Dexalgin injection solution for injections 25mg/ml in ampoules 2ml №5

Name:
Dexalgin injection solution for in./conc. d / adj. inf. solution 25mg/ml in amp. 2 ml in pack. No. 5
Description:
The solution for intravenous and intramuscular administration is transparent, colorless, with a characteristic odor of alcohol. The main active ingredient Dexketoprofen Release form The solution for intravenous and intramuscular administration is transparent, colorless, with a characteristic odor of alcohol. 2 ml – dark glass ampoules (5) – plastic trays (1) – cardboard packs. Special instructions In patients with disorders of the digestive system or a history of gastrointestinal diseases, constant monitoring is necessary. In the event of gastrointestinal bleeding or ulcerative lesions, therapy with Dexalgin® should be discontinued. Because all NSAIDs can inhibit platelet aggregation and increase bleeding time due to a slowdown in prostaglandin synthesis, in controlled clinical trials, the simultaneous administration of dexketoprofen trometamol and prophylactic doses of low molecular weight heparin in the postoperative period was studied. No effect on coagulation parameters was observed. However, while prescribing Dexalgin® with other drugs that affect blood clotting, careful medical monitoring is necessary. Like other NSAIDs, Dexalgin® can lead to an increase in plasma creatinine and nitrogen levels. Like other inhibitors of prostaglandin synthesis, Dexalgin® can have a side effect on the urinary system, which can lead to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure. During therapy with Dexalgin®, as with other NSAIDs, there may be a slight transient increase in some hepatic parameters, as well as a significant increase in the level of AST and ALT in the blood serum. At the same time, monitoring of liver and kidney functions is necessary in elderly patients. In case of a significant increase in the corresponding indicators, Dexalgin® should be canceled. Like other NSAIDs, dexketoprofen trometamol may mask the symptoms of infectious diseases. In case of symptoms of a bacterial infection or deterioration of health during therapy with Dexalgin®, the patient should inform the doctor about this. Each ampoule of Dexalgin® contains 200 mg of ethanol. Influence on the ability to drive vehicles and control mechanisms In connection with possible dizziness and drowsiness during treatment with Dexalgin®, a decrease in the ability to concentrate and speed of psychomotor reactions is possible. Pharmacological action Non-steroidal anti-inflammatory drug (NSAID). It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis at the level of COX-1 and COX-2. Analgesic effect occurs 30 minutes after parenteral administration. The duration of the analgesic effect after administration at a dose of 50 mg is 4-8 hours. In combination therapy with opioid analgesics dexketoprofen, trometamol significantly (up to 30-45%) reduces the need for opioids. PharmacokineticsAbsorption After intramuscular administration of dexketoprofen trometamol, Cmax in serum is reached after an average of 20 minutes (10-45 minutes). AUC after a single dose of 25-50 mg is dose-proportional, both intramuscularly and intravenously. The corresponding pharmacokinetic parameters are similar after single and repeated intramuscular or intravenous administration, which indicates the absence of cumulation of the drug. Distribution Dexketoprofen trometamol has a high level of plasma protein binding (99%). The average value of Vd is less than 0.25 l / kg, the half-life is about 0.35 hours. Withdrawal The main route of elimination of dexketoprofen is its conjugation with glucuronic acid, followed by excretion by the kidneys. T1 / 2 of dexketoprofen trometamol is about 1-2.7 hours. Pharmacokinetics in special clinical situations In the elderly, there is an increase in the duration of T1 / 2 (both after a single and after repeated intramuscular or intravenous administration) to an average of 48% and a decrease in the total clearance of the drug. Indications for use – relief of pain syndrome of various origins (including postoperative pain, pain with bone metastases, post-traumatic pain, pain with renal colic, algomenorrhea, sciatica, sciatica, neuralgia, toothache); – symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, spondyloarthritis, arthrosis, osteochondrosis). Dosage and administration Dexalgin® is intended for intravenous and intramuscular administration. Recommended dose for adults: 50 mg every 8-12 hours. If necessary, it is possible to re-administer the drug with a 6-hour interval. The daily dose is 150 mg. In elderly patients and patients with impaired liver and / or kidney function, therapy with Dexalgin should be started with lower doses; the daily dose is 50 mg. Dexalgin® is intended for short-term (no more than 2 days) use during an acute pain syndrome. In the future, it is possible to transfer the patient to analgesics for oral administration. Rules for the preparation and administration of solutions The contents of one ampoule (2 ml) are slowly injected deep into the / m. The contents of one ampoule (2 ml) are administered by slow intravenous injection for at least 15 seconds. The contents of one ampoule (2 ml) are diluted in 30-100 ml of physiological saline, glucose solution or Ringer’s solution (lactate). The solution should be prepared under aseptic conditions and always protected from exposure to daylight. The diluted solution (should be clear) is administered by slow IV infusion over 10-30 minutes. Use during pregnancy and lactation The use of the drug Dexalgin® during pregnancy and lactation is contraindicated. Precautions The drug should be used with caution in a history of allergic conditions; violations of the hematopoietic system; with SLE or mixed connective tissue diseases; simultaneously with other drugs; in case of predisposition to hypovolemia; with ischemic heart disease; in elderly patients (over 65 years of age). Interaction with other drugs The following drug interactions are typical for all NSAIDs, including Dexalgin®. Undesirable combinations The simultaneous appointment of several NSAIDs, including high doses of salicylates (more than 3 g / day) increases the risk of gastrointestinal bleeding and ulcers due to synergistic action. With simultaneous use with oral anticoagulants, heparin in doses exceeding prophylactic doses, and ticlopidine, the risk of bleeding increases due to inhibition of platelet aggregation and damage to the gastrointestinal mucosa. NSAIDs increase the concentration of lithium in the blood plasma, up to toxic, and therefore this indicator must be monitored when prescribing, changing the dose, and after discontinuing NSAIDs. When used with methotrexate in high doses (15 mg / week or more), there is an increase in hematological toxicity of methotrexate due to a decrease in its renal clearance during NSAID therapy. With simultaneous use with hydantoins and sulfanilamide drugs, there is a risk of increasing the toxic effect of these drugs. Combinations requiring caution If simultaneous use with diuretics, ACE inhibitors is necessary, it should be borne in mind that NSAID therapy is associated with a risk of developing acute renal failure in patients with dehydration (decrease in glomerular filtration due to inhibition of prostaglandin synthesis). NSAIDs may reduce the hypotensive effect of some drugs. When co-administered with diuretics, it is necessary to ensure that the patient’s water balance is adequate and to monitor renal function before prescribing NSAIDs. With simultaneous use with low doses of methotrexate (less than 15 mg / week), it is possible to increase the hematological toxicity of methotrexate due to a decrease in its renal clearance during NSAID therapy. It is necessary to monitor the number of blood cells weekly in the first weeks of simultaneous therapy. In the presence of impaired renal function, even in a mild degree, as well as in the elderly, careful medical supervision is necessary. With simultaneous use with pentoxifylline, the risk of bleeding increases. Intensive clinical monitoring and frequent monitoring of bleeding time (blood clotting time) is required. With simultaneous use with zidovudine, there is a risk of increased toxic effects on erythrocytes due to effects on reticulocytes, with the development of severe anemia a week after the appointment of NSAIDs. It is necessary to control all blood cells and reticulocytes in 1-2 weeks. after initiation of NSAID therapy. It is possible to increase the hypoglycemic effect of sulfonylurea derivatives due to its displacement from the binding sites with plasma proteins under the influence of NSAIDs. With simultaneous use with drugs of low molecular weight heparin, the risk of bleeding increases. Combinations to be considered NSAIDs may reduce the hypotensive effect of beta-blockers due to inhibition of prostaglandin synthesis. When used simultaneously with cyclosporine and tacrolimus, NSAIDs can increase nephrotoxicity, which is mediated by the action of renal prostaglandins. During combination therapy, it is necessary to monitor renal function. With simultaneous appointment with thrombolytics, the risk of bleeding increases. With simultaneous use with probenecid, an increase in plasma concentrations of NSAIDs is possible, which may be due to inhibition of renal secretion and / or conjugation with glucuronic acid. This requires dose adjustment of NSAIDs. NSAIDs can cause an increase in the concentration of cardiac glycosides in the blood plasma. Due to the theoretical risk of changing the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors, NSAIDs