Profenid-E 50mg 10pcs

Indications

The indications for ketoprofen are based on its anti-inflammatory, analgesic, and antipyretic properties. Ketoprofen is suitable for symptomatic treatment:

• Rheumatoid arthritis
• degenerative joint disease
• Musculoskeletal and joint diseases, such as tendinitis, sprain
• Pain, regardless of its origin, such as toothache, headache, and primary dysmenorrhea.

Pharmacology

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that has analgesic and antipyretic effects. In addition to inhibiting prostaglandin synthesis, it also stabilizes lysosomal membranes inside and outside the body, inhibits leukotriene synthesis at high concentrations in vitro, and also exhibits anti-bradykinin activity in vivo. Ketoprofen produces analgesic effects by inhibiting the synthesis of central and peripheral prostaglandins. Ketoprofen is also believed to inhibit prostaglandin synthesis in the central nervous system (possibly in the hypothalamus), leading to its antipyretic effect.

Ketoprofen can be absorbed rapidly and almost completely from the gastrointestinal tract. Approximately 99% is bound to plasma proteins, mainly albumin. The average elimination half-life of the drug is 1.14 hours after single or multiple oral administration to healthy adults. It is rapidly and extensively metabolized in the liver, primarily by binding to glucuronic acid. After a single oral administration of ketoprofen in healthy adults, about 50-90% of the drug is excreted in the urine within 15 days and about 18% is excreted in the feces; most urine excretion occurs within 12 to 24 hours, and most fecal excretion occurs within 15 days. 2448 In a matter of hours. In the case of IM injection, a maximum concentration of approximately 10 mg / L is reached approximately 0.50.75 hours after the 100 mg dose. The elimination half-life is approximately 1.88 hours.

Dosage & Administration

Anti-inflammatory dosage: The recommended starting dose is 150 to 300 mg/day in 3 divided doses. Once the maintenance dosage has been established (usually 100 to 200 mg/day), the patient may be tried on a twice daily dose regimen. Alternatively, switching to the once daily form at the same dosage may be considered. The recommended maximum daily dose is 300 mg.

Management of pain and primary dysmenorrhea: The usual recommended dose is 25 to 50 mg, every 6 to 8 hours as necessary. The total daily dose should not exceed 300 mg. 

Interaction

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.

Platelet aggregation inhibitor.

Thrombin inhibitors.

Direct factor Xa inhibitors.

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.

Contraindications

Ketoprofen is contraindicated in patients who have a history of hypersensitivity reactions such as asthmatic attacks or other allergic-type reactions to ketoprofen, ASA, or other NSAIDs. Severe, rarely fatal, anaphylactic reactions have been reported in such patients. Ketoprofen is also contraindicated in the following cases:

• Severe heart failure
• Active or history of peptic ulcer/hemorrhage
• History of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy
• Severe hepatic insufficiency
• Severe renal insufficiency
• The third trimester of pregnancy
• Rectitis or history of proctorrhagia

Side Effects

• Blood and lymphatic system disorders- Rare: hemorrhagic anaemia; Unknown: agranulocytosis, thrombocytopenia, bone marrow failure, hemolytic anemia, leucopenia
• Immune system disorders- Unknown: anaphylactic reactions (including shock) Psychiatric disorders; Unknown: depression, hallucinations, confusion, mood altered
• Nervous system disorders- Uncommon: headache, dizziness, somnolence, Rare: paraesthesia; Unknown: aseptic meningitis, convulsions, dysgeusia, vertigo
• Eye disorders- Rare: vision blurred
• Ear and labyrinth disorders- Rare: tinnitus
• Cardiac disorders- Unknown: exacerbation of heart failure, atrial fibrillation
• Vascular disorders- Unknown: hypertension, vasodilatation, vasculitis.
• Respiratory, thoracic and mediastinal disorders- Rare: asthma; Unknown: bronchospasm
• Gastrointestinal disorders- Common: dyspepsia, nausea, abdominal pain, vomiting; Uncommon: constipation, diarrhoea, flatulence, gastritis; Rare: stomatitis, peptic ulcer; Unknown: exacerbation of colitis and Crohn’s disease, gastrointestinal haemorrhage and perforation, pancreatitis
• Hepatobiliary disorders- Rare: hepatitis, transaminases increased
• Skin and subcutaneous disorders- Uncommon: rash, pruritis; Unknown: photosensitivity reaction, alopecia, urticaria, angioedema, bullous eruption including Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis Renal and urinary disorders- Unknown: renal failure acute, tubulointerstitial nephritis, nephritic syndrome, renal function tests abnormal
• General disorders and administration site conditions- Uncommon: edema Metabolism and nutritional disorders; Unknown: hyponatremia, hyperkalemia Investigations; Rare: weight increased.

Pregnancy & Lactation

During the first and second trimesters of pregnancy: Because the safety of ketoprofen in pregnant women has not been established, it should be avoided during the first and second trimesters of pregnancy. During the third trimester of pregnancy: Prodenid is not recommended during the third trimester. Ketoprofen should not be used by nursing moms.

 Precautions & Warnings

Oral dosage form: Patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease) should use NSAIDs with caution because their condition may worsen. At the beginning of treatment, the renal function of patients with heart failure, cirrhosis, and kidney disease, patients receiving diuretic therapy, and patients with chronic renal failure, especially in elderly patients, should be carefully monitored. In these patients, the administration of ketoprofen can cause a decrease in renal blood flow caused by the inhibition of prostaglandins and cause renal degradation.

Patients with a history of mild to moderate hypertension and / or congestive heart failure should be cautious due to reports of fluid retention and edema associated with NSAID treatment.

It has been reported that there is an increased risk of atrial fibrillation associated with the use of NSAIDs. Hyperkalemia may occur, especially in patients with underlying diabetes, renal failure, and / or concurrent treatment with promoters of hyperkalemia. In these cases, the potassium content must be controlled.

Like other non-steroidal anti-inflammatory drugs, in the presence of infectious diseases, it should be noted that the anti-inflammatory, analgesic and antipyretic properties of ketoprofen can mask common signs of infection progression, such as fever.

For patients with abnormal liver function tests or a history of liver disease, transaminase levels should be assessed regularly, especially during long-term treatment. Rare cases of jaundice and hepatitis have been described as the use of ketoprofen.

If vision disorders such as blurred vision occur, treatment should be stopped. The use of non-steroidal anti-inflammatory drugs can affect female fertility and is not recommended for women who are trying to become pregnant. For women who have difficulty conceiving or are undergoing infertility testing, NSAIDs should be considered to be discontinued. 

Storage Conditions

Protect from light. Store below 30°C. Do not use it 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.