Lek d.d./Novartis Neva LLC, Slovenia, 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 - ankylosing spondylitis, psoriatic arthritis, reactive arthritis (Reiter's syndrome); gout, pseudogout; osteoarthritis; - pain syndrome: headache; tendonitis, bursitis, myalgia, neuralgia, radiculitis; post-traumatic and postoperative pain syndrome; pain syndrome in cancer; algodismenorrhea.
Symptomatic treatment of painful and inflammatory processes of various origins, including: inflammatory and degenerative diseases of the musculoskeletal system: - rheumatoid arthritis; - seronegative arthritis (ankylosing spondylitis / Bechterew's disease /, psoriatic arthritis, reactive arthritis / Reiter's syndrome/); - gout, pseudogout; - osteoarthritis. pain syndrome: - headache; - tendinitis, bursitis, myalgia, neuralgia, radiculitis; - post-traumatic and postoperative pain syndrome; - pain syndrome in oncological diseases; - algodismenorrhea.
Inside. The standard dose of Ketonal-Duo for adults and children over 15 years of age is 150 mg/day (1 modified-release capsule). Capsules should be taken during or after meals with water or milk (the volume of liquid must be at least 100 ml). The maximum dose of ketoprofen is 200 mg/day.
Hypersensitivity to ketoprofen or other components of the drug, as well as salicylates, tiaprofenic acid or other NSAIDs; - complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history); - erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; - ulcerative colitis, Crohn's disease; - hemophilia and other bleeding disorders; - severe liver failure; - active liver disease; - severe renal failure (creatinine clearance less than 30 ml/min); - progressive kidney diseases; - decompensated heart failure; - postoperative period after coronary artery bypass grafting; - gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding); - diverticulitis; - inflammatory bowel diseases; - confirmed hyperkalemia; - chronic dyspepsia; - children under 15 years of age; - III trimester of pregnancy; - period of breastfeeding; - lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome. The drug should be prescribed with caution if there is a history of peptic ulcer disease, a history of bronchial asthma, clinically significant cardiovascular, cerebrovascular diseases and peripheral arterial diseases, dyslipidemia, progressive liver diseases, liver failure, hyperbilirubinemia, alcoholic cirrhosis of the liver, renal failure (QC 30- 60 ml/min), chronic heart failure, arterial hypertension, blood diseases, dehydration, diabetes mellitus, medical history of the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, severe somatic diseases, smoking, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid), oral corticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, sertraline), long-term use of NSAIDs, elderly patients (including those taking diuretics), patients with reduced blood volume .
Instructions for medical use of the drug
Description of pharmacological action
Indications for use
Rheumatoid arthritis;
- seronegative spondyloarthritis (including ankylosing spondylitis, psoriatic arthritis, reactive arthritis);
- gout, pseudogout;
- arthrosis;
- extra-articular rheumatism (including tendinitis, bursitis, capsulitis of the shoulder joint);
- pain syndrome (including post-traumatic, post-operative, algodismenorrhea, with bone metastases in patients with cancer).
Release form
modified release capsules 150 mg; blister 10, cardboard pack 2;
modified release capsules 150 mg; blister 10, cardboard pack 3;
Compound
Modified release capsules 1 cap.
pellet core
active substance:
ketoprofen 150 mg
excipients: MCC; lactose monohydrate; povidone; croscarmellose sodium; polysorbate 80
pellet shell: Eudragit RS 30D (ethyl acrylate, methyl methacrylate and trimethylammonioethyl methacrylate copolymer); Eudragit RL 30D (ethyl acrylate, methyl methacrylate and trimethylammonioethyl methacrylate copolymer); triethyl citrate; polysorbate 80; talc; iron (III) oxide yellow (E172); colloidal silicon dioxide
capsule shell composition: gelatin; indigo carmine (E132); titanium dioxide (E171)
blister contains 10 capsules; There are 2 or 3 blisters in a cardboard pack.
Pharmacodynamics
NSAIDs. It has a pronounced analgesic and anti-inflammatory effect.
