Ketoprofen

Indications

Ketoprofen is used for: Rheumatic disorders, Pain and inflammation, Musculoskeletal and joint disorders,

Adult 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. Pain and inflammation Adult: 25-50 mg every 6-8 hr. Max: 300 mg/day in divided doses. Elderly: >75 yr Reduce initial dose. Hepatic impairment: W/ serum albumin <3.5 g/dL: Max: 100 mg/day. 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. Rectal as suppository Rheumatic disorders Adult: 100 mg at night or bid. Recommended total dose (combined oral and rectal): Not to exceed 200 mg/day.

Child Dose

Safety and efficacy not established

Renal Dose

Renal impairment: Mild: Max: 150 mg/day. Severe: Max: 100 mg/day.

Administration

Should be taken with food. Preferably taken w/ or after meals.

Contra Indications

For all routes: Hypersensitivity to aspirin or other NSAIDs or those suffering from asthma, angioedema, urticaria or rhinitis. Active GI disease (e.g. bleeding or ulcer). Severe heart failure, and renal insufficiency. Treatment of perioperative pain in the setting CABG surgery. Rectal: Patients w/ history of proctitis or haemorrhoids.

Precautions

History of GI disease (e.g. bleeding or ulcer). Hypertensive patients; renal or hepatic impairment. Pregnancy, lactation, elderly. Monitoring Parameters Close monitoring of BP during initiation and throughout the therapy. Complete blood cell count, chemistry profile, liver and renal function test performed periodically for patients receiving long-term ketoprofen therapy.

Pregnancy-Lactation

Pregnancy Category: B; D in late pregnancy because of inhibition of ductus arteriosus closure Lactation: unknown whether excreted in breast milk, not recommended

Interactions

Increases plasma concentrations of lithium and methotrexate. Reduces effects of antihypertensives (e.g. ACE inhibitors, angiotensin II receptor antagonists). Increased risk of GI bleeding w/ warfarin. Decreased protein binding of ketoprofen and increased risk for serious GI events w/ aspirin and other NSAIDs. Increased risk of developing renal failure w/ diuretics. Increased risk of GI bleeding and ulceration w/ corticosteroids. Increased plasma levels w/ probenecid. Salicylate reduces conjugation and renal elimination of ketoprofen.

Adverse Effects

Side effects of Ketoprofen : >10% Increased liver function test (up to 15%), Dyspepsia (12%) 1-10% Dizziness (3-9%), Headache (3-9%), Impaired renal function disorder (3-9%), Upper GI ulcers, 3-6 mth treatment; 2-4%, 1 yo treatment), Nausea (>3%), Diarrhea (>3%), Abdominal pain (>3%), Constipation (>3%), Flatulence (>3%), Rash (1-3%), Stomatitis (1-3%), Insomnia (1-3%), Malaise (1-3%), Depression (1-3%), Ketoprofen-induced peptic ulcer, GI bleeding (>2% in long-term studies);, Peripheral edema (2%), Bronchospasm (<2%), Myocardial infarction (<2%) <1% Congestive heart failure (<1%), Hypertension (<1%), Scaling eczema, Stevens-Johnson syndrome (<0.1%), Gastrointestinal hemorrhage (<1%), Gastrointestinal perforation (<1%), Melena (<1%), Agranulocytosis (<1%), Anemia (<1%), Thrombocytopenia (<1%), Hepatitis (<1%), Anaphylactoid reaction (<1%), Immune hypersensitivity reaction, Cerebrovascular accident, Interstitial nephritis (<1%), Renal failure (<1%) Potentially Fatal: Anaphylaxis, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Mechanism of Action

Ketoprofen exhibits anti-inflammatory, analgesic and antipyretic properties. It potently inhibits the enzyme cyclooxygenase resulting in prostaglandin synthesis inhibition.