TORADOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TORADOL (TORADOL).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis.
| Metabolism | Primarily hepatic via conjugation (glucuronidation) and hydroxylation; cytochrome P450 involvement is minor. |
| Excretion | Renal: approximately 92% (unchanged: 60%, metabolites: 32%); fecal: 6%; biliary: <2%. |
| Half-life | Terminal elimination half-life: 5-6 hours, prolonged to 13-17 hours in elderly and up to 19 hours in renal impairment (creatinine clearance <30 mL/min). |
| Protein binding | Highly protein bound (≥99%) primarily to albumin. |
| Volume of Distribution | Vd: 0.15-0.45 L/kg. Low Vd indicates limited extravascular distribution, consistent with high protein binding. |
| Bioavailability | Intramuscular: 100%; Oral: 80-100% (due to first-pass metabolism, actual systemic availability ~60-80%). |
| Onset of Action | Intravenous: 10-30 minutes; Intramuscular: 15-45 minutes; Oral: 30-60 minutes. |
| Duration of Action | Analgesic duration: 4-6 hours (IV/IM); 4-6 hours (oral). Note: Short-term use only (≤5 days) due to gastrointestinal and renal risks. |
20 mg IM/IV once, then 10 mg IM/IV every 4-6 hours; maximum 120 mg/day (including oral). Oral: 10 mg every 4-6 hours, maximum 40 mg/day.
| Dosage form | TABLET |
| Renal impairment | Creatinine clearance 30-50 mL/min: maximum dose 60 mg/day IM/IV, 20 mg/day oral. Creatinine clearance <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh class B or C: maximum dose 60 mg/day IM/IV, 20 mg/day oral. Not recommended in severe hepatic impairment. |
| Pediatric use | ≥2 years: 0.5 mg/kg IV/IM single dose, maximum 15 mg; then 0.5 mg/kg every 6 hours, maximum 60 mg/day. Not recommended for >5 days. |
| Geriatric use | ≥65 years: maximum dose 60 mg/day IM/IV, 20 mg/day oral. Use shortest duration possible; increased risk of GI and renal adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TORADOL (TORADOL).
| Breastfeeding | Excreted into human milk; M/P ratio not established. Avoid use during breastfeeding due to potential adverse effects on neonatal cardiovascular and renal systems. If essential, use lowest effective dose for shortest duration. |
| Teratogenic Risk | Pregnancy Category C (first and second trimester) and Category D (third trimester). First trimester: No adequate studies; potential risk based on prostaglandin synthesis inhibition affecting implantation and embryo development. Second trimester: Limited data; avoid prolonged use. Third trimester: Contraindicated due to risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
■ FDA Black Box Warning
NSAIDs cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. Risk increases with duration of use. Contraindicated for treatment of perioperative pain in coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Active peptic ulcer disease, recent GI bleeding, history of asthma or allergic-type reactions to aspirin or NSAIDs, severe renal impairment (CrCl <30 mL/min), perioperative pain in CABG surgery, advanced renal disease, labor and delivery (may inhibit uterine contractions and affect fetal circulation).
| Precautions | Risk of GI bleeding, ulceration, and perforation; increased cardiovascular risk; renal toxicity; anaphylactoid reactions; inhibits platelet aggregation; may cause hypertension; caution in patients with asthma, liver or renal impairment. |
Loading safety data…
| Fetal Monitoring | Monitor fetal heart rate, amniotic fluid index, and ductus arteriosus patency via ultrasound if used in second/third trimester. Assess maternal renal function and platelet count. In neonates, monitor for signs of renal impairment and bleeding tendencies if exposed near delivery. |
| Fertility Effects | Ketorolac may inhibit ovulation and impair female fertility due to prostaglandin synthesis inhibition. Reversible upon discontinuation. No specific impact on male fertility reported. |