Cardisave 75 mg tablets # 50
Author Ольга Кияница
|Amount in a package||50|
|Manufacturer||Farmak OJSC (Ukraine, Kiev)|
|The main medicament||-|
Acetylsalicylic Acid instructions for use
active ingredient: acetylsalicylic acid; 1 tablet contains acetylsalicylic acid in terms of 100% dry matter 75 mg;
auxiliary substances: magnesium hydroxide, pregelatinized starch, microcrystalline cellulose (200), silicon dioxide colloidal anhydrous, magnesium stearate; film shell: Opadry II 85G18490 white (polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide (E 171), lecithin).
Basic physical and chemical properties
Round tablets with a biconvex surface, film-coated, white or almost white.
Antithrombotic agents. Code ATX B01A C06.
Acetylsalicylic acid is an analgesic, anti-inflammatory, antipyretic and antiplatelet agent.
The main pharmacological effect is the inhibition of the formation of prostaglandins and thromboxanes.
The analgesic effect is an additional effect, which is caused by the inhibition of the cyclooxygenase enzyme. The anti-inflammatory effect is associated with reduced blood flow caused by inhibition of PGE2 synthesis.
Acetylsalicylic acid irreversibly inhibits the synthesis of prostaglandins G / H, its effect on prostaglandins lasts longer than acetylsalicylic acid is in the body. The effect of acetylsalicylic acid on the biosynthesis of thromboxane in platelets and at the time of bleeding continues for a long time after discontinuation of treatment. The action stops only after the appearance of new platelets in the plasma.
Magnesium hydroxide has an antacid effect and protects the mucosa of the digestive tract from the irritating effect of acetylsalicylic acid.
Absorption. After ingestion, acetylsalicylic acid is rapidly absorbed from the digestive tract. Absorption rate decreases with food intake and in patients with migraine attacks, increases in patients with achlorhydria or in patients who take polysorbates or antacids. The maximum concentration in the blood serum is achieved after 0.5-2 hours.
When administered orally, magnesium is slowly absorbed from the small intestine in small amounts.
Distribution. The binding of acetylsalicylic acid to plasma proteins is 80-90%. The volume of distribution in adults is 170 ml / kg of body weight. Salicylates strongly bind to plasma proteins and rapidly spread throughout the body. Salicylates penetrate the breast milk and can penetrate the placental barrier. Magnesium is distributed with proteins in a bound form (approximately 25-30%). A small amount is excreted in breast milk. Magnesium can penetrate the placental barrier.
Metabolism. Acetylsalicylic acid is hydrolyzed to the active metabolite - salicylate - in the wall of the stomach. After absorption, acetylsalicylic acid quickly turns into salicylic acid, but within the first 20 minutes after ingestion it is the dominant one in the plasma.
Excretion. Salicylate is excreted mainly due to hepatic metabolism. Half-life is 2-3 hours. At a high dose of acetylsalicylic acid, the elimination half-life increases to 15-30 hours. Salicylate is also excreted unchanged in urine. The withdrawn volume depends on the level of the dose and the pH of the urine. Approximately 30% of the dose is excreted in the urine, if the urine reaction is alkaline, and only 2% - if acidic. A small amount of magnesium is excreted in the urine, but most are reabsorbed and excreted with feces.
- Acute (unstable angina, acute myocardial infarction) and chronic ischemic heart disease.
- Prevention of repeated thrombosis.
- Primary prophylaxis of thrombosis, cardiovascular diseases such as acute coronary syndrome in patients older than 50 years who have cardiovascular disease development factors: hypertension, hypercholesterolemia, diabetes mellitus, obesity (body mass index ˃30), hereditary anamnesis ( myocardial infarction at least one of the parents or a brother or sister under the age of 55 years).
Hypersensitivity to the components of the drug, other salicylates; stomach ulcer in the phase of exacerbation; tendency to bleeding (vitamin K deficiency, thrombocytopenia, hemophilia); hepatic failure of severe degree, severe renal dysfunction (glomerular filtration rate <10 ml / min); severe heart failure; asthma, Quincke's edema, caused by the use of salicylates or non-steroidal anti-inflammatory drugs (NSAIDs), in the anamnesis.
Interaction with other drugs and other interactions
Contraindications for simultaneous use.
Methotrexate. The use of acetylsalicylic acid and methotrexate at doses of 15 mg / week or more increases the hematological toxicity of methotrexate (decreased renal clearance of methotrexate by anti-inflammatory agents and the displacement of methotrexate from salicylates due to plasma proteins).
ACE inhibitors. Angiotensin converting enzyme (ACE) inhibitors in combination with high doses of acetylsalicylic acid cause a decrease in glomerular filtration due to inhibition of the prostaglandin vasodilator effect and reduction of the antihypertensive effect.
Acetazolamide. A possible increase in the concentration of acetazolamide can lead to the penetration of salicylates from the blood plasma into the tissue and cause toxicity of acetazolamide (fatigue, lethargy, drowsiness, confusion, hyperchloremic metabolic acidosis) and salicylate toxicity (vomiting, tachycardia, hyperpnoea, confusion).
