ÄѬßá½ú¿¡® 25

General characteristics. Structure:

Active ingredient:
Deksketoprofena трометамол – 36,90 mg
equivalent of a deksketoprofen – 25,00 mg

Excipients: cellulose microcrystallic-141,20 mg, starch corn - 49,60 mg, sodium carboxymethylstarch (type A) – 27,10 mg, glyceryl palmitostearat-5,20 mg.

Film cover: a gipromelloza – 1,34 mg, titanium dioxide (Е 171) – 0,36 mg, a macrogoal of 6000 - 0,60 mg, propylene glycol – 0,42 mg.

Pharmacological properties:

Pharmacodynamics. Deksketoprofena трометамол – active ingredient of the drug Дексалгин® 25 – 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 cyclooxygenases (TsOG-1 and TsOG-2).

The Analgeziruyushchy effect occurs in 30 min. after oral administration, duration of therapeutic action reaches 4 - 6 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 oral administration of a deksketoprofen of a trometamol is reached on average in 30 min. (15-60 min.). The concomitant use of food slows down drug absorption. The areas under a curve "concentration time" (AUC) after single and repeated receptions are similar that indicates lack of cumulation of drug.

Distribution. High level of linkng with proteins of a blood plasma (99%) is characteristic of a deksketoprofen of a trometamol. Average value of volume of distribution (Vd) makes less than 0,25 l/kg, the period 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 removal by kidneys. The elimination half-life (T1/2) of a deksketoprofen of a trometamol makes 1,65 h. At elderly people lengthening of an elimination half-life 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 colic, альгодисменорея, an ischialgia, radiculitis, neuralgia, a dentagra , etc.);
• symptomatic treatment of acute and chronic inflammatory, inflammatory and degenerative and metabolic diseases of a musculoskeletal system (including pseudorheumatism, spondylarthritis, osteoarthrosis, osteochondrosis).

Drug is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use.

Route of administration and doses:

ÄѬßá½ú¿¡® 25 accept inside during food. Depending on intensity of a pain syndrome the recommended dose for adults makes 12,5 mg (1/2 tablets) each 4 - 6 h or 25 mg (1 tablet) each 8 h.

The maximum daily dose – 75 mg.

At patients of advanced age and patients with an abnormal liver function and/or kidneys therapy by the drug Дексалгин® 25 should be begun with lower doses. The maximum daily dose makes 50 mg.

ÄѬßá½ú¿¡® 25 it is not provided for long therapy, the course of treatment drug should not exceed 3-5 days.

Features of use:

For patients with disturbances from digestive tract or gastrointestinal diseases in the anamnesis careful observation is necessary. In case of developing of gastrointestinal bleeding or an ulcer therapy by the drug Дексалгин® 25 should be cancelled.

It is clinically proved that simultaneous use of a deksketoprofen and drugs of low-molecular heparin in preventive doses in the postoperative period does not change coagulability indicators. Nevertheless, at simultaneous use of the drug Дексалгин® 25 with other drugs influencing coagulability of blood careful medical control of system of coagulability of blood is necessary.

As well as other NPVP, Дексалгин® 25 can lead to increase in concentration of creatinine and nitrogen in a blood plasma. As well as other inhibitors of synthesis of prostaglandins, Дексалгин® 25 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 Дексалгин® 25 small passing increase in some hepatic indicators, and also substantial increase of activity of nuclear heating plant and ALT in blood serum can be observed. At the same time control of function of a liver and kidneys is necessary at elderly people. In case of substantial increase of the corresponding indicators Дексалгин® 25 it is necessary to cancel.

As well as other NPVP, декскетопрофен can mask symptoms of infectious diseases. In case of detection of symptoms of an infection or deterioration in health against the background of therapy by the drug Дексалгин® 25 the patient needs to see a doctor at once.

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

Due to possible dizziness and drowsiness during administration of drug Дексалгин® 25, ability to concentration of attention and speed of psychomotor reactions at patients can decrease in the first hour after administration of drug. Therefore during treatment by the drug Дексалгин® 25 it is necessary to be careful at control of vehicles and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Possible side effects at use of the drug Дексалгин® 25, as well as at use of other drugs of a deksketoprofen, are given below on decrease of frequency of emergence: 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.

Disturbances from blood and lymphatic system
Very seldom: neutropenia, thrombocytopenia.

Disturbances from a nervous system
 Infrequently: headache, dizziness, sleeplessness, drowsiness.
Seldom: paresthesias.

Disturbances from sense bodys
 Seldom: sonitus.
Very seldom: indistinct sight

Disturbances from cardiovascular system
Infrequently: feeling of heat, hyperemia of integuments.
Seldom: premature ventricular contraction, increase in arterial pressure.
Very seldom: tachycardia, lowering of arterial pressure.

