Pharmacodynamics and pharmacokinetics
The main active ingredient is acetylsalicylic acid . Aspecard has a pronounced antipyretic, analgesic, and anti-inflammatory effect, which is achieved through inhibition of cyclooxygenases 1,2. COX1 and COX2 regulate the production of prostaglandins , which are responsible for the formation of edema and pain. A decrease in the level of prostaglandins in the thermoregulation center is manifested by increased sweating and dilation of skin vessels, which leads to a decrease in body temperature.
The analgesic effect is achieved by both peripheral and central action of the drug.
Aspecard reduces adhesion and aggregation of platelets , suppresses the production of thromboxane in them, which leads to a decrease in thrombus formation. The antiplatelet effect after a single dose of the drug lasts a week (more pronounced in men than in women). When taking the drug, the risk of developing myocardial infarction with concomitant unstable angina , and mortality is reduced. Aspecard is used for primary and secondary prevention of myocardial infarction. A daily dosage of 6 grams increases prothrombin time , suppresses the production of prothrombin in the liver, enhances the fibrinolytic activity of plasma, stimulates the excretion of uric acid by disrupting its reabsorption in the tubules of the renal system.
Pharmacological properties of the drug Aspecard
Aspecard has antithrombotic, as well as anti-inflammatory, antipyretic and analgesic effects, characteristic of acetylsalicylic acid. The mechanism of action of acetylsalicylic acid is based on the inactivation of the COX enzyme, as a result of which the synthesis of prostaglandins, prostacyclins and thromboxane is disrupted. Due to a decrease in the production of prostaglandins, their pyrogenic effect on thermoregulation centers is reduced. The sensitizing effect of prostaglandins on sensory nerve endings is reduced, which leads to a decrease in their sensitivity to pain mediators. An irreversible disruption of the synthesis of thromboxane A2 in platelets causes the antiplatelet effect of acetylsalicylic acid. Absorption of acetylsalicylic acid in the digestive tract occurs quickly and completely. The maximum level of concentration in blood plasma is reached after 10–20 minutes. The degree of binding to plasma proteins depends on the concentration and ranges from 49–70%. About 50% of acetylsalicylic acid is metabolized during the initial passage through the liver. Excreted in the form of metabolites in the urine. The half-life of salicylic acid is 20 minutes and increases with increasing dosage of the drug. Penetrates through the BBB into the CSF, synovial fluid, and breast milk.
Indications for use
Aspecard is used for rheumatoid arthritis , pericarditis , rheumatism , infectious-allergic myocarditis . Prescribed for the relief of pain ( lumbago , neuralgia , migraine , arthralgia, thoracic radicular syndrome, algodismenorrhea ), febrile syndrome.
As an antiplatelet agent, it is used for unstable angina, silent myocardial ischemia, stent installation, aortoarteritis , balloon coronary angioplasty, heart valve replacement, atrial fibrillation, pulmonary infarction , mitral valve prolapse , acute thrombophlebitis , recurrent pulmonary embolism, 's syndrome , Kawasaki disease , Takayasu .
In allergology and immunology, it is used in increasing dosages in patients with the “aspirin” triad and “aspirin” asthma.
Aspicard enteric tablets p/o 75 mg No. 10x5
Name
Aspicard.
Release forms
Pills.
INN
Acetylsalicylic acid
FTG
Non-steroidal anti-inflammatory drugs.
Description
Film-coated tablets, pink, round, with a biconvex surface.
Compound
One tablet contains: active ingredient – acetylsalicylic acid – 75 mg or 150 mg; excipients – starch 1500 (partially pregelatinized corn starch), microcrystalline cellulose, stearic acid, opadry (contains: hypromellose, triacetin, talc), acrylic (contains: methacrylic acid and ethyl acrylate copolymer (1: 1), talc, triethyl citrate, anhydrous colloidal silicon dioxide, sodium carbonate, sodium lauryl sulfate, titanium dioxide (E 171), yellow iron oxide (E 172), red iron oxide (E 172)).
Pharmacotherapeutic group
Platelet aggregation inhibitors, excluding heparin. ATX code: B01AC06.
Indications for use
- Unstable angina - as part of standard therapy. — Acute myocardial infarction – as part of standard therapy. — Prevention of recurrent myocardial infarction. — Prevention of repeated transient ischemic attack (TIA) and repeated cerebral infarction. — Prevention of thrombosis after surgery and invasive vascular interventions (for example, after coronary artery bypass grafting (CABG) or primary percutaneous coronary intervention (PCI). — Prevention of cardiovascular diseases in high-risk patients is possible only as prescribed by a doctor if the benefit from therapy exceeds the risk of adverse events, in particular bleeding, and there is the possibility of diagnosing hidden bleeding.Note: acetylsalicylic acid in a single dose of 75-150 mg is not intended for the treatment of pain.
