Ketonal capsules 150 instructions for use. Ketonal duo - description of the drug, instructions for use, reviews. With kidney failure
Lek d.d./Novartis Neva Ltd., 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 - Bechterew's disease, psoriatic arthritis, reactive arthritis (Reiter's syndrome); gout, pseudogout; osteoarthritis; - pain syndrome: headache; tendinitis, bursitis, myalgia, neuralgia, sciatica; post-traumatic and postoperative pain syndrome; pain syndrome in oncological diseases; algomenorrhea.
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 / Bechterew's disease /, psoriatic arthritis, reactive arthritis / Reiter's syndrome /); - gout, pseudogout; - osteoarthritis. pain syndrome: - headache; - tendinitis, bursitis, myalgia, neuralgia, sciatica; - post-traumatic and postoperative pain syndrome; - pain syndrome in oncological diseases; - algomenorrhea.
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 a meal with water or milk (the volume of liquid should 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, thiaprofenic 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 history); - erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; - ulcerative colitis, Crohn's disease; - hemophilia and other blood clotting disorders; - severe liver failure; - active liver disease; - severe renal failure (CC less than 30 ml / min); - progressive kidney disease; - decompensated heart failure; - postoperative period after coronary artery bypass grafting; - gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding); - diverticulitis; - inflammatory bowel disease; - confirmed hyperkalemia; - chronic dyspepsia; - children's age up to 15 years; - III trimester of pregnancy; - the period of breastfeeding; - lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome. With caution, the drug should be prescribed for a history of peptic ulcer disease, a history of bronchial asthma, clinically significant cardiovascular, cerebrovascular and peripheral arterial diseases, dyslipidemia, progressive liver disease, 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 gastrointestinal ulcers, the presence of Helicobacter pylori infection, with severe somatic diseases, smoking, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (eg, acetylsalicylic acid), oral corticosteroids (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, sertraline), long-term use of NSAIDs, elderly patients (including those taking diuretics), patients with decreased ionic bcc.
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Ketonal Duo - drug from the category of non-steroidal anti-inflammatory drugs. It is best known as a drug that eliminates severe pain of various origins. However, it is also used to relieve various inflammations and inflammatory processes.
About the drug
Ketonal Duo has anti-inflammatory and analgesic effect and can also reduce fever. Thanks to the double structure of the capsules, the drug quickly penetrates the organ and quickly begins to exert its therapeutic effect, while the action of the drug lasts for a long time, up to about 30 hours.
The drug is absorbed by the body by 90%, while 80% of the drug is excreted through the kidneys, and the rest through the digestive organs.
Manufacturer
The drug is created by the company Lek, which is localized in Slovenia.
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Irina Martynova. Graduated from the Voronezh State Medical University. N.N. Burdenko. Clinical intern and neurologist of BUZ VO \"Moscow Polyclinic\".
Release form and composition
Medication available in modified release capsules. Capsules consisting of pellets of two colors - yellow and white. The active ingredient in the structure of the drug is ketoprofen in the amount of 0.15 g. Additional substances lactose monohydrate, microcrystalline cellulose, povidone, croscarmellose sodium, polysorbate 80.
The pellet shell consists of eudragit RS 30D, RL 30D, triethyl citrate, polysorbate 80, talc, iron, yellow oxide or E172, colloidal dioxide.
Capsule shell made of gelatin, indigo carmine or E132, titanium dioxide or E171.
Tablets are packed in blisters, each of which has ten pieces, and blisters in cardboard packaging.
Ketonal Duo capsules differ from the usual Ketonal in the amount of active substance in one dose, only 0.05 mg is present in the Ketonal structure. ketoprofen. In addition, Duo capsules have a modified release, unlike simple Ketonal. However, the advantage of the latter is the multiplicity of dosage forms - tablets, solution, suppositories, cream, gel.
Method of application and dosage
Instructions for using Ketonal Duo are as follows. Medication taken orally, that is, inside. The usual dose of the drug is 0.15 g. in a day.
Take the capsules after meals or with meals. Wash down with water or milk, but the amount of liquid should not be less than 0.1 liters.
Ketonal Duo is able to have a strong effect, so it is important to follow the dosage and not exceed the maximum dose of the drug, which is 200 mg / day.
