Dexalgin solution for injection 25mg / ml, 2ml No. 10

• Relief of pain syndrome of various origins (including postoperative, post-traumatic pain, pain in bone metastases, 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).

V / v, v / m.

The recommended dose for adults: 50 mg every 8-12 hours. If necessary, the drug may be re-administered at intervals of 6 hours. The daily dose is 150 mg.

In elderly patients and patients with impaired liver and / or kidney function, therapy with DexalginЃ should be started with lower doses; the daily dose is 50 mg.

DexalginЃ is intended for short-term (no more than 2 days) use during the period of acute pain syndrome. In the future, it is possible to transfer the patient to oral analgesics.

The technique of carrying out i / m injection. Contents 1 amp. (2 ml) is slowly injected deep into the / m.

IV injection technique. If necessary, contents of 1 amp. (2 ml) DexalginЃ can be administered by slow intravenous injection for at least 15 seconds.

IV infusion technique. Contents 1 amp. (2 ml) is diluted in 30-100 ml of physiological solution, glucose solution or Ringer's solution (lactate). The solution should be prepared aseptically and protected from daylight at all times. The diluted solution (should be clear) is administered by slow intravenous infusion for 10Ц30 minutes.

Solution for intravenous and intramuscular administration

1 amp.

active substance:

dexketoprofen trometamol 73.8 mg (corresponds to 50 mg dexketoprofen)

excipients: ethanol 96% - 200 mg; sodium chloride - 8 mg; sodium hydroxide - up to pH 7.4; water for injection - up to 2 ml

• Hypersensitivity to dexketoprofen or other NSAIDs, or any of the excipients that make up the drug;

• 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 (Cl creatinine <50 ml / min);

• bronchial asthma (including history);

• severe heart failure;

• treatment of pain in coronary artery bypass grafting;

• hemorrhagic diathesis or other coagulation disorders;

• childhood.

DexalginЃ is contraindicated for neuraxial (epidural or intrathecal, intrathecal) administration due to the ethanol contained in the drug.

With care: history of allergic conditions; violation of the hematopoietic system; systemic lupus erythematosus or mixed connective tissue diseases; simultaneous therapy with other drugs (see 'Interaction'); predisposition to hypovolemia; coronary heart disease; advanced age (over 65).

pharmachologic effect

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. The 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. When combined therapy with opioid analgesics, dexketoprofen trometamol significantly (up to 30-45%) reduces the need for opioids.

Pharmacokinetics

Suction

After intramuscular administration of dexketoprofen trometamol, Cmax in the blood serum is reached after an average of 20 minutes (10-45 minutes). AUC after a single injection at a dose of 25-50 mg is dose proportional, both with i / m and i / v. The corresponding pharmacokinetic parameters are similar after a single and repeated intramuscular or intravenous administration, which indicates the absence of drug accumulation. Distribution Dexketoprofen trometamol is characterized by a high level of binding to plasma proteins (99%). The average Vd value is less than 0.25 l / kg, the half-distribution time is about 0.35 hours. Elimination The main route of dexketoprofen elimination is its conjugation with glucuronic acid followed by renal excretion. T1 / 2 of dexketoprofen trometamol is about 1-2.7 hours.

Pharmacokinetics in special clinical situations

In elderly people, there is an increase in the duration of T1 / 2 (both after a single and after repeated intramuscular or intravenous administration) on average up to 48% and a decrease in the total clearance of the drug.

Side effect

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 gastrointestinal 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 - menstrual irregularities, in men - dysfunction of the prostate gland.

From the musculoskeletal system: rarely - muscle spasm, difficulty in movement 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, facial edema.

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).

Application during pregnancy and lactation

The use of the drug DexalginЃ during pregnancy and lactation is contraindicated.

Application for violations of liver function

The drug is contraindicated in severe liver dysfunction (10-15 points on the Child-Pugh scale). In patients with milder liver dysfunctions, Dexalgin therapy should be started with lower doses; the daily dose is 50 mg.

Application for impaired renal function

The drug is contraindicated in severe renal impairment (CC <50 ml / min). In patients with milder renal impairment, Dexalgin therapy should be started with lower doses; the daily dose is 50 mg.

Application in children

Contraindication: childhood.

