Instructions for Fazostabil (Acetylsalicylic acid, Magnesium hydroxide)
Fazostabil is an antiplatelet agent.
Release form and composition:
Dosage form - film-coated tablets: round, biconvex, almost white or white, slight marbling of the surface is possible, an almost white core and a film shell are visible on the fracture; on one of the sides of the 150 mg + 30.39 mg tablet there is a dividing line (10, 20, 25 and 30 pcs. in cell contour packages, in a cardboard box 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 packs; 10, 20, 30, 40, 50, 60, 70, 80, 90 and 100 in cans sealed with pull-off lids with first-tamper control or screw-on lids with a push-turn system or with control first opening, or in dark glass vials, sealed with a screw cap with a built-in removable silica gel capsule and a first opening control ring, in a cardboard box 1 can or 1 bottle.
Composition of 1 tablet:
active ingredients: acetylsalicylic acid - 75 mg and magnesium hydroxide - 15.2 mg or acetylsalicylic acid - 150 mg and magnesium hydroxide - 30.39 mg; auxiliary components
povidone-K25
magnesium stearate
croscarmellose sodium
microcrystalline cellulose
film shell
hypromellose
titanium dioxide, macrogol-4000.
Fazostabil Pharmacodynamics:
The action of Phazostabil is due to the properties of its active component - acetylsalicylic acid (ASA). It irreversibly inhibits cyclooxygenase (COX-1), whereby the synthesis occurs blocking thromboxane A 2 and platelet aggregation inhibition. It is believed that ASA has other mechanisms for suppressing platelet aggregation, which expands the scope of its application in patients with various vascular diseases.
The drug also has antipyretic, anti-inflammatory and analgesic effects. Magnesium hydroxide - the second active component of Phazostabil - has an antacid effect, protects the mucous membrane of the gastrointestinal tract (GIT) from the irritating effect of ASA.
Fazostabil Pharmacokinetics:
ASA from the gastrointestinal tract is absorbed quickly and almost completely, this process slows down with simultaneous food intake. It is partially metabolized during absorption. During absorption and after absorption, ASA is biotransformed into the main metabolite - salicylic acid, which is metabolized by enzymes, mainly in the liver, as a result of which metabolites (glucuronide salicylate, salicyluric acid, phenyl salicylate) are formed, which are found in many body fluids and tissues. The metabolic process in women is slower than in men, which is manifested by a lower activity of enzymes in the blood serum. After taking Fazostabil C max (maximum plasma concentration) ASA is noted after 10–20 minutes, salicylic acid - after 0.3–2 hours. Acetylsalicylic and salicylic acids are characterized by a high degree of connection with blood plasma proteins, are quickly distributed in the body.
The binding of salicylic acid to plasma proteins is nonlinear and depends on the concentration: at low concentrations (<100 μg / ml) it binds up to 90%, at high concentrations (> 400 μg / ml) - up to 75%. The bioavailability of salicylic acid is 90-100%, ASA - 50-68%. Salicylic acid crosses the placental barrier and into breast milk. In patients with renal insufficiency, pregnant women and newborns, salicylates are able to displace bilirubin from the association with albumin, and also cause the development of bilirubin encephalopathy. ASA and its metabolites are excreted from the body mainly by the kidneys. In the case of taking the drug in low doses, the half-life (T 1/2 ) of the main substance is about 15-20 minutes, the metabolite - salicylic acid - 2-3 hours.
In patients receiving ASA in high doses, these indicators significantly increase due to saturation enzyme systems. Unlike other salicylates, non-hydrolyzed ASA with repeated administration of the drug does not accumulate in the blood serum. With normal renal function, 80 to 100% of a single dose of ASA is excreted within 24-72 hours. Magnesium hydroxide in doses contained in Phazostabil does not affect the pharmacokinetic characteristics of the drug.
Fazostabil Indications:
treatment of unstable angina pectoris; prevention of thromboembolism after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty); primary prevention of cardiovascular diseases (thrombosis and acute heart failure) in patients at risk (for example, in the presence of arterial hypertension, diabetes mellitus, hyperlipidemia,
obesity, as well as in smokers and the elderly); prevention of recurrent myocardial infarction and blood vessel thrombosis.
Contraindications Fazostabil:
Absolute: bronchial asthma caused by the intake of salicylates / non-steroidal anti-inflammatory drugs (NSAIDs); complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses with intolerance to ASA or other NSAIDs, including COX-2 inhibitors, currently or in history; chronic heart failure III – IV functional class according to NYHA classification; bleeding tendency (vitamin K deficiency, hemorrhagic diathesis, thrombocytopenia); hemorrhage in the brain; gastrointestinal bleeding; erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; moderate to severe hepatic impairment (class B and C according to the Child-Pugh classification); severe renal failure [creatinine clearance (CC) <30 ml / min]; deficiency of glucose-6-phosphate dehydrogenase; I and III trimesters of pregnancy; lactation period; age under 18; the need to use methotrexate in a weekly dose of more than 15 mg; hypersensitivity to any component of Phazostabil or other NSAIDs.
The drug should be used with caution in the following cases: hay fever, nasal polyposis, allergic conditions, bronchial asthma; mild to moderate renal impairment (CC> 30 ml / min); mild hepatic impairment (class A according to the Child-Pugh classification); a history of gastrointestinal bleeding or ulcerative lesions of the gastrointestinal tract; hyperuricemia; gout; diabetes; elderly age; II trimester of pregnancy; simultaneous use of the following drugs: ethanol: (including alcoholic beverages), carbonic anhydrase inhibitors (acetazolamide), narcotic analgesics, selective serotonin reuptake inhibitors, systemic glucocorticosteroids, thrombolytic and antiplatelet agents, anticoagulants (including sulfonamides) trimoxazole), oral hypoglycemic agents (sulfonylurea derivatives) and insulin, high-dose NSAIDs and salicylates, weekly methotrexate <15 mg, ibuprofen, lithium, digoxin, valproic acid.
METHOD AND DOSAGE:
Fazostabil tablets should be taken orally: swallow whole and drink plenty of water. The doses of the drug described below are calculated based on the ASA content.
Recommended dosage regimens: unstable angina pectoris, prevention of recurrent myocardial infarction and blood vessel thrombosis and prevention of thromboembolism after vascular surgery: 75–150 mg once a day; primary prevention of cardiovascular diseases: the first day - 150 mg, from the second day - 75 mg once a day.
Phazostabil is intended for long-term use.
The duration of treatment is determined by the doctor individually. If you miss the next appointment, you should take Fazostabil as soon as possible. It is forbidden to take a double dose, so if the time for taking the next dose is approaching, the missed pill should not be taken.
