Features of the composition and pharmacological action of Dexalgin
The components of one tablet are presented:
- dexketoprofen trometamol;
- corn starch;
- glycerol palmitostearate;
- microcrystalline cellulose;
- titanium dioxide;
- propylene glycol;
- sodium carboxymethyl starch;
- hypromellose;
- Macragol 600.
The injection solution contains a similar active ingredient, additional components are sodium chloride and hydroxide, ethanol, and purified water.
The medicine is included in the subgroup of NSAIDs; half an hour after use, a decrease in pain and temperature is noted. The drug has an anti-inflammatory effect. The maximum concentration of Dexalgin when taken orally occurs after 40 minutes, the half-life by the kidneys does not exceed 2 hours. With MK injections it is achieved after 10 minutes.
The inflammatory reaction is a general biological response of the body to the action of any damaging factors. In periodontics, the damaging effects are caused largely by plaque microbes. In turn, the inflammatory reaction itself, especially pronounced and prolonged, leads to profound morphological and functional disorders in tissues. Therefore, if removal of dental plaque does not provide the desired effect, it is necessary to use anti-inflammatory drugs in complex pathogenetic therapy.
In dental practice, drugs of both general and local action are widely used [3, 5]. There are groups of pharmacological agents that have a direct effect on one or more phases of the inflammatory response simultaneously. Such drugs are actually anti-inflammatory. Like antibacterial, anti-inflammatory drugs should be prescribed only reasonably, taking into account the peculiarities of the course of the inflammatory process in each individual case.
If the constant change in the antibiotic market is determined mainly by the development of microbial resistance, then the search for new anti-inflammatory drugs is largely due to their lack of effectiveness and/or side effects.
Nonsteroidal anti-inflammatory drugs (NSAIDs) have an anti-inflammatory effect because they affect two phases of inflammation: exudative and proliferative. There are compelling reasons for their widespread use in the treatment of inflammatory periodontal lesions - gingivitis and periodontitis [1].
The mechanisms of the pathogenetic action of NSAIDs are that they, like hormonal drugs, stabilize cellular and intracellular membranes and suppress the synthesis of prostaglandins and small peptides (oligopeptides), which in turn are mediators of inflammation, pain and fever. This explains their not only anti-inflammatory, but also pronounced analgesic effect. In addition, NSAIDs reduce the level of free radicals in tissues and affect cells that are directly involved in inflammatory reactions. In particular, their effect on neutrophils increases the bactericidal effect of these cells. As a result, the destruction of pathogenic microorganisms is accelerated and the normalization of periodontal tissue occurs faster [6].
Due to the diversity of their chemical structure, a perfect classification of NSAIDs does not yet exist. There are many NSAIDs used in dentistry. Despite the diversity of the chemical structure of non-steroidal drugs, the main mechanism of action of most of them is the inhibition of the synthesis of prostaglandins, which take an active part in the formation and course of inflammatory reactions.
One of the leading positions in medical practice and in dentistry, in particular, over the last few decades has been occupied by the drug ketoprofen, a derivative of propionic acid. The drug is a racemic mixture of enantiomers. The mechanism of its action is associated with inhibition of the activity of cyclooxygenase, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever.
However, numerous studies have shown that only the S(+) isomer inhibits cyclooxygenase isoenzymes. In humans, approximately 10% of R(-)-ketoprofen is converted to the S(+) isomer, although this amount varies significantly between individuals. To increase therapeutic efficacy, the S(+)-isomer was isolated from the racemic mixture and presented in the form of a water-soluble salt as a new NSAID - dexketoprofen trometamol. As a result, the resulting salt of dexketoprofen trometamol has improved physicochemical properties, avoids the development of undesirable metabolic effects, and has low toxicity [2, 4].
In 2008, a new generation NSAID, dexalgin, was registered in Russia. The drug is widely used both in trauma medicine and in the complex treatment of chronic diseases. The main active ingredient is dexketoprofen trometamol. The combination of dexketoprofen with trometamol promotes accelerated absorption of the active substance and a rapid effect. Compared to ketoprofen, the maximum concentration of dexketoprofen trometamol achieves higher results, and the analgesic effect occurs faster - 30 minutes after administration and lasts 4-6 hours.
The high inhibitory activity of dexalgin against cyclooxygenases determines its peripheral and central analgesic effects, while the high anti-inflammatory activity of the drug is combined with good tolerability. However, in each specific case the possibility of side effects and contraindications should be taken into account.
