Lospirin enteric-coated tablets 75 mg strip No. 120

Instructions for Lospirin enteric-coated tablets 75 mg strip No. 120

Composition

active ingredient: acetylsalicylic acid;

1 tablet contains 75 mg of acetylsalicylic acid;

excipients: microcrystalline cellulose, pregelatinized starch, colloidal anhydrous silicon dioxide, stearic acid, Opadry Y-1-7000 white, Acryl-Eze 9ZO18359 white.

Dosage form

Enteric-coated tablets.

Main physicochemical properties: round biconvex tablets, coated with a white coating.

Pharmacotherapeutic group

Antithrombotic agents. ATX code B01A C06.

Pharmacological properties

Pharmacodynamics.

Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxane A2. Its mechanism of action is the irreversible inactivation of the enzyme cyclooxygenase (COX-1). This inhibitory effect is particularly pronounced for platelets, since they are unable to resynthesize this enzyme.

Acetylsalicylic acid also exhibits other inhibitory effects on platelets. Due to these effects, it can be used in many vascular diseases.

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

Orally, in higher doses, acetylsalicylic acid can be used to relieve pain and mild feverish conditions such as colds and flu, to reduce fever and relieve joint and muscle pain, and in acute and chronic inflammatory diseases such as rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.

Pharmacokinetics.

After oral administration, acetylsalicylic acid is rapidly and completely absorbed from the gastrointestinal tract. During and after absorption, it is converted into the main active metabolite, salicylic acid.

The maximum concentration of acetylsalicylic acid in the blood plasma is reached after 10-20 minutes, salicylic acid - after 20-120 minutes, respectively. Due to the enteric coating of Lospirin® tablets, the release of the active substance does not occur 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 taking the tablet, coated with an enteric coating, compared with a regular acetylsalicylic acid tablet.

Acetylsalicylic and salicylic acids are completely bound to blood plasma proteins and are rapidly distributed in the body. Salicylic acid crosses the placenta and also enters breast milk.

Salicylic acid is metabolized primarily in the liver. The metabolites of salicylic acid are salicylic acid, phenolic and acyl glucuronides, gentisic acid and gentisinuric acid.

The elimination kinetics of salicylic acid are dose-dependent, as metabolism is limited by the activity of liver enzymes. The half-life is dose-dependent and increases from 2-3 hours at low doses to 15 hours at high doses. Salicylic acid and its metabolites are excreted from the body mainly by the kidneys.

Indication

To reduce risk:

fatal outcome in patients with suspected acute myocardial infarction;

morbidity and mortality in patients who have had myocardial infarction;

transient ischemic attacks (TIA) and stroke in patients with TIA;

morbidity and mortality in stable and unstable angina;

myocardial infarction in patients with a high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension) and individuals with a multifactorial risk of cardiovascular disease (hyperlipidemia, obesity, smoking, old age).

For prevention:

thrombosis and embolism after vascular surgery (percutaneous transluminal catheter angioplasty, carotid endarterectomy, coronary artery bypass grafting, arteriovenous bypass grafting);

deep vein thrombosis and pulmonary embolism after long-term immobilization (after surgery).

For secondary prevention of strokes.

Contraindication

Hypersensitivity to acetylsalicylic acid, other salicylates or to any component of the drug.

History of asthma induced by the use of salicylates or substances with a similar effect, especially NSAIDs.

Hemorrhagic diathesis.

Acute peptic ulcers.

Severe renal failure.

Severe liver failure.

Severe heart failure.

Gout.

Combination with methotrexate at a dosage of 15 mg/week or more (see section “Interaction with other medicinal products and other types of interactions”).

Age under 18 years. Acetylsalicylic acid can cause the development of Reye's syndrome.

The last trimester of pregnancy.

Interaction with other medicinal products and other types of interactions

Contraindicated combinations for simultaneous use.

