reactions
- Hematologic toxicity (anemia, neutropenia)
Monitoring Parameters
- Pain assessment and relief
- Blood pressure regularly
- Renal function (BUN, creatinine)
- Hepatic function (ALT, AST)
- Hemoglobin/hematocrit with chronic use
- Signs of GI bleeding
- Signs of fluid retention
- Injection site reactions
Patient Education
- This medication is for short-term use in hospital settings
- Report any signs of allergic reaction immediately (rash, itching, swelling)
- Notify healthcare providers of any unusual bleeding or bruising
- Inform providers of all medications being taken
- Report signs of GI discomfort or blood in stool
- Be aware of potential dizziness or drowsiness
- Notify providers of history of heart, kidney, or liver problems
- Understand that this medication is not for long-term use
References
1. Dyloject [package insert]. Lake Forest, IL: Hospira Inc.; 2021. 2. Sinatra RS, Jahr JS, Reynolds LW, et al. Efficacy and safety of single and repeated administration of 1 gram intravenous acetaminophen injection (paracetamol) for pain management after major orthopedic surgery. Anesthesiology. 2005;102(4):822-831. 3. American Pain Society. Principles of Analgesic Use in the Treatment of Acute Pain and Cancer Pain. 7th ed. American Pain Society; 2016. 4. Bombardier C, Laine L, Reicin A, et al. Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. N Engl J Med. 2000;343(21):1520-1528. 5. FDA Drug Safety Communication: FDA strengthens warning that non-aspirin nonsteroidal anti-inflammatory drugs (NSAIDs) can cause heart attacks or strokes. US Food and Drug Administration. July 2015.