Aspirin Cardio - instructions for use, dose, side effects, contraindications

auxiliary substances: cellulose, powder 10 mg or 30 mg, corn starch 10 mg or 30 mg; (1: 1) 7.857 mg or 21.709 mg, polysorbate 80 0.186 mg or 0.514 mg, sodium lauryl sulfate 0.057 mg or 0.157 mg, talc 8,100 mg or 22,380 mg, triethylcigrate 0.800 mg or 2.240 mg .

Description:Round biconvex tablets of white color; on a transverse section a homogeneous mass of white, surrounded by a shell of white.

Pharmacotherapeutic group:Antiaggregant agent

ATX: & nbsp

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

Pharmacodynamics:

The mechanism of antiplatelet effect of acetylsalicylic acid (ASA) is irreversible inhibition of cyclooxygenase (COX-1), which blocks the synthesis of thromboxane A2 and suppresses platelet aggregation.The antiaggregant effect is most pronounced in platelets, since they are not able to re-synthesize cyclooxygenase. It is believed that ASA has other mechanisms for suppressing platelet aggregation, which expands its use in various vascular diseases.

ASA also has anti-inflammatory, analgesic and antipyretic effects.

Pharmacokinetics:Suction

After oral administration ASA is quickly and completely absorbed from the gastrointestinal tract (GIT). ASA is partially metabolized during absorption. During and after absorption, ASA is converted to a major metabolite, salicylic acid. Due to the fact that the tablets are covered with an acid-resistant coating, ASA is released not in the stomach, but in the alkaline medium of the duodenum. The maximum concentration of acetylsalicylic acid in the blood plasma (Cmax) is reached approximately 2-7 hours after taking the tablets, thus, the absorption of ASA in the form of tablets coated with an enteric coating is slowed down compared to conventional tablets (without an enteric coating).

With simultaneous intake with food, a decrease in ASA suction is noted without affecting the degree of absorption.The lower absorption rate of ASA tablets coated with an enteric-coated membrane does not affect the exposure of ASA in blood plasma and its ability to inhibit platelet aggregation during prolonged therapy with low doses of the drug. However, in order to maximize the stability of Aspirin Cardio® tablets in the stomach, it is recommended that you take the drug 30 minutes before eating, squeezed with plenty of fluids (see section "Method of administration and dose").

Distribution

ASA and salicylic acid are largely associated with blood plasma proteins and are rapidly distributed in the body. Salicylic acid penetrates the placenta and is excreted in breast milk.

Metabolism

The main metabolite of ASA is salicylic acid. Metabolism of salicylic acid is carried out in the liver with the formation of salicylic acid, phenolic glucuronide of salicylic acid, salicylglucuronide and gentisuric acid. Excretion

Elimination of salicylic acid is dose-dependent, since its metabolism is limited by the possibilities of the enzymatic system. The half-life is between 2-3 hours when using ASA inlow doses and up to 15 hours when the drug is used in high doses (usual doses of acetylsalicylic acid as an analgesic agent). Salicylic acid and its metabolites are excreted by the kidneys.

According to pharmacokinetic data, there are no clinically significant deviations in the concentration-dose curve when taking ASA in a dose of 100 mg to 500 mg.

Indications:

- Primary 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 angina (including suspected development of acute myocardial infarction) and stable angina;

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

- Prophylaxis of transient cerebral circulation disorder;

- 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, carotid angioplasty)

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

Contraindications:

- Hypersensitivity to acetylsalicylic acid, excipients in the drug or non-steroidal anti-inflammatory drugs (NSAIDs);

- Bronchial asthma induced by the intake of salicylates and other NSAIDs; combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to ASA

- Erosive-ulcerative lesions of the gastrointestinal tract (in the stage of exacerbation)

- Gastrointestinal bleeding

- Hemorrhagic diathesis

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

- Pregnancy (I and III trimester) and the period of breastfeeding

- Children and adolescents under 18 years of age (due to lack of data on effectiveness and safety)

- Severe renal dysfunction

- Severe liver dysfunction

- Chronic heart failure III-IV functional class by classification NYHA.

