Ketoprofen
Overview
Ketoprofen is NSAID (non-steroidal anti-inflammatory drug). Ketoprofen a propionic acid derivative and widely used in the treatment of pateints with rheumatic diseases. It reduces fever, inflammation or swelling and relieves pain. used to treat pain, swelling and stiffness associated with arthritis. also used to treat headaches, muscle aches and dental pain. available for oral, rectal, parentral and topical administration. Chemically Ketoprofen is (R, S)-2-(3-benzoylpheny) propionicacid. It inhibits cyclooxygenase actvity with reduction in the tissue production of prostaglandins such as PGE-2 and PGF-2a.
Primary Characteristics
It is of Synthetic origin and belongs to Propionic Acid. It belongs to Cyclo-oxygenase inhibitor pharmacological group on the basis of mechanism of action and also classified in Analgesics and Anti-inflammatory Agents pharmacological group. The Molecular Weight of Ketoprofn is 254.30.
Its pKa is 4.55.
Indications
Primarily indicated in conditions like Ankylosing spondylitis, Bursitis, Gastro-oesophageal reflux disease, Gout, Lumbago, Management of cushing`s syndrome, Musculoskeletal disorders, Osteoarthritis, Pain, Rheumatic diseases, Rheumatoid and arthritis, Synovitis, Tendinitis, Tenosynovitis, and can also be given in adjunctive therapy as an alternative drug of choice in Dental pain, Dysmenorrhoea, Fever, fever, Infections, Migraine, Orthopedic manipulations.
Pharmacokinetics
Oral absorption of Ketoprofen found to be 94% ±4. Volume of distribution found to be 0.11 l/kg and plasma protien binding is 95%. Presystemic metabolism noted to be 45.5% ±4.5 and metabolism reported extensively by liver. Renal Excretion accounts for 1% (unchanged) and plasma half life is 1.5-4 hr.
Pharmacodynamics
Ketoprofen a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties. Pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. Ketoprofen used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and alleviate moderate pain.
Mechanism of action
The anti-inflammatory effects of ketoprofen believed to be due to inhibition cylooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. Ketoprofen a non-specific cyclooxygenase inhibitor and inhibition of COX-1 thought to confer some of its side effects, such as GI upset and ulceration. Ketoprofen is thought to have anti-bradykinin activity, as well as lysosomal membrane-stabilizing action. Antipyretic effects may due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Contraindications
Ketoprofen contraindicated in conditions like Peptic ulcer, Bronchospasm and Rhinitis, Renal insufficiency.
Side Effects
The severe or irreversible adverse effects of Ketoprofen, which give rise to further complications include Reduced GFR (glomerular filtration rate), Acute interstitial nephritis and Platelet dysfunction.
Produces potentially life-threatening effects which include Gastrointestinal hemorrhage. which responsible for the discontinuation of Ketoprofen therapy.
The signs and symptoms that produced after the acute overdosage of Ketoprofen include Hypotension, Vomiting, Bronchospasm, Drowsiness, Drowsiness, Abdominal pain and GI hemorrhage.
The symptomatic adverse reactions produced by Ketoprofen more or less tolerable and if they become severe, they can treated symptomatically, these include Vertigo, Nausea, Vomiting, Diarrhea, Constipation, Photosensitivity, Skin rash, Dyspepsia, GI upset, Bullous rash, dyspepsia and Gastric pain.
Warning / Precautions
Ketoprofen used with caution in patients with intrinsic coagulation defects and those on anticoagulant therapy. It should used with caution in patients with compromised cardiac function, hypertension other condition predisposing to fluid retention. It should be used with extra care in the presence of existing controlled infection. Perform periodic auditory (hearing) function and test during chronic therapy. Discontinue drug if skin reaction occurs. Ketoprofen not recommended in the patient who have experienced a severe Aspirin hypersensitivity reactions. IM injection administered cautiouly to patient receiving .