Fazostabil - Instructions For Use, Price, Reviews, Analogs Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Phazostabil

Fazostabil: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Fazostabil

ATX code: B01AC30

Active ingredient: acetylsalicylic acid (Acetylsalicylic acid) + magnesium hydroxide (Magnesium hydroxide)

Manufacturer: Ozone LLC (Russia)

Description and photo update: 2019-10-07

Prices in pharmacies: from 119 rubles.

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Phazostabil 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 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 blister contour packs, 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 opening control or screw caps with 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. Each pack also contains instructions for the use of Fazostabil).

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.

Pharmacological properties

Pharmacodynamics

The action of Phazostabil is due to the properties of its active component - acetylsalicylic acid (ASA). It irreversibly inhibits cyclooxygenase (COX-1), as a result of which thromboxane A ₂ synthesis 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 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.

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 communication with blood plasma proteins, are quickly distributed in the body. The binding of salicylic acid to plasma proteins is non-linear and depends on the concentration: at low 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 does not accumulate in the blood serum with repeated administration of the drug. 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.

Indications for use

• treatment of unstable angina pectoris;
• prevention of thromboembolism after surgical interventions on the vessels (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 repeated myocardial infarction and blood vessel thrombosis.

Contraindications

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, at present 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 up to 18 years;
• 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 liver failure (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.

Fazostabil, instructions for use: 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.

Side effects

The side effects described below are classified as follows: very common - ≥ 1/10; often - from ≥ 1/100 to <1/10; infrequently - from ≥ 1/1000 to <1/100; rarely - from ≥ 1/10000 to <1/1000; very rare - <1/10 000, including individual messages:

• respiratory system: often - bronchospasm;
• Gastrointestinal tract: very often - heartburn; often - nausea, vomiting; infrequently - abdominal pain, ulceration of the mucous membrane of the stomach and duodenum (including rarely - perforated ulcers), gastrointestinal bleeding; very rarely - colitis, esophagitis, stomatitis, irritable bowel syndrome, erosive lesions of the upper gastrointestinal tract (including with strictures);
• nervous system: often - headache, insomnia; infrequently - drowsiness, dizziness; rarely - tinnitus, intracerebral hemorrhage;
• immune system: infrequently - swelling of the nasal mucosa, rhinitis, skin rash, urticaria, itching of the skin, angioedema; very rarely - anaphylactic shock, cardio-respiratory distress syndrome;
• kidneys and urinary tract: very rarely - functional impairment of the kidneys;
• blood and lymphatic system: very often - increased bleeding, rarely - anemia; very rarely - eosinophilia, neutropenia, thrombocytopenia, agranulocytosis, leukopenia, hypoprothrombinemia, aplastic anemia; in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency - hemolytic anemia, hemolysis;
• laboratory data: rarely - increased activity of hepatic enzymes.

Overdose

In the case of a single dose of a toxic dose of ASA or taking the drug for 2 or more days in a row in daily doses exceeding 100 mg / kg, salicylism syndrome develops. Overdose is especially dangerous for elderly patients.

Overdose of mild to moderate ASA (single dose <150 mg / kg):

• symptoms: nausea and vomiting, increased sweating, hearing loss, tinnitus, dizziness, headache, tachypnea, confusion, hyperventilation, respiratory alkalosis;
• treatment: gastric lavage, repeated intake of activated carbon, forced alkaline diuresis, restoration of acid-base state and water-electrolyte balance.

Symptoms of moderate and severe ASA overdose (single doses of 150-300 mg / kg and> 300 mg / kg, respectively):

• cardiovascular system: a pronounced decrease in blood pressure, heart rhythm disturbances, inhibition of cardiac activity;
• digestive system: gastrointestinal bleeding;
• nervous system: depression of the function of the central nervous system (confusion, drowsiness, convulsions, coma), toxic encephalopathy;
• hematopoietic system: hypoprothrombinemia, prolongation of prothrombin time, hematological diseases from inhibition of platelet aggregation to coagulopathy;
• water and electrolyte balance: dehydration, impaired renal function from oliguria up to the development of renal failure with hypernatremia, hypokalemia, hyponatremia;
• glucose metabolism: hypoglycemia (especially in children), hyperglycemia, ketoacidosis;
• organ of hearing: tinnitus, deafness;
• others: hyperpyrexia, respiratory alkalosis with compensatory metabolic acidosis, noncardiogenic pulmonary edema, respiratory depression, hyperventilation, asphyxia.

Treatment of moderate and severe overdose is carried out in a hospital setting. First of all, gastric lavage and repeated intake of activated carbon are necessary. Requires forced alkaline diuresis, restoration of acid-base state and water-electrolyte balance. Further treatment is symptomatic.

special instructions

Fazostabil should only be used as directed by the attending physician.

