2010/12/12

Aspirin



Release form, composition and packing

Tablets

1 tab. acetylsalicylic acid 500 mg.

Clinico-pharmacological group: NSAID. Antiaggregant

Pharmacological action

NSAID, has anti-inflammatory, analgesic and antipyretic effects associated with non-selective inhibition of activity TSOG1 and TSOG2 regulating the synthesis of Pg. As a result, are not formed Pg, providing formation of edema and giperalgezii. Reduction of Pg (mainly E1) in the center of thermoregulation leads to a reduction in body temperature due to expansion of vessels in the skin and increase perspiration. Analgesic effect is caused by both central and peripheral actions. Reduces the aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Antiplatelet effect lasts for 7 days after a single dose (more pronounced in males than in females). Reduces the mortality and risk of myocardial infarction in unstable angina. Effective in the primary prevention of CVD, particularly myocardial infarction in men older than 40 years, and for secondary prevention of myocardial infarction. At a daily dose of 6 g or more inhibits the synthesis of prothrombin in the liver and increases the prothrombin time. Increases the fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Speeds up hemorrhagic complications during surgery, increases the risk of bleeding during therapy with anticoagulants. Stimulates the excretion of uric acid (violating its reabsorption in the renal tubules), but in high doses. TSOG1 blockade in the gastric mucosa leads to inhibition of gastroprotective Pg, which can cause ulceration of the mucous membrane and subsequent bleeding. Less irritating to the mucous membrane of the digestive tract have formulations containing buffering agents, enteric shell, as well as special "sparkling" form of tablets.

Statement
rheumatism,
rheumatoid arthritis,
infectious-allergic myocarditis,
pericarditis.
febrile syndrome in infectious and inflammatory diseases.
pain syndrome (various origins): headache (including associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, lumbago, thoracic radicular syndrome, myalgia, arthralgia, algomenorrhea.

As antiplatelet drugs (doses up to 300 mg / day): IHD
the presence of several risk factors for CHD,
silent myocardial ischemia,
Unstable angina,
myocardial infarction (to reduce the risk of another heart attack and death after myocardial infarction)
repeated transient cerebral ischemia and ischemic stroke in men
prosthetic heart valves (the prevention and treatment of venous thromboembolism),
balloon coronary angioplasty and stent (reducing the risk of re-stenosis and the treatment of secondary stratification of coronary artery disease),
at neateroskleroticheskih coronary artery disease (Kawasaki disease), aortoarteriit (Takayasu's disease),
mitral valve heart disease and atrial fibrillation, mitral valve prolapse (prevention of thromboembolism),
recurrent pulmonary embolism
pulmonary infarction,
Acute thrombophlebitis
Dressler's syndrome.

In clinical immunology and allergy: a gradually increasing doses for long, "aspirin" desensitization and the formation of stable tolerance to NSAIDs in patients with "aspirin" asthma and "aspirin triad."

Dosing regimen

Soluble tablets: inside, previously dissolved in a small amount of water - at 400-800 mg 2-3 times a day (not more than 6 g).

In acute rheumatism - 100 mg / kg / day in 5-6 receptions. Tablets containing ASA at doses above 325 mg (400-500 mg), designed for use as an analgesic and anti-inflammatory drugs, in doses 50-75-100-300-325 mg - in adults, especially as antiplatelet drugs.

Inside, with a frenetic and pain for adults - 0.5-1 g / d (up to 3 g) were divided into 3 doses.

Duration of treatment should not exceed 2 weeks.

Effervescent tablets dissolved in 100-200 ml of water and taken orally after a meal, a single dose - 0.25-1 g, take 3-4 times a day.

Duration of treatment - from a single dose of up to many months of the course.

To improve the blood rheology - 0.15-0.25 g / day for several months.

Myocardial infarction, as well as for secondary prevention in patients with myocardial infarction - 40-325 mg 1 time a day (usually 160 mg). As an inhibitor of platelet aggregation - 300-325 mg / day for a long time.

