Caiver solution for injections 25mg/ml in ampoules 2ml №5×2

NameCaver solution for injection/conc. for pr. inf. solution 25mg/ml in amp. 2ml in bl. in pack. No. 5×2 Main active ingredient 1 ml of solution contains 25 mg of dexketoprofen (in the form of dexketoprofen trometamol 36.9 mg) Release form Solution for injection / concentrate for infusion solution. Dosage 25 mg / ml Pharmacological properties Pharmacodynamics Dexketoprofen trometamol is a propionic acid salt that has analgesic, anti-inflammatory and antipyretic effects and belongs to the class of non-steroidal anti-inflammatory drugs (NSAIDs). The mechanism of its action is based on a decrease in the synthesis of prostaglandins due to the inhibition of cyclooxygenase. In particular, the conversion of arachidonic acid into cyclic endoperoxides PGG2 and PGH2 is inhibited, from which prostaglandins PGE1, PGE2, PGF2a, PGD2, as well as prostacyclin PGI2 and thromboxanes TxA2 and TxB2 are formed. In addition, inhibition of prostaglandin synthesis may affect other inflammatory mediators, such as kinins, which may also indirectly affect the main effect of the drug. The inhibitory effect of dexketoprofen trometamol on the activity of cyclooxygenase-1 and cyclooxygenase-2 was revealed. Clinical studies in various types of pain have shown that dexketoprofen trometamol has a pronounced analgesic effect. The analgesic effect of dexketoprofen trometamol when administered intramuscularly and intravenously to patients with pain of moderate to severe intensity was studied in various types of pain during surgical interventions (orthopedic and gynecological operations, abdominal operations), as well as in musculoskeletal pain (acute pain in the lower sections back) and renal colic. In the studies conducted, the analgesic effect of the drug began quickly and reached a maximum within the first 45 minutes. The duration of the analgesic effect after the use of dexketoprofen trometamol 50 mg is usually 8 hours. The use of the drug Kaver allows you to significantly reduce the dose of opiates when they are used simultaneously to relieve postoperative pain. Patients who were prescribed morphine for postoperative pain relief using a patient-controlled analgesia device and were also prescribed dexketoprofen trometamol, they required significantly less morphine (35-45%) than patients who received placebo. Pharmacokinetics After intramuscular administration of dexketoprofen trometamol, the maximum concentration is reached after approximately 20 minutes (10-45 minutes). It has been proven that with a single intramuscular or intravenous administration of 25-50 mg of the drug, the area under the AUC curve (“concentration – time”) is proportional to the dose. Pharmacokinetic studies of repeated use of the drug proved that AUC and Cmax (average maximum value) after the last intramuscular and intravenous administration do not differ from those after a single use, which indicates the absence of cumulation of the drug. Similar to other drugs with a high degree of binding to plasma proteins (99%), the volume of distribution of dexketoprofen averages 0.25 l / kg. The half-life is approximately 0.35 hours, and the half-life is 1-2.7 hours. The metabolism of dexketoprofen mainly occurs by conjugation with glucuronic acid and subsequent excretion by the kidneys. After the introduction of dexketoprofen trometamol in the urine, only the optical isomer S – (+) is determined, which indicates the absence of transformation of the drug into the optical isomer R – (-). After the introduction of single and multiple doses, the degree of effect of the drug on healthy elderly volunteers (over 65 years old) who took part in the study was significantly higher (up to 55%) than on young volunteers, however, there was a statistically significant difference in the maximum concentration and time of its achievement was not observed. The mean elimination half-life increased (up to 48%), and the defined total clearance decreased. Indications for use Symptomatic treatment of acute pain of moderate to severe intensity in cases where oral administration of the drug is impractical, for example, with postoperative pain, renal colic and pain in the lower back. Dosage and administrationAdults. The recommended dose is 50 mg every 8-12 hours. If necessary, a second dose is administered after 6 hours. The maximum daily dose should not exceed 150 mg. The drug is intended for short-term use, so it should be used only during acute pain (no more than 2 days). Patients should be switched to oral analgesics whenever possible. Adverse reactions can be reduced by using the lowest effective dose for the shortest possible time necessary to improve the condition. For postoperative pain of moderate or severe severity, the drug can be used according to indications in the same recommended doses in combination with opioid analgesics. Elderly patients. Dose adjustment is usually not required. However, due to the physiological decline in renal function, a lower dose is recommended, namely: the maximum daily dose is 50 mg