Use in elderly patients

The drug should be used with caution in elderly patients (over 65 years old).

special instructions

Patients with a history of digestive disorders or gastrointestinal diseases require constant monitoring. In the event of gastrointestinal bleeding or ulcerative lesions, therapy with DexalginЃ should be canceled. Because All NSAIDs can inhibit platelet aggregation and increase bleeding time due to slowing down the synthesis of prostaglandins; in controlled clinical trials, the simultaneous administration of dexketoprofen trometamol and low molecular weight heparin preparations in prophylactic doses in the postoperative period was studied. No effect on coagulation parameters was observed. However, with the simultaneous administration of DexalginЃ with other drugs that affect blood clotting, careful medical monitoring is required. Like other NSAIDs,DexalginЃ can lead to an increase in plasma creatinine and nitrogen levels. Like other inhibitors of prostaglandin synthesis, DexalginЃ can have side effects on the urinary system, which can lead to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure. Against the background of therapy with DexalginЃ, like 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, DexalginЃ should be canceled. Like other NSAIDs, dexketoprofen trometamol can mask the symptoms of infectious diseases.In the event of symptoms of a bacterial infection or deterioration of health during therapy with DexalginЃ, the patient should inform the doctor about it. Each ampoule of DexalginЃ contains 200 mg of ethanol. Influence on the ability to drive vehicles and control mechanisms Due to possible dizziness and drowsiness during treatment with DexalginЃ, the ability to concentrate and the speed of psychomotor reactions may decrease.Influence on the ability to drive vehicles and control mechanisms Due to possible dizziness and drowsiness during treatment with DexalginЃ, the ability to concentrate and the speed of psychomotor reactions may decrease.Influence on the ability to drive vehicles and control mechanisms Due to possible dizziness and drowsiness during treatment with DexalginЃ, the ability to concentrate and the speed of psychomotor reactions may decrease.

Overdose

Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia. Treatment: symptomatic therapy; if necessary, gastric lavage, dialysis.

Drug interactions

The following drug interactions are typical for all NSAIDs, including DexalginЃ. Undesirable combinations The simultaneous administration of several NSAIDs, including salicylates in high doses (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 ones, 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.and more) there is an increase in the hematological toxicity of methotrexate due to a decrease in its renal clearance during NSAID therapy. With simultaneous use with hydantoins and sulfa drugs, there is a risk of increasing the toxic effect of these drugs. Combinations requiring caution If it is necessary to use it simultaneously with diuretics, ACE inhibitors, it should be borne in mind that NSAID therapy is associated with the risk of developing acute renal failure in patients with dehydration (decreased glomerular filtration due to inhibition of prostaglandin synthesis). NSAIDs can reduce the antihypertensive effect of some drugs. When administered simultaneously with diuretics, it is necessary to make sure that the patient's water balance is adequate, and to monitor renal function before prescribing NSAIDs.With simultaneous use with methotrexate in low doses (less than 15 mg / week), an increase in the hematological toxicity of methotrexate is possible 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 concurrent 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 necessary. With simultaneous use with zidovudine, there is a risk of an increase in the toxic effect on erythrocytes due to exposure to reticulocytes, with the development of severe anemia a week after the appointment of NSAIDs.It is necessary to control all blood cells and reticulocytes after 1-2 weeks. after starting NSAID therapy. It is possible that the hypoglycemic effect of sulfonylurea derivatives is enhanced due to its displacement from the sites of binding to plasma proteins under the influence of NSAIDs. With simultaneous use with drugs of low molecular weight heparin, the risk of bleeding increases. Combinations that must be taken into account NSAIDs can reduce the hypotensive effect of beta-blockers, which is 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 administration 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 changes in the effectiveness of mifepristone under the influence of inhibitors of prostaglandin synthesis, NSAIDs should not be prescribed earlier than 8-12 days after discontinuation of mifepristone. The data obtained in experimental studies on animals indicate a high risk of developing convulsions when prescribing NSAIDs during therapy with high doses of ciprofloxacin. Pharmaceutical interactions DexalginЃ should not be mixed in one syringe with a solution of dopamine, promethazine, pentazocine, pethidine or hydroxyzine (a precipitate is formed).DexalginЃ can be mixed in one syringe with a solution of heparin, lidocaine, morphine and theophylline. The diluted solution of the drug DexalginЃ for infusion must not be mixed with promethazine or pentazocine. Diluted solution of DexalginЃ for infusion is compatible with the following injection solutions: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline. When storing diluted solutions of DexalginЃ for infusion in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride, the absorption of the active substance by the listed materials does not occur.The diluted solution of the drug DexalginЃ for infusion should not be mixed with promethazine or pentazocine. Diluted solution of DexalginЃ for infusion is compatible with the following injection solutions: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline. When storing diluted solutions of DexalginЃ for infusion in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride, the absorption of the active substance by the listed materials does not occur.The diluted solution of the drug DexalginЃ for infusion should not be mixed with promethazine or pentazocine. Diluted solution of the drug DexalginЃ for infusion is compatible with the following injection solutions: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline. When storing diluted solutions of DexalginЃ for infusion in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride, the absorption of the active substance by the listed materials does not occur.When storing diluted solutions of DexalginЃ for infusion in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride, the absorption of the active substance by the listed materials does not occur.When storing diluted solutions of DexalginЃ for infusion in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride, the absorption of the active substance by the listed materials does not occur.