Ketonal injection 50mg / ml 2 ml ampoules 10 pcs

Description

Composition
Active substance:
1 ampoule contains: Ketoprofen – 100 mg ;.
Excipients:
Propylene glycol – 800 mg; Ethanol – 200 mg; benzyl alcohol – 40 mg; Water for injection – up to 2 mL.
Description:
Transparent, colorless or slightly yellowish solution.
Product form:
Solution for intravenous and intramuscular administration of 50 mg / ml.
2 ml of the formulation was put in dark glass ampoules of hydrolytic class I with a point of fracture red. On the upper part of the ampoule yellow ring. Ampoule glued label.
5 or 10 vials were placed in a transparent blister open or transparent blister, coated white resin film.
2 or 5 blisters (5 vials) were placed in a cardboard box, together with instructions for medical use.
5 blisters (10 vials) were placed in a cardboard box, together with instructions for medical use (for hospitals).
Contraindications
Hypersensitivity to ketoprofen or other components of the drug as well as salicylates and other nonsteroidal anti-inflammatory drugs (NSAIDs); complete or partial combination of asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history..); gastric ulcer or duodenal ulcer in the acute stage; ulcerative colitis, Crohn’s disease; hemophilia and other bleeding disorders; children’s age (15 years); severe hepatic impairment; expressed renal insufficiency: severe renal failure (creatinine clearance (CC) of less than 30 ml / min), confirmed hyperkalemia, progressive renal disease; decompensated heart failure; postoperative period after coronary artery bypass surgery; gastrointestinal, and other cerebrovascular bleeding (bleeding or suspected); chronic dyspepsia; III trimester of pregnancy; during breastfeeding.
Precautions: peptic ulcer history, the presence of infection Helicobacter pylori; bronchial asthma in history; symptomatic cardiovascular disease, cerebrovascular disease and peripheral arterial disease; dyslipidemia, hepatic failure, hyperbilirubinemia, alcoholic cirrhosis; chronic renal failure (creatinine clearance of 30-60 ml / min); chronic heart failure, hypertension, blood diseases; Dehydration, diabetes mellitus; smoking; elderly age; prolonged use of NSAIDs, simultaneous anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), oral corticosteroids (including prednisone), selective serotonin reuptake inhibitors (including fluoxetine, paroxetine, citalopram, sertraline) (see. see “The interaction with other drugs”).
Dosage
50 mg / ml
Indications
Symptomatic treatment of pain, including in inflammatory processes of various origins: rheumatoid arthritis; seronegative arthritis, ankylosing spondylitis (Bechterew’s disease), psoriatic arthritis, reactive arthritis (Reiter’s syndrome); gout, pseudogout; degenerative diseases of the musculoskeletal system, including osteoarthritis; mild, moderate and severe pain headache, migraine, tendinitis, bursitis, myalgia, neuralgia, sciatica; posttraumatic and postoperative pain, incl accompanied by inflammation and fever..; pain in cancer syndrome; algomenorrhea.
The drug is intended for the symptomatic therapy reduce pain and inflammation at the time of use, does not affect the progression of the disease.
Interaction with other drugs
Adverse drug combination
Not recommended for the combined use of ketoprofen with other NSAIDs (including selective COX-2 inhibitors), salicylates in high doses, due to increased risk of gastrointestinal bleeding and ulceration of the gastrointestinal mucosa.
The simultaneous use of anticoagulants (heparin, warfarin), antiplatelet agents (ticlopidine, clopidogrel) increases the risk of bleeding. If the use of such a combination is unavoidable, should carefully monitor the patient.
While the use of drugs lithium may increase the concentration of lithium in the blood plasma of up to toxic values. You should carefully monitor the concentration of lithium in blood plasma and in a timely manner to adjust the dose of lithium medicines during and after treatment with NSAIDs.
Increases hematological toxicity of methotrexate, especially when used at high doses (higher than 15 mg per week). The time interval between the termination or the start of therapy and methotrexate ketoprofen should be at least 12 hours.
Combinations to be used with caution
The therapy ketoprofen patients taking diuretics, especially in the development of dehydration, have a higher risk of developing kidney failure due to a reduction in renal blood flow caused by the inhibition of prostaglandin synthesis. Before the start of the application of ketoprofen in these patients should be performed rehydration event. After the start of treatment necessary to monitor renal function.
The combined use of the drug with ACE inhibitors and angiotensin II receptor blockers in patients with impaired renal function (the dehydration, in the elderly) can lead to aggravation of renal impairment, including the development of acute renal failure.
