Dexalgin, Ampoules 25mg/ml 2ml, 5pcs

Composition

Active ingredients:

dexketoprofen trometamol 36.9 mg (73.8 mg), which corresponds to the content of dexketoprofen 25 mg (50 mg).

Auxiliary substances:

ethanol 96% – 200 mg,

sodium chloride-8 mg,

sodium hydroxide – up to pH 7.4,

d/i water-up to 2 ml

Pharmacological action

Pharmacodynamics

Nonsteroidal 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 use. The duration of the analgesic effect after use at a dose of 50 mg is 4-8 hours.

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

Pharmacokinetics

Suction

After intravenous use of dexketoprofen trometamol, Cmax in blood serum is reached on average in 20 minutes (10-45 minutes). AUC after a single dose of 25-50 mg is proportional to the dose, both with intravenous and intravenous use. The corresponding pharmacokinetic parameters are similar after a single and repeated IV or IV use, which indicates that there is no accumulation of the drug.

Distribution

Dexketoprofen trometamol is characterized by a high level of binding to plasma proteins (99%). The average Vd is less than 0.25 l / kg, and the half – life is about 0.35 hours.

Deduction

The main route of elimination of dexketoprofen is its conjugation with glucuronic acid and subsequent elimination by the kidneys. T1 / 2 of dexketoprofen trometamol is about 1-2.7 hours

. Pharmacokinetics in special clinical cases

In the elderly, there is an increase in the duration of T1 / 2 (both after a single and after repeated IV or iv use) by an average of 48% and a decrease in the total clearance of the drug.

Indications

• relief of pain syndrome of different Genesis (including postoperative pain, pain in bone metastases, post-traumatic pain, pain in renal colic, algomenorrhea, sciatica, sciatica, myalgia, neuralgia, toothache);
• symptomatic treatment of acute and chronic inflammatory, inflammatory, degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, spondylitis, osteoarthritis, osteochondrosis).

Use during pregnancy and lactation

The use of Dexalgin® during pregnancy and lactation is contraindicated.

Contraindications

• hypersensitivity to dexketoprofen or other NSAIDs or to any of the excipients that make up the drug.
• gastric ulcer and duodenal ulcer;
• gastrointestinal bleeding, a history of other active bleeding (including suspected intracranial bleeding), anticoagulant therapy;
• gastrointestinal diseases (Crohn’s disease, ulcerative colitis);
• severe disturbances of liver function (10-15 points on a scale child-Pugh);
• severe impairment of renal function (QC < 50 ml/min);
• asthma (including in the anamnesis);
• severe heart failure;
• treatment of the pain syndrome in the coronary artery bypass surgery;
• bleeding diathesis or other coagulation disorders;
• children’s age.

It is contraindicated for epidural, subshell or intra-shell use due to the ethanol contained in the preparation.

With caution: the drug should be used for a history of allergic conditions; disorders of the hematopoietic system; with SLE or mixed connective tissue diseases; simultaneously with other medications; in case of predisposition to hypovolemia; with coronary heart disease; in elderly patients (older than 65 years).

Side effects

Frequency of side effects:

• frequently (1-10%);
• infrequently (0.1-1%) rarely (0.01-0.1%);
• very rarely (less than 0.01%, including individual messages).

From the hematopoietic system:  rarely-anemia; very rarely-neutropenia, thrombocytopenia.

From the central nervous system:  infrequently-headache, dizziness, insomnia, drowsiness; rarely-paresthesia.

From the side of the senses:  infrequently-blurred vision; rarely-tinnitus.

From the cardiovascular system:  infrequently-hypotension, fever, hyperemia of the skin; rarely-extrasystole, tachycardia, hypertension, peripheral edema, superficial thrombophlebitis.

Respiratory system disorders:  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 – pancreatic damage, liver damage.

From the urinary system:  rarely-polyuria, renal colic; very rarely-nephritis or nephrotic syndrome.

From the side of the reproductive system:  rarely-in women-a violation of the menstrual cycle, in men-a violation of the function of the prostate gland.

Musculoskeletal disorders:  rarely-muscle spasm, difficulty moving in the joints.

Dermatological reactions:  sometimes-dermatitis, rash, sweating; rarely-acne; very rarely-photosensitization.

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.

From the side of laboratory parameters:  rarely – ketonuria, proteinuria.

Local and general reactions:  often-pain at the injection site; infrequently-inflammatory reaction, hematoma, hemorrhages at the injection site, feeling hot, chills, fatigue; rarely-back pain, fainting, fever; very rarely-anaphylactic shock, facial edema.

Other services:  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).

Interaction

The following drug interactions are common for all NSAIDs, including Dexalgin.

Unwanted combinations

Concomitant use of several NSAIDs, including salicylates in high doses (more than 3 g / day) increases the risk of gastrointestinal bleeding and ulcers due to the synergy of action.