Contraindications
- hypersensitivity to salicylic acid derivatives or cyclooxygenase inhibitors (for example, in some patients with asthma) and any of the excipients; - exacerbation or recurrent gastric ulcer and/or intestinal bleeding or other types of bleeding, such as cerebrovascular bleeding; - hemorrhagic diathesis, bleeding disorders such as hemophilia and thrombocytopenia; - severe liver or kidney failure; - doses more than 100 mg/day during the third trimester of pregnancy; - taking methotrexate in doses >15 mg/week.
Directions for use and doses
— Unstable angina: 75-150 mg 1 time per day. — Acute myocardial infarction: 75-150 mg 1 time per day. — Prevention of recurrent myocardial infarction: 300 mg 1 time per day. — Prevention of repeated transient ischemic attack (TIA) and repeated cerebral infarction: 75-150 mg 1 time per day. - Prevention of thrombosis after surgery and invasive vascular interventions (for example, after coronary artery bypass grafting (CABG) or primary percutaneous coronary intervention (PCI)): 75-150 mg 1 time per day. Antiplatelet therapy with acetylsalicylic acid is recommended to begin 24 hours after CABG or PCI surgery. — Prevention of cardiovascular diseases in patients at high risk (possible only as prescribed by a doctor, if the benefits of therapy outweigh the risk of adverse events): 75 mg 1 time per day. It is recommended to take acetylsalicylic acid once a day, before meals, with plenty of liquid. In case of acute myocardial infarction, it is recommended to chew the first tablet and drink plenty of water. Acetylsalicylic acid 75 mg (150 mg) is intended for long-term use. The duration of therapy is determined by the doctor.
Side effect
Side effects are grouped based on organ system class. In each class, frequencies are defined as: very often (≥1/10), often (from ≥1/100 to
Precautionary measures
Aspicard is not suitable for use as an anti-inflammatory, analgesic or antipyretic agent. This medication is not recommended for use in adolescents (children) under 16 years of age unless the expected benefits outweigh the potential risks. Aspicardium may be an etiological factor in Reye's syndrome in some children. There is an increased risk of bleeding, especially during or after surgery (even minor procedures such as tooth extraction). In this case, it may be necessary to temporarily stop treatment 1-2 days before surgery. Aspicard is not recommended during menorrhagia and may increase menstruation. Aspicard should be used with caution in patients with hypertension and a history of gastric or duodenal ulcers or hemorrhagic episodes, or if the patient is being treated with drugs that alter hemostasis (i.e., anticoagulants such as warfarin, thrombolytic and antiplatelet agents, anti-inflammatory drugs and selective serotonin reuptake inhibitors). Patients should report any unusual bleeding to their doctor. If gastrointestinal bleeding or ulceration occurs, treatment should be discontinued. Aspicard should be used with caution in patients with moderate renal or hepatic impairment (contraindicated in severe impairment), or in patients who are dehydrated. Aspicardium may provoke bronchospasm and asthma attacks or other hypersensitivity reactions. Risk factors: existing asthma, hay fever, nasal polyposis or exacerbation of chronic respiratory diseases, allergic reaction to other substances (skin reactions, itching or hives). Serious skin reactions, including Stevens-Johnson syndrome, have rarely been observed in association with the use of Aspicard. Use should be discontinued at the first appearance of a skin rash, mucosal lesions, or any other sign of hypersensitivity. Elderly patients are particularly sensitive to the adverse effects of NSAIDs, including acetylsalicylic acid. In case of long-term therapy, patients should be regularly monitored by a doctor. Particular attention should be paid to patients receiving concomitant medications that increase the risk of ulceration, such as oral corticosteroids, selective serotonin reuptake inhibitors and deferasirox. Aspicard in low doses reduces the excretion of uric acid; in patients with a predisposition to gout, this can provoke an attack. In case of an overdose of acetylsalicylic acid, the hypoglycemic effect of sulfonylurea and insulin may be enhanced.
Pregnancy and breastfeeding
Low doses (up to 100 mg/day): these doses, with limited use and special monitoring, are safe. Doses 100-500 mg/day and above: inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryonic/fetal development. During the first and second trimester of pregnancy, you should not take acetylsalicylic acid unless absolutely necessary. If acetylsalicylic acid is used by a woman during the first and second trimester of pregnancy, or just planning pregnancy, then the dose should be as low as possible and the duration of treatment as short as possible. During the third trimester of pregnancy, all prostaglandin synthesis inhibitors can lead to: - cardiopulmonary toxicity (premature closure of the ductus arteriosus and pulmonary hypertension) in the fetus; - renal dysfunction, which can progress to renal failure with oligohydroamnion. In mother and fetus - prolongation of bleeding time, antiaggregation effect at the end of pregnancy, even when taken in very low doses. In the mother - to suppression of uterine contractions and, as a result, delayed or protracted labor. Therefore, acetylsalicylic acid at a dose of 100 mg/day and above is contraindicated in the third trimester of pregnancy. Lactation Short-term use of the recommended dose does not require weaning the baby. In cases of prolonged use and/or administration of higher doses, breastfeeding should be discontinued.