Indications for use
It is used in the treatment of diseases of the musculoskeletal system, which have an inflammatory and degenerative character. These include:
- rheumatoid arthritis;
- ankylosing spondylitis;
- Reiter's syndrome;
- inflammation of the joints in patients with psoriasis;
- gout, incl. pseudogout;
- osteoarthritis.
Used to reduce and eliminate pain, such as:
- headache;
- with inflammation of the articular bag;
- with inflammation of the tendons;
- muscle pain;
- neuralgia;
- radiculitis;
- pain after injuries and operations;
- algosmenorrhea (pain during menstruation);
- with oncology.
Contraindications
Medicine has some contraindications to treatment. It can not be used for diseases such as:
- bronchial asthma, a syndrome of inflammation of the nasal mucosa, a history of urticaria, which were provoked by taking acetylsalicylic acid or certain NSAIDs;
- stomach ulcer and 12 duodenal ulcer during exacerbation;
- nonspecific ulcerative colitis and Crohn's disease during exacerbation;
- inflammation of the intestine during exacerbation;
- chronic bleeding and other pathologies in blood clotting;
- insufficient liver and kidneys of a pronounced degree;
- developing pathologies of the kidneys;
- decompensated heart failure;
- after coronary artery bypass grafting;
- bleeding or suspicion of them from the digestive organs, brain, etc .;
- chronic indigestion;
- age up to 15 years;
- third trimester of pregnancy;
- lactation;
- special sensitivity to the composition of the drug, salicylates and other NSAIDs.
Used with caution when:
- ulcer pathology, history of bronchial asthma;
- the presence of symptoms of diseases of the organs of the heart, brain, periphery of the arteries;
- dyslipidemia;
- developing liver diseases;
- increase in the amount of bilirubin;
- kidney failure;
- heart failure of a chronic nature;
- increased pressure;
- blood diseases;
- dehydration of the body;
- diabetes mellitus;
- smoking, alcoholism.
special instructions
Among the special instructions, it is worth noting the moment of monitoring the state of the blood, the activity of the liver and kidneys, in particular in the elderly over 65 years old, if the medication is taken for a sufficiently long period.
When treating patients with high blood pressure and cardiovascular pathologies, which are ways to retain fluid in the body, it is necessary to frequently monitor the pressure in the arteries and be careful.
Ketonal Duo has the ability to mask the symptoms of infectious pathologies.
The drug is not taken for liver and kidney failure of a pronounced nature due to contraindications.
Use by pregnant and lactating women
The drug can be used in the treatment of pregnant women in the first and second trimesters of pregnancy, if the possible benefit to the mother is higher than the likely risk to the child.
Breastfeeding women are not recommended to take the medicine.
Use in children and the elderly
It is contraindicated for children under 15 years of age to take the medication, and for the elderly it is possible, but with caution and special care, as well as in compliance with all recommendations.
Adverse reactions and overdose
Ketonal Duo, if the dosage is not observed, can cause negative consequences in the form of an overdose. This may show up:
- nausea and vomiting reactions;
- pain in the abdomen;
- emetic reactions with blood secretions, chalky;
- disorder of consciousness;
- respiratory depression;
- convulsive reactions;
- violation of the kidneys, incl. kidney failure.
In case of an overdose, you should consult a specialist. As a first aid, it is worth rinsing the stomach and drinking activated charcoal.
The medication can provoke adverse reactions, among which negative reactions from the digestive organs, central nervous system, sensory organs, heart, hematopoietic system, urogenital organs are noted, allergic reactions and some others may also occur.
Interaction with other drugs
The drug does not always interact well with other medicines.
| Name | Reaction |
|---|---|
| Diuretics, antihypertensive drugs | Ketonal Duo is able to weaken their effect |
| Hypoglycemic (by mouth) and some anti-seizure drugs | Ketonal may enhance their effects |
| Parallel reception with NSAIDs, salicylates, corticosteroids, ethanol | The risk of negative phenomena in the digestive organs increases |
| Anticoagulants, thrombolytics, antiplatelet agents | Increased risk of bleeding |
| Diuretics or ACE inhibitors | Increased risk of kidney damage |
| Cardiac glycosides, slow calcium channel blockers, lithium preparations, cyclosporine, methotrexate | Increases their content in plasma |
| Mifepristone | Reduces their effectiveness. In this regard, Ketonal Duo treatment can be started no earlier than 8 to 12 days after the first one is canceled. |
Storage and dispensing from pharmacies
Storage conditions are standard - not higher than 25 0 C and in a place far from children. Shelf life - 24 months.