The use of acetylsalicylic acid and methotrexate in doses of 15 mg/week or more increases the hematological toxicity of methotrexate (due to a decrease in the renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from plasma protein binding by salicylates).

Combinations not recommended for simultaneous use.

Uricosuric agents (benzobromarone, probenecid)

Salicylates reduce the therapeutic efficacy of uricosuric agents for the excretion of uric acid. This may provoke the development of gout in patients with reduced uric acid excretion. The combined use of acetylsalicylic acid and uricosuric agents should be avoided.

Combinations that should be used with caution.

Anticoagulants, thrombolytics/other inhibitors of platelet aggregation/hemostasis.

The simultaneous use of acetylsalicylic acid and anticoagulants, thrombolytics/other inhibitors of platelet aggregation/hemostasis enhances their effects and increases the risk of bleeding.

Selective serotonin reuptake inhibitors.

When used with selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases due to a possible synergistic effect.

Oral antidiabetic drugs

Salicylates may enhance the hypoglycemic effect of oral antidiabetic drugs, including those from the sulfonylurea group.

Barbiturates, sulfonamides, triiodothyronine

Acetylsalicylic acid may enhance their effect.

Digoxin/lithium

When acetylsalicylic acid is used simultaneously with digoxin/lithium, their plasma concentrations increase due to reduced renal excretion. It is recommended to monitor plasma digoxin/lithium concentrations at the beginning and in the event of discontinuation of acetylsalicylic acid treatment, as dose adjustment may be necessary.

Diuretics and antihypertensives

Nonsteroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, may reduce the antihypertensive effect of diuretics and other antihypertensive drugs. The use of NSAIDs with angiotensin-converting enzyme (ACE) inhibitors increases the risk of acute renal failure. Patients receiving acetylsalicylic acid and these drugs concomitantly are advised to closely monitor blood pressure and adjust the dose if necessary.

Diuretics.

Concomitant use of acetylsalicylic acid with diuretics may contribute to the development of acute renal failure due to a decrease in glomerular filtration due to a decrease in prostaglandin synthesis. It is recommended to hydrate the patient and monitor renal function at the beginning of therapy.

Carbonic anhydrase inhibitors (acetazolamide)

Concomitant use of carbonic anhydrase inhibitors with acetylsalicylic acid may lead to serious acidosis and increased central nervous system toxicity.

Systemic corticosteroids.

Concomitant use of acetylsalicylic acid and systemic corticosteroids may increase the risk of ulceration and bleeding in the gastrointestinal tract.

Methotrexate at doses less than 15 mg/week.

When using acetylsalicylic acid and methotrexate in doses less than 15 mg/week, the hematological toxicity of methotrexate increases (reduction in renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from plasma protein binding by salicylates). Weekly blood count monitoring is necessary during the first weeks of therapy. Careful monitoring is recommended for patients with impaired renal function, even moderate, as well as for the elderly.

Other NSAIDs

Concomitant use of acetylsalicylic acid and other NSAIDs may be accompanied by an increase in their effects and adverse reactions. The risk of ulceration and bleeding in the gastrointestinal tract increases.

Ibuprofen.

Concomitant use with ibuprofen prevents irreversible inhibition of platelets by acetylsalicylic acid. Treatment with ibuprofen in patients at risk of cardiovascular disease may limit the cardioprotective effect of acetylsalicylic acid (see section "Special warnings and precautions for use").

Cyclosporine, tacrolimus.

Concomitant use of NSAIDs with cyclosporine or tacrolimus may increase the nephrotoxicity of cyclosporine and tacrolimus. Renal function should be monitored when these drugs are used concomitantly with acetylsalicylic acid.

Antacids.

The combined use of acetylsalicylic acid with antacids may lead to increased excretion (due to an increase in urine pH).

Antiepileptic drugs (phenytoin, valproate)

Increased plasma levels of phenytoin and valproate. When used simultaneously with valproic acid, acetylsalicylic acid displaces it from its binding to plasma proteins. As a result, plasma levels of valproate increase, which leads to an increase in the frequency of adverse reactions to signs of intoxication, such as tremor, nystagmus, ataxia and personality changes.