Impact on the ability to drive vehicles and operate machinery
Aspicard does not affect the reaction and ability to drive.
Interaction with other drugs
Contraindicated combinations Methotrexate (used in doses >15 mg/week): methotrexate and acetylsalicylic acid increase the hematological toxicity of methotrexate. Not recommended combinations Drugs for removing uric acid, for example, probenecid. Combinations that require precautions for use or must be taken into account Anticoagulants, for example, coumarins, heparin, warfarin. Increased risk of bleeding. Bleeding time should be monitored. Antiplatelet agents (clopidogrel and dipyridamole) and selective serotonin reuptake inhibitors (SSRIs, such as sertraline or paroxetine): increased risk of gastrointestinal bleeding. Antidiabetics, such as sulfonylureas: acetylsalicylic acid may increase their hypoglycemic effect. Digoxin and lithium: Monitoring plasma concentrations of digoxin and lithium is recommended when initiating and stopping treatment with Aspicard. Dosage regimen adjustments may be required. Diuretics and antihypertensive drugs: NSAIDs may reduce the antihypertensive effect of diuretics and other antihypertensive drugs. When NSAIDs are co-administered with ACE inhibitors, the risk of acute renal failure increases. Diuretics: risk of acute renal failure. It is recommended to monitor the patient's fluid intake and renal function at the beginning of treatment. Carbonic anhydrase inhibitors (acetazolamide): severe acidosis and increased central nervous system toxicity. Systemic corticosteroids: Increased risk of gastrointestinal ulceration and bleeding. Methotrexate (when used in doses less than 15 mg/week): May increase the hematologic toxicity of methotrexate. Weekly blood monitoring is required during the first weeks of use. Enhanced control even with slightly impaired renal function and in the elderly. Other NSAIDs: Increased risk of ulcers and gastrointestinal bleeding due to synergistic effects. Ibuprofen: You should avoid using this combination of drugs on a regular basis. Cyclosporine, tacrolimus: may increase the nephrotoxic effects of cyclosporine and tacrolimus. Renal function should be monitored during concomitant use of these drugs and Aspicard. Valproate: Acetylsalicylic acid increases plasma concentrations of valproate at steady state. Phenytoin: The therapeutic effect of phenytoin, in general, will not be significantly altered. Alcohol: Concomitant use of alcohol and Aspicard increases the risk of gastrointestinal bleeding.
Overdose and relief measures
The toxic dose is approximately 200 mg/kg in adults and 100 mg/kg in children. The lethal dose of acetylsalicylic acid is 25-30 grams. Plasma concentrations of salicylates above 300 mg/l indicate intoxication. Plasma concentrations above 500 mg/l in adults and 300 mg/l in children usually cause severe intoxication. Overdose can be dangerous for elderly patients and especially young children. Symptoms of moderate intoxication include tinnitus, hearing loss, headache, dizziness, confusion and gastrointestinal symptoms (nausea, vomiting and abdominal pain). Symptoms of severe intoxication: severe acid-base imbalance. In addition, the following symptoms may be observed: hyperthermia and sweating, as a result of dehydration: anxiety, convulsions, hallucinations and hypoglycemia. Depression of the nervous system can lead to coma, cardiovascular failure, or respiratory arrest. Treatment of overdose: If a toxic dose is taken orally, hospitalization is not required. In case of moderate intoxication, it is necessary to try to induce vomiting. If this does not help, gastric lavage may be attempted within the first hour after taking a significant amount of the drug. Subsequently, the patient should be given activated charcoal (an adsorbent) and sodium sulfate (a laxative). Activated carbon once (50 g for an adult, 1 g/kg body weight for a child under 12 years of age). Alkalinization of urine (250 mmol NaHCO3, for three hours) is necessary under control of the urine pH level. For other symptoms, symptomatic therapy is carried out.
Package
10 tablets in a blister pack made of polyvinyl chloride film and aluminum foil. 3, 5 or 10 blister packs together with an insert sheet are placed in a cardboard pack (No. 10×3, No. 10×5, No. 10×10).
Storage conditions
In a place protected from light and moisture, at a temperature not exceeding 25°C. Keep out of the reach of children.