The mechanism of action of Ketonal DUO is associated with inhibition of the biosynthesis of prostaglandins and leukotrienes by suppressing the activity of COX-1 and COX-2, which catalyze the synthesis of prostaglandins from arachidonic acid. Ketoprofen stabilizes lysosome membranes and has anti-bradykinin activity.
Pharmacokinetics
Ketonal DUO capsules contain two types of pellets: standard (white) and coated (yellow). Ketoprofen is quickly released from white pellets (60% of the total amount) and slowly from yellow pellets (40% of the total amount), which allows you to combine fast and prolonged action. The effect begins to appear 20 minutes after taking the drug.
Suction
The drug is well absorbed from the gastrointestinal tract and its bioavailability when taken orally is 90%. Food intake does not affect overall bioavailability, but reduces the rate of absorption.
After oral administration of ketoprofen at a dose of 150 mg, Tmax is 1.76 hours.
Distribution
Binding to blood proteins (mainly to the albumin fraction) - 99%. Vd is 0.1-0.2 l/kg. Ketoprofen penetrates into the synovial fluid and reaches a concentration there equal to 50% of the plasma concentration (1.5 mcg/ml).
Metabolism
Ketoprofen is metabolized in the liver.
Removal
T1/2 of ketoprofen (from white pellets) is 2 hours. About 60-75% of ketoprofen is excreted in the urine, mainly in the form of a conjugate with glucuronic acid, less than 10% is excreted in feces.
Thanks to the modified release of the active substance from yellow pellets coated with a special enteric coating, the duration of the effect of Ketonal DUO reaches 18-20 hours, which allows you to take the drug 1 time.
Use during pregnancy
The use of the drug during pregnancy and breastfeeding is contraindicated.
Use for renal impairment
The use of the drug is contraindicated in cases of severe renal dysfunction.
Other special occasions at reception
The use of the drug is contraindicated in cases of severe liver dysfunction.
Contraindications for use
Gastrointestinal diseases in the acute phase (gastritis, gastric ulcer);
- severe liver dysfunction;
- severe renal dysfunction;
- disorders of the hematopoietic system (including leukopenia, thrombocytopenia, hemocoagulation disorders);
- pregnancy;
- lactation period (breastfeeding);
- children under 15 years of age;
- hypersensitivity to ketoprofen, acetylsalicylic acid or other NSAIDs (history of bronchospasm, urticaria or rhinitis associated with taking acetylsalicylic acid).
Side effects
From the digestive system: often - loss of appetite, nausea, vomiting (including blood), flatulence, abdominal pain, constipation, diarrhea (such undesirable effects can be avoided by taking the drug after meals); very rarely - liver dysfunction.
From the side of the central nervous system: rarely - headache, dizziness, drowsiness, depression, insomnia, nervousness; very rarely - visual disturbances, tinnitus.
Allergic reactions: rarely - skin rashes, anaphylactic shock, bronchospasm, attack of bronchial asthma.
From the hematopoietic system: very rarely - agranulocytosis, thrombocytopenia, anemia.
Other: rarely - peripheral edema; very rarely - renal dysfunction.
As a rule, unwanted side effects are mild.
Directions for use and doses
The standard dose of Ketonal® DUO for adults and children over 15 years of age is 150 mg/day (1 modified-release capsule). Capsules should be taken during or after meals with water or milk (the volume of liquid must be at least 100 ml).
The maximum dose of ketoprofen is 200 mg/day.
Overdose
Symptoms: nausea, vomiting (including blood), abdominal pain, black feces, impaired consciousness, respiratory depression, convulsions, impaired renal and hepatic function.
Treatment: gastric lavage, use of activated charcoal, symptomatic treatment - weakening the effects of ketoprofen using histamine H2 receptor blockers, proton pump inhibitors and prostaglandins. There is no specific antidote.
Interactions with other drugs
Ketoprofen may weaken the effect of diuretics and antihypertensive drugs and enhance the effect of oral hypoglycemic and some anticonvulsants (phenytoin).
Combined use with other NSAIDs, salicylates, corticosteroids, ethanol increases the risk of developing adverse events from the gastrointestinal tract. Simultaneous administration with anticoagulants, thrombolytics, and antiplatelet agents increases the risk of bleeding.
