"Nimesulide": reviews, application, analogues
Non-steroidal anti-inflammatory drugs are a special class of drugs that have three significant effects: anti-inflammatory, antipyretic and analgesic. Due to such pharmacodynamic features this group of drugs is widely used in practical medicine. Let's analyze the features of the use of the drug "Nimesulide", reviews of patients about this drug, as well as possible adverse effects and dosing features.
Pharmacodynamic features of
"Nimesulide" is a representative of a group of non-steroidal anti-inflammatory drugs. In its group, the drug belongs to selective inhibitors of the enzyme cyclooxygenase-2, which effectively ensures the suppression of prostaglandin production in the inflammatory focus.
Another distinguishing feature in the mechanism of action of the drug "Nimesulide" is its ability to inhibit the release of an enzyme called myeloperoxidase, which significantly inhibits the production of free radicals, without affecting the processes of chemo- and tigmotaxis, as well as phagocytosis. In addition, Nimesulide promotes the suppression of the formation of tumor necrosis factor and other mediators involved in inflammatory reactions of the body.
Pharmacokinetic features of
The main way of administration of this drug is oral, which is due to the high bioavailability of the drug, the rate of reaching the maximum concentration in the blood plasma of patients. Thus, the highest concentration is achieved after 120-180 minutes after administration, and the degree of binding of the drug to blood plasma proteins is close to 98% of the initially administered amount of Nimesulide( reviews of patients and doctors confirm this).
The main organ in which the metabolism of the drug occurs is the liver. Thus in the course of biotransformation an active metabolite is formed called hydroxynimidesulide. The main way to remove the drug is its excretion in the urine( this is how about 65% of the drug is excreted), about 35% of the drug is excreted with fecal masses.
Almost all patients before admission are interested in any additional information about the drug "Nimesulide".Instructions for use, analogs, indications and contraindications, side effects are the most frequently asked questions.
Indications for use
Indications for the appointment of the drug "Nimesulide" is not so much. Among them, there is an acute pain syndrome, a primary osteoarthritis with a pain syndrome, as well as a primary dysmenorrhea. In pediatric practice, the use of the drug is just as effective. This is evidenced by the feedback about the receipt of the Nimesulide funds. For children under 12 years of age it is not recommended to purchase it - this should be remembered.
Contraindications to the prescription of
Like all non-steroidal anti-inflammatory drugs, Nimesulide is contraindicated in the presence of a gastric ulcer or duodenal ulcer in the acute stage, reducing the detoxification function of the liver, concomitant administration of a drug with hepatotoxic drugs. The drug is contraindicated in people with a significant decrease in excretory function of the kidneys( creatinine clearance less than 30 ml / min), hematologic disorders and problems of the blood coagulation system, in patients with impaired cardiovascular function.
"Nimesulide" is contraindicated in patients with surgical pathology, pregnant and lactating, and children under 12 due to the high likelihood of adverse reactions. It is not necessary to appoint "Nimesulide" for the treatment of influenza and influenza-like conditions, hyperthermia.
Side effects of
This drug is characterized not only by its high anti-inflammatory activity, but also by the high incidence of adverse reactions. They occur, as a rule, during the first week of therapy with Nimesulide. Feedback on the occurrence of side effects leave much to be desired.
From the side of the skin and skin, side effects are associated with allergic manifestations and reactions to the drug, which are manifested in the form of pruritus and rash, dermatitis, redness, urticaria. Significantly less common side effects such as toxic epidermal necrolysis, Stevens-Johnson syndrome.
On the part of the gastrointestinal tract, bleeding and perforation of ulcerative defects are rarely possible. Much more often there are pain in the epigastric region, nausea, vomiting, diarrhea, or constipation.
From the central nervous system may occur apathy, excessive drowsiness, persistent headaches and unreasonable dizziness, vestibular disorders.
On the part of the hematopoiesis and cardiovascular system, the development of eosinophilia, thrombocytopenia and pancytopenia, anemic syndrome, tachycardia, increased blood pressure, the development of hyperkalemia.
Application of Nimesulide and feedback from
The use of Nimesulide has firmly taken its place in the clinical practice of rheumatological diseases of the musculoskeletal system. Despite significant limitations in indications to the drug "Nimesulide", reviews about it are positive because of its high effectiveness in the treatment of rheumatic diseases. This is due to the specificity of the effect on cyclooxygenase-2 and a high degree of selectivity to this enzyme.
Special instructions
What should I fear when taking a drug such as Nimesulide? Instructions for use, patients' reviews inform about some warnings. An important point in the appointment of the drug "Nimesulide" is the use of a minimal therapeutic dose of the drug. In the absence of efficacy of the drug with minimal dosing, the drug should be discontinued.
If the hepatotoxic action of the drug develops( which is monitored by biochemical blood counts), the drug should also be stopped immediately. This group of patients( in whom cell damage to the liver develops) is later prohibited the appointment of "Nimesulide."It should be noted that even in the absence of side effects from the liver, the drug should not be combined with hepatotoxic drugs, other non-steroidal anti-inflammatory drugs, analgesics. You should also refrain from drinking alcohol.
Nimesulide should be given with high caution to patients who have hepatic or renal failure to avoid the risk of progression of the latter.
Special attention should be paid to prescribing the drug to patients with influenza-like symptoms. This is due to the fact that "Nimesulide" has antipyretic effect and is able to mask the manifestations of bacterial infection.
Drug Interactions
Because of the high ability of the drug to cause intestinal bleeding, "Nimesulide" should not be combined with anticoagulants, such as "Warfarin", since there is a high risk of side effects.
The ability of the drug to disrupt the function of cytochrome P450 is known. In view of the inhibition of the functional activity of this enzyme, the dose of drugs metabolized by this cytochrome should be revised downward.
"Nimesulide": analogues, reviews
The main analogues( according to the active substance) are "Nimid", "Nimesil", "Remesulid", "Toro-sanovel".The drug is available in tablet form, a sachet of 100 mg or in the form of a gel of 10 mg( in 1 g of gel).The therapeutic activity of the analogues of the drug is good, so the reviews of the patients about them leave also positive. Patients, leaving about the tool "Nimesulid" reviews, pills get less than a drug in the form of a sachet.
Conclusion
"Nimesulide" is a powerful anti-inflammatory agent for the treatment of inflammatory diseases, mainly of the musculoskeletal system. In view of the high risk of side effects, it is essential to consult with your doctor about taking Nimesulide. The opinions of the doctors prescribing this drug and the patients taking it are positive, as it contributes to the rapid reduction of the symptoms of the disease.