Indications
Rheumatic diseases: for anti-inflammatory and analgesic use in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis.
Periarticular and musculoskeletal indications: for analgesia in bursitis, tendinitis, synovitis, tenosynovitis, lumbago.
Migraine headache: Prophylaxis and treatment of migraine headache.
Surgical and traumatic uses: for analgesic action after sports injuries, orthopaedic manipulations, dental extraction, surgery.
Infectious diseases: for analgesic, anti-inflammatory and antipyretic purposes.
Gynaecological uses: in dysmenorrhoea, following IUCD insertion and for uterine relaxation and analgesia in the post-partum, non-nursing mother.
Therapeutic Class
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Pharmacology
Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic actions. In addition to the inhibition of prostaglandin synthesis, it stabilizes lysosomal membranes in vitro and in vivo, inhibits leukotriene synthesis in vitro at high concentrations, and also exhibits antibradykinin activity in vivo. Ketoprofen produces analgesia by inhibiting the synthesis of prostaglandins peripherally and centrally. It has also been suggested that Ketoprofen causes the suppression of prostaglandin synthesis in the CNS (probably in the hypothalamus) leading to its antipyretic effect.
Ketoprofen is rapidly and almost completely absorbed from the GI tract. It is approximately 99% bound to plasma protein, mainly albumin. Following single or multiple oral doses in healthy adults, the elimination half-life of the drug has averaged 1.1-4 hours. It is rapidly and extensively metabolized in the liver, principally via conjugation with glucoronic acid. Following a single oral dose of Ketoprofen in healthy adults, about 50-90% of the drug is excreted in urine and about 1-8% in faeces within 1-5 days ; most urinary excretion occurs within 12-24 hours and most faecal excretion occurs within 24-48 hours. In case of IM injection, peak concentration of approximately 10 mg/L is reached at about 0.5-0.75 hour after a 100 mg dose. The elimination half-life is approximately 1.88 hour.
Dosage & Administration
Intramuscular-
Pain and inflammation associated with musculoskeletal and joint disorders, Pain following orthopaedic surgery:
Adult: 50-100 mg by deep inj into the gluteal muscle every 4 hr. Max: 200 mg in 24 hr for up to 3 days.
Oral-
Pain and inflammation:
Adult: 25-50 mg every 6-8 hr. Max: 300 mg/day in divided doses.
Elderly: >75 yr Reduce initial dose.
Oral-
Rheumatic disorders:
Adult: 100-200 mg/day in 2-4 divided doses. Max: 300 mg/day in divided doses. As modified-release formulation: Administer dose once daily.
Elderly: >75 yr Reduce initial dose.
Rectal-
Rheumatic disorders:
Adult: 100 mg at night or bid. Recommended total dose (combined oral and rectal): Not to exceed 200 mg/day.
Topical/Cutaneous-
Local pain relief:
Adult: As 2.5% gel: Apply onto affected areas 2-4 times daily for up to 10 days. As 30 mg plaster: Apply 1 plaster bid.
Interaction
Increases plasma concentrations of lithium and methotrexate. Reduces effects of antihypertensives (e.g. ACE inhibitors, angiotensin II receptor antagonists). Increased risk of GI bleeding with warfarin. Decreased protein binding of ketoprofen and increased risk for serious GI events with aspirin and other NSAIDs. Increased risk of developing renal failure with diuretics. Increased risk of GI bleeding and ulceration with corticosteroids. Increased plasma levels with probenecid. Salicylate reduces conjugation and renal elimination of ketoprofen.
Contraindications
Hypersensitivity to Ketoprofen
Patients with rhinitis, nasal polyps and asthma associated with Aspirin may show cross sensitivity with other NSAIDs including Ketoprofen
Patients with active ulceration or chronic dyspepsia
Severe renal insufficiency
Side Effects
Adverse reactions to Ketoprofen are usually mild and mainly involve the GI tract, particularly upper GI tract. Most Ketoprofen-induced adverse effects occur during the first month of treatment, and the frequency of adverse effects generally decreases with continued therapy. Adverse reactions involving digestive system are dyspepsia, nausea, abdominal pain, diarrhoea, constipation, flatulence, anorexia, vomiting, stomatitis and that involving nervous system are headache, dizziness, malaise, depression, nervousness, dreams, etc. Other reactions are tinnitus, visual disturbance, rash, impairment of renal function, signs or symptoms of urinary-tract irritation.
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