When taking NSAIDs concomitantly with diuretics or ACE inhibitors, the risk of renal dysfunction increases. Increases plasma concentrations of cardiac glycosides, CCBs, lithium preparations, cyclosporine, methotrexate.
NSAIDs may reduce the effectiveness of mifepristone. NSAIDs should be started no earlier than 8–12 days after mifepristone is discontinued.
Special instructions for use
With long-term use of NSAIDs, it is necessary to monitor the state of the blood, as well as the functional state of the kidneys and liver, especially in elderly patients (over 65 years of age).
It is necessary to be careful and monitor blood pressure more often when using ketoprofen to treat patients suffering from hypertension and cardiovascular diseases, which lead to fluid retention in the body. Like other NSAIDs, ketoprofen can mask signs of infectious diseases.
Effect on ability to concentrate
There is no data on the negative effect of Ketonal® DUO at recommended doses on the ability to drive a car or operate machinery. At the same time, patients who notice unusual effects when taking Ketonal® DUO should be careful when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Storage conditions
List B: In a place protected from light, at a temperature not exceeding 25 °C.
Best before date
ATX classification:
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Excipients: microcrystalline cellulose - 34 mg, lactose monohydrate - 20 mg, - 5 mg, croscarmellose sodium - 10 mg, polysorbate 80 - 1 mg.
Composition of pellet shell 1: Eudragit RS 30D (copolymer of ethyl acrylate, methyl methacrylate and trimethylammonioethyl methacrylate) - 4.908 mg, Eudragit RL 30D (copolymer of ethyl acrylate, methyl methacrylate and trimethylammonioethyl methacrylate) - 4.908 mg, triethyl citrate - 0.88 mg, polysorbate 80 - 0.0 08 mg, talc - 1.76 mg, iron (III) yellow oxide (E172) - 0.08 mg, talc 2 - 0.2 mg, colloidal silicon dioxide 2 - 0.2 mg.
Composition of capsule shell 1L970/53.051: gelatin - up to 100%, (E132) - 0.4%, titanium dioxide (E171) - 0.9%.
1 in a capsule only 40% of the pellets are coated;
2 the amount of talc (0.2 mg) colloidal silicon dioxide is not taken into account when calculating the mass of the capsule contents.
10 pieces. - blisters (1) - cardboard packs.
10 pieces. - blisters (2) - cardboard packs.
10 pieces. - blisters (3) - cardboard packs.
pharmachologic effect
NSAID, propionic acid derivative. It has analgesic, anti-inflammatory and antipyretic effects. Ketoprofen blocks the action of the enzyme COX-1 and COX-2 and partially lipoxygenase, which leads to suppression of prostaglandin synthesis (including in the central nervous system, most likely in the hypothalamus).
Stabilizes lysosomal membranes in vitro and in vivo; at high concentrations in vitro, ketoprofen suppresses the synthesis of bradykinin and leukotrienes.
Ketoprofen does not have a negative effect on the condition of articular cartilage.
Pharmacokinetics
Suction
Duo is a new dosage form that differs from conventional capsules in the way it releases the active substance. Modified release capsules contain two types of pellets: white (about 60% of the total) and yellow (coated). Ketoprofen is released quickly from white pellets and slowly from yellow ones, which results in a combination of fast and prolonged action.
The drug is well absorbed after oral administration.
The bioavailability of ketoprofen in the form of regular and modified-release capsules is 90%.
Food intake does not affect the overall bioavailability (AUC) of ketoprofen, but reduces the rate of absorption. After oral administration of ketoprofen at a dose of 150 mg in the form of capsules with modified release, C max in the blood is 9036.64 ng/ml for 1.76 hours.
Distribution
The binding of ketoprofen to plasma proteins (mainly albumin) is 99%. V d - 0.1-0.2 l/kg. Ketoprofen penetrates well into the synovial fluid, where it reaches 30% of the plasma concentration. Significant concentrations of ketoprofen in the synovial fluid are stable and persist for up to 30 hours, resulting in a long-term reduction in pain and joint stiffness.
