Sanovasque - instructions for use, doses, side effects, contraindications

Excipients (core): lactose monohydrate is 31.50 mg, 47.25 mg or 63.00 mg, microcrystalline cellulose is 16.30 mg, 24.40 mg or 32.60 mg, silicon colloidal dioxide is 1.70 mg, 2.60 mg or 3.40 mg, sodium carboxymethyl starch - 0.50 mg, 0.75 mg or 1.00 mg.

Auxiliary substances (shell): copolymer of methacrylic acid and ethyl acrylate [1: 1] - 3.35 mg, 6.70 mg or 10.05 mg, povidone K17 0.56 mg, 1.12 mg or 1.68 mg, talc 0.75 mg , 1.50 mg or 2.25 mg, macrogol 4000 to 0.34 mg, 0.68 mg or 1.02 mg.

Description:

Round, biconvex tablets, covered with enteric film coating, white or almost white. On the cross-section: the core is white or almost white in color and a thin stripe of the shell.

Pharmacotherapeutic group:antiplatelet agent

ATX: & nbsp

N.02.B.A Salicylic acid and its derivatives

Pharmacodynamics:

The mechanism of action of acetylsalicylic acid (ASA) is irreversible inhibition of cyclooxygenase (COX-1), which blocks the synthesis of prostaglandins, prostacyclin and thromboxane. Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.

Increases fibrinolytic activity of blood plasma and reduces concentration vitamin K-dependent coagulation factors (II, VII, IX, X). The antiaggregant effect is most pronounced in platelets, since they are not able to re-synthesize cyclooxygenase. Antiaggregant effect develops after the application of small doses of the drug and persists for 7 days after a single dose. These properties of ASA are used in the prevention and treatment of myocardial infarction, ischemic heart disease, complications of varicose veins.

ASA also has an anti-inflammatory, analgesic, antipyretic effect.

Pharmacokinetics:

When administered orally, ASA is absorbed rapidly and completely from the gastrointestinal tract. ASA is partially metabolized during absorption. During and after absorption, ASA is converted into a major metabolite, salicylic acid, which is metabolized, mainly,In the liver under the influence of liver enzymes with the formation of such metabolites as phenyl salicylate, glucuronide salicylate and salicylic acid, found in many tissues and in urine. In women, the metabolic process is slower (less enzyme activity in the blood serum). ASA and salicylic acid are highly associated with blood plasma proteins (from 66 to 98%: depending on the dose) and are quickly distributed in the body. Salicylic acid penetrates the placenta and is excreted in breast milk.

The half-life of ASA from the blood plasma is about 15-20 minutes. Unlike other salicylates, with repeated administration of the drug, unhydrolyzed ASA does not accumulate in the blood serum. Only 1% of an oral ASA excreted by the kidneys in the form negidrolizirovannoy ACK, the remainder is output as salicylates and their metabolites. In patients with normal renal function 80-100% a single dose of the drug is excreted by the kidneys within 24-72 hours.

Indications:

- Prevention of acute myocardial infarction in the presence of risk factors (eg, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age) and repeated myocardial infarction;

- unstable and stable angina;

- prevention of stroke (including in patients with transient impairment of cerebral circulation);

- prophylaxis of transient impairment of cerebral circulation;

- prevention of thromboembolism after surgery and invasive vascular interventions (eg, coronary artery bypass grafting, carotid endarterectomy, arteriovenous shunting, angioplasty and stenting of the coronary arteries);

- prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches (including during prolonged immobilization as a result of extensive surgical intervention).

Contraindications:

- Hypersensitivity to acetylsalicylic acid, to auxiliary substances in the preparation and other non-steroidal anti-inflammatory drugs (NSAIDs);

- erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

- gastrointestinal bleeding (GIT);

- hemorrhagic diathesis;

- The bronchial asthma, induced by the intake of salicylates and other NSAIDs; a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid;

- combined use with methotrexate at a dose of 15 mg per week or more;

- pregnancy (I and III trimester) and the period of breastfeeding;

- age to 18 years;

- severe renal failure (creatinine clearance (CK) less than 30 ml / min);

- severe hepatic insufficiency (grade B and higher on the Child-Pugh scale);

- chronic heart failure III-IV functional class by classification NYHA;

- lactose intolerance, lactase deficiency, glucose / galactose absorption disorder, since the drug contains lactose monohydrate.

Carefully:

With gout, hyperuricemia, peptic ulcer and duodenal ulcer or gastrointestinal hemorrhage (in the anamnesis), renal failure (QC more than 30 ml / min), cardiovascular disorders (eg, chronic heart failure, hypovolemia, Serious surgical intervention, sepsis, or cases of massive bleeding-the risk of developing kidney failure and acute renal failure), liver failure (below grade B on the Child-Pugh scale), bronchial asthma, chronic diseases aniyah respiratory,hay fever, nasal polyposis, drug allergy, including to the group of NSAIDs, analgesics, anti-inflammatory, antirheumatic drugs; severe forms of glucose-6-phosphate dehydrogenase deficiency, since ASA can cause hemolysis and hemolytic anemia (factors that may increase the risk of hemolysis include high drug dosage, fever and acute infections), pregnancy (II trimester), with the proposed surgical intervention (including minor, for example, tooth extraction); with simultaneous admission with the following medicines (see section "Interaction with other drugs");

- methotrexate in a dose of less than 15 mg per week;

- with anticoagulants, thrombolytic or antiplatelet agents;

- with NSAIDs and salicylic acid derivatives in large doses;

- with digoxin;

- with hypoglycemic agents for oral administration (derivatives of sulfonylureas) and insulin;

- with valproic acid;

- with alcohol (alcoholic beverages in particular);

- with selective serotonin reuptake inhibitors;

- with ibuprofen.

