Ketonal pills 100mg, 20pcs

Composition

1 tablet contains:

Active ingredient:

ketoprofen – 100 mg.

Auxiliary substances:

magnesium stearate,

colloidal silicon dioxide,

corn starch,

povidone,

talc,

lactose.

Shell composition:

hypromellose, macrogol 400, indigo carmine (E132), titanium dioxide, talc, Carnauba wax.

Pharmacological action

Ketoprofen is rapidly absorbed from the gastrointestinal tract. Bioavailability after oral use of 50 mg of ketoprofen is 90% and increases sequentially with increasing dose.

Food intake does not affect the total bioavailability (AUC) of ketoprofen, but reduces the rate of absorption. Ketoprofen is 99% bound to plasma proteins, mainly to the albumin fraction. The volume of distribution is 0.1-0.2 l / kg. After oral use of ketoprofen, the peak plasma concentration is reached in 1 h. 22 min.

In the synovial fluid, the concentration of ketoprofen reaches 50% of the plasma concentration (1.5 mcg / ml); ketoprofen is removed from the synovial fluid slowly – within 24 hours. It is metabolized in the liver, where it is conjugated with glucuronic acid. About 75% of ketoprofen is excreted in the urine, mainly as a conjugate with glucuronic acid.

Less than 10% is excreted unchanged in the faeces. Ketoprofen does not accumulate in the tissues. The half-life of ketoprofen is 2 hours. In patients with renal insufficiency, ketoprofen is excreted more slowly, and its half-life is extended by 1 hour. They also have a reduced clearance of ketoprofen.

In severe renal insufficiency, a dose reduction is required. In patients with hepatic insufficiency, the concentration of ketoprofen in the blood plasma is increased approximately 2 times, which requires the appointment of the lowest possible daily dose. Ketonal ® forte has anti-inflammatory, analgesic and antipyretic effects.

The mechanism of action is associated with inhibition of prostaglandin and leukotriene biosynthesis by suppressing the activity of the cyclooxygenase enzyme (cyclooxygenase-1 and cyclooxygenase-2), which catalyzes the synthesis of prostaglandins from arachidonic acid. Ketoprofen stabilizes lysosomal membranes and has anti-radikinin activity.

Indications

1. Rheumatic diseases: rheumatoid arthritis seronegative spondyloarthritis (ankylosing spondylitis, reactive arthritis) gout, pseudogout osteoarthritis extra-articular rheumatism (tendinitis, bursitis, shoulder capsulitis)

2. Pain syndrome: post-traumatic postoperative algodismenorrhea pain in bone metastases in patients with cancer.

Contraindications

• A history of bronchial asthma, rhinitis, and urticaria caused by taking acetylsalicylic acid or other NSAIDs.
• Peptic ulcer of the stomach and duodenum in the acute phase.
• UC, Crohn’s disease.
• Hemophilia and other blood clotting disorders.
• Severe liver failure.
• Severe renal failure.
• Progressive kidney diseases.
• Uncompensated heart failure.
• Postoperative period after coronary artery bypass grafting.
• Gastrointestinal, cerebrovascular, and other bleeding (or suspected bleeding).
• Chronic dyspepsia.
• Children under 15 years of age.
• Third trimester of pregnancy.
• The period of lactation (breastfeeding).
• Hypersensitivity to ketoprofen or other components of the drug, as well as salicylates or other NSAIDs.

With caution:  the drug should be prescribed for a history of peptic ulcer disease, a history of bronchial asthma, clinically expressed cardiovascular, cerebrovascular diseases, peripheral artery diseases, dyslipidemia, liver failure, hyperbilirubinemia, alcoholic cirrhosis of the liver, renal failure, chronic heart failure, arterial hypertension, blood diseases, dehydration, diabetes mellitus, anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, smoking, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid), oral corticosteroids (for example, prednisone), selective serotonin reuptake inhibitors (for example, citalopram, sertraline).

Side effects

When assessing the frequency of occurrence of various adverse reactions, the following gradations were used: ” very often ” – 10%, ” often ” – from 1% to ? 10%, “infrequently” – from 0.1% to 1%, “rarely” – from 0.01% to 0.1%, “very rarely” – 0.01%.