Best before date
2 years. Do not use after expiration date.
Conditions for dispensing from pharmacies
Over the counter.
Buy Aspicard tablet, film-coated, 75 mg in container pack No. 10x5 in the pharmacy
Price for Aspicard tablet, film-coated, 75 mg in container pack No. 10x5
Instructions for use for Aspicard tablet, film-coated, 75 mg in container pack No. 10x5
Contraindications
Aspecard is not used for hemorrhagic diathesis (telangiectasia, von Willebrand disease , hemophilia), ulcerative lesions of the digestive tract, dissecting aortic aneurysm, severe damage to the renal and hepatic systems, vitamin K deficiency, initial hypoprothrombinemia, nephrolithiasis , hyperuricemia, thrombocytopenic purpura .
Aspecard is not used during pregnancy, breastfeeding, or in pediatrics (up to 14 years).
Side effects of the drug Aspecard
from the gastrointestinal tract: abdominal pain, microhemorrhages, nausea, vomiting, diarrhea, discomfort in the epigastric region, erosive and ulcerative lesions of the stomach, gastric bleeding, liver dysfunction; from the blood system: thrombocytopenia, anemia; from the urinary system: impaired renal function; allergic reactions: skin rash, itching, urticaria; from the side of metabolism : hypoglycemia.
Side effects
Taking Aspecard may be accompanied by NSAID gastropathy, dizziness, tinnitus, leukopenia , thrombocytopenia , Reye's syndrome , bronchospasm , urticaria, aspirin-induced asthma, anemia, eosinophilic rhinitis, hyperplastic sinusitis.
Long-term use of the drug in large dosages leads to the development of prerenal azotemia, interstitial nephritis , nephrotic syndrome, papillary necrosis , aseptic meningitis , and acute renal failure.
There is an increase in the level of aminotransferases .
Overdose of the drug Aspecard, symptoms and treatment
Mild intoxication may cause nausea, vomiting, pain in the epigastric region, tinnitus, dizziness, headache, decreased visual acuity and hearing (especially in children and elderly patients). With a significant overdose, incoherent thinking, confusion, drowsiness, collapse, tremor, shortness of breath, an attack of suffocation, severe dehydration of the body (decrease in the buffer capacity of tissue fluid), hyperthermia, coma, alkaline reaction of urine, impaired core function (first respiratory alkalosis, then metabolic alkalosis) are noted. acidosis), carbohydrate metabolism disorders (decreased blood glucose levels). The lethal dose of acetylsalicylic acid for adults is more than 10 g, for children - 3 g. Depending on the state of the core and electrolyte balance, infusion solutions of sodium bicarbonate, sodium citrate or sodium lactate are administered.
Overdose
Salicylic syndrome, convulsions, stupor, coma , severe dehydration, non-cardiogenic pulmonary edema , shock, and renal failure are noted.
Treatment: taking activated carbon, laxatives, provoking vomiting, alkalizing urine, inducing diuresis , restoring blood volume. Hemodialysis may be used.
For pulmonary edema, artificial ventilation of the lungs with an oxygen mixture is recommended; for cerebral edema, osmotic diuresis and pulmonary hyperventilation .
Interaction
Aspecard reduces renal clearance, toxicity, and effectiveness of methotrexate , NSAIDs, reserpine, thrombolytics, sulfonamides , indirect anticoagulants, heparin, and oral hypoglycemic drugs.
The drug reduces the effectiveness of antihypertensive, diuretic (furosemide, spironolactone), uricouric (sulfinpyrazone, benzbromarone) drugs.
Aspecard increases the level of lithium salts, barbiturates , digoxin in the blood.
Myelotoxic drugs increase the hematotoxicity of the drug.
special instructions
When prescribing tablets for pain relief, the course of treatment should not exceed 7 days, to reduce high fever - no more than 3 days.
Before surgical treatment to prevent bleeding, the drug is discontinued 7 days before surgery.
To reduce the irritating effect of the drug on the digestive tract, it is recommended to simultaneously use drugs that reduce the acidity of gastric juice, use buffer additives, and thoroughly crush the tablets before use.
Does not mix with ethanol.
Analogs
Level 4 ATC code matches:
Persantine
Aegitromb
Plavix
Coplavix
Chime
Cardiomagnyl
Polocard
Thrombo ACC
Brilinta
Magnicor
Plagril
Dipyridamole
Clopidogrel
Lopirel
Sylt
CardiASK
Aspirin Cardio
Acecardole
Aspinat
Aspicor
Analogs are the following drugs: Akard , Anopyrin , Aspenorm , Aspirin Cardio , Acecardin , Godasal , Cardisave , Lospirin , Polocard , Reocard , Thrombo Ass , Trombogard , Ecorin .