Carefully:

- Hypersensitivity to analgesics, anti-inflammatory drugs, anti-rheumatic drugs, as well as allergic reactions to other substances.

- Presence in the anamnesis of ulcerative lesions of the gastrointestinal tract, including chronic and recurrent lesions of the gastrointestinal tract or gastrointestinal hemorrhages in the anamnesis.

- Simultaneous use with anticoagulants (see section "Interaction with other drugs")

- With gout, hyperuricemia

- When a violation of liver function

- In case of impaired renal function

- In cases of circulatory disorders that occur as a result of atherosclerosis of the renal arteries, congestive heart failure, hypovolemia, extensive surgical intervention, sepsis, cases of massive bleeding

- With bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, chronic diseases of the respiratory system, as well as allergic reactions to other drugs (for example, skin reactions, itching, urticaria)

- In severe forms of deficiency of glucose-6-phosphate dehydrogenase

- In the second trimester of pregnancy

- With the proposed surgical intervention (including minor, for example, tooth extraction)

- When combined with the following drugs (cm.section "Interaction with other drugs"):

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

- with anticoagulant, thrombolytic or other antiplatelet agents

- with NSAIDs (including ibuprofen, naproxen);

- 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.

Pregnancy and lactation:Application in pregnancy

Inhibition of prostaglandin synthesis can have a negative effect on pregnancy and the development of an embryo or fetus.

Data from epidemiological studies on the use of inhibitors of prostaglandin synthesis in early pregnancy raise concerns about the risk of abortion and fetal malformations, presumably increasing with increasing doses and duration of treatment. The available data do not confirm the relationship between the intake of acetylsalicylic acid and the increased risk of abortion.There are conflicting epidemiological studies on the relationship between the use of acetylsalicylic acid and fetal development defects, which do not allow excluding the increased risk of gastroschisis. A prospective study of 14,800 women in early pregnancy (1-4 months) showed no increase in fetal development defects with acetylsalicylic acid. Animal studies have demonstrated the reproductive toxicity of acetylsalicylic acid. In the first trimester of pregnancy, the use of drugs containing acetylsalicylic acid is contraindicated.

In the second trimester of pregnancy, salicylates can be prescribed only with strict risk assessment and benefit to the mother and fetus.

Women planning a pregnancy or in the second trimester of pregnancy should minimize the dose of acetylsalicylic acid and the duration of treatment.

In the III trimester of pregnancy, prostaglandin synthesis inhibitors can cause suppression of uterine contractions, leading to inhibition of labor, increased bleeding time and increased antiaggregant effect (even with low-dose acetylsalicylic acid).

The fetus may develop cardiopulmonary intoxication with premature closure of the arterial duct and the development of pulmonary hypertension, as well as impaired renal function, up to the development of kidney failure, accompanied by malnutrition. The use of acetylsalicylic acid in the third trimester of pregnancy is contraindicated.

Application in the period of breastfeeding

Salicylates and their metabolites penetrate into breast milk in small amounts. Episodic salicylates during the period of breastfeeding 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 as soon as possible.

Dosing and Administration:

Tablets of the drug ASPIRIN® CARDIO should be taken at least 30 minutes before meals, washed down with plenty of water. To ensure the release of ASA in the alkaline environment of the duodenum, the tablets should not be broken, chopped or chewed. Aspirin® CARDIO tablets are taken once a day or every other day.ASPIRIN® CARDIO is intended for long-term use. The duration of therapy is determined by the doctor.

Primary prevention of acute myocardial infarction in the presence of risk factors: 100 mg / day or 300 mg every other day.

Prevention of recurrent myocardial infarction, stable and unstable angina: 100-300 mg / day.

Unstable angina (with suspected development of acute myocardial infarction): the initial dose of 100-300 mg (the tablet must be broken, chopped or chewed for faster absorption) should be accepted by the patient as soon as possible after the suspicion of the development of 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: 100-300 mg / day.

