Aspenorm 100 mg tablets # 20

Author Ольга Кияница

2017-05-11

Amount in a package 20
Product form Pills
Manufacturer Pharmmex Group Ltd. (Ukraine, Borispol)
Registration certificate UA/12353/01/01
The main medicament -
morion code 160899

Aspenorm (ASPENORM) instructions for use

Composition of the medicinal product

active ingredient: acetylsalicylic acid; 1 tablet contains acetylsalicylic acid (in terms of 100% dry matter) 100 mg or 300 mg;
auxiliary substances: microcrystalline cellulose, corn starch, crospovidone;
shell - colic MAE, propylene glycol, titanium dioxide (E 171), talc.

Dosage form

Film-coated tablets. Round, biconvex tablets, coated with a coat of white or almost white.

Pharmacological group

Antiplatelet agents . The ATS code is B01A C06.

Acetylsalicylic acid suppresses platelet aggregation by blocking the synthesis of thromboxane 2. The mechanism of its action is the irreversible inactivation of the enzyme cyclooxygenase (COX-1). This inhibitory effect is particularly pronounced for platelets, since they are not capable of resynthesis of the said enzyme. It is also noted that acetylsalicylic acid also has other inhibitory effects on platelets. Thanks to these effects, it is used in many vascular diseases.

Acetylsalicylic acid belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs) with analgesic, antipyretic and anti-inflammatory properties. Oral at higher doses, acetylsalicylic acid is used to relieve pain and in light febrile conditions such as the common cold and the flu, to reduce temperature and relieve joint and muscle pain, with acute and chronic inflammatory diseases such as rheumatoid arthritis, osteoarthritis and ankylosing spondylitis .

After ingestion, acetylsalicylic acid is rapidly and completely absorbed from the gastrointestinal tract. During and after absorption, it turns into the main active metabolite - acid salicylic. The maximum concentration of acetylsalicylic acid in the blood plasma is reached after 10-20 minutes, salicylic acid - after 20-120 minutes. Due to the enteric coating of tablets Aspenorm 100 mg and 300 mg, the release of the active substance occurs not in the stomach, but in the alkaline environment of the intestine. Therefore, the absorption of acetylsalicylic acid is slowed down to 3-6 hours after the application of the tablet coated with an enteric-coated membrane, compared to a conventional tablet of acetylsalicylic acid.

Acetylsalicylic and salicylic acids completely bind to blood plasma proteins and are quickly distributed in the body.Salicylic acid penetrates the placenta, and also enters the breast milk.

Salicylic acid is metabolized in the liver. Metabolites of salicylic acid are salicylurea, salicylphenol glucuronide, salicylacyl glucuronide, gentisic acid and gentisine-sulfuric acid.

The kinetics of elimination of salicylic acid depends on the dose, since the metabolism is limited by the activity of liver enzymes. The half-life period depends on the dose and increases from 2-3 hours when low doses are used up to 15 hours when high doses are used. Salicylic acid and its metabolites are excreted mainly by the kidneys.

Preclinical data

The preclinical safety profile of acetylsalicylic acid is well documented.

It is known that salicylates at high doses cause kidney damage without other organic lesions.

Acetylsalicylic acid has been extensively studied for mutagenicity, but there has been no evidence of a mutagenic potential. The same goes for carcinogenicity studies. It is also known that salicylates have a teratogenic effect.

Implantation abnormalities, embryotoxic and fetotoxic effects, and impaired ability to learn from offspring after application of the drug in the prenatal period were described.

Indications

To reduce the risk:

  • death in patients with suspected acute myocardial infarction;
  • morbidity and mortality in patients with myocardial infarction
  • transient ischemic attacks (TIA) and stroke in patients with TIA;
  • morbidity and death in stable and unstable angina;
  • myocardial infarction in patients with a high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension) and people with a multifactorial risk of cardiovascular diseases (hyperlipidemia, obesity, smoking, old age, etc.).

For prevention:

  • thrombosis and embolism after vascular surgery (percutaneous transluminal catheter angioplasty (PTCA), carotid endarterectomy, coronary artery bypass grafting (CABG), arteriovenous shunting);
  • deep vein thrombosis and pulmonary embolism after prolonged immobilization (after surgical operations).

For secondary prevention of stroke.

