Dexalgin - instructions for use, doses, side effects, contraindications

Dexketoprofen trometamol - active substance of the preparation Dexalgin® - a non-steroidal anti-inflammatory agent that has analgesic, anti-inflammatory and antipyretic effects.The mechanism of action is associated with inhibition of the synthesis of prostaglandins at the level of cyclooxygenases 1 and 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 (up to 30-45%) reduces the need for opioids.

Pharmacokinetics:

Suction

The maximum concentration in serum (C_mOh) after intramuscular injection of dexketoprofen trometamol is achieved on average after 20 min (10-45 min). The area under the concentration-time curve (AUC) after a single administration in a dose of 25-50 mg is proportional to the dose, 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

For dexketoprofen, trometamol is characterized by a high level of binding to plasma proteins (99%). The average value of the volume of distribution (V_d) is less than 0.25 l / kg, half-distribution time is about 0.35 h.

Excretion

The main way to excrete dexketoprofen is its conjugation with glucuronic acid, followed by the release through the kidneys. The half-life (T_1/2) of dexketoprofen trometamol is about 1-2 hours.

In elderly people, the half-life is prolonged (both after a single injection and after repeated intramuscular or intravenous administration) on average to 48% and a decrease in the overall clearance of the drug.

Indications:

- The relief of pain syndrome of various genesis (including postoperative pain, bone metastases, posttraumatic pain, pain in renal colic, algodismenorea, ishalgia, sciatica, neuralgia, toothache);

- symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, spondylitis, arthrosis, osteochondrosis).

Contraindications:

- Hypersensitivity to dexketoprofen or other NSAIDs or to any of the excipients that make up the drug (see "Composition");

- peptic ulcer of the stomach and duodenum;

- gastrointestinal hemorrhages in 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 (creatinine clearance <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;

- childhood.

Dexalgin® is contraindicated for non-varicose (epidural or intrathecal, intrathecal) administration due to ethanol included in the formulation.

Carefully:

- Allergic conditions in the anamnesis;

- disturbance of the hematopoiesis system;

- systemic lupus erythematosus or mixed connective tissue diseases;

- simultaneous therapy with other medications (see "Interaction with other medicinal products ");

- predisposition to hypovolemia;

- cardiac ischemia;

- Older age (over 65 years).

Pregnancy and lactation:

Application of the drug Dexalgin® during pregnancy and during lactation is contraindicated.

Dosing and Administration:

Dexalgin® is intended for intravenous and intramuscular administration.

Recommended adult dose: 50 mg every 8-12 h. 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 drug therapy Dexalgin® should start with lower doses; the daily dose is 50 mg.

Dexalgin® is intended for short-term (not more than 2 days) use during acute pain syndrome. In the future, the patient can be transferred to oral analgesics.

Intramuscular injection technique

The contents of one ampoule (2 ml) are slowly injected deeply intramuscularly.

The technique of intravenous injection

If necessary, the contents of one ampoule (2 ml) of the drug Dexalgin® can be administered by slow intravenous injection lasting at least 15 seconds.

The technique of intravenous infusion

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 dilute solution (should be clear) is administered by slow intravenous infusion of 10-30 min.

Side effects:

Possible side effects with the use of dexketoprofen trometamol, as well as with the use of other drugs dexketoprofen, are given below on the descending frequency of occurrence: often (1-10% of patients), infrequently (0.1-1% of patients) rarely (0.01-0, 1% of patients), very rarely (less than 0.01% of patients), including individual reports.

From the side of the circulatory and lymphatic systems

Rarely: anemia.

Rarely: neutropenia, thrombocytopenia.

From the central nervous system

Infrequently: headache, dizziness, insomnia, drowsiness.

Rarely: paresthesia.

From the sense organs

Infrequently: blurred vision.

Rarely: noise in ears.

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.

Co of the respiratory system

Rarely: bradypnoe.

Rarely: bronchospasm, dyspnoea.

From the gastrointestinal tract

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.

Rarely: defeat of the pancreas.

From the liver and gallbladder

Rarely: increased activity of hepatic enzymes, jaundice.

Rarely: liver damage.

From the urinary system

Rarely: polyuria, renal colic.

Rarely: nephritis or nephrotic syndrome.

From the side of the reproductive system

Rarely: in women - a menstrual cycle, in men - a violation of the function of the prostate.

From the side of the musculoskeletal system

Rarely: muscular spasm, obstruction of joint movements.

From the skin

Infrequently: dermatitis, rash, sweating.

Rarely: urticaria, acne.

Rarely: severe skin reactions (Stevens-Johnson syndrome, Lyell's syndrome), angioedema, allergic dermatitis, photosensitivity.

From the side of metabolism

Rarely: hyperglycemia, hypoglycemia, hypertriglyceridemia.

From the 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.

Rarely: anaphylactic shock, swelling of the face.

Other violations: Aseptic meningitis, which occurs mainly in patients with systemic lupus erythematosus or mixed connective tissue diseases, hematologic disorders (purpura, aplastic and hemolytic anemia, rarely - agranulocytosis and bone marrow hypoplasia).

Overdose:

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

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

Interaction:

Dexalgin® Do not mix in a single syringe with a solution of dopamine, promethazine, pentazocine, pethidine or hydroxysin (a precipitate is formed).

Dexalgin® can be mixed in one syringe with a solution of heparin, lidocaine, morphine and theophylline.

Dexalgin® - dilute solution for infusion should not be mixed with promethazine or pentazocine.