for mild renal impairment. Liver diseases. For patients with mild or moderate liver disease (5-9 points on the Child-Pugh scale), the maximum daily dose should be reduced to 50 mg and liver function should be carefully monitored. In severe liver disease, the drug is contraindicated (10-15 points on the Child-Pugh scale). Kidney dysfunction. For patients with mild renal impairment (creatinine clearance 50-80 ml / min), the maximum daily dose should be reduced to 50 mg. In case of impaired renal function of moderate or severe degree (creatinine clearance <50 ml / min), the drug is contraindicated. Children and teenagers. The drug should not be used due to lack of data on its efficacy and safety. Intramuscular administration. The solution for injection should be slowly injected deep into the muscle. Intravenous infusion. For infusion, dilute the contents of a 2 ml ampoule in 30-100 ml of 0.9% sodium chloride solution, glucose solution or Ringer's lactate solution. The solution for infusion should be prepared under aseptic conditions, avoiding the influence of natural daylight. The prepared solution should be clear. Infusion should be carried out within 10-30 minutes. Do not allow exposure to natural daylight on the prepared solution. Caiver, diluted in 100 ml of 0.9% sodium chloride solution or glucose solution, can be mixed with dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline. Caiver solution for injection or concentrate for infusion solution must not be mixed in solution for infusion with promethazine and pentazocine. Intravenous injection (bolus injection). If necessary, the contents of 1 ampoule (2 ml solution for injection) are administered intravenously for at least 15 seconds. The drug can be mixed in small volumes (for example, in a syringe) with solutions for injection of heparin, lidocaine, morphine and theophylline. Caiver solution for injection or concentrate for the preparation of an infusion solution should not be mixed in small volumes (for example, in a syringe) with solutions of dopamine, promethazine, pentazocine, pethidine and hydroxyzine, because as a result, a precipitate forms in the solution. The drug can only be mixed with drugs that are listed above. For intramuscular or intravenous injection, the drug should be administered immediately after it has been taken from the ampoule. Solution for intravenous infusion should be used immediately after preparation. In the future, the responsibility for the conditions and duration of storage lies with the medical worker. The prepared solution retains its properties for 24 hours at a temperature of 25 ºС, provided that it is protected from exposure to daylight. When storing diluted solutions of the drug in plastic bags or in products adapted for administration made of ethyl vinyl acetate, cellulose propionate, low-density polyethylene and polyvinyl chloride, no changes in the content of the active substance due to sorption were observed. Keyver is intended for single use, so the remaining solution should be poured out. Before administering the drug, make sure that the solution is clear and colorless. A solution containing solid particles must not be used. Children and adolescents The drug should not be used in children and adolescents due to the lack of data on its efficacy and safety. Application during pregnancy and lactation The use of the drug Keyver is contraindicated in the III trimester of pregnancy and during lactation. Suppression of prostaglandin synthesis can adversely affect pregnancy and/or fetal development. According to the results of epidemiological studies, the use of drugs that suppress the synthesis of prostaglandins in early pregnancy increases the risk of miscarriage, the occurrence of heart disease in the fetus and non-closure of the anterior abdominal wall. So the absolute risk of developing anomalies of the cardiovascular system increased from <1% to about 1.5%. It is believed that the risk of such phenomena increases with an increase in the dose of the drug and the duration of therapy. The appointment of dexketoprofen trometamol in the I and II trimesters of pregnancy is possible only if absolutely necessary. If it is necessary to prescribe dexketoprofen trometamol to women planning a pregnancy, or in the I and II trimesters of pregnancy, the minimum effective dose should be used for the shortest possible duration of treatment. During the third trimester, all inhibitors of prostaglandin synthesis cause risks: for the fetus: - cardiopulmonary toxic syndrome (with premature closure of the ductus arteriosus and pulmonary hypertension); - impaired renal function, which can progress to renal failure with the development of oligohydramnios; at the end of pregnancy for mother and child: - prolongation of bleeding time (platelet aggregation suppression effect), even when using low doses; - delays in uterine contraction, which leads to delayed labor and prolonged labor. There are no data on the penetration of dexketoprofen into breast milk. Precautions Use with caution in patients with a history of allergic