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Ketoprofen

Ketoprofen – Popular Nsaid to Manage the Pain & Help You Feel Better

ketoprofen is a non-steroidal anti-inflammatory drug (NSAID),  which exhibits analgesic, antipyretic and anti-inflammatory properties.

Like all anti-inflammatories, ketoprofen is indicated for a series of conditions of inflammatory origin, such as arthritis, trauma, dental inflammation, postoperative pain and pain in general.

There are many drugs on the market which have in their formula ketoprofen such as: Bi Profenid , Ceprofen , Flamador , Artrosil and Artrinid .

Note: Dexketoprofen is a drug with a chemical composition similar to ketoprofen. With the exception of the posology, the other information contained in this article is valid for both medicines.

Uses

Ketoprofen is an anti-inflammatory drug indicated for the treatment of mild to moderate intensity pain.

Among the most suitable conditions we can mention:

  • Arthritis is rheumatoid .
  • Psoriasic arthritis.
  • Ankylosing spondylitis.
  • Osteoarthrosis .
  • Dysmenorrhea (menstrual colic) .
  • Acute episodes of gout .
  • Tonsillitis .
  • Migraine.
  • Kidney stone .
  • Odontological inflammations.
  • Tendinitis , tenosynovitis and bursitis;
  • Low back pain and pain in the joints and spine.
  • Trauma
  • Relief of pain in general, such as sore throat , earache or pain in the postoperative period.

Ketoprofen gel is indicated for the treatment of pain of mild intensity of muscular or joint origin, such as low back pain, torticollis, sprains, tendinitis, muscular distensions and injuries of slight severity resulting from the practice of sports.

Dosage

Pills

The usual recommended dose is 200 mg per day (1 pasilla of 100 mg of 12/12 hours or 1 tablet of 50 mg of 6/6 hours). In cases of more intense pain, the maximum dose can be 300 mg per day (1 tablet of 100 mg of 8 / 8h or 1 tablet of 150 mg of 12/12 h).

The 200 mg tablets are prolonged-release and their dose is only 1 tablet a day.

Due to the increased risk of adverse effects, in elderly patients it is recommended not to exceed the dose of 200 mg per day.

The pills can not be split, opened or chewed and should be ingested preferably during or just after meals.

Drops

Each drop contains 1 mg of ketoprofen (presentation of 20 mg / ml).

The recommended doses are:

  • Children over 1 year: 1 drop per kg of weight every 6 or 8 hours.
  • Children from 7 to 11 years old: 25 drops every 6 or 8 hours.
  • Over 12 years old: 50 drops every 6 or 8 hours.

Suppository

1 suppository of 100 mg of 12/12 hours.

As with all anti-inflammatories, the time of use of ketoprofen should be as short as possible.

Special Cases Dosage

Children:

The safety and efficacy of the use of ketoprofen drops in children under 1 year have not yet been established.

Patients with renal insufficiency and the elderly:

It is advisable to reduce the initial dose and keep these patients at the lowest effective dose. An individual dosage adjustment should be considered only after establishing good individual tolerance.

Patients with hepatic impairment:

These patients should be carefully monitored and the lowest daily effective dose should be maintained.

There are no studies of the effects of ketoprofen drops administered by routes not recommended. Therefore, for safety and to ensure the efficacy of this medicinal product, the administration should be only orally.

Capsules

The capsules should be swallowed without chewing with a sufficient amount of liquid (approximately ½ to 1 glass), preferably during or shortly after meals.

Ketoprofen capsules 50 mg:

2 capsules, twice daily; or 1 capsule 3 times daily. Recommended maximum daily dose: 300 mg.

Side Effects

By virtue of being a non-steroidal anti-inflammatory drug (NSAID), ketoprofen shares all the adverse effects of this class of drugs, the most common being:

  • Dyspepsia (burning sensation in the stomach) – 11%.
  • Abdominal pain – 3 to 9%.
  • Constipation – 3 to 9%.
  • Diarrhea – 3 to 9%.
  • Flatulence – 3 to 9%.
  • Nausea- 3 to 9%.
  • Acute renal failure – 3 to 9%.
  • Edemas – 2%.
  • Peptic ulcer – 2%.
  • Digestive hemorrhage – 2%.
  • Dizziness – less than 1%.
  • Visual changes – less than 1%
  • Stomatitis – less than 1%.
  • Leather Rash – less than 1%.

Note: Ketoprofen gel has low systemic absorption and the side effects described are usually not present.

Two serious complications of ketoprofen that deserve a little more attention are peptic ulcer and renal failure , situations that can occur with the prolonged use of any NSAID. Patients with chronic use of any anti-inflammatory drug also have an increased risk of cardiovascular complications.

NSAIDs are also known to interfere with the control of blood pressure and can cause hypertension and resistance to antihypertensive medications.

Contraindications

Ketoprofen should not be given to any patient who has suffered an allergic reaction or bronchospasm crisis related to any NSAID or acetylsalicylic acid (aspirin).

As anti-inflammatories inhibit the action of platelets, in patients with scheduled surgery, ketoprofen should be discontinued at least 48 hours before the procedure to minimize the risk of bleeding intra and postoperatively.