Metabolism and excretion
Ketoprofen undergoes intensive metabolism with the participation of microsomal liver enzymes. It binds to glucuronic acid and is excreted as a glucuronide. There are no active metabolites of ketoprofen. T 1/2 - less than 2 hours.
Approximately 80% of ketoprofen is excreted in the urine, mainly as ketoprofen glucuronide. About 10% is excreted through the intestines.
When using ketoprofen in a dose of 100 mg or more, excretion by the kidneys may be difficult.
Pharmacokinetics in special clinical situations
In patients with severe renal impairment, most of the drug is excreted through the intestines. When taken in high doses, hepatic clearance is also increased. Up to 40% of the drug is excreted through the intestines.
In patients with liver failure, the plasma concentration of ketoprofen is increased by 2 times (probably due to hypoalbuminemia and, as a result, a high level of unbound active ketoprofen); such patients must be prescribed the drug in a minimum therapeutic dose.
In patients with renal failure, the clearance of ketoprofen is reduced, but dose adjustment is required only in cases of severe renal failure.
In elderly patients, the metabolism and elimination of ketoprofen is slower, which is of clinical significance only for patients with severe renal impairment.
Indications
Symptomatic treatment of painful and inflammatory processes of various origins, including:
inflammatory and degenerative diseases of the musculoskeletal system:
- rheumatoid arthritis;
- seronegative arthritis (ankylosing spondylitis / Bechterew's disease /, psoriatic arthritis, reactive arthritis / Reiter's syndrome/);
- gout, pseudogout;
- osteoarthritis.
pain syndrome:
- headache;
- tendonitis, bursitis, myalgia, neuralgia, radiculitis;
- post-traumatic and postoperative pain syndrome;
- pain syndrome in cancer;
- algodismenorrhea.
Contraindications
- hypersensitivity to ketoprofen or other components of the drug, as well as salicylates, tiaprofenic acid or other NSAIDs;
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance or other NSAIDs (including a history);
- erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
- ulcerative colitis, Crohn's disease;
- hemophilia and other bleeding disorders;
- severe liver failure;
- active liver disease;
- severe renal failure (creatinine clearance less than 30 ml/min);
- progressive kidney disease;
- decompensated failure;
- postoperative period after coronary artery bypass surgery;
- gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding);
- diverticulitis;
- inflammatory bowel diseases;
- confirmed hyperkalemia;
- chronic dyspepsia;
- children under 15 years of age;
- III trimester of pregnancy;
- breastfeeding period;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.
Carefully the drug should be prescribed for a history of peptic ulcer disease, a history of bronchial asthma, clinically pronounced cardiovascular, cerebrovascular diseases and peripheral arterial diseases, dyslipidemia, progressive liver diseases, liver failure, hyperbilirubinemia, alcoholic cirrhosis of the liver, renal failure (CC 30-60 ml /min), chronic heart failure, arterial hypertension, blood diseases, dehydration, diabetes mellitus, anamnesis data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, severe somatic diseases, smoking, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents ( for example, acetylsalicylic acid), oral corticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, sertraline), long-term use of NSAIDs, elderly patients (including those taking diuretics), patients with reduced blood volume.
Dosage
Inside. Standard dose of Ketonal Duo for adults and children over 15 years old is 150 mg/day (1 modified-release capsule). Capsules should be taken during or after meals with water or milk (the volume of liquid must be at least 100 ml).
The maximum dose of ketoprofen is 200 mg/day.
Side effects
Determination of frequency categories of adverse effects (according to WHO): very often (≥1/10), often (≥1/100,<1/10), нечасто (≥1/1000, <1/100), редко (≥10 000, <1/1000), очень редко (<1/10 000), частота неизвестна (частоту возникновения нежелательных эффектов невозможно определить на основании имеющихся данных).
From the blood and lymphatic system: rarely - hemorrhagic anemia, purpura; frequency unknown - agranulocytosis, thrombocytopenia, impaired bone marrow hematopoiesis.
From the immune system: frequency unknown - anaphylactic reactions (including anaphylactic shock).
