Dexalgin 25,25mg 10 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drugs (NSAIDs).

ATX code: M01AE17

Pharmacological properties

Pharmacodynamics

Dexketoprofen trometamol, the active ingredient of the drug Dexalgin^® 25, refers to non-steroidal anti-inflammatory drugs (NSAIDs) with analgesic, anti-inflammatory and antipyretic effects. The mechanism of action of dexketoprofen is based on inhibition of prostaglandin synthesis at the level of cyclooxygenases (COX-1 and COX-2).

The analgesic effect occurs within 30 minutes after oral administration with a therapeutic effect duration of 4-6 hours.

Pharmacokinetics

absorption. The time to reach the maximum concentration (TSmax) of dexketoprofen in blood plasma after a single oral single dose is on average 30 min (15-60 min). Simultaneous intake of food slows down absorption of dexketoprofen. Areas under the curve “concentration-time” (AUC) after a single and repeated doses are similar, indicating that there is no cumulation of the drug.

Distribution Dexectoprofen is characterized by high degree of binding to the blood plasma proteins (99 %). The mean volume of distribution (Vd) is less than 0.25 l/kg, the half-life is about 0.35 h.

Metabolism and excretion. The main route of metabolism of dexketoprofen is its conjugation with glucuronic acid with subsequent excretion by the kidneys. The half-life (T1/2) of dexketoprofen is 1.65 h. In elderly patients the elimination half-life is prolonged up to 48% and total clearance of the drug decreases.

Indications

Active ingredient

Composition

Active ingredient: Dexketoprofen trometamol – 36.90 mg, (Dexketoprofen equivalent) – 25.00 mg.

Auxiliary substances:microcrystalline cellulose, corn starch, sodium carboxymethyl starch (type A), glycerol distearate.

Film coating:hypromellose, titanium dioxide (E 171), macrogol 6000, propylene glycol.

How to take, the dosage

The drug Dexalgin ® 25 is taken orally with meals. Simultaneous intake of food slows down absorption of Dexectoprofen, therefore in case of acute pain it is recommended to use the drug at least 30 minutes before a meal.

Depending on the intensity of the pain syndrome, the recommended dose for adults is 12.5 mg dexketoprofen (1/2 tablet of the drug Dexalgin

sup>® 25) every 4-6 hours or 25 mg dexketoprofen (1 tablet of Dexalgin® 25) every 8 hours.

The maximum daily dose is 75 mg.

The drug Dexalgin® 25 is not intended for long-term therapy, the course of treatment with the drug should not exceed 3-5 days.

Patients 65 years and older

Patients of advanced age should take Dexalgin® 25 starting with the lowest recommended dose. The maximum daily dose is 50 mg. If well tolerated, doses recommended for the general population may be used.

Patients with hepatic impairment

Patients with mild to moderate hepatic impairment should take Dexalgin® 25 starting with the minimum recommended dose. The maximum daily dose is 50 mg.

The use of Dexalgin® 25 in patients with severe hepatic impairment is contraindicated.

Patients with renal insufficiency

. Patients with mild renal insufficiency – chronic kidney disease, stage 2 (GFR 60-89 ml/min/1.73 m2) should take Dexalgin® 25 starting with the lowest recommended dose. The maximum daily dose is 50 mg. The use of Dexalgin® 25 in patients with chronic kidney disease stages 3a (FFR 45-59 ml/min/1.73 m2), 3b (FFR 30-44 ml/min/1.73 m2) and 4 (FFR < 30 ml/min/1.73 m2) is contraindicated.

Interaction

The following interactions are typical for all NSAIDs.

Unwanted combinations

With other NSAIDs, including salicylates in high doses (more than 3 g/day): concomitant use of multiple NSAIDs due to synergistic effects increases the risk of gastrointestinal bleeding and ulceration.

With anticoagulants:Dexketoprofen, like other NSAIDs, may increase the effect of anticoagulants such as warfarin due to the high degree of binding to plasma proteins, inhibition of platelet aggregation and damage to the gastrointestinal mucosa. If concomitant use is necessary, close monitoring of the patient’s condition and regular monitoring of laboratory parameters are required.

With heparin:concomitant use increases the risk of bleeding (due to inhibition of platelet aggregation and damaging effect on gastrointestinal mucosa). If simultaneous use is necessary, close monitoring of the patient’s condition and regular monitoring of laboratory parameters are required.

With glucocorticosteroids: Concurrent use increases the risk of gastrointestinal ulcers and bleeding.

With lithium preparations:Lithium NSAIDs increase the concentration of lithium in plasma up to toxic concentration and therefore this index must be controlled when using with Dexectoprofen, when changing the dosage and also after discontinuation of NSAIDs.

