Ketoprofen
Ketoprofen
Generic Name
Ketoprofen
Mechanism
- Cyclo‑oxygenase (COX) inhibition
- Potently blocks both COX‑1 and COX‑2 isoenzymes, decreasing prostaglandin synthesis.
- Moderately favors COX‑2 inhibition, which contributes to its anti‑inflammatory efficacy while retaining some gastrointestinal (GI) protective properties.
- Resulting effects
- ↓ prostaglandins → ↓ pain, fever, and edema.
- ↓ COX‑1 activity → potential GI mucosal damage, renal vasoconstriction, and platelet inhibition.
Pharmacokinetics
| Parameter | Value & Notes |
| Absorption | Rapid oral bioavailability (~70–80 %). Peak plasma concentration 30–60 min post‑dose. |
| Distribution | High protein binding (~95 %); distribution into tissues and CSF. |
| Metabolism | Hepatic via glucuronidation and sulfonation; minor CYP450 involvement. |
| Elimination | Renal (≈80 %) and biliary routes; half‑life 2–3 h (oral), 4–5 h (IV). |
| Drug Interactions | ↑ serum levels of warfarin, ACE inhibitors, and diuretics; ↓ ketoprofen clearance in hepatic impairment. |
Indications
- Acute musculoskeletal pain (sprains, strains).
- Relief of arthritic pain—oligoarthritis, rheumatoid arthritis, ankylosing spondylitis.
- Dental and post‑operative analgesia.
- Topical use for localized joint or muscle pain (0.5 % cream/gel).
- Premenstrual dysphoric syndrome (oral therapy).
Contraindications
- Absolute contraindications
- History of GI ulcer or perforation.
- Severe hepatic or renal disease.
- Active peptic ulcer disease.
- Known hypersensitivity to ketoprofen or other NSAIDs.
- Warnings
- Cardiovascular: ↑ risk of myocardial infarction and stroke, especially at high doses or long duration.
- GI: ulceration, bleeding, perforation.
- Renal: acute kidney injury, especially in volume‑depleted states or concomitant ACEI/ARB use.
- Pregnancy: contraindicated in third trimester; safe only in first trimester for specific indications under supervision.
- Lactation: excreted in milk—avoid in nursing mothers.
Dosing
| Regimen | Adults (≤ 50 kg) | Adults (> 50 kg) |
| Oral immediate‑release | 50 mg BID, max 250 mg/day. | 100 mg BID, max 250 mg/day. |
| Oral enteric‑coated | 100 mg BID, max 200 mg/day. | 200 mg BID, max 200 mg/day. |
| IV | 30 mg, 2–3 × day, ≈ 4 h interval. | |
| Topical | 0.5 % gel/cream: 2 × daily, 0.5–1 g per application. | – |
| Short‑term therapy | ≤ 7 days for acute pain. | ≤ 7 days for acute pain. |
*Adjust doses for renal/hepatic impairment and elderly patients.*
Monitoring
- Baseline and periodic: CBC, renal profile (creatinine, uric acid), liver enzymes (AST/ALT), electrolytes.
- Blood pressure: every 2–4 weeks during long‑term use.
- GI surveillance: assess for dyspepsia or melena; consider endoscopy if risk factors are present.
- Drug‑specific: monitor for signs of hypersensitivity and renal function.
Clinical Pearls
- Use the lowest effective dose for the shortest duration to mitigate GI and CV risks.
- Enteric-coated formulations significantly reduce GI upset but have slightly lower bioavailability—ideal for patients with chronic pain who need extended daily dosing.
- Topical ketoprofen circumvents systemic exposure, making it a safer alternative for patients at high GI or cardiac risk.
- Co‑prescribing an antacid (e.g., proton‑pump inhibitor) or using gastro‑protective agents can markedly decrease ulcer risk in high‑dose or long‑term regimens.
- Avoid concurrent use with other COX‑2 inhibitors or aspirin; the additive platelet inhibition raises bleeding risk.
- Pregnancy considerations: if used, restrict to the first trimester under strict medical supervision; avoid in 3rd trimester.
- Drug interaction caution: ketoprofen can potentiate the effects of nephrotoxic antibiotics (e.g., aminoglycosides) and antihypertensives (ACEI, ARBs, diuretics).
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• *This drug card consolidates high‑yield information to support clinical decision‑making, with emphasis on safety and individualized patient care.*