Veldexal, 25 mg/ml 2 ml 5 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID).

The ATX code: [M01AE17]

Pharmacological properties

Pharmacodynamics

Dexketoprofen trometamol refers to non-steroidal anti-inflammatory drugs (NSAIDs), a propionic acid derivative. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is related to the inhibition of prostaglandin synthesis at the level of cyclooxygenase-1 and cyclooxygenase-2.

Analgesic effect comes 30 min after parenteral administration. Duration of analgesic effect after administration of 50 mg is 4-8 hours.

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

Pharmacokinetics

After intramuscular (i/m) administration of dexketoprofen the maximum concentration (Cmax) in blood serum is reached in average 20 min (10-45 min). The area under the curve “concentration-time” (AUC) after a single administration at a dose of 25-50 mg is proportional to the dose, both when administered v/m and intravenous (IV). The corresponding pharmacokinetic parameters are similar after single and repeated v/m or v/v administration, indicating that there is no cumulation of the drug.

Distribution

Dexketoprofen is characterized by high level of binding to plasma proteins (99%). Mean Vd value is less than 0.25 l/kg, the half-distribution time is about 0.35 h. Excretion

The metabolism of dexketoprofen mainly occurs by conjugation with glucuronic acid with subsequent excretion by the kidneys. The elimination half-life (T1/2) of dexketoprofen trometamol is about 1-2.7 h.

Pharmacokinetics in elderly persons

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

Indications

– relief of pain syndrome of various origins (including postoperative pain, pain with bone metastases, post-traumatic pain, pain with renal colic, algodismenorrhea, sciatica, sciatica, neuralgia, toothache);

– symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, osteoarthritis, spondyloarthritis: ankylosing spondylitis, reactive arthritis, psoriatic arthritis).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.

Pharmacological effect

Pharmacotherapeutic group: non-steroidal anti-inflammatory drug (NSAID).

ATX code: [M01AE17]

Pharmacological properties

Pharmacodynamics

Dexketoprofen trometamol is a non-steroidal anti-inflammatory drug (NSAID), a derivative of propionic acid. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis at the level of cyclooxygenase-1 and cyclooxygenase-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 with opioid analgesics, dexketoprofen significantly (up to 30-45%) reduces the need for opioids.

Pharmacokinetics

Suction

After intramuscular (IM) administration of dexketoprofen, the maximum concentration (Cmax) in the blood serum is achieved on average after 20 minutes (10-45 minutes). The area under the concentration-time curve (AUC) after a single dose of 25-50 mg is proportional to the dose, both with IM and intravenous (IV) administration. The corresponding pharmacokinetic parameters are similar after single and repeated intramuscular or intravenous administration, indicating the absence of drug accumulation.

Distribution

Dexketoprofen 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-life of distribution is about 0.35 hours. Elimination

Metabolism of dexketoprofen mainly occurs by conjugation with glucuronic acid followed by excretion by the kidneys. The half-life (T1/2) of dexketoprofen trometamol is approximately 1-2.7 hours.

Pharmacokinetics in the elderly

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

Special instructions

Persons with symptoms of gastrointestinal disorders or a history of gastrointestinal diseases require medical supervision, especially in case of gastrointestinal bleeding. In cases of gastrointestinal bleeding in patients taking dexketoprofen, the drug should be discontinued immediately.

Caution should be exercised when prescribing the drug to patients concomitantly taking medications that may increase the risk of ulceration or bleeding: corticosteroids, anticoagulants (for example, warfarin), selective serotonin reuptake inhibitors or antiplatelet agents (including acetylsalicylic acid).

Dexketoprofen may cause a reversible inhibition of platelet aggregation and increase bleeding time.

Dexketoprofen should be prescribed with caution to patients with a history of allergies. Dexketoprofen should be prescribed with caution to patients with chronic heart failure of NYHA functional class I-II.

Dexketoprofen can cause an increase in the level of creatinine and nitrogen in the blood plasma, have a negative effect on the urinary system, leading to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure.

As with the use of other NSAIDs, there may be a slight transient increase in the parameters of some liver tests, a significant increase in the activity 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, Dexketoprofen should be discontinued.

Dexketoprofen should be prescribed with caution to patients with hematopoietic disorders, patients with systemic lupus erythematosus or other connective tissue diseases.

Like other NSAIDs, dexketoprofen may mask the symptoms of infectious diseases. Isolated cases of exacerbation of infectious processes localized in soft tissues have been reported when using NSAIDs. Therefore, medical supervision is required for patients with signs of bacterial infection or worsening of their condition during treatment with dexketoprofen.

Caution should be exercised when prescribing the drug to patients with impaired liver, kidney, heart function or with conditions that may cause fluid retention in the body. In these patients, the use of NSAIDs can lead to worsening of the condition and fluid retention in the body. Caution should also be exercised when prescribing dexketoprofen to patients using diuretics or predisposed to hypovolemia, since they have an increased risk of developing nephrotoxicity.

