Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Anti-inflammatory non-steroidal drug from the sulfonamide . Has anti-inflammatory, antipyretic and analgesic effects.
Wikipedia indicates that the active substance acts as a type 2 cyclooxygenase , responsible for the biosynthesis of prostaglandins .
Pharmacokinetics
After administration, it is well absorbed from the intestines, reaching its highest concentration in the blood after 2-3 hours. Reaction with plasma proteins is 97.5%. The half-life is 4-5 hours. Quickly penetrates histohematic barriers.
Transformed in the liver under the influence of cytochrome P450 . The main active metabolite is hydroxynimesulide , which is excreted in bile in a glucuronidated form. It is excreted from the body mainly by the kidneys (about half of the dose taken).
Pharmacological properties
The active component of Nimesil powder is a selective antagonist of the COX-2 enzyme (cyclooxygenase-2), suppressing its activity. COX-2 catalyzes the conversion of arachidonic acid into the main mediators of the inflammatory reaction, prostaglandins, which are synthesized by cells of the immune system in response to the development of a pathological process. A decrease in the concentration of prostaglandins leads to a decrease in the manifestations of the inflammatory reaction, which include pain (prostaglandins irritate sensitive nerve endings), tissue swelling (the release of the liquid part of the blood from the vascular bed into the intercellular substance of the tissues), as well as stagnation of blood in the vessels of the microvasculature.
After taking a suspension prepared from Nimesil powder, the active component is quickly and completely absorbed into the blood. It is evenly distributed in tissues, where it has therapeutic effects. Nimesulide is metabolized primarily in the liver to form inactive products that are excreted in the urine. The half-life (the time it takes for half the entire dose of a drug to be eliminated from the body) for nimesulide is about 6 hours.
Contraindications for Nimesil
Contraindications for use:
- history of hepatotoxic reactions
- bronchospasm , urticaria , rhinitis associated with the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs in the anamnesis;
- concomitant use of drugs with potential hepatotoxicity;
- condition after coronary artery bypass surgery ;
- inflammatory bowel diseases ( ulcerative colitis, Crohn's disease ) in the acute stage;
- increased body temperature in infectious and inflammatory diseases;
- exacerbation of peptic ulcer , ulcer , perforation or bleeding in the digestive tract;
- a combination of bronchial asthma , nasal polyposis and intolerance to non-steroidal anti-inflammatory drugs ;
- bleeding of cerebrovascular or other localizations; diseases accompanied by pathological bleeding;
- decompensated heart failure;
- severe blood clotting disorders;
- decompensated renal failure, hyperkalemia;
- liver diseases;
- liver failure;
- alcoholism , drug addiction;
- pregnancy or lactation ;
- age under 12 years;
- hypersensitivity to the components of the drug.
The abstract recommends using the drug Nimesil with caution if severe forms type 2 diabetes mellitus or arterial hypertension ; ischemic disease, heart failure, dyslipidemia , cerebrovascular diseases, peripheral arterial diseases, old age; peptic ulcer in the past, infections associated with Helicobacter pylori; long-term previous use of non-steroidal anti-inflammatory drugs ; decompensated somatic diseases; with smoking and concomitant treatment with anticoagulants, oral glucocorticosteroids, antiplatelet agents, selective serotonin reuptake blockers.
Nimesil for toothache
The active substance Nimesil is an aniline derivative and is widely used to treat inflammatory diseases. The mechanism of action is to stop the synthesis of prostaglandins. Already 30 minutes after taking a single dosage of Nimesil, the main symptoms of inflammation decrease: swelling and pain. The drug specifically acts on the accumulation of lymphatic fluid, reducing unpleasant symptoms.
Nimesil alleviates the condition of the following diseases:
- toothache of various etiologies
- flux
- periodontitis of the tooth
- gingivitis
- damage to the integrity of the tooth as a result of trauma.
Nimesil powder for toothache should be diluted in warm boiled water. The contents of the sachet are stirred in 100 ml of liquid until a homogeneous consistency is obtained. Repeated administration of the drug is possible only after 12 hours.
20 minutes after administration, the concentration of the active substance in the body is 50%. This is enough to suppress the inflammatory process. The duration of action of Nimesil is about 5-6 hours.
