2010/09/17

Actasulid

Composition, structure and packing

Tablets are round, smooth, pale yellow, with a dividing line on one side.

1 tab. - Nimesulide 100 mg

Excipients: lactose monohydrate, corn starch, silicon dioxide, povidone K-30, magnesium stearate.

Clinico-pharmacological group

NSAIDs. Selective COX-2 inhibitor

Pharmacological action

NSAID class of sulfone-anilidov. Is a selective competitive inhibitor of cyclooxygenase-2 (COX-2) - an enzyme involved in the synthesis of prostaglandins - mediators of edema, inflammation and pain. Has anti-inflammatory, analgesic and antipyretic effect expressed.

Reversible inhibition of prostaglandin E2 in the inflammation, and in the ways of ascending nociceptive system, including ways to conduct pain impulses of the spinal cord.

Reduces the concentration of short-lived prostaglandin H2, from which under the action of prostaglandin isomerase produced prostaglandin E2. Reducing the concentration of prostaglandin EP resulted in less activation prostanoidnyh EP type receptors, resulting in analgesic and anti-inflammatory effect.

Marginally affects COX-1, virtually preventing the formation of prostaglandin E2 from arachidonic acid in physiological conditions, which reduces the number of side effects of the drug. The drug also inhibits platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane A2 inhibits platelet aggregation factor, inhibits the activation of plasminogen by increasing the concentration of inhibitor-1. Inhibits release of histamine and reduces the degree of bronchoconstriction-induced histamine and acetaldehyde. Inhibits release of tumor necrosis factor α, causing the formation of cytokinins.

We show that nimesulide is able to suppress the synthesis of interleukin-6 and urokinase, thereby preventing the destruction of cartilage. Inhibits metalloproteinase (elastase, collagenase), preventing the destruction of proteoglycans and collagen of cartilage.

It has antioxidant properties, inhibits the formation of toxic decomposition products of oxygen by reducing the activity of myeloperoxidase. Interact with glucocorticoid receptors, activating them by phosphorylation, which also enhances anti-inflammatory drug.

Pharmacokinetics

Absorption of ingestion - is high. Eating lowers the rate of absorption, without affecting its degree. Time to reach Cmax of the active substance in the blood plasma - 1.5-2.5 hours Communication with plasma proteins is 95%, with the red cells - 2%, with lipoproteins -1%, with α1-acid glycoproteins - 1%.

The dose of the drug did not affect the degree of its binding with blood proteins. Cmax of nimesulide in plasma reaches 3.5-6.5 mg / liter. Vd - 0.19-0.35 L / kg. Penetrates the tissues of female genital mutilation, where, after a single administration, its concentration is about 40% of plasma concentrations. Well into the acidic environment chamber inflammation (40%), synovial fluid (43%). Easily penetrates through histohematogenous barriers.

Metabolised in the liver tissue monooxygenases. The main metabolite - 4-gidroksinimesulid (25%) has a similar pharmacological activity.

T1 / 2 of nimesulide was 1.56-4.95 h, 4-gidroksinimesulida - 2.89-4.78 pm 4-gidroksinimesulid displays kidneys (65%) and bile (35%). In patients with renal insufficiency (creatinine clearance 1.8-4.8 L / h or 30-80 ml / min), as well as children and the elderly pharmacokinetic profile of nimesulide has not significantly changed.

Indications for use of the drug
rheumatoid arthritis;
osteoarthritis;
arthritis of various etiologies;
arthralgia;
myalgia;
postoperative and posttraumatic pain;
bursitis;
tendenit;
algomenorrhea;
tooth and headache.

Dosage regimen

Inward 1 tablet (100 mg) 2 tablets taken with plenty of water preferably before meals. In the presence of digestive medicine is desirable to take at the end of a meal or after eating.