From the nervous system: infrequently - headache, dizziness, drowsiness; rarely - paresthesia; frequency unknown - convulsions, taste disturbances, emotional lability.
From the senses: rarely - blurred vision, tinnitus.
From the cardiovascular system: frequency unknown - heart failure, increased blood pressure, vasodilation.
From the respiratory system: rarely - exacerbation of bronchial asthma; frequency unknown - bronchospasm (especially in patients with established hypersensitivity to NSAIDs), rhinitis.
From the gastrointestinal tract: often - nausea, vomiting, dyspepsia, abdominal pain; uncommon - constipation, diarrhea, bloating, gastritis; rarely - peptic ulcer, stomatitis; very rarely - exacerbation of ulcerative colitis or Crohn's disease, gastrointestinal bleeding and perforation.
From the liver and biliary tract: rarely - hepatitis, increased levels of liver transaminases and bilirubin.
For the skin and subcutaneous tissues: uncommon - skin rash, itching; frequency unknown - photosensitivity, alopecia, urticaria, angioedema, erythema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the urinary system: very rarely - acute renal failure, interstitial nephritis, nephritic syndrome, nephrotic syndrome, abnormal values of renal function indicators.
Other: infrequently - swelling, fatigue; rarely - weight gain; frequency unknown - increased fatigue.
Overdose
Symptoms: As with other NSAIDs, an overdose of ketoprofen may cause nausea, vomiting, abdominal pain, hematemesis, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function and renal failure.
Treatment: in case of overdose, gastric lavage and the use of activated carbon are indicated. Carrying out symptomatic therapy. The effect of ketoprofen on the gastrointestinal tract can be weakened with the help of drugs that reduce the secretion of gastric glands (for example, proton pump inhibitors) and prostaglandins. In case of development of renal failure, hemodialysis is recommended.
Drug interactions
Ketoprofen may weaken the effect diuretics and antihypertensive drugs and enhance the effect oral hypoglycemic and some anticonvulsants(phenytoin).
Sharing with others NSAIDs, salicylates, corticosteroids, ethanol increases the risk of developing adverse events from the gastrointestinal tract.
Simultaneous use with anticoagulants(heparin, warfarin), thrombolytics, antiplatelet agents(ticlopidine, clopidogrel) increases the risk of bleeding.
Simultaneous use with potassium salts, potassium-sparing diuretics, ACE inhibitors, NSAIDs, low molecular weight heparins, cyclosporine, tacrolimus And trimethoprim increases the risk of developing hyperkalemia.
Increases plasma concentration cardiac glycosides (including digoxin), slow calcium channel blockers, lithium preparations, cyclosporine, methotrexate.
Increases toxicity methotrexate and nephrotoxicity cyclosporine.
Simultaneous use with probenecid significantly reduces the clearance of ketoprofen in blood plasma.
Combined use with GKS And other NSAIDs(including selective COX-2 inhibitors) increases the likelihood of adverse reactions (in particular, from the gastrointestinal tract).
NSAIDs may reduce effectiveness mifepristone. Taking NSAIDs should be started no earlier than 8-12 days after stopping mifepristone.
special instructions
With long-term use of NSAIDs, it is necessary to monitor the blood condition, as well as kidney and liver function, especially in elderly patients (over 65 years of age).
It is necessary to be careful and monitor blood pressure more often when using ketoprofen to treat patients with arterial hypertension and cardiovascular diseases that lead to fluid retention in the body.
Like other NSAIDs, ketoprofen can mask signs of infectious diseases.
Impact on the ability to drive vehicles and operate machinery
There is no data on the negative effect of Ketonal Duo in recommended doses on the ability to drive a car or operate machinery. At the same time, patients who notice unusual effects when taking Ketonal Duo should be careful when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Pregnancy and lactation
Inhibition of prostaglandin synthesis may have undesirable effects on pregnancy and/or embryonic development. Data obtained from 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%).
Prescribing the drug to pregnant women in the first and second trimesters of pregnancy is possible only when the benefits for the mother justify the possible risk to the fetus.
