Ketropel
Ketopropel: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Ketoprovel
ATX code: M01AE03
Active ingredient: ketoprofen (Ketoprofen)
Manufacturer: OOO Velpharm (Russia)
Description and photo update: 2020-01-08
Ketopropel is a non-steroidal anti-inflammatory drug (NSAID) that has analgesic, antipyretic and anti-inflammatory effects.
Release form and composition
The drug is produced in the form of tablets, film-coated, round, biconvex; the film shell is almost white or white, the core in the cross section has a color from almost white to white instructions for medical use; in polymer cans made of polypropylene or low-pressure polyethylene of 10, 20, 30 or 50 tablets, in a pack of cardboard 1 can and instructions for use of Ketopropel].
Composition of one film-coated tablet:
- active ingredient: ketoprofen - 100 mg;
- additional substances: mannitol (mannitol), MCC (microcrystalline cellulose), magnesium stearate, hydroxypropyl cellulose (hyprolose), primellose (croscarmellose sodium), aerosil (colloidal silicon dioxide);
- film casing: white Opadray 03F180011 (titanium dioxide, hypromellose, macrogol).
Pharmacological properties
Pharmacodynamics
Ketoprofen, the active ingredient of Ketopropel, is an NSAID that has analgesic, antipyretic and anti-inflammatory effects. The effect of the drug is associated with inhibition of the synthesis of prostaglandins [in the central nervous system (CNS) inclusive, most likely in the hypothalamus], due to blocking the action of cyclooxygenase-1 and cyclooxygenase-2, as well as, to some extent, lipoxygenase.
Ketoprofen stabilizes in vivo and in vitro liposomal membranes, at high concentrations in vitro inhibits the synthesis of leukotrienes and bradykinin.
Ketopropel has no negative effect on the condition of the articular cartilage.
Pharmacokinetics
Pharmacokinetic characteristics of ketoprofen:
- absorption: the absorption of ketoprofen from the gastrointestinal tract (GIT) is easy, bioavailability reaches 90%. The substance binds to proteins of blood plasma (mainly with the albumin fraction) by 99%. The maximum concentration (C max) in the blood plasma after oral administration of ketoprofen at a dose of 100 mg is observed after about 80 minutes and is 10.4 μg / ml;
- distribution: the volume of distribution is 0.1 l / kg. Ketoprofen penetrates into the synovial fluid, reaching a concentration there equal to 30% of the concentration in blood plasma. Plasma clearance of the substance is about 0.08 l / kg / h;
- metabolism and excretion: under the influence of microsomal liver enzymes, ketoprofen undergoes intensive metabolism, while no active metabolites are found in it. The half-life (T 1/2) is less than 2 hours. The substance binds to glucuronic acid and is removed from the body in the form of glucuronide. About 80% is excreted in the urine during the day, mainly in the form of ketoprofen glucuronide. Excretion of ketoprofen by the kidneys may be difficult if taken at a dose of ≥ 100 mg.
Features of the pharmacokinetics of ketoprofen in certain categories of patients:
- patients with liver dysfunction: a twofold increase in the concentration of ketoprofen in plasma was noted (a likely cause may be hypoalbuminemia and, as a consequence, a high level of unbound active ketoprofen), and therefore indicated the appointment of ketoprofen in the minimum therapeutic dose;
- patients with renal dysfunction: there is a decrease in ketoprofen clearance, but there is no need for dose adjustment, except in cases of severe renal failure (in patients with this pathology, most of ketoprofen is removed from the body through the intestine). Reception of Ketopropel in high doses also leads to an increase in hepatic clearance. Up to 40% of ketoprofen is excreted through the intestines;
- elderly patients: there is a slowdown in metabolic processes and the elimination of ketoprofen from the body; this fact is of clinical significance only for patients with severe renal failure.