With methotrexate at high doses (15 mg/week or more):Hematological toxicity of methotrexate may increase due to decreased renal clearance with NSAIDs.

With hydantoins and sulfonamides:their toxic effects may be increased.

Combinations requiring caution

Combinations.With diuretics, angiotensin-converting enzyme (ACE) inhibitors, antibiotics from the group of aminoglycosides, angiotensin-II receptor antagonists: concomitant use with NSAIDs is associated with the risk of acute renal failure in dehydrated patients (decreased glomerular filtration due to reduced prostaglandin synthesis). Concomitant use of NSAIDs may reduce the antihypertensive effect of some drugs. In concomitant use of dexectoprofen and diuretics it is necessary to make sure that the patient does not have signs of dehydration, and also at the beginning of concomitant use monitor renal function.

With methotrexate at low doses (less than 15 mg/week):Hematological toxicity of methotrexate may increase due to decreased renal clearance in combination with NSAIDs. Blood cell counts are necessary at the beginning of concomitant use. In the presence of renal dysfunction, even of mild degree, as well as in elderly patients, close medical supervision is necessary.

With pentoxifylline:the risk of bleeding may increase. Close clinical monitoring and regular monitoring of bleeding time (clotting time) is necessary.

With zidovudine:there is a risk of increased erythrocyte toxicity due to effects on reticulocytes, with development of severe anemia one week after initiation of NSAID use. It is necessary to perform a general blood test with reticulocyte count 1-2 weeks after the start of NSAID therapy.

With oral hypoglycemic agents: NSAIDs may increase the hypoglycemic effect of sulfonylurea drugs due to displacement of sulfonylurea from plasma protein binding sites.

Combinations to be considered

With β-adrenoblockers: When used concomitantly with NSAIDs, the antihypertensive effect of β-adrenoblockers may be reduced due to inhibition of prostaglandin synthesis.

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

With thrombolytics:the risk of bleeding increases.

The risk of bleeding from the gastrointestinal tract is increased when concomitant use with serotonin reuptake inhibitors (citalopram, fluoxetine, sertraline) and anticoagulants.

With probenecid:Possible increase in plasma concentrations of NSAIDs, which may be due to the inhibitory effect of probenecid on renal tubular secretion and/or conjugation with glucuronic acid; dosage adjustment of NSAIDs may be required.

With cardiac glycosides: Concomitant use with NSAIDs may lead to increased plasma concentrations of cardiac glycosides.

With mifepristone: Due to the theoretical risk of prostaglandin inhibitors changing the effectiveness of mifepristone, NSAIDs should not be used earlier than 8-12 days after mifepristone withdrawal.

With quinolones:The data obtained in experimental animal studies indicate a high risk of seizures when NSAIDs are used simultaneously with quinolones at high doses.

If simultaneous use of Dexalgin® 25 with the above drugs is necessary, a physician should be consulted.

Special Instructions

Indesirable side effects can be minimized by using the drug at the lowest effective dose with the shortest duration of use necessary for pain relief.

The risk of GI complications is increased in patients with a history of GI ulcers, in elderly patients, with increasing doses of NSAIDs; therefore, Dexalgin® 25 should be started with the lowest recommended dose in these patients.

Patients in the above categories, as well as patients who require concomitant use of low doses of acetylsalicylic acid or other agents that increase the risk of GI complications, additional concomitant use of gastroprotectors (misoprostol or proton pump blockers) is recommended.

In patients concomitantly taking anticoagulants or anticoagulants, glucocorticosteroids, the risk of gastrointestinal bleeding also increases.

Patients with gastrointestinal disorders or a history of gastrointestinal disease should be under close medical supervision. If gastrointestinal bleeding or ulcerative lesions occur, the use of Dexalgin® 25 should be discontinued.

The drug Dexalgin ®25 should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease) because exacerbation of these diseases is possible.

All NSAIDs may inhibit platelet aggregation and increase bleeding time due to inhibition of prostaglandin synthesis. In this regard, the use of Dexalgin® 25 in patients simultaneously taking drugs that affect the hemostatic system, such as warfarin, coumarin derivatives and heparins, is not recommended.

Like other NSAIDs, Dexalgin® 25 may increase plasma creatinine and nitrogen concentrations. Like other inhibitors of prostaglandin synthesis, Dexalgin® 25 may have adverse effects on the urinary system, which may lead to glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure. Caution should be exercised when using the drug in patients concomitantly using diuretics and in patients who may develop hypovolemia due to increased risk of nephrotoxicity.

As with other NSAIDs, during the therapy with Dexalgin® 25 a slight transient increase of liver enzymes activity may be observed. In elderly patients it is necessary to monitor the liver and renal function. In case of significant increase of the corresponding indicators the use of Dexalgin® 25 should be discontinued.