Penicillin

Prolongation of the half-life of penicillin from blood plasma.

The combined use of acetylsalicylic acid with alcohol may increase the risk of ulcers and bleeding in the gastrointestinal tract.

Application features

Acetylsalicylic acid at a dosage of 75 mg is not intended for use as an anti-inflammatory/analgesic/antipyretic.

Recommended for use in adults. The drug is contraindicated for use in patients under 18 years of age due to the risk of Reye's syndrome (see sections "Contraindications" and "Children").

Reye's syndrome

Reye's syndrome may occur when drugs containing acetylsalicylic acid are used in children with acute respiratory viral infections (ARI), with or without fever, without consulting a doctor. Some viral diseases, especially influenza A, influenza B and chickenpox, carry a risk of developing Reye's syndrome, which is a very rare but life-threatening illness requiring immediate medical attention. The risk may be increased if acetylsalicylic acid is used as a concomitant drug, but a causal relationship in this case has not been proven. If these conditions are accompanied by persistent vomiting, this may be a manifestation of Reye's syndrome.

The drug should be used with caution in the following situations:

hypersensitivity to analgesic, anti-inflammatory, antirheumatic drugs, as well as in case of allergies to other substances;

nasal polyps;

the presence of symptoms of chronic gastric or duodenal dyspepsia or their recurrence;

gastrointestinal ulcers, including chronic and recurrent peptic ulcers or a history of gastrointestinal bleeding;

arterial hypertension;

simultaneous use of anticoagulants;

in patients with impaired renal function or patients with cardiovascular circulatory disorders (e.g. renal vascular pathology, congestive heart failure, hypovolemia, extensive surgery, sepsis or severe bleeding), since acetylsalicylic acid may also increase the risk of impaired renal function and acute renal failure;

In patients with severe glucose-6-phosphate dehydrogenase deficiency, acetylsalicylic acid may 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.

Ibuprofen may inhibit the effect of low doses of acetylsalicylic acid on platelet aggregation when used concomitantly with acetylsalicylic acid (see section "Interaction with other medicinal products and other forms of interaction"). When using Lospirin, the patient should consult a doctor before starting to take ibuprofen as an analgesic.

Hypersensitivity

Acetylsalicylic acid may cause hypersensitivity reactions, including bronchospasm/asthma attack or other reactions. Risk factors for hypersensitivity reactions when using acetylsalicylic acid include a history of asthma, hay fever, nasal polyps or chronic respiratory disease, allergic reactions (e.g. skin reactions, itching, urticaria) that occurred when using other substances. The drug should be used with caution in case of hypersensitivity to analgesics, anti-inflammatory, antirheumatic drugs, as well as in case of allergy to other substances.

The drug should be discontinued at the first signs of hypersensitivity reactions (e.g., skin rash, mucosal lesions).

Serious skin adverse reactions.

Rare cases of serious skin reactions, including Stevens-Johnson syndrome, have been reported with the use of acetylsalicylic acid (see section 4.8). The drug should be discontinued if any clinical signs of hypersensitivity reactions, including skin and mucous membrane rash, appear.

Risk of bleeding/increased bleeding during surgical interventions

The antiplatelet effect of acetylsalicylic acid persists for several days after administration, which may increase the likelihood of bleeding or increase bleeding during surgery (including minor surgical interventions, such as tooth extraction). Temporary withdrawal of the drug may be necessary.

Gastrointestinal bleeding/ulcers

Patients should report any unusual bleeding symptoms to their doctor. If gastrointestinal bleeding or ulceration occurs, treatment should be discontinued.

Menorrhagia.

Acetylsalicylic acid is not recommended for use in women with menorrhagia (during menstruation) as it may increase menstrual bleeding.