Preventive maintenance of a thromboembolism after operation and invasive interventions on vessels: 100-300 mg / day.

Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches: 100-200 mg / day or 300 mg every other day.

Actions when missing one or more doses of the drug: Take the missed pill right away, as soon as you remember it and on. Continue reception as usual. To avoid doubling the dose, do not take the missed tablet if the next tablet time is approaching.

Features of the drug during the first admission and when it is canceled: Features of the drug at the first admission and its cancellation was not observed.

Special patient groups

Children

Safety and efficacy of Aspirin® Cardio in children and adolescents under the age of 18 years is not established. The use of Aspirin® Cardio in patients younger than 18 years is contraindicated.

Patients with impaired hepatic function

Aspirin® Cardio is contraindicated in patients with severe hepatic impairment. Care should be taken with Aspirin® Cardio in patients with impaired liver function.

Patients with impaired renal function

Aspirin® Cardio is contraindicated in patients with severe renal impairment. Care should be taken with Aspirin® Cardio in patients with impaired renal function,as taking Aspirin® Cardio may increase the risk of developing kidney failure and acute kidney failure.

Side effects:

The adverse reactions presented below are obtained as spontaneous reports in the process of post-marketing use of preparations containing acetylsalicylic acid, therefore the frequency of their occurrence can not be established. Adverse reactions are listed in accordance with the defeat of organs and organ systems. To classify and describe a specific reaction, its synonyms and associated states, the most appropriate term is used from the Medical Dictionary for regulatory activity (MedDRA).

Violations from the blood and lymphatic system:

Hemorrhagic anemia ^a,

Iron-deficiency anemia ^a with the relevant clinical and laboratory features and symptoms,

hemolysis ^b,

hemolytic anemia ^b.

Immune system disorders:

Hypersensitivity, drug intolerance,

Allergic edema and angioedema (Quincke's edema),

anaphylactic reactions,

anaphylactic shock with appropriate laboratory and clinicalmanifestations.

Impaired nervous system:

Hemorrhagic stroke or intracranial hemorrhage,

dizziness.

Hearing disorders and labyrinthine disturbances:

Noise in ears.

Heart Disease:

Cardio-respiratory distress syndrome ^at.

Vascular disorders:

Hemorrhage,

surgical bleeding,

hematomas,

muscle hemorrhage.

Disturbances from the respiratory system, chest and mediastinal organs:

Nose bleed,

analgesic asthmatic syndrome (bronchospasm),

rhinitis,

nasal congestion.

Disorders from the gastrointestinal tract:

Dyspepsia,

pain from the gastrointestinal tract,

abdominal pain,

bleeding gums,

inflammation of the gastrointestinal tract,

gastrointestinal bleeding,

ulcers of the mucous membrane of the stomach and duodenum,

perforated ulcers of the mucous membrane of the stomach and duodenum (with the corresponding clinical symptoms and laboratory changes).

Disorders from the liver and bile ducts:

Violation of the function of the liver,

increased activity of hepatic transaminases.

Disturbances from the skin and subcutaneous tissues:

Skin rash,

itching,

hives.

Disorders from the kidneys and urinary tract:

Bleeding from the genitourinary tract,

impaired renal function ^g,

acute renal failure ^g.

Trauma, intoxication and complications of manipulation:

see the section "Overdose"

a - is associated with bleeding;

b - is associated with severe forms of deficiency of glucose-6-phosphate dehydrogenase;

c - is associated with severe allergic reactions;

g - in patients with impaired renal function or cardiovascular disorders present prior to initiation of treatment with Aspirin® Cardio.

