Ketoprofen - instructions for use, doses, side effects, contraindications

Excipients: propylene glycol 400 mg, ethanol (ethyl alcohol rectified brand "Extra") 100 mg, benzyl alcohol 20 mg, sodium hydroxide solution 1 M to a pH of 6.5-7.5, water for injection up to 1 ml.

Description:

Transparent colorless or with a yellowish tinge of liquid.

Pharmacotherapeutic group:non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

M.02.A.A.10 Ketoprofen

Pharmacodynamics:

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID), has anti-inflammatory, analgesic and antipyretic effects associated with inhibition of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) activity regulating the synthesis of prostaglandinsPg).

Pharmacokinetics:

Bioavailability is more than 90%. The connection with plasma proteins is 99%. The time to reach the maximum concentration (TFROM_mOh) with parenteral administration - 15-30 minutes. The therapeutic concentration in the synovial fluid persists for 6-8 hours. In significant amounts it does not penetrate the blood-brain barrier (BBB).

Almost completely metabolized in the liver by glucuronizing, has the effect of "first passage" through the liver.

It is excreted mainly by the kidneys.

Do not cumulate.

Indications:

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic arthritis, Bechterew's disease (ankylosing spondylitis), gouty arthritis, osteoarthritis. It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Pain syndrome: myalgia, ossalgia, neuralgia, tendonitis, arthralgia, bursitis, radiculitis, adnexitis, otitis media, headache and toothache, pain with oncological diseases, post-traumatic and postoperative pain syndrome accompanied by inflammation.

Algodismenorea.

Contraindications:

Hypersensitivity (including to other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in anamnesis), peptic ulcer of stomach and duodenum (exacerbation), ulcerative colitis (exacerbation), diverticulitis, peptic ulcer,hemophilia and other disorders of blood coagulation, active gastrointestinal bleeding; severe renal failure (KK less than 30 ml / min), progressive kidney disease, severe hepatic insufficiency or active liver disease, condition after aortocoronary shunting, confirmed hyperkalaemia, inflammatory bowel disease, children (under 18 years), pregnancy (III trimester) , lactation period.

Carefully:Anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic liver cirrhosis, hyperbilirubinemia, liver failure, dehydration, sepsis, chronic heart failure (CHF), edema, hypertension, blood diseases (including leukopenia), stomatitis, ischemic heart disease , cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, chronic renal failure (QC 30-60 ml / min) ulcerative lesions of the gastrointestinal tract in history, the presence of Helicobacter pylori infection, prolonged use of NSAIDs, severe somatic diseases,simultaneous administration of oral glucocorticoids (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), advanced age, pregnancy (I, II trimester).

Pregnancy and lactation:

The use of ketoprofen in the I and II trimesters of pregnancy is possible only if the potential benefit to the mother exceeds the risk to the fetus.

The use of the drug in the third trimester of pregnancy is contraindicated.

If it is necessary to use ketoprofen during lactation, the question of stopping breastfeeding should be solved.

Dosing and Administration:

Intravenous, intramuscular.

Intramuscularly (in / m) - 100 mg (1 ampoule) 1-2 times a day.

Intravenous (IV) infusion administration should be performed only in a hospital setting.

A short intravenous infusion: 100-200 mg (1-2 ampoules) is dissolved in 100 ml of 0.9% sodium chloride solution and injected for 0.5-1 hour; it is possible to re-introduce after 8 hours.

Continuous intravenous infusion: 100-200 mg (1-2 ampoules) are dissolved in 500 ml of infusion solution (0.9% solution of sodium chloride, Ringer's solution,5% dextrose solution) and administered for 8 hours; it is possible to re-introduce after 8 hours.

Because of the photosensitivity, a bottle or a plastic bag with an infusion solution of ketoprofen should be wrapped with dark paper or aluminum foil.

The maximum daily dose is 200 mg.

Ketoprofen can be used in combination with analgesics of the central actions; it can be mixed with morphine in one bottle.

The drug should not be taken more than 2-3 days, if necessary - use other dosage forms.

Side effects:

From the digestive system: NSAIDs-gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, decreased appetite, diarrhea), stomatitis, impaired liver function; ulceration of the mucous membrane of the gastrointestinal tract, gingival, gastrointestinal, hemorrhoidal bleeding; change of taste.

From the nervous system: headache, dizziness, insomnia, agitation, nervousness, drowsiness, depression, asthenia, confusion or loss of consciousness, forgetfulness, migraine, peripheral neuropathy.

From the sense organs: noise or ringing in the ears, blurred vision, conjunctivitis, dry eye mucosa, eye pain, conjunctival hyperemia, hearing loss, vertigo.

From the cardiovascular system: increased blood pressure, tachycardia.

On the part of the organs of hematopoiesis: agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, leukopenia.

From the urinary system: edematous syndrome, cystitis, urethritis, renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria.

Allergic reactions: skin rash (including erythematous, urticaria), skin itching, rhinitis, angioedema, bronchospasm, exfoliative dermatitis, anaphylactic shock.

Other: increased sweating, hemoptysis, epistaxis, myalgia, muscle twitching, shortness of breath, thirst, photosensitivity, with prolonged use in large doses - vaginal bleeding.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, vomiting with blood, melena, impaired consciousness, respiratory depression, seizures, impaired renal function, renal failure.

Treatment: in case of an overdose, symptomatic therapy, monitoring of respiratory and cardiovascular activity should be carried out, use of blockers H₂-gistaminovyh receptors, inhibitors Pg. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

Pharmaceutically incompatible with tramadol solution.

Reduces the effectiveness of uricosuric medicines (drugs), enhances the effect of anticoagulants, antiaggregants, fibrinolytics, ethanol, side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

Joint use with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, an increased risk of kidney dysfunction.

Simultaneous administration with oral anticoagulants, heparin, thrombolytic agents, antiaggregants, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.

Increases hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

Increases plasma concentrations of verapamil and nifedipine, lithium preparations (Li+), methotrexate.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

The use of ketoprofen can mask the signs of an infectious disease. If the kidney and liver function is impaired, a dose reduction and careful monitoring is necessary.

To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 50 mg / ml.

Packaging:

2 ml in ampoules of light-protective neutral glass.

10 ampoules are placed in boxes of cardboard.

5 ampoules are placed in contoured cell packs from a polyvinylchloride film and aluminum foil or without aluminum foil.

1, 2 contoured cell packs are stacked in cardboard packs.

In each pack, the box is attached instructions for use, the ampullar scarifier.

Ampoule scapper does not invest when using ampoules with a kink ring or with an incision and a point.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000042

Date of registration:18.11.2010

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp30.10.2013

Illustrated instructions

Instructions

Ketoprofen (Ketoprofen)