Phasostabil, 75 mg+15, 2 mg 100 pcs

The mechanism of action of acetylsalicylic acid (ASA) is based on irreversible inhibition of cyclooxygenase (COX-1), resulting in blocked synthesis of thromboxane A2 and suppressed platelet aggregation. It is believed that ASA has other mechanisms to inhibit platelet aggregation, which expands the field of its use in various vascular diseases.

ASK also has anti-inflammatory, analgesic and antipyretic effects. The anti-inflammatory effect is associated with decreased blood flow due to inhibition of prostaglandin E2 synthesis.

Magnesium hydroxide, which is part of the drug Fasostabil, has an antacid effect and protects the mucous membrane of the gastrointestinal tract from the effects of ASA.

Indications

Primary prevention 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).
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.

Pharmacological effect

The mechanism of action of acetylsalicylic acid (ASA) is based on irreversible inhibition of cyclooxygenase (COX-1), as a result of which 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 the scope of its use in various vascular diseases.

ASA also has anti-inflammatory, analgesic, and antipyretic effects. 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 drug Fazostabil, has an antacid effect and protects the mucous membrane of the gastrointestinal tract from the effects of ASA.

Special instructions

The drug should be used as prescribed by a doctor.

ASA can provoke bronchospasm, as well as cause attacks of bronchial asthma and other hypersensitivity reactions. Risk factors include a history of asthma, hay fever, nasal polyposis, chronic respiratory diseases, and allergic reactions to other drugs (for example, skin reactions, itching, urticaria).

ASA can cause bleeding of varying severity during and after surgery.
Several days before planned surgery, the risk of bleeding should be assessed in comparison with the risk of ischemic complications in patients taking low doses of ASA. If the risk of bleeding is significant, ASA should be temporarily discontinued.

The simultaneous use of ASA with anticoagulants, thrombolytics and antiplatelet drugs is accompanied by an increased risk of bleeding.

In case of impaired renal function (creatinine clearance more than 30 ml/min), as well as in cases of circulatory disorders resulting from atherosclerosis of the renal arteries, chronic heart failure, extensive surgery, sepsis, cases of massive bleeding, caution should be exercised, since in all of these cases, ASA may increase the risk of developing acute renal failure/deterioration of renal function.

It is known that the risk of developing acute renal failure increases when other NSAIDs are used concomitantly with ACE inhibitors or diuretics.

In patients with mild to moderate hepatic impairment, liver function should be regularly monitored.

ASA in low doses can provoke the development of gout in predisposed patients (those with reduced excretion of uric acid).

The combination of ASA with methotrexate is accompanied by an increased incidence of side effects from the hematopoietic organs; combined use with valproic acid increases the risk of its toxicity. During the first weeks of simultaneous use of Fazostabil and methotrexate at a dose of less than 15 mg per week, blood tests should be performed weekly. Careful monitoring should be carried out in the presence of even slight impairment of 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 damaging effects on the mucous membrane of the gastrointestinal tract.

The simultaneous use of 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 physician.

It is recommended to monitor plasma concentrations of digoxin and lithium when starting or ending concomitant use of Fazostabil; Dose adjustment may be required.

When used together with diuretics and antihypertensive drugs (for example, ACE inhibitors), a possible decrease in their effectiveness should be taken into account.

High doses of ASA have a hypoglycemic effect, which must be kept in mind when prescribing it to patients with diabetes mellitus receiving oral hypoglycemic agents and insulin.

When using systemic glucocorticosteroids and salicylates simultaneously, it should be remembered that during treatment the concentration of salicylates in the blood is reduced, and after discontinuation of systemic glucocorticosteroids, an overdose of salicylates is possible. Long-term use of low doses of ASA as antiplatelet therapy requires caution in elderly patients due to the risk of gastrointestinal bleeding.

With long-term use of the drug Fazostabil, you should periodically monitor a complete blood count and stool test for occult blood, as well as the functional state of the liver.

When taking ASA simultaneously with alcohol, there is an increased risk of damage to the mucous membrane of the gastrointestinal tract and prolongation of bleeding time.

In severe forms of glucose-6 phosphate dehydrogenase deficiency, ASA can cause hemolysis and hemolytic anemia. Factors that increase the risk of developing hemolysis and hemolytic anemia are fever, acute infections and high doses of ASA.

Impact on the ability to drive vehicles and operate machinery

During treatment with Fazostabil, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Acetylsalicylic acid, [Magnesium hydroxide]

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,

magnesium stearate – 1.90 mg.

Excipients (shell):

hypromellose – 2.40 mg,

macrogol-4000 – 0.60 mg,

titanium dioxide – 1.00 mg.

Contraindications

Hypersensitivity to ASA, excipients of the drug and other non-steroidal anti-inflammatory drugs (NSAIDs);
Bleeding in the brain;
Tendency to bleeding (vitamin K deficiency, thrombocytopenia, hemorrhagic diathesis);
Chronic heart failure functional class III-IV according to the NYHA classification;
Bronchial asthma induced by taking salicylates and NSAIDs;
Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and intolerance to ASA or other NSAIDs, including cyclooxygenase-2 (COX-2) inhibitors (including a history);
Erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase);
Gastrointestinal bleeding;
Severe renal failure (creatinine clearance (CC) less than 30 ml/min.);
Liver failure (class B and C according to the Child-Pugh classification);
Pregnancy (I and III trimesters), breastfeeding period;
Glucose-6-phosphate dehydrogenase deficiency;
Concomitant use with methotrexate (more than 15 mg per week);
Children under 18 years of age.