ASA can cause attacks of bronchial asthma, bronchospasm and other hypersensitivity reactions. The risk group includes patients with nasal polyposis, hay fever, a history of bronchial asthma, chronic diseases of the respiratory system, as well as the presence of allergic reactions to other drugs (manifested, for example, urticaria, itching, skin rashes).

Patients for whom surgery is planned should warn the doctor about taking Fazostabil, since ASA during and after surgery can cause bleeding of varying intensity. A few days before surgery, the ratio of the likelihood of bleeding when taking the drug and the occurrence of ischemic complications in case of its cancellation should be assessed. If there is a significant threat of bleeding, Fazostabil should be canceled.

An increased chance of bleeding is noted with the simultaneous use of ASA and thrombolytics, anticoagulants, antiplatelet agents.

Caution should be observed when prescribing the drug to patients with impaired renal function (CC> 30 ml / min) and circulatory disorders caused by massive bleeding, extensive surgery, renal artery atherosclerosis, sepsis, and chronic heart failure. In these cases, there is a high risk of deterioration in renal function and the development of acute renal failure. Its likelihood increases with the simultaneous use of other NSAIDs with diuretics and angiotensin-converting enzyme (ACE) inhibitors.

With prolonged use of Fazostabil, systematic monitoring of the functional state of the liver, general blood count and fecal occult blood test is shown.

In elderly patients who have been receiving low doses of ASA for a long time as an antiplatelet agent, the risk of bleeding in the gastrointestinal tract is increased, so caution should be exercised.

In predisposed patients (in the case of reduced uric acid excretion), ASA in low doses can cause gout.

In high doses, ASA has a hypoglycemic effect. This should be taken into account by patients with diabetes mellitus receiving insulin or hypoglycemic oral agents.

It was reported about the development of hemolytic anemia and hemolysis in patients with severe glucose-6-phosphate dehydrogenase deficiency who received ASA. The threat of diseases from the blood increases in the following cases: taking ASA in high doses, the presence of fever or acute infections.

Ethanol, used simultaneously with ASA, increases the likelihood of damage to the gastrointestinal mucosa and lengthening the bleeding time.

If it is necessary to prescribe systemic glucocorticosteroids, it is necessary to take into account that with their simultaneous use, the concentration of salicylates in the blood decreases, and after they are canceled, it increases, which is fraught with an overdose.

Fazostabil is not recommended for use in conjunction with ibuprofen in patients at risk of cardiovascular disease, since a decrease in the antiplatelet effect of ASA in daily doses up to 300 mg helps to reduce the cardioprotective effect. If a patient is taking ibuprofen as a pain reliever, they should inform their doctor.

Methotrexate at a weekly dose of <15 mg increases the incidence of adverse hematopoietic effects. During the combined treatment, a blood test should be performed once a week during the first few weeks.

With the joint appointment of lithium or digoxin preparations, their plasma concentrations must be carefully monitored during the period of Fazostabil's use and after its cancellation. If necessary, the dosage is adjusted.

Influence on the ability to drive vehicles and complex mechanisms

Due to the likelihood of adverse reactions from the nervous system during the period of taking Phazostabil, patients are advised to be careful when driving and engaging in activities that require an increased reaction rate and increased concentration of attention.

Application during pregnancy and lactation

• I trimester of pregnancy: Phazostabil is contraindicated, since ASA can cause fetal defects (heart defects, split palate);
• II trimester of pregnancy: the drug can only be used in women in whom the expected benefit from therapy definitely outweighs the potential risks. It is recommended to prescribe ASA in a daily dose of not more than 150 mg for a short time;
• III trimester of pregnancy: salicylates in high daily doses (> 300 mg) help inhibition of labor, cause increased bleeding in the mother and fetus, as well as closure of the ductus arteriosus in the fetus. When they are taken immediately before childbirth, intracranial hemorrhage may develop in newborns, especially premature babies. In this regard, in the last trimester, the appointment of Fazostabil is contraindicated;
• the period of breastfeeding: there is not enough data on the basis of which it would be possible to fully establish the possibility or impossibility of taking ASA during lactation. It is known that salicylates and their metabolites are excreted in small amounts in mother's milk. Accidental (one-time) intake of ASA during lactation does not cause side effects in the child, therefore it does not require the termination of feeding. If a high dose is taken, breastfeeding should be stopped immediately. If long-term treatment with Fazostabil is necessary, it is recommended to transfer the child to artificial feeding.

Pediatric use

Fazostabil tablets are prohibited for children and adolescents under 18 years of age.