Released without a doctor's prescription.
Analogues
The drug has a number of analogues, similar in active ingredient - ketoprofen.
Ketonal DUO: instructions for use and reviews
Ketonal DUO is a drug with analgesic, anti-inflammatory and antipyretic effects.
Release form and composition
Dosage form of release of Ketonal DUO - capsules with modified release: size No. 1; case - transparent, cap - blue; capsules contain yellow and white pellets (10 pcs. in blisters, in a cardboard bundle 1-3 blisters).
Composition of 1 capsule:
- active substance: ketoprofen - 150 mg;
- auxiliary components: lactose monohydrate - 20 mg; croscarmellose sodium - 10 mg; povidone - 5 mg; microcrystalline cellulose - 34 mg; polysorbate-80 - 1 mg;
- capsule shell: titanium dioxide (E 171) - 0.9%; indigo carmine (E 132) - 0.4%; gelatin - up to 100%;
- pellet shell: colloidal silicon dioxide - 0.2 mg; talc - 0.2 and 1.760 mg; Eudragit RL 30 D [copolymer of methyl methacrylate, ethyl acrylate and trimethylammonioethyl methacrylate (2: 1: 0.2)] - 4.908 mg; eudragit RS 30 D [copolymer of methyl methacrylate, ethyl acrylate and trimethylammonioethyl methacrylate (2: 1: 0.1)] - 4.908 mg; iron oxide (III) yellow (E 172) - 0.08 mg; triethyl citrate - 0.88 mg; polysorbate-80 - 0.008 mg.
Pharmacological properties
Pharmacodynamics
Ketonal DUO is one of the non-steroidal anti-inflammatory drugs (NSAIDs). It has analgesic, antipyretic and anti-inflammatory effects.
Due to the inhibition of COX-1 and COX-2 (cyclooxygenase) and (partly) lipoxygenase, ketoprofen stabilizes lysosomal membranes and inhibits the synthesis of bradykinin and prostaglandins.
Ketoprofen does not have a negative effect on articular cartilage.
Pharmacokinetics
Ketonal DUO is presented in a new dosage form, which differs from conventional capsules in a special release of the active substance. The capsules contain 2 types of pellets: about 60% of the total amount are white, the rest are yellow (coated). The active substance is released quickly from white pellets, slowly from yellow ones. This leads to a combination of prolonged and rapid action.
After oral administration, Ketonal DUO is well absorbed.
The bioavailability of the substance in the form of conventional capsules / capsules with modified release is 90%.
The overall bioavailability (AUC) of ketoprofen is not affected by food intake, but the absorption rate decreases. After oral administration of 150 mg Ketonal DUO Cmax (maximum concentration of the substance) in the blood plasma is reached in 1.76 hours and is 9036.64 ng / ml.
99% of ketoprofen binds to plasma proteins (mainly to albumins). The volume of distribution is 0.1–0.2 l/kg. The substance penetrates well into the synovial fluid and reaches 30% of the plasma concentration. Significant concentrations in the synovial fluid remain stable for up to 30 hours, as a result of which joint stiffness and pain are reduced for a long time.
Ketoprofen with the participation of microsomal liver enzymes undergoes intensive metabolism. Binding occurs with glucuronic acid, is excreted in the form of glucuronide. Ketoprofen has no active metabolites. The half-life is less than 2 hours.
Approximately 80% of ketoprofen is excreted in the urine, mainly (more than 90%) - in the form of ketoprofen glucuronide, about 10% is excreted through the intestines.
The plasma concentration of ketoprofen in liver failure increases by 2 times (probably due to hypoalbuminemia and the associated high level of unbound active ketoprofen). In this group of patients, the drug should be prescribed in the minimum therapeutic dose.
In renal insufficiency, the clearance of ketoprofen is reduced, and dose adjustment is required.
Indications for use
Capsules Ketonal DUO 150 mg are prescribed for the symptomatic treatment of inflammatory / painful processes of various etiologies, including:
- diseases of the musculoskeletal system of inflammatory and degenerative etiology: rheumatoid arthritis, gout, pseudogout, seronegative arthritis (including psoriatic arthritis, ankylosing spondylitis, reactive arthritis), osteoarthritis;
- pain syndrome: headache, algomenorrhea, neuralgia, tendinitis, myalgia, bursitis, sciatica, post-traumatic and postoperative pain, pain syndrome in oncological diseases.