should not be prescribed earlier than 8-12 days after mifepristone is discontinued. Data obtained in experimental animal studies indicate a high risk of convulsions in the appointment of NSAIDs during therapy with high doses of ciprofloxacin. Pharmaceutical Interactions Dexalgin® must not be mixed in the same syringe with a solution of dopamine, promethazine, pentazocine, pethidine or hydroxyzine (a precipitate forms). Dexalgin® can be mixed in one syringe with a solution of heparin, lidocaine, morphine and theophylline. A diluted solution of Dexalgin® for infusion must not be mixed with promethazine or pentazocine. The diluted solution of Dexalgin® for infusion is compatible with the following injection solutions: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline. When storing diluted solutions of Dexalgin® for infusion in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low-density polyethylene or polyvinyl chloride, absorption of the active substance by the listed materials does not occur. Contraindications – peptic ulcer of the stomach and duodenum; – history of gastrointestinal bleeding, other active bleeding (including suspected intracranial bleeding), anticoagulant therapy; – gastrointestinal diseases (Crohn’s disease, ulcerative colitis); – severe liver dysfunction (10-15 points on the Child-Pugh scale); – severe renal dysfunction (CC < 50 ml / min); - bronchial asthma (including history); - severe heart failure; — treatment of pain syndrome in coronary artery bypass grafting; - hemorrhagic diathesis or other coagulation disorders; - childhood; - hypersensitivity to dexketoprofen or other NSAIDs or to any of the excipients that make up the drug. Contraindicated for epidural, intrathecal or intrathecal administration due to the ethanol present in the preparation. Composition In 1 ml of dexketoprofen trometamol 36.9 mg (1 amp. 73.8 mg), which corresponds to the content of dexketoprofen 25 mg 50 mg Excipients: ethanol 96% - 200 mg, sodium chloride - 8 mg, sodium hydroxide - up to pH 7.4, water for injection - up to 2 ml. Overdose Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia. Treatment: symptomatic therapy; if necessary - gastric lavage, dialysis. Side effect The frequency of side effects: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%, including individual reports). From the hematopoietic system: rarely - anemia; very rarely - neutropenia, thrombocytopenia. From the side of the central nervous system: infrequently - headache, dizziness, insomnia, drowsiness; rarely - paresthesia. From the senses: infrequently - blurred vision; rarely - tinnitus. From the side of the cardiovascular system: infrequently - arterial hypotension, a feeling of heat, hyperemia of the skin; rarely - extrasystole, tachycardia, arterial hypertension, peripheral edema, superficial thrombophlebitis. From the respiratory system: rarely - bradypnea; very rarely - bronchospasm, dyspnea. From the digestive system: often - nausea, vomiting; infrequently - abdominal pain, dyspepsia, diarrhea, constipation, hematemesis, dry mouth; rarely - erosive and ulcerative lesions of the digestive tract, including bleeding and perforation, anorexia, increased activity of liver enzymes, jaundice; very rarely - damage to the pancreas, liver damage. From the urinary system: rarely - polyuria, renal colic; very rarely - nephritis or nephrotic syndrome. On the part of the reproductive system: rarely - in women - a violation of the menstrual cycle, in men - a violation of the function of the prostate gland. From the musculoskeletal system: rarely - muscle spasm, difficulty moving in the joints. Dermatological reactions: sometimes - dermatitis, rash, sweating; rarely - acne; very rarely - photosensitivity. Allergic reactions: rarely - urticaria; very rarely - severe skin reactions (Stevens-Johnson syndrome, Lyell's syndrome), angioedema, allergic dermatitis. From the side of metabolism: rarely - hyperglycemia, hypoglycemia, hypertriglyceridemia. On the part of laboratory parameters: rarely - ketonuria, proteinuria. Local and general reactions: often - pain at the injection site; infrequently - an inflammatory reaction, hematoma, hemorrhages at the injection site, a feeling of heat, chills, fatigue; rarely - back pain, fainting, fever; very rarely - anaphylactic shock, swelling of the face. Others: aseptic meningitis, which occurs mainly in patients with systemic lupus erythematosus or mixed connective tissue diseases, hematological disorders (purpura, aplastic and hemolytic anemia, rarely - agranulocytosis and bone marrow hypoplasia). Storage conditions The drug should be stored out of the reach of children, protected from light place at a temperature not exceeding 25°C. Buy Dexalgin injection solution for injection 25mg/ml in ampoules 2ml №5