Contraindications

Hypersensitivity to acetylsalicylic acid, other salicylates or to any component of the drug.
Asthma caused by the intake of salicylates or substances with a similar effect, especially NSAIDs in the history.
Acute peptic ulcers.
Hemorrhagic diathesis.
Renal failure is severe.
Hepatic insufficiency is severe.
Heart failure is severe.
Combination with methotrexate in a dosage of 15 mg / week or more (see Section "Interaction with Other Drugs and Other Interactions").

Special caveats

Aspenorm is used with caution in the following situations:

  • hypersensitivity to analgesic, anti-inflammatory, antirheumatic drugs, as well as in the presence of allergies to other substances contained in the preparation;
  • gastrointestinal ulcers, including chronic and recurrent ulcerative diseases or gastrointestinal hemorrhages in an anamnesis
  • simultaneous use of anticoagulants;
  • impaired renal function or cardiovascular circulatory disorders (eg, kidney vascular pathology, congestive heart failure, hypovolemia, extensive surgery, sepsis, or severe bleeding), as acetylsalicylic acid may also increase the risk of impaired kidney function and acute renal failure
  • severe insufficiency of glucose-6-phosphate dehydrogenase, since 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 an acute infectious process,
  • abnormal liver function.

Ibuprofen may reduce the inhibitory effect of acetylsalicylic acid on platelet aggregation. In case of using Aspenorma, before starting the administration of ibuprofen as an anesthetic, the patient should consult a physician.

Acetylsalicylic acid can cause the development of bronchospasm or an attack of bronchial asthma, as well as other hypersensitivity reactions. Risk factors include history of asthma, hayfever, polyposis or chronic respiratory diseases, allergic reactions (skin reactions, pruritus, urticaria) to other substances in the anamnesis.

Through 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 chance / increase 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 an attack of gout in predisposed patients.

Do not use drugs containing 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 chickenpox, there is a risk of developing Ray's syndrome, which is a very rare but life-threatening disease, requires urgent medical intervention. The risk can 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 and lactation

The inhibition of prostaglandin synthesis may adversely affect pregnancy and / or fetal / intrauterine development. There is evidence that there is a risk of miscarriage and fetal malformations after the use of inhibitors of prostaglandin synthesis in early pregnancy. The risk rises depending on the increase in dose and duration of therapy.

There are known epidemiological data on the occurrence of malformations is not consistent, but the increased risk of gastroschisis can not be excluded with the use of acetylsalicylic acid. During the I and II trimesters of pregnancy, preparations containing acetylsalicylic acid should not be administered without a clear clinical need. For women who may be pregnant or in the first and second trimesters of pregnancy, the dose of drugs containing acetylsalicylic acid should be as low as possible, and the duration of treatment can be shorter.

In the third trimester of pregnancy, all inhibitors of prostaglandin synthesis can affect the fetus in the following way:

cardiopulmonary toxicity (with premature closure of the arterial duct and pulmonary hypertension)
disturbance of kidney function with possible subsequent development of renal insufficiency with oligohydroamniozom.
On a woman and a child at the end of pregnancy, the inhibitors of prostaglandin synthesis can influence this way:

  • the possibility of prolonging the time of bleeding, an antiaggregant effect that can occur even after very low doses;
  • weakening uterine contractions, which can lead to a delay or an increase in the duration of labor.

Despite this, acetylsalicylic acid is contraindicated in the third trimester of pregnancy.

Salicylates and their metabolites are found in breast milk in small amounts.

Since there was no adverse effect on the baby after taking the drug by women during lactation, it is usually not necessary to interrupt breastfeeding. However, in cases of regular use or with the use of high doses of breast-feeding, it is necessary to stop at early stages.

The ability to influence the reaction rate when driving vehicles or other mechanisms

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

Children

According to the indications (see the section "Indications"), Aspenorm is not prescribed for children.

The use of acetylsalicylic acid in children under the age of 16 can cause severe side effects (including Reye's syndrome, one of the symptoms of which is constant vomiting). Please refer to the information in the "Special instructions" section.

Dosing and Administration

The drug is taken orally, 30-60 minutes before meals, without chewing, squeezed with enough liquid.

To reduce the risk of death in patients with suspected acute myocardial infarction, a drug in the dose of 100-300 mg per day is used. Within 30 days after a heart attack continue to take a maintenance dose of 100-300 mg per day. After 30 days, further prevention of recurrence of myocardial infarction should be considered.

To achieve rapid absorption, if used in the case of this indication, the first tablet must be chewed.