Contraindications
Absolute:
- exacerbation of peptic ulcer of the stomach and duodenum;
- indications of a history of rhinitis, bronchial asthma, urticaria associated with taking acetylsalicylic acid and other NSAIDs;
- nonspecific ulcerative colitis,
- exacerbation of inflammatory bowel disease;
- exacerbation of Crohn's disease;
- severe hepatic and (or) renal failure;
- hemophilia and other blood clotting disorders;
- decompensated heart failure;
- progressive kidney disease;
- postoperative period after coronary artery bypass grafting;
- chronic dyspepsia;
- cerebrovascular, gastrointestinal and other bleeding (including the presence of suspicion of them);
- age up to 15 years;
- III trimester of pregnancy and the period of breastfeeding;
- individual intolerance to the components of the drug, as well as salicylates or other NSAIDs.
Relative (diseases / conditions in the presence of which the appointment of Ketonal DUO requires caution):
- indications in the anamnesis of peptic ulcer, peptic ulcer of the gastrointestinal tract and bronchial asthma;
- clinically expressed cerebrovascular and cardiovascular diseases;
- peripheral arterial disease;
- progressive liver disease;
- dyslipidemia;
- hyperbilirubinemia;
- chronic heart failure;
- kidney failure;
- arterial hypertension;
- diabetes;
- blood diseases;
- dehydration;
- alcoholism;
- smoking;
- long-term use of NSAIDs;
- concomitant use with the following drugs: anticoagulants (warfarin), antiplatelet agents (acetylsalicylic acid), oral glucocorticosteroids (prednisolone), selective serotonin reuptake inhibitors (sertraline, citalopram);
- I-II trimesters of pregnancy.
Instructions for use Ketonal DUO: method and dosage
Capsules Ketonal DUO 150 mg are taken orally with water or milk (at least 100 ml), preferably during or after meals.
The standard dose is 1 capsule per day.
The maximum daily dose of ketoprofen is 200 mg.
Side effects
Possible adverse reactions (> 10% - very often; > 1% and< 10% – часто; >0.1% and< 1% – нечасто; >0.01% and< 0,1% – редко; < 0,01% – очень редко):
- urinary system: rarely - impaired renal function, nephrotic syndrome, interstitial nephritis, hematuria (more often occurs in patients taking diuretics and NSAIDs for a long time);
- cardiovascular system: infrequently - peripheral edema, arterial hypertension, tachycardia;
- central nervous system: often - nightmares, sleep disturbances, dizziness, headache, nervousness, fatigue; rarely - peripheral polyneuropathy, migraine; very rarely - speech disorder, disorientation, hallucinations;
- digestive system: often - dyspepsia (in the form of nausea, diarrhea or constipation, flatulence, vomiting, decrease or increase in appetite), stomatitis, abdominal pain, dry mouth; infrequently (with prolonged use of high doses) - ulceration of the mucous membrane of the gastrointestinal tract, impaired hepatic function; rarely - perforation of the gastrointestinal tract, gastrointestinal bleeding, melena, transient increase in liver enzymes, exacerbation of Crohn's disease;
- hematopoietic system: decreased platelet aggregation; rarely - thrombocytopenia, anemia, purpura, agranulocytosis;
- allergic reactions: often - skin reactions (in the form of itching, urticaria); infrequently - anaphylactoid reactions, shortness of breath, rhinitis, angioedema, bronchospasm;
- sensory organs: rarely - conjunctivitis, change in taste, tinnitus, blurred vision;
- others: rarely - menometrorrhagia, hemoptysis.
Overdose
The main symptoms are vomiting (including blood), convulsions, respiratory depression, nausea, abdominal pain, melena, impaired consciousness, impaired renal function and renal failure.
Therapy: gastric lavage, activated charcoal; symptomatic treatment. The effect on the gastrointestinal tract can be reduced by the use of prostaglandins, proton pump inhibitors and histamine H2 receptor blockers.
special instructions
When conducting prolonged therapy, monitoring of the state of the blood, as well as renal / hepatic function, is required, especially in elderly patients.
Against the background of arterial hypertension and cardiovascular diseases, which can lead to fluid retention in the body, taking Ketonal DUO requires caution and more frequent monitoring of blood pressure.