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

When stored Dexalgin® - diluted solutions for infusion in plastic containers or using infusion systems made from ethyl vinyl acetate, cellulose propionate, low density polyethylene or polyvinyl chloride, no absorption of the active ingredient with the listed materials.

The following interactions are typical for all NSAIDs.

Unwanted combinations

With other NSAIDs, including salicylates in high doses (more than 3 g / day): the simultaneous administration of several NSAIDs due to the synergistic effect increases the risk of gastrointestinal bleeding and ulcers.

With oral anticoagulants, heparin in doses exceeding preventive, and ticlopidine: increased risk of bleeding due to inhibition of platelet aggregation and damage to the mucous membrane of the gastrointestinal tract.

With lithium preparations: NSAIDs increase the level of lithium in the blood, down to toxic, and therefore this indicator should be monitored when appointing, changing the dose and after the abolition of NSAIDs.

With methotrexate in high doses (15 mg / week and more): rise hematological toxicity of methotrexate in connection with a decrease in its renal clearance against the background of therapy with NSAIDs.

With hydantoins and sulfonamide preparations: risk of increase toxic effects of these drugs.

Combinations that require caution

With diuretics, angiotensin-converting enzyme inhibitors: therapy with NSAIDs is associated with a risk of developing acute renal failure in dehydrated patients (decreased glomerular filtration due to reduced synthesis of prostaglandins). 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.

With methotrexate in low doses (less than 15 mg / week): increase of hematological toxicity of methotrexate in connection with a decrease in its renal clearance against the background of therapy with NSAIDs.It is necessary to conduct a weekly count of blood cells 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 pentoxifylline: increased risk of bleeding. It requires intensive clinical monitoring and frequent checking of bleeding time (blood clotting time).

With zidovudine: the risk of increasing 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 count all blood cells and reticulocytes 1-2 weeks after the initiation of NSAID therapy.

With sulfanilamide preparations: NSAIDs can enhance the hypoglycemic effect of sulfonylurea due to its displacement from binding sites to plasma proteins.

With preparations of low-molecular heparin: increased risk of bleeding.

Combinations that need to be taken into account

With β-blockers: NSAIDs can reduce the hypotensive effect of β-blockers, which is due to inhibition of prostaglandin synthesis.

With cyclosporine and tacrolimus: NSAIDs can increase nephrotoxicity, which is mediated by the action of renal prostaglandins. During the simultaneous therapy, it is necessary to monitor the kidney function.

With thrombolytics: increased risk of bleeding.

With probenecid: plasma concentrations of NSAIDs may increase, which may be due to an inhibitory effect on renal tubular secretion and / or conjugation with glucuronic acid, which requires correction of the NSAID dose.

With cardiac glycosides: NSAIDs can lead to an increase in the concentration of glycosides in the plasma.

With mifepristone: 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.

With ciprofloxacin: the data obtained in experimental studies on animals indicate a high risk of convulsions in the appointment of NSAIDs with ciprofloxacin in high doses.

Special instructions:

In patients with disorders of the gastrointestinal tract or gastrointestinal diseases in a history, continuous monitoring is necessary.In the event of gastrointestinal bleeding or ulcers, drug therapy Dexalgin® should be canceled.

Since all NSAIDs may inhibit platelet aggregation and increase bleeding time, due to the deceleration of prostaglandin synthesis, in controlled clinical trials co-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. Nevertheless, with the simultaneous administration of the drug Dexalgin® with other drugs that affect blood clotting, careful medical supervision.

Like other NSAIDs, Dexalgin® can lead to an increase in the level of creatinine and nitrogen in the blood plasma.

Like other inhibitors of prostaglandin synthesis, Dexalgin® It may 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.

As in the case of other NSAIDs, against the background of drug therapy Dexalgin® there may be a slight transient increase in some hepatic parameters, as well as a significant increase in the level of aspartic and alanine transaminases (AsT and AlT) in serum. At the same time, control of hepatic and renal functions is necessary in the elderly. In the case of a significant increase in the corresponding indicators Dexalgin® should be canceled.

Like other NSAIDs, dexketoprofen trometamol can mask the symptoms of infectious diseases. In case of detection of signs of bacterial infection or deterioration of well-being on the background of drug therapy Dexalgin® the patient should immediately consult a doctor.

AT each ampule of the drug Dexalgin® is contained 200 mg of ethanol.

Effect on the ability to drive transp. cf. and fur:

In connection with possible dizziness and drowsiness during the period of taking the drug Dexalgin® the ability to concentrate and the speed of psychomotor reactions in patients can be reduced.

Form release / dosage:

Solution for intravenous intramuscular and administration, 25 mg / ml.

Packaging:

2 ml of the drug in dark glass ampoules (type I) with a white dot in the upper part of the ampoule.

For 1, 5 or 10 ampoules per package, the contour plastic (pallet), together with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C, in a place protected from light.

After dilution, the solution is stored for 24 hours, at a temperature of 2 to 8 ° C, in a dark place.

Keep the medicinal product out of the reach of children.

Shelf life:

5 years.

Use only clear and colorless solutions.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002674/08

Date of registration:10.04.2008

Expiration Date:Unlimited

The owner of the registration certificate:Berlin-Chemie / Menarini Pharma, GmbH Berlin-Chemie / Menarini Pharma, GmbH Germany

Manufacturer: & nbsp

A.MENARINI Manufacturing Logistics and Servicer Italy

Representation: & nbspBERLIN-CHEMI / MENARINI PHARMA GmbH BERLIN-CHEMI / MENARINI PHARMA GmbH Germany

Information update date: & nbsp22.04.2017

Illustrated instructions

Instructions

Dexalgin® (Dexalgin®)