Nise-gel is a synthetic drug. It belongs to the category of Coxibs: non-steroidal anti-inflammatory drugs that have a selective effect on Cyclo-oxygenase-2 (COX-2).
COX-2 is an enzyme (catalyst) that affects the synthesis of prostaglandins. Prostaglandins are hormone-like substances with numerous functions, including effects on the inflammatory process.
Composition and pharmacological action
Nise-gel is available on the basis of Nimesulide, a non-acidic sulfonamide derivative. Nonsteroidal anti-inflammatory drugs of this class have a selective (selective) effect on cyclooxygenase-2, with little effect on COX-1.
The active substance Nimesulide inhibits the action of the enzyme COX-2, which is responsible for the production of inflammatory prostaglandins. Nonsteroidal anti-inflammatory drug reduces pain, reduces inflammation.
Pain syndrome has a complex mechanism of perception. Chemical, thermal, traumatic exposure leads to the response of the body - an increase in blood levels of histamine and bradykinin (organic compounds).
Prostaglandins are regulators and mediators in the development of a pathological reaction to an exogenous (external) or endogenous (internal) stimulus.
When the levels of bradykinin and histamine exceed the genetically determined threshold, pain receptors (nociceptors) are connected. According to them, the signal enters the spinal cord, and then into the brain.
Nociceptive neurons are located in the upper layers of the skin, periosteum, articular bag.
Prostaglandins enhance the sensitivity of nociceptors, reducing the pain threshold, increase the effectiveness of histamine (dilated capillaries, obstruction of outflow, the appearance of edema).
By its anti-inflammatory and analgesic effects, Nimesulide is inferior to acidic derivatives: Diclofenac, Ibuprofen, Indomethacin, Phenylbutazone, Acetylsalicylic acid.
According to the mechanism of action, Nimesulide exceeds the acid analogues of NSAIDs without causing such side effects. The cause of the sparing action is a selective effect on COX-2 (inflammatory enzyme) and to a lesser extent on COX-1 (protection enzyme).
Non-steroidal anti-inflammatory drugs of acidic origin act equally on COX-1, COX-2. The enzyme Cyclo-oxygenase-1 controls the production of prostaglandins, which perform a protective function of the mucous membrane of the stomach and bronchi. Reducing the number of prostaglandins leads to a stomach ulcer and bronchospasm.
Cyclo-oxygenases are involved in the synthesis of thromboxanes (derivatives of polysaturated fatty acids). Thromboxanes cause capillary constriction, platelet sticking. Inhibition of COX-2 creates the prerequisites for the development of peripheral vascular thrombosis.
Nimesulide affects lipid metabolism, which blocks the destruction of cartilage collagen. The drug is an antioxidant, reducing the amount of degradation products that cause toxic effects; interacts with hormonal receptors, activating them and enhancing the anti-inflammatory effect.
Indications and contraindications
Nise-gel is recommended for degenerative and inflammatory conditions of the bone and cartilage system, acute pain of any kind.
Indications for treatment:
- osteoarthritis (damage to the cartilage tissue of the joint);
- periarthritis (inflammation of the periarticular ligaments, muscles);
- tendinitis (inflammation of the tendons);
- tenosynovitis (inflammation of the tendon sheath);
- lumbago (acute pain in the lumbar region);
- sprains of muscles and ligaments;
- gout attack (diseases of the joints due to metabolic disorders);
- bursitis (inflammation of the articular bag);
- neuralgia (pain along the nerve);
- Bechterov's disease (diseases of the spine and joints);
- myalgia (muscle pain).
Contraindications:
- acute and chronic forms of gastric disease (gastritis, ulcer);
- liver failure;
- renal failure;
- pregnancy;
- lactation;
- viral and bacterial infection with fever and chills;
- children's age up to 7 years.
Instructions for use
Release form: an aluminum tuba of 20 and 50 g. Gel of 1%.
Active ingredient: Nimesulide. Used as an external agent. The dosage does not depend on age.
Method of application: 3 cm of gel is applied to the sore spot. Absorption occurs without rubbing into the skin; application under the dressing is not allowed.
