Excretion of salicylic acid is dose-dependent, because its metabolism may limit the enzyme system. Half-life is 2-3 hours when applied at low doses of ASA and 15 hours when using the drug in high dose (usual dose of acetylsalicylic acid as an analgesic). Unlike other salicylates, when multiple dose ASA negidrolizirovannaya drug does not accumulate in the serum. Salicylic acid and its metabolites are excreted by the kidneys. In patients with normal renal function 80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours.
Primary prevention of acute myocardial halotestin buy infarction in the presence of risk factors (eg, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age), and recurrent myocardial infarction.
Unstable angina (including suspicion of acute myocardial infarction) and stable angina pectoris.
Prevention of ischemic stroke (including patients with transient ischemic attack).
– Prevention of thromboembolism after surgery and invasive procedures on vessels (eg, coronary artery bypass surgery, endarterectomy of the carotid arteries, arteriovenous bypass, angioplasty and stenting of the coronary arteries, angioplasty of the carotid arteries).
Prevention of deep vein thrombosis and pulmonary artery and its branches (including during prolonged immobilization resulting from extensive surgery).
– Hypersensitivity to acetylsalicylic acid, auxiliary substances in the composition of the drug and other nonsteroidal anti-inflammatory drugs (NSAIDs).
– Asthma induced by intake of salicylates and other NSAIDs; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis, and paranasal sinuses, intolerance to ASA and other NSAIDs.
– erosive and ulcerative lesions of the gastrointestinal tract (acute stage).
– Gastrointestinal bleeding.
– Hemorrhagic diathesis.
– The combined use with methotrexate at a dose of 15 mg per week or more.
– Pregnancy (I and III trimester) and lactation.
– Children under 18 years old.
– Severe renal impairment (creatinine clearance (CC) of less than 30 ml / min.).
– Severe hepatic impairment (class B or higher on the scale of Child-Pugh).
– Chronic heart failure (III-IV NYHA functional class classification).
– lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
– When gout, hyperuricemia, as ASA in low doses, reduces the excretion of uric acid; it should be borne in mind that the ASA in low doses can trigger the development of gout in predisposed patients (with decreased excretion of uric acid).
– If you have a history of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding.
– If abnormal liver function (lower class at the scale of Child-Pugh).
– If the kidney function (creatinine clearance 30 mL / min.).
– in bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergy, including the group of NSAIDs (analgesics, anti-inflammatory, antirheumatic drugs).
– in the II trimester.
– When the intended surgical procedure (including minor, for example, extraction of a tooth), as ASA may cause bleeding propensity to develop within a few days after ingestion.
Pregnancy and lactation
The use of high doses of salicylates in the first 3 months of pregnancy is associated with an increased rate of fetal defects (cleft palate, heart defects). Appointment of salicylates in the I trimester of pregnancy is contraindicated. In the II trimester of pregnancy salicylates can be given only on the basis of strict risk assessment for fetal and benefits for the mother, preferably in doses not exceeding 150 mg / day and short-lived.
In the last trimester of pregnancy salicylates in high doses (more than 300 mg / day) caused a weakening of labor activity, premature closure of the ductus arteriosus in the fetus, increased bleeding in the mother and the fetus, and the appointment just before birth may cause intracranial hemorrhage, especially in preterm infants. Purpose of salicylates in the last trimester of pregnancy is contraindicated.
Salicylates and their metabolites in small amounts into breast milk. Accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in children and does not require stopping breastfeeding. However, long-term use of the drug or to appoint him to a high dose of breast-feeding should be discontinued immediately.
Dosing and Administration
The tablets of the drug desirable to take before eating, drinking plenty of fluids. The duration of therapy is determined by the doctor. Primary prevention of acute myocardial infarction in the presence of risk factors: 50-100 mg / day. Prophylaxis of recurrent myocardial infarction, stable and unstable angina: . 50-100 mg / day halotestin buy Unstable angina (in cases of suspected development of acute myocardial infarction) : 50-100 mg / day. Prophylaxis of ischemic stroke and transient ischemic attack: 50-100 mg / day.Prevention of thromboembolism after surgery and invasive procedures on vessels: 50-100 mg / day. Prevention of deep vein thrombosis and pulmonary embolism and its branches: 50-100 mg / day.
Side effects From the digestive system: most frequently reported nausea, heartburn, vomiting, abdominal pain; rarely – ulcers of the stomach and duodenum; very rarely – a perforated ulcer of the gastric mucosa and duodenal ulcers, gastrointestinal bleeding, transient liver function abnormalities with increased activity of “liver” transaminases. From the system of blood: the appointment of ASA associated with an increased risk of bleeding due to the inhibitory effect of ASA on platelet aggregation, rarely – anemia. Allergic reactions: skin rash, pruritus, urticaria, angioedema, rhinitis, swelling of nasal mucosa, rhinitis, cardiorespiratory distress syndrome as well as severe reactions, including anaphylactic shock. On the part of the central nervous system: dizziness, hearing loss, headache, tinnitus.