It must be taken into account that the drug can mask the signs of infectious diseases.
Influence on the ability to drive vehicles and complex mechanisms
When driving vehicles, it is necessary to take into account the individual response of the patient to the therapy being carried out.
Use during pregnancy and lactation
- III trimester of pregnancy, lactation period - taking Ketonal DUO is contraindicated;
- I-II trimesters of pregnancy - therapy can be carried out with caution in cases where the expected benefit is higher than the potential harm.
Application in childhood
According to the instructions, Ketonal DUO is not prescribed for children under 15 years of age.
For impaired renal function
Contraindication to taking Ketonal DUO is severe renal failure.
For impaired liver function
Contraindication to taking Ketonal DUO is severe liver failure.
drug interaction
Possible interactions:
- diuretics and antihypertensives: weakening their action;
- other NSAIDs, salicylates, glucocorticosteroids, ethanol: an increase in the likelihood of adverse effects from the digestive system;
- oral hypoglycemic and some anticonvulsants (phenytoin): enhancing their action;
- mifepristone: a decrease in its effectiveness (you should not start taking Ketonal DUO earlier than 8-12 days after the abolition of mifepristone);
- anticoagulants, thrombolytics, antiplatelet agents: an increase in the likelihood of bleeding;
- cardiac glycosides, slow calcium channel blockers, lithium preparations, cyclosporine, methotrexate: an increase in their plasma concentration;
- diuretics or angiotensin-converting enzyme inhibitors: increased risk of impaired renal function.
Analogues
Analogs of Ketonal DUO are Arketal Rompharm, Fastum gel, Valusal, Bystrumgel, Flamax, Bystrumcaps, Artrozilen, Ketonal, OKI, Artrum, Febrofid, Pentalgin, Flexen, Ketoprofen, etc.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 °C. Keep away from children.
Shelf life - 2 years.
One capsule contains
active substance (pellet core) - ketoprofen 150 mg,
excipients (pellet shell): microcrystalline cellulose pellet shell - 34.000 mg, lactose monohydrate - 20.000 mg, povidone - 5.000 mg, croscarmellose sodium - 10.000 mg, polysorbate 80 - 1.000 mg,
pellet shell: eudragit RS 30 D - 4.908 mg, eudragit RL 30 D - 4.908 mg, triethyl citrate - 0.880 mg, polysorbate 80 - 0.008 mg, talc - 1.760 mg, yellow iron oxide (E172) - 0.080 mg, colloidal anhydrous silicon dioxide - 0.200 mg.
capsule cap composition: indigotine (E 132) - 0.40%, titanium dioxide (E 171) - 0.90%, gelatin up to 100%.
capsule body composition: gelatin 100%.
Description
Hard gelatin capsules with a transparent body and blue cap. The contents of the capsules are white and yellow pellets.
Pharmacotherapeutic group
Non-steroidal anti-inflammatory drugs. propionic acid derivatives. Ketoprofen.
ATX code M01AE03
Pharmacological properties
Pharmacokinetics
Ketonal DUO capsules are a new dosage form that differs from the standard one in a different release of the active substance. Capsules contain two types of pellets: standard (white) and coated (yellow). Ketoprofen is rapidly released from white pellets (60% of the total) and slowly from yellow pellets (40% of the total), which allows a combination of fast and prolonged action. The effect begins to appear 20 minutes after ingestion.
Capsules Ketonal DUO 150 mg are well absorbed and oral bioavailability of ketoprofen is 90%. Eating does not affect the overall bioavailability, 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. Ketoprofen penetrates into the synovial fluid and reaches a concentration there equal to 30% of the plasma concentration.
After oral administration of ketoprofen 150 mg capsules with a modified release, the maximum plasma concentration is reached within 1.76 hours.
The half-life of ketoprofen (from white pellets) is 2 hours. However, due 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 once a day.
Ketoprofen is metabolized in the liver. About 60-75% ketoprofen
excreted in the urine, mainly in the form of a conjugate with glucuronic acid. Less than 10% is excreted unchanged in the feces.
Pharmacodynamics
Ketoprofen is a non-steroidal antirheumatic drug with analgesic and anti-inflammatory effects.