Overdose:

Salicylate intoxication (developing with ASA taken at a dose of more than 100 mg / kg / day for more than 2 days) may result from prolonged use of toxic doses of the drug in the context of improper therapeutic use of the drug (chronic intoxication) or a single incidental or intentional administration of a toxic dose of the drug adult or child (acute intoxication). Symptoms chronic intoxication derivatives of salicylic acid are non-specific and are often difficult to diagnose.Intoxication of mild severity usually develops only after repeated use of large doses of the drug and is manifested by dizziness, vertigo, noise in the ears, hearing loss, increased sweating, nausea and vomiting, headache and confusion. This symptomatology disappears after a decrease in the dose of the drug. Noise in the ears can appear with an ASA concentration in the blood plasma from 150 to 300 μg / ml. More severe symptoms are manifested when the concentration of ASA in the blood plasma is above 300 μg / ml. The main manifestation acute intoxication is a serious violation of the acid-base state, the manifestations of which can vary depending on the age of the patient and the severity of intoxication. The most typical development in children is development metabolic acidosis. Since the rate of absorption of ASA may be reduced due to delayed emptying of the stomach, the formation of concrements or the administration of drugs resistant to gastrointestinal juice, it is impossible to judge the severity of intoxication only by changing the concentration of salicylates in the blood plasma. Treatment of intoxication is carried out in accordance with accepted standards anddepends on the degree of severity of intoxication and clinical picture and should be directed mainly to accelerate the elimination of the drug and restore the water-electrolyte balance and acid-base state.

Below are the symptoms and laboratory data in case of salicylate poisoning and therapeutic measures.

Overdose Symptoms	Laboratory and instrumental data	Therapeutic measures
From mild to moderate severity		Gastric lavage, repeated intake of activated charcoal, forced alkaline diuresis
Tachypnea, hyperventilation, respiratory alkalosis	Alkalemia, alkaluria	Restoration of water electrolyte balance and acid-base state.
Profuse sweating
Nausea, vomiting
Medium to severe		Gastric lavage, repeated intake of activated charcoal, forced alkaline diuresis; in severe cases of hemodialysis.
Respiratory alkalosis with compensatory metabolic acidosis	Aciduria, aciduria	Restoration of water electrolyte balance and acid-base state.
Hyperpyrexia (extremely high body temperature)		Restoration of water electrolyte balance and acid-base state.
Respiratory disorders: hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, asphyxia;
Disorders from the cardiovascular system: heart rhythm disturbances, arterial hypotension, oppression of cardiac activity	Change in blood pressure, ECG
Violations of water electrolyte balance: dehydration, impaired renal function from oliguria up to the development of renal failure	Hypokalemia, hypernatremia, hyponatremia, impaired renal function	Restoration of water electrolyte balance and acid-base state.
Disturbance of glucose metabolism, ketosis	Hyperglycemia, hypoglycemia (especially in children), ketoacidosis
Noise in the ears, deafness
Gastrointestinal bleeding
Hematologic disorders: from inhibition of platelet aggregation to coagulopathy	Prothrombin time prolongation, hypoprothrombinemia
Neurological disorders: toxic encephalopathy and depression of CNS function (drowsiness, confusion, coma, convulsions)

Interaction:

With the simultaneous use of ASA enhances the effect of the following medicines:

- methotrexate by reducing renal clearance and displacing it from the bond with proteins; use of Aspirin® Cardio together with methotrexate is contraindicated if the dose of the latter exceeds 15 mg per week (see the section "Contraindications") and possibly with caution - with a dose of methotrexate less than 15 mg per week;

- heparin and indirect anticoagulants due to impaired platelet function and the displacement of indirect anticoagulants from the connection with proteins;

- when used simultaneously with anticoagulants, thrombolytic and antiplatelet agents, there is an increased risk of bleeding as a result of synergism of the main therapeutic effects of the drugs used;

- with simultaneous use with drugs that have anticoagulant, thrombolytic or antiaggregant effect, there is a marked increase in the damaging effect on the mucosa of the gastrointestinal tract;

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

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

- hypoglycemic drugs (insulin, sulfonylureas) due to the hypoglycemic properties of ASA itself at high doses and the displacement of sulfonylurea derivatives from the connection with blood plasma proteins;

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

- NSAIDs (increased risk of ulcerogenic effect and bleeding from the gastrointestinal tract as a result of synergistic action);

- Ethanol (alcoholic beverages) (increased risk of damage to the mucous membrane of the gastrointestinal tract and prolonged bleeding time due to the mutual enhancement of the effects of ASA and ethanol).

