Дексалгин®

General characteristics. Structure:

Contains in one ampoule (2 ml):

Active ingredient: Deksketoprofena трометамол – 73,8 mg (that corresponds to 50,0 mg of a deksketoprofen).

Excipients: ethanol (96%) – 200,0 mg, sodium chloride – 8,0 mg, sodium hydroxide to рН 7,4, water for injections to 2,0 ml.

Pharmacological properties:

Pharmacodynamics. Deksketoprofena трометамол – active ingredient of the drug Deksalgin® – the non-steroidal anti-inflammatory drug having analgeziruyushchy antiinflammatory and febrifugal effect. The mechanism of action is connected with inhibition of synthesis of prostaglandins at the level of cyclooxygenase 1 and 2.

Analgeziruyushchy action comes in 30 min. after parenteral administration. Duration of analgeziruyushchy effect after introduction in a dose of 50 mg makes 4-8 h.

At a combination therapy with analgetics of an opioid number of a deksketoprofen трометамол considerably reduces the need for opioids (to 30-45%).

Pharmacokinetics. Absorption. The maximum concentration in serum (Cmax) after intramuscular introduction of a deksketoprofen of a trometamol is reached on average in 20 min. (10-45 min.). The area under a curve "concentration time" (AUC) after single introduction in a dose of 25-50 mg is proportional to a dose, both at intramuscular, and at intravenous administration. The corresponding pharmacokinetic parameters are similar after single and repeated intramuscular or intravenous administration that indicates lack of cumulation of drug.

Distribution. High level of linkng with proteins of plasma (99%) is characteristic of a deksketoprofen of a trometamol. Average value of volume of distribution (Vd) makes less than 0,25 l/kg, time of semi-distribution makes about 0,35 h.

Removal. The main way of removal of a deksketoprofen is its conjugation with glucuronic acid with the subsequent renal elimination. The elimination half-life (T1/2) of a deksketoprofen of a trometamol makes about 1-2,7 h. At elderly people lengthening of an elimination half-life (both after single, and after repeated intramuscular or intravenous administration) on average to 48% and decrease in the general clearance of drug is observed.

Indications to use:

• Stopping of a pain syndrome of various genesis (including postoperative pains, pain at metastasises in bones, posttraumatic pains, pain at renal gripes, альгодисменорея, an ishalgiya, radiculitis, neuralgia, a dentagra);
• symptomatic treatment of acute and chronic inflammatory, inflammatory and degenerative and metabolic diseases of a musculoskeletal system (including pseudorheumatism, spondylarthritis, arthrosis, osteochondrosis).

Route of administration and doses:

Дексалгин® it is intended for intravenous and intramuscular administration.

The recommended dose for adults: 50 mg each 8-12 h. If necessary perhaps repeated administration of drug with a 6-hour interval. The daily dose makes 150 mg.

At patients of advanced age and patients with an abnormal liver function and/or kidneys therapy by the drug Deksalgin® should be begun with lower doses; the daily dose makes 50 mg.

Дексалгин® it is intended for short-term (no more than 2 days) uses in the period of an acute pain syndrome. Further transfer of the patient into peroral analgetics is possible.

Technology of carrying out an intramuscular injection

Contents of one ampoule (2 ml) are slowly entered deeply intramusculary.

Technology of carrying out an intravenous injection

If necessary, contents of one ampoule (2 ml) of the drug Deksalgin® can be entered by a slow intravenous injection lasting not less than 15 pages.

Technology of performing intravenous infusion

Contents of one ampoule (2 ml) are parted in 30-100 ml of normal saline solution, solution of glucose or Ringer's (lactate) solution. Solution should be prepared in aseptic conditions and always to protect from daylight influence. Weak solution (has to be transparent) is entered by slow intravenous infusion lasting 10-30 min.

Features of use:

At patients with disturbances from digestive tract or gastrointestinal diseases in the anamnesis constant control is necessary. In case of developing of gastrointestinal bleeding or an ulcer therapy by the drug Deksalgin® should be cancelled.

As everything NPVP can inhibit aggregation of thrombocytes and increase a bleeding time owing to delay of synthesis of prostaglandins, in controlled clinical trials co-administration of a deksketoprofen of a trometamol and drugs of low-molecular heparin in preventive doses in the postoperative period was studied. No impact on parameters of coagulation was observed. Nevertheless, at co-administration of the drug Deksalgin® with other drugs influencing coagulability of blood careful medical control is necessary.

As well as can lead other NPVP, Deksalgin® to increase in level of creatinine and nitrogen in a blood plasma. As well as other inhibitors of synthesis of prostaglandins, Deksalgin® can have side effect on an urinary system that can lead to development of a glomerulonephritis, intersticial nephrite, a papillary necrosis, nephrotic syndrome and an acute renal failure.