The duration of therapy is at least 28 days, multiplicity 3-4 times a day. Place of application should be clean, dry, free from wounds, damage, signs of skin diseases.
The maximum concentration in the blood comes in a day. The analgesic effect is manifested in relieving pain, improving joint mobility.
After using an external agent, wash your hands thoroughly, avoiding contact with the gel in your eyes or mucous membranes.
If a similar situation arises, wash your eyes and mucous membranes under running water.
Store 2 years in a dark place at a temperature of +1 to +25 degrees.
Features of use during pregnancy and lactation
The use of the drug during pregnancy, starting from 6 months, can lead to complications. A side effect for a pregnant woman is the effect on the fetus: renal impairment, closure of the ductus arteriosus (botallova).
In the early stages (up to 20 weeks), the gel can cause a miscarriage, regardless of the amount applied.
When breastfeeding, Nimesulide passes into the milk, which can adversely affect kidney function and cause anemia.
Side effects and overdose
Excess doses or prolonged use of the drug cause side effects similar to those of non-selective NSAIDs.
Niz-gel in such cases can cause systemic disorders:
- digestive organs;
- the kidneys;
- the liver;
- central nervous system.
On the part of the gastrointestinal tract, the negative effect of the drug is manifested in the form of nausea and vomiting with a significant single overdose: 500 mg.
Reduced prostaglandin synthesis affects the blood supply to the kidneys. The result of taking an external agent can be renal failure, fluid retention in the body, increased blood pressure. Chronic kidney disease, especially in the acute stage, can cause puffiness and a decrease in excretory function.
Hepotoxicity of NSAIDs is due to the fact that the removal of the products of the decomposition of the Nise-gel occurs through the liver. Excess dosage causes signs of liver failure.
The local reaction of the gel - skin rash in the form of urticaria, itching, change in skin color.
Drug interactions, special instructions
Nimesulide has an effect through plasma proteins. Drugs that have a similar mechanism of influence, are competitors and can either block or enhance the therapeutic effect of the gel.
Do not use simultaneously with the following drugs:
- other types of NSAIDs;
- Digoxin;
- Phenytoin;
- Cyclosporine;
- diuretic;
- lowering pressure, blood sugar.
Inhibition of the enzyme inflammation of COX-2 causes a disturbance in the activity of the circulatory and hematopoietic systems: a narrowing of the peripheral vessels and an increase in blood clotting. The risk of myocardial infarction, stroke, thrombosis increases.
Price and analogues
Price Niz-gel from 149 rub. for 20 g, from 270 rubles. for 50 g. Manufacturing country India.
Generic drugs in tablet form (the same composition under a different name):
- Nimesan (from 137 rubles, India);
- Nimesulide-Teva (from 108 rubles, Israel);
- Nimika (from 129 rubles., India);
- Nimesil (from 676 rubles, USA)
Nonsteroidal anti-inflammatory drugs based on other active agents:
- Teraflex Chondrokrem Forte;
- Diclofenac gel;
- Voltaren emulgel;
- Fastum gel.
The choice of NSAIDs is diverse, has a large variation in price. Selection of the drug should be carried out individually, after establishing an accurate diagnosis.
Reviews
Often I have an aggravation of neuralgia on the outer side of the thigh. Diclofenac quickly relieves pain, but sensitively decreases urine flow. When applying Nize gel effect occurs more slowly, but there is no such side effects.
Valeria, 32 years old, Moscow
I apply Nise gel for the treatment of bursitis. Before that, he was treated with other non-steroid drugs. There have always been side effects from the stomach. Had to take gastric protectors. With Nise this does not happen.
Anatoly, 41, Omsk
Nise-gel is used as an anti-inflammatory agent for joint and muscle pain. The drug has a selective (selective) effect on the enzyme inflammation (COX-2) and a little affecting the protection enzyme (COX-1).
The mechanism of action is to block the pathways of signal transmission, reduce the symptoms of inflammation and swelling. The main contraindications are associated with complete and partial inhibition of COX-2 and COX-1. Drugs-analogues, with the exception of generics, have a wider range of contraindications due to non-selective nature.
Additional information about nonsteroidal anti-inflammatory drugs can be found in the following video.