Common: dyspeptic symptoms, decreased appetite, nausea, vomiting, flatulence, abdominal pain, constipation

Infrequently: diarrhea, gastritis headache, dizziness, drowsiness skin rash

Rare: hemorrhagic anemia, leukopenia depression, insomnia, nervousness, paresthesia visual impairment tinnitus stomatitis, stomach and duodenal ulcers hepatitis, increased transaminases and bilirubin levels body weight gain anaphylactic shock bronchospasm, asthma attack

Very rare: exacerbation of colitis and Crohn’s disease, gastrointestinal bleeding impaired liver function acute renal failure, tubulointerstitial nephritis hypernatremia, hyperkalemia agranulocytosis, thrombocytopenia convulsions heart failure arterial hypertension rhinitis photosensitization, Angioedema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

Interaction

Ketonal should not be used in combination with other nonsteroidal anti-inflammatory drugs and salicylates. When combined with corticosteroids, the risk of ulceration and gastrointestinal bleeding increases.

Anticoagulants (heparin and warfarin) and platelet aggregation inhibitors (i. e. ticlopidine, clopidogrel) increase the risk of bleeding. If co-admission is unavoidable, careful monitoring of the patient is necessary. Ketonal reduces the effectiveness of antihypertensive and diuretic drugs.

The risk of developing renal failure is higher in patients who take diuretics, antihypertensive agents or ACE inhibitors simultaneously with nonsteroidal anti-inflammatory drugs.

Potassium supplements, potassium-sparing diuretics, ACE inhibitors, heparins (low molecular weight or undivided into fractions), cyclosporine, tacrolimus and trimethoprim when used concomitantly with nonsteroidal anti-inflammatory drugs may contribute to the occurrence of hyperkalemia. Ketonal increases the effect of oral hypoglycemic drugs and some anticonvulsants (phenytoin).

Ketonal, like other non-steroidal anti-inflammatory drugs, reduces the excretion, and thereby increases the toxicity of cardiac glycosides, lithium, cyclosporine, and methotrexate. Nonsteroidal anti-inflammatory drugs may reduce the effectiveness of mifepristone.

Nonsteroidal anti-inflammatory drugs should be started no earlier than 8-12 days after mifepristone is discontinued. Concomitant use of cyclosporine with ketonal increases the risk of toxic kidney damage.

How to take, course of use and dosage

Adults: the drug is prescribed 1-2 capsules 2-3 times a day, or 1 tab. 2 times/day, or 1 tablet of prolonged action 1 time/day.

Capsules and tablets should be taken during or immediately after a meal, without chewing, with a sufficient amount of water or milk (liquid volume – at least 100 ml).

Oral forms can be combined with the use of rectal suppositories or dosage forms of Ketonal for external use (cream, gel).

The maximum daily dose (including when using various dosage forms) is 200 mg.

Overdose

Symptoms:  nausea, vomiting, abdominal pain, vomiting with blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function, renal failure.

Treatment:  gastric lavage, use of activated charcoal, and symptomatic therapy are performed. The use of histamine H2-receptor blockers, proton pump inhibitors, and prostaglandin inhibitors is indicated. There is no specific antidote.

Special instructions

Ketonal® can be washed down with milk or taken with antacids to reduce the frequency of gastrointestinal disorders (milk and antacids do not affect the absorption of ketoprofen). With prolonged use of NSAIDs, it is necessary to monitor the condition of the blood, as well as liver and kidney function, especially in elderly patients.

It is necessary to exercise caution and monitor blood pressure more often when using ketoprofen for the treatment of patients with arterial hypertension, cardiovascular diseases that lead to fluid retention.

Like other NSAIDs, ketoprofen may mask the symptoms of infectious diseases.

Influence on the ability to drive motor vehicles and manage mechanisms

There are no data on the negative effect of Ketonal in the recommended doses on the ability to drive a car or work with mechanisms.

At the same time, patients who report non-standard effects when taking Ketonal® should be careful when engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets

Storage conditions

Keep out of reach of children at a temperature not exceeding 25°C.

Shelf

life is 5 years.

Active ingredient

Ketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

Tablets