Ankylosing Spondylitis, Osteoarthritis, & Rheumatoid Arthritis, Bursitis & Tendinitis, Dysmenorrhoea or postoperative pain & acute gout or soft-tissue disorders.
Propionic Acid Derivatives; NSAID
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.
Tablet: 50-100 mg daily, taken with food to minimize gastrointestinal disturbance. For rheumatic disease, 100-200 mg daily in 2-4 divided doses with food. For pain & dysmenorrhoea, 50 mg up to 3 times daily. SR Capsule: 100-200 mg once daily.Elderly: As with other medications it is generally advisable in the elderly to begin ketoprofen therapy at the lower end of the dose range. Paediatric dosage: Not established for intramuscular use.
Not recommended drug associations Other NSAIDs (including cyclooxygenase-2 selective inhibitors) and high dose salicylates: Increased risk of gastrointestinal ulceration and bleeding. 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, 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 NSAID therapy.
Methotrexate at doses greater than 15mg/week: Increased risk of haematologic toxicity of methotrexate, particularly if administered at high doses (>15 mg/week), possibly related to displacement of protein-bound methotrexate and to its decreased renal clearance.
Drug associations requiring precautions for use Medicinal products and therapeutic categories that can promote hyperkalemia (i.e. potassium salts, potassium-sparing diuretics, ACE inhibitors and angiotensin II antagonists, NSAIDs, heparins (low molecular-weight or unfractioned), cyclosporin, tacrolimus and trimethoprim): The risk of hyperkalemia can be enhanced when the drugs mentioned above are administered concomitantly.
Corticosteroids: increased risk of gastrointestinal ulceration or bleeding.
Diuretics: 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 co-administration therapy and renal function monitored when the treatment is started.
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.
Nicorandil: In patients concomitantly receiving nicorandil and NSAIDs, there is an increased risk for severe complications such as gastrointestinal ulceration, perforation and hemorrhage.
Cardiac glycosides: A pharmacokinetic interaction between ketoprofen and digoxin has not been demonstrated. However, caution is advised, in particular in patients with renal impairment, since NSAIDs may reduce renal function and decrease renal clearance of cardiac glycosides.
Cyclosporin: Increased risk of nephrotoxicity.
Tacrolimus: Increased risk of nephrotoxicity.
Methotrexate 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.
Pentoxifylline: There is an increased risk of bleeding. More frequent clinical monitoring and monitoring of bleeding time is required.
Tenofovir: Concomitant administration of tenofovir disoproxil fumarate and NSAIDs may increase the risk of renal failure.
Drug associations to be taken into account Antihypertensive agents (beta-blockers, angiotensin converting enzyme inhibitors, diuretics): Risk of decreased antihypertensive potency (inhibition of vasodilator prostaglandins by NSAIDs).
Thrombolytics: Increased risk of bleeding. Probenecid: Concomitant administration of probenecid may markedly reduce the plasma clearance of ketoprofen.
Selective serotonin reuptake inhibitors (SSRIs): increased risk of gastrointestinal bleeding.
Ketoprofen is contraindicated in patients with known hypersensitivity to the drug. Ketoprofen is contraindicated in patients in whom asthma, urticaria, or other sensitivity reaction is precipitated by aspirins or other NSAIDs. Adverse GI Effects should be considered in patients receiving Ketoprofen.
Dyspepsia, nausea, abdominal pain, diarrhoea, constipation, flatulence, anorexia, vomiting, stomatitis, headache, dizziness, malaise, depression, nervousness, dreams, tinnitus, visual disturbance, rash, impairment of renal function, signs or symptoms of urinary-tract irritation.
It is recommended to avoid medication during pregnancy, should not be used during breast feeding unless unavoidable.
Cases of overdose have been reported with doses up to 2.5 g of ketoprofen. In most instances, the symptoms observed have been benign and limited to lethargy, drowsiness, nausea, vomiting and epigastric pain. There are no specific antidotes to ketoprofen overdosages. In cases of suspected massive overdosages, a gastric lavage is recommended and symptomatic and supportive treatment should be instituted to compensate for dehydration, to monitor urinary excretion and to correct acidosis, if present. If renal failure is present, hemodialysis may be useful to remove circulating drug.
Protect from light. Store below 30°C. Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.
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