Probenecid, sulfinpyrazone. When using probenecid and high doses of salicylates (˃500 mg), the metabolism of both drugs is inhibited, and excretion of uric acid can also decrease.
Combinations that must be used with caution.
Methotrexate. When using acetylsalicylic acid and methotrexate in doses less than 15 mg / week, hematological toxicity of methotrexate (reduction of renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from salicylates from plasma proteins) is increased.
Clopidogrel, ticlopidine. The combined use of clopidogrel and acetylsalicylic acid has a synergistic effect. This combined use is carried out with caution, as this increases the risk of bleeding.
Anticoagulants (warfarin, fenprokumon). It is possible to reduce the production of thrombin, resulting in an indirect effect on the decrease in platelet activity (a vitamin K antagonist) and the risk of bleeding increases.
Abciximab, tirofiban, eptifibatid. Possible inhibition of glycoprotein IIb / IIIa receptors on platelets, which leads to an increased risk of bleeding.
Heparin. Possible reduction in thrombin production, resulting in an indirect effect on the decrease in platelet activity, which leads to an increased risk of bleeding.
If two or more of the above substances are used together with acetylsalicylic acid, this can lead to a synergistic effect of enhancing the inhibition of platelet activity and, as a result, enhancement of hemorrhagic diathesis.
NSAIDs and COX-2 inhibitors (celecoxib). Joint application increases the risk of gastrointestinal disorders, which can lead to gastrointestinal bleeding.
Ibuprofen. Simultaneous use of ibuprofen inhibits irreversible platelet aggregation due to the action of acetylsalicylic acid. Treatment with ibuprofen patients with an increased risk of cardiovascular effects may limit the cardioprotective effect of acetylsalicylic acid. Patients who take acetylsalicylic acid once a day to prevent cardiovascular disease and from time to time take ibuprofen should take acetylsalicylic acid at least 2 hours before taking ibuprofen.
Furosemide. Possible inhibition of proximal tubular elimination of furosemide, which leads to a decrease in the diuretic effect of furosemide.
Quinidine. Perhaps an additive effect on platelets, which leads to an increase in the duration of bleeding.
Spironolactone. A modified effect of renin is possible, which leads to a decrease in the effectiveness of spironolactone.
Selective serotonin reuptake inhibitors. Joint application increases the risk of gastrointestinal disorders, which can lead to gastrointestinal bleeding.
Valproate. With simultaneous use with valproate, acetylsalicylic acid displaces it from its association with plasma proteins, increasing the toxicity of the latter (central nervous system depression, gastrointestinal disorders).
Systemic glucocorticosteroids (excluding hydrocortisone, which is used for replacement therapy in Addison's disease) reduce the level of salicylates in the blood and increase the risk of overdose after the end of treatment.
Antidiabetic drugs. Simultaneous use of acetylsalicylic acid and antidiabetic drugs increases the risk of hypoglycemia.
Antacids. It is possible to increase renal clearance and reduce renal absorption (due to increased urine pH), which leads to a decrease in the effect of acetylsalicylic acid.
Vaccine against varicella. Joint application increases the risk of developing Ray's syndrome.
Ginkgo biloba. A joint application with ginkgo biloba interferes with the aggregation of platelets, which leads to an increased risk of bleeding.
Digoxin. With simultaneous use with digoxin, the concentration of the latter in the blood plasma increases due to a decrease in renal excretion.
Alcohol contributes to damage to the mucous membrane of the gastrointestinal tract and prolongs the time of bleeding due to synergism of acetylsalicylic acid and alcohol.
The drug Cardisave is used with caution in the following cases:
- hypersensitivity to analgesic, anti-inflammatory, anti-rheumatic drugs, as well as allergy to other substances;
- gastrointestinal ulcers, including chronic and recurrent ulcerative diseases or gastrointestinal hemorrhages in the anamnesis;
- simultaneous use of anticoagulants;
- patients with impaired renal function or with impaired cardiovascular circulation (eg, kidney vascular pathology, congestive heart failure, hypovolemia, extensive surgery, sepsis, or severe bleeding), as acetylsalicylic acid also increases the risk of impaired kidney function and acute renal failure;
- patients with severe glucose-6-phosphate dehydrogenase deficiency, since acetylsalicylic acid can cause hemolysis or hemolytic anemia, especially in the presence of risk factors (eg, high doses, fever or acute infectious process);
- violations of the liver.
Ibuprofen can reduce the inhibitory effect of acetylsalicylic acid against platelet aggregation. In the case of Cardisave preparation, the patient should consult a physician before taking ibuprofen as an anesthetic.
Acetylsalicylic acid can cause the development of bronchospasm or an attack of bronchial asthma or other reactions of hypersensitivity. Risk factors include history of asthma, hay fever, nasal polyposis or chronic respiratory disease, allergic reactions (eg, skin reactions, pruritus, urticaria) to other substances in the anamnesis.
Because of the inhibitory effect of acetylsalicylic acid on platelet aggregation, which persists for several days after ingestion, the use of drugs containing acetylsalicylic acid increases the risk of bleeding in surgical operations (including minor surgical interventions, such as tooth extraction).
