Ketoprovel pills 100mg, 30pcs

Composition

Per tablet:

Active ingredient: ketoprofen-100 mg.

Excipients: hyprolose (hydroxypropylcellulose), mannitol( mannitol), croscarmellose sodium (primellose), microcrystalline cellulose, colloidal silicon dioxide (aerosil), magnesium stearate; shell composition: opadray 03F180011 white (hypromellose, titanium dioxide, macrogol).

Pharmacological action

Pharmacotherapy group: nonsteroidal anti-inflammatory drug (NSAID)

ATX code: M 01 AE 03

Pharmacological properties

Pharmacodynamics

Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID). It has anti-inflammatory, analgesic and antipyretic effects. Ketoprofen blocks the action of cyclooxygenase 1 and 2 (COX-1 and COX-2) and, partially, lipoxygenase, which leads to suppression of prostaglandin synthesis (including in the central nervous system (CNS), most likely in the hypothalamus). It stabilizes liposomal membranes in vitro and in vivo, and suppresses the synthesis of bradykinin and leukotrienes at high concentrations in vitro.

Ketoprofen does not have a negative effect on the condition of articular cartilage.

Pharmacokinetics

Absorption rate

Ketoprofen is easily absorbed from the gastrointestinal tract( GIT), bioavailability -90

%. Binding to plasma proteins is 99%. When 100 mg of ketoprofen is taken orally, the maximum concentration (Cmax) in blood plasma (10.4 mcg/ml) is reached after 1 hour and 22 minutes.

Distribution

Ketoprofen is 99% bound to blood proteins, mainly to the albumin fraction. The volume of distribution is 0.1 l/kg. Ketoprofen penetrates the synovial fluid and reaches a concentration there equal to 30% of the concentration in blood plasma. The plasma clearance of ketoprofen is approximately 0.08 l/kg/h.

Metabolism and elimination

Ketoprofen undergoes intensive metabolism under the influence of microsomal liver enzymes, with a half-life (T1 / 2) of less than 2 hours. Ketoprofen binds to glucuronic acid and is eliminated from the body in the form of glucuronide. Ketoprofen has no active metabolites. Up to 80% of ketoprofen is excreted by the kidneys within 24 hours, mainly in the form of ketoprofen glucuronide. When using ketoprofen at a dose of 100 mg or more, renal excretion may be difficult.

In patients with hepatic insufficiency, the plasma concentration of ketoprofen is doubled (probably due to hypoalbuminemia and, consequently, high levels of unbound active ketoprofen): such patients should be prescribed ketoprofen at the minimum therapeutic dose.

In patients with renal insufficiency, the clearance of ketoprofen is reduced, but dose adjustment is required only in cases of severe renal insufficiency. In severe renal insufficiency, most of the ketoprofen is released through the intestines. When taking high doses, hepatic clearance also increases. About 40% of ketoprofen is excreted through the intestines. In elderly patients, ketoprofen metabolism and elimination are slower, which is of clinical significance only for patients with severe renal insufficiency.

Indications

Symptomatic therapy of painful and inflammatory processes of various origins, including inflammatory and degenerative diseases of the musculoskeletal system:

– rheumatoid arthritis;

– seronegative arthritis: ankylosing spondylitis (ankylosing spondylitis), psoriatic arthritis, reactive arthritis (Reiter syndrome);

– gout, pseudogout;

– osteoarthrosis;

– tendonitis, bursitis, myalgia, neuralgia, sciatica;

pain syndrome, including weak, moderate and pronounced;

– headache;

– toothache;

– post-traumatic and postoperative pain;

pain syndrome with cancer;

– algomenorrhea.

Use during pregnancy and lactation

Inhibition of prostaglandin synthesis may have undesirable effects on the course of pregnancy and / or embryonic development. Data obtained in epidemiological studies with the use of prostaglandin synthesis inhibitors in early pregnancy confirm an increased risk of spontaneous abortion and the formation of heart defects (about 1-1.5%).

Use the drug in pregnant women in the first and second trimesters of pregnancy is possible only if the potential benefit to the mother exceeds the possible risk to the fetus.