Indications for use
Ketopropel is prescribed for the symptomatic treatment of painful and inflammatory processes of various origins, including diseases of the musculoskeletal system of an inflammatory and degenerative nature:
- pain syndrome of mild, moderate and severe degree;
- pain syndrome in cancer;
- postoperative and post-traumatic pain syndrome;
- algodismenorrhea;
- toothache;
- headache;
- gout, pseudogout;
- seronegative arthritis: Reiter's syndrome (reactive arthritis), psoriatic arthritis, ankylosing spondylitis (ankylosing spondylitis);
- rheumatoid arthritis;
- osteoarthritis;
- neuralgia, myalgia, bursitis, tendinitis, radiculitis.
Contraindications
Absolute:
- complete and incomplete Fernand-Vidal triad, including bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including a history);
- ulcerative colitis (NUC), Crohn's disease;
- stage of exacerbation of gastric / duodenal ulcer;
- chronic dyspepsia;
- bleeding (cerebrovascular, gastrointestinal, etc.) or suspicion of them;
- postoperative period after coronary artery bypass grafting;
- hemophilia and other blood clotting disorders;
- decompensated heart failure;
- renal failure of severe degree with creatinine clearance (CC) <30 ml / min;
- severe liver failure;
- confirmed hyperkalemia, diverticulitis, progressive kidney disease, inflammatory bowel disease, active liver disease;
- lactation period (breastfeeding);
- third trimester of pregnancy;
- age up to 15 years;
- established sensitivity to ketoprofen or other components of ketopropel, salicylates or other NSAIDs.
Relative (the drug must be taken with caution, strictly following the instructions for the dosage regimen and the recommendations of the attending physician):
- clinically expressed diseases of the peripheral arteries, as well as cerebrovascular and cardiovascular diseases;
- dyslipidemia;
- history of bronchial asthma;
- renal failure with QC from 30 to 60 ml / min;
- liver failure, progressive liver disease, alcoholic liver cirrhosis, hyperbilirubinemia;
- blood diseases;
- arterial hypertension, chronic heart failure (CHF);
- severe somatic diseases;
- presence of Helicobacter pylori infection, history of the development of ulcerative lesions of the gastrointestinal tract;
- diabetes;
- dehydration;
- a decrease in the volume of circulating blood (BCC);
- smoking;
- second and third trimesters of pregnancy (only if the potential benefits to the mother exceed the possible risks to the fetus);
- elderly age;
- taking diuretics in old age;
- long-term NSAID therapy;
- simultaneous administration of anticoagulants (such as warfarin, etc.), antiplatelet agents (ASA, etc.), oral glucocorticosteroids (prednisolone, etc.), selective serotonin reuptake inhibitors (such as sertraline, citalopram, etc.).
Ketopropel, instructions for use: method and dosage
Ketopropel tablets are taken orally, during or after a meal, swallowing whole and washed down with water (milk can be used) in a volume of at least ½ cup.
Recommended dosage: 1 pc. twice a day.
Oral (oral) ketoprofen preparations can be combined with rectal suppositories. So, in the morning, the patient can take 1 tablet (100 mg of ketoprofen) Ketoprofen, and in the evening - enter 1 suppository (100 mg of ketoprofen) rectally.
The maximum dose of ketoprofen, equal to 200 mg per day, should not be exceeded.
To reduce the risk of developing adverse reactions from the gastrointestinal tract, patients with risk factors are prescribed proton pump inhibitors (PPIs) simultaneously with ketoprofen.
Side effects
Adverse reactions are classified as follows: very often - more than 1/10; often - more than 1/100, but less than 1/10; infrequently - more than 1/1000, but less than 1/100; rarely - more than 1/10 000, but less than 1/1000; extremely rare - less than 1/10 000, including single messages; with an unknown frequency - it is impossible to determine the incidence of adverse reactions based on the available data.
