Phasostabil, 150 mg+30.39 mg 50 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. ASA also has anti-inflammatory, analgesic, and antipyretic effects. Its anti-inflammatory effect is related to decrease of blood flow due to inhibition of prostaglandin E2 synthesis.
Magnesium hydroxide contained in the preparation Fasostabil has an antacid effect and protects the mucous membrane of the gastrointestinal tract from ASA.
Pharmacokinetics
Absorption
After oral administration ASK is quickly and almost completely absorbed from the gastrointestinal tract. Simultaneous intake of food slows down absorption. Partially metabolized during absorption.
Distribution and metabolism
During and after absorption ASK is converted to the main metabolite – salicylic acid, which is metabolized under the influence of enzymes, mainly in the liver to form metabolites (phenylsalicylate, salicylate glucuronide and salicyluric acid) found in many tissues and body fluids. In women the metabolic process is slower (lower activity of enzymes in blood serum).
Maximal ASK concentration in blood plasma is reached in 10-20 minutes after oral intake, salicylic acid – in 0.3-2 hours. Asc and salicylic acid are highly bound to blood plasma proteins and rapidly distributed in the body. The degree of binding of salicylic acid to plasma proteins is concentration-dependent, not linear. At low concentrations (less than 100 µg/ml) up to 90% of salicylic acid is bound to blood plasma proteins, at high concentrations (more than 400 µg/ml) – up to 75%.
The bioavailability of ASA is 50-68%, salicylic acid – 80-100%. Salicylic acid penetrates the placental barrier and is found in breast milk.
In renal insufficiency, during pregnancy and in infants, salicylates may displace bilirubin from binding to albumin and contribute to bilirubin encephalopathy.
Excretion
ASK and its metabolites are excreted primarily by the kidneys.
The half-life of ASK is 15-20 minutes, salicylic acid is 2-3 hours when taking ASK in low doses and increases significantly when taking ASK in high doses as a result of enzyme system saturation. Unlike other salicylates, non-hydrolyzed ASA does not accumulate in blood serum when repeatedly administered. In patients with normal renal function 80-100% of a single dose of ASA is excreted by kidneys within 24-72 hours.
Magnesium hydroxide in administered doses does not affect the bioavailability of ASA.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

The drug should be used as prescribed by a doctor.
ASK may provoke bronchospasm, as well as cause attacks of bronchial asthma and other hypersensitivity reactions. Risk factors include a history of bronchial asthma, hay fever, nasal polyposis, chronic respiratory diseases, as well as allergic reactions to other drugs (e.g., skin reactions, itching, urticaria).
ASA can cause bleeding of varying severity during and after surgical interventions.
Several days before the planned surgical intervention, the risk of bleeding should be assessed compared to the risk of ischemic complications in patients taking low-dose ASA. If the risk of bleeding is significant, ASA administration should be temporarily stopped.
Concomitant use of ASA with anticoagulants, thrombolytics and antiplatelet agents is accompanied by an increased risk of bleeding.
In renal dysfunction (CK more than 30 ml/min), as well as in circulatory disorders due to atherosclerosis of the renal arteries, chronic heart failure, extensive surgery, sepsis, cases of massive bleeding, caution should be exercised because in all these cases ASA may increase the risk of acute renal failure/worsening of renal function (see section “Caution.
It is known that the risk of acute renal failure increases with coadministration of other NSAIDs with ACE inhibitors or diuretics.
In patients with mild to moderate hepatic impairment, liver function should be monitored regularly (see section “With caution”.)
ASK in low doses may provoke development of gout in predisposed patients (who have reduced excretion of uric acid).
Combination of ASK with methotrexate is accompanied by an increased frequency of side effects from the organs of hematopoiesis, concomitant use with valproic acid increases the risk of toxicity. During the first weeks of concomitant administration of Fazostabil and methotrexate in dose less than 15 mg weekly, a weekly blood test should be performed. Even with minor renal dysfunction and in elderly patients it is necessary to monitor carefully (see sect. “Contraindications”, “Caution”, “Interaction with other medicinal agents”).
Simultaneous administration of ASA with anticoagulants, thrombolytics and antiplatelet agents is associated with increased risk of bleeding and damaging effects on the mucosa of the gastrointestinal tract (see sections “Caution”, “Interaction with other medicinal products”). It is not recommended concomitant administration of Fazostabil and ibuprofen in patients with increased risk of cardio-vascular diseases, because the reduction of antiaggregant effect of ASA in doses up to 300 mg leads to the reduction of cardioprotective effect. Patients taking ibuprofen for pain relief should inform the physician about this (see sections “Caution”, “Interaction with other medicinal products”).
It is recommended to monitor plasma concentrations of digoxin and lithium at the beginning or at the end of concomitant administration of Fazostabil; dose adjustment may be required (see sect.
When concomitant use with diuretics and hypotensive agents (e.g. ACE inhibitors) the possible decrease of their effectiveness should be considered (see sect.
High doses of ASA have a hypoglycemic effect, which should be borne in mind when prescribing it to patients with diabetes mellitus receiving oral hypoglycemic agents and insulin.
When concomitant use of systemic glucocorticosteroids and salicylates, it should be remembered that during treatment the concentration of salicylates in blood is reduced, and after cancellation of systemic glucocorticosteroids, an overdose of salicylates is possible. With long-term use of low doses of ASA as anti-aggregant therapy it is necessary to be cautious in elderly patients due to the risk of gastrointestinal bleeding.
In long-term use of Fazostabil it is necessary to periodically control general blood count and fecal occult blood test as well as liver function tests.
Simultaneous administration of ASA with alcohol increases the risk of gastrointestinal mucosa damage and prolongation of bleeding time.
With severe forms of glucose-6 phosphate dehydrogenase deficiency ASA may cause hemolysis and hemolytic anemia (see section “Contraindications”). Factors that increase the risk of hemolysis and hemolytic anemia are fever, acute infections, and high doses of ASA.

When treating with Fasostabil it is necessary to be careful when driving vehicles and engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reaction.

Contraindications

. In gout, hyperuricemia, history of gastrointestinal ulcers or gastrointestinal bleeding, mild to moderate renal failure (CK more than 30 ml/min), liver failure (class A according to the Child-Pugh classification), bronchial asthma, hay fever, nasal polyposis, allergic conditions, in II trimester of pregnancy, in diabetes, elderly age; concomitant use with the following medications: methotrexate (less than 15 mg weekly), anticoagulants, thrombolytics and antiaggregants, high-dose NSAIDs and salicylates, narcotic analgesics, sulfonamides (including co-trimoxazole), carboanhydrase inhibitors (acetazolamide), digoxin, lithium, oral hypoglycemic agents (sulfonylurea derivatives), insulin, valproic acid, selective serotonin reuptake inhibitors, ibuprofen, systemic glucocorticosteroids, ethanol (alcohol-containing drugs, drinks).

Side effects

Overdose

Similarities