Ketoprofen


Generic Medicine Info
Indications and Dosage
Oral
Ankylosing spondylitis, Bursitis, Osteoarthritis, Pain and inflammation associated with musculoskeletal and joint disorders, Rheumatoid arthritis, Tendinitis
Adult: As conventional cap: 50 mg 4 times daily, or 75 mg tid. Max: 300 mg daily. As modified-release cap: 100-200 mg once daily, depending on patient weight and severity of symptoms. Max: 200 mg daily. Use the lowest effective dose for the shortest possible duration.
Elderly: Use the lowest effective dose for the shortest possible duration.

Oral
Dysmenorrhoea
Adult: As conventional cap: 25-50 mg 6-8 hourly as necessary. As modified-release cap: 100-200 mg once daily, depending on patient weight and severity of symptoms. Max: 200 mg daily. Use the lowest effective dose for the shortest possible duration.
Elderly: Use the lowest effective dose for the shortest possible duration.

Oral
Mild to moderate pain
Adult: As conventional cap: 25-50 mg 6-8 hourly as necessary. Use the lowest effective dose for the shortest possible duration.
Elderly: Use the lowest effective dose for the shortest possible duration.

Rectal
Osteoarthritis, Rheumatoid arthritis
Adult: As supp: 100 mg once daily at night, or 100 mg bid. May be supplemented with oral doses as needed. Max: 200 mg daily (combined rectal and oral dose). Use the lowest effective dose for the shortest possible duration.

