Composition, form of production and packaging
The solution for intravenous and / or injection is clear, colorless, with a characteristic smell of alcohol.
1 ml of 1 amp.
dexketoprofen trometamol 36.9 mg 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 d / u - up to 2 ml.
2 ml - dark glass ampoules (1) - plastic pallets (1) - cardboard packs.
2 ml - ampoules of dark glass (5) - plastic pallets (1) - cardboard packs.
2 ml - dark glass ampoules (10) - plastic pallets (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Non-steroidal anti-inflammatory drug (NSAID). Has analgesic, anti-inflammatory and antipyretic effect. 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 in a dose of 50 mg is 4-8 hours.
With combined therapy with opioid analgesics of dexketoprofen, trometamol significantly (to 30-45%) reduces the need for opioids.
After the / m administration of dexketoprofen trometamol C max in the blood serum is achieved on average after 20 min (10-45 min). AUC after a single injection in a dose of 25-50 mg is proportional to the dose, both with / m and with iv introduction. The corresponding pharmacokinetic parameters are similar after a single and repeated IM or IV injection, which indicates the absence of cumulation of the drug.
For dexketoprofen, trometamol is characterized by a high level of binding to plasma proteins (99%). The average value of V d is less than 0.25 l / kg, half-distribution time is about 0.35 h.
The main way of eliminating dexketoprofen is its conjugation with glucuronic acid followed by excretion by the kidneys. T 1/2 of dexketoprofen trometamol is about 1-2.7 hours.
Pharmacokinetics in special clinical cases
In elderly people, an increase in the duration of T 1/2 (either after a single dose or after repeated IM or IV injection) is observed on an average of 48% and a decrease in the overall clearance of the drug.
- relief of pain syndrome of various genesis (including postoperative pain, pain in bone metastases, posttraumatic pain, pain in renal colic, algodismenorea, sciatica, radiculitis, neuralgia, toothache);
- symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, spondyloarthritis, arthrosis, osteochondrosis).
Dexalgin В® is intended for intravenous and / or intravenous administration.
The recommended adult dose is 50 mg every 8-12 hours. If necessary, repeated administration of the drug with a 6-hour interval is possible. The daily dose is 150 mg.
In elderly patients and patients with impaired liver and / or kidney function, therapy with Dexalgin В® should be started with lower doses; the daily dose is 50 mg.
Dexalgin В® is intended for short-term (no more than 2 days) use during acute pain syndrome. In the future, the patient can be transferred to analgesics for oral administration.
Rules for the preparation and administration of solutions
The contents of one ampoule (2 ml) are slowly injected deeply into the / m .
The contents of one ampoule (2 ml) is administered by slow intravenous injection for a duration of at least 15 seconds.
The contents of one ampoule (2 ml) are diluted in 30-100 ml of physiological solution, glucose solution or Ringer's solution (lactate). The solution should be prepared under aseptic conditions and always protected from daylight. The diluted solution (should be transparent) is administered by slow intravenous infusion with aduration of 10-30 minutes.
Frequency of side effects development: often (1-10%), infrequently (0.1-1%) rarely (0.01-0.1%), very rarely (less than 0.01%, including individual reports).
From the hemopoietic 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 - noise in the ears.
From 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 - bradypnoe; very rarely - bronchospasm, dyspnoea.
On the part of 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 hepatic enzymes, jaundice; very rarely - the defeat of 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 menstrual cycle, in men - a violation of the function of the prostate.
From the musculoskeletal system: rarely - muscle spasm, difficulty in movement in the joints.
Dermatological reactions: sometimes - dermatitis, rash, sweating; rarely - acne; very rarely photosensitization.
Allergic reactions: rarely - hives; 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 indicators: rarely - ketonuria, proteinuria.
Local and general reactions: often - pain at the injection site; infrequently - 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.
Other: aseptic meningitis, which occurs predominantly in patients with systemic lupus erythematosus or mixed connective tissue diseases, hematologic disorders (purpura, aplastic and hemolytic anemia, rarely - agranulocytosis and bone marrow hypoplasia).
- Stomach ulcer and duodenal ulcer;
- gastrointestinal hemorrhages in the anamnesis, other active bleeding (including suspicion of intracranial bleeding), anticoagulant therapy;
- gastrointestinal diseases (Crohn's disease, ulcerative colitis);
- severe violations of the liver (10-15 points on the scale Child-Pugh);
- severe renal dysfunction (CK <50 ml / min);
- bronchial asthma (including in the anamnesis);
- severe heart failure;
- Treatment of pain syndrome in aortocoronary shunting;
- hemorrhagic diathesis or other coagulation disorders;
- 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 in the formulation.
With caution should apply the drug in allergic conditions in history; violations of the hematopoiesis system; with SLE or mixed connective tissue diseases;concomitantly with other medications; in case of predisposition to hypovolemia; with IHD; in elderly patients (over 65 years).
PREGNANCY AND LACTATION
The use of the drug Dexalgin В® during pregnancy and during lactation is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated in cases of severe renal dysfunction (KK <50 ml / min).
Have patients with more mild impairment of renal function, Dexalgin should be started with lower doses; the daily dose is 50 mg.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated in severe violations of liver function (10-15 points on the scale Child-Pugh).
In patients with more mild violations of liver function, Dexalgin should be started with lower doses; the daily dose is 50 mg.
APPLICATION FOR CHILDREN
Contraindication: children's age.