Taking Ketopropel tablets can lead to the development of the following undesirable phenomena on the part of systems and organs:
- immune system: with an unknown frequency - anaphylactic reactions (including anaphylactic shock);
- blood and lymphatic system: rarely - hemorrhagic anemia; with an unknown frequency - dysfunction of the bone marrow, thrombocytopenia, agranulocytosis;
- CNS: infrequently - drowsiness, dizziness, headache; rarely - paresthesia; with an unknown frequency - violation of taste sensations, convulsions;
- psyche: with an unknown frequency - emotional lability;
- heart: with an unknown frequency - heart failure;
- vessels: with an unknown frequency - vasodilation, increased blood pressure (BP);
- respiratory system, chest and mediastinal organs: rarely - exacerbation of bronchial asthma; with an unknown frequency - rhinitis, bronchospasm (especially in patients with hypersensitivity to NSAIDs);
- skin and subcutaneous tissue: infrequently - itching / rash; with unknown frequency - bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), erythema, urticaria, alopecia, photosensitivity, angioedema;
- digestive tract: often - abdominal pain, nausea / vomiting, dyspepsia; infrequently - gastritis, bloating, diarrhea / constipation; rarely - stomatitis, peptic ulcer; extremely rare - perforation, bleeding from the gastrointestinal tract, exacerbation of NUC or Crohn's disease;
- liver and biliary tract: rarely - increased concentration of bilirubin, hepatitis, increased activity of hepatic transaminases;
- kidneys and urinary tract: with an unknown frequency - abnormal values of indicators of renal function, acute renal failure, nephrotic syndrome, interstitial nephritis, nephritic syndrome;
- organ of hearing and labyrinthine disorders: rarely - tinnitus;
- organ of vision: rarely - blurred vision;
- general disorders and disorders at the injection site: infrequently - edema; rarely - an increase in body weight; with an unknown frequency - increased fatigue.
Overdose
Symptoms of an overdose of ketoprofen, like other NSAIDs, can be manifested by abdominal pain, nausea, vomiting (including blood), chalk, convulsions, respiratory depression, impaired consciousness, impaired renal function and renal failure.
Treatment for overdose is symptomatic. First of all, gastric lavage is carried out and the intake of adsorbing agents (for example, activated carbon) is prescribed. The effects of ketoprofen on the digestive tract can be weakened by drugs that reduce gastric gland secretion, such as PPIs and prostaglandins.
special instructions
It is not recommended to take Ketopropel with other NSAIDs and / or cyclooxygenase-2 inhibitors.
With prolonged use of NSAIDs, regular monitoring of renal / liver function is necessary, especially in elderly patients (from 65 years), an assessment of a clinical blood test, an analysis of feces for occult blood.
When treating Ketoprovel patients with arterial hypertension, cardiovascular diseases that contribute to fluid retention in the body, caution should be exercised and blood pressure should be monitored more often.
If the patient has visual disturbances, drug therapy is immediately stopped.
Ketoprofen, like other NSAIDs, is able to mask the symptoms of infectious and inflammatory diseases. If you find signs of infection or a deterioration in health while using Ketopropel, you should immediately seek medical help.
If in the patient's history there is information about the presence of contraindications from the gastrointestinal tract (peptic ulcer, perforation, bleeding), therapy with Ketoprovel should be accompanied by careful supervision of a specialist. Such monitoring by a physician is required when using high doses of ketoprofen and during long-term therapy.
Prostaglandins play an important role in maintaining renal blood flow, therefore, when using ketoprofen, special care should be taken in the following categories: patients with heart or renal failure, elderly patients taking diuretics, patients who have a decrease in BCC (regardless of the cause of this phenomenon).
Before major surgical intervention, the use of Ketopropel should be discontinued.
Ketoprofen is capable of affecting female fertility, and therefore, the drug is not recommended for patients suffering from infertility (including women undergoing examination).
Influence on the ability to drive vehicles and complex mechanisms
There are no data on the negative effect of ketoprofen on the ability to drive vehicles or work with complex mechanisms, provided that it is used in recommended doses. However, it should be taken into account that dizziness, drowsiness, other adverse effects from the central nervous system, and visual impairment may occur against the background of Ketopropel therapy. With the development of such symptoms, patients should refuse to drive a car or any other means of transport, as well as engage in potentially hazardous activities that require quick psychomotor reactions and increased concentration of attention.
