NSAIDs, antiplatelet agents. The mechanism of action of aspirin is irreversible inhibition of the enzyme COX-1, resulting in blocked the synthesis of thromboxane A2 and inhibiting platelet aggregation. It is believed that acetylsalicylic acid also has other mechanisms of inhibition of platelet aggregation that expands the scope of its application in various vascular diseases. Aspirin also has anti-inflammatory, analgesic and antipyretic activity.
Magnesium hydroxide, which is part of cardiomagnyl, protect the gastrointestinal mucosa against acetylsalicylic acid.
After oral administration, acetylsalicylic acid is absorbed from the gastrointestinal tract almost completely.
Bioavailability of acetylsalicylic acid is about 70%, but this value is characterized by considerable individual variability due to first-pass hydrolysis in the gastrointestinal mucosa and in the liver with the formation under the action of enzymes of salicylic acid. Bioavailability of salicylic acid is 80-100%.
T1 / 2 of acetylsalicylic acid is about 15 minutes, because the participation of enzymes, it is rapidly hydrolyzed to salicylic acid in the intestine, liver, and blood plasma. T1 / 2 Salicylic acid - about 3 hours, but when taking aspirin at high doses (> 3 g), this figure could be increased significantly as a result of saturation of enzyme systems.
Magnesium hydroxide (used in doses) does not affect the bioavailability of acetylsalicylic acid.
- The tablets should be swallowed whole with water. If you wish, you can break the tablet in half, chew or previously grind.
- For primary prevention of cardiovascular diseases such as thrombosis and acute heart failure in the presence of risk factors (eg, diabetes, hyperlipidemia, hypertension, obesity, smoking, older age) appoint 1 tablet of cardiomagnyl containing acetylsalicylic acid at a dose of 150 mg the first day, followed by 1 tablet of cardiomagnyl containing acetylsalicylic acid 75 mg 1 time / day.
- For the prevention of repeated myocardial infarction and thrombosis of blood vessels appoint 1 tablet of cardiomagnyl containing acetylsalicylic acid at a dose of 75-150 mg 1 time / day.
- For the prevention of thromboembolic events after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty) appoint 1 tablet of cardiomagnyl containing acetylsalicylic acid at a dose of 75-150 mg 1 time / day.
- In unstable angina appoint 1 tablet of cardiomagnyl containing acetylsalicylic acid at a dose of 75-150 mg 1 time / day.
- Acetylsalicylic acid 150 mg
- Magnesium hydroxide, 30.39 mg
- Other ingredients: corn starch - 19.0 mg, microcrystalline cellulose - 25.0 mg, magnesium stearate - 305 mcg, potato starch - 4.0 mg.
- Cover structure: Valium (methylhydroxypropylcellulose 15) - 1.2 mg, propylene glycol - 240 mcg, talc - 720 micrograms.
- Overdose symptoms of moderate severity: nausea, vomiting, tinnitus, hearing loss, dizziness, confusion.
- Treatment: should be made gastric lavage, should be appoint activated charcoal, symptomatic therapy.
- Overdose symptoms of severe fever, hyperventilation, ketosis, respiratory alkalosis, coma, cardiovascular and respiratory insufficiency, severe hypoglycemia.
- Treatment: immediate hospitalization in specialized departments for emergency therapy - gastric lavage, determination of the acid-alkaline balance, alkaline and forced alkaline diuresis, hemodialysis, introduction of saline solution, activated carbon, symptomatic therapy. During the alkali diuresis is necessary to achieve a pH between 7.5 and 8. Forced alkali diuresis should be performed when the salicylate concentration in plasma is greater than 500 mg / l (3.6 mmol / l) in adults and 300 mg / l (2.2 mmol / L) in children.
With simultaneous application of acetylsalicylic acid increases the effect of these drugs:
- Methotrexate (due to reduction in renal clearance and ousting him from association with proteins);
- Heparin and indirect anticoagulants (due to platelet dysfunction and displacing anticoagulants from binding protein);
- Thrombolytic and antiplatelet and anticoagulant drugs (ticlopidine);
- Digoxin (due to the decrease of its renal excretion);
- Hypoglycemic agents for oral use (sulfonylurea derivatives) and insulin (due hypoglycemic properties of the acetylsalicylic acid in high doses and sulfonylurea derivatives of displacement due to plasma proteins);
- Valproic acid (due to displacement from its association with proteins).
- Concomitant use of aspirin with ibuprofen reduces the cardioprotective effects of acetylsalicylic acid.
- An additive effect is observed while taking aspirin and ethanol (alcohol).
- Aspirin reduces the effect of uricosuric agents (benzbromarone) due to competitive tubular elimination of uric acid.
- Leveraging the elimination of salicylates, systemic corticosteroids weaken their effect.
- Antacids and cholestyramine while applying Cardiomagnyl reduce absorption of the drug.
Pregnancy and lactation:
The use of salicylates in high doses in the I trimester of pregnancy is associated with increased frequency of malformations of the fetus. In the II trimester salicylates can be given only with the rigorous assessment of the risks and benefits. In the III trimester of pregnancy salicylates at high doses (> 300 mg / day) cause inhibition of labor, premature closure of the ductus arteriosus in the fetus, increased bleeding in the mother and fetus, and the appointment just before birth may cause intracranial hemorrhage, especially in preterm infants. Appointment of salicylates in I and III trimesters of pregnancy is contraindicated.