To reduce the risk of morbidity and death of patients who underwent myocardial infarction, apply 100-300 mg per day.

For secondary prevention of stroke, the drug is used in a dose of 100-300 mg per day.

To reduce the risk of TIA and stroke in patients with TIA used 100-300 mg per day.

To reduce the risk of developing the disease and death in patients with stable and unstable angina, 100-300 mg per day is prescribed.

For prophylaxis of thromboembolism after operations on vessels (percutaneous transluminal catheter angioplasty, carotid endarterectomy, coronary artery bypass grafting, arteriovenous shunting), the drug is used at a dose of 100-200 mg per day daily or 300 mg per day every other day.

For prevention of deep vein thrombosis and pulmonary embolism after a prolonged state of immobilization (after surgery) - 100-200 mg per day or 300 mg per day every other day.

For the prevention of myocardial infarction in patients with a high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension) and people with a multifactorial risk of cardiovascular diseases (hyperlipidemia, obesity, smoking, old age, etc.) Apply 100 mg per day or 300 mg per day every other day.

Overdose

The toxic effect of salicylates is possible due to chronic intoxication caused by prolonged therapy (the use of more than 100 mg / kg / day for more than 2 days can cause toxic effects), as a result of acute intoxication, which carries a life threat (overdose) and whose cause may be, for example, accidental use by children or an unexpected overdose.

Chronic poisoning with salicylates can be of a hidden nature, since its signs and symptoms are nonspecific. Moderate chronic intoxication caused by salicylates, or salicylism, is observed, as a rule, only after repeated doses of large doses.

Symptoms: dizziness, ringing in the ears, deafness, increased sweating, nausea and vomiting, headache, confusion.These symptoms can be controlled by lowering the dose. Ringing in the ears is possible with a concentration of salicylates in the blood plasma above 150-300 μg / ml. Serious adverse reactions are observed when the concentration of salicylates in the blood plasma is above 300 μg / ml.

Acute intoxication is indicated by a marked change in the acid-base balance, which may differ depending on the age of the patient and the severity of intoxication. Most often, its manifestation in children is metabolic acidosis. The severity of the condition can not be estimated solely on the basis of the concentration of salicylates in the plasma. Absorption of acetylsalicylic acid may slow down due to a delay in gastric release, the formation of concrements in the stomach or in the case of taking the drug in the form of tablets coated with an enteric-dissolvable coating.

Treatment.

Treatment of acute intoxication caused by an overdose of acetylsalicylic acid is determined by the severity, clinical symptoms and is provided by standard methods that are used in poisoning. All measures taken should be aimed at accelerating the removal of the drug and restoring the electrolyte and acid-base balance.

Through complex pathophysiological effects of salicylate poisoning, the manifestations and symptoms / test results may include:

Manifestations and symptoms test results therapeutic activities
Intoxication of mild to moderate   Gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis
Tachypnea, hyperventilation, respiratory alkalosis Alkalemia, alkaluria Recovery of electrolyte and acid-base balance

 

Hyperhidrosis (excessive sweating)    
Nausea, vomiting    
Intoxication of moderate or severe degree   Gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis, hemodialysis in severe cases
Respiratory alkalosis with compensatory metabolic acidosis Aciduria, aciduria Recovery of electrolyte and acid-base balance
hyperpyrexia   Recovery of electrolyte and acid-base balance
Respiratory: hyperventilation, noncardiogenic pulmonary edema, respiratory failure, asphyxia    
Cardiovascular: dysarthritis, arterial hypotension, cardiovascular failure For example, changes in blood pressure, ECG  
Loss of fluid and electrolytes dehydration, oliguria, renal failure For example, hypokalemia, hypernatremia, hyponatremia, changes in kidney function Recovery of electrolyte and acid-base balance
Disturbance of glucose metabolism, ketoacidosis Hyperglycemia, hypoglycemia (especially in children). Elevated level of ketone bodies  
Ringing in the ears, deafness    
Gastrointestinal: bleeding in the gastrointestinal tract    
Hematologic: inhibition of platelets, coagulopathy For example, prolongation of PT, hypoprothrombinemia  
Neurological: toxic encephalopathy and CNS depression with such manifestations as lethargy, confusion, coma and convulsions    

Side effects

Gastrointestinal disorders: frequent manifestations and symptoms of dyspepsia, pain in the epigastric region and abdominal pain in some cases - inflammation of the digestive tract, erosive and ulcerative lesions of the gastrointestinal tract, which can in rare cases cause gastrointestinal hemorrhages and perforations with appropriate laboratory indicators and clinical manifestations.