The use of ketoprofen is contraindicated in pregnant women during the third trimester of pregnancy due to the possibility of developing weakness of uterine labor activity and/or premature closure of the arterial duct, possible increase in bleeding time, lack of water and renal failure.

Currently, there are no data on the excretion of ketoprofen in breast milk, so if you need to use ketoprofen during breastfeeding, you should decide whether to stop breastfeeding.

Contraindications

– hypersensitivity to Ketoprofen or other components of the drug, as well as salicylates or other NSAIDs;

– complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);

– ulcer of the stomach or duodenum in the acute phase;

ulcerative colitis: Crohn’s disease;

– hemophilia and other blood clotting;

– severe liver failure;

– severe renal insufficiency (creatinine clearance less than 30 ml/min);

decompensated heart failure;

post – operative period after coronary artery bypass surgery;

gastrointestinal, cerebrovascular, and other bleeding (or suspected bleeding);

– progressing kidney disease, diverticulitis, active liver disease, inflammatory bowel diseases, confirmed hyperkalemia;

chronic dyspepsia;

– children’s age up to 15 years;

III trimester of pregnancy;

– the period of breastfeeding.

With caution

A history of bronchial asthma, clinically expressed cardiovascular, cerebrovascular and peripheral arterial diseases, dyslipidemia, progressive liver diseases, liver failure, hyperbilirubinemia, alcoholic cirrhosis of the liver, renal failure (creatinine clearance 30-60 ml/min), chronic heart failure, arterial hypertension, blood diseases, dehydration, diabetes mellitus, anamnestic data on development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, severe somatic diseases, advanced age, smoking, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid), oral glucocorticosteroids (for example, prednisone), selective serotonin reuptake inhibitors (for example, citalopram, sertraline), long-term use of NSAIDs; elderly patients taking diuretics; patients with reduced circulating blood volume.

Side effects

the incidence of side effects was determined in accordance with the classification of the world health organization (who): very often (>1/10), often (>1/100, <1/10), infrequently (>1/1000,

<1/100), rare (>1/10000, <1/1000), very rare (<1/10000), the unknown frequency (frequency of occurrence cannot be determined based on available data).

Disorders of the blood and lymphatic system: rarely-hemorrhagic anemia; frequency unknown-agranulocytosis, thrombocytopenia, impaired bone marrow function.

Immune system disorders: frequency unknown – anaphylactic reactions (including anaphylactic shock).

Nervous system disorders: infrequently-headache, dizziness, drowsiness; rarely-paresthesia; frequency unknown-convulsions, impaired taste sensations.

Mental disorders: frequency unknown-emotional lability.

Visual disturbances: rarely – blurred vision.

Hearing disorders and labyrinth disorders: rarely-tinnitus.

Cardiac disorders: frequency unknown-heart failure.

Vascular disorders: frequency unknown-increased blood pressure, vasodilation.

Respiratory, thoracic and mediastinal disorders: rarely-exacerbation of bronchial asthma; frequency unknown-bronchospasm (especially in patients with hypersensitivity to NSAIDs), rhinitis.

Gastrointestinal disorders: often – nausea, vomiting, dyspepsia, abdominal pain; infrequently-constipation, diarrhea, bloating, gastritis; rarely-peptic ulcer, stomatitis; very rarely-exacerbation of ulcerative colitis or Crohn’s disease, gastrointestinal bleeding, perforation.

Liver and biliary tract disorders: rarely-hepatitis, increased activity of “hepatic” transaminases, increased bilirubin concentration.

Skin and subcutaneous tissue disorders: infrequently-skin rash, pruritus; frequency unknown-photosensitization, alopecia, urticaria, angioedema, erythema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis. Renal and urinary tract disorders: frequency unknown-acute renal failure, interstitial nephritis, nephritic syndrome, nephrotic syndrome, abnormal values of renal function indicators.

General disorders and disorders at the injection site: infrequently-edema; rarely-weight gain; frequency unknown-increased fatigue.

