Ketoprofen

BRANDS OF KETOPROFEN IN KENYA

Ketesse®, Menarini


Ketoprofen in Kenya: Chemical Structure
Ketoprofen Chemical Structure

KETOPROFEN MODE OF ACTION
Ketoprofen is used for its antipyretic, analgesic, and anti-inflammatory properties by inhibiting cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes reversibly, which decreases the production of proinflammatory prostaglandin precursors.

INDICATIONS

Ketoprofen is recommended in the management of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute articular and peri-articular disorders, (bursitis, capsulitis, synovitis, tendinitis), cervical spondylitis, low back pain (strain, lumbago, sciatica, fibrositis), painful musculoskeletal conditions, acute gout, dysmenorrhoea and control of pain and inflammation following orthopedic surgery

DOSAGE AND ADMINISTRATION

Adults: 100 – 200 mg once daily, depending on patient weight and on the severity of symptoms.

The maximum daily dose is 200 mg. The balance of risks and benefits should be carefully considered before commencing treatment with 200 mg daily, and higher doses are not recommended

Elderly: The elderly are at increased risk of the serious consequences of adverse reactions. If an NSAID is considered necessary, the lowest effective dose should be used and for the shortest possible duration. The patient should be monitored regularly for GI bleeding during NSAID therapy.

Pediatric dosage not established.

Undesirable effects may be minimized by using the lowest effective dose for the shortest duration necessary to control symptoms

CONTRAINDICATIONS

Ketoprofen is contraindicated in patients who have a history of hypersensitivity reactions such as bronchospasm, asthmatic attacks, rhinitis, angioedema, urticaria, or other allergic-type reactions to ketoprofen, any other ingredients in this medicine, ASA or other NSAIDs. Severe, rarely fatal, anaphylactic reactions have been reported in such patients.

Ketoprofen is contraindicated in patients with hypersensitivity to any of the excipients of the drug.

Ketoprofen is also contraindicated in the third trimester of pregnancy.

Ketoprofen is contraindicated in the following cases:

– Severe heart failure

– active peptic ulcer, or any history of gastrointestinal bleeding, ulceration or perforation

– hemorrhagic diathesis

– severe hepatic insufficiency

– severe renal insufficiency

DRUG INTERACTIONS

Anticoagulants:

Increased risk of bleeding

– Heparin

– Vitamin K antagonists (such as warfarin)

– Platelet aggregation inhibitors (such as ticlopidine, clopidogrel)

– Thrombin inhibitors (such as dabigatran)

– Direct factor Xa inhibitors (such as apixaban, rivaroxaban, edoxaban)

If coadministration is unavoidable, the patient should be closely monitored.

Lithium:

Risk of elevation of lithium plasma levels, sometimes reaching toxic levels due to decreased lithium renal excretion. Where necessary, plasma lithium levels should be closely monitored and the lithium dosage levels adjusted during and after NSAIDs therapy.

Other analgesics/NSAIDs (including cyclooxygenase-2 selective inhibitors) and high dose salicylates:

Avoid concomitant use of two or more NSAIDs (including aspirin) as this may increase the risk of adverse effects, particularly gastrointestinal ulceration, and bleeding.

Methotrexate:

Serious interactions have been recorded after the use of high dose methotrexate with NSAIDs, including ketoprofen, due to decreased elimination of methotrexate. At doses greater than 15 mg/week:

Increased risk of hematologic toxicity of methotrexate, particularly if administered at high doses (> 15 mg/week), possibly related to the displacement of protein-bound methotrexate and to its decreased renal clearance. At doses lower than 15mg/week: During the first weeks of combination treatment, full blood count should be monitored weekly. If there is any alteration of the renal function or if the patient is elderly, monitoring should be done more frequently.

Mifepristone:

NSAIDs should not be used for 8 – 12 days after mifepristone administration as NSAIDs can reduce the effect of mifepristone.

Pentoxifylline:

There is an increased risk of bleeding. More frequent clinical monitoring and monitoring of bleeding time is required.

Antihypertensive agents (beta-blockers, angiotensin-converting enzyme inhibitors, diuretics):

Risk of decreased antihypertensive potency (inhibition of vasodilator prostaglandins by NSAIDs.

Diuretics:

Risk of reduced diuretic effect. Patients and particularly dehydrated patients taking diuretics are at a greater risk of developing renal failure secondary to a decrease in renal blood flow caused by prostaglandin inhibition. Such patients should be rehydrated before initiating coadministration therapy and renal function monitored when the treatment is started.

Cardiac glycosides:

NSAIDs may exacerbate cardiac failure, reduce GFR, and increase plasma glycoside levels.

