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 (e.g., diabetes, 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.

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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 (coating):

hypromellose – 2.40 mg,

macrogoal-4000 – 0.60 mg,

titanium dioxide – 1.00 mg.

How to take, the dosage

Orally, film-coated tablets of the preparation Fasostabil should be swallowed whole with water.
The preparation Fasostabil is intended for long-term treatment.

The duration of treatment is determined by the doctor.

– Primary prevention of cardiovascular diseases such as thrombosis and acute heart failure in the presence of risk factors (e.g. diabetes, hyperlipidemia, arterial hypertension, obesity, smoking, old age).
One tablet of the preparation Fazostabil, containing ASK in the dosage of 150 mg during the first 24 hours and then one tablet with ASK in the dosage of 75 mg once a day.

– Prophylaxis of recurrent myocardial infarction and blood vessel thrombosis
1 tablet of the preparation Fazostabil, containing ASK in the dosage of 75-150 mg once a day.

– Prophylaxis of thromboembolism after surgical interventions on the vessels (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty).
1 tablet of the preparation Fasostabil, containing ASA at a dose of 75-150 mg once a day.

– Unstable angina pectoris
1 tablet of the preparation Fasostabil, containing ASA in the dosage of 75-150 mg once a day.

If the next dose of Fasostabil is missed it should be taken as soon as the patient remembers it. To avoid doubling the dose you should not take the missed tablet if the time of the next dose is approaching.

No special effects were observed when taking or cancelling the drug for the first time.

Interaction

• Concomitant use of ASA increases the effect and increases the risk of toxicity:

– methotrexate (due to decreased renal clearance and its displacement from binding to blood plasma proteins);

– Valproic acid (by displacing it from plasma protein binding);

• AASC enhances the effect and increases the risk of adverse reactions:

– narcotic analgesics, other non-steroidal anti-inflammatory drugs (due to synergistic action)

– Hypoglycemic oral hypoglycemic agents (sulfonylurea derivatives) and insulin due to the hypoglycemic properties of Asc in high doses (over 2 g per day) and the displacement of sulfonylurea derivatives from bond with blood plasma proteins

– thrombolytics, heparin, indirect anticoagulants (ticlopidine, warfarin), antiplatelet agents (including clopidogrel, dipyridamole) – due to synergism of main therapeutic effects and displacement from plasma protein binding;

– sulphonamides, including co-trimoxazole – due to displacement from plasma protein binding and increased concentration in blood plasma;

– carbohydrate inhibitors (acetazolamide). Concomitant use with ASA may lead to development of severe acidosis and increased toxic effect on the central nervous system;

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

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

– additive effect is observed in coadministration of ASA with ethanol (alcohol): increased damage to the gastrointestinal tract mucosa and prolonged bleeding time (due to the additive effect of ethanol and ASA).

• Decrease the antiaggregant effect of ASA:

– ibuprofen (due to antagonism with respect to suppression of platelet aggregation);

– Systemic glucocorticosteroids (except for hydrocortisone used in substitution therapy for Addison’s disease) (increases the elimination of salicylates);

– Antacids containing aluminum and/or magnesium hydroxide, colestyramine (reduce absorption of ASA in the gastrointestinal tract);

• ASK at low doses weakens the effect of uricosuric agents (benzbromaron, probenecid, sulfinpyrazone) due to competitive tubular elimination of uric acid.
• ACC in high doses, as well as other NSAIDs, may decrease antihypertensive effect of diuretics (due to decreased glomerular filtration rate due to inhibition of renal prostaglandin synthesis) and hypotensive agents. In particular, due to competitive blockade of prostacyclin synthesis, the effectiveness of angiotensin-converting enzyme inhibitors (ACE) may decrease.
  

Special Instructions

The drug should be used as prescribed by a physician.

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 disease, and allergic reactions to other medications (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 should be temporarily stopped.

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

. Caution should be exercised in cases of impaired renal function (CK greater 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, since in all the above cases ASA may increase the risk of acute renal failure/renal function impairment.

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

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

ASK at low doses may provoke the development of gout in predisposed patients (who have decreased uric acid excretion).

Combination of Asc and methotrexate is accompanied by increased incidence of side effects from the hematopoietic organs, concomitant use with valproic acid increases the risk of its 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 in case of small renal dysfunctions and in elderly patients careful monitoring is necessary.

Simultaneous administration of ASA with anticoagulants, thrombolytics and antiplatelet agents is associated with increased risk of bleeding and damaging effect on mucosa of gastrointestinal tract.