conditions. Avoid using Keyver in combination with other NSAIDs, including selective cyclooxygenase-2 inhibitors. Adverse reactions can be reduced by using the minimum effective dose for the shortest possible time necessary to improve the condition. Gastrointestinal bleeding, ulceration or perforation, in some cases fatal, was observed with the use of NSAIDs at different stages of treatment, regardless of the presence of precursor symptoms or a history of serious pathology from the digestive tract. With the development of gastrointestinal bleeding, the use of the drug should be discontinued. The risk of gastrointestinal bleeding, ulcer formation or perforation increases with increasing dose of NSAIDs in patients with a history of ulcer, especially complicated by bleeding or perforation, as well as in elderly patients. In elderly patients, the frequency of adverse reactions to NSAIDs is increased, especially gastrointestinal bleeding and perforation, sometimes with a fatal outcome. Treatment of such patients should begin with the lowest possible dose. NSAIDs should be used with caution in patients with a history of digestive tract diseases (ulcerative colitis, Crohn's disease), since there is a risk of their exacerbation. Before starting the use of dexketoprofen trometamol in patients with a history of esophagitis, gastritis and / or peptic ulcer, you should make sure that these diseases are in remission. In patients with existing symptoms of the pathology of the digestive tract and with a history of diseases of the digestive tract during the use of the drug, it is necessary to monitor the condition of the digestive tract for the occurrence of possible disorders, especially gastrointestinal bleeding. For such patients and patients taking low doses of acetylsalicylic acid or other drugs that increase the risk of adverse reactions from the digestive tract, combination therapy with protective drugs, such as misoprostol or proton pump inhibitors, should be considered. Patients, especially the elderly, with a history of adverse reactions from the digestive tract, it is necessary to inform the doctor about all unusual symptoms associated with the digestive system, in particular gastrointestinal bleeding, especially in the initial stages of treatment. It should be used with caution in patients who are concomitantly taking agents that increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants (eg, warfarin), selective serotonin reuptake inhibitors, or antiplatelet agents such as aspirin. Non-selective NSAIDs can reduce platelet aggregation and increase bleeding time by inhibiting prostaglandin synthesis. The concomitant use of dexketoprofen trometamol and low molecular weight heparin at prophylactic doses in the postoperative period has been studied in clinical trials, and no effect on coagulation parameters was found. However, patients taking dexketoprofen trometamol concomitantly with drugs that affect hemostasis, such as warfarin, other coumarin drugs or heparins, should be under close medical supervision. Patients with arterial hypertension and / or congestive heart failure of mild or moderate severity should be under close medical supervision due to possible fluid retention in the body and the appearance of peripheral edema. According to available clinical and epidemiological data, the use of some NSAIDs, especially at high doses and for a long time, slightly increases the risk of conditions caused by arterial thrombosis, such as myocardial infarction or stroke. There are insufficient data to exclude such a risk from the use of dexketoprofen trometamol. In uncontrolled arterial hypertension, congestive heart failure, confirmed coronary heart disease, peripheral arterial and / or cerebral vascular disease, dexketoprofen trometamol should be used only after a thorough assessment of the patient's condition. Such an assessment should also be done before starting long-term treatment in patients with risk factors for cardiovascular diseases, such as arterial hypertension, hyperlipidemia, diabetes mellitus, and smoking. There have been reports of rare cases of serious skin reactions (some fatal) with the use of NSAIDs, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. The greatest risk of their occurrence is observed in patients at the beginning of treatment, in most patients they occurred during the 1st month of therapy. If a skin rash, signs of mucosal damage, or other symptoms of hypersensitivity appear, Keyver should be withdrawn. Like all NSAIDs, the drug is able to increase the level of urea nitrogen and creatinine in blood plasma. Like other inhibitors of prostaglandin synthesis, it can cause adverse reactions from the kidneys, which can lead to glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure. Like other NSAIDs, the drug may cause a temporary slight increase in certain liver tests, as well as a significant increase in the levels of AST and ALT. With an increase in these indicators, treatment should be discontinued. Caution should be exercised when prescribing the drug to