During the first weeks, the simultaneous application of ketoprofen and methotrexate at a dose not exceeding 15 mg / week should be monitored weekly blood test. In elderly patients, or in the event of any signs of impaired renal function should be performed more frequently study.
Combinations to be taken into account
Ketoprofen may weaken the effect of antihypertensive drugs (beta-blockers, ACE inhibitors, diuretics). The simultaneous use of selective serotonin reuptake inhibitors (SSRIs) increases the risk of gastrointestinal bleeding. The simultaneous use of thrombolytic agents increases the risk of bleeding.
The simultaneous use of potassium salts, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor blockers, NSAIDs, low molecular weight heparin, cyclosporin, tacrolimus and trimethoprim increases the risk of hyperkalemia.
At simultaneous application with cyclosporine, tacrolimus possible risk of additive nephrotoxic action, especially in elderly patients.
Applying multiple antiplatelet agents (tirofiban, eptifibarid, abciximab, iloprost) increases the risk of bleeding.
Increasing the concentration in the blood plasma of cardiac glycosides, blockers “slow” calcium channels, cyclosporine, methotrexate and digoxin.
Ketoprofen may enhance the effect of oral hypoglycemic and some anticonvulsants (phenytoin).
The simultaneous use of probenecid significantly reduces the clearance of ketoprofen in plasma.
Nonsteroidal anti-inflammatory drugs may decrease the effectiveness of mifepristone. NSAIDs should be started no earlier than 8-12 days after withdrawal of mifepristone.
Pharmaceutical incompatible with a solution of tramadol because of precipitation.
Overdose
In overdose ketoprofen may experience a headache, nausea, vomiting, abdominal pain, vomiting of blood, melena, disturbance of consciousness, respiratory depression, convulsions, impaired kidney function and kidney failure.
In overdose shown gastric lavage, and the use of activated carbon. Treatment – symptomatic and supportive therapy; ketoprofen effect on the gastrointestinal tract can be reduced by means of reducing the secretion of gastric glands (e.g., proton pump inhibitors) and prostaglandins, monitoring of respiratory and cardiovascular activity, it has been detected a specific antidote, hemodialysis ineffective.
pharmachologic effect
Pharmacological group:
Nonsteroidal anti-inflammatory drug (NSAID).
Pharmacodynamics:
Ketoprofen is a non-steroidal anti-inflammatory drug. Ketoprofen has anti-inflammatory, analgesic and antipyretic action.
Ketoprofen blocks the action of the enzyme cyclooxygenase 1 and 2 (and TSOG1 TSOG2) and partially lipoxygenase, leading to the suppression of prostaglandin synthesis (including in the central nervous system, probably in the hypothalamus). Stabilizes in vitro and in vivo liposomal membrane at high concentrations in vitro ketoprofen inhibits the synthesis of leukotrienes and bradykinin. Ketoprofen has no negative impact on the status of the articular cartilage.
Pharmacokinetics:
Suction
When administered intravenously, the average plasma concentration of ketoprofen after 5 minutes from the start of the infusion and 4 min after cessation of 26.4 ± 5.4 ug / ml. Bioavailability is 90%.
For a single intramuscular administration of 100 mg of ketoprofen drug detected in plasma 15 minutes after the start of the infusion, and the peak concentration (1.3 .mu.g / ml) is achieved within 2 hours. The bioavailability of the drug increases linearly with increasing dose.
Distribution
Ketoprofen is 99% bound to plasma proteins, mainly albumin fraction. The volume of distribution in tissues was 0.1-0.2 l / kg.
Ketoprofen penetrates into the synovial fluid, and by intravenous administration of 100 mg in 3 hours it reaches a concentration of 1.5 ug / ml, which is 50% of the plasma concentration (about 3 ug / ml). After 9 hours the concentration in synovial fluid was 0.8 mg / ml, and plasma – 0.3 mcg / ml, which means that ketoprofen penetrates slowly into the synovial fluid and slower derived therefrom. Stationary plasma concentration of ketoprofen determined even after 24 hours after administration.
Following a single intramuscular administration of 100 mg of ketoprofen drug detected in cerebrospinal fluid, like blood serum after 15 min.
Metabolism
Ketoprofen undergoes extensive metabolism involving liver microsomal enzymes. It binds to glucuronic acid and excreted as glucuronide. No active metabolites of ketoprofen.
breeding
The half-life (T1 / 2) ketoprofen is 2 hours up to 80% ketoprofen excreted by the kidneys within 24 hours, mostly (> 90%) in the form of ketoprofen glucuronide, and about 10% -. through the intestine.
