KETRUM [Ketoprofen] 100 mg/2 ml Solution for intramuscular injection
KETRUM
instructions for medical use of the medicinal product
Tradename
Ketrum, Ketrum
International non-proprietary name
Ketoprofen, Ketoprofen
Compound
Each 2 ml solution for injection (1 ampoule) contains 100 mg of ketoprofen.
Excipients: arginine, benzyl alcohol, citric acid, water for injection.
Dosage form
Injection.
Pharmacotherapeutic group
Non-steroidal anti-inflammatory and antirheumatic drugs, derivatives of propionic acid.
Pharmacological properties
Pharmacodynamics
Ketrum is a non-steroidal antirheumatic drug with anti-inflammatory, analgesic and antipyretic effects.
Ketoprofen, the active substance of the drug, inhibits the synthesis of prostaglandins and leukotrienes by blocking the enzyme cyclooxygenase (COX-1 and COX-2), which catalyzes the synthesis of prostaglandins in the metabolism of arachidonic acid. Ketoprofen stabilizes lysosomal membranes in vitro and in vivo, inhibits the synthesis of leukotrienes in vitro at high concentrations and has anti-bradykinin activity. The mechanism of antipyretic action of ketoprofen is unknown. Perhaps ketoprofen inhibits the synthesis of prostaglandins in the central nervous system (most likely in the hypothalamus). In some women, ketoprofen reduces symptoms of primary dysmenorrhea, probably by inhibiting the synthesis and/or efficacy of prostaglandins.
Pharmacokinetics
Mean plasma levels measured 5 minutes after initiation of intravenous infusion
100 mg of ketoprofen and 4 minutes after the end of administration, are 26.4 ± 5.4 μg / ml. Bioavailability - 90%. When administered intramuscularly, in most patients, ketoprofen was detected in the blood after 15 minutes, and the peak plasma concentration was reached 2 hours after administration. The bioavailability of ketoprofen when injected increases linearly with increasing dose of the drug. 99% of Ketoprofen binds to plasma proteins, mainly to albumin. The volume of distribution in tissues is 0.1-0.2 l / kg. Ketoprofen slowly penetrates into the synovial fluid and is also slowly excreted from it against the background of a continuing decrease in plasma concentration. Equilibrium concentrations of ketoprofen are established 24 hours after its administration. In elderly patients, the equilibrium concentration was reached after 8.7 hours and was 6.3 μg / ml.
Ketoprofen is extensively metabolized by hepatic microsomal enzymes.
It binds to glucuronic acid and is excreted from the body in this form. After oral administration, its plasma clearance is 1.16 ml / min / kg. The biological half-life is only 2 hours. Liver failure can cause a prolongation of the half-life, in these circumstances cumulation is possible.
Up to 80% of ketoprofen is excreted in the urine and about 10% is excreted in the feces. In patients with renal insufficiency, ketoprofen is excreted more slowly, the biological half-life is increased by an hour. In older people, the metabolism and excretion of ketoprofen are slowed down. This is clinically significant only in patients with reduced renal function.
Indications for use
It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.
Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic arthritis, ankylosing spondylitis, gouty arthritis, osteoarthritis.
Pain syndrome: myalgia, ossalgia, neuralgia, tendonitis, arthralgia, bursitis, sciatica, adnexitis, otitis media, headache and toothache, pain in oncological diseases, post-traumatic and postoperative pain syndrome, accompanied by inflammation.
Algodysmenorrhea.
Contraindications
The drug is contraindicated in the following cases:
- a history of urticaria reactions, or other allergic reactions after taking ketoprofen, acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs);
- hypersensitivity to ketoprofen or any of the excipients of the drug;
- third trimester of pregnancy;
- severe heart failure;
- peptic ulcer in the active phase, as well as gastrointestinal bleeding, ulcer or perforation in history;
- hemorrhagic diathesis;
- severe liver failure;
- severe renal failure;
- cerebrovascular or other active bleeding.
The drug is contraindicated in patients with impaired hemostasis or undergoing treatment with anticoagulants.
Use during pregnancy or lactation
The use of the drug in the III trimester of pregnancy is contraindicated.
The use of ketoprofen in the I and II trimesters of pregnancy is possible only if the potential benefit to the mother outweighs the risk to the fetus.
If necessary, the use of ketoprofen during lactation should decide on the termination of breastfeeding.