Topical/Cutaneous
Pain and inflammation associated with musculoskeletal and joint disorders
Adult: As 2.5% gel: Apply approx 2-4 g (approx 5-10 cm) 2-4 times daily on the affected area(s) for up to 7 days. Max: 15 g daily. Alternatively, apply a thin layer 1-3 times daily. Massage treated area(s) gently to enhance absorption. As 30 mg plaster: Apply 1 plaster onto affected area bid. Use the lowest effective dose for the shortest possible duration. Dosage recommendations may vary among individual products or between countries (refer to detailed product guideline).
Special Patient Group
Oral:
Debilitated patients: Lower initial doses may be considered.
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 asthma, bronchospasm, rhinitis, urticaria or other allergic-type reactions after taking aspirin or other NSAIDs. Oral, rectal: History of gastrointestinal bleeding, perforation, or ulceration related to previous NSAID therapy; active peptic ulcer, history of gastrointestinal ulceration or haemorrhage, chronic dyspepsia; severe heart failure, treatment of perioperative pain in the setting of CABG surgery, haemorrhagic diathesis. History of proctitis or haemorrhoids (rectal); pathological skin changes (e.g. dermatosis, eczema, infected skin lesions, acne, open wounds), history of photosensitivity reactions (topical). Severe renal and hepatic impairment (oral, rectal). Pregnancy (3rd trimester).
Special Precautions
Patient with history of gastrointestinal disease (e.g. ulcerative colitis, Crohn’s disease); SLE, mixed connective tissue disease, uncontrolled hypertension, established ischaemic heart disease, recent MI, mild to moderate heart failure, peripheral arterial disease, cerebrovascular disease, risk factors for CV disease (e.g. hyperlipidaemia, diabetes mellitus, smoking), coagulation disorders, other forms of asthma, oedema, cirrhosis, nephrosis. Not indicated for prolonged use. Renal and hepatic impairment. Elderly and debilitated patients. Pregnancy (1st-2nd trimester) and lactation. Concomitant use of other NSAIDs, corticosteroids, antiplatelets, and anticoagulants.
Adverse Reactions
Significant: CNS effects (e.g. drowsiness, dizziness), blurred vision, Na and fluid retention, new-onset or exacerbated hypertension, hyperkalaemia, liver function abnormalities (e.g. increased transaminase levels), renal impairment (e.g. increased BUN, oedema), decreased platelet aggregation, prolonged bleeding time, anaemia; may mask signs of infection; photosensitivity (topical).
Blood and lymphatic system disorders: Rarely, severe blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia).
Cardiac disorders: Exacerbation of heart failure.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbances.
General disorders and administration site conditions: Application site erythema, burning sensation, dryness, or irritation (topical); local pain, burning sensation, or pruritus (rectal).
Gastrointestinal disorders: Dyspepsia, nausea, abdominal pain, vomiting, constipation, diarrhoea, flatulence.
Metabolism and nutrition disorders: Anorexia.
Nervous system disorders: Headache, aseptic meningitis.
Renal and urinary disorders: Urinary tract irritation.
Skin and subcutaneous tissue disorders: Rash, pruritus, eczema (topical).
Vascular disorders: Vasodilation.
Potentially Fatal: Serious CV thrombotic events, including MI and stroke; serious gastrointestinal bleeding, ulceration and perforation; severe bronchospasm, drug reaction with eosinophilia and systemic symptoms. Rarely, severe anaphylactic reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis, hepatotoxicity (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure).
Parenteral/PO/Rectal: Z (NSAIDs caused foetal ductus arteriosus premature closure, foetal renal impairment and persistent pulmonary hypertension. Avoid near term, else use lowest dose for shortest time.)
Patient Counseling Information
Oral, rectal: This drug may cause drowsiness, dizziness and visual disturbances, if affected, do not drive or operate machinery. Topical: Avoid exposure of treated area(s) to direct sunlight or UV light during and for 2 weeks after treatment discontinuation. Do not use with occlusive dressing.
Monitoring Parameters
Monitor blood pressure at the start of therapy and periodically during use; CBC, chemistry profile, LFTs, renal function (e.g. creatinine, urine output, serum BUN), and ophthalmic exam periodically during prolonged use. Asses for weight gain, oedema, and signs of gastrointestinal bleeding. Evaluate cardiac risk and potential for gastrointestinal bleeding.
Overdosage
Symptoms: Lethargy, drowsiness, headache, epigastric pain, nausea, vomiting, respiratory depression, convulsion, and coma. Rarely, gastrointestinal bleeding, hypotension, hypertension, and acute renal failure. Management: Symptomatic and supportive treatment. Administer activated charcoal within 1 hour of ingestion to reduce absorption or perform gastric lavage. May give IV diazepam for frequent or prlonged convulsions.
Drug Interactions
May increase the risk of toxicity of lithium and methotrexate. Increased risk of renal toxicity with ACE inhibitors, diuretics, angiotensin II receptor antagonists, ciclosporin, and tacrolimus. May reduce the therapeutic effects of diuretics and antihypertensive agents. Increased serum concentration with probenecid. Increased risk of renal failure when given with tenofovir disoproxil fumarate. May elevate the plasma levels of digoxin.
Potentially Fatal: Increased risk of gastrointestinal ulceration and bleeding with other NSAIDs, aspirin, corticosteroids, SSRIs and anticoagulants (e.g. warfarin, heparin).
Food Interaction
Decreased rate of absorption with food; however, bioavailability is not altered. 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, leading to decreased formation of prostaglandin precursors.
Onset: Conventional cap: <30 minutes.
Duration: Conventional cap: Up to 6 hours.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract (conventional cap). Decreased rate of absorption with food (bioavailability is not affected). Bioavailability: Approx 90%. Time to peak plasma concentration: 0.5-2 hours (conventional cap); 6-7 hours (modified-release cap); approx 1 hour (rectal supp).
Distribution: Distributed into the synovial fluid and CNS. Crosses the 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 into an unstable acyl-glucuronide.
Excretion: Mainly via urine (approx 80%, primarily as glucuronide metabolite). Elimination half-life: 2-4 hours (conventional cap); approx 3-7.5 hours (modified-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
Conventional/modified-release cap: Store between 20-25°C. Protect from light and excessive heat and humidity. Rectal supp/topical gel: Store below 25°C. Topical plaster: Store below 30°C. Protect from direct sunlight.
MIMS Class
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
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 25/01/2022.

Anon. Ketoprofen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 25/01/2022.

Buckingham R (ed). Ketoprofen. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/01/2022.

Fastum Gel (A. Menarini Singapore Pte. Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 25/01/2022.

Joint Formulary Committee. Ketoprofen. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/01/2022.

KefenTech Air (Pharmaforte Singapore Pte. Ltd.). MIMS Singapore. http://www.mims.com/singapore. Accessed 25/01/2022.

Ketoprofen 2.5% w/w Gel (Pinewood Laboratories Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/11/2021.

Ketoprofen Capsule (Misemer Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 25/01/2022.

Ketoprofen Capsule Extended-Release (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 25/01/2022.

Ketoprofen Capsules BP 50 mg (Ennogen Pharma Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/11/2021.

Ketotop Plaster (Zuellig Pharma Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 25/01/2022.

Oruvail 200 mg Prolonged-Release Hard Capsules (Aventis Pharma Limited, Trading as: Sanofi). MHRA. https://products.mhra.gov.uk. Accessed 25/01/2022.

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 © 2022 MIMS. All rights reserved. Powered by MIMS.com
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