Thus, the high efficiency and good safety profile of dexalgin suggest its wider use not only in general medical practice, but also in periodontology, in particular, both at the stages of eliminating acute inflammation and in the postoperative period.
Contraindications and indications for Dexalgin therapy
The instructions recommend using tablets to relieve pain caused by:
- surgical interventions - in the postoperative period;
- radiculitis, algodismenorrhea;
- menstruation, dental diseases;
- neuralgia, sciatica;
- arthrosis, rheumatoid arthritis;
- osteochondrosis, spondyloarthritis;
- proliferation of metastases in bone tissue.
The solution in injections is prescribed when it is impossible to take Dexalgin orally - after injuries, operations, and with renal colic.
The drug is contraindicated in patients:
- with individual intolerance to the component composition;
- pathologies of the gastrointestinal tract, heart, liver and kidneys;
- bronchial asthma;
- undergoing anticoagulant therapy.
Dexalgin is not prescribed to minors, during pregnancy and breastfeeding.
Indications
Dexalgin 25 is used to relieve pain of various origins (for example, with renal colic, toothache, neuralgia, radiculitis, as well as sciatica, with algodismenorrhea, in the event of post-traumatic and postoperative pain, pain with bone metastases).
Dexalgin 25 is indicated for the symptomatic treatment of both acute and chronic inflammatory, inflammatory-degenerative, and metabolic diseases of the musculoskeletal system (in the case of spondyloarthritis, rheumatoid arthritis, osteochondrosis and osteoarthritis).
In these cases, Dexalgin 25 is prescribed for pain relief and as an anti-inflammatory agent.
Adverse reactions
During therapeutic procedures, non-standard effects may occur, manifested by:
- vomiting with nausea, high blood pressure;
- tachycardia, nettle fever, chills;
- redness, skin rashes, dermatitis;
- anemic and fainting states, cephalalgia;
- sleep disturbances, digestive disorders, bleeding.
Dexalgin tablets can cause discomfort in the epigastric area and heartburn. The injection solution causes pain and local temperature increase in the injection area, hematomas and inflammation.
The medicine must not be mixed with alcoholic beverages. Violation of the rules can provoke severe intoxication with clinical symptoms of poisoning.
The nuances of taking Dexalgin
The instructions draw attention to the following rules for using tablets:
- the dosage is calculated by the doctor individually;
- a single dose is 0.5-2 tablets (25 mg each), procedures are performed 2-6 times a day;
- the maximum daily volume of medication cannot exceed 3 tablets;
- The duration of therapy is 5 days.
The injection solution is prescribed according to a specific scheme:
- intramuscular administration - 2 ml slowly, every 8-12 hours, 50 mg, daily dosage does not exceed 0.15 g, treatment lasts for 2 days;
- intravenous – carried out according to the dosages of intramuscular treatment, the medication is administered for about 15 seconds;
- drip – 2 ml of the drug is diluted in 100 ml of physiological solution, the dropper is placed for 15-30 minutes.
Accidentally taking an excess amount of medication provokes sleep disturbances, problems with orientation in space, cephalgia, and nausea. In case of intoxication, symptomatic therapy is used.
Mode of application
Dexalgin 25 is taken orally with meals.
The dosage depends on the intensity of the pain syndrome, with the recommended dose for adults being 12.5 mg (1/2 tablet) every 4-6 hours or 25 mg (1 tablet) every 8 hours. The maximum daily dose is 75 mg.
In patients of the older age group, as well as in patients with impaired liver and/or kidney function, use
Dexalgin 25 is started with lower doses, and the maximum daily dose is 50 mg.
It should be remembered that Dexalgin 25 is not intended for long-term therapy; the course of treatment should not exceed 3-5 days.
Features of interaction
The abstract draws attention to the following nuances of joint therapy with Dexalgin:
- an increased risk of bleeding occurs when using anticoagulants, NSAIDs, Heparin, Ticlopidine, Citalopram, Fluoxetine, Sertraline;
- danger of toxic effects on the body - when treated with lithium preparations, Methotrexate, sulfonamides;
- prohibition on combination with cardiac glycosides, thrombolytics, quinolones without supervision by the attending physician;
- The development of acute renal failure can be provoked by diuretics and ACE inhibitors.
The injection solution must not be mixed in the same syringe with individual medications, the list includes: Pethidine, Hydroxyzine, Dopamine, Promethesine, Pentazocine.