Ciclosporin:

Increased risk of nephrotoxicity, particularly in elderly subjects.

Corticosteroids:

Increased risk of gastrointestinal ulceration or bleeding.

Quinolone antibiotics:

Animal data indicate that NSAIDs can increase the risk of convulsions associated with quinolone antibiotics. Patients taking NSAIDs and quinolones may have an increased risk of developing convulsions.

Tacrolimus:

Possible increased risk of nephrotoxicity when NSAIDs are given with tacrolimus, particularly in elderly subjects.

Thrombolytics:

Increased risk of bleeding.

Probenecid:

Concomitant administration of probenecid may markedly reduce the plasma clearance of ketoprofen.

Anti-platelet agents and Selective serotonin reuptake inhibitors (SSRIs):

Increased risk of gastrointestinal bleeding.

ACE inhibitors and Angiotensin II Antagonists:

In patients with compromised renal function (e.g. dehydrated patients or elderly patients the co-administration of an ACE inhibitor or Angiotensin II antagonist and agents that inhibit cyclooxygenase may result in further deterioration of renal function, including possible acute renal failure.

Zidovudine:

Increased risk of hematological toxicity when NSAIDs are given

ADVERSE EFFECTS

Ketoprofen in adults:

Blood and lymphatic system disorders

– rare: hemorrhagic anemia, anemia due to bleeding

– not known: agranulocytosis, thrombocytopenia, bone marrow failure, neutropenia

Immune system disorders

– rare: anaphylactic reactions (including shock)

Psychiatric disorders

– not known: mood altered

Nervous system disorders

– uncommon: headache, dizziness, somnolence

– rare: paraesthesia

– not known: convulsions, dysgeusia, depression, confusion, hallucinations, vertigo, malaise, drowsiness, reports of aseptic meningitis (especially in patients with existing auto-immune disorders such as systemic lupus erythematosus, mixed connective tissue disease) with symptoms such as the stiff neck, headache, nausea, vomiting, fever or disorientation.

Eye disorders

– rare: visual disturbances such as blurred vision.

– not known: optic neuritis

Ear and labyrinth disorders

– rare: tinnitus

Cardiac disorders

– not known: heart failure, edema

Vascular disorders

– not known: hypertension, vasodilatation

Respiratory, thoracic and mediastinal disorders

– rare: asthma, asthmatic attack

– not known: bronchospasm (particularly in patients with known hypersensitivity to ASA and other NSAIDs), rhinitis, non-specific allergic reactions, dyspnoea

Gastrointestinal disorders

– common: dyspepsia, nausea, abdominal pain, vomiting

– uncommon: constipation, diarrhea, flatulence, gastritis

– rare: stomatitis, peptic ulcer

– very rare: pancreatitis (very rare reports of pancreatitis have been noted with NSAIDs)

– not known: exacerbation of colitis and Crohn’s disease, gastrointestinal hemorrhage and perforation, gastralgia, melaena, haematemesis

Gastrointestinal bleeding may sometimes be fatal, particularly in the elderly.

Hepatobiliary disorders

– rare: hepatitis, transaminases increased, elevated serum bilirubin due to hepatitis disorders

– not known: abnormal liver function, jaundice

Skin and subcutaneous disorders

– uncommon: rash, pruritis

– not known: photosensitivity reactions, alopecia, urticaria, angioedema, bullous eruption including Stevens-Johnson syndrome and toxic epidermal necrolysis, exfoliative and bullous dermatoses (including epidermal necrolysis, erythema multiforme), purpura

Renal and urinary disorders

– not known: renal failure acute, tubulointerstitial nephritis, nephritic syndrome, renal function tests abnormal

General disorders and administration site conditions

– uncommon: edema, fatigue

– not known: headache, taste perversion

Investigations

– rare: weight increased

Clinical trial and epidemiological data suggest that use of some NSAIDs (particularly at high doses and in long term treatment) may be associated with an increased risk of arterial thrombotic events (for example myocardial infarction or stroke).

In all cases of major adverse effects, Ketoprofen should be withdrawn at once.


Ketoprofen in Kenya
Cost of Ketoprofen in Kenya
Drugs alternatives to Ketoprofen in Kenya
Trade names of Ketoprofen in Kenya

Clinical | Pharmacokinetic data


Pregnancy Category: C (D in 3rd trimester)
Routes of Administration: Oral, topical
Bioavailability:
Protein Binding: 99%
Metabolosim:
Onset of Action:
Elimination Half life: 2–2.5 hours
Excretion:

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
Tablets , Gel

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