Кардиомагнил®

General characteristics. Structure:

Active ingredients: Acetylsalicylic acid of 75 mg or 150 mg
Magnesium hydroxide of 15,2 mg or 30,39 mg

Excipients: starch corn, cellulose microcrystallic, magnesium stearate, potato starch, gipromelloza (methylhydroxypropyl cellulose 15), macrogoal (propylene glycol), talc.

Description
Tablets are the film coated, containing 75 mg / 15,2 mg of acetylsalicylic acid and magnesium of hydroxide, respectively: tablets, film coated, white color in the form of the stylized "heart"
Tablets are the film coated, containing 150 mg / 30,39 mg of acetylsalicylic acid and magnesium of hydroxide, respectively: tablets, film coated, white color, an oval form with risky on one party.

Pharmacological properties:

Pharmacodynamics. The irreversible ingibition of cyclooxygenase (TsOG-1) therefore synthesis of A2 thromboxane is blocked is the cornerstone of the mechanism of effect of acetylsalicylic acid (ASK) and aggregation of thrombocytes is suppressed. Consider that ASK has also other mechanisms of suppression of aggregation of thrombocytes that broadens area of its use at various vascular diseases. ASK has also antiinflammatory, anesthetizing, febrifugal effect. Magnesium the hydroxide which is Kardiomagnil's part protects a mucous membrane of digestive tract from influence of acetylsalicylic acid.

Pharmacokinetics. ASK is soaked up from digestive tract almost completely. The elimination half-life of ASK makes about 15 minutes since with the participation of ASK enzymes it is quickly hydrolyzed in the salicylic acid (SA) in intestines, a liver and a blood plasma. The elimination half-life of SK makes about 3 hours, but it can increase considerably at simultaneous introduction of high doses of ASK (more than 3,0 g) as a result of saturation of fermental systems.
Bioavailability of ASK makes about 70%, but this size substantially fluctuates as ASK is exposed to presistemny hydrolysis (mucous digestive tract, a liver) in SK under the influence of enzymes. Bioavailability of SK makes 80-100%.
The used doses of magnesium of hydroxide do not influence bioavailability of acetylsalicylic acid.

Indications to use:

Primary prevention of cardiovascular diseases, such as thrombosis and acute heart failure with risk factors (for example, a diabetes mellitus, a lipidemia, arterial hypertension, obesity, smoking, advanced age).
Prevention of a repeated myocardial infarction and thrombosis of blood vessels.
Prevention of a thromboembolism after surgical interventions on vessels (aortocoronary shunting, transdermal transluminal coronary angioplasty).
Unstable stenocardia.

Route of administration and doses:

Tablets are swallowed entirely, washing down with water. At desire the tablet can be pulled down in half, to chew or previously to pound.

Primary prevention of cardiovascular diseases, such as thrombosis and acute heart failure with risk factors (for example, a diabetes mellitus, a lipidemia, an arterial gipergenziya, obesity, smoking, advanced age) 
1 tablet of Kardiomagnil containing ASK in a dose of 150 mg in the first days then on 1 tablet of Kardiomagnil containing ASK in a dose of 75 mg of 1 times a day.

Prevention of a repeated myocardial infarction and thrombosis of blood vessels
1 tablet of Kardiomagnil containing ASK in a dose of 75 - 150 mg of 1 times a day.

Prevention of a thromboembolism after surgical interventions on vessels (aortocoronary shunting, transdermal transluminal coronary angioplasty) 
1 tablet of Kardiomagnil containing ASK in a dose of 75 - 150 mg of 1 times a day.

Unstable stenocardia
1 tablet of Kardiomagnil containing ASK in a dose of 75 - 150 mg of 1 times a day.

Features of use:

Drug should be used after appointment of the doctor.
ASK can provoke a bronchospasm, and also cause attacks of bronchial asthma and other hypersensitivity reactions. Risk factors are existence of bronchial asthma in the anamnesis, hay fever, the polypose of a nose, chronic diseases of respiratory system, and also allergic reactions to other drugs (for example, skin reactions, an itch, urticaria). 
ASK can cause bleedings of various degree of manifestation in time and after surgical interventions.
ASK combination to anticoagulants, trombolitika and antithrombocytic drugs is followed by the increased risk of development of bleedings.
ASK in low doses can provoke development of gout in the predisposed persons (having reduced excretion of uric acid).
ASK combination to a methotrexate is followed by the increased frequency of development of side effects from bodies of a hemopoiesis.
High doses of ASK render hypoglycemic effect that patients need to mean at appointment it with the diabetes mellitus receiving hypoglycemic means.
At the combined purpose of GKS and salicylates it is necessary to remember that during treatment the level of salicylates in blood is reduced, and after cancellation of GKS the overdose of salicylates is possible.
ASK combination to an ibuprofen as the last worsens beneficial effect of ASK on life expectancy is not recommended. Exceeding of a dose of ASK is accompanied by risk of gastrointestinal bleeding. The overdose is especially dangerous at patients of advanced age.
At ASK combination to alcohol the risk of injury of a mucous membrane of digestive tract and lengthening of a bleeding time is increased.

Influence on ability to manage the car / moving mechanisms
It is not observed.

Side effects:

Frequency of the side reactions given below was defined according to the following:
- very often ≥ 1/10;
- often> 1/100, <1/10:
- sometimes> 1/1000, <1/100;
- seldom> 1/10 000, <1/1000;
- very seldom <1/10 000, including separate messages.