The mechanism of action of Ketonal is associated with inhibition of the biosynthesis of prostaglandins and leukotrienes by suppressing the activity of the cyclooxygenase enzyme (COX-1 and COX-2), which catalyzes the synthesis of prostaglandins from arachidonic acid. Ketoprofen stabilizes lysosome membranes and has anti-bradykinin activity.
Indications for use
Rheumatoid arthritis
Seronegative spondyloarthritis (ankylosing spondylitis, psoriatic arthritis, reactive arthritis)
Gout, pseudogout
Osteoarthritis
Extra-articular rheumatism (tendinitis, bursitis, capsulitis of the shoulder joint)
Pain syndrome:
Postoperative
Algodysmenorrhea
Pain with bone metastases in cancer patients.
Dosage and administration
Capsules Ketonal DUO should be swallowed with a full glass of water, you can also drink milk.
The standard dose is one capsule of Ketonal DUO (150 mg) once a day. The maximum daily dose is 200 mg.
To reduce the risk of side effects from the gastrointestinal tract, it is recommended to take antacids (drugs that reduce the secretion of gastric juice).
The duration of the course of treatment is determined by the attending physician
Liver failure
In hepatic insufficiency, patients should take the minimum daily dose of ketoprofen, since even this is sufficient to obtain the desired therapeutic effect.
kidney failure
In patients with severe renal insufficiency, the dose of ketoprofen should be reduced accordingly.
Elderly patients
Elderly patients are at high risk of developing severe side effects. If treatment with non-steroidal anti-inflammatory drugs (NSAIDs) is necessary, the lowest dose should be used and the patient should be monitored closely for gastrointestinal bleeding every four weeks after initiation of NSAID treatment.
Side effects
Dyspeptic phenomena, loss of appetite, nausea, vomiting, flatulence, abdominal pain
Diarrhea, gastritis, constipation, flatulence
Headache, dizziness, drowsiness
Skin rash, itching
Posthemorrhagic anemia, leukopenia
Depression, insomnia, nervousness, paresthesia
Visual impairment (blurred vision)
Noise in ears
Stomatitis, gastric and duodenal ulcer
Hepatitis, increased levels of transaminases and bilirubin
Weight gain
Anaphylactic shock
Bronchospasm, asthma attack
Rarely:
Exacerbation of colitis and Crohn's disease, gastrointestinal bleeding, perforation, melena, hematemesis
Impaired liver function
Acute renal failure, tubulointerstitial nephritis, nephritic syndrome, abnormal kidney function tests
Hypernatremia, hyperkalemia
Agranulocytosis, thrombocytopenia, bone marrow failure
Seizures, dysgeusia
Heart failure
Arterial hypertension, vasodilation
Photosensitivity, alopecia, urticaria, angioedema, bullous rash including Stevens-Johnson syndrome, toxic epidermal necrolysis
Anaphylactic reactions (including shock), mood variability
Fatigue
Contraindications
Individual hypersensitivity to ketoprofen or any auxiliary component of the drug
Patients with a history of rhinitis, bronchospasm, asthma, allergic rashes or allergic reactions caused by taking ketoprofen or similar active substances, such as other non-steroidal anti-inflammatory drugs or salicylates (for example, such as acetylsalicylic acid)
severe heart failure
For the treatment of postoperative pain in case of surgical coronary artery bypass grafting
Patients with a history of chronic dyspepsia
Patients with an active peptic ulcer, or any history of gastrointestinal bleeding, ulceration, or perforation
Bleeding (gastrointestinal, cerebrovascular, or other active bleeding)
Tendency to bleed
Severe liver or kidney dysfunction
Blood disorders (leukopenia, thrombocytopenia, hemocoagulation disorders)
Patients with hereditary galactose intolerance, lactose deficiency or malabsorption of glucose or galactose (contains lactose).
Pregnancy and lactation
Children's age up to 18 years
Drug Interactions
Simultaneous administration of antacids or other drugs that reduce the acidity of gastric juice does not affect the rate and volume of absorption of the drug.
Ketonal DUO reduces the effect of diuretics and antihypertensive drugs, and increases the effect of oral hypoglycemic drugs and some antiepileptic drugs (phenytoin).
Potassium preparations, potassium-sparing diuretics, ACE inhibitors, heparins (low molecular weight or non-fractionated), cyclosporine, tacrolimus and trimethoprim, when used simultaneously with non-steroidal anti-inflammatory drugs, can contribute to the occurrence of hyperkalemia.