Children older than 12 years at the rate prescribed a single dose of 1.5 mg / kg body weight of the child 2-3, the maximum daily dose - 5 mg / kg. Teenagers with body weight over 40 kg - 100 mg no more than 2 times /

Side effect

The frequency is classified under the headings, depending on the occurrence of cases: very often (> 1 / 10), often (<1> 1 / 100), infrequent (<1> 1 / 1000), rarely ( <1> 1 / 10000), very rarely (<1 / 10000).
On the part of the digestive system: often - diarrhea, nausea, vomiting, infrequently - constipation, flatulence, gastritis, and very rare - abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum.
From the side of the central nervous system: Infrequent - dizziness, rarely - a feeling of fear, nervousness, nightmares, very rarely - headache, drowsiness, and encephalopathy (Reye syndrome).
On the part of the respiratory system: infrequent - wheeze, very rarely - asthma, bronchospasm.
Since the cardiovascular system: infrequent - arterial hypertension, rarely - tachycardia, hemorrhage, "tides".
From the sensory organs: rarely - blurred vision, very rarely - dizziness.
From the skin and mucous sheets: infrequent - itching, rash, sweating, rarely - erythema, dermatitis, very rarely - urticaria, angioedema, edema of the face, erythema multiforme exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the liver and biliary system: often - increased hepatic transaminases, very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.
From the kidney and urinary system: Infrequent - edema, rare - dysuria, hematuria, urinary retention, hyperkalemia, very rarely - renal failure, oliguria, interstitial nephritis.
On the part of the hemopoietic system: rarely - anemia, eosinophilia, very rarely - thrombocytopenia, pancytopenia, purpura, bleeding time prolongation.

Allergic reactions: seldom - hypersensitivity reactions, very rarely - anaphylactoid reaction.

General reactions: seldom - general weakness, very rarely - hypothermia.

In the case of others, not mentioned above side effects or worsening state of health should immediately seek medical attention.

Contraindications to the use of the drug
hypersensitivity;
erosive-ulcerative lesions GIT (exacerbation);
bleeding from the gastrointestinal tract;
intracranial hemorrhage;
"Aspirin" asthma;
hepatic impairment;
renal failure (CC less than 30 ml / min);
severe heart failure;
Pregnancy
lactation;
children's age (12 years).

Precautions: hypertension, heart failure, diabetes mellitus type 2.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Application for violations of liver function

The drug is contraindicated in hepatic failure.

Application for violations of renal function

The drug is contraindicated in renal failure (CC less than 30 ml / min).

Cautions

Aktasulid be applied with caution to patients who have observed a tendency to bleeding, patients with upper GIT or patients receiving drugs that reduce blood clotting, or drugs that inhibit platelet aggregation.

Since Aktasulid partly derived by the kidneys, the dose for patients with impaired renal function should be reduced depending on the level of urine.

Given the allegations of violations of patients taking other NSAIDs, treatment should be discontinued immediately in case of any breach of view, and the patient should be examined by a doctor, optometrist.

The drug can cause water retention in the tissues, so patients with high blood pressure and cardiac abnormalities Aktasulid should be applied with extreme caution. Patients should undergo regular medical control, if they, along with Aktasulidom take medications that affect the digestive tract.

Effects on ability to drive vehicles and management mechanisms

Patients whose labor activity requires concentration (sustained attention) should be aware that the drug may cause drowsiness or dizziness.

Overdose

Symptoms: lethargy, drowsiness, nausea, vomiting. They are usually reversible if the provision of supportive care. There may be a gastro-intestinal bleeding, arterial hypertension, acute renal failure, respiratory depression.

Treatment: Symptomatic treatment requires a patient and supportive care for him. No specific antidote. If an overdose has occurred in the last 4:00, it is necessary to induce vomiting, to ensure the reception of activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis and hemodialysis are not effective because of the high regard of the drug with proteins.

Drug Interactions

The drugs that reduce blood clotting, increases with their simultaneous application with nimesulide.

Nimesulide can reduce the effect of furosemide.

Nimesulide may increase the possibility of occurrence of side effects while taking methotrexate.

The level of lithium in the plasma increased, while taking drugs lithium and nimesulide.

Due to the high degree of binding of nimesulide to plasma proteins, patients are simultaneously treated with hydantoin and sulphonamide, should be under the supervision of a physician, passing examinations at short intervals.

Nimesulide may exacerbate the effects of cyclosporine on the kidney.

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Drug prescription.

Terms and Conditions of storage

Store at temperatures not above 25 ° C, protected from light and the reach of children.

Shelf life - 3 years. The drug should not be used after the expiry date stated on the packaging.