Disturbances from respiratory system
Seldom: брадипноэ.
Very seldom: bronchospasm, asthma.

Disturbances from digestive tract
Often: nausea, vomiting, abdominal pain, dyspepsia, diarrhea.
Infrequently: a lock, dryness in a mouth, a meteorism.
Seldom: GIT erosive cankers, helcomenia or its perforation, anorexia.
Very seldom: damage of a pancreas.

Disturbances from a liver and biliary tract
 Seldom: increase in activity of "hepatic" enzymes, including aspartate aminotransferases and alaninaminotranspherases (nuclear heating plant and ALT), jaundice.
Very seldom: damage of a liver.

Disturbances from kidneys and urinary tract
 Seldom: polyuria.
Very seldom: nephrite or nephrotic syndrome.

Disturbances from reproductive system
 Seldom: women have a disturbance of a menstrual cycle, men have passing dysfunctions of a prostate at prolonged use.

Disturbances from a musculoskeletal system
 Seldom: a dorsodynia, a muscular spasm, difficulty of movements in joints.

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

Disturbances from a metabolism
 Seldom: hyperglycemia, hypoglycemia, gipertriglitseridemiya.

Datas of laboratory
 Seldom: ketonuria, proteinuria.

Disturbances from the general status
 Infrequently: fever, fatigue.
Very seldom: acute anaphylaxis, face edema.

Other disturbances
 Infrequently: 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).
Seldom: agranulocytosis and hypoplasia of marrow.

Interaction with other medicines:

The following interactions are characteristic of all NPVP.

Undesirable combinations

With other NPVP, including salicylates in high doses (more than 3 g/days): simultaneous use 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 concentration of lithium in blood, up to toxic in this connection, this indicator needs to be controlled at use, 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 sulfonamides: risk of strengthening of toxic effect of these drugs.

The combinations demanding care

With diuretics, inhibitors of an angiotensin-converting enzyme: 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 anti-hypertensive effect of some drugs.

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.

Increase in risk of development of GITs bleedings at a combination to inhibitors of the return serotonin reuptake (to tsitalopra, fluoxetine, sertraline), peroral glucocorticoids.

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 strengthening of 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 the general blood test with calculation of quantity of reticulocytes in 1-2 weeks after the beginning of therapy of NPVP.

With sulphonylurea derivatives: NPVP can strengthen hypoglycemic effect of sulphonylurea owing to replacement it from places of linkng with proteins of a blood 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 a blood plasma can increase that can be caused by the inhibiting effect of a probenetsid 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 a blood 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.

From hinolona: the data obtained in pilot studies on animals indicate high risk of development of spasms at use of NPVP against the background of therapy of a hinolonama in high doses.

Contraindications:

• hypersensitivity to a deksketoprofen or other NPVP or to any of the excipients which are a part of drug;
• a peptic ulcer of a stomach and duodenum in an aggravation phase;
• gastrointestinal bleedings in the anamnesis, other active bleedings (including suspicion of intracranial bleeding), anticoagulating therapy;
• inflammatory diseases of intestines (a disease Krone, ulcer colitis) in an aggravation phase;
• heavy abnormal liver functions (10 - 15 points on a scale of Chayld-Pyyu);
• moderate or heavy renal failures (clearance of creatinine <50 ml/min.);
• a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);
• heavy heart failure;
• the period after performing aortocoronary shunting;
• hemorrhagic diathesis or other disturbances of coagulation;
• age up to 18 years (there are no data on efficiency and safety of drug).

With care
• allergic reactions in the anamnesis;
• disturbance of system of a blood coagulation;
• a system lupus erythematosus or the mixed diseases of connecting fabric;
• simultaneous therapy by other medicines (see the section Interaction with other medicines);
• a condition of the expressed hypovolemia;
• coronary heart disease;
• cerebrovascular diseases;
• diabetes mellitus, lipidemia,
• diseases of peripheral arteries;
• anamnestic data on development of a canker of a GIT;
• prolonged use of NPVP;
• alcoholism, malicious smoking;
• advanced age (65 years are more senior).

Use at pregnancy and a lactation

Use of the drug Дексалгин® 25 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, a hemodialysis.

Storage conditions:

To store at a temperature not above 30 °C, in the place protected from light. To store medicine, in the place, unavailable to children! Period of validity 2 years. Not to apply after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 25 mg.

On 10 tablets in a blister strip packaging (blister) [an aluminum white opaque PVC film / foil].

On 1 blister together with the application instruction in a cardboard pack.