Pregnancy and lactation:

Application in pregnancy

The use of large doses of salicylates in the first 3 months of pregnancy is associated with an increased incidence of fetal developmental defects (cleft palate, heart defects). The appointment of salicylates in the first trimester of pregnancy is contraindicated.

In the second trimester of pregnancy, salicylates can only be given taking into account a strict risk assessment and benefit for the mother and fetus, preferably at doses not higher than 150 mg / day and for a short time.

In the last trimester of pregnancy, salicylates in high doses (more than 300 mg / day) cause inhibition of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhages, especially in premature infants. The appointment of salicylates in the last trimester of pregnancy is contraindicated.

Application during lactation

Salicylates and their metabolites penetrate into breast milk in small amounts. The accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in the child and does not require the cessation of breastfeeding.However, with prolonged use of the drug or its administration in a high dose, breast-feeding should be stopped immediately.

Dosing and Administration:

Inside, not liquid, squeezed large amounts of liquid, it is desirable to take before eating. Tablets are taken once a day.

The duration of therapy is determined by the attending physician.

Primary prevention of acute myocardial infarction in the presence of risk factors:

50-100 mg / day.

Prevention of repeated myocardial infarction, unstable and stable angina:

50-100 mg / day.

Unstable angina (with suspected development of acute myocardial infarction):

The initial dose of 100 mg (the first tablet must be chewed for more rapid absorption) should be accepted by the patient as soon as possible after the suspicion of developing an acute myocardial infarction has arisen. In the next 30 days after the development of myocardial infarction, a dose of 200-300 mg / day should be maintained. After 30 days, appropriate therapy should be prescribed to prevent recurrent myocardial infarction.

Prevention of stroke and transient impairment of cerebral circulation:

75-100 mg / day.

Prevention of thromboembolism after surgery and invasive vascular interventions:

50-100 mg / day.

Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches:

100-200 mg / day.

Side effects:

From the digestive system: often - nausea, heartburn, vomiting, pain in the abdomen; rarely - stomach ulcers and duodenal ulcers; very rarely - perforated ulcers of the mucous membrane of the stomach and duodenum, gastrointestinal bleeding, transitory violations of liver function with increased activity of "liver" transaminases.

From the central nervous system: dizziness, hearing loss, tinnitus, which may be a sign of drug overdose (see "Overdose").

On the part of the hematopoiesis system: increased frequency of perioperative (intra- and postoperative) bleeding, bruising (bruising), nasal bleeding, bleeding gums, bleeding from the genitourinary tract. There are reports of serious cases of bleeding, which include gastrointestinal bleeding and hemorrhage in the brain (especially in patients with hypertension,who did not reach the target of blood pressure (BP) and / or who received concomitant therapy with anticoagulant drugs), which in some cases may be life-threatening. Bleeding can lead to the development of acute or chronic posthemorrhagic / iron deficiency anemia (for example, due to latent bleeding) with appropriate clinicaboratory symptoms (asthenia, pallor, hypoperfusion).

There are reports of hemolysis and hemolytic anemia in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.

Allergic reactions: skin rash, itching, urticaria, Quincke's edema, rhinitis, swelling of the nasal mucosa, bronchospasm, cardiorespiratory distress syndrome, and severe reactions, including anaphylactic shock.

From the urinary system: there are reports of cases of renal failure and acute renal failure.

Overdose:

It can have serious consequences, especially in elderly patients and children. The syndrome of salicylism develops when taking ASA at a dose of more than 100 mg / kg / day for more than 2 days due to consumptiontoxic doses of the drug in the context of improper therapeutic use (chronic poisoning) or a single accidental or intentional administration of a toxic dose of the drug to an adult or child (acute poisoning).

Symptoms of overdose:

- With light and medium 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 charcoal, forced alkaline diuresis, restoration of water-electrolyte balance and acid-base state.

- With moderate to severe severity (a single dose of 150 mg / kg - 300 mg / kg - an average 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 disturbances, marked decrease in blood pressure, suppression of cardiac activity; from the side of the 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; noise in the ears, 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 therapy - gastric lavage, repeated intake of activated carbon, forced alkaline diuresis, hemodialysis, restoration of water-electrolyte balance and acid-base state, symptomatic therapy.