The concomitant use of Fazostabil with ibuprofen in patients with increased risk of cardiovascular events is not recommended because the reduction of the antiplatelet effect of ASA at doses up to 300 mg will decrease the cardioprotective effects. Patients taking ibuprofen for pain relief should inform their physician about this.

Monitoring of plasma concentrations of digoxin and lithium at the beginning or at the end of concomitant use of Fazostabil is recommended; dose adjustment may be required.

When concomitant use with diuretics and hypotensive agents (e.g., ACE inhibitors) a possible decrease of their effectiveness should be considered.

High doses of Asc have hypoglycemic effect, and this must be considered when prescribing it for patients with diabetes mellitus who receive 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 antiplatelet therapy care must be taken in elderly patients because of the risk of gastrointestinal bleeding.

In long-term use of Fazostabil it is necessary to periodically control general blood count and stool test for occult blood as well as functional state of liver.

In concomitant use of ASA with alcohol, there is an increased risk of gastrointestinal mucosal damage and prolongation of bleeding time.

In severe forms of glucose-6 phosphate dehydrogenase deficiency, ASK may 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 driving and operating machinery

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

• High sensitivity to ASA, excipients of the drug and other non-steroidal anti-inflammatory drugs (NSAIDs);

• Cerebral hemorrhage;

• .Bleeding tendency (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;

• The complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and sinuses, and intolerance of ASA or other NSAIDs, including cyclooxygenase-2 (COX-2) inhibitors (including a history);
• Erho-ulcerative lesions of the gastrointestinal tract (acute phase);
• Severe renal failure (creatinine clearance (CK) less than 30 ml/min.)
• Hepatic failure (Child-Pugh class B and C)
• Pregnancy (I and III trimesters), breastfeeding period

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• Deficiency of glucose-6-phosphate dehydrogenase;
• .Concurrent use with methotrexate (more than 15 mg per week);
• Children under 18 years of age.



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Side effects

The frequency of adverse reactions below, according to the World Health Organization classification, was determined accordingly as follows:

very frequently (≥1/10); frequently (>1/100, <1/10);

infrequently (>1/1000, <1/100);

rarely (>1/10000, <1/1000);

very rarely (<1/10000), including individual messages.

Immune System:

infrequent – urticaria, angioedema (Quincke’s edema), skin rash, skin itching, rhinitis, nasal mucous membrane edema;

very rare – anaphylactic shock, cardio-respiratory distress syndrome.

Gastrointestinal tract:

very often – heartburn;

often – nausea, vomiting;

infrequently – abdominal pain, gastric and duodenal mucosa ulcers, including perforative (rare), gastrointestinal bleeding;

very rarely – stomatitis, esophagitis, erosive lesions of upper gastrointestinal tract (including strictures), colitis, irritable bowel syndrome.

Respiratory system, chest and mediastinal organs:

often – bronchospasm.

Blood and lymphatic system:

very often – increased bleeding;

rarely – anemia; very rarely – aplastic anemia, hypoprothrombinemia, thrombocytopenia, neutropenia, leukopenia, eosinophilia, agranulocytosis.

There have been reported cases of hemolysis and hemolytic anemia in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.

Nervous system:

often – headache, insomnia;

infrequently – dizziness, somnolence; rarely – tinnitus, intracerebral hemorrhage.

Renal and urinary tract:

very rarely – renal dysfunction.

Effect on the results of laboratory and instrumental studies:

rarely – increased activity of “liver” enzymes.

Overdose

Salicylitis syndrome develops when receiving 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 within therapeutic misuse (chronic poisoning) or a single accidental or intentional administration of a toxic dose of the drug by an adult or child (acute poisoning).

Overdose is especially dangerous in elderly patients.

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

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

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

Symptoms of overdose at moderate and severe degree of severity (single dose of 150 mg/kg – 300 mg/kg – moderate degree of severity, more than 300 mg/kg – severe degree of poisoning):

Respiratory alkalosis with compensatory metabolic acidosis, hyperpyrexia, hyperventilation, noncardiogenic pulmonary edema, respiratory depression, asphyxia;

cardiovascular system disorders:

– cardiac rhythm disturbance, pronounced BP decrease,

– depression of cardiac activity;

from the side of water-electrolyte balance:

– dehydration,

– impairment of renal function from oliguria up to development of renal failure, characterized by hypokalemia, hypernatriemia, hyponatremia;

– disruption of 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 central nervous system function (drowsiness, confusion, coma, seizures).

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

Similarities

Cardiomagnil, Trombital, Trombital Forte