The available clinical data is insufficient to establish the ability or inability to use during breastfeeding. Before the appointment of acetylsalicylic acid during breastfeeding should assess the potential benefits of therapy with respect to the potential risk to the infant.
The frequency of adverse reactions listed below was determined according to the following: very common (≥1 / 10); common (> 1/100, <1/10); sometimes (> 1/1000, <1/100); rare (> 1/10 000, <1/1000); very rare (<1/10 000, including isolated reports).
- Allergic reactions: often - urticaria, angioedema; sometimes - anaphylactic reactions.
- From the digestive system: very often - heartburn; often - nausea, vomiting; sometimes - pain in the stomach area, ulceration of the mucous membrane of the stomach and duodenal ulcers, gastrointestinal bleeding; rarely - ulcer perforation of the stomach or duodenal ulcers, elevated liver enzymes; very rarely - stomatitis, esophagitis, erosive lesions of upper gastrointestinal strictures, colitis, irritable bowel syndrome.
- From respiratory system: often - bronchospasm.
- From hemopoiesis system: very often - increased bleeding; rarely - anemia; very rarely - hypoprothrombinemia, thrombocytopenia, neutropenia, aplastic anemia, eosinophilia, agranulocytosis.
- CNS: sometimes - dizziness, drowsiness; often - headache, insomnia; rarely - ringing in the ears, intracerebral hemorrhage.
Indications of use:
- Primary prevention of cardiovascular diseases such as thrombosis and acute heart failure in the presence of risk factors (eg, diabetes, hyperlipidemia, hypertension, obesity, smoking, old age);
- Prevention of recurrent myocardial infarction and thrombosis of blood vessels;
- Prevention of thromboembolic events after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty);
- Unstable angina.
- Bleeding in the brain;
- Tendency to bleeding (vitamin K deficiency, anemia, hemorrhagic diathesis);
- Asthma induced by intake of salicylates and NSAIDs;
- Erosive and ulcerative lesions GIT (exacerbation);
- Gastro-intestinal bleeding;
- Renal failure, severe stage (creatinine clearance <10 ml / min);
- Lack of glucose-6-phosphate dehydrogenase;
- Concomitant use of methotrexate (> 15 mg per week);
- I and III trimesters of pregnancy;
- Lactation (breastfeeding);
- Children and teens age under 18;
- Hypersensitivity to acetylsalicylic acid, the drug auxiliary substances and other NSAIDs.
- Precautions should be appoint a drug in gout, hyperuricemia, ulcers or gastrointestinal bleeding from the gastrointestinal tract in anamnesis, renal and / or liver failure, asthma, hay fever, nasal polyps, allergic conditions, in the II trimester of pregnancy.
- Drug should be taken after doctor prescription.
- Aspirin may provoke bronchospasm and induce asthma attacks or other hypersensitivity reactions. Risk factors include the presence of asthma in anamnesis, hay fever, nasal polyposis, chronic respiratory diseases and allergic reactions (e.g., skin reactions, pruritus, urticaria) to other drugs.
- Aspirin can cause bleeding of varying severity during and after surgery.
- A few days before the planned surgery should be assess the risk of bleeding compared to the risk of ischemic complications in patients taking low doses of acetylsalicylic acid. If the risk of bleeding is significant, taking of aspirin should be temporarily discontinued.
- The combination of aspirin with anticoagulants, thrombolytic and antiplatelet agents associated with an increased risk of bleeding.
- Acetylsalicylic acid in low doses can trigger the development of gout in susceptible individuals (with decreased excretion of uric acid).
- The combination of aspirin with methotrexate is accompanied by an increased incidence of side effects of the hemopoietic organs.
- Admission of acetylsalicylic acid in high doses has a hypoglycemic effect, it is necessary to bear in mind when assigning it to patients with diabetes receiving hypoglycemic agents for oral intake and insulin.
- At concomitant use of systemic corticosteroids and salicylates should be remembered that during treatment the concentration of salicylates in the blood is reduced, and after the abolition of systemic GCS possible overdose of salicylates.
- Not recommended combination with acetylsalicylic acid ibuprofen in patients with an increased risk of cardiovascular disease: the simultaneous use of ibuprofen observed decrease antiplatelet action of acetylsalicylic acid in doses up to 300 mg, which reduces the cardioprotective effects of acetylsalicylic acid.
- Excess of dose of acetylsalicylic acid over the recommended therapeutic dose is associated with a risk of gastrointestinal bleeding.
- With prolonged use of aspirin in low doses as an antiplatelet therapy, caution is necessary in elderly patients due to the risk of gastrointestinal bleeding.
- At the same time taking acetylsalicylic acid and ethanol increased risk of damage to the gastrointestinal mucosa and prolonged bleeding.
Effects on ability to drive vehicles and management mechanisms:
- During the period of treatment with acetylsalicylic acid, patients should be careful when driving and activities potentially hazardous activities that require high concentration and speed of psychomotor reactions.
With kidney disorders:
- Drug is contraindicated in severe renal insufficiency (creatinine clearance less than 10 ml / min); with kidney failure should be used with caution.
If abnormal liver function:
- When liver failure should be used with caution.
Application in childhood:
- Is contraindicated in children and adolescents up to 18 years.