patients with impaired liver and / or kidney function, as well as to patients with arterial hypertension and / or congestive heart failure, since they may experience worsening of kidney function, fluid retention in the body and the appearance of peripheral edema during the use of NSAIDs. Due to the increased risk of nephrotoxicity, the drug should be used with caution in the treatment of diuretics, as well as in patients who may develop hypovolemia. Particular care should be taken when treating patients with a history of heart disease, including those with previous episodes of heart failure, since the risk of heart failure increases with the use of the drug. Elderly patients are more prone to impaired renal function, cardiovascular system and liver occurs in elderly patients. Caiver should be used with caution in patients with hematopoietic disorders, systemic lupus erythematosus and mixed connective tissue diseases. Like other NSAIDs, dexketoprofen trometamol is able to mask the symptoms of infectious diseases during its use. When using NSAIDs, there were reports of activation of infectious processes localized in soft tissues. Thus, if the symptoms of a bacterial infection appear or increase during use, patients are advised to immediately consult a doctor. Like all other NSAIDs, dexketoprofen trometamol can reduce female fertility, so it is not recommended for women who are planning a pregnancy. If a woman has problems conceiving or is being tested for infertility, discontinuation of the drug should be considered. The appointment of the drug in the I and II trimesters of pregnancy is possible in cases of emergency. Each ampoule of Caver contains 200 mg of ethanol, which corresponds to 5 ml of beer or 2.08 of wine per dose. The drug can adversely affect people suffering from alcoholism. The ethanol content should be taken into account when using the drug in women in the I and II trimesters of pregnancy, children and patients at risk, for example, with liver diseases, as well as patients with epilepsy. Keyver contains less than 1 mmol/dose of sodium, i.e. practically free of sodium. Interaction with other drugs The simultaneous use of the following drugs with NSAIDs is not recommended: - other NSAIDs, including high doses of salicylates (≥3 g / day). With the simultaneous use of several NSAIDs, the risk of ulcers in the digestive tract and gastrointestinal bleeding increases due to their mutual enhancement of action; anticoagulants: NSAIDs enhance the effect of anticoagulants, such as warfarin, due to the high degree of binding of dexketoprofen to plasma proteins, as well as inhibition of platelet function and damage to the mucous membrane of the stomach and duodenum. If simultaneous use is necessary, it should be carried out under close medical supervision with control of appropriate laboratory parameters; - heparin: increased risk of bleeding (due to inhibition of platelet function and damage to the mucous membrane of the stomach and duodenum). If simultaneous use is necessary, it should be carried out under the close supervision of a physician with the control of relevant laboratory parameters; - corticosteroids: increased risk of ulcers in the digestive tract and gastrointestinal bleeding; - lithium (there have been reports of several NSAIDs): NSAIDs increase the level of lithium in the blood, which can lead to intoxication (decreased excretion of lithium by the kidneys). Therefore, at the beginning of the use of dexketoprofen, when adjusting the dose or discontinuing the drug, it is necessary to control the level of lithium in the blood; - methotrexate in high doses (more than 15 mg per week). By reducing the renal clearance of methotrexate against the background of the use of NSAIDs in general, its negative effect on the blood system is enhanced; hydantoin derivatives and sulfonamides: possible increased toxicity of these substances. The simultaneous use of the following drugs with NSAIDs requires caution: diuretics, angiotensin-converting enzyme (ACE) inhibitors, antibacterial drugs from the aminoglycoside group and angiotensin II receptor antagonists. Dexketoprofen reduces the effectiveness of diuretics and other antihypertensive agents. In some patients with impaired renal function (eg, dehydration or the elderly), the use of cyclooxygenase inhibitors concomitantly with ACE inhibitors, angiotensin II receptor antagonists, or aminoglycosides may worsen renal function, which is usually reversible. When using dexketoprofen together with any diuretic, make sure that the patient is not dehydrated, and at the beginning of treatment it is necessary to monitor kidney function; - methotrexate in low doses (less than 15 mg per week): due to a decrease in the renal clearance of methotrexate against the background of the use of NSAIDs, its negative effect on the blood system as a whole increases. In the first weeks of simultaneous use, it is necessary to conduct a weekly blood test. Even with a slight impairment of kidney function, as well as in elderly patients, treatment should be carried out