Allergic reactions: small tortoiseshell (often), Quincke's edema (often).

Immune system: anaphylactic reactions (sometimes).

Digestive tract: nausea (often), heartburn (very often), vomiting (often), pain in a stomach, ulcers of a mucous membrane of a stomach and a duodenum (sometimes), including perforative (seldom), gastrointestinal bleedings (sometimes), increase in activity of "hepatic" enzymes (rarely), stomatitis (very seldom), an esophagitis (very seldom), erosive damages of upper parts of digestive tract (very seldom), strictures (very seldom), colitis (very seldom), a syndrome of the angry intestines (very seldom).

Respiratory system: bronchospasm (often)

System of a hemopoiesis: the raised bleeding (very often), anemia (seldom), a prothrombinopenia (very seldom), thrombocytopenia (very seldom), a neutropenia, aplastic anemia (very seldom), an eosinophilia (very seldom), an agranulocytosis (very seldom).

Central nervous system: dizziness (sometimes), headache (often), sleeplessness (often), drowsiness (sometimes), sonitus, intracerebral bleeding (rarely).

Interaction with other medicines:

At simultaneous use of ASK strengthens effect of the following medicines:
• a methotrexate due to decrease in renal clearance and its replacement from communication with proteins
• heparin and indirect anticoagulants due to dysfunction of thrombocytes and replacement of indirect anticoagulants from communication with proteins
• thrombolytic and antithrombocytic drugs (tiklopidin)
• digoxin owing to decrease in its renal excretion
• hypoglycemic means (insulin and derivatives of sulphonylurea) due to hypoglycemic properties of the ASK in high doses and replacement of derivatives of sulphonylurea from communication with proteins
• valproic acid due to its replacement from communication with proteins
The additive effect is observed at a concomitant use of ASK with ethanol (alcohol).
ASK weakens action of uricosuric means (benzbromaron) owing to competitive tubular elimination of uric acid.
Strengthening elimination of salicylates. system glucocorticosteroids (GKS) weaken their action.
Antacids and Colestyraminum reduce drug absorption.

Contraindications:

Hypersensitivity to ASK, excipients of drug and other NPVP, hemorrhage in a brain; tendency to bleeding (insufficiency of vitamin K, thrombocytopenia, hemorrhagic diathesis); the bronchial asthma induced by reception of salicylates and NPVP; an erosive canker of a gastro intestinal path (in an aggravation phase); gastrointestinal bleeding; heavy renal failure (clearance of creatinine less than 10 ml/min.); pregnancy (I and III trimesters); lactation period; deficit glyukozo-6-fosfatdegidrogenazy; a concomitant use with a methotrexate (more than 15 mg a week); children's age up to 18 years.

With care
At gout, a hyperuricemia, existence in the anamnesis of cankers of digestive tract or gastrointestinal bleedings, a renal and/or liver failure, bronchial asthma, hay fever, a nose polypose, allergic states, in the II trimester of pregnancy.

Use during pregnancy
Use of high doses of salicylates in the first 3 months of pregnancy is associated with the increased frequency of defects of fetation. In the II trimester of pregnancy it is possible to appoint salicylates only taking into account strict assessment of risk and advantage.
In the last trimester of pregnancy salicylates in a high dose (more than 300 mg/days) cause braking of patrimonial activity, premature closing of an arterial channel in a fruit, the raised bleeding in mother and a fruit, and appointment just before childbirth can cause intracraneal hemorrhages, especially in premature children. Purpose of salicylates in the last trimester of pregnancy is contraindicated.

Use in the period of a lactation
Salicylates and their metabolites in small amounts get into breast milk. Accidental reception of salicylates in the period of a lactation is not followed by development of side reactions in the child and does not demand the breastfeeding termination. However, at prolonged use of drug or appointment it in a high dose feeding by a breast should be stopped immediately.

Overdose:

Symptoms of overdose of moderate severity
nausea, vomiting, sonitus, deterioration in hearing, dizziness, confusion of consciousness.
Treatment: to wash out a stomach, to accept absorbent carbon. Symptomatic treatment.

Symptoms of overdose of heavy degree
fever, hyperventilation, ketoacidosis, respiratory alkalosis, coma, cardiovascular and respiratory insufficiency, the expressed hypoglycemia.
Treatment: immediate hospitalization in specialized departments for performing the emergency therapy - gastric lavage, determination of acid-base balance, the alkaline and forced alkaline diuresis, a hemodialysis, administration of solutions, absorbent carbon, symptomatic therapy. When carrying out an alkaline diuresis it is necessary to achieve values рН between 7.5 and 8. The forced alkaline diuresis should be carried out when concentration of salicylates in plasma makes more than 500 mg/l (3,6 mmol/l) at adults and children have 300 mg/l (2,2 mmol/l).

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity of 5 years. Not to use until expiry date.

Issue conditions:

Without recipe

Packaging:

Tablets film coated 75 mg +15,2 mg and 150 mg + 30.39 mg 
On 30 or 100 tablets in the glass bottles of brown color corked by the screw-on cover of white color (from polyethylene) with the built-in removable cap with a sealant to which the ring for a separation of the condensing laying providing control of the first opening is attached. A part of the label is attached to a bottle by a special adhesive tape which allows to raise the label. The application instruction in the form of the developing leaf is located under a mobile part of the label.