Description
Pharmacological action of
The mechanism of action of acetylsalicylic acid (ASA) is based on the irreversible inhibition of cyclooxygenase (COX-1), as a result, the synthesis of thromboxane A2 is blocked and platelet aggregation is suppressed. It is believed that ASA has other mechanisms for suppressing platelet aggregation, which expands its scope in various vascular diseases.
ASA also has anti-inflammatory, analgesic, antipyretic effect. The anti-inflammatory effect is associated with a decrease in blood flow due to inhibition of prostaglandin E2 synthesis.
Magnesium hydroxide, which is part of the Phasostabil preparation, has an antacid effect and protects the mucous membrane of the gastrointestinal tract from the effects of ASA.
Indications
Primary prevention of cardiovascular disease, such as thrombosis and acute heart failure in the presence of risk factors (for example, diabetes mellitus, hyperlipidemia, arterial hypertension, obesity, smoking, old age).
Prevention of recurrent myocardial infarction and blood vessel thrombosis.
Prevention of thromboembolism after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty).
Unstable angina pectoris.
Contraindications
Hypersensitivity to ASA, excipients and other non-steroidal anti-inflammatory drugs (NSAIDs)
Cerebral hemorrhage
Tendency to bleed (vitamin K deficiency, thrombocytopenia, hemorrhagic diathesis)
Chronic heart failure of functional class III-IV according to NYHA classification
Bronchial asthma induced by salicylates and NSAIDs
Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and other intolerance to ASA or Cycloid intolerance 2 (COX-2) (including a history)
Erosive-ulcerative lesion of the gastrointestinal tract (in the acute phase)
Gastrointestinal bleeding
Severe renal failure ness (creatinine clearance (CC) less than 30 ml / min.)
Hepatic insufficiency (Child-Pugh class B and C)
Pregnancy (I and III trimesters), breastfeeding period
Deficiency of glucose-6-phosphate dehydrogenase
Concomitant use with methotrexate (more than 15 mg per week)
Children under 18 years of age.
Special instructions
The drug should be used as directed by a doctor.
ASA can provoke bronchospasm, as well as cause attacks of bronchial asthma and other hypersensitivity reactions. Risk factors are a history of asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system, as well as allergic reactions to other drugs (for example, skin reactions, itching, urticaria).
ASA can cause bleeding of varying severity during and after surgery.
A few days before the planned surgical intervention, the risk of bleeding should be assessed compared with the risk of developing ischemic complications in patients taking low doses of ASA. If the risk of bleeding is significant, taking ASA should be temporarily stopped.
The simultaneous use of ASA with anticoagulants, thrombolytics and antiplatelet drugs is associated with an increased risk of bleeding.
In case of impaired renal function (CC more than 30 ml / min), as well as circulatory disorders resulting from atherosclerosis of the renal arteries, chronic heart failure, extensive surgery, sepsis, cases of massive bleeding, care should be taken, since in all of the listed cases, ASA may increase the risk of developing acute renal failure / impaired renal function.
known that the risk of developing acute renal failure increases with the combined use of other NSAIDs with ACE inhibitors or diuretics.
In patients with mild to moderate liver failure, liver function should be monitored regularly.
ASA in low doses can trigger the development of gout in susceptible patients (with decreased uric acid excretion).
The combination of ASA with methotrexate is accompanied by an increased incidence of side effects from the hematopoiesis, combined use with valproic acid increases the risk of toxicity. During the first weeks of simultaneous use of the drug Fazostabil and methotrexate at a dose of less than 15 mg per week, a blood test should be performed weekly. Careful monitoring must be carried out in the presence of even small impaired renal function, as well as in elderly patients.
The simultaneous use of ASA with anticoagulants, thrombolytic and antiplatelet drugs is associated with an increased risk of bleeding and damage to the mucous membrane of the gastrointestinal tract.
The simultaneous use of the drug Fazostabil with ibuprofen is not recommended in patients with an increased risk of developing cardiovascular diseases, since a decrease in the antiplatelet effect of ASA in doses up to 300 mg leads to a decrease in cardioprotective effects. Patients taking ibuprofen for pain relief should inform their doctor about this.
Recommended monitoring of plasma concentrations of digoxin and lithium at the beginning or at the end of the simultaneous use of the drug Fazostabil may require dose adjustment.
When used together with diuretics and antihypertensive drugs (e.g., ACE inhibitors), a possible decrease in their effectiveness should be considered.
High doses of ASA have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents for oral administration and insulin.
With the simultaneous use of systemic glucocorticosteroids and salicylates, it should be remembered that during treatment, the concentration of salicylates in the blood is reduced, and after the cancellation of systemic glucocorticosteroids, an overdose of salicylates is possible. With prolonged use of low doses of ASA as an antiplatelet therapy, caution should be exercised in elderly patients due to the risk of gastrointestinal bleeding.
With prolonged use of the drug Fazostabil, a general blood test and analysis of feces for occult blood, as well as the functional state of the liver, should be periodically monitored.
While taking ASA with alcohol, the risk of damage to the mucous membrane of the gastrointestinal tract and prolonged bleeding time is increased.
In severe forms of glucose-6 phosphate dehydrogenase deficiency, ASA can cause hemolysis and hemolytic anemia. Factors that increase the risk of hemolysis and hemolytic anemia are fever, acute infections, and high doses of ASA.
Influence on the ability to drive vehicles and work with mechanisms
During treatment with the drug Fazostabil, care must be taken when driving vehicles and engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
Composition
Active ingredients:
acetylsalicylic acid – 75.00 mg
magnesium hydroxide – 15.20 mg.
