Ketoprofen


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Pain and inflammation associated with musculoskeletal and joint disorders; Rheumatoid arthritis; Osteoarthritis; Ankylosing spondylitis; Bursitis; Tendinitis; Postoperative pain As conventional cap: 50 mg 4 times daily or 75 mg tid. Max: 300 mg/day. As extended – release cap: 100-200 mg once daily, depending on patient weight and severity of symptoms. Max: 200 mg/day. Mild to moderate pain; Dysmenorrhoea As conventional cap: 25-50 mg 6-8 hourly as necessary. As extended-release cap: 100-200 mg once daily, depending on patient weight and on severity of symptoms. Rectal Rheumatoid arthritis; Osteoarthritis 100 once daily (at night time) or bid. Max: 200 mg/day. Topical/Cutaneous Local pain relief As 2.5% gel: Approx 2-4 g 2-4 times daily up to 7 days. Max: 15 g/day. As 30 mg medicinal plaster: Apply 1 plaster to the affected area bid.
Dosage Details
Oral
Ankylosing spondylitis, Arthritis, rheumatoid, Bursitis, OA (osteoarthritis), Pain and inflammation associated with musculoskeletal and joint disorders, Postoperative pain, Rheumatoid arthritis, Tendinitis
Adult: As conventional cap: 50 mg 4 times daily or 75 mg tid. Max: 300 mg daily. As extended-release cap: 100-200 mg once daily, depending on patient weight and severity of symptoms. Max: 200 mg daily.
Elderly: Lowest initial and maintenance dose with shortest possible duration.

Oral
Dysmenorrhoea, Mild to moderate pain
Adult: As conventional cap: 25-50 mg 6-8 hourly as necessary. As extended-release cap: 100-200 mg once daily, depending on patient weight and on severity of symptoms.
Elderly: Lowest initial and maintenance dose with shortest possible duration.

Rectal
Osteoarthritis, Rheumatoid arthritis
Adult: 100 mg once daily (at night time) or bid. Max: 200 mg daily.