Caution is necessary when prescribing the drug to elderly people, since they are more likely to have impaired renal, liver or cardiovascular function, as well as the occurrence of undesirable reactions, for example, gastrointestinal bleeding or intestinal perforation.

Each ampoule of the drug contains 200 mg of ethanol.

Impact on the ability to drive vehicles and machinery

Due to possible dizziness and drowsiness during the period of taking the drug, the ability to concentrate and the speed of psychomotor reactions may decrease.

Active ingredient

Dexketoprofen

Composition

For 1 ml:

Pregnancy

The use of the drug during pregnancy and breastfeeding is contraindicated.

Contraindications

– hypersensitivity to dexketoprofen, as well as to other NSAIDs or to any of the excipients included in the drug;

– complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history);

– erosive and ulcerative lesions of the gastrointestinal tract and duodenum;

– history of gastrointestinal bleeding, other active bleeding (including suspected intracranial bleeding), anticoagulant therapy;

– inflammatory bowel diseases (ulcerative colitis, Crohn’s disease) in the acute stage;

– severe liver dysfunction (10-15 points on the Child-Pugh scale);

– progressive kidney disease, severe renal dysfunction (creatinine clearance less than 30 ml/min);

– confirmed hyperkalemia;

– decompensated heart failure;

– the period after coronary artery bypass grafting;

– hemophilia and other blood clotting disorders;

– pregnancy, breastfeeding period;

– age under 18 years (efficacy and safety have not been established).

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

With caution

Peptic ulcer of the stomach and duodenum, ulcerative colitis, Crohn’s disease, history of liver disease, hepatic porphyria, chronic renal failure (creatinine clearance 30-60 ml/min), chronic heart failure, arterial hypertension, significant decrease in circulating blood volume (including after surgery), elderly patients (over 65 years of age, including those receiving diuretics, weakened patients and low body weight), bronchial asthma, simultaneous use of glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), coronary heart disease, cerebrovascular diseases, dielipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, Helicobacter pylori infection, systemic connective tissue diseases, long-term use of non-steroidal anti-inflammatory drugs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases.

Side Effects

The frequency of adverse reactions that were observed during the above clinical studies is presented in accordance with the WHO classification: very often ≥ 10%; often ≥ 1% and < 10%; uncommon ≥ 0.1% and < 1%; rarely ≥ 0.01% and

<0.1%; very rarely <0.01%; frequency unknown - it is not possible to determine the frequency of occurrence of an adverse reaction from the available data.

Local reactions

Often – pain at the injection site; uncommon – inflammatory reaction, hematoma, hemorrhage at the injection site, feeling of heat, chills, fatigue; rarely – back pain, fainting, fever; very rarely – anaphylactic shock, facial swelling.

From the central nervous system

Uncommon: headache, dizziness, insomnia, drowsiness; rarely – paresthesia.

From the skin

Uncommon – dermatitis, rash, sweating; rarely – acne, urticaria; very rarely – severe skin reactions (Stevens-Johnson syndrome, Lyell’s syndrome), angioedema, allergic dermatitis, photosensitivity.

From the urinary system

Rarely – polyuria, renal colic; very rarely – nephritis or nephrotic syndrome.

Metabolism

Rarely: hyperglycemia, hypoglycemia, hypertriglyceridemia.

From the musculoskeletal system

Rarely – muscle spasm, difficulty moving in joints.

From the digestive system

Often – nausea, vomiting; uncommon – abdominal pain, dyspepsia, diarrhea, constipation, hematemesis, dry mouth; rarely – erosive and ulcerative lesions of the gastrointestinal tract (GIT), including bleeding and perforation, anorexia, increased activity of liver enzymes, jaundice; very rarely – pancreatic damage, liver damage.

From the hematopoietic organs

Rarely – anemia; very rarely – neutropenia, thrombocytopenia.

From the respiratory system

Rarely – bradypnea; very rarely – bronchospasm, dyspnea.

From the senses

Uncommon: blurred vision; rarely – tinnitus.

From the cardiovascular system

Uncommon – arterial hypotension, feeling of heat, hyperemia of the skin; rarely – extrasystole, tachycardia, arterial hypertension, peripheral edema, superficial thrombophlebitis.

From the reproductive system

Rarely – in women – menstrual irregularities, in men – dysfunction of the prostate gland.

Laboratory indicators

Rarely – ketonuria, proteinuria.

Others

Aseptic meningitis, occurring predominantly 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

Undesirable combinations

Overdose

Cases of overdose have not been described.

Symptoms: possible vomiting, nausea, anorexia, abdominal pain, dizziness, disorientation, headache, drowsiness.

Treatment: symptomatic therapy; if necessary, hemodialysis.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life

2 years.

Do not use after expiration date.

Manufacturer

Velfarm LLC, Russia