Dexalgin, 25 mg/ml 2 ml 5 pcs

Pharmacodynamics

A nonsteroidal anti-inflammatory drug (NSAID). It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is related to inhibition of prostaglandin synthesis at the level of COX-1 and COX-2.

The analgesic effect occurs 30 minutes after parenteral administration. Duration of analgesic effect after administration of 50 mg is 4-8 hours.

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

Pharmacokinetics

Absorption

After the oral administration of dexketoprofen trometamol, Cmax in serum is reached on average in 20 min (10-45 min). The AUC after a single administration at a dose of 25-50 mg is proportional to the dose, both when administered v/m and v/v. 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

The high level of binding to plasma proteins (99%) is characteristic of dexketoprofen tromethamol. The average Vd value is less than 0.25 l/kg and the half-distribution time is about 0.35 h.

Elimination

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

Pharmacokinetics in special clinical cases

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

Indications

Active ingredient

Composition

Active ingredients:

Dexketoprofen trometamol 36.9 mg (73.8 mg), corresponding to dexketoprofen 25 mg (50 mg).

Auxiliary substances:

Ethanol 96% – 200 mg,

Sodium chloride – 8 mg,

Sodium hydroxide – to pH 7.4,

d/i water – up to 2 ml

How to take, the dosage

Dexalgin® is intended for intravenous and intravenous administration.

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

In elderly patients and patients with hepatic and/or renal impairment therapy with Dexalgin® should be started at lower doses; the daily dose is 50 mg.

Dexalgin® is intended for short-term (not more than 2 days) use during acute pain syndrome. Later it is possible to transfer the patient to analgesics for oral administration.

Regulations for preparing and administering solutions

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

The contents of one ampoule (2 ml) are administered by slow intravenous injection for a minimum of 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 exposure to daylight. The diluted solution (should be clear) is administered by slow IV infusion lasting 10-30 minutes.

Interaction

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

Unwanted combinations

The simultaneous use 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.

Concomitant use with oral anticoagulants, heparin in doses higher than prophylactic and ticlopidine increases the risk of bleeding due to inhibition of platelet aggregation and gastrointestinal mucosa lesions.

The NSAIDs increase plasma lithium concentration, up to and including toxic, and therefore this indicator should be monitored when prescribing, changing doses and after discontinuation of NSAIDs.

When used with methotrexate at high doses (15 mg/week or more) there is an increase in hematological toxicity of methotrexate due to its decreased renal clearance with NSAID therapy.

In concomitant use with hydantoins and sulfonamides there is a risk of increased toxicity of these drugs.

Combinations requiring caution

When concomitant use with diuretics, ACE inhibitors is necessary, note that NSAID therapy is associated with the risk of acute renal failure in patients with dehydration (decreased glomerular filtration due to inhibition of prostaglandin synthesis). NSAIDs may reduce the hypotensive effect of some drugs. If concomitant administration with diuretics, it is necessary to ensure that the patient’s water balance is adequate and to monitor renal function before prescribing NSAIDs.

Concomitant use with methotrexate at low doses (less than 15 mg/week) may increase hematologic toxicity of methotrexate due to decreased renal clearance with NSAID therapy. It is necessary to monitor the blood cell count weekly during the first weeks of concomitant therapy. In the presence of renal dysfunction, even in mild cases, as well as in elderly patients, close medical supervision is necessary.

Concomitant use with pentoxifylline increases the risk of bleeding. Intensive clinical monitoring and frequent monitoring of bleeding time (clotting time) is necessary.

In concomitant use with zidovudine there is a risk of increased toxic effects on red blood cells due to the effect on reticulocytes, with the development of severe anemia one week after administration of NSAIDs. Monitoring of all blood cells and reticulocytes 1-2 weeks after initiation of NSAID therapy is necessary.

The hypoglycemic effect of sulfonylurea derivatives may be enhanced due to its displacement from plasma protein binding sites by NSAIDs.

Concomitant use with preparations of low molecular weight heparin increases the risk of bleeding.

Combinations to consider

NSAIDs may decrease the hypotensive effect of beta-adrenoblockers due to inhibition of prostaglandin synthesis.

In concomitant use with cyclosporine and tacrolimus, NSAIDs may increase nephrotoxicity which is mediated by the action of renal prostaglandins. Renal function should be monitored during combination therapy.

Concomitant administration with thrombolytics increases the risk of bleeding.

Concomitant use with probenecid may increase plasma concentrations of NSAIDs which may be due to inhibition of renal secretion and/or conjugation with glucuronic acid. This requires adjustment of the dose of NSAIDs.

