Lospyrin 75 mg pills number 120

Lospyrin (Acetylsalicylic acid) Instructions for use

Storage

active ingredient: acetylsalicylic acid; 1 tablet contains acetylsalicylic acid 75 mg;
Excipients: Microcrystalline cellulose, Pregelatinised starch, Silicon dioxide, Colloidal anhydrous, Stearic acid, Opadry Y-1-7000 White, Acryl-Eze 93018359 White.

Medicinal form

Tablets coated, casings soluble.

Basic physical and chemical properties.

Round biconvex tablets coated with white color.

Pharmacotherapeutic group

Antithrombotic agents. Code ATX B01A C06.

Pharmacological properties

Pharmacodynamics. Acetylsalicylic acid suppresses platelet aggregation by blocking the synthesis of thromboxane A2.The mechanism of its action is the irreversible inactivation of the enzyme cyclooxygenase (COX-1). Acetylsalicylic acid also detects other inhibitory effects on platelets.

Acetylsalicylic acid belongs to a group of nonsteroidal anti-inflammatory drugs (NSAIDs) with analgesic, antipyretic and anti-inflammatory properties.

Pharmacokinetics. After ingestion, acetylsalicylic acid is rapidly and completely absorbed from the gastrointestinal tract.During and after absorption, it becomes the main active metabolite - acid salicylum. The maximum concentration of acetylsalicylic acid in plasma is achieved after 10-20 minutes, salicylic acid - after 20-120 minutes, respectively. Due to the enteric soluble shell of Lospyrene tablets, the release of the active substance occurs not in the stomach, but in the alkaline medium of the intestine. Therefore, the absorption of acetylsalicylic acid is slowed down to 3-6 hours after the use of a capsule-coated tablet compared to a conventional tablet of acetylsalicylic acid.

Acetylsalicylic acid and salicylic acid are fully bound to plasma proteins and are rapidly distributed in the body. Salicylic acid penetrates the placenta, as well as breast milk. Salicylic acid undergoes metabolism predominantly in the liver.Metabolites of salicylic acid are salicylic acid, salicylic phenol glucuronide, salicylic acid glucuronide, gentiin acid and gentamicin acid. The kinetics of salicylic acid excretion is dose dependent, since metabolism is limited by the activity of liver enzymes. The half-life is dose-dependent and increases from 2-3 hours at low doses up to 15 hours - with the use of high doses. Salicylic acid and its metabolites are excreted mainly from the body by the kidneys.

Indication

To reduce risk:

• the lethal effect of patients with suspected acute myocardial infarction;
• morbidity and mortality of patients who have suffered myocardial infarction;
• transient ischemic attacks (TIA) and stroke in patients with TIA;
• morbidity and mortality in a stable and unstable angina;
• Myocardial infarction in patients at high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension), and those with multi-factorial risk of cardiovascular disease (hyperlipidemia, obesity, smoking, old age).

For prevention:

• thrombosis and embolism after operations on the vessels (percutaneous transluminal catheter angioplasty (RTSA), endarterectomy of the carotid artery, coronary artery bypass graft (CABG), arteriovenous shunting);
• deep vein thrombosis and embolism of the pulmonary artery after long-term immobilization (after surgical operations);
• stroke (as a secondary prevention).

Contraindication

• Hypersensitivity to acetylsalicylic acid, to other salicylates or to any component of the drug.
• Asthma, caused by the use of salicylates or substances with similar effects, especially NSAIDs, in history.
• Acute peptic ulcer.
• Hemorrhagic diathesis.
• Severe renal insufficiency.
• Hepatic insufficiency of severe degree.
• Cardiac insufficiency of severe severity.
• A combination of methotrexate at a dosage of 15 mg / week or more (see section "Interaction with other medicines and other forms of interaction").

Special safety measures

Use Lospyrin with caution in the following situations:

• Hypersensitivity to analgesic, anti-inflammatory, anti-rheumatic drugs, as well as in the presence of allergies to other substances;
• ulcers of the gastrointestinal tract, including chronic and recurrent peptic ulcer or gastrointestinal bleeding in history;
• simultaneous application of anticoagulants;
• in patients with impaired renal function or in patients with impaired cardiovascular circulation (eg renal vascular pathology, congestive heart failure, hypovolemia, extensive surgery, sepsis or severe bleeding), since acetylsalicylic acid may also increase the risk of renal dysfunction and acute renal failure ;
• in patients with severe deficiency of glucose-6-phosphate dehydrogenase, acetylsalicylic acid can cause hemolysis or hemolytic anemia. Especially in the presence of factors that may increase the risk of hemolysis, such as high doses of the drug, fever or acute infectious process;
• liver dysfunction.

