ASPIL [Acetylsalicylic acid] 100 mg Tablets
instructions for the medical use of
the medicinal product
ASPIL
Tradename:
Aspil, Аспил
International
non-proprietary name or generic name:
Acetylsalicylic acid, Ацетилсалициловая кислота
Dosage form: enteric-coated tablets.
Composition
Each tablet contains:
active substance: acetylsalicylic acid 100 mg;
excipients: Starch, pregelatinized starch,
talc, tartaric acid, sodium starch glycolate, purified water.
Pharmacotherapeutic group: Antiplatelet agent.
Code АТХ: В01АС06
Pharmacological properties
Pharmacodynamics
The
mechanism of antiplatelet action of acetylsalicylic acid (ASA) is based on
irreversible inhibition of cyclooxygenase (COX-1), which blocks the synthesis
of thromboxane A2 and suppresses platelet aggregation. The antiplatelet effect
develops even after the use of small doses of the drug and lasts for 7 days
after a single dose. It is believed that ASA also has other mechanisms for
suppressing platelet aggregation. In high doses, ASA (over 300 mg/day) also has
anti-inflammatory, antipyretic and analgesic effects.
Pharmacokinetics
After oral
administration, ASA is rapidly and completely absorbed from the
gastrointestinal tract (GIT). ASA is partially metabolized during absorption.
During and after absorption, ASA is converted into the main metabolite,
salicylic acid, which is metabolized mainly in the liver under the influence of
enzymes to form metabolites such as phenyl salicylate, salicylic acid
glucuronide, and salicyluric acid, which are found in many tissues and in
urine. In women, the metabolism process is slower (lower enzyme activity in the
blood serum).
The
maximum concentration of ASA in the blood plasma is achieved 10-20 minutes
after oral administration, salicylic acid - after 0.3-2 hours.
Due to the
fact that the tablets are coated with an acid-resistant coating, ASA is released
not in the stomach (the coating effectively blocks the dissolution of the drug
in the stomach), but in the alkaline environment of the duodenum. Thus, the
absorption of ASA in the form of enteric-coated tablets is delayed by 3-6 hours
compared to conventional (non-coated) tablets.
ASA and
salicylic acid bind to plasma proteins (from 66% to 98% depending on the dose)
and are quickly distributed in the body. Salicylic acid penetrates the placenta
and into breast milk.
The
excretion of salicylic acid is dose-dependent, since its metabolism is limited
by the capabilities of the enzymatic system. The half-life is from 2-3 hours
when using ASA in low doses and up to 15 hours when using the drug in high
doses (usual doses of acetylsalicylic acid as an analgesic). Unlike other
salicylates, with repeated administration of the drug, non-hydrolyzed ASA does
not accumulate in the blood serum. Salicylic acid and its metabolites are
excreted by the kidneys. In patients with normal renal function, 80-100% of a
single dose of the drug is excreted by the kidneys within 24-72 hours.
Indications for use
- prevention of
acute myocardial infarction in the presence of risk factors (e.g. diabetes
mellitus, hyperlipidemia, arterial hypertension, obesity, smoking, old age) and
recurrent myocardial infarction;
- unstable
angina;
- prevention of
ischemic stroke (including in patients with transient ischemic attack);
- prevention of
thromboembolism after surgery and invasive interventions on vessels (e.g.
coronary artery bypass grafting, carotid endarterectomy, arteriovenous bypass
grafting, coronary artery angioplasty and stenting, carotid angioplasty);
- prevention of
deep vein thrombosis and pulmonary embolism of the artery and its branches
(including during prolonged immobilization as a result of extensive surgery).
Contraindications
Hypersensitivity
to ASA, erosive and ulcerative gastrointestinal tract lesions (in the acute
phase), gastrointestinal bleeding, hemorrhagic diathesis, bronchial asthma
induced by taking salicylates, complete or incomplete combination of bronchial
asthma, recurrent nasal polyposis and paranasal sinuses and ASA intolerance,
severe renal failure (creatinine clearance (CC) less than 30 ml / min), severe
liver failure (class B and C on the Child-Pugh scale), chronic heart failure
(III-IV functional class according to the NYHA classification), concomitant
administration of methotrexate at a dose of 15 mg / week or more, pregnancy,
lactation, childhood under 18 years.
Method of administration
and dosage
Take before
meals with plenty of liquid, once a day. The duration of therapy is determined
by the doctor.
Prevention of suspected acute myocardial infarction: 100 mg daily or 300 mg every other day (the first tablet should be chewed
for faster absorption).
Prevention of first-time acute myocardial infarction in the presence of
risk factors: 100 mg daily or 300 mg every other
day.
Prevention of recurrent myocardial infarction and unstable angina: 100-300 mg daily.
Prevention of ischemic stroke and transient ischemic attack: 100-300 mg daily.
Prevention of thromboembolism after surgery and invasive vascular
interventions: 100-300 mg daily.
Prevention of deep vein thrombosis and pulmonary embolism of the artery
and its branches: 100 mg daily or 300 mg
every other day.
From the digestive system: nausea, heartburn,
vomiting, abdominal pain; ulcers of the gastric mucosa and duodenum; perforated
ulcers of the stomach and duodenum, gastrointestinal bleeding, transient liver
dysfunction with increased activity of "liver" transaminases.
From the hematopoietic
system: risk
of bleeding due to the inhibitory effect of ASA on platelet aggregation,
anemia.