Like other NSAIDs, Dexectoprofen may mask the symptoms of infectious diseases. If signs of infection or worsening of well-being are found while using Dexalgin® 25, the patient should consult a physician immediately.

The drug may cause fluid retention in the body, therefore Dexalgin® 25 should be used with extreme caution in patients with arterial hypertension, renal and/or heart failure. If the condition worsens, the use of Dexalgin® 25 should be discontinued.

In patients with uncontrolled arterial hypertension, coronary heart disease, congestive heart failure, peripheral artery disease and/or cerebrovascular disease the drug should be used with caution. The same approach is applicable for patients with risk factors of cardiovascular diseases (arterial hypertension, hyperlipidemia, diabetes mellitus, smoking).

Persons with a history of cardiovascular disease, especially those with heart failure, should be cautious when prescribing Dexalgin® 25 because of the possible risk of progression.

Clinical studies and epidemiological data suggest that NSAIDs, especially at high doses and with long-term use, may result in a small risk of acute myocardial infarction or stroke. There are insufficient data to exclude the risk of these events with dexectoprofen.

Elderly patients are particularly susceptible to adverse reactions when using NSAIDs, including the risk of gastrointestinal bleeding and perforations, which are life-threatening for the patient, decreased renal, hepatic and cardiac function. Proper clinical monitoring is necessary when using Dexalgin® 25 in this patient population.

There are data on the occurrence of rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) when using NSAIDs. At the first manifestations of skin rash, lesions of mucous membranes or other signs of allergic reactions the use of Dexalgin® 25 should be stopped immediately and a physician should be consulted.

Influence on driving and other machinery

In view of possible dizziness and drowsiness during the use of Dexalgin.sup>® 25, concentration ability and psychomotor reaction speed may decrease in patients, especially in the first hour after administration. Therefore, during the use of the drug Dexalgin® 25, caution should be exercised while driving vehicles and engaging in potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

Contraindications

Side effects

Possible side effects are listed according to World Health Organization classifications below in descending order of frequency of occurrence: very frequently (≥ 1/10), frequently (≥ 1/100, < 1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, < 1/1000), very rarely (< 1/10000) including individual reports.

Blood and lymphatic system disorders

Very rare: neutropenia, thrombocytopenia.

Disorders of the immune system

Rarely: laryngeal edema;

very rare:anaphylactic reactions, including anaphylactic shock.

Nervous system disorders

Infrequent: headache, dizziness, somnolence;

Rarely:paresthesias, syncopal states (transient transient syncope).

Mental disorders

Infrequent:insomnia, feelings of anxiety.

Hearing organ and labyrinth disorders

Infrequent: vertigo;

very rarely: tinnitus.

Visual disturbances

very rarely:blurred vision.

Disorders of the cardiovascular system

Infrequent: palpitations, fever, skin hyperemia;

Rarely: increased blood pressure;

very rarely: tachycardia, decreased blood pressure.

Relatory system disorders

Rarely: bradypnea;

very rarely: bronchospasm, dyspnea.

Gastrointestinal tract disorders

Frequently: nausea, vomiting, abdominal pain, dyspepsia, diarrhea;

Infrequent: gastritis, constipation, dry mouth, flatulence;

Rarely: gastrointestinal (GI) ulcerative lesions, ulcer bleeding or perforation;

very rare:pancreatic lesions.

Liver and biliary tract disorders

Rarely: hepatitis, increased activity of “liver” enzymes (ALT, AST);

very rare:liver damage.

Renal and urinary tract disorders

Rarely: polyuria, acute renal failure;

very rarely: nephritis or nephrotic syndrome.

Reproductive system disorders

Rarely: In women, menstrual disorders; in men, transient impairment of prostate function with prolonged use.

Motor system disorders

Rarely:back pain.

Skin and subcutaneous tissue disorders

Infrequent: skin rash;

Seldom: urticaria, acne, increased sweating;

Very rare: severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome)), angioedema, facial edema, allergic dermatitis, photosensitization, skin itching.

Metabolic disorders

Rarely:anorexia.

General disorders

Infrequent: increased fatigue, asthenia, chills, general malaise;

very rarely:peripheral edema.

As with other NSAIDs, the following side effects are possible: aseptic meningitis, developing mainly in patients with systemic lupus erythematosus or other systemic connective tissue diseases, hematological disorders (thrombocytopenic purpura, aplastic and hemolytic anemia, in rare cases – agranulocytosis and bone marrow hypoplasia).

Overdose

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

Treatment:symptomatic therapy, if necessary – gastric lavage, taking activated charcoal; hemodialysis is ineffective.

Pregnancy use

Similarities