Toradol
Toradol
Generic Name
Toradol
Mechanism
- Selective COX‑1 and COX‑2 inhibition:
- Ketorolac is a reversible, non‑selective cyclo‑oxygenase (COX) inhibitor, suppressing prostaglandin E₂ synthesis.
- COX‑1 blockade reduces gastrointestinal (GI) prostaglandins, predisposing to ulcers and bleeding.
- COX‑2 inhibition provides the primary analgesic and anti‑inflammatory effect.
- Peripheral and central effects:
- Decreases peripheral sensitization of nociceptors.
- Modest central nervous system penetration may augment analgesia without typical central side effects of opioids.
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Pharmacokinetics
| Parameter | Details |
| Absorption | Oral: peak 15–60 min; IV: 5–10 min |
| Bioavailability | Oral ~60–70 % (decreases with food) |
| Distribution | Highly protein‑bound (~99 % to albumin) |
| Metabolism | Hepatic via conjugation (mainly glucuronidation) |
| Elimination | Renal tubular secretion; half‑life 3.5–4 h (renal) |
| Excretion | 80–90 % unchanged in urine; minimal fecal excretion |
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Indications
- Acute postoperative pain (≤ 5 days).
- Traumatic injury pain control (≤ 5 days).
- Acute gouty arthritis or inflammatory pain short‑term.
- Adjunct analgesia when opioid sparing is desired.
*Not approved for chronic pain management due to cumulative GI and renal toxicity.*
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Contraindications
- Absolute contraindications:
- History of hypersensitivity to ketorolac or other NSAIDs.
- Active GI ulceration or bleeding.
- Known renal insufficiency (CrCl < 30 mL/min).
- Pregnancy (3rd trimester) and lactation.
- Relative risks:
- Cardiovascular events (MI, stroke) in patients with pre‑existing CVD.
- Hepatic dysfunction.
- Severe comorbidities requiring prolonged use.
Warnings:
• GI complications: ulcer, perforation, bleeding.
• Renal impairment: AKI, acute tubular necrosis.
• Bleeding risk: coagulation interference; avoid concurrent anticoagulants.
• Caution in elderly: higher susceptibility to GI/renal side effects.
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Dosing
| Form | Typical Dose | Duration | Max Daily Dose |
| IV/IM | 15 mg every 6 hr, up to 120 mg/day | ≤ 5 days | 120 mg/day |
| PO | 10 mg every 6 hr, up to 120 mg/day | ≤ 5 days | 120 mg/day |
| SC | 10 mg every 6 hr | ≤ 5 days | 120 mg/day |
• Loading dose: 30 mg IV or IM may be considered for severe pain but rarely required.
• Titration: Start with lowest effective dose; increment only if pain persists and patient tolerates.
• Discontinuation: Stop abruptly after 5 days; switching to long‑acting analgesic (e.g., NSAID or opioid) is advisable for sustained pain.
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Adverse Effects
Common (≥ 2–5 %)
• Nausea, dyspepsia, abdominal discomfort.
• Headache, dizziness.
• Somnolence, blurred vision.
• Minor edema or fluid retention.
Serious (≤ 1 %)
• GI ulceration, perforation, hemorrhage.
• Acute kidney injury (AKI), renal insufficiency.
• Bleeding diathesis (especially with anticoagulants).
• Hypersensitivity reactions (rash, angioedema).
• Pulmonary edema (rare).
• Cardiovascular events (MI, stroke).
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Monitoring
| Parameter | Frequency | Rationale |
| Renal function (CrCl/BUN/Creatinine) | Baseline, then every 48–72 h during therapy | Detect AKI early. |
| Hemoglobin/Hematocrit | Baseline, then weekly | Monitor for GI bleeding. |
| BP & HR | Baseline, then every 2–3 days | NSAIDs may alter BP control. |
| GI signs (abdominal pain, melena) | Continuous patient assessment | Early sign of ulceration. |
| Coagulation panel if on warfarin | Baseline, then 3–5 days | NSAIDs potentiate anticoagulation. |
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Clinical Pearls
1. “Five‑day rule” – Toradol should not exceed 5 days of continuous therapy in any patient; this limits cumulative GI and renal risk while maintaining efficacy.
2. Avoid concurrent NSAIDs – Co‑administration can double the risk of GI bleeding; safe only if clinically justified and with gastroprotection.
3. Pre‑operative handover – Document prior NSAID exposure; patients with chronic NSAID use need tapering or alternative analgesia to prevent AKI.
4. Elderly caution – Their decreased renal reserve and increased GI fragility make dosing at the low end of the spectrum imperative; consider 5 mg q6h PO.
5. Post‑delivery postpartum – Not recommended due to bleeding risk; use paracetamol/acetaminophen as first line.
6. Acute gout flare – Ketorolac’s COX‑2 inhibition offers anti‑inflammatory benefit, but be wary of renal congestion; check serum creatinine before use.
7. Drug–drug synergy – Ketorolac increases warfarin’s INR; hold warfarin for 24 h after last ketorolac dose and recheck INR.
8. Enteral administration – Take on an empty stomach with plenty of water to improve absorption; avoid food which can delay onset by 20–30 min.
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• *Sources: UpToDate (2023), FDA prescribing info for Toradol, NCCN Clinical Practice Guidelines for Pain Management.*