Side effects
For toothache, headaches , colds, and menstruation, Nimesil is often used in medical practice, which can cause the following side effects:
- allergic reactions - sweating , rash , itching , erythema, anaphylactoid reactions, dermatitis, urticaria, erythema multiforme, angioedema, Stevens-Johnson syndrome, Lyell's syndrome ;
- hematopoietic disorders - eosinophilia, pacitopenia, anemia, thrombocytopenia, hemorrhagic syndrome, thrombocytopenic purpura;
- visual disturbances – blurred vision;
- disorders of nervous activity - feelings of fear, dizziness , headache , nightmares, drowsiness , nervousness, encephalopathy ;
- circulatory disorders - hot flashes, tachycardia, arterial hypertension , sudden changes in blood pressure ;
- digestive system disorders - nausea, diarrhea , vomiting, flatulence, constipation , abdominal pain, gastritis , dyspepsia , tarry stools, stomatitis , bleeding from the digestive tract, gastric perforation or ulcer duodenal perforation or ulcer , hepatitis, cholestasis, jaundice , increased levels of liver enzymes ;
- breathing disorders - shortness of breath , attacks of bronchial asthma ;
- general disorders – asthenia , general malaise, hypothermia ;
- disorders of the genitourinary system - renal failure, hematuria , urinary retention, dysuria , oliguria, interstitial nephritis ;
- other disorders – hyperkalemia .
Instructions for use of Nimesil (Method and dosage)
Instructions on how to dilute Nimesil
The drug in powder (granules) is placed in a glass and diluted in approximately 100 ml of water. The prepared solution cannot be stored; it must be taken as soon as possible. There is a common question: “in what water should the powder be dissolved?” The instructions recommend dissolving the medicine in warm, boiled water.
Nimesil powder, instructions for use
The medicine (after preparation) is taken orally, 1 sachet twice a day, after meals. The maximum duration of treatment is two weeks.
To reduce the risk of side effects, it is recommended to use the lowest effective dosage for the shortest possible period of time.
Instructions for use of Nimesil for children
Nimesil (as well as tablets or ointment based on nimesulide ) is prohibited for use in children under 12 years of age. Children 12-18 years old are recommended to take standard doses.
Instructions on how to take granules for people with kidney disorders
There is no need to change the dose in persons with mild to moderate renal impairment.
How to take Nimesil powder for elderly patients
When treating elderly patients, the need to change the daily dosage is determined by the doctor, taking into account the possibility of interaction with other medications taken.
How to dilute Nimesil powder?
Nimesil powder is intended for the preparation of a suspension that is taken orally. The contents of the sachet are dissolved in approximately 100 ml of water at room temperature. A white or light yellow suspension is formed. The prepared suspension should be used immediately; it cannot be stored.
The diluted Nimesil solution has a pleasant orange smell and taste.
Overdose
Signs of overdose: vomiting, drowsiness, apathy , nausea, epigastric pain. The development of gastrointestinal bleeding is possible. In extremely rare cases, there is a possibility of increased blood pressure, acute kidney failure, respiratory depression, anaphylactoid reactions, and coma .
Treatment of overdose is symptomatic. selective antidote . If no more than 4 hours have passed since the overdose, it is necessary to rinse the stomach and ensure the intake of enterosorbenes , for which activated charcoal or an osmotic laxative . Monitoring the functioning of the kidneys and liver is indicated.
Nimesil and Nimesulide are the same thing, which is better
Nimesulide tablets are produced by domestic pharmaceutical factories. It contains the same active ingredient as Nimesil, so their therapeutic properties are absolutely similar.
But there are differences: the powder acts faster. After all, after taking Nimesulide, it takes time to release the main component from the base of the tablets.
Interaction
When used simultaneously with glucocorticosteroids ulcers or bleeding from the stomach and intestines increases
When used with antiplatelet agents and selective serotonin reuptake inhibitors, the likelihood of gastric or intestinal bleeding also increases.
Non-steroidal anti-inflammatory drugs may enhance the effects of anticoagulants , so this combination is not recommended for persons with severe coagulation . If this combination cannot be avoided, careful monitoring of blood clotting parameters is necessary.
Anti-inflammatory non-steroidal drugs can weaken the effects of diuretics .
Nimesulide is able to temporarily reduce the evacuation of sodium and potassium under the influence of Furosemide and thereby weaken the diuretic effect of the latter. It must also be remembered that such co-prescription of drugs requires caution in persons with impaired renal and cardiac function.
Nonsteroidal anti-inflammatory drugs may reduce the effect of antihypertensive drugs . In persons with compensated renal failure, with the simultaneous administration of ACE blockers , angiotensin type II receptor antagonists or cycloxygenase inhibitors , progression of renal function deterioration and the development of reversible renal failure .
Anti-inflammatory non-steroidal drugs reduce the clearance of lithium , which causes an increase in the level of the latter in the blood.
When prescribing Nimesil less than a day before or after using Methotrexate, caution must be exercised, since in such cases the content of Methotrexate in the blood and its toxic effects may increase.
Nimesulide is capable of stimulating the nephrotoxicity of cyclosporines .
How long does it take for Nimesil to start working?
Liquid forms of painkillers are quickly absorbed in the digestive system. The active substance enters the stomach already dissolved, which reduces the time spent on breaking down tablets or capsules.
