Introduction
Caldolor (ibuprofen) injection is a nonsteroidal anti-inflammatory drug (NSAID) available in intravenous formulation. It represents an important therapeutic option for patients who cannot tolerate oral medications or require rapid onset of analgesic, antipyretic, or anti-inflammatory effects. Approved by the FDA in 2009, IV ibuprofen provides clinicians with an alternative to oral NSAIDs in hospital settings.
Mechanism of Action
Caldolor exerts its pharmacological effects through inhibition of prostaglandin synthesis via non-selective cyclooxygenase (COX) inhibition. It reversibly inhibits both COX-1 and COX-2 enzymes, thereby reducing the formation of prostaglandin precursors. This mechanism provides analgesic, antipyretic, and anti-inflammatory effects. The inhibition of prostaglandin synthesis is dose-dependent and correlates with clinical efficacy.
Indications
FDA-approved indications include:
- Management of mild to moderate pain
- Management of moderate to severe pain as an adjunct to opioid analgesia
- Reduction of fever in adults
Clinical applications often extend to postoperative pain management, musculoskeletal pain, and inflammatory conditions where oral administration is not feasible.
Dosage and Administration
Standard dosing:- Pain: 400-800 mg IV every 6 hours as needed
- Fever: 400 mg IV initially, then 400 mg every 4-6 hours or 100-200 mg every 4 hours as needed
- Must be diluted to a final concentration of 4 mg/mL or less in 0.9% NaCl, 5% Dextrose, or Lactated Ringer's solution
- Infuse over at least 30 minutes
- Maximum daily dose: 3200 mg
- Renal impairment: Use caution; avoid in advanced renal disease
- Hepatic impairment: Use caution in severe hepatic impairment
- Elderly: Consider reduced doses due to increased NSAID sensitivity
- Pediatrics: Safety and efficacy not established for patients <17 years
Pharmacokinetics
Absorption: Complete bioavailability following IV administration Distribution: Volume of distribution approximately 0.15 L/kg; 99% protein-bound Metabolism: Hepatic metabolism primarily via CYP2C9 with minor CYP2C8 involvement Elimination: Renal excretion (90% as metabolites, <1% unchanged); elimination half-life 2-2.5 hoursContraindications
- Known hypersensitivity to ibuprofen 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
Boxed Warning: Risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal- Increased risk of serious gastrointestinal bleeding, ulceration, and perforation
- Risk of renal injury, including acute renal failure
- Hepatic injury, including rare cases of fatal hepatitis
- Hypertension exacerbation and heart failure worsening
- Anaphylactoid reactions possible
- Hematologic effects including anemia and bleeding
Drug Interactions
Significant interactions:- Aspirin: Reduced cardioprotective effects; avoid concomitant use
- Anticoagulants (warfarin): Increased bleeding risk
- ACE inhibitors/ARBs: Reduced antihypertensive effect; renal risk
- Diuretics: Reduced diuretic efficacy; renal risk
- Lithium: Increased lithium levels
- Methotrexate: Increased methotrexate toxicity
- SSRIs/SNRIs: Increased bleeding risk
- Cyclosporine: Increased nephrotoxicity
Adverse Effects
Common (≥1%):- Nausea, vomiting, flatulence
- Headache, dizziness
- Edema, hypertension
- Anemia
- Gastrointestinal bleeding/perforation
- Myocardial infarction, stroke
- Acute renal failure
- Severe cutaneous adverse reactions
- Anaphylaxis
- Hepatotoxicity
Monitoring Parameters
- Pain assessment and fever monitoring
- Renal function (BUN, creatinine)
- Hepatic function (ALT, AST)
- Complete blood count
- Blood pressure
- Signs of gastrointestinal bleeding
- Fluid status and edema
- Therapeutic response and adverse effects
Patient Education
- Report any signs of bleeding (unusual bruising, blood in stool)
- Monitor for cardiovascular symptoms (chest pain, shortness of breath)
- Report signs of allergic reaction (rash, swelling, difficulty breathing)
- Avoid concurrent aspirin use unless specifically directed
- Report symptoms of gastrointestinal upset or ulceration
- Inform all healthcare providers of Caldolor use
- Do not use during late pregnancy
- Report any visual changes or hearing problems
References
1. FDA Prescribing Information: Caldolor (ibuprofen) Injection. 2021 2. Southworth S, et al. Pharmacotherapy. 2009;29(12):1459-1470 3. Kroll PB, et al. Clin Ther. 2007;29(11):2516-2529 4. American Society of Health-System Pharmacists. AHFS Drug Information. 2023 5. Lexicomp Online. Ibuprofen (Intravenous). Wolters Kluwer Clinical Drug Information 6. Clinical Pharmacology [database online]. Tampa, FL: Elsevier 7. Cochrane Database Syst Rev. 2015;(7):CD011558 8. Ann Pharmacother. 2010;44(5):924-933
This information is intended for educational purposes only and should not replace professional medical advice. Always consult with qualified healthcare providers for medical decisions.