As well as in case of other NPVP, against the background of therapy by the drug Deksalgin® small passing increase in some hepatic indicators, and also substantial increase of level of asparaginic and alanine transaminases (NUCLEAR HEATING PLANT and ALT) in blood serum can be observed. At the same time control of hepatic and renal functions is necessary at elderly people. In case of substantial increase of the corresponding indicators of Deksalgin® it is necessary to cancel.

As well as other NPVP, the deksketoprofena трометамол can mask symptoms of infectious diseases. In case of detection of symptoms of a bacterial infection or deterioration in health against the background of therapy by the drug Deksalgin® the patient needs to see a doctor at once.

Each ampoule of the drug Deksalgin® contains 200 mg of ethanol.

Influence on ability to driving of motor transport and to control of mechanisms

Due to possible dizziness and drowsiness during administration of drug of Deksalgin® ability to concentration of attention and speed of psychomotor reactions at patients can decrease.

Side effects:

Possible side effects at use of a deksketoprofen of a trometamol, as well as at use of other drugs of a deksketoprofen, are given below on the descending emergence frequency: often (1-10% of patients), infrequently (0,1-1% of patients) it is rare (0,01-0,1% of patients), is very rare (less than 0,01% of patients), including separate messages.

From circulatory and lymphatic systems
 Seldom: anemia.
Very seldom: neutropenia, thrombocytopenia.

From the central nervous system
 Infrequently: headache, dizziness, sleeplessness, drowsiness.
Seldom: paresthesia.

From sense bodys
 Infrequently: sight illegibility.
Seldom: sonitus.

From cardiovascular system
 Infrequently: arterial hypotension, feeling of heat, hyperemia of integuments.
Seldom: premature ventricular contraction, tachycardia, arterial hypertension, peripheral hypostasis, superficial thrombophlebitis.

From respiratory system
 Seldom: брадипноэ.
Very seldom: bronchospasm, диспноэ.

From digestive tract
 Often: nausea, vomiting.
Infrequently: abdominal pain, dyspepsia, diarrhea, lock, hematemesis, dryness in a mouth.
Seldom: erosive cankers of bodies of a GIT, including bleedings and perforation, anorexia.
Very seldom: damage of a pancreas.

From a liver and gall bladder
 Seldom: increase in activity of liver enzymes, jaundice.
Very seldom: damage of a liver.

From an urinary system
Seldom: polyuria, renal colic.
Very seldom: nephrite or nephrotic syndrome.

From reproductive system
 Seldom: women have a disturbance of a menstrual cycle, men have a dysfunction of a prostate.

From a musculoskeletal system
 Seldom: a muscular spasm, difficulty of movements in joints.

From integuments
 Infrequently: dermatitis, rash, perspiration.
Seldom: urticaria, acne rash.
Very seldom: heavy skin reactions (Stephens-Johnson's syndrome, Lyell's disease), Quincke's disease, allergic dermatitis, photosensitization.

From a metabolism
 Seldom: hyperglycemia, hypoglycemia, gipertriglitseridemiya.

From laboratory indicators
 Seldom: ketonuria, proteinuria.

Local and general reactions
 Often: pain in the place of an injection.
Infrequently: inflammatory reaction, a hematoma, hemorrhages in the place of an injection; feeling of heat, fever, exhaustion.
Seldom: dorsodynia, faint, fever.
Very seldom: acute anaphylaxis, face edema.

Other disturbances: the aseptic meningitis arising preferential at patients with a system lupus erythematosus or the mixed diseases of connecting fabric, hematologic disturbances (a purpura, aplastic and hemolitic anemias, it is rare – an agranulocytosis and a hypoplasia of marrow).

Interaction with other medicines:

Дексалгин® it is impossible to mix in one syringe with solution of a dopamine, promethazine, pentazocine, pethidine or Hydroxyzinum (the deposit is formed).

Дексалгин® it is possible to mix in one syringe with solution of heparin, lidocaine, morphine and theophylline.

Дексалгин® – weak solution for infusions cannot be mixed with promethazine or pentazocine.

Дексалгин® – weak solution for infusions is compatible to the following solutions for injections: dopamine, heparin, Hydroxyzinum, lidocaine, morphine, pethidine and theophylline.

At storage of Deksalgin® – weak solutions for infusions in plastic containers or when using the infusional systems made of ethylvinyl acetate, cellulose of propionate, polyethylene of low density or polyvinylchloride, absorption of active ingredient by the listed materials does not occur.

The following interactions are characteristic of all NPVP.

Undesirable combinations

With other NPVP, including salicylates in high doses (more than 3 g/days): co-administration of several NPVP owing to synergy effect increases risk of developing of gastrointestinal bleedings and an ulcer.

With peroral anticoagulants, heparin in the doses exceeding preventive, and tiklopidiny: increase in risk of developing of bleedings in connection with inhibition of aggregation of thrombocytes and damage of a mucous membrane of digestive tract.