With the simultaneous use of oral anticoagulants, heparin in doses exceeding preventive, and ticlopidine increases the risk of bleeding due to inhibition of platelet aggregation and a lesion of the mucous membrane of the gastrointestinal tract.

NSAIDs increase the concentration of lithium in blood plasma, up to toxic, in connection with which the indicator is necessary to control the assignment change the dose after discontinuation of NSAIDs.

When used with methotrexate in high doses (15 mg / week. increased hematological toxicity of methotrexate occurs due to a decrease in its renal clearance during NSAID therapy.

When used concomitantly with hydantoins and sulfonamide preparations, there is a risk of increasing the toxic effect of these drugs.

Combinations that require caution

If concomitant 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 rate due to inhibition of prostaglandin synthesis). NSAIDs may reduce the antihypertensive effect of certain medications. 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.

When used concomitantly 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 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.

When used concomitantly with pentoxifylline, the risk of bleeding increases. Intensive clinical monitoring and frequent monitoring of bleeding time (blood clotting time) is required.

When used concomitantly with zidovudine, there is a risk of increased toxic effects on red blood cells due to exposure to reticulocytes, with the development of severe anemia one week after the appointment of NSAIDs. All blood cells and reticulocytes should be monitored 1-2 weeks after starting NSAID therapy.

It is possible to increase the hypoglycemic effect of sulfonylurea derivatives due to its displacement from the sites of binding to plasma proteins under the influence of NSAIDs.

When used concomitantly with low-molecular-weight heparin preparations, the risk of bleeding increases.

Combinations that should be considered

NSAIDs may reduce the hypotensive effect of beta-blockers, due to inhibition of prostaglandin synthesis.

When used concomitantly with cyclosporine and tacrolimus, NSAIDs may increase nephrotoxicity, which is mediated by the action of renal prostaglandins. During combination therapy, renal function should be monitored.

When administered concomitantly with thrombolytics, the risk of bleeding increases.

When used concomitantly with probenecid, plasma concentrations of NSAIDs may increase, which may be due to inhibition of renal secretion and/or conjugation with glucuronic acid. This requires a 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 withdrawal.

Data obtained in experimental animal studies indicate a high risk of convulsions when prescribing NSAIDs against the background of high-dose ciprofloxacin therapy.

Pharmaceutical interaction

Dexalgin® should 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.

Dilute solution of Dexalgin® for infusions should not be mixed with promethazine or pentazocine.

The dilute solution of Dexalgin® for infusions is compatible with the following solutions for injection: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline.

When dilute solutions of Dexalgin® for infusions are stored in plastic containers or when using infusion systems made of ethyl vinyl acetate, cellulose propionate, low-density polyethylene or polyvinyl chloride, the Active ingredient is not absorbed by the listed materials.

How to take, course of use and dosage

Dexalgin® is intended for intravenous and intramuscular use.

Recommended dose for adults: 50 mg every 8-12 hours. If necessary, repeated use 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, Dexalgin therapy should be initiated at a lower dose; the daily dose is 50 mg.

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

Rules for the preparation and use of solutions

The contents of one ampoule (2 ml) are slowly injected deeply in/m.

The contents of one ampoule (2 ml) are administered by slow intravenous injection lasting at least 15 seconds.

The contents of one ampoule (2 ml) are diluted in 30-100 ml of saline, 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 clear) is administered by slow intravenous infusion lasting 10-30 minutes.

Overdose

Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia.

Treatment: symptomatic therapy; if necessary — gastric lavage, dialysis.

Special instructions

In patients with a history of digestive disorders or gastrointestinal diseases, constant monitoring is necessary. If gastrointestinal bleeding or ulcerative lesions occur, Dexalgin therapy should be discontinued.

Since all NSAIDs can inhibit platelet aggregation and increase bleeding time due to slowing prostaglandin synthesis, controlled clinical trials have studied the concomitant use of dexketoprofen trometamol and low-molecular-weight heparin preparations in prophylactic doses in the postoperative period. No effect on coagulation parameters was observed. However, careful medical monitoring is necessary when Dexalgin is co-administered with other medications that affect blood clotting. As with other NSAIDs, Dexalgin® can lead to an increase in plasma creatinine and nitrogen levels.

Like other prostaglandin synthesis inhibitors, 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 liver parameters, as well as a significant increase in serum AST and ALT levels. 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 discontinued.

Like other NSAIDs, dexketoprofen trometamol may mask the symptoms of infectious diseases. If symptoms of bacterial infection appear or if you feel unwell during Dexalgin therapy, the patient should inform their doctor.

Each ampoule of Dexalgin® contains 200 mg of ethanol.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Due to possible dizziness and drowsiness during treatment with Dexalgin®, the ability to concentrate attention and the speed of psychomotor reactions may decrease.

Form of production

Solution for injection

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Dexketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

For adults as directed by your doctor

Indications

Arthritis, Trigeminal Neuralgia, Osteochondrosis, Lumbago, Sciatica, Sciatica, Rheumatoid Arthritis, Osteoarthritis