Application during pregnancy and lactation
Inhibition of prostaglandin synthesis can adversely affect the course of pregnancy and / or fetal development. Data obtained from epidemiological studies on the use of inhibitors of prostaglandin synthesis in early pregnancy indicate an increased risk of developing heart defects in the fetus (approximately 1-1.5%) and spontaneous abortion. The use of Ketopropel in the third trimester of pregnancy is contraindicated for a number of reasons, including a possible increase in bleeding time, premature closure of the ductus arteriosus and / or the development of weakness in labor activity of the uterus, renal failure and oligohydramnios.
In the first and second trimesters of pregnancy, the use of ketoprofen is allowed only if the potential benefits to the mother exceed the possible risks to the fetus.
There are currently no data on the excretion of ketoprofen into breast milk. If it is necessary to use Ketopropel during lactation, it is necessary to resolve the issue of stopping breastfeeding.
Pediatric use
Children and adolescents under 15 years of age are contraindicated to take Ketopropel tablets.
With impaired renal function
Patients with progressive kidney disease and severe renal failure (CC <30 ml / min) are contraindicated in taking the drug.
In case of moderate renal failure (CC from 30 to 60 ml / min), Ketopropel should be taken with caution.
For violations of liver function
The drug is contraindicated in patients with active liver disease and severe hepatic insufficiency.
With liver failure, progressive liver disease, alcoholic cirrhosis of the liver, hyperbilirubinemia, Ketopropel should be taken with caution.
Use in the elderly
Elderly patients should take Ketopropel with caution, especially with concomitant use of diuretics.
Drug interactions
- diuretics and antihypertensive drugs: Ketopropel can weaken their effect;
- phenytoin and some other anticonvulsants, hypoglycemic drugs for oral administration: ketoprofen may enhance their effect;
- other NSAIDs, salicylates, glucocorticosteroids (GCS), ethanol: when taken together with the drug, the risk of developing adverse reactions from the gastrointestinal tract increases;
- pentoxifylline, thrombolytics, antiplatelet agents (for example, clopidogrel, ticlopidine), anticoagulants (for example, warfarin, heparin): combined use with ketoprofen increases the risk of bleeding;
- cyclosporine, tacrolimus, trimethoprim, potassium-sparing diuretics, potassium salts, low molecular weight heparins, angiotensin-converting enzyme (ACE) inhibitors, NSAIDs: increase the risk of hyperkalemia;
- blockers of slow calcium channels (BMCC), cyclosporin, digoxin, methotrexate, cardiac glycosides, lithium preparations: Ketopropel increases the concentration of these agents in the blood plasma; increases the nephrotoxicity of cyclosporine and the toxicity of methotrexate;
- probenecid: while taking ketoprofen plasma clearance is significantly reduced;
- glucocorticosteroids and other NSAIDs (including selective inhibitors of cyclooxygenase-2): the likelihood of side effects (in particular, from the gastrointestinal tract) increases;
- mifepristone: NSAIDs can reduce the effectiveness of mifepristone, so they should be taken no earlier than 8-12 days after discontinuation.
Analogs
Arketal Rompharm, Artrum, Artrozilen, Bystrumgel, Bystrum Forte, Bystrum caps, VALUSAL, Ketonal, Ketonal UNO, Ketonal Aktiv, Ketonal Aktiv Plus, Ketonal DUO, Ketoprofen, Ketoprofen Organika, Ketoprofen-Ketoprofen-Ketoprofen-Solofen, Ketoprofen-Lekpharm, Spazgel, OKI, Pentalgin extra-gel, Flamax Forte, Flamax, Febrofid, Fastum, Flexen, etc.
Terms and conditions of storage
Keep out of the reach of children. Store in a dark place at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ketoprovel
On the Internet, there are no reviews about Ketopropel. However, there are many reports of drugs whose active ingredient is ketoprofen. The funds are responded positively, noting their rapid analgesic effect, convenient dosing regimen and affordable cost.
Some reviews contain information about the insufficient effect of Ketopropel in diseases with pronounced edematous pain syndrome, such as radiculopathy. In addition, the disadvantages are the presence of a large list of side effects and the lack of the possibility of use in children.
Price for Ketopropel in pharmacies
The price of Ketopropel, film-coated tablets, 100 mg, in pharmacy chains is 108–120 rubles. per pack of 20
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