Topical/Cutaneous
Local pain relief
Adult: As 2.5% gel: Approx 2-4 g 2-4 times daily. Massage gently on the painful or inflamed area up to 7 days. Max: 15 g/day. As 30 mg medicinal plaster: Apply 1 plaster to the affected area bid.
Child: ≥15 years As 2.5% gel: Same as adult dose.
Renal Impairment
Oral/Rectal:
Severe: Contraindicated.
Hepatic Impairment
Oral/Rectal:
Severe: Contraindicated.
Administration
Should be taken with food. Preferably taken w/ or after meals.
Contraindications
Hypersensitivity to ketoprofen, aspirin or other NSAIDs. History of gastrointestinal bleeding, perforation, or ulceration related to NSAID therapy. Aspirin-sensitive asthma, gastrointestinal ulceration, haemorrhage, chronic dyspepsia, severe heart failure, treatment of perioperative pain in the setting of CABG, haemorrhagic diathesis. History of proctitis or haemorrhoids (rectal); pathological skin changes (e.g. dermatosis, eczema, infected skin lesion or open wounds), history of photosensitivity reactions (topical). Severe renal and hepatic impairment (oral/rectal). Pregnancy (3rd trimester).
Special Precautions
Patients with history of aseptic meningitis, SLE, heart failure or fluid retention, hypertension, gastrointestinal disease (e.g. ulcerative colitis, Crohn’s disease), oedema, cirrhosis, nephrosis. Renal and hepatic impairment. Children and elderly. Pregnancy (1st-2nd trimester) and lactation. Concomitant use of other NSAIDs, corticosteroids, antiplatelets, anticoagulants. Not for prolonged use.
Adverse Reactions
Significant: Na and fluid retention, CNS effects (e.g. drowsiness, dizziness), risk of hyperkalaemia, blurred vision, anaemia, rare severe blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anemia), liver function abnormalities (e.g. increased transaminase enzyme levels), renal impairment (increased BUN, oedema), photosensitivity.
Cardiac disorders: Heart failure.
Ear and labyrinth disorders: Tinnitus.
Gastrointestinal disorders: Gastralgia, stomatitis, vomiting, nausea, abdominal pain, dyspepsia, flatulence, constipation, gastritis, dry mouth, diarrhoea, peptic ulcer.
Immune system disorders: Urticaria.
Metabolism and nutrition disorders: Anorexia.
Renal and urinary disorders: UTI.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Peripheral oedema, hypertension, vasodilation.
Potentially Fatal: Anaphylaxis reaction, myocardial infarction, stroke, gastrointestinal bleeding, ulceration and perforation, bronchospams; Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN), exfoliative dermatitis. Rarely, hepatotoxicity (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure).
PO: C (Avoid during 3rd trimester or near delivery.)
Patient Counseling Information
This drug may cause somnolence, dizziness and visual disturbances, if affected, do not drive or operate machinery. Topical: Avoid use of occlusive dressing. Avoid exposure of affected area to direct sunlight or solarium UV light.
MonitoringParameters
Monitor blood pressure, CBC, chemistry profile, wt gain, oedema, occult blood loss, and periodic LFT; renal function (e.g. urine output, serum BUN, creatinine); ophthalmic exam (prolonged use). Evaluate cardiac risk and potential for gastrointestinal bleeding.
Overdosage
Symptoms: Drowsiness, epigastric pain, lethargy, nausea, and vomiting, coma, disorientation, dizziness, excitation, fainting, headache, tinnitus, rarely diarrhoea and occasionally convulsions. Management: Symptomatic and supportive treatment. Administration of activated charcoal within 1 hour of ingestion to reduce absorption or perform gastric lavage.
Drug Interactions
Increased levels and risk of toxicity with lithium, digoxin, methotrexate. Increased risk of gastrointestinal ulceration, perforation and bleeding with other NSAIDs, aspirin, corticosteroids, SSRI and anticoagulants (e.g. warfarin, heparin). Exacerbate cardiac failure with cardiac glycoside. Increased risk of hyperkalaemia and renal toxicity with ACE inhibitors, diuretics, angiotensin receptor antagonists, heparin, ciclosporin, tacrolimus, trimethoprim. Reduces effects of diuretics and ACE inhibitors or other antihypertensive agents. Increased serum concentration with probenecid. Increased risk of nephrotoxicity with ciclosporin and tacrolimus.
Food Interaction
Decreased absorption with food and milk. Increased risk of gastrointestinal bleeding with alcohol.
Lab Interference
May cause false-positive aldosterone/renin ratio. May interfere with the detection of albumin, bile salts, 17-ketosteroids or 17-hydroxycorticosteroid in urine.
Action
Description: Ketoprofen, a propionic acid derivative, is an NSAID that has antipyretic, anti-inflammatory and analgesic properties. It reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, resulting to decreased formation of prostaglandin precursors.
Onset: Conventional cap: <30 minutes.
Duration: Conventional cap: Up to 6 hours.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Decreased absorption rate with food. Bioavailability: Approx 90%. Time to peak plasma concentration: 0.5-2 hours (conventional cap); 6-7 hours (extended release cap).
Distribution: Readily distributed into the CNS and synovial fluid. Crosses placenta and enters breast milk. Volume of distribution: 0.1 L/kg. Plasma protein binding: >99% mainly to albumin.
Metabolism: Metabolised in the liver via glucuronide conjugation to form an unstable acyl-glucuronide.
Excretion: Mainly via urine as glucuronide metabolite (approx 80%). Elimination half-life: 2-4 hours (conventional cap); approx. 3-7.5 hours (extended-release cap).
Chemical Structure

Chemical Structure Image
Ketoprofen

Source: National Center for Biotechnology Information. PubChem Database. Ketoprofen, CID=3825, https://pubchem.ncbi.nlm.nih.gov/compound/Ketoprofen (accessed on Jan. 21, 2020)

Storage
Store below 25°C; Plaster: Store below 30°C. Protect from light.
ATC Classification
M01AE03 - ketoprofen ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.
M02AA10 - ketoprofen ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.
References
Anon. Ketoprofen. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 12/02/2019.

Anon. Ketoprofen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/02/2019.

Buckingham R (ed). Ketoprofen. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/02/2019.

KefenTech Air (Jeil Health Science Inc). MIMS Singapore. http://www.mims.com/singapore. Accessed 11/02/2019.

Ketoprofen Capsule (Heritage Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 18/02/2019.

Ketoprofen Capsule (Mylan Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/02/2019.

Disclaimer: This information is independently developed by MIMS based on Ketoprofen from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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