Allergic reactions: skin rash, skin itching,
urticaria, Quincke's edema, rhinitis, swelling of the nasal mucosa,
cardiorespiratory distress syndrome, as well as severe reactions, including
anaphylactic shock.
From the respiratory
system: bronchospasm.
From the central nervous
system: dizziness,
hearing loss, headache, tinnitus.
If any of the side effects
listed in the instructions get worse, or you notice any other side effects not
listed in the instructions, tell your doctor.
Special instructions and precautions
Before using the drug, consult a doctor.
Taking the drug may cause gastrointestinal
bleeding and exacerbation of gastric ulcer or duodenal ulcer, the risk of
adverse effects increases in patients with impaired renal and hepatic function.
Acetylsalicylic acid can cause an asthma attack in patients with bronchial
asthma.
Long-term use of acetylsalicylic acid in doses
greater than 1000 mg / day can cause the development of iron deficiency anemia
and nephrotoxic effects.
It should be used with caution in patients with a
history of hemostasis disorders, thrombocytopenia, dysmenorrhea, chronic heart
failure and arterial hypertension, glucose-6-phosphate dehydrogenase
deficiency, with the simultaneous use of other antithrombotic agents, as well
as in women using intrauterine contraceptives.
Acetylsalicylic acid should be discontinued 5 - 7
days before planned surgery. It is recommended to stop taking salicylates 24-48
hours before pulse therapy with methotrexate.
During treatment with acetylsalicylic acid,
alcoholic beverages should not be consumed, since this increases the risk of
undesirable effects from the gastrointestinal tract.
In patients over 65 years of age, acetylsalicylic
acid should be used in lower doses and at longer intervals. The use of
acetylsalicylic acid in children under 15 years of age against the background
of hyperthermia in cases of viral infections can cause the development of
Reye's syndrome.
Take with caution in gout, hyperuricemia, since
ASA in low doses reduces the excretion of uric acid; it should be borne in mind
that ASA in low doses can provoke the development of gout in predisposed
patients (with reduced excretion of uric acid); gastric ulcer and duodenal
ulcer or gastrointestinal bleeding (in history); liver dysfunction (Child-Pugh
class A); renal dysfunction (CC more than 30 ml/min); bronchial asthma, chronic
respiratory diseases, hay fever, nasal polyposis, drug allergy; concomitant administration
of methotrexate at a dose of less than 15 mg/week; concomitant therapy with
anticoagulants, pregnancy (II trimester); in case of expected surgical
intervention (including minor ones, such as tooth extraction), since ASA can
cause a tendency to develop bleeding within a few days after taking the drug.
Interaction with other medicinal products
When used simultaneously, ASA enhances the effect of the following
drugs:
- methotrexate due to decreased renal clearance and its displacement
from plasma protein binding; also, the combination of acetylsalicylic acid with
methotrexate is accompanied by an increased incidence of side effects from the
hematopoietic organs;
- heparin and indirect anticoagulants due to impaired platelet function
and displacement of indirect anticoagulants from plasma protein binding;
- thrombolytic agents and antiplatelet agents;
- digoxin due to decreased renal excretion;
- hypoglycemic agents (insulin and sulfonylurea derivatives) due to the
hypoglycemic properties of acetylsalicylic acid itself in high doses and
displacement of sulfonylurea derivatives from plasma protein binding;
- valproic acid due to its displacement from plasma protein binding. The
combination of acetylsalicylic acid with anticoagulants, thrombolytics and
antiplatelet agents is accompanied by an increased risk of bleeding.
When acetylsalicylic acid is taken simultaneously with alcohol, there is
an increase in the toxic effect of alcohol on the central nervous system, an
increased risk of damage to the gastrointestinal mucosa and an increase in
bleeding time.
ASA weakens the effect of uricosuric drugs - benzbromarone (a decrease
in the uricosuric effect due to competitive suppression of renal tubular
excretion of uric acid), angiotensin-converting enzyme (ACE) inhibitors (a
dose-dependent decrease in the glomerular filtration rate is noted as a result
of inhibition of prostaglandins with a vasodilating effect, respectively, a
weakening of the hypotensive effect), diuretics (with combined use with ASA in
high doses, a decrease in the glomerular filtration rate is noted as a result
of a decrease in the synthesis of prostaglandins in the kidneys). By enhancing
the elimination of salicylates, systemic glucocorticosteroids (GCS) weaken
their effect.
Symptoms:
- in
case of moderate overdose (administration in doses of 150-300 mg/kg) - nausea,
vomiting, tinnitus, hearing loss, dizziness, confusion;
- in
case of severe overdose (administration in doses over 300 mg/kg) - fever,
hyperventilation, ketoacidosis, respiratory alkalosis, coma, cardiovascular and
respiratory failure, severe hyperglycemia.
Treatment: discontinue or reduce the dose of the drug in
agreement with the doctor, drink plenty of alkaline fluids (alkaline mineral
waters, milk, baking soda solution), in severe cases - immediate
hospitalization for emergency therapy and symptomatic treatment.
Release form
10 tablets in an
aluminum foil blister. 5 blisters together with instructions for use in a
cardboard box.
Storage conditions
Store
in a dry place at a temperature not exceeding 30°C.
Keep
out of reach of children!
Shelf life
3
years. Do not use after the expiration date stated on the package.
Vacation conditions
By prescription.