APPLICATION IN ELDERLY PATIENTS
With caution should be used in elderly patients (over 65 years).
In patients with disorders of the digestive system or gastrointestinal diseases in a history, continuous monitoring is necessary. In the event of gastrointestinal bleeding or ulcerative lesions, DexalginВ® treatment should be discontinued.
Because all NSAIDs can inhibit platelet aggregation and increase bleeding time due to a slowdown in 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 the drug Dexalgin В® with other drugs that affect blood clotting, careful medical control is necessary.
Like other NSAIDs, DexalginВ® can lead to increased levels of creatinine and nitrogen in the blood plasma. Like other inhibitors of prostaglandin synthesis, DexalginВ® may 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.
Against the background of therapy with the drug Dexalgin В® , as well as 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, control of liver and kidney functions is necessary in elderly patients. In the case of a significant increase in the corresponding indicators, DexalginВ® should be canceled.
Like other NSAIDs, dexketoprofen trometamol can mask the symptoms of infectious diseases. In case of symptoms of bacterial infection or worsening of well-being on the background of therapy with Dexalgin В® the patient should inform the doctor about it.
Each ampoule of DexalginВ® contains 200 mg of ethanol.
Impact on the ability to drive vehicles and manage mechanisms
In connection with the possible dizziness and drowsiness on the background of treatment with the drug Dexalgin В® , a decrease in the ability to concentrate and speed of psychomotor reactions is possible.
Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia.
Treatment: symptomatic therapy; if necessary, gastric lavage, dialysis.
The following drug interaction is typical for all NSAIDs, including DexalginВ®.
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 at doses exceeding preventive, and ticlopidine increases the risk of bleeding due to inhibition of platelet aggregation and damage to the gastrointestinal mucosa.
NSAIDs increase the concentration of lithium in the blood plasma, down to toxic, and therefore this indicator should be monitored when appointing, changing the dose and after the abolition of NSAIDs.
When applied 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 against the background of therapy with NSAIDs.
At simultaneous application with hydantoins and sulfanilamide preparations there is a risk of intensifying the toxic effect of these drugs.
Combinations that require caution
If simultaneous use with diuretics, ACE inhibitors is necessary, it should be taken into account that NSAID therapy is associated with the risk of acute renal failure in patients with dehydration (reduced glomerular filtration due to oppression of prostaglandin synthesis). NSAIDs can reduce the hypotensive effect of certain drugs.With simultaneous appointment with diuretics, it is necessary to make sure that the patient's water balance is adequate, and to monitor the kidney function before prescribing NSAIDs.
When used simultaneously with methotrexate in low doses (less than 15 mg / week), it is possible to increase the hematological toxicity of methotrexate due to a decrease in its renal clearance against the background of therapy with NSAIDs. It is necessary to monitor the number of blood cells weekly in the first weeks of simultaneous therapy. In the presence of a violation of kidney function, even in an easy degree, as well as in the elderly, careful medical supervision is necessary.
With simultaneous use with pentoksifillinom increases the risk of bleeding. It requires intensive clinical monitoring and frequent monitoring of bleeding time (blood clotting time).
With simultaneous use with zidovudine, there is a risk of increasing the toxic effect on red blood cells caused by 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 in 1-2 weeks. after initiation of therapy with NSAIDs.
It is possible to increase the hypoglycemic effect of sulfonylurea derivatives due to its displacement from the binding sites to plasma proteins under the influence of NSAIDs.
With the simultaneous use of low-molecular weight heparin with drugs, the risk of bleeding increases.
Combinations that need to be taken into account
NSAIDs can reduce the hypotensive effect of beta-blockers, which is due to inhibition of the synthesis of prostaglandins.
When used simultaneously with cyclosporine and tacrolimus, NSAIDs can enhance nephrotoxicity, which is mediated by the action of renal prostaglandins. During the combination therapy it is necessary to monitor the kidney function.
With concomitant administration with thrombolytics, the risk of bleeding increases.
With simultaneous application with probenecid, an increase in plasma NSAID concentrations is possible, which may be due to inhibition of renal secretion and / or conjugation with glucuronic acid. This requires correction of the dose of NSAIDs.
NSAIDs can cause an increase in the concentration of cardiac glycosides in blood plasma.
In connection with the theoretical risk of changing the effectiveness of mifepristone under the influence of inhibitors of prostaglandin synthesis, NSAIDs should not be prescribed earlier than 8-12 days after the withdrawal of mifepristone.
The data obtained in experimental studies on animals indicate a high risk of convulsions in the appointment of NSAIDs with ciprofloxacin in high doses.
Dexalgin В® can not be mixed in a single syringe with a solution of dopamine, promethazine, pentazocine, pethidine or hydroxysin (a precipitate is formed).
Dexalgin В® can be mixed in a single syringe with a solution of heparin, lidocaine, morphine and theophylline.
A diluted solution of the drug Dexalgin В® for infusion should not be mixed with promethazine or pentazocine.
A diluted solution of the drug Dexalgin В® for infusion is compatible with the following solutions for injection: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline.
When diluted solutions of the DexalginВ® preparation are stored for infusions in plastic containers or when infusion systems made of ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride are used, no absorption of the active substance by the listed materials occurs.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of no higher than 25 В° C. Shelf life - 5 years. Use only clear and colorless solutions.
After dilution, the solution is stored for 24 hours at a temperature of 2 В° to 8 В° C in a dark place.