Interaction

Ketoprofen may weaken the effect of diuretics and antihypertensive agents and increase the effect of hypoglycemic drugs for oral use and some anticonvulsants (phenytoin).

Concomitant use with other NSAIDs, salicylates, glucocorticosteroids, and ethanol increases the risk of gastrointestinal adverse events.

Concomitant use with anticoagulants (heparin, warfarin), thrombolytics, antiplatelet agents (ticlopidine, clopidogrel), pentoxifylline increases the risk of bleeding.

Concomitant use with potassium salts, potassium-sparing diuretics, ACE inhibitors, NSAIDs, low-molecular-weight heparins, cyclosporine, tacrolimus and trimethoprim increases the risk of hyperkalemia.

Ketoprofen increases plasma concentrations of cardiac glycosides,

slow calcium channel blockers, lithium, cyclosporine, methotrexate, and digoxin. Increases methotrexate toxicity and cyclosporine nephrotoxicity. Concomitant use with probenecid significantly reduces the clearance of ketoprofen in blood plasma.

Concomitant use with glucocorticosteroids and other NSAIDs (including selective COX-2 inhibitors) increases the likelihood of side effects (in particular, from the gastrointestinal tract).

NSAIDs may reduce the effectiveness of mifepristone. NSAIDs should be started no earlier than 8-12 days after mifepristone is discontinued.

How to take, course of use and dosage

Inside.

The drug should be swallowed whole during or after a meal, washed down with water or milk (the volume of liquid should be at least 100 ml).

Usually, the drug is prescribed 1 tablet 2 times a day.

Oral ketoprofen preparations can be combined with the use of rectal suppositories, for example, the patient can take 1 tablet (100 mg) of ketoprofen in the morning and enter 1 suppository (100 mg) rectally in the evening.

The maximum dose of ketoprofen is 200 mg / day.

It is not recommended to exceed the maximum daily dose of the drug.

In order to reduce the risk of adverse events from the gastrointestinal tract (GIT), patients with risk factors are recommended to take proton pump inhibitors at the same time.

Overdose

Symptoms

As with other NSAIDs, an overdose of ketoprofen may cause nausea, vomiting, abdominal pain, vomiting with blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function and renal failure.

In case of overdose, gastric lavage and the use of activated charcoal are indicated.

Treatment

Treatment is symptomatic. The effects of ketoprofen on the gastrointestinal tract can be reduced with the help of agents that reduce the secretion of gastric glands (for example, proton pump inhibitors), and prostaglandins.

Description

Round biconvex tablets, film-coated in white or almost white color. On a cross-section – the core is white or almost white in color.

Special instructions

Ketoprofen should not be combined with other NSAIDs and/or COX-2 inhibitors. With long-term use of NSAIDs, it is necessary to periodically evaluate a clinical blood test, monitor kidney and liver function, especially in elderly patients (over 65 years), and conduct a fecal occult blood test.

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 in the body.

If visual disturbances occur, treatment should be stopped immediately.

Like other NSAIDs, ketoprofen can mask the symptoms of infectious and inflammatory diseases. In case of signs of infection or deterioration of health during the use of the drug, you should immediately consult a doctor.

If there is a history of contraindications from the gastrointestinal tract (bleeding, perforation, peptic ulcer disease), long-term therapy and the use of high doses of ketoprofen, the patient should be under close medical supervision.

Due to the important role of prostaglandins in maintaining renal blood flow, special care should be taken when using ketoprofen in patients with cardiac or renal insufficiency, as well as in the treatment of elderly patients taking diuretics, and patients who, for any reason, have a decrease in the volume of circulating blood. The use of the drug should be discontinued before major surgical intervention.

The use of ketoprofen may affect female fertility, so patients with infertility (including those undergoing examination) are not recommended to use the drug.

Influence on the ability to drive vehicles and mechanisms

There are no data on the negative effect of ketoprofen in the recommended doses on the ability to drive a car or work with mechanisms. At the same time, patients who experience drowsiness, dizziness or other unpleasant sensations from the nervous system, including visual disturbances, should refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Ketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

Tablets