Side Effects

The frequency of adverse reactions listed below, in accordance with the classification of the World Health Organization, was determined according to the following:

very often (≥1/10); often (>1/100, <1/10);uncommon (>1/1000, <1/100);rare (>1/10000, <1/1000);very rare (< 1/10000), including isolated reports.From the immune system:uncommon – urticaria, angioedema (Quincke’s edema), skin rash, itching, rhinitis, swelling of the nasal mucosa;very rarely – anaphylactic shock, cardiorespiratory 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 perforation (rarely), gastrointestinal bleeding;very rarely – stomatitis, esophagitis, erosive lesions of the upper gastrointestinal tract (including strictures), colitis, irritable bowel syndrome.From the respiratory system, chest and mediastinal organs:often – bronchospasm.From the blood and lymphatic system:very often – increased bleeding;rarely – anemia; very rarely – aplastic anemia, hypoprothrombinemia, thrombocytopenia, neutropenia, leukopenia, eosinophilia, agranulocytosis.Cases of hemolysis and hemolytic anemia have been reported in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.From the nervous system:often – headache, insomnia;infrequently – dizziness, drowsiness; rarely – tinnitus, intracerebral hemorrhage.From the kidneys and urinary tract:very rarely – renal dysfunction.Influence on the results of laboratory and instrumental studies:rarely – increased activity of liver enzymes.

Interaction

When used simultaneously, ASA enhances the effect and increases the risk of toxicity:
– methotrexate (by reducing renal clearance and displacing it from connection with blood plasma proteins);

– valproic acid (due to displacement from the connection with blood plasma proteins);
ASA enhances the effect and increases the risk of adverse reactions:
– narcotic analgesics, other non-steroidal anti-inflammatory drugs (due to synergistic action)

– hypoglycemic agents for oral administration (sulfonylurea derivatives) and insulin due to the hypoglycemic properties of ASA itself in high doses (more than 2 g per day) and displacement of sulfonylurea derivatives from connection with blood plasma proteins

– thrombolytic agents, heparin, indirect anticoagulant (ticlopidine, warfarin), antiplatelet agents (including clopidogrel, dipyridamole) – due to the synergism of the main therapeutic effects and displacement from binding with blood plasma proteins;

– sulfonamides, including co-trimoxazole – due to displacement from connection with blood plasma proteins and increased concentration in blood plasma;

– carbonic anhydrase inhibitors (acetazolamide). Concomitant use with ASA may lead to the development of severe acidosis and increased toxicity to the central nervous system;

– digoxin and lithium – due to a decrease in the renal excretion of digoxin and lithium with an increase in their concentration in the blood plasma;

– selective serotonin reuptake inhibitors (including sertraline, paroxetine), which may lead to an increased risk of bleeding from the upper gastrointestinal tract (synergism with ASA);

– an additive effect is observed when taking ASA simultaneously with ethanol (alcohol): damage to the mucous membrane of the gastrointestinal tract increases and bleeding time prolongs (due to the additive effect of ethanol and ASA).
Reduces the antiplatelet effect of ASA:
– ibuprofen (due to antagonism towards inhibition of platelet aggregation);

– systemic glucocorticosteroids (with the exception of hydrocortisone, used for replacement therapy of Addison’s disease) (increase the elimination of salicylates);

– antacids containing aluminum and/or magnesium hydroxide, cholestyramine (reduce the absorption of ASA in the gastrointestinal tract);
ASA in low doses weakens the effect of uricosuric drugs (benzbromarone, probenecid, sulfinpyrazone) due to competitive tubular elimination of uric acid.

ASA in high doses, like other NSAIDs, can reduce the antihypertensive effect of diuretics (due to a decrease in glomerular filtration rate due to suppression of renal prostaglandin synthesis) and antihypertensive drugs. In particular, due to competitive blockade of prostacyclin synthesis, the effectiveness of angiotensin-converting enzyme (ACE) inhibitors may decrease.

Overdose

Salicylic syndrome develops when taking acetylsalicylic acid 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 intake of a toxic dose of the drug by an adult or child (acute poisoning).

Overdose is especially dangerous in elderly patients.

Symptoms of overdose in mild to moderate severity (single dose less than 150 mg/kg):

Dizziness, tinnitus, hearing loss, increased sweating, nausea and vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis.

Treatment: gastric lavage, repeated intake of activated carbon, forced alkaline diuresis, restoration of water-electrolyte balance and acid-base state.

Symptoms of overdose with moderate and 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;

from the cardiovascular system:

– heart rhythm disturbance, marked decrease in blood pressure,

– depression of cardiac activity;

from the side of water-electrolyte balance:

– dehydration,

– impaired renal function from 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;

– hematological disorders: from inhibition of platelet aggregation to coagulopathy, prolongation of prothrombin time, hypoprothrombinemia;

– neurological disorders: toxic encephalopathy and depression of the central nervous system (drowsiness, confusion, coma, convulsions).

Treatment: immediate hospitalization in specialized departments for emergency treatment – gastric lavage, repeated intake of activated charcoal, restoration of water-electrolyte balance and acid-base status, forced alkaline diuresis, symptomatic therapy.

Storage conditions

In a place protected from light at a temperature not exceeding 25 °C.
Keep out of the reach of children.

Shelf life

2 years.
Do not use the drug after the expiration date.

Manufacturer

Ozon, Russia