With lithium drugs: NPVP increase lithium level in blood, up to toxic in this connection this indicator needs to be controlled at appointment, change of a dose and after cancellation of NPVP.

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

With hydantoins and sulfanamide drugs: risk of increase in toxic effect of these drugs.

The combinations demanding care

With diuretics, angiotensin-converting enzyme inhibitors: therapy of NPVP is connected with risk of development of an acute renal failure in the dehydrated patients (the decrease in glomerular filtering caused by reduced synthesis of prostaglandins). NPVP can reduce hypotensive effect of some drugs. At co-administration with diuretics it is necessary to be convinced that the water balance of the patient is adequate and to carry out control of function of kidneys before purpose of NPVP.

With a methotrexate in low doses (less than 15 mg/week): increase in hematologic toxicity of a methotrexate in connection with decrease in its renal clearance against the background of therapy of NPVP. It is necessary to carry out weekly calculation of blood cells to the first weeks of simultaneous therapy. In the presence of a renal failure even in easy degree, and also at elderly people careful medical observation is necessary.

With pentoksifilliny: increase in risk of development of bleedings. Intensive clinical monitoring and frequent check of a bleeding time (time of coagulability of blood) is necessary.

With a zidovudine: risk of increase in the toxic action on erythrocytes caused by impact on reticulocytes with development of heavy anemia in a week after purpose of NPVP. It is necessary to carry out calculation of all blood cells and reticulocytes in 1-2 weeks after the beginning of therapy of NPVP.

With sulfanamide drugs: NPVP can strengthen hypoglycemic effect of sulphonylurea owing to replacement it from places of linkng with proteins of plasma.

With drugs of low-molecular heparin: increase in risk of development of bleedings.

Combinations which need to be taken into account

With β-adrenoblockers:::::::::: NPVP can reduce hypotensive effect of β-adrenoblockers, that is caused by inhibition of synthesis of prostaglandins.

With cyclosporine and takrolimusy: NPVP can increase nephrotoxicity that is mediated by effect of renal prostaglandins. During performing simultaneous therapy it is necessary to control function of kidneys.

From trombolitika: the increased risk of development of bleedings.

With probenetsidy: concentration of NPVP in plasma can increase that can be caused by the inhibiting effect on renal tubular secretion and/or conjugation with glucuronic acid that demands dose adjustment of NPVP.

With cardiac glycosides: NPVP can lead to increase in concentration of glycosides in plasma.

With mifepristone: in connection with theoretical risk of change of efficiency of mifepristone under the influence of inhibitors of synthesis of prostaglandins, NPVP it is not necessary to appoint earlier, than in 8-12 days after mifepristone cancellation.

With ciprofloxacin: the data obtained in pilot studies on animals indicate high risk of development of convulsions at purpose of NPVP against the background of therapy by ciprofloxacin in high doses.

Contraindications:

• Hypersensitivity to a deksketoprofen or other NPVP or to any of the excipients which are a part of drug (see Structure);
• peptic ulcer of a stomach and duodenum;
• gastrointestinal bleedings in the anamnesis, other active bleedings (including suspicion of intracranial bleeding), anticoagulating therapy;
• gastrointestinal diseases (disease Krone, nonspecific ulcer colitis);
• heavy abnormal liver functions (10-15 points on a scale of Chayld-Pyyu);
• heavy renal failures (clearance of creatinine <50 ml/min.);
• bronchial asthma (including in the anamnesis);
• heavy heart failure;
• treatment of a pain syndrome at aortocoronary shunting;
• hemorrhagic diathesis or other disturbances of coagulation;
• children's age.

Дексалгин® it is contraindicated for nevraksialny (epidural or the subshell, the intra shell) introductions because of the ethanol drug which is a part.

With care:
• allergic states in the anamnesis;
• disturbance of system of a hemopoiesis;
• a system lupus erythematosus or the mixed diseases of connecting fabric;
• simultaneous therapy by other medicines (see Interaction with other medicines);
• predisposition to a hypovolemia;
• coronary heart disease;
• advanced age (65 years are more senior).

Use at pregnancy and a lactation

Use of the drug Deksalgin® at pregnancy and in the period of a lactation contraindicated.

Overdose:

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

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

Storage conditions:

At a temperature not above 25 °C in the place protected from light.

After dilution solution is stored during 24 h at a temperature from 2 to 8 °C in the place protected from light.

To store medicine in the place, unavailable to children!

Period of validity of 5 years. To use only transparent and colourless solutions.

Not to apply after expiry date.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular and introductions of 25 mg/ml. On 2 ml of drug in ampoules of dark glass (type I) with a white point in an upper part of an ampoule. On 5 ampoules in packaging planimetric plastic (pallet), together with the application instruction in a cardboard pack.