An overdose of
salicylate intoxication (developed with ASA in a dose of 100 mg / kg / day for more than 2 days) may result from prolonged use of toxic doses of the drug within the wrong therapeutic use of the drug (chronic toxicity), or a single accidental or intentional receive a toxic dose drug or an adult child (acute intoxication). Symptoms of chronic intoxication with salicylic acid derivatives are non-specific and are often diagnosed with difficulty. Mild intoxication usually develop only after repeated use of high doses of the drug and is manifested by dizziness, tinnitus, hearing loss, increased sweating, nausea and vomiting, headache and confusion. The above symptoms disappear after reducing the dose. Tinnitus may occur if plasma levels of ASA from 150 to 300 pg / ml. More severe symptoms when the concentration of ASA in the blood plasma levels above 300 micrograms / ml. The main manifestation of acute intoxication is severe disturbance of acid-base status, the manifestations of which may vary depending on the patient’s age and the degree of severity of intoxication. In children, the most common is the development of metabolic acidosis. Intoxication Treatment is carried out in accordance with accepted standards and depends on the severity of poisoning and the clinical picture and should be aimed mainly at accelerating the excretion of the drug and the restoration of water and electrolyte balance and acid-base status.
Overdose is especially dangerous in elderly patients. Symptoms of overdose from mild to moderate severity: Vertigo, tinnitus, hearing loss, increased sweating, nausea, vomiting, goal ovnaya pain, confusion, profuse sweating, tachypnea, hyperventilation, respiratory alkalosis. Treatment: gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis, restoring fluid and electrolyte balance and acid-base status. overdose symptoms of moderate to severe: – respiratory alkalosis with compensatory metabolic acidosis; – hyperpyrexia (extremely high body temperature); – violation of breathing: hyperventilation, non-cardiogenic pulmonary edema, depression breathing, asphyxia; – disorders of the cardiovascular system: cardiac arrhythmias, lowering the pressure, depression of cardiac activity; – violations of water-electrolyte balance: dehydration (dehydration), renal dysfunction by oliguria up to the development of renal failure, characterized by hypokalemia, hypernatremia, hyponatremia; – impaired glucose metabolism: hyperglycemia, hypoglycemia (especially in children), ketoacidosis; – tinnitus, deafness; – gastrointestinal bleeding; – haematological disorders: by inhibiting the aggregation of platelets to coagulopathy, prolonged prothrombin time, hypoprothrombinemia; – neurological disorders: toxic encephalopathy and central nervous system depression (drowsiness, confusion, coma, convulsions). Treatment: immediate hospitalization in specialized departments for emergency therapy – gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis, hemodialysis, water-recovery electrolyte balance and acid-base status, symptomatic therapy.
Interaction with other drugs
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KardiASK ® while the application increases the effects of the following medicines:
– methotrexate by reducing renal clearance and ousting it from the connection with plasma proteins, the combination of acetylsalicylic acid with methotrexate is accompanied by an increased incidence of side effects of hematopoiesis;
– heparin and indirect anticoagulants due to dysfunction of platelets and displacing anticoagulants from binding with plasma proteins;
– thrombolytic and antiplatelet agents (ticlopidine)
– digoxin due to the decrease in its renal excretion;
– hypoglycemic agents (insulin and sulfonylurea derivatives) due to the hypoglycemic properties of the acetylsalicylic acid and high doses of sulfonylureas displacement connection with plasma proteins;
– valproic acid by displacement from its association with plasma proteins. The combination of aspirin with anticoagulant, thrombolytic and antiplatelet agents associated with an increased risk of bleeding. At the same time taking aspirin with alcohol there is an additive effect and an increased risk of damage to the mucous membrane of the gastrointestinal tract and prolongation of bleeding time.
The ACK reduces the effect of uricosuric agents – benzbromaron (decrease urikozuricheskogo effect due to competitive suppression of renal tubular excretion of uric acid), angiotensin converting enzyme inhibitors ( ACE) (indicates a dose-dependent decrease halotestin buy in glomerular filtration rate by inhibiting prostaglandins possessing vasodilating action, hypotensive action weakening respectively), diuretics (when used in conjunction with high doses of ASA in a decline in glomerular filtration rate by reducing the synthesis of prostaglandins in the kidneys). Leveraging the elimination of salicylates, systemic glucocorticosteroids (GCS) weaken their effect. online anabolic steroids pharmacy
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