Interaction with other drugs
Pharmaceutical incompatible with tramadol solution. Reduces the effectiveness of uricosuric drugs (PM), enhances the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics. Combined use with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increased risk of developing renal dysfunction.
Simultaneous administration with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding. Increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is required).
Increases the plasma concentration of verapamil and nifedipine, lithium preparations (Li +), methotrexate. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. If you are taking other medications, you should consult your doctor.
Special instructions and precautions
Particular caution should be observed when co-administered with drugs that can increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants (eg, warfarin), selective serotonin reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid, or nicorandil .
The simultaneous use of the drug with other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided.
The risk of gastrointestinal bleeding, ulcers or perforation increases with increasing doses of NSAIDs, in patients with a history of peptic ulcer, especially complicated by bleeding or perforation, and in the elderly. Treatment of these patients should be initiated at the lowest available dose. If gastrointestinal bleeding or ulceration occurs during treatment, treatment with the drug should be discontinued.
NSAIDs should be used with caution in patients with a history of gastrointestinal disease (ulcerative colitis, Crohn's disease), as they may experience exacerbations of these diseases.
C caution in prescribing the drug to patients with arterial hypertension, heart failure, impaired liver and kidney function.
In women, NSAIDs can reduce fertility. Therefore, NSAIDs are not recommended for women trying to conceive.
This drug may cause an asthma attack or bronchospasm, especially in people who are allergic to acetylsalicylic acid or NSAIDs.
With prolonged treatment, it is necessary to control the level of potassium.
Influence on the ability to drive vehicles and mechanisms
This drug may cause drowsiness, dizziness, seizures, or visual disturbances. In this regard, it is not recommended to drive vehicles and not work with mechanisms when these symptoms appear.
Dosage and administration
Enter intramuscularly at 100 mg once or twice a day.
The maximum daily dose is 200 mg of ketoprofen.
It is recommended not to prescribe injections for longer than 3 days.
Upon reaching a satisfactory response, the drug is prescribed in the form for oral administration.
If necessary, the drug can be combined with ketoprofen in the form for oral, rectal or transdermal administration.
Side effect
From the hemopoietic system: hemorrhagic anemia, hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia, bone marrow dysfunction.
From the immune system: anaphylactic reactions (including anaphylactic shock).
From the nervous system: insomnia, depression, asthenia, headache, dizziness, drowsiness, paresthesia, confusion or loss of consciousness, peripheral polyneuropathy, convulsions, taste disturbance, emotional lability.
From the senses: blurred vision, tinnitus, conjunctivitis, dryness of the mucous membrane of the eye, eye pain, hearing loss, optic neuritis.
From the side of the cardiovascular system: tachycardia, heart failure, increased blood pressure, vasodilation.
From the respiratory system: exacerbation of bronchial asthma, nosebleeds, laryngeal edema, bronchospasm (especially in patients with hypersensitivity to NSAIDs), rhinitis.
From the digestive system: nausea, vomiting, dyspepsia, pain in the abdomen, NSAID-gastropathy, constipation, diarrhea, bloating, gastritis, peptic ulcer, stomatitis, exacerbation of ulcerative colitis or Crohn's disease, gingival, gastrointestinal, hemorrhoidal bleeding, melena, gastrointestinal perforation, gastrointestinal discomfort, stomach pain.
From the side of the liver and biliary tract: increased activity of liver enzymes in the blood, increased concentration of bilirubin in the blood.
From the urinary system: cystitis, urethritis, hematuria, acute renal failure, interstitial nephritis, nephrotic syndrome, abnormal values of renal function.
From the skin and subcutaneous tissues: skin rash, pruritus, photosensitivity, alopecia, urticaria, exacerbation of chronic urticaria, angioedema, erythema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis, purpura.
Other: peripheral edema, fatigue, hemoptysis, menometrorrhagia, shortness of breath, thirst, muscle twitching.
Overdose
In adults, the main symptoms of overdose are headache, dizziness, drowsiness, nausea, vomiting, diarrhea and abdominal pain. In severe intoxication, arterial hypotension, respiratory depression and
gastrointestinal bleeding. The patient is immediately hospitalized and treated symptomatically. The specific antidote is unknown.
Storage conditions
Store in a place protected from light, at a temperature not exceeding 30 °C.
Keep out of the reach of children !
Best before date
3 years. Do not use after the expiry date stated on the package.
Holiday conditions
Released by prescription.
Release form
3 ampoules of 2 ml together with instructions for medical use in a cardboard box.