Interaction:

With the simultaneous use of ASA enhances the effect of the following drugs; if it is necessary to simultaneously prescribe ASA with the listed means, consideration should be given to the need to reduce the dose of these funds:

- methotrexate, by reducing renal clearance and displacing it from the bond with proteins;

- with simultaneous use with anticoagulants, thrombolytic and antiplatelet agents (ticlopidine) there is an increased risk of bleeding as a result of synergism of the main therapeutic effects of the drugs used;

- when used simultaneously with drugs that have anticoagulant, thrombolytic or antiplatelet effect, there is an increase in the damaging effect on the gastrointestinal mucosa;

- selective serotonin reuptake inhibitors, which may lead to an increased risk of bleeding from the upper GI tract (synergy with ASA);

- digoxin, due to a decrease in its renal excretion, which can lead to an overdose;

- hypoglycemic agents for oral administration (sulfonylurea derivatives) and insulin due to hypoglycemic properties of ASA itself at high doses and displacement of sulfonylurea derivatives from binding to plasma proteins;

- when used with valproic acid, its toxicity increases due to its displacement from the connection with blood plasma proteins;

- NSAIDs and salicylic acid derivatives in high doses (increased risk of ulcerogenic effect and bleeding from the gastrointestinal tract as a result of synergism of action); when used simultaneously with ibuprofen, antagonism is noted with respect to irreversible platelet suppression caused by the action of ASA, which leads to a decrease in the cardioprotective effects of ASA;

- ethanol (increased risk of damage to the gastrointestinal mucosa and prolongation of bleeding time as a result of the mutual enhancement of the effects of ASA and ethanol).

Simultaneous administration of ASA in high doses may impair the action of the medicines listed below; if it is necessary to simultaneously prescribe ASA with the listed means, consideration should be given to the need to correct the dose of the listed drugs:

- any diuretics (when combined with ASA in high doses, there is a decrease in the glomerular filtration rate (GFR) as a result of a decrease in the synthesis of prostaglandins in the kidneys);

- angiotensin-converting enzyme (ACE) inhibitors (a dose-dependent decrease in GFR due to inhibition of prostaglandins with vasodilator action, respectively,weakening of hypotensive action. Clinical decline in GFR is observed with a daily dose of ASC greater than 160 mg. In addition, there is a decrease in the positive cardioprotective effect of ACE inhibitors assigned to patients for chronic heart failure therapy. This effect is also manifested when applied in conjunction with ASA in large doses.

- drugs with uricosuric action - benzbromarone, probenecid (reduction of uricosuric effect due to competitive suppression of renal tubular excretion of uric acid);

- when used simultaneously with systemic glucocorticosteroids (with the exception of hydrocortisone used for the replacement therapy of Addison's disease), the salicylate excretion is increased and, accordingly, their effect is weakened.

Special instructions:

The drug should be used after the appointment of a doctor.

ASA can provoke bronchospasm, as well as cause seizures of bronchial asthma and other reactions of hypersensitivity. Risk factors are the availability of a history of asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system as well as of allergic reactions to other drugs (e.g., skin reactions, pruritus, urticaria).

The inhibitory effect of ASA on platelet aggregation persists for several days after admission, which may increase the risk of bleeding during surgery or in the postoperative period. If absolute elimination of bleeding is necessary in the course of surgical intervention, it is necessary, if possible, to completely abandon the use of ASA in the preoperative period.

The combination of ASA with anticoagulants, thrombolytic agents and antiaggregant drugs is accompanied by an increased risk of bleeding.

ASA in low doses can provoke the development of gout in predisposed individuals (having a decreased excretion of uric acid).

The combination of ASA with methotrexate is accompanied by an increased incidence of side effects from the hematopoiesis.

High doses of ASA have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents for oral administration (sulfonylurea derivatives) and insulin.

With the simultaneous administration of glucocorticosteroids (GCS) and salicylates, it should be remembered that during treatment, the level of salicylates in the blood is reduced, and after overtreatment of SCS, an overdose of salicylates is possible.

The combination of ASA with ibuprofen in patients with an increased risk of cardiovascular disease is not recommended, as the latter reduces the positive effect of ASA on life expectancy (reduces the cardioprotective effect of ASA). Excess dose of ASA is associated with a risk of gastrointestinal bleeding. Overdose is especially dangerous in elderly patients.

When a combination of ASA with ethanol (alcoholic beverages) is increased the risk of damage to the mucosa of the gastrointestinal tract and prolong the time of bleeding.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, as the use of ASA may cause dizziness.

Form release / dosage:Tablets coated with enteric film coating, 50 mg, 75 mg or 100 mg.

Packaging:

10 tablets per contour cell pack.

For 30 and 60 tablets in a jar of polymer materials.

3 or 6 contour squares or 1 can of polymeric materials are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003515

Date of registration:22.03.2016

Expiration Date:22.03.2021

The owner of the registration certificate:IRBITSK HFZ, OJSC IRBITSK HFZ, OJSC Russia

Manufacturer: & nbsp

IRBITSK HFZ, OJSC Russia

Information update date: & nbsp06.08.2016

Illustrated instructions

Instructions

Sanovas® (Sanovasc®)