NSAIDs may cause increased plasma concentrations of cardiac glycosides.

Because of the theoretical risk of prostaglandin inhibitors altering mifepristone’s effectiveness, NSAIDs should not be started earlier than 8-12 days after mifepristone withdrawal.

The data obtained in experimental animal studies indicate a high risk of convulsions when NSAIDs are prescribed with high-dose ciprofloxacin therapy.

Pharmaceutical interactions

Dexalgin® must not be mixed in the same syringe with dopamine, promethazine, pentazocine, pethidine or hydroxyzine solution (precipitate is formed).

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

The diluted solution of Dexalgin® for infusion must not be mixed with promethazine or pentazocine.

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

When diluted solutions of Dexalgin® for infusion are stored in plastic containers or when using infusion systems made of ethylvinyl acetate, propionate cellulose, low density polyethylene or polyvinyl chloride there is no absorption of the active substance by the listed materials.

Special Instructions

In patients with a history of digestive system disorders or gastrointestinal diseases, continuous monitoring is necessary. If gastrointestinal bleeding or ulcers occur, therapy with Dexalgin® should be discontinued.

While all NSAIDs can inhibit platelet aggregation and increase bleeding time due to inhibition of prostaglandins synthesis, in controlled clinical trials simultaneous administration of Dexketoprofen trometamol and agents of low molecular weight heparin in prophylactic doses during postoperative period has been studied. No effect on coagulation parameters was observed. Nevertheless, when concomitant administration of Dexalgin® with other drugs affecting blood clotting, careful medical monitoring is necessary. As other NSAIDs, Dexalgin® may increase plasma creatinine and nitrogen levels.

Like other prostaglandin synthesis inhibitors, Dexalgin® may have adverse effects on the urinary system, which may lead to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome, and acute renal failure.

With Dexalgin® therapy, as well as with other NSAIDs, a slight transient increase of some hepatic parameters and significant increase of serum AST and ALT levels may be observed. In this case, monitoring of liver and kidney functions is necessary in elderly patients. In case of significant increase of the corresponding indicators Dexalgin® should be discontinued.

Like other NSAIDs, dexketoprofen tromethamol may mask the symptoms of infectious diseases. If there are symptoms of bacterial infection or if there is a deterioration of well-being during therapy with Dexalgin® the patient should inform the physician.

Each ampule of Dexalgin® contains 200 mg of ethanol.

Impact on ability to drive vehicles and other mechanisms requiring high concentration

In connection with possible dizziness and somnolence during treatment with Dexalgin® , the ability to concentrate and the speed of psychomotor reactions may be reduced.

Contraindications

Side effects

Frequency of side effects:

Blood system: rare – anemia; very rare – neutropenia, thrombocytopenia.

CNS disorders: infrequent headache, dizziness, insomnia, somnolence; rarely – paresthesia.

Sensory system disorders: infrequent blurred vision; rarely – tinnitus.

Cardiovascular system: infrequent arterial hypotension, fever, skin hyperemia; rarely – extrasystole, tachycardia, arterial hypertension, peripheral edema, superficial thrombophlebitis.

Respiratory system: rarely – bradypnoea; very rarely – bronchospasm, dyspnoea.

Digestive system disorders: frequent – nausea, vomiting; infrequent – abdominal pain, dyspepsia, diarrhea, constipation, hematemesis, dry mouth; rare – erosive and ulcerative lesions of the gastrointestinal tract, including bleeding and perforations, anorexia, increased activity of liver enzymes, jaundice; very rare – pancreatic lesions, liver damage.

As to the urinary system: rarely – polyuria, renal colic; very rarely – nephritis or nephrotic syndrome.

Reproductive system disorders: rare – in women – menstrual disorders, in men – disorders of prostate function.

Muscular system: rare – muscle spasm, difficulty with movement in the joints.

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

Allergic reactions: rare – urticaria; very rare – severe skin reactions (Stevens-Johnson syndrome, Lyell syndrome), angioedema, allergic dermatitis.

Metabolism disorders: rarely – hyperglycemia, hypoglycemia, hypertriglyceridemia.

Laboratory disorders: rarely – ketonuria, proteinuria.

Local and general reactions: often – pain at the injection site; infrequent – inflammatory reaction, hematoma, hemorrhages at the injection site, fever, fatigue; rarely – back pain, fainting, fever; very rare – anaphylactic shock, facial edema.

Other: aseptic meningitis, occurring 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.

Pregnancy use

The use of the drug Dexalgin® is contraindicated in pregnancy and lactation.

Similarities