Pain reduction begins within 10-15 minutes. The maximum effect develops 2 hours after application. It is at this time that the maximum concentration of the active substance in the blood is reached. The effect of Nimesil lasts for 6-12 hours, after which the drug is gradually eliminated from the body.
special instructions
Side effects can be minimized by using the lowest effective dosage of the drug in a minimally short course.
Nimesil powder medicine should be used with caution in persons with a history of gastrointestinal diseases, since exacerbation of these diseases is possible.
Since the drug is partially evacuated by the kidneys, its dosage for persons with impaired renal function should be reduced depending on the volume of urine excreted.
When the first symptoms of liver damage appear (itching, yellowing of the skin, nausea, abdominal pain, vomiting, dark urine, increased liver transaminases), you must stop taking the medication and consult a doctor.
If any signs of visual impairment appear during drug therapy, the patient should be examined by an ophthalmologist.
Nimesil can provoke fluid retention in the body, so people with high blood pressure and heart disease should use the drug with extreme caution.
If symptoms of an acute respiratory infection of a viral nature occur during drug therapy, Nimesil should be stopped.
Nimesil should not be used simultaneously with other anti-inflammatory non-steroidal drugs .
Nimesulide can change the characteristics of platelets , so care must be taken when using the drug in patients with hemorrhagic diathesis . It is worth remembering that the medicine does not replace the preventive effect of acetylsalicylic acid for diseases of the circulatory system.
Nimesil for headaches
Nimesil quickly and effectively eliminates the cause of headaches by blocking pain impulses. The drug is applicable for pinching, compression of the vertebrae (osteochondrosis), migraine. Indications for use of Nimesil are mild to moderate headaches.
The drug differs from other analgesics in its rapid relief of headaches. Symptoms usually go away within 5-10 minutes after application. The effect of Nimesil lasts for 6 hours. Repeated administration of the drug is possible no earlier than after 8 hours. The optimal regimen for use is to dilute the powder 2 times a day with an interval of 12 hours.
If symptoms do not go away within 3 days, you should consult a doctor for advice.
Nimesil's analogs
Level 4 ATX code matches:
Nimulid
Diacerein
Aponil
Chondroitin sulfate
Sigan
Don
Nimegesic
Artiflex
Nimika
Artron Hondrex
Artron Flex
Artron Complex
Arthroker
Arthrodarin
Nemulex
Chondroitin
Glucosamine Hydrochloride
Glucosamine
Nimid Forte
Nimid
The price of Nimesil analogues is usually lower than that of the described product. Below are medications with an identical composition that can replace Nimesil: Ameolin (tablets), Aponil (tablets), Affida Fort (granules for preparing a suspension), Mesulide (tablets), Nise (tablets, suspension), Nigan (tablets), Nimegesic ( tablets, suspension), Nimesin (tablets), Nimesulide (tablets, gel), Nimid (tablets, granules), Nimujet (injection solution), Nimulid (tablets, suspension, injection solution, gel), Nimuspaz (tablets), Pansulide (tablets ), Remesulide (tablets), Sulidin (gel), Taro-Sanovel (tablets).
Nise or Nimesil - which is better?
Nise and Nimesil are analogues. The main difference between the drugs is that the first is available in the form of a gel for topical use and tablets, and the cost of Nise is an order of magnitude lower. The choice should be made based on the doctor’s recommendations, type of indication and economic considerations.
Peculiarities
Before you start taking a suspension prepared from Nimesil powder, it is important to carefully read the instructions for the medication. There are several features of the correct use of the drug, which include:
- The active ingredient of the drug may interact with drugs from other pharmacological groups, so when using them you should consult a medical specialist.
- The likelihood of developing negative reactions is reduced when using the drug for a minimum course in an effective minimum dosage.
- Moderate kidney failure requires a reduction in the dosage of Nimesil powder.
- An auxiliary component of the drug is sucrose, which must be taken into account when prescribing to patients with concomitant diabetes mellitus.
- Nimesil powder should not be taken simultaneously with other non-steroidal anti-inflammatory drugs.
- The effect of the drug on the functional activity of the central nervous system has not been reliably studied, therefore, while using Nimesil powder, it is recommended to be careful when engaging in activities that require a sufficient speed of reactions.
In the pharmacy chain, Nimesil powder is available with a doctor's prescription. It is not recommended to take the drug on your own without appropriate prescriptions.
Nimesil for children
Nimesil (as well as tablets or ointment based on nimesulide ) is prohibited for use in children under 12 years of age. The instructions for the drug for children indicate that the method of using Nimesil (how to apply and how to dilute the powder) is no different for other age groups. How to use the powder, how to dilute Nimesil in powder, as well as how to drink Nimesil in powder, is described in the section “Instructions for use of Nimesil (Method and dosage)”
Is it possible to give Nimesil to children with fever?