Ketoprofen should also be avoided in patients with the following conditions:

  • Heart failure .
  • High risk of cardiovascular diseases such as heart attack .
  • Gastritis  or  peptic ulcer .
  • History of  digestive hemorrhage .
  • Renal insufficiency .
  • Advanced liver disease, such as  cirrhosis .
  • Badly controlled arterial hypertension .
  • Active bleeds.
  • Thrombocytopenia (very low blood platelet level).
  • Hyperkalemia (elevated levels of potassium in the blood)
  • Pregnancy.
  • Breastfeeding.

Precautions

Ketoprofen can impair fertility and, therefore, should be avoided in women who are trying to conceive.

The use of any anti-inflammatory in the elderly should be done carefully, because the risk of kidney injury and gastrointestinal bleeding in this population is very high. You should always use the lowest effective dose for the shortest possible period.

Ketoprofen should be used with caution in patients with a history of Peptic ulcer disease (PUD).

If gastrointestinal bleeding occurs, treatment should be discontinued. It should be used with caution in patients with severe renal insufficiency , since the elimination of the medicine is done mainly by the urine . There is a possibility of vertigo or dizziness with the use of ketoprofen, therefore, patients who operate machinery or drive vehicles should be warned about this possibility. Elderly (over 65 years) should only use the medicine under medical supervision.

Ketoprofen should not be administered directly into the mouth. It should always be diluted in a little water.

Caution should be exercised when ketoprofen is administered in patients with a history of gastrointestinal disease ( ulcerative colitis, Crohn’s disease ), as these conditions may be exacerbated.

At the start of treatment, renal function should be closely monitored in patients with heart failure, cirrhosis and nephrosis, those taking diuretics or in patients with chronic renal failure, especially if these patients are elderly. In these patients, administration of ketoprofen may induce a reduction in renal blood flow caused by inhibition of prostaglandin and lead to renal decompensation.

Caution should be exercised in the use of ketoprofen in patients with a history of hypertension and / or mild to moderate congestive heart failure, since fluid retention and edema have been reported following administration of NSAIDs.

Increased risk of atrial fibrillation was reported in association with the use of NSAIDs.

Hyperkalemia may occur, especially in patients with underlying diabetes, renal failure and / or concomitant treatment with agents that promote hyperkalemia.

Potassium levels should be monitored under these circumstances.

Pregnancy and Lactation

The use of NSAIDs may impair female fertility and is not recommended in women who are trying to conceive. In women who are difficult to conceive or who are under investigation for infertility, discontinuation of NSAID therapy should be considered.

During the first and second trimesters of gestation

There is no evidence of teratogenicity or embryotoxicity in mice and rats. Mild embryotoxicity effects probably related to maternal toxicity have been reported in rabbits.

As the safety of ketoprofen in pregnant women has not been evaluated, its use should be avoided during the first and second trimesters of pregnancy.

During the third trimester of gestation

All inhibitors of prostaglandin synthesis, including ketoprofen, may induce cardiopulmonary and renal toxicity in the fetus. At the end of pregnancy, bleeding time of the mother and fetus may increase. Therefore, ketoprofen is contraindicated during the last trimester of pregnancy.

Risk category in pregnancy (1st and 2nd gestational trimesters): C.

This medicine should not be used by pregnant women without medical advice or by the dentist.

Drug Interactions

The Concomitant administration of ketoprofen with other medications can cause the following adverse effects due to drug interaction:

  • Any other NSAID – high risk of gastrointestinal injury.
  • Alcohol: high risk of gastrointestinal adverse effects and liver toxicity.
  • Anticoagulants (heparin and warfarin) – increased risk of bleeding.
  • Inhibitors of platelet aggregation eg ticlopidine and clopidogrel ) – increased risk of bleeding.
  • Lithium – risk of increased levels of lithium in the blood.
  • Methotrexate in doses greater than 15 mg / week: increased risk of haematological toxicity, during the first few weeks of combination treatment, the complete blood count should be monitored once a week. If there is any change in renal function or if the patient is elderly, monitoring should be performed more frequently.
  • Colchicine – increased risk of gastrointestinal ulceration or gastrointestinal hemorrhage.
  • Corticosteroids (eg prednisone, prednisolone, dexamethasone) – increased risk of ulceration or gastrointestinal bleeding.
  • Diuretics (eg furosemide, hydrochlorothiazide, chlorthalidone) – Patients using diuretics, particularly dehydrated ones, are at increased risk of developing renal insufficiency due to decreased renal blood flow caused by inhibition of prostaglandin. These patients should be rehydrated prior to initiation of concomitant treatment and renal function should be monitored when treatment is initiated.
  • ACE inhibitors (eg, ramipril, enalapril, lisinopril) or angiotensin II antagonists (eg, irbesartan, losartan, valsartan) – In patients with impaired renal function (eg dehydrated patients or elderly patients), coadministration of an ACE inhibitor or an angiotensin II antagonist and an agent that inhibits cyclooxygenase may promote deterioration of renal function, including the possibility of acute renal failure. In addition to an increased risk of hyperkalemia (high potassium in the blood) and acute kidney injury.
  • Tenofovir – higher risk of acute kidney injury.
  • Antihypertensive drugs – risk of reducing the antihypertensive effect due to inhibition of vasodilator prostaglandins by NSAIDs.
  • Cyclosporine- greater risk of acute kidney injury and arterial hypertension.
  • Selective serotonin reuptake inhibitors (eg, fluoxetine, paroxetine, sertraline) – increased risk of gastrointestinal bleeding.
  • Probenecid – Concomitant administration with probenecid can markedly reduce plasma clearance of ketoprofen.