Excipients (core):
microcrystalline cellulose – 83.90 mg, croscarmellose sodium
– 8.00 mg, povidone-K25
– 6.00 mg
, 1.90 mg
magnesium stearate.
Excipients (shell):
hypromellose – 2.40 mg,
macrogol-4000 – 0.60 mg,
titanium dioxide – 1.00 mg.
Dosage and administration
Inside, film-coated tablets of the drug Phasostabil are swallowed whole with water.
The drug Phasostabil is intended for long-term treatment.
The duration of treatment is determined by the doctor.
– Primary prophylaxis of cardiovascular diseases such as thrombosis and acute heart failure in the presence of risk factors (for example, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age)
1 tablet of the drug Phazostabil containing ASA in a dose of 150 mg on the first day, then 1 tablet containing ASA in a dose of 75 mg 1 time per day.
– Prevention of recurrent myocardial infarction and blood vessel thrombosis
1 tablet of the drug Fazostabil containing ASA in a dose of 75-150 mg 1 time per day.
– Prevention of thromboembolism after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty)
1 tablet of the drug Phasostabil, containing ASA in a dose of 75-150 mg 1 time per day.
– Unstable angina
1 tablet of the drug Fazostabil containing ASA in a dose of 75-150 mg 1 time per day.
If you skip the next dose of Fazostabil, you must take the missed dose of the drug as soon as the patient remembers this. To avoid doubling the dose, you should not take the missed tablet if the time for taking the next dose is approaching.
Peculiarities of action during the first administration or withdrawal of the drug were not observed.
Side effects
The frequency of adverse reactions given below, according to the classification of the World Health Organization, was determined according to the following:
very often ( 1/10) often (> 1/100, <1/10) infrequently (> 1 / 1000, <1/100) rare (> 1/10000, <1/1000) very rare (<1/10000), including single messages. On the part of the immune system: infrequently – urticaria, angioedema (Quincke’s edema), skin rash, itching, rhinitis, swelling of the nasal mucosa of the nasal cavity very rarely – anaphylactic shock, cardio-respiratory distress syndrome. From the gastrointestinal tract: very often – heartburn often – nausea, vomiting infrequently – pain in the abdomen, ulcers of the mucous membrane of the stomach and duodenum, including perforated (rarely), gastrointestinal bleeding very rarely – stomatitis, esophagitis, upper gastrointestinal tract (including with strictures), colitis, irritable bowel syndrome. From the respiratory system, chest and mediastinal organs: is often a bronchospasm. From the blood and lymphatic system: very often – increased bleeding rare – anemia very rare – aplastic anemia, hypoprothrombinemia, thrombocytopenia, neutropenia, leukopenia, eosinophilia, agranulocytosis. Cases of hemolysis and hemolytic anemia have been reported in patients with severe glucose-6-phosphate dehydrogenase deficiency. From the nervous system: often – headache, insomnia infrequently – dizziness, drowsiness rarely – tinnitus, intracerebral hemorrhage. From the side of the kidneys and urinary tract: is very rare – impaired renal function. Influence on the results of laboratory and instrumental studies: rarely – increased activity of “liver” enzymes. Overdose of Salicylism syndrome develops when acetylsalicylic acid is taken in a dose of more than 100 mg / kg / day for more than 2 days due to the use of toxic doses of the drug as part of improper therapeutic use (chronic poisoning) or a single accidental or intentional administration of a toxic dose of the drug adult or child (acute poisoning). Overdose is especially dangerous in elderly patients. Overdose symptoms in mild to moderate severity (single dose less than 150 mg / kg): Dizziness, tinnitus, hearing loss, sweating, nausea and vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis. Treatment: gastric lavage, repeated use of activated carbon, forced alkaline diuresis, restoration of water-electrolyte balance and acid-base state. Overdose symptoms in moderate to severe severity (single dose 150 mg / kg – 300 mg / kg – moderate severity, more than 300 mg / kg – severe poisoning): Respiratory alkalosis with compensatory metabolic acidosis, hyperpyrexia, hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, asphyxia of from the cardiovascular system: – heart rhythm disturbance, marked decrease in blood pressure, – inhibition of cardiac activity from the side of water-electrolyte balance: – dehydration, – on the outside s renal function by oliguria until renal failure characterized by hypokalemia, hypernatremia, hyponatremia – impaired glucose metabolism: hyperglycemia, hypoglycemia (especially in children), ketoacidosis – tinnitus, deafness – gastrointestinal bleeding – hematologic disorders: from inhibition of platelet aggregation to coagulopathy, neuroprotection, neuroprotection, neuroprotection, neuroprotection, neuroprotection, neuroprotection, neuroprotection, neuroprotection, neuroprotection, coagulopathy, neuroprotection, coagulopathy, disorders: toxic encephalopathy and inhibition of central nervous system function (drowsiness, confusion, coma, convulsions). Treatment: immediate hospitalization in specialized departments for emergency therapy – gastric lavage, repeated use of activated carbon, restoration of water-electrolyte balance and acid-base state, forced alkaline diuresis, symptomatic therapy. Storage conditions In a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children. Expiration 2 years. Do not use after expiration date. Conditions of sale from pharmacies Without a prescription For the prescribed For adults as prescribed by the doctor, Pregnant as prescribed by the doctor, Nursing mothers 70 prescription 70 Adults prescribed by a doctor, Pregnant women only II trimester as prescribed by a doctor