At the dynamic cerebral circulatory disorders in men, cerebral embolism - 325 mg / day with gradual increase to a maximum of 1 g / day, for the prevention of relapse - 125-300 mg / day.

For the prevention of thrombosis or occlusion of the aortic graft - 325 mg every 7 h after nasal gastric tube set, and then oral - 325 mg 3 times daily (usually in combination with dipyridamole, which overturned in a week, continuing long-term treatment ASA).

With active rheumatoid arthritis administered (currently not assigned) in a daily dose of 8.5 g for adults and 100-125 mg / kg - for teenagers (15-18 years), the multiplicity of applications - 4-5 times a day.

After 1-2 weeks of treatment for children, reduce the dose to 60-70 mg / kg / day treatment for adults continue in the same dose, duration of treatment - up to 6 weeks.

Cancellation produced gradually over 1-2 weeks

Side effect

Nausea, decreased appetite, stomachodynia, diarrhea, allergic reactions (skin rash, angioedema, bronchospasm), abnormal liver function and / or kidney disease; thrombocytopenia, anemia, leukopenia, Reye syndrome (encephalopathy and acute fatty liver with rapid development of liver failure) , the formation of haptenic-based mechanism "aspirin" asthma and "aspirin triad" (the combination of asthma, recurrent polyposis of the nose and paranasal sinuses and the intolerance of ASA and LS pyrazolone series).

With prolonged use - dizziness, headache, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, hypocoagulation, hemorrhage (including gastrointestinal), visual impairment, hearing loss, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with increasing creatinine in blood and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of heart failure, edema, increased activity of liver transaminases.

Contraindications
hypersensitivity;
erosive and ulcerative lesions of the gastrointestinal tract (in acute phase),
gastrointestinal bleeding;
"Aspirin" triad (a combination of asthma, recurrent polyposis of the nose and paranasal sinuses and the intolerance of ASA and LS series of pyrazolone);
hemorrhagic diathesis (haemophilia, von Willebrand disease, telangiectasia, gipoprotrombinemiey, thrombocytopenia, thrombocytopenic purpura);
dissecting aortic aneurysm, portal hypertension, a deficiency of vitamin K;
hepatic / renal failure;
pregnancy (I and III trimesters)
lactation;
deficiency of glucose-6-phosphate dehydrogenase,
childhood (up to 15 years - the risk of Reye's syndrome in children with hyperthermia against viral diseases)

. C care. Hyperuricemia, urate nefrourolitiaz, gout, liver disease, peptic ulcer and / or 12 duodenal ulcer (history), decompensated heart failure.

Pregnancy and lactation

Drug use is prohibited.

Cautions

Duration of treatment (without consulting a doctor) must not exceed 7 days when administered as analgesic drugs and more than 3 days as antipyretic. Currently, the use of ASA as an anti-inflammatory drugs in a daily dose of 5-8 g is limited due to the high probability of adverse effects from the gastrointestinal tract (NSAID gastropathy).

Before surgery to reduce bleeding during surgery and postoperative period should stop taking salicylates for 5-7 days and notify the physician.

During long-term therapy is necessary to carry out blood tests and study fecal occult blood.

Children should not be prescribed drugs containing ASA, as in the case of viral infection, they may increase the risk of Reye's syndrome. Symptoms of Reye's syndrome are persistent vomiting, severe encephalopathy, liver enlargement. Appointment of tablets after meals, their thorough grinding, the use of pills with buffer additives or a special enteric-coated membrane, as well as the simultaneous use of drugs to neutralize the acidity of gastric juice, reduce the irritating effect on the gastrointestinal tract.

Has a teratogenic effect, when used in the I trimester leads to splitting of the upper sky, in the III trimester caused inhibition of labor activity (inhibition of synthesis of Pg), premature closure of the ductus arteriosus in the fetus, pulmonary vascular hyperplasia and hypertension in a "small" circle of blood.

Excreted in breast milk, which increases the risk of bleeding in a child due to dysfunction of platelets. ASA, even in small doses reduces the excretion of uric acid from the body, which can cause the development of an acute attack of gout in susceptible patients.

During the period of treatment should refrain from receiving ethanol.

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