The use of ketoprofen in pregnant women during the third trimester of pregnancy is contraindicated due to the possibility of developing weakness of labor in the uterus and/or premature closure of the ductus arteriosus, a possible increase in bleeding time, oligohydramnios and renal failure.
To date, there is no data on the excretion of ketoprofen in breast milk, therefore, if it is necessary to use ketoprofen in a nursing mother, the issue of stopping breastfeeding should be addressed.
Use in childhood
Contraindicated in children and adolescents under 15 years of age.
Instructions for use Ketonal Duo
Buy Ketonal Duo caps 150mg
Dosage forms
modified release capsules 150 mg
Manufacturers
Lek d.d. (Slovenia)
Group
Anti-inflammatory drugs - propionic acid derivatives
Compound
The active substance is ketoprofen.
International nonproprietary name
Ketoprofen
Synonyms
Arketal Rompharm, Artrosilene, Artrum, Bystrumgel, Bystrumcaps, Valusal, Ketonal, Ketoprofen, Ketoprofen MV, Ketoprofen Organica, Ketoprofen-Verte, Ketoprofen-Vramed, Oki, Fastum, Febrofid, Flamax, Flamax forte, Flexen
pharmachologic effect
Anti-inflammatory, analgesic, antipyretic, antiaggregant. It has anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to tissue destruction during chronic inflammation. When administered orally, it is absorbed quite completely. Absorption is accompanied by a “first pass” effect through the liver. The concentration in the blood is dose-dependent. Easily passes through histohematic barriers and is distributed in tissues and organs. Biotransforms in the liver (almost completely). Metabolites are excreted in the urine. Reduces morning stiffness and swelling of joints, increases range of motion.
Indications for use
Rheumatoid arthritis, nonspecific spondylitis (ankylosing and psoriatic spondylitis), pain syndrome (postoperative, post-traumatic pain, pain with bone metastases), gouty arthritis, pseudogout, osteoarthritis, extra-articular rheumatism (tenosynovitis, bursitis, capsulitis), renal colic, algodismenorrhea. Gel - uncomplicated injuries (sprains and ruptures of tendons and ligaments, muscle bruises, swelling).
Contraindications
Hypersensitivity, renal and liver failure, peptic ulcer of the stomach and duodenum in the acute phase, "aspirin" asthma, pregnancy and childhood. Candles - proctitis and proctorragia; Gel - dermatoses, eczema, infected abrasions and wounds (wetting).
Side effect
Headache, dizziness, tinnitus, drowsiness, weakness, visual disturbances, dyspeptic symptoms (nausea, vomiting, abdominal pain, diarrhea, flatulence, constipation, anorexia), stomatitis, impaired renal and liver function, hyperemia, allergic reactions.
Interaction
Increases the toxicity of methotrexate. The concentration of ketoprofen in plasma increases against the background of probenecid (inhibits renal excretion). Enhances the effect of anticoagulants, heparin, ticlopidine, corticosteroids, oral antidiabetic agents and alcohol, weakens the effect of spironolactone, peripheral vasodilators.
Overdose
No data.
special instructions
Taking ketoprofen can mask the signs of an infectious disease. If renal or liver function is impaired, dose reduction and careful monitoring are necessary. Do not allow the gel to come into contact with mucous membranes or eyes. Use with caution while working for vehicle drivers and people whose profession involves increased concentration. During treatment you should stop drinking alcoholic beverages. In patients with bronchial asthma or allergic diathesis, the use of Ketoprofen may cause bronchospasm.
Storage conditions
List B. At room temperature in a dry place, protected from light and out of reach of children.
M54.1 Radiculopathy M54.3 Sciatica M54.4 Lumbago with sciatica M65 Synovitis and tenosynovitis M70 Diseases of soft tissues associated with stress, overload and pressure M71 Other bursopathies M79.1 Myalgia M79.2 Neuralgia and neuritis, unspecified N94.4 Primary dysmenorrhea N94 .5 Secondary dysmenorrhea R51 Headache R52.0 Acute pain R52.2 Other persistent pain T14.3 Dislocation, sprain and strain of the capsular ligamentous apparatus of a joint of an unspecified area of the body
Pharmacological group
pharmachologic effect
Non-steroidal anti-inflammatory drug (NSAID). It has analgesic, anti-inflammatory and antipyretic effects.