Dexalgin injection solution 25mg/ml 2ml amp 5 pcs
Dexalgin® should not be mixed in the same syringe with a solution of dopamine, promethazine, pentazocine, pethidine or hydroxyzine (a precipitate will form). Dexalgin® can be mixed in one syringe with a solution of heparin, lidocaine, morphine and theophylline.
Dexalgin® - diluted solution for infusion should not be mixed with promethazine or pentazocine.
Dexalgin® - diluted solution for infusion is compatible with the following injection solutions: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline.
When storing Dexalgin® - diluted solutions for infusion in plastic containers or when using infusion systems made from ethyl vinyl acetate, cellulose propionate, low-density polyethylene or polyvinyl chloride, absorption of the active substance by the listed materials does not occur.
The following interactions are common to all NSAIDs.
Undesirable combinations
With other NSAIDs, including salicylates in high doses (more than 3 g/day): simultaneous administration of several NSAIDs due to a synergistic effect increases the risk of gastrointestinal bleeding and ulcers.
With oral anticoagulants, heparin in doses exceeding prophylactic doses, 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, up to toxic levels, and therefore this indicator must be monitored when prescribing, changing the dose and after discontinuation of NSAIDs.
With methotrexate in high doses (15 mg/week or more): increased hematological toxicity of methotrexate due to a decrease in its renal clearance during NSAID therapy.
With hydantoins and sulfa drugs: the risk of increased toxic effects of these drugs.
Combinations requiring caution
With diuretics, angiotensin-converting enzyme inhibitors: NSAID therapy is associated with a risk of acute renal failure in dehydrated patients (decreased glomerular filtration due to reduced prostaglandin synthesis). NSAIDs may reduce the hypotensive effect of some drugs. When coadministered with diuretics, ensure that the patient's fluid balance is adequate and monitor renal function before prescribing NSAIDs.
With methotrexate in low doses (less than 15 mg/week): increased hematological toxicity of methotrexate due to a decrease in its renal clearance during NSAID therapy. It is necessary to conduct weekly blood cell counts during the first weeks of concomitant therapy. In the presence of even mild renal dysfunction, as well as in elderly people, careful medical supervision is necessary.
With pentoxifylline: increased risk of bleeding. Intensive clinical monitoring and frequent checking of bleeding time (blood clotting time) is necessary.
With zidovudine: risk of increased toxicity to red blood cells due to effects on reticulocytes, with the development of severe anemia one week after administration of NSAIDs. It is necessary to count all blood cells and reticulocytes 1-2 weeks after starting NSAID therapy.
With sulfonamide drugs: NSAIDs may enhance the hypoglycemic effect of sulfonylurea due to its displacement from sites of binding to plasma proteins.
With low molecular weight heparin preparations: increased risk of bleeding.
Combinations to consider
With beta-blockers: NSAIDs may reduce the hypotensive effect of beta-blockers due to inhibition of prostaglandin synthesis.
With cyclosporine and tacrolimus: NSAIDs may increase nephrotoxicity, which is mediated by the action of renal prostaglandins. During concomitant therapy, renal function should be monitored.
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, requiring NSAID dose adjustment.
With cardiac glycosides: NSAIDs may lead to increased plasma concentrations of glycosides.
With mifepristone: due to the theoretical risk of changes in the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors, NSAIDs should not be prescribed earlier than 8-12 days after discontinuation of mifepristone.
With ciprofloxacin: data obtained from experimental studies in animals indicate a high risk of developing convulsions when NSAIDs are prescribed during therapy with high doses of ciprofloxacin.
Analogs
If side effects or signs of intolerance to Dexalgin appear, the drug must be replaced with a suitable remedy. The list of analogues is presented:
- Depiofen, Brufen, Bofen;
- Vimovo, Brustan, Dexifen;
- Zo-tek, Ibuprex, Ibuprom;
- Ibunorm, Ibufen, Ibuprofen;
- Ibutard, Imet, Ketonal, Ivalgin;
- Irfen, Naproff, Majezik-sanovel;
- Novigan, Nurofen, Nurosan, Faspik, Promax.
The cost of the original and replacements may vary significantly.
Terms of sale and storage
Dexalgin is sold in pharmacies only with a doctor's prescription. The drug is stored in dark rooms at temperatures up to 25 degrees. The medicine is suitable:
- tablets - for 2 years, after expiration of the period they are disposed of together with household waste;
- solution in ampoules - up to 5 years; after preparation, the medicine retains its properties for no more than one day (provided the temperature is from 3 to 9 degrees and in a dark place).
Dexalgin in ampoules costs from 265 rubles, the price of tablets depends on the number of units in the package and starts from 279 rubles.