This medicine is not the drug of choice for reducing body temperature, although it has a mild antipyretic effect. Nimesil should be used only for the purpose of relieving mild and moderately mild pain. Prohibited for the treatment of children under 12 years of age.
Is it possible to drink Nimesil during pregnancy?
Like other drugs from the class of NSAIDs that inhibit prostaglandin synthesis, nimesulide can adversely affect the course of pregnancy and/or embryo development and can lead to premature closure of the ductus arteriosus, hypertension in the fetal pulmonary artery system, impaired renal function, which can progress to renal failure with oliguria in the fetus, an increased risk of bleeding, decreased contractility of the uterus, and the occurrence of peripheral edema in the mother.
Data obtained from epidemiological studies indicate a possible increase in the risk of spontaneous abortion, the risk of heart disease and gastroschisis when using drugs that block prostaglandin synthesis in early pregnancy. The absolute risk of developing a cardiovascular abnormality increases from approximately 1% to 1.5%. The risk is believed to increase with increasing dose and duration of use.
There is no data on the penetration of nimesulide into breast milk.
The use of Nimesil during pregnancy and breastfeeding is contraindicated.
The use of nimesulide may adversely affect female fertility and is not recommended for women planning pregnancy. When planning a pregnancy, consultation with your doctor is necessary.
Reviews about Nimesil
For toothache and other types of pain (associated with injuries, algodismenorrhea ), Nimesil powder is widely used. Reviews of its use among patients are positive and there is little evidence of the development of undesirable effects.
Reviews from doctors about Nimesil also well characterize the drug as a remedy that effectively relieves pain of a traumatic nature and pain localized in the musculoskeletal system. However, it is worth remembering that in a number of countries nimesulide are completely prohibited due to increased hepatotoxicity.
Is Nimesil an antibiotic or not?
A common question among patients. Nimesil is not an antibiotic and does not have an antibacterial effect. Its main effects: antipyretic, analgesic, anti-inflammatory.
Indications for use
Taking a suspension prepared from Nimesil powder is indicated to reduce the severity of the inflammatory reaction and pain in certain diseases, which include:
- Pain in the back, lower back, which is of inflammatory origin.
- Various pathological processes in the structures of the musculoskeletal system, which include previous injuries, inflammation of the ligaments (tendinitis), sprains, dislocations and subluxations of various joints.
- Toothache.
- Headache of various origins, including moderate migraine.
- Painful menstruation in women (dysalgomenorrhea).
The drug is intended only for symptomatic and pathogenetic treatment of pain and inflammatory syndrome. It does not affect the main cause of the development of the pathological process.
Nimesil price, where to buy
The price of Nimesil powder (9 sachets) in Russia reaches 615 rubles. For comparison, the price of 1 sachet of Nimesil is 25-32 rubles.
The average price in Ukraine for drug No. 1 is approximately 9 hryvnia, and the price of a package including 30 sachets ranges from 210-260 hryvnia.
How much does the analogue of Nimesil Nise cost?
The cost of this drug in Russia in the form of 100 mg tablet No. 20 is 175-215 rubles, and the ointment of the same name 1% 20 grams will cost 180-200 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Nimesil granules for Prig Susp.
for internal approx. 100 mg pack. 2g 9 pcs Laboratorios Menarini/Fine Foods & Pharmaceuticals RUB 324 order - Nimesil granules for Prig Susp. for internal approx. 100 mg 30 pcs. Laboratorios Menarini/Fine Foods & Pharmaceuticals
RUR 665 order
Pharmacy Dialogue
- Nimesil (pack 2g No. 30)Berlin-Chemie AG/Menarini
RUR 724 order
- Nimesil (pack No. 1)Berlin-Chemie AG/Menarini
RUR 773 order
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Pharmacy24
- Nimesil 2 g N30 powder Laboratorios Menarini S.A./Fine Foods and Pharmaceuticals N.T.M.S.P.A., Spain/Italy
279 UAH.order
PaniPharmacy
- Nimesil Nimesil granules for the preparation of suspension 100 mg 2 g No. 30 Spain, Lab. Menarini
314 UAH. order
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Release form, composition
The drug Nimesil is available in a dosage form, a powder for the preparation of a suspension, which is intended for oral administration. It has a light green color, coarse grain, and an orange scent. The main active component of the drug is nimesulide, its content in 1 sachet of powder is 100 mg. The drug also contains additional compounds, which include:
- Sucrose.
- Orange flavor.
- Ketomacrogol.
- Anhydrous citric acid.
- Maltodextrin.
Nimesil powder is packaged in aluminum foil bags of 2 g each. A cardboard pack contains 9, 15 or 30 bags.
