CALDOLOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CALDOLOR (CALDOLOR).
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing synthesis of prostaglandins involved in inflammation, pain, and fever.
| Metabolism | Primarily hepatic via CYP2C9; also undergoes glucuronidation; inactive metabolites excreted renally. |
| Excretion | Renal (primarily as glucuronide conjugates and inactive metabolites; <10% unchanged). Biliary/fecal elimination is negligible. |
| Half-life | 2-4 hours (terminal half-life). Clinical context: Requires dosing every 6-8 hours for sustained effect; no accumulation with normal hepatic function. |
| Protein binding | >99% bound, primarily to albumin. |
| Volume of Distribution | 0.1-0.2 L/kg. Clinical meaning: Low Vd indicates limited tissue distribution, consistent with high protein binding and hydrophilic properties. |
| Bioavailability | Intravenous: 100%. Oral: Not applicable (Caldolor is IV only); prodrug ibuprofen lysine has similar pharmacokinetics to oral ibuprofen but with faster absorption. |
| Onset of Action | Intravenous: 15-30 minutes (analgesic effect). |
| Duration of Action | 4-6 hours (analgesic/antipyretic). Clinical note: Longer duration may be observed with higher doses or in patients with hepatic impairment. |
| Molecular Weight | 206.28 |
800 mg IV every 8 hours as a 30-minute infusion; alternatively, 400 mg IV every 6 hours. Maximum daily dose: 2400 mg.
| Dosage form | SOLUTION |
| Renal impairment | Contraindicated in patients with advanced renal disease or CrCl <30 mL/min. For CrCl 30-60 mL/min: reduce dose to 400 mg every 8 hours or 200 mg every 6 hours. For CrCl >60 mL/min: no adjustment. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50% (e.g., 400 mg IV every 8 hours). Child-Pugh Class C: avoid use (contraindicated). |
| Pediatric use | Weight-based: 20 mg/kg IV every 8 hours, maximum single dose 800 mg, maximum daily dose 2400 mg. For patients <6 months: 10 mg/kg IV every 8 hours, maximum daily dose 600 mg. |
| Geriatric use | Reduce initial dose to 400 mg IV every 8 hours; monitor renal function and adjust accordingly. Use the lowest effective dose for the shortest duration. |
| 1st trimester | Avoid unless clearly needed; NSAIDs including ibuprofen have been associated with increased risk of miscarriage and congenital malformations (e.g., cardiac defects) in some studies. |
| 2nd trimester | Use with caution; generally considered safer than third trimester, but may reduce amniotic fluid and affect fetal renal function; lowest effective dose for shortest duration. |
| 3rd trimester | Avoid from 30 weeks onward; associated with premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment; risk of periventricular hemorrhage. |
Clinical note
Comprehensive clinical and safety monograph for CALDOLOR (CALDOLOR).
| Placental transfer | Crosses placenta; detectable in fetal plasma and amniotic fluid. Degree of transfer increases with gestational age. |
| Breastfeeding | Ibuprofen (CALDOLOR) is excreted into breast milk in very small amounts; considered compatible with breastfeeding. Peak milk concentration is minimal (<1% of maternal weight-adjusted dose). No adverse effects reported in infants. Use lowest effective dose for shortest duration. |
■ 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. NSAIDs are contraindicated for the 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.
| Serious Effects |
History of hypersensitivity to ibuprofen or any NSAIDActive or history of recurrent peptic ulcer disease/hemorrhageSevere heart failure (NYHA class III-IV)Severe renal impairment (eGFR <30 mL/min/1.73 m²)Treatment of perioperative pain in coronary artery bypass graft (CABG) surgeryThird trimester of pregnancy
| Precautions | Cardiovascular thrombotic events (MI, stroke), Gastrointestinal bleeding, ulceration, and perforation, Hypertension, Heart failure and edema, Renal toxicity (especially in patients with impaired renal function), Anaphylactoid reactions, Serious skin reactions (e.g., Stevens-Johnson syndrome), Hematologic effects (inhibition of platelet aggregation), Hepatic effects (elevated liver enzymes, rare hepatic failure) |
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| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | NSAIDs, including ibuprofen (CALDOLOR), are contraindicated in the third trimester due to risk of premature closure of the ductus arteriosus and oligohydramnios. In the first and second trimesters, use only if clearly needed; potential risks include spontaneous abortion and congenital malformations (e.g., gastroschisis), though data are conflicting. |
| Fetal Monitoring | Monitor for oligohydramnios (sonographic amniotic fluid index) and fetal ductus arteriosus patency (Doppler echocardiography) if used in the third trimester. Maternal monitoring includes blood pressure, renal function, and signs of bleeding. |
| Fertility Effects | Reversible inhibition of ovulation and delayed conception due to interference with prostaglandin synthesis. Effect is dose-dependent and resolves upon discontinuation. |
| Food/Dietary | Avoid alcohol consumption. No specific food restrictions, but taking with food may reduce GI upset. Grapefruit juice has no known interaction. |
| Clinical Pearls | CALDOLOR (ibuprofen) injection is used for mild to moderate pain and for moderate to severe pain as an adjunct to opioids. Onset of action is within 15-30 minutes. Monitor renal function in elderly, volume-depleted, or those with renal impairment. Avoid use in patients with significant renal impairment (CrCl <30 mL/min). Contraindicated in perioperative CABG surgery pain. May increase risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke. Use the lowest effective dose for shortest duration. |
| Patient Advice | Take this medication exactly as prescribed by your doctor. · Do not take more than prescribed or for longer than directed. · Avoid drinking alcohol while taking this medicine. · Tell your doctor if you have a history of stomach ulcers, bleeding problems, heart disease, high blood pressure, or kidney disease. · Contact your doctor immediately if you experience signs of stomach bleeding (black/bloody stools, coffee-ground vomit) or cardiovascular events (chest pain, shortness of breath, slurred speech). · Do not take other NSAIDs or aspirin while on this medication without doctor approval. |