Due to the inhibition of COX-1 and COX-2, and partially lipoxygenase, ketoprofen suppresses the synthesis of prostaglandins and bradykinin, stabilizes lysosomal membranes.
Ketoprofen does not have a negative effect on articular cartilage.
Pharmacokinetics
Suction
Ketonal ® Duo capsules are presented in a new dosage form, which differs from conventional capsules in the special release of the active substance. The capsules contain two types of pellets: white (about 60% of the total) and yellow (coated). Ketoprofen is released quickly from white pellets and slowly from yellow ones, which results in a combination of fast and prolonged action.
The drug is well absorbed after oral administration.
The bioavailability of ketoprofen in the form of regular and modified-release capsules is 90%.
Food intake does not affect the overall bioavailability (AUC) of ketoprofen, but reduces the rate of absorption. After oral administration of ketoprofen at a dose of 150 mg in the form of modified-release capsules, Cmax in blood plasma is 9036.64 ng/ml for 1.76 hours.
Distribution
The binding of ketoprofen to plasma proteins (mainly albumin) is 99%. V d - 0.1-0.2 l/kg. Ketoprofen penetrates well into the synovial fluid, where it reaches 30% of the plasma concentration. Significant concentrations of ketoprofen in the synovial fluid are stable and persist for up to 30 hours, resulting in a long-term reduction in pain and joint stiffness.
Metabolism and excretion
Ketoprofen undergoes intensive metabolism with the participation of microsomal liver enzymes. It binds to glucuronic acid and is excreted as a glucuronide. There are no active metabolites of ketoprofen. T 1/2 - less than 2 hours.
Approximately 80% of ketoprofen is excreted in the urine, mainly in the form of ketoprofen glucuronide (more than 90%). About 10% is excreted through the intestines.
Pharmacokinetics in special clinical situations
In patients with liver failure, the plasma concentration of ketoprofen is increased by 2 times (probably due to hypoalbuminemia and the resulting high level of unbound active ketoprofen); such patients must be prescribed the drug in a minimum therapeutic dose.
In patients with renal failure, the clearance of ketoprofen is reduced, which requires dose adjustment.
In elderly patients, the metabolism and excretion of ketoprofen is slow, but this is of clinical significance only for patients with reduced renal function.
Symptomatic treatment of painful and inflammatory processes of various origins, including:
inflammatory and degenerative diseases of the musculoskeletal system:
Rheumatoid arthritis;
Seronegative arthritis (ankylosing spondylitis / Bechterew's disease /, psoriatic arthritis, reactive arthritis / Reiter's syndrome/);
Gout, pseudogout;
Osteoarthritis.
pain syndrome:
Headache;
Tendinitis, bursitis, myalgia, neuralgia, radiculitis;
Post-traumatic pain;
Postoperative pain;
Algodismenorrhea;
Pain syndrome in cancer.
Bronchial asthma, rhinitis, urticaria in history caused by taking acetylsalicylic acid or other NSAIDs;
Peptic ulcer of the stomach and duodenum in the acute phase;
UC, Crohn's disease in the acute phase, inflammatory bowel diseases in the acute phase;
Hemophilia and other bleeding disorders;
Severe liver failure;
Severe renal failure;
Progressive kidney diseases;
Decompensated heart failure;
Postoperative period after coronary artery bypass surgery;
Gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding);
Chronic dyspepsia;
Children under 15 years of age;
III trimester of pregnancy;
Lactation period (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 pronounced cardiovascular, cerebrovascular diseases and peripheral arterial diseases, dyslipidemia, progressive liver diseases, hyperbilirubinemia, alcoholism, renal failure, chronic heart failure, arterial hypertension, blood diseases, dehydration, diabetes mellitus, history of development of gastrointestinal ulcers, smoking, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid), oral corticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, sertraline), long-term use of NSAIDs.
