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Active ingredients
Ketoprofen
Release form
Capsules
Composition
1 capsule contains: Active substance: ketoprofen 50 mg. Auxiliary substances: lactose, magnesium stearate, colloidal silicon dioxide. The composition of the capsule shell: gelatin, titanium dioxide, dye blue patent Patent blue V.
Pharmacological effect
NSAIDs, a derivative of propionic acid. It has an analgesic, anti-inflammatory and antipyretic effect. Due to inhibition of COX-1 and COX-2 and, in part, of lipoxygenase, ketoprofen inhibits the synthesis of prostaglandins and bradykinin, stabilizes lysosomal membranes. Ketoprofen does not adversely affect the state of articular cartilage.
Pharmacokinetics
Absorption When ingested, ketoprofen is easily absorbed from the gastrointestinal tract. Bioavailability - 90%. When taking the drug in a dose of 100 mg Cmax in the blood plasma is reached after 1 h 22 min and is 10.4 mcg / ml. When taking the pills, the prolonged action of Cmax is achieved in 4-6 hours. Eating does not affect the bioavailability of ketoprofen. The distribution of Vd is 0.1-0.2 l / kg. Plasma protein binding is 99%. Ketoprofen penetrates well into the synovial fluid. Metabolism Exposure to intense metabolism in the liver through microsomal enzymes, conjugates with glucuronic acid. Excretion of ketoprofen T1 / 2 - 1.6-1.9 h. Ketoprofen is mainly metabolized in the liver. About 80% of ketoprofen is excreted in the urine, mostly as a conjugate with glucuronic acid (90%). About 10% is excreted unchanged through the intestines. Pharmacokinetics in special clinical situations In patients with renal insufficiency, ketoprofen is eliminated more slowly, T1 / 2 increases by 1 hour. In patients with hepatic insufficiency, ketoprofen may accumulate in the tissues. In elderly patients, metabolism and elimination Ketoprofena occur more slowly, but this is of clinical significance only for patients with reduced kidney function.
Contraindications
diseases of the gastrointestinal tract in the acute phase, pronounced abnormal liver function, pronounced renal dysfunction, blood disorders (leukopenia, thrombocytopenia, disorders of the blood coagulation system), Infancy is up to 15 years old, hemorrhoids and proctitis (for suppositories), hypersensitivity to ketoprofen, acetylsalicylic acid or other NSAIDs (indications of a history of bronchospasm, urticaria and rhinitis caused by acetylsalicylic acid).
Use during pregnancy and lactation
The use of ketoprofen in the third trimester of pregnancy is contraindicated. In the first and second trimesters of pregnancy, the prescription of a drug is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. When taking the drug during lactation, it is necessary to decide whether to stop breastfeeding.
Dosage and administration
Adults: the drug is prescribed in 1-2 caps. 2-3 times / day, or 1 tab. 2 times / day, or 1 tab. prolonged action 1 time / day. Capsules and pills should be taken during or immediately after a meal, without chewing, with a sufficient amount of water or milk (liquid volume is not less than 100 ml). Oral forms can be combined with the use of rectal suppositories or dosage forms Ketonal for external use (cream, gel). The maximum daily dose (including the use of various dosage forms) is 200 mg.
Side effects
Allergic reactions: common - skin reactions (itching, urticaria); non-prevalent - rhinitis, shortness of breath, bronchospasm, angioedema, anaphylactoid reactions. Digestive system: common - dyspepsia (nausea, diarrhea or constipation, flatulence, vomiting, decreased or increased appetite), abdominal pain, stomatitis, dry mouth, non-spreading long-term use in large doses) - ulceration of the gastrointestinal mucosa, impaired liver function; rare - perforation of the digestive tract, exacerbation of Crohn's disease, melena, gastrointestinal bleeding. CNS: common - headache, dizziness, sleep disturbance, fatigue, nervousness, nightmarish dreams; rare - migraine, peripheral polyneuropathy; very rare - hallucinations, disorientation and speech disorder. Sensory organs: rare - tinnitus, change in taste, blurred visual perception, conjunctivitis. CCC: unpredictable - tachycardia, arterial hypertension, peripheral edema. The urinary system: rare - impaired kidney function, interstitial; nephritis, nephrotic syndrome, hematuria (most often develop in people who take NSAIDs for a long time and diuretics). Others: rare - hemoptysis, menometerorrhagia. Laboratory values: ketoprofen reduces aggregation mbotsitov; transient increase in the level of liver enzymes; rare - anemia, thrombocytopenia, agranulocytosis, purpura.
Overdose
Symptoms: nausea, vomiting, abdominal pain, vomiting of blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function, renal failure. Treatment: gastric lavage, the appointment of activated carbon, carry out symptomatic therapy. The use of histamine H2-receptor blockers, proton pump inhibitors, and prostaglandin inhibitors has been shown. There is no specific antidote.
Interaction with other drugs
Ketoprofen reduces the effect of diuretics, antihypertensive drugs. Strengthens the effect of oral hypoglycemic drugs. Strengthens the effect of some anticonvulsants (such as phenytoin). When used simultaneously with other NSAIDs, salicylates, GCS and ethanol increases the risk of gastrointestinal bleeding. , thrombolytic agents, antiplatelet agents increase the risk of bleeding. The risk of developing impaired renal function is increased when taken simultaneously with iuretikami or inhibitors APF.Pri applied simultaneously increases the concentration of cardiac glycosides, calcium channel blockers slow, lithium preparations cyclosporin metotreksata.Ketoprofen may reduce the effectiveness of mifepristone. Acceptance of NSAIDs should begin no earlier than 8-12 days after the abolition of mifepristone.
special instructions
Ketonal can be taken with milk or taken with antacids to reduce the frequency of gastrointestinal disorders (milk and antacids do not affect the absorption of ketoprofen). With prolonged use of NSAIDs, it is necessary to monitor the condition of the blood, as well as liver and kidney function, especially in elderly patients . It is necessary to be careful and more often to control blood pressure when using ketoprofen for the treatment of patients with arterial hypertension, cardiovascular diseases that lead to fluid retention. To K and other NSAIDs, ketoprofen can mask the symptoms of infectious diseases. Effect on ability to drive vehicles and control mechanisms There are no data on the negative effect of ketonal in the recommended doses on the ability to drive a car or work with mechanisms.At the same time, patients who notice non-standard effects while taking the drug Ketonal should be careful when practicing potentially hazardous activities that require high concentration of attention and speed of psychomotor reactions.