Simultaneous administration of ASA in high doses may weaken the effect of the following medicines:

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

- inhibitors of angiotensin-converting enzyme (ACE) (there is a dose-dependent decrease in glomerularfiltration (GFR) as a result of inhibition of prostaglandins with vasodilating action, respectively, weakening of hypotensive action;

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

With simultaneous (within one day) application with ibuprofen and naproxen antagonism is noted with respect to the irreversible inhibition of platelets caused by the action of ASA. The clinical significance of this effect is unknown. The combination of ASA with ibuprofen in patients with a high risk of cardiovascular disease is not recommended because of a possible reduction in the cardioprotective effects of ASA. When used simultaneously with systemic glucocorticosteroids (SCS) (with the exception of hydrocortisone or another SCS used for the replacement therapy of Addison's disease), there is an increase in the elimination of salicylates and, accordingly, a weakening of their action. When combined use of GCS and salicylates should be remembered that during treatment, the level of salicylates in the blood is reduced,and after the cancellation of SCS, an overdose of salicylates is possible.

Special instructions:

Aspirin® Cardio should be used with caution under the following conditions:

- Hypersensitivity to analgesics, anti-inflammatory drugs, anti-rheumatic drugs, as well as allergic reactions to other substances.

- Presence in the anamnesis of ulcerative lesions of the gastrointestinal tract, including including chronic and recurrent lesions of the gastrointestinal tract, or gastrointestinal hemorrhages in the anamnesis.

- Simultaneous use with anticoagulants (see section "Interaction with other drugs and / or food")

- In case of impaired renal function or circulatory failure resulting from arteriosclerosis of the renal arteries, congestive heart failure, hypovolemia, extensive surgical intervention, sepsis or cases of massive bleeding, as in all of these cases ASA may increase the risk of acute renal failure and renal dysfunction.

- In severe forms of deficiency of glucose-6-phosphate dehydrogenase, ASA can cause hemolysis and hemolytic anemia.Factors that may increase the risk of hemolysis are fever, acute infections and high doses of the drug.

- When a violation of liver function

- Some NSAIDs (ibuprofen, naproxen) can weaken the inhibitory effect of ASA on platelet aggregation. Patients taking ASA and planning to take NSAIDs should discuss this with the attending physician (see the section "Interaction with other medicinal products and / or food products").

- 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 (including minor surgeries, such as tooth extraction).

- ASA in low doses reduces the excretion of uric acid, which can lead to gout attacks in patients prone to this disease.

- Excess dose of ASA is associated with a risk of gastrointestinal bleeding.

- Overdose is especially dangerous in elderly patients.

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

Taking Aspirin® Cardio does not affect the ability to drive a car / moving machinery.

Form release / dosage:Tablets coated with enteric coating 100 mg, 300 mg.

Packaging:Intestinal-coated tablets 100 mg:

on 10 or 14 tablets in blisters from Al / PP. For 2 blisters for 10 tablets or 2, 4 or 7 blisters for 14 tablets together with instructions for use in a cardboard box.

Intestinal-coated tablets 300 mg:

on 10 or 14 tablets in blisters from Al / PP. For 2 blisters for 10 tablets or 2 or 4 blisters for 14 tablets together with instructions for use in a cardboard pack.

Storage conditions:At a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:П N015400 / 01

Date of registration:24.11.2009 / 23.08.2017

Expiration Date:Unlimited

The owner of the registration certificate:Bayer Konsyumer Kare AGBayer Konsyumer Kare AG Switzerland

Manufacturer: & nbsp

BAYER BITTERFELD, GmbH Germany

Representation: & nbspBAYER, AOBAYER, AO

Information update date: & nbsp19.10.2017

Illustrated instructions

Instructions

Aspirin® Cardio (Aspirin® Cardio)