Ibuprofen may reduce the inhibitory effect of acetylsalicylic acid on platelet aggregation. In case of taking Lospirin before taking ibuprofen as an analgesic, the patient should consult a physician.

Acetylsalicylic acid can cause the development of bronchospasm or bronchial asthma attack or other reactions of high sensitivity. Risk factors include asthma in history, hay fever, nasal polyposis or chronic respiratory disease, allergic reactions (eg, skin reactions, itching, urticaria) to other substances in the history.

Due to the inhibitory effect of acetylsalicylic acid on platelet aggregation, which persists for several days after ingestion, the use of drugs containing acetylsalicylic acid may increase the likelihood / increased bleeding in surgical operations (including minor surgical interventions such as tooth extraction). Therefore, 5-7 days before the planned operation or extraction of teeth should stop the use of the drug.

With the use of small doses of acetylsalicylic acid, uric acid output may decrease. This can lead to an attack of gout in patients who are prone to it. Do not use drugs containing acetylsalicylic acid in children and adolescents with acute respiratory viral infection (ARI), which is accompanied or not accompanied by an increase in body temperature without consulting a physician. In some viral diseases, especially with influenza A, influenza B and chickenpox, there is a risk of Ray syndrome, which is a very rare, but life-threatening illness requiring urgent medical intervention. The risk may be increased if acetylsalicylic acid is used as an adjunct drug, but the cause-effect relationship in this case is not proven. If these conditions are accompanied by constant vomiting, this may be a manifestation of Ray's syndrome. At simultaneous application of acetylsalicylic acid and alcohol, the risk of lesions of the mucous membrane of the gastrointestinal tract and the prolongation of bleeding time increases.

The use of the drug in high doses causes a hypoglycemic effect, which should be taken into account when appointing it to patients with diabetes mellitus. Regular hematological control (hemoglobin and coagulation parameters) is required for long-term use of the dasg in high doses.

Interaction with other drugs and other types of interactions

Contraindications for simultaneous use. The use of acetylsalicylic acid and methotrexate at doses of 15 mg / week and more increases the hematologic toxicity of methotrexate (reduced renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate by salicylates in connection with plasma protein proteins).

Combinations to be used with caution. In the use of acetylsalicylic acid and methotrexate in doses less than 15 mg / week, hematological toxicity of methotrexate is increased (reduction of renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate by salicylates in connection with blood plasma proteins).

The simultaneous use of acetylsalicylic acid with ibuprofen prevents irreversible platelet inhibition by acetylsalicylic acid.Treatment with ibuprofen in patients at risk for cardiovascular disease may limit the cardioprotective effect of acetylsalicylic acid.

When co-administration of Lospyrin and anticoagulants, thrombolytics / other platelet aggregation inhibitors / hemostasis increases the risk of bleeding. At the simultaneous application of high doses of salicylates with NSAIDs (due to the mutually exerting effect), the risk of ulceration and gastro-intestinal bleeding increases.

When applied with selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases as a result of a possible synergistic effect.

When co-administered with digoxin, the concentration of the latter in plasma is increased due to a decrease in renal excretion. When simultaneous use of high doses of acetylsalicylic acid and antidiabetic drugs from the group of sulfonylureas derivatives, the hypoglycemic effect of the latter is exacerbated by the displacement of sulfonylureas bound to blood plasma proteins, acetylsalicylic acid.

Diuretic agents in combination with high doses of acetylsalicylic acid reduce glomerular filtration by reducing the synthesis of prostaglandins in the kidneys. Systemic glucocorticosteroids (excluding hydrocortisone, used for substitution therapy in Addison's disease) reduce the level of salicylates in the blood and increase the risk of overdose after treatment.

Angiotensin converting enzymes (ACEs) in combination with high doses of acetylsalicylic acid cause a decrease in filtration in the glomeruli as a result of inhibiting the vasodilator effect of prostaglandins and reducing the antihypertensive effect.

When used simultaneously with valproic acid, acetylsalicylic acid displaces it from the plasma proteins, increasing the toxicity of the latter.

Alcohol contributes to damage to the mucous membrane of the gastrointestinal tract and prolongs bleeding time due to the synergism of acetylsalicylic acid and alcohol.

Simultaneous administration with uricosuric drugs, such as benzobarbanorone, probenecid, reduces the effect of uric acid excretion (as a result of competition with the removal of uric acid by the renal tubules).

Application features

Use during pregnancy or breastfeeding . The inhibition of prostaglandin synthesis may adversely affect pregnancy and / or embryo / fetal development. Available data from epidemiological studies indicate the risk of miscarriage and fetal malformations after the use of prostaglandin synthesis inhibitors at the beginning of pregnancy. The risk increases depending on the increase in dose and duration of therapy. According to available data, the association between acetylsalicylic acid and increased risk of miscarriage has not been confirmed.

Available epidemiological data on developmental malformations are not consistent, but the increased risk of gastroschisis can not be excluded in the use of acetylsalicylic acid. The results of a prospective early-pregnancy study (1-4 month) involving approximately 14,800 female-child pairs did not indicate any association with the increased risk of malformations.

Animal studies indicate reproductive toxicity. During the 1st and 2nd trimester of pregnancy, acetylsalicylic acid preparations should not be prescribed without a clear clinical need. In women who are likely to be pregnant or during the 1st and 2nd trimester of pregnancy, the dose of acetylsalicylic acid should be as low as possible and the duration of treatment as short as possible.

During the third trimester of pregnancy, all inhibitors of prostaglandin synthesis can affect the fetus as follows:

• cardio-pulmonary toxicity (with premature closure of arterial duct and pulmonary hypertension);
• renal dysfunction with possible subsequent development of renal failure with oligohydroamniosis;
• on the woman and the child at the end of pregnancy the inhibitors of prostaglandin synthesis can be influenced as follows:

1. the possibility of prolonging bleeding time, an anti-aggregate effect that may occur even after very low doses;
2. inhibition of uterine contractions, which can lead to delay or prolongation of the duration of labor.

In view of this, acetylsalicylic acid is contraindicated during the third trimester of pregnancy. Salicylas and their metabolites penetrate breast milk in small quantities.

Since no harmful effects of the drug on the child were detected after it was received by women, interrupting breastfeeding is usually not required. However, in case of regular use or when using high doses, breastfeeding should be stopped at an early stage.

Ability to influence the reaction speed when driving or working with other mechanisms.

There was no impact on the ability to drive a car and other mechanisms.

Method of administration and dose

The drug is taken internally, 30-60 minutes before eating, without chewing, drinking enough fluids.

To reduce the risk of death in patients with suspected acute myocardial infarction, use a drug at a dose of 75-300 mg per day. Within 30 days after the heart attack, continue to take a maintenance dose of 75-300 mg per day. After 30 days, consideration should be given to further prevention of recurrence of myocardial infarction.

To reduce the risk of morbidity and mortality in patients who have had myocardial infarction, use 75-300 mg per day.

For secondary prevention of stroke, use a drug at a dose of 75-300 mg per day.

To reduce the risk of TIA and stroke in patients with TIA, use 75-300 mg per day.

To reduce the risk of developing the disease and the lethal effect in patients with stable and unstable angina: 75-300 mg per day.

To prevent thromboembolism after surgery on the vessels (percutaneous translyuminal aneuplasty catheter (RTSA), endarterectomy of the carotid artery, coronary artery bypass graft (CABG), arteriovenous shunting), use the drug at a dose of 75-150 mg per day or 300 mg daily in a day.

For prophylaxis of deep vein thrombosis and pulmonary embolism after long-term immobilization (after surgical operations) - 75-150 mg per day or 300 mg per day in a day.

To prevent myocardial infarction in patients at high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension) and individuals with multi-factorial risk of cardiovascular disease (hyperlipidemia, obesity, smoking, old age), use 75 mg per day or 300 mg per day after day

Children.

According to the indications (see section "Indications"), the drug Lospyrin should not be used by children.

The use of acetylsalicylic acid in children under the age of 16 years can cause serious side effects (including Ray syndrome, one of the symptoms of which is persistent vomiting). Please read the information provided in the section "Special Safety Precautions".

Overdose

The toxic effect of salicylates is possible due to chronic intoxication resulting from prolonged therapy (the use of more than 100 mg / kg / day for more than 2 days may cause toxic effects) due to acute intoxication which is life-threatening (overdose), and the cause of which may be, for example , accidental use by children or unforeseen overdose. Chronic poisoning with salicylates may have a latent character, since signs and symptoms are nonspecific. Moderate chronic intoxication, caused by salicylates, or salicillosis occurs, usually only after repeated doses of large doses.

Symptoms Dizziness, vertigo, ringing in the ears, deafness, increased sweating, nausea and vomiting, headache, confusion of consciousness. These symptoms can be controlled by lowering the dose. The ringing in the ears can occur when the concentration of salicylates in the blood plasma is higher than 150-300 μg / ml. Serious side-effects occur at concentrations of salicylates in plasma above 300 μg / ml.

Acute intoxication is indicated by a pronounced change in the acid-base balance, which may vary depending on the age and severity of intoxication. The most common manifestation in children is metabolic acidosis. The severity of the condition can not be assessed solely on the basis of the concentration of salicylates in the blood plasma. Absorption of aspirin may slow down due to the delay gastric release, formation of concretions in the stomach or in the case of the drug in the form of tablets, coated enteric-soluble shell.

Treatment. Treatment of acute intoxication caused by an overdose of aspirin determined severity, clinical symptoms and provides standard methods used for poisoning. All measures should be used to strengthen drug removal and recovery of electrolyte and acid-base balance.

Because of the complex pathophysiological effects of salicylates poisoning signs and symptoms / test results may include:

Manifestations and symptoms	results of tests	Therapeutic measures
Intoxication mild or moderate		Gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis
Tachypnea, hyperventilation, respiratory alkalosis	Alkalaemia, alkaluriya	Restoration of electrolyte and acid-base balance
Diaforez (sweating)
Nausea, vomiting
Intoxication medium or severe		Gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis, hemodialysis in severe cases
Respiratory alkalosis with compensatory metabolic acidosis	Acidemia, atsyduriya	Restoration of electrolyte and acid-base balance
hyperpyrexia		Restoration of electrolyte and acid-base balance
Respiratory: hyperventilation, non-cardiogenic pulmonary edema, respiratory failure, asphyxia
Cardiovascular: dyzarytmiyi, hypotension, cardiovascular failure	For example, changes in blood pressure, ECG
The loss of fluids and electrolytes, dehydration, oliguria, renal failure	For example, hypokalemia, hypernatremia, hyponatremia, changes in renal function	Restoration of electrolyte and acid-base balance
Metabolism of glucose, ketoacidosis	Hyperglycemia, hypoglycemia (especially in children). Elevated levels of ketone bodies
Tinnitus, deafness
Gastro-intestinal: bleeding in the gastrointestinal tract
Hematologic: inhibition of platelets, coagulopathy	For example, extension PT, gipoprotrombinemii
Neurologic: Toxic encephalopathy and CNS depression with symptoms such as lethargy, confusion, coma and convulsions

Adverse reactions

From the digestive system: dyspepsia, epigastric pain, abdominal pain, nausea, vomiting, diarrhea, heartburn, anorexia, inflammation of the gastrointestinal tract, erosive and ulcerative lesions of the gastrointestinal tract, which can in rare cases cause gastrointestinal hemorrhage and perforation of relevant laboratory parameters and clinical manifestations.

From the circulatory system: bleeding (intraoperative hemorrhage, bruising, bleeding of the urinary system, nosebleeds, bleeding gums, hemorrhages of the gastrointestinal tract, bleeding in the brain (especially in patients with uncontrolled hypertension and / or during concomitant use of anticoagulants) with relevant clinical symptoms, including fatigue, pale skin, hypoperfusion.

Blood system: thrombocytopenia, anemia (posthemorrhagic / iron) with relevant laboratory parameters and clinical manifestations; hemolysis and hemolytic anemia (patients with severe deficiency of glucose-6-phosphate-dehydrogenase).

Immune System: hypersensitivity reactions with respective laboratory and clinical signs including asthmatic condition, skin reactions mild or moderate, as well as the respiratory system, gastrointestinal tract and cardiovascular system, including symptoms such as rash, nettle ' Janko, swelling, itching, rhinitis, nasal congestion, cardio-respiratory failure and rarely - severe reactions, including anaphylaxis.

On the part of the urinary tract, renal dysfunction, acute renal failure.

Nervous system: headache, dizziness, disorientation.

From the hearing: hearing loss, tinnitus (tynitus).

Liver and biliary tract: transient liver failure, liver transaminase elevations.

Metabolic disorders: hyperuricemia relevant laboratory parameters and clinical manifestations (gout attack).

Expiration date

4 years.

Storage conditions

Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Packaging

10 tablets in a strip; 3 or 10 strips in a cardboard box. 30 tablets in a strip; 1 or 4 strips in a cardboard box.

Category of departure

No prescription.