Due to the increased risk of gastrointestinal bleeding and ulceration, patients taking Ketonal DUO with anticoagulants or corticosteroids require constant monitoring.
Anticoagulants (heparin and warfarin) and inhibitors of platelet aggregation (eg ticlopidine, clopidogrel) increase the risk of bleeding.
Ketonal DUO reduces excretion and thereby increases the toxicity of cardiac glycosides, lithium, cyclosporine and methotrexate.
Ketonal DUO may reduce the effectiveness of mifepristone.
Reception of NSAIDs should be started no earlier than 8-12 days after the abolition of mifepristone.
Ketonal DUO should not be co-administered with other NSAIDs and salicylates.
special instructions
Non-steroidal anti-inflammatory drugs, including Ketonal DUO, have an aggressive effect on the mucous membrane of the gastrointestinal tract and prolonged, uncontrolled use of these drugs can lead to the development of stomach ulcers.
With extreme caution, ketoprofen should be prescribed to patients with a history of gastrointestinal disease. Bleeding and perforation may develop suddenly without previous symptoms. Special attention also requires the use of the drug in patients with impaired hemostasis, hemophilia, von Willebrand disease, severe thrombocytopenia, renal or hepatic insufficiency, as well as in patients taking anticoagulants (coumarin and heparin derivatives, mainly low molecular weight heparins).
Caution should also be exercised in patients taking medications that may increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants (eg warfarin), selective serotonin reuptake inhibitors, or antiplatelet agents (including acetylsalicylic acid). In such cases, combination therapy with drugs that have a protective effect on the gastrointestinal tract (for example, misoprostol or proton pump inhibitors) should be considered.
Patients with diseases of the gastrointestinal tract (especially elderly patients) should inform the doctor about any abdominal symptoms.
In the event of gastrointestinal bleeding or ulceration in the gastrointestinal tract, treatment should be discontinued immediately.
With caution, the drug should be prescribed to older people. Ketonal DUO should be used with caution in patients suffering from hypertension and heart disease, accompanied by fluid retention in the body. Blood pressure monitoring is recommended, especially in patients with cardiovascular disease.
Excipients: microcrystalline cellulose - 34 mg, lactose monohydrate - 20 mg, - 5 mg, croscarmellose sodium - 10 mg, polysorbate 80 - 1 mg.
The composition of the 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 - 0.008 mg, iron (III) - 1.76 mg yellow oxide (E172) - 0.08 mg, talc 2 - 0.2 mg, colloidal silicon dioxide 2 - 0.2 mg.
The composition of the capsule shell 1L970/53.051: gelatin - up to 100%, (E132) - 0.4%, titanium dioxide (E171) - 0.9%.
1 in the capsule only 40% of the pellets are coated;
2 the amount of talc (0.2 mg) of colloidal silicon dioxide is not taken into account by the mass of the contents of the capsule.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
pharmachologic effect
NSAIDs, a derivative of propionic acid. 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 the synthesis of prostaglandins (including in the central nervous system, most likely in the hypothalamus).
Stabilizes in vitro and in vivo lysosomal membranes, at high concentrations in vitro, ketoprofen inhibits the synthesis of bradykinin and leukotrienes.
Ketoprofen does not adversely affect the condition of the articular cartilage.
Pharmacokinetics
Suction
Duo is a new dosage form that differs from conventional capsules in the way the active substance is released. Modified release capsules contain two types of pellets: white (about 60% of the total) and yellow (coated). Ketoprofen is rapidly released from white pellets and slowly from yellow ones, resulting 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 capsules and capsules with modified release 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, 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, as a result of which pain and stiffness of the joints decrease for a long time.
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 at a dose of 100 mg or more, excretion by the kidneys may be difficult.
Pharmacokinetics in special clinical situations
In patients with severe renal insufficiency, most of the drug is excreted through the intestines. When taken in high doses, hepatic clearance also increases. Up to 40% of the drug is excreted through the intestines.
In patients with hepatic insufficiency, the plasma concentration of ketoprofen is increased by 2 times (probably due to hypoalbuminemia, and as a result of this high level of unbound active ketoprofen); such patients should be prescribed the drug in the minimum therapeutic dose.
In patients with renal insufficiency, the clearance of ketoprofen is reduced, however, dose adjustment is required only in case of severe renal insufficiency.