In patients with renal insufficiency ketoprofen displayed slower it T1 / 2 is increased at 1 hr.
In patients with hepatic insufficiency T1 / 2 increases, so it can accumulate in the tissues of ketoprofen.
Elderly patients metabolism and excretion of ketoprofen are slower, which has clinical significance only for patients with severe renal insufficiency.
Pregnancy and breast-feeding
Inhibition of prostaglandin synthesis may have an undesirable influence on the pregnancy and / or fetal development. Data obtained during epidemiological studies in the application of inhibitors of prostaglandin synthesis in early pregnancy, confirm an increased risk of miscarriage and forming heart defects (1.5%) and congenital defects of the anterior abdominal wall. The risk increases with the dose and duration of treatment.
Prescribed the drug to pregnant women in I and II trimesters of pregnancy is possible only when the benefits to the mother justifies the potential risk to the fetus. In such a case it is necessary to use the minimum effective dose short course possible.
Contraindicated the use of ketoprofen in pregnant women during the III trimester of pregnancy due to the possible development of uterine inertia uterine activity, increased bleeding time, antiplatelet effect (even when taken in small doses), as well as the effects on the fetus (cardio-pulmonary toxicity, in Vol. h. The premature closure of the ductus arteriosus and pulmonary hypertension, renal dysfunction, which may progress to renal failure with the development of low water).
To date, no data on the allocation of ketoprofen into breast milk, so the need for appointing ketoprofen nursing mothers should decide the issue of termination of breastfeeding.
Conditions of supply of pharmacies
Prescription.
side effects
According to the World Health Organization (WHO), undesirable effects are classified according to their rate of development as follows: very common (> 1/10), common (> 1/100,
special instructions
With prolonged use of NSAIDs is necessary to periodically evaluate the clinical analysis of blood and to control the function of the kidneys and liver, especially in elderly patients (65 years), to analyze the fecal occult blood. Care should be taken more frequently monitor blood pressure during application of ketoprofen to treat patients suffering from hypertension, cardiovascular diseases, which result in fluid retention.
In the event of violations of the organs of vision, treatment should be immediately discontinued.
Like other NSAIDs, ketoprofen may mask the symptoms of infectious-inflammatory diseases. In the event of evidence of infection or degradation being against application of the drug to immediately seek medical attention.
With a history of contraindications of the gastrointestinal tract (bleeding, perforation, ulcers), conducting long-term therapy and the use of high doses of ketoprofen patient should be under close medical supervision.
Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful in the appointment of ketoprofen in patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, the decrease in the volume of circulating observed blood (for example, after surgery). Use of ketoprofen can affect female fertility, so patients with infertility (including passing examination) is not recommended to apply the preparation.
During the period of the drug should be careful when driving and busy with other potentially hazardous activities that require high concentration and speed of psychomotor reactions, because the drug can cause dizziness and other side effects that may affect these abilities.
Storage conditions
Store at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Intravenously, intramuscularly.
To reduce the incidence of adverse reactions is recommended to use the minimum effective dose. The maximum daily dose is 200 mg. ratio anticipated benefits and risks must be thoroughly evaluated before the beginning of reception of ketoprofen, 200 mg / day.
Intramuscular: 100 mg (1 ampoule) 1-2 times a day.
Intravenous infusion administration of ketoprofen should be performed only in a hospital. Infusion duration should be from 0.5 to 1 hour. Intravenous route of administration should be used not more than 48 hours.
A short intravenous infusion of from 100 (200) mg of (1-2 ampoules) ketoprofen, diluted in 100 ml 0.9% sodium chloride solution is introduced for 0.5-1 hours.
Continuous intravenous infusion: 100 (200) mg of (1-2 ampoules) ketoprofen, diluted in 500 ml infusion solution (0.9% sodium chloride, lactated Ringer’s solution, 5% dextrose) is administered for 8 hours; maybe reintroduction through 8 hours. The maximum daily dose is 200 mg.
Ketoprofen may be combined with a centrally acting analgesics; it may be mixed with opioids (e.g., morphine) in the same vial, with a solution of a pharmaceutically compatible tramadol due to precipitation.
Parenteral administration Ketonal® drug can be combined with the use of oral dosage forms (tablets, capsules) or rectal suppositories.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist