Lospirin

General characteristics. Structure:

Active ingredient: Acetylsalicylic acid; 1 tablet contains acetylsalicylic acid 75 mg.

Auxiliary veshchestva:tsellyuloza microcrystallic, starch prezhelatinizovanny, silicon dioxide colloid anhydrous, stearic acid, covering of Opadry Y-1-7000 white, Acryl-Eze 93018359 covering white.

Pharmacological properties:

Pharmacodynamics. Acetylsalicylic acid – renders analgeziruyushchy, febrifugal, antiinflammatory and anti-aggregation actions.
Inhibits cyclooxygenase (TsOG) and brakes a cyclooxygenase way of metabolism of arachidonic acid, blocks thromboxane synthesis. Reduction of content of A2 thromboxane in thrombocytes leads to irreversible oppression of aggregation, provides insignificant vasoconstrictive effect. Uvelivayet fibrinolitic activity of plasma also reduces concentration of vitamin-to-dependent factors of coagulation (II, VII, IX, X).
Reduces a lethality and risk of development of a myocardial infarction at unstable stenocardia. Effective at primary prevention of cardiovascular diseases, especially at men 40 years are more senior than a myocardial infarction, and at secondary prevention of a myocardial infarction. In a daily dose of 900 mg and reduces the frequency of ischemic strokes and mortality from them, the frequency of a recurrence of disturbances of cerebral circulation above at patients who had a stroke.
Reduces coagulability of blood owing to reduction of aggregation of thrombocytes due to oppression of synthesis of A2 thromboxane in them. Use of tablets, film coated, kishechnorastvorimy, reduces the frequency of side effects from a stomach.

Pharmacokinetics. After oral administration it is almost completely soaked up in a digestive tract. During absorption gives in to presistemny elimination in a wall of intestines and in a liver it (is deacetylated). Rezorbirovanny part is very quickly hydrolyzed by special esterases therefore the elimination half-life makes no more than 15-20 min. In an organism circulates (for 75-90% contacts albumine) and it is distributed in fabrics in the form of anion of salicylic acid. The maximum concentration in a blood plasma is reached in 2 hours. Serumal level of salicylates very variable. Practically does not contact proteins of a blood plasma. Biotransformation of salicylates happens preferential in a liver to formation of 4 main metabolites which are defined in many fabrics and urine. Excretion of salicylates occurs preferential by active secretion in tubules of kidneys in not changed look (60%) and in the form of metabolites. Removal of not changed salicylate depends from рН urine (when alkalifying urine ionization of salicylates increases, their reabsorption worsens and considerably excretion increases). Speed of excretion depends on a dose - at reception of small doses the elimination half-life makes 2-3 hours, and with increase in a dose can grow till 15-30 o'clock.

Indications to use:

Primary prevention of a myocardial infarction at patients with stenocardia; secondary prevention of a myocardial infarction; prevention of thromboses and embolisms, including patients with the increased risk have their emergence (after heart operations and vessels, coronary shunting); prevention of disturbances of cerebral circulation on ischemic type.

Route of administration and doses:

The drug Lospirin® is used inside, after food, washing down with enough water. At primary prevention of a myocardial infarction at patients with stenocardia; secondary prevention of a myocardial infarction should accept 75–150 mg of drug a day.
For prevention of thromboses and embolisms, including patients with the increased risk have their emergence (after heart operations and vessels, coronary shunting); prevention of disturbances of cerebral circulation on ischemic type it is necessary to accept 75–300 mg of drug a day.
It is necessary to swallow of tablets without chewing, washing down with a small amount of liquid. It is not recommended to break tablets.

Features of use:

With care appoint drug at gout, a hyperuricemia as acetylsalicylic acid reduces removal of uric acid that can provoke a bad attack of gout at patients with disturbance of exchange of uric acid.
With care appoint drug also at digestive tract pathology, a renal failure and a liver, bronchial asthma, chronic diseases of a respiratory organs, hay fever, a polypose of a mucous membrane of a nose, allergic reactions to medicines, at deficit of vitamin K and glyukozo-6-fosfatdegidrogenazy.
Drug can cause bleedings of varying severity in time and after carrying out surgical interventions therefore in 5–7 days prior to planned operation or extraction of teeth it is necessary to stop administration of drug.
Use of drug in high doses causes hypoglycemic effect that patients need to consider at its appointment with a diabetes mellitus. In case of prolonged use of drug in high doses regular hematologic control (level of hemoglobin and indicators of system of coagulation) is necessary.

Ability to influence speed of response at control of motor transport or other mechanisms.
There are no data on negative influence of acetylsalicylic acid on ability to manage motor transport or to work with other mechanisms.

Use during pregnancy or breastfeeding.
Drug is contraindicated in I and II trimesters of pregnancy; in case of need use is possible only when the expected advantage for mother exceeds potential risk for a fruit.
In need of treatment by drug it is necessary to stop feeding by a breast.

Children. Drug is contraindicated to children because of possible risk of emergence of a syndrome of Ray.

Special security measures.
At simultaneous use of acetylsalicylic acid and alcohol the risk of damage of a mucous membrane of bodies of digestive tract and lengthening of a bleeding time increases.

Side effects:

Generally Lospirin® is transferred well thanks to the low content of acetylsalicylic acid. Side effects are noted only in some cases.
- Allergic reactions: bronchospasm, skin rashes; patients have risk groups - provocation of attacks of bronchial asthma.
- From digestive organs: nausea, vomiting, diarrhea; sometimes, at prolonged use, erosion, stomach ulcer and a duodenum and gastrointestinal bleedings are possible.
- From bodies of a hemopoiesis: the thrombocytopenia, an iron deficiency anemia (connected with bleedings from digestive tract).
- From a reproductive system: lengthening of duration of periods.

Interaction with other medicines:

At simultaneous use with antacids absorption of acetylsalicylic acid from digestive tract decreases. At a combination with glucocorticosteroids removal of salicylates amplifies and the risk of gastrointestinal bleedings increases; combinations with all non-steroidal anti-inflammatory drugs are also undesirable.
At simultaneous use with acetylsalicylic acid effect of heparin and indirect anticoagulants owing to dysfunction of thrombocytes and replacement of indirect anticoagulants from communication with proteins of a blood plasma amplifies. Drug also strengthens effect of thrombolytic and anti-thrombolytic medicines (including тиклопидин).
Acetylsalicylic acid reduces action of antihypertensives, increases concentration of digoxin in a blood plasma and strengthens its effects by decrease in removal.
Acetylsalicylic acid strengthens effect of hypoglycemic drugs (insulin and derivatives of sulphonylurea) owing to gipoglikemiziruyushchy effect of acetylsalicylic acid and replacement of derivatives of sulphonylurea from communication with blood proteins.
At use with uricosuric means (benzbromarony), furosemide, Spironolactonum acetylsalicylic acid weakens their action. It is not necessary to use at the same time drug with a methotrexate as acetylsalicylic acid strengthens its action thanks to reduction of renal clearance and its replacement from communication with blood proteins.

Contraindications:

Hypersensitivity to acetylsalicylic acid and other salicylates. Digestive tract erosive cankers in an aggravation phase; hemorrhagic diathesis, thrombocytopenia, hemophilia; liver failure and oksaluriya; bronchial asthma; simultaneous treatment by anticoagulants; deficit glyukozo-6-fosfatdegidrazy. Period of pregnancy and feeding by a breast. Children's age up to 18 years.

Overdose:

The overdose is more probable at patients of advanced age.
Symptoms: nausea, vomiting, a sonitus, decrease in auditory acuity, dizziness, confusion of consciousness, fever, a hyperventilation, ketoacidosis, a respiratory alkalosis, a coma, cardiovascular and respiratory insufficiency, the expressed hypoglycemia, hemorrhages.
Treatment: hospitalization; use of absorbent carbon, a gastric lavage, definition of indicators of acid-base balance, infusional therapy, the artificial diuresis shown at concentration of salicylates in a blood plasma at adults above than 500 mg/l (in/in infusion of hydrosodium carbonate 88 мэкв in 1 l of 5% of solution of glucose with a speed of 10-15 ml/kg/h), a hemodialysis. Therapy is symptomatic.

Storage conditions:

To store in the dry, protected from light place at a temperature not over 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in strips; on 3 strips in cardboard packaging.