Due antiplatelet action on platelets acetylsalicylic acid can be associated with the risk of bleeding. We observed bleeding such as Perioperative hemorrhage, hematoma, bleeding of the urogenital system, epistaxis, bleeding gums; rarely or very rarely - severe bleeding such as gastrointestinal hemorrhage, cerebral hemorrhage (especially in patients with uncontrolled hypertension, and / or while the application antigemostatichnih funds), which in some cases could potentially be life threatening.

Hemorrhage may lead to acute and chronic posthemorrhagic anemia / iron deficiency anemia (due to the so-called hidden mikrokrovotecheniya) with corresponding laboratory manifestations and clinical symptoms such as fatigue, pallor of skin, hypoperfusion.

In patients with severe deficiency of glucose-6-phosphate dehydrogenase were observed hemolysis and hemolytic anemia.

It reported renal dysfunction and acute renal failure.

hypersensitivity reaction with the appropriate laboratory and clinical manifestations include asthmatic condition, skin reactions mild or moderate, as well as from the respiratory tract of the reaction, the digestive tract and cardiovascular system, including symptoms such as rash, urticaria, swelling, itching, rhinitis , nasal congestion, cardio-pulmonary insufficiency, and very rarely - severe reactions, including anaphylactic shock.

Very rarely it reported transient liver failure with increased levels of liver transaminases.

There were dizziness and ringing in the ears, which may indicate an overdose.

Interaction with other drugs and other interactions

Contraindications for simultaneous use.

Use of acetylsalicylic acid and methotrexate at a dose of 15 mg / week or more increases hematologic toxicity of methotrexate (MTX decrease renal clearance and anti-inflammatory agents salicylates displacement of methotrexate from binding with plasma proteins).

Combinations to be used with caution.

In the application of acetylsalicylic acid and methotrexate at doses less than 15 mg per week increases hematological toxicity of methotrexate (MTX decrease renal clearance and anti-inflammatory agents salicylates displacement of methotrexate from binding with plasma proteins).

Concomitant use of aspirin ibuprofen prevents the irreversible inhibition of platelet acetylsalicylic acid. Ibuprofen treatment of patients at risk of cardiovascular disease may limit the cardioprotective effect of acetylsalicylic acid.

With simultaneous application Aspenormu and anticoagulants, thrombolytics / other platelet aggregation inhibitors / hemostasis increases the risk of bleeding.

With the simultaneous application of high doses of salicylates with NSAIDs (via vzaemoposilyuvalny effect) increases the risk of ulcers and gastrointestinal bleeding.

When applying a selective serotonin reuptake inhibitor increases the risk of gastrointestinal bleeding due to a possible synergy effect.

While the use of digoxin in plasma concentration of the latter is increased by reducing the renal excretion.

With the simultaneous application of high-dose acetylsalicylic acid and antidiabetic agents from the group of sulfonylurea hypoglycemic effect of the latter is amplified by displacing sulfonylurea acetylsalicylic acid associated with plasma proteins.

Diuretics in combination with high doses of aspirin reduced glomerular filtration by reducing the synthesis of prostaglandins in the kidney.

Systemic corticosteroids (except hydrocortisone, which is used for replacement therapy in Addison's disease), reduce the level of salicylate in blood and increase the risk of overdose salicylates after treatment corticosteroids.

ACE (ACE) inhibitors in combination with high doses of aspirin cause a decrease in glomerular filtration by inhibiting prostaglandin vasodilator effect and reduced antihypertensive effect.

While the use of valproic acid, acetylsalicylic acid displaces it from the connection with plasma proteins, increasing the toxicity of the latter.

Alcohol promotes damage the mucosa of the digestive tract and prolongs bleeding time owing to the synergy of acetylsalicylic acid and alcohol.

The simultaneous use of uricosuric agents such as benzobromaron, probenecid decreases uricosuric effect (owing to competition excretion of uric acid renal tubules).

Shelf life

2 years.

Storage conditions

Stored in original package at a temperature not higher than 25 ° C. Keep out of reach of children.

Packaging

10 tablets in a blister, 2 blisters in a pack.

Category of leave

Without recipe.

 

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