With impaired renal function

Phasostabil is contraindicated in patients with CC <30 ml / min (severe renal failure).

The drug should be used with caution in the treatment of patients with CC> 30 ml / min (mild and moderate renal failure).

For violations of liver function

Phazostabil is contraindicated in class B and C liver failure according to the Child-Pugh classification (moderate and severe).

The drug should be used with caution in the treatment of patients with class A hepatic insufficiency according to the Child-Pugh classification (mild severity), it is necessary to regularly monitor liver function.

Use in the elderly

Fazostabil should be used with caution in elderly patients.

Drug interactions

ASA enhances the action and increases the toxicity of the following drugs:

• valproic acid - due to its displacement from the connection with plasma proteins;
• methotrexate - due to a decrease in renal clearance and its displacement from the connection with plasma proteins.

ASA increases the impact and risk of side effects of the following drugs:

• sulfonamides, including co-trimoxazole - by increasing their concentration in the blood plasma and displacing them from the connection with plasma proteins;
• other NSAIDs, narcotic analgesics - due to the synergism of action;
• carbonic anhydrase inhibitors, including acetazolamide - salicylates can increase their toxicity to the central nervous system and the likelihood of developing severe acidosis;
• lithium and digoxin - due to a decrease in their renal excretion and a decrease in plasma concentrations;
• selective serotonin reuptake inhibitors, including sertraline and paroxetine - as a result of synergism with ASA, the risk of bleeding from the upper gastrointestinal tract increases;
• antiplatelet agents, including clopidogrel and dipyridamole, indirect anticoagulants, including ticlopidine and warfarin, thrombolytic agents, heparin - due to displacement from the connection with blood plasma proteins and synergism of the main therapeutic effects;
• hypoglycemic oral agents, which are derivatives of sulfonylureas, and insulin - since ASA in daily doses of more than 2000 mg exhibits hypoglycemic activity; in addition, it displaces sulfonylurea derivatives from the bond with plasma proteins;
• ethanol and alcoholic beverages - due to the additive action, damage to the gastrointestinal mucosa increases and bleeding time is lengthened.

The following drugs reduce the antiplatelet effect of ASA:

• cholestyramine and antacids containing magnesium and / or aluminum hydroxide - due to a decrease in the absorption of ASA in the gastrointestinal tract;
• systemic glucocorticosteroids, with the exception of hydrocortisone, prescribed as substitution therapy for Addison's disease - due to increased elimination of salicylates;
• ibuprofen - due to the manifestation of antagonist properties in relation to the suppression of platelet aggregation.

In low doses, ASA weakens the effect of uricosuric agents (sulfinpyrazone, probenecid, benzbromarone), which is due to the competitive tubular elimination of uric acid.

In high doses, ASA is able to reduce the hypotensive effect of diuretics (due to a decrease in the glomerular filtration rate against the background of suppression of the synthesis of renal prostaglandins) and antihypertensive drugs. In particular, ASA can reduce the effect of ACE inhibitors due to the competitive blockade of prostacyclin synthesis.

Analogs

The analogs of Fazostabil are Agrenox, Antagrex, Aspirin Cardio, Brilinta, Ventavis, Detromb, Ilomedin, Zilt, Cardiomagnyl, Clapitax, Cardogrel, Clopidogrel, Lirta, Monafram, Plavix, Sanovask, Trombex, Effludergl, Effrombomag,

Terms and conditions of storage

Store the drug in a dark place, out of the reach of children, at a temperature not exceeding 25 ° C.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Available without a prescription.

Reviews about Phazostabil

According to reviews, Fazostabil is a good drug that prevents the development of thrombosis, strokes and cardiovascular complications.

There are no reported side effects.

The price of Fazostabil in pharmacies

The price of Fazostabil depends on the dosage, the number of tablets in the package, as well as the region of sale and the pharmacy chain that sells the drug. The approximate cost for a pack of 100 film-coated tablets, 75 mg + 15.2 mg each is 133-154 rubles, 150 mg + 30.39 mg each - 198-325 rubles.

Fazostabil: prices in online pharmacies

Drug name Price Pharmacy

Phazostabil 150 mg + 30.39 mg film-coated tablets 50 pcs. 119 RUB Buy

Phazostabil tablets p.p. 150mg + 30.39mg 50 pcs. 134 r Buy

Phazostabil 75 mg + 15.2 mg film-coated tablets 100 pcs. RUB 138 Buy

Phazostabil 150 mg + 30.39 mg film-coated tablets 100 pcs. 188 r Buy

Phazostabil tablets p.p. 150mg + 30.39mg 100 pcs. 249 r Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!