The incidence of side effects is characterized as very common (>10%), common (>1%<10%), нераспространенные (>0.1% <1%), редкие (>0.01% < 0.1%) и очень редкие (< 0.01%).
From the digestive system: common - dyspepsia (nausea, diarrhea or constipation, flatulence, vomiting, decreased or increased appetite), abdominal pain, stomatitis, dry mouth; uncommon (with long-term use in large doses) - ulceration of the gastrointestinal mucosa, impaired liver function; rare - perforation of the gastrointestinal tract, exacerbation of Crohn's disease, melena, gastrointestinal bleeding, transient increase in the level of liver enzymes.
From the side of the central nervous system: common - headache, dizziness, sleep disturbance, fatigue, nervousness, nightmares; rare - migraine, peripheral polyneuropathy; very rare - hallucinations, disorientation and speech disorder.
From the senses: rare - tinnitus, change in taste, blurred vision, conjunctivitis.
From the cardiovascular system: uncommon - tachycardia, arterial hypertension, peripheral edema.
From the hematopoietic system: decreased platelet aggregation; rare - anemia, thrombocytopenia, agranulocytosis, purpura.
From the urinary system: rare - renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria (more often develops in people taking NSAIDs and diuretics for a long time).
Allergic reactions: common - skin reactions (itching, urticaria); uncommon - rhinitis, shortness of breath, bronchospasm, angioedema, anaphylactoid reactions.
Others: rare - hemoptysis, menometrorrhagia.
Overdose
Symptoms: nausea, vomiting, abdominal pain, hematemesis, melena, impaired consciousness, respiratory depression, convulsions, renal dysfunction and renal failure.
Treatment: in case of overdose, gastric lavage and the use of activated carbon are indicated. Symptomatic therapy is carried out. The effect of ketoprofen on the gastrointestinal tract can be weakened with the help of histamine H2 receptor blockers, proton pump inhibitors and prostaglandins.
special instructions
With long-term use of NSAIDs, it is necessary to monitor the blood condition, as well as kidney and liver function, especially in elderly patients (over 65 years of age).
It is necessary to be careful and monitor blood pressure more often when using ketoprofen to treat patients with arterial hypertension and cardiovascular diseases that lead to fluid retention in the body.
Like other NSAIDs, ketoprofen can mask signs of infectious diseases.
Impact on the ability to drive vehicles and operate machinery
There is no data on the negative effect of Ketonal ® Duo in recommended doses on the ability to drive a car or operate machinery. At the same time, patients who notice unusual effects when taking Ketonal ® Duo should be careful when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
For renal failure
The drug is contraindicated in cases of severe renal failure.
In case of liver dysfunction
The drug is contraindicated in cases of severe liver failure.
Use during pregnancy and breastfeeding
The use of ketoprofen in the third trimester of pregnancy is contraindicated. In the first and second trimesters of pregnancy, the drug can be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus.
When taking the drug during lactation, the issue of stopping breastfeeding should be decided.
Drug interactions
Ketoprofen may weaken the effect of diuretics and antihypertensive drugs, and enhance the effect of oral hypoglycemic and some anticonvulsants (phenytoin).
Combined use with other NSAIDs, salicylates, corticosteroids, ethanol increases the risk of developing adverse events from the gastrointestinal tract.
Simultaneous administration with anticoagulants, thrombolytics, and antiplatelet agents increases the risk of bleeding.
When taking NSAIDs concomitantly with diuretics or ACE inhibitors, the risk of renal dysfunction increases.
Increases plasma concentrations of cardiac glycosides, slow calcium channel blockers, lithium preparations, cyclosporine, methotrexate.
NSAIDs may reduce the effectiveness of mifepristone. Taking NSAIDs should be started no earlier than 8-12 days after stopping mifepristone.
Inside. Standard dose of Ketonal ® Duo for adults and children over 15 years old is 150 mg/day. Capsules should be taken during or after meals with water or milk (the volume of liquid must be at least 100 ml).
The maximum dose of ketoprofen is 200 mg/day.
Storage conditions and shelf life
The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25°C. Shelf life - 2 years.