Food Interaction

Concomitant use with food may delay the absorption of ketoprofen, however, no clinically significant interactions have been observed.

Laboratory Tests

The use of ketoprofen may interfere with the determination of urinary albumin, bile salts, 17-ketosteroids, and 17-hydroxycorticosteroids that are based on acid precipitation or colorimetric reaction of carbonyl groups.

Trade Names

Ketoprofen can be found in its generic form or through the various commercial names available in the market, among which we highlight:

  • Argentina:  Salicrem K.
  • Chile:  Dolofar, Dolostat, Profenid, Relatene, Talflex.
  • Colombia:  Ketoflex, Profenid.
  • Spain:  Fastum, Extraplus, Orudis,
  • Mexico:  Arthril, Bi-profenid, Dolo Bedoyecta, Ketoflex, Profenid,
  • Paraguay:  Flogostone, Iprofen, Ketoflog, Ketopromin, Milenos, Profenid.
  • Uruguay:  Ketofen, Novobealgia, Orudis, Profenid, Ruprof, Sindol

Ketoprofen can be found in the forms of 50,100, 150 or 200 mg pills, drops, syrup, suppository or gel.

There is also the injectable form for intrahospital administration, used in cases of severe pain, such as postoperative or episodes of renal colic.

Pharmacokinetics

Absorption

Ketoprofen is rapidly and completely absorbed from the gastrointestinal tract. Peak plasma levels are obtained within 60 to 90 minutes after oral administration. When ketoprofen is administered with food, the absorption rate decreases, resulting in delay and reduction in plasma concentration ( Cmax ), however, the total bioavailability is not altered.

Distribution

Ketoprofen is 99% bound to plasma proteins. It diffuses through the synovial fluid, intra-articular, capsular, synovial and tendinous tissues and crosses the placental and blood-brain barrier. The plasma elimination half-life is approximately 2 hours.

Metabolism

The biotransformation of ketoprofen is characterized by two main processes: by hydroxylation and by conjugation with glucuronic acid, the latter being the main route in man.

The excretion of ketoprofen in the unchanged form is very low (less than 1%). Almost the entire dose administered is excreted as metabolites in the urine, of which 65 to 85% of the administered dose is excreted as a glucuronide metabolite.

Elimination

Fifty percent (50%) of the administered dose is excreted in the urine within 6 hours after administration of the drug. For 5 days after oral administration, approximately 75 to 90% of the dose is excreted primarily by urine. Fecal excretion is very small (1 to 8%).

Efficacy Studies

An open clinical study by Addy (1985) evaluated the use of ketoprofen at a dose of 50mg 3 times a day during the menstrual period for 3 months in 42 women with dysmenorrhea. At the end of the study 95% of the women returned to their normal activities and presented a good tolerability to the treatment.

Barbieri (1987) conducted a double-blind, randomized, placebo-controlled study of 60 pediatric patients (1 to 10 years) with acute bacterial tonsillitis who required amoxicillin as antibiotic therapy. All clinical parameters considered, such as oropharyngeal appearance, edema , exudate and hypertrophy of the tonsils showed a statistically significant improvement, with the superiority of the ketoprofen group compared to placebo. All patients took antibiotics for 7 to 10 days.

An open study by Kokki et al (2000) evaluated 611 children (1-9 years) who used ketoprofen in the postoperative period of adenoidectomy. The study evaluated pain, presence of adverse events and bleeding during the first postoperative week. The dose used reached 5mg / kg / day. Ketoprofen demonstrated good analgesic efficacy and safety during the short period of use. There was no clinically significant bleeding and no child needed intervention, reoperation, or even hospitalization for bleeding.

A study by Spongsveen et al. (1978) evaluated the use of ketoprofen at a dose of 50mg 3 times daily in patients with chronic osteoarticular diseases. These patients were followed up for a minimum period of 3 months to 12 months. Ketoprofen promoted clinical improvement in the majority of patients, proving its efficacy among the patients evaluated. The number of adverse events occurred in 13% of the patients, with gastrointestinal events, mainly dyspepsia , being the most frequent. However there were no events considered serious.

Karvonen et al (2008) conducted a double-blind, randomized, placebo-controlled, parallel group study in which the use of paracetamol and ketoprofen in the postoperative pain control of 60 adult patients submitted to total hip prosthesis was evaluated. The use of oral ketoprofen at a dose of 300mg daily reduced opioid consumption by 22% on the 1st postoperative day.

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