In elderly patients, the metabolism and excretion of ketoprofen are slower, which is of clinical importance 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 / Bechterew's disease /, psoriatic arthritis, reactive arthritis / Reiter's syndrome /);
- gout, pseudogout;
- osteoarthritis.
pain syndrome:
- headache;
- tendinitis, bursitis, myalgia, neuralgia, sciatica;
- post-traumatic and postoperative pain syndrome;
- pain syndrome in oncological diseases;
- algomenorrhea.
Contraindications
- hypersensitivity to ketoprofen or other components of the drug, as well as salicylates, thiaprofenic 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 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 (CC less than 30 ml / min);
- progressive kidney disease;
- decompensated insufficiency;
- postoperative period after coronary artery bypass grafting;
- gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding);
- diverticulitis;
- inflammatory bowel disease;
- confirmed hyperkalemia;
- chronic dyspepsia;
- children's age up to 15 years;
- 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 significant cardiovascular, cerebrovascular 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 gastrointestinal ulcers, the presence of Helicobacter pylori infection, with severe somatic diseases, 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), long-term use of NSAIDs, elderly patients (including those taking diuretics), patients with reduced BCC.
Dosage
inside. The 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 a meal with water or milk (the volume of liquid should be at least 100 ml).
The maximum dose of ketoprofen is 200 mg/day.
Side effects
Definition of categories of frequency of undesirable 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; the frequency is unknown - convulsions, a violation of taste sensations, emotional lability.
From the sense organs: rarely - blurred vision, tinnitus.
From the side of the cardiovascular system: the frequency is unknown - heart failure, increased blood pressure, vasodilation.
From the respiratory system: rarely - exacerbation of bronchial asthma; the frequency is unknown - bronchospasm (especially in patients with established hypersensitivity to NSAIDs), rhinitis.
From the gastrointestinal tract: often - nausea, vomiting, dyspepsia, pain in the abdomen; infrequently - constipation, diarrhea, bloating, gastritis; rarely - peptic ulcer, stomatitis; very rarely - exacerbation of ulcerative colitis or Crohn's disease, gastrointestinal bleeding and perforation.
From the side of the liver and biliary tract: rarely - hepatitis, increased levels of hepatic transaminases and bilirubin.
From the skin and subcutaneous tissues: infrequently - skin rash, skin 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.
Other: infrequently - swelling, fatigue; rarely - weight gain; frequency unknown - increased fatigue.
Overdose
Symptoms: as with other NSAIDs, overdose of ketoprofen may cause nausea, vomiting, abdominal pain, vomiting of blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function and renal failure.
Treatment: in case of overdose, gastric lavage and the use of activated charcoal are indicated. Carrying out symptomatic therapy. The effect of ketoprofen on the gastrointestinal tract can be reduced by drugs that reduce the secretion of the gastric glands (for example, proton pump inhibitors) and prostaglandins. In the event of renal failure, hemodialysis is recommended.
drug interaction
Ketoprofen may weaken the effect diuretics and antihypertensives and enhance action oral hypoglycemic and some anticonvulsants(phenytoin).
Sharing with others NSAIDs, salicylates, corticosteroids, ethanol increases the risk of adverse events in 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 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. NSAIDs should be started no earlier than 8-12 days after the abolition of mifepristone.
special instructions
With prolonged use of NSAIDs, it is necessary to monitor the state of the blood, as well as the functions of the kidneys and liver, especially in elderly patients (over 65 years of age).
It is necessary to be careful and control 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.
Like other NSAIDs, ketoprofen may mask signs of infectious diseases.
Influence on the ability to drive vehicles and control mechanisms
There are no data on the negative effect of Ketonal Duo at recommended doses on the ability to drive a car or work with mechanisms. At the same time, patients who notice non-standard 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 an undesirable effect on the course of pregnancy and/or embryonic development. Data obtained in the course of 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 I and II trimesters of pregnancy is possible only if the benefits to 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 the labor activity of the uterus and / or premature closure of the ductus arteriosus, a possible increase in bleeding time, oligohydramnios and renal failure.
To date, there are no data on the excretion of ketoprofen with breast milk, therefore, if it is necessary to use ketoprofen in a nursing mother, the issue of stopping breastfeeding should be resolved.
Application in childhood
Contraindicated in children and adolescents under 15 years of age.