With the use of small doses of acetylsalicylic acid, the excretion of uric acid may decrease. This can lead to a fit of gout in patients prone to it.
Do not use drugs that contain acetylsalicylic acid, children and adolescents with acute respiratory viral infection (ARVI), which is accompanied or not accompanied by an increase in body temperature, without consulting a doctor. With some viral diseases, especially with influenza A, influenza B and chicken pox, there is a risk of developing Ray's syndrome, a very rare but life-threatening disease that requires urgent medical intervention. The risk may be increased if acetylsalicylic acid is used as a concomitant drug, but the cause-and-effect relationship is not proven in this case. If these conditions are accompanied by constant vomiting, this may be a manifestation of Ray's syndrome.
Use during pregnancy or lactation
The decision to use Cardidesave in the I-II trimester of pregnancy and during lactation should be taken after a thorough assessment of the benefit / risk ratio. The drug in such cases used in the lowest possible doses (up to 100 mg per day) and under close supervision. The period of application is as short as possible.
The drug is contraindicated in the third trimester of pregnancy.
The ability to influence the reaction rate when driving vehicles or other mechanisms
Does not affect.
Dosing and Administration
Acute and chronic ischemic heart disease.
The recommended initial dose is 150 mg per day. The maintenance dose is 75 mg per day.
Acute myocardial infarction. Unstable angina.
The recommended dose is 150-450 mg, used as soon as possible after the onset of symptoms.
Prevention of repeated thrombosis.
The recommended initial dose is 150 mg per day. The maintenance dose is 75 mg per day.
Primary prophylaxis of thrombosis, cardiovascular diseases, such as acute coronary syndrome in patients who have cardiovascular disease development factors.
The recommended preventive dose is 75 mg per day.
Tablets are swallowed whole, if necessary, washed down with water. If desired, the tablet can be broken in half, chewed or pre-grated.
The doctor determines the course of treatment individually, depending on the indications and severity of the disease.
The drug should not be used in children.
A dangerous dose for adults is 150 mg / kg body weight.
Symptoms of chronic moderate poisoning (the result of prolonged use of high doses of the drug): dizziness, ringing in the ears, deafness, vasodilation, excessive sweating, nausea, vomiting, headache, blurred consciousness.
Symptoms of severe and acute poisoning (due to an overdose): hyperventilation of the lungs, fever, anxiety, ketosis, respiratory alkalosis and metabolic acidosis.
In case of severe poisoning, central nervous system depression can lead to coma, cardiovascular collapse and respiratory arrest.
Acute poisoning with acetylsalicylic acid (> 300 mg / kg) often causes acute hepatic impairment, and a dose of more than 500 mg / kg can be fatal.
Treatment. In case of acute overdosage, it is necessary to wash the stomach and take activated charcoal.
It is necessary to restore the balance of fluid and electrolytes to avoid acidosis, hyperpyrexia, hyperkalemia and dehydration. Effective methods of removing salicylate from the blood plasma is alkaline diuresis, hemodialysis or hemoperfusion.
Undesirable effects on the incidence rate are classified into these categories: very often (> 1/10); often (> 1/100, <1/10);infrequently (> 1/1000, <1/100), rarely (> 1/10000, <1/1000), very rarely (<1/10000, including isolated cases).
Violations of the blood and lymphatic system.
Very often: increased bleeding, inhibition of platelet aggregation.
Infrequently: latent bleeding.
Rarely: anemia in case of prolonged therapy.
Very rarely: hypoprothrombinemia (high doses), thrombocytopenia, neutropenia, aplastic anemia, eosinophilia, agranulocytosis.
Impaired immune system.
Infrequently: anaphylactic reactions, allergic rhinitis.
Disorders from the endocrine system.
Violations from the nervous system.
Often: headache, insomnia.
Infrequently: dizziness (vertigo), drowsiness.
Rarely: intracerebral hemorrhage.
Disorders from the senses.
Infrequent: ringing in the ears.
Rarely: dose-dependent reversible hearing loss and deafness.
Disturbances from the respiratory system.
Often: bronchospasm (in patients with asthma).
Disorders from the digestive tract.
Very often: heartburn, reflux.
Often: erosive lesions of the upper part of the digestive tract, nausea, indigestion, vomiting, diarrhea.
Infrequently: ulcers of the upper part of the digestive tract, including vomiting with blood and tarry stools.
Rarely: gastrointestinal bleeding, perforation.
Very rare: stomatitis, esophagitis, toxic damage to the ulcers of the lower digestive tract, strictures, colitis, exacerbation of irritable bowel syndrome.
Violations by the liver.
Rare: increase in transaminases and alkaline phosphatase, serum.
Very rare: acute hepatitis oboratimy dose-dependent moderate.
Violations of the skin.
Common: urticaria, rash of various kinds, angioedema, purpura, hemorrhagic vasculitis, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.
2 years. Do not use the product after the expiration date printed on the package.
Stored in original package at a temperature not higher than 25 ° C. Keep out of the reach of children.
10 tablets in a blister pack. 3 or 5 blisters in a pack.
Category of leave
Without a prescription - 30 pills.
Prescription - 50 pills.