under the strict supervision of a physician; – pentoxifylline: there is a risk of bleeding. It is necessary to strengthen control and check the bleeding time indicator more often; - zidovudine: there is a risk of increased toxic effects on erythrocytes due to the effect on reticulocytes, which after the 1st week of NSAID use leads to severe anemia. Within 1-2 weeks after the start of the use of NSAIDs, a blood test should be done and the content of reticulocytes should be checked; - sulfonylurea drugs: NSAIDs can enhance the hypoglycemic effect of these drugs by replacing them in compounds with blood plasma proteins. Possible interactions should be taken into account when using the following agents: - beta-blockers: NSAIDs can weaken their hypotensive effect by inhibiting the synthesis of prostaglandins; cyclosporine and tacrolimus: possible increased nephrotoxicity due to the effect of NSAIDs on renal prostaglandins. In combination therapy, renal function should be monitored; thrombolytic agents: increased risk of bleeding; antiplatelet agents and selective serotonin reuptake inhibitors: increased risk of gastrointestinal bleeding; probenecid: an increase in the concentration of dexketoprofen in the blood plasma is possible, which is probably due to inhibition of tubular secretion and conjugation of the drug with glucuronic acid and requires dose adjustment of dexketoprofen; cardiac glycosides: NSAIDs can increase the concentration of glycosides in blood plasma; mifepristone: due to the theoretical likelihood of a decrease in the effectiveness of mifepristone under the influence of prostaglandin synthetase inhibitors, NSAIDs should be prescribed only 8-12 days after mifepristone therapy; quinolone: Animal studies have shown that high doses of quinolone derivatives in combination with NSAIDs increase the risk of seizures. Contraindications - Hypersensitivity to dexketoprofen, any other non-steroidal anti-inflammatory drug (NSAID) or excipients of the drug; - the drug is contraindicated if substances of a similar effect, for example, acetylsalicylic acid or other NSAIDs, provoke the development of asthma attacks, bronchospasm, acute rhinitis or cause the development of nasal polyps, the appearance of urticaria or angioedema; - active phase of peptic ulcer or bleeding, suspicion of them, recurrent peptic ulcer or bleeding in history (at least two confirmed facts of ulcer or bleeding); - gastrointestinal bleeding, other bleeding in the active phase or increased bleeding; history of gastrointestinal bleeding or perforation associated with previous NSAID therapy; - Crohn's disease or ulcerative colitis; - history of bronchial asthma; - severe heart failure; - impaired renal function of moderate or severe degree (creatinine clearance <50 ml / min); - severe liver dysfunction (10-15 points on the Child-Pugh scale); - hemorrhagic diathesis and other blood clotting disorders; use for the purpose of neuraxial (intrathecal or epidural) administration (due to the ethanol content). Active ingredient: 1 ml of solution contains 25 mg of dexketoprofen (in the form of dexketoprofen trometamol 36.9 mg); excipients: ethanol 96%, sodium chloride, sodium hydroxide, water for injection. Overdose Symptoms of overdose are unknown. Similar drugs cause disorders of the digestive tract (vomiting, anorexia, abdominal pain) and the nervous system (drowsiness, dizziness, disorientation, headache). In case of accidental overdose, symptomatic treatment should be started immediately in accordance with the patient's condition. Dexketoprofen trometamol is removed from the body by dialysis. Side effects Possible development of peptic ulcer, perforation or gastrointestinal bleeding, sometimes fatal, especially in elderly patients. According to available data, against the background of the use of the drug, nausea, vomiting, diarrhea, flatulence, constipation, dyspepsia, abdominal pain, melena, vomiting with blood, ulcerative stomatitis, exacerbation of colitis and Crohn's disease may occur. Rarely observed gastritis. Edema, arterial hypertension and heart failure have also been noted, which can be caused by taking NSAIDs. As with other NSAIDs, the following adverse reactions are possible: aseptic meningitis, which occurs in patients with systemic lupus erythematosus or mixed connective tissue diseases, and reactions from the blood (purpura, aplastic and hemolytic anemia, rarely - agranulocytosis and bone marrow hypoplasia) . Bullous reactions are possible, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rare). According to clinical trials and epidemiological data, the use of some NSAIDs, especially at high doses and for a long time, slightly increases the risk of developing pathologies caused by arterial thrombosis, such as myocardial infarction and stroke. Storage conditions Store in the original package to protect from light at a temperature not exceeding 25 ° C. Keep out of the reach of children. Buy Caver injection solution 25mg/ml in 2ml ampoules No. 5x2 Price for Caver injection solution 25mg/ml in 2ml ampoules No. 5x2