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. |
| Molecular Weight | 376.41 |
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 | Avoid use in first trimester due to risk of adverse effects; limited data on safety. |
| 2nd trimester | Use only if clearly needed; may cause premature closure of ductus arteriosus and oligohydramnios. |
| 3rd trimester | Contraindicated in third trimester due to risk of premature closure of ductus arteriosus and oligohydramnios. |
Clinical note
Comprehensive clinical and safety monograph for TORADOL (TORADOL).
| Placental transfer | Ketorolac crosses the placenta; detectable in fetal plasma and amniotic fluid. |
| Breastfeeding | Toradol (ketorolac) is excreted into breast milk in low amounts. Due to potential adverse effects on infant cardiovascular system and risk of gastrointestinal bleeding, use is not recommended in nursing mothers. |
■ 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 diseaseRecent gastrointestinal bleeding or perforationHistory of asthma, urticaria, or allergic-type reactions after aspirin or other NSAIDsAdvanced renal diseaseRisk of or existing cerebrovascular bleedingConcomitant use of probenecid or pentoxifyllineSuspected or confirmed intracranial hemorrhageThird trimester of pregnancyBreastfeeding (relative, but often considered absolute in clinical practice)Hypersensitivity to ketorolac or any component of the formulation
| 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. |
| Food/Dietary | Take with food or milk to reduce gastrointestinal irritation. Avoid alcohol as it may increase the risk of GI bleeding. Grapefruit juice may increase drug levels; although interaction is not well-established, caution is advised. |
Loading safety data…
| Lactation Rating |
| L3 (Moderately Safe) – Use with caution; alternative preferred. |
| 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. |
| 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. |
| Clinical Pearls | Toradol (ketorolac tromethamine) is an NSAID for short-term (≤5 days) management of moderate-to-severe acute pain. Avoid in patients with active peptic ulcer disease, renal impairment (CrCl <30 mL/min), bleeding diathesis, or those at high risk for cardiovascular events. Maximum duration is 5 days; do not use for minor or chronic pain. Administer with food to reduce GI irritation. Intramuscular injection should be given deeply and slowly to minimize pain and sterile abscess formation. Contraindicated in patients with nasal polyps, angioedema, or bronchospasm after aspirin or other NSAIDs. Use lowest effective dose for shortest duration. Monitor renal function, especially in elderly or dehydrated patients. |
| Patient Advice | Take Toradol exactly as prescribed, usually for no longer than 5 days as it can cause serious side effects with longer use. · Swallow tablets whole with food or milk to reduce stomach upset. · Avoid taking more than one NSAID (e.g., ibuprofen, naproxen, aspirin) as it increases risk of stomach bleeding or ulcers. · Report black or bloody stools, vomit that looks like coffee grounds, chest pain, shortness of breath, or signs of allergic reaction (rash, swelling, difficulty breathing) immediately. · Toradol can cause dizziness or drowsiness; avoid driving or operating heavy machinery until you know how it affects you. · Limit alcohol intake as it increases the risk of stomach bleeding. · Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding, as Toradol is not recommended in late pregnancy. · Do not use Toradol if you have active peptic ulcer disease, kidney disease (CrCl <30 mL/min), or bleeding problems. |