Impaired kidney or liver function

Acetylsalicylic acid should be used with caution in patients with moderate renal or hepatic impairment (contraindicated in severe cases) or in patients with signs of dehydration, since the use of NSAIDs may lead to deterioration of renal function. In patients with hepatic insufficiency (mild or moderate), liver function tests should be monitored.

Elderly patients are particularly susceptible to the development of adverse reactions to NSAIDs, including acetylsalicylic acid, in particular gastrointestinal bleeding and perforation, which can be fatal (see section "Method of administration and dosage"). If long-term therapy with acetylsalicylic acid is necessary, patients should be regularly examined.

Gout

When using low doses of acetylsalicylic acid, the excretion of uric acid may be reduced. This may lead to an attack of gout in patients prone to it. The use of acetylsalicylic acid is contraindicated in patients with gout (see section "Contraindications").

Drugs that alter hemostasis

Due to the increased risk of bleeding, the concomitant use of acetylsalicylic acid with other medicinal products that alter haemostasis (e.g. anticoagulants such as warfarin, thrombolytics, antiplatelet agents, anti-inflammatory agents, selective serotonin reuptake inhibitors) is not recommended unless the combination is clearly necessary (see section 4.5). In the event of such a combination, close monitoring of the patient for signs of bleeding is recommended.

Ulcerogenic effect

Due to the increased risk of ulcerogenic effects, caution should be exercised when concomitantly using acetylsalicylic acid with oral corticosteroids, selective serotonin reuptake inhibitors, deferasirox (see section "Interaction with other medicinal products and other types of interactions").

Hypoglycemia

Acetylsalicylic acid, when used in high doses, may potentiate the hypoglycemic effect of sulfonylureas and insulin, which may increase the risk of hypoglycemia (see section "Interaction with other medicinal products and other types of interactions").

Use during pregnancy or breastfeeding

Pregnancy.

Salicylates should be used with caution in the first and second trimesters of pregnancy. Salicylates are contraindicated in the third trimester of pregnancy.

Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryonal/fetal development. Available epidemiological data indicate a risk of miscarriage and foetal malformations (cardiac malformations and gastroschisis) after the use of prostaglandin synthesis inhibitors in early pregnancy. The risk increases with increasing dose and duration of therapy. According to the available data, an association between the use of acetylsalicylic acid and an increased risk of miscarriage has not been confirmed.

The available epidemiological data on the occurrence of malformations are not consistent, but an increased risk of gastroschisis cannot be excluded with the use of acetylsalicylic acid. The results of a prospective study of exposure in early pregnancy (1-4 months) involving approximately 14,800 woman-child pairs do not indicate any association with an increased risk of malformations.

Animal studies indicate reproductive toxicity.

During the first and second trimesters of pregnancy, preparations containing acetylsalicylic acid should not be prescribed unless clearly necessary. In women who may be pregnant or during the first and second trimesters of pregnancy, the dose of preparations containing acetylsalicylic acid should be as low as possible and the duration of treatment should be as short as possible.

Cases of implantation disorders, embryotoxic and fetotoxic effects, and effects on the child's learning ability have been reported following prenatal exposure to salicylates.

According to animal studies, the use of salicylates causes adverse reactions in the fetus (such as increased mortality, growth disorders, salicylate intoxication), however, controlled studies involving pregnant women have not been conducted.

According to previous experience, the risk is low when using the drug in therapeutic doses.

During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may affect

on the fruit as follows:

cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);

impaired renal function with possible subsequent development of renal failure with oligohydramnios;

on the woman and child at the end of pregnancy as follows:

possibility of prolongation of bleeding time, antiplatelet effect, which may occur even after very low doses;

inhibition of uterine contractions, which can lead to a delay or prolongation of labor.

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

Breast-feeding.

Salicylates and their metabolites pass into breast milk. Concentrations in breast milk are equivalent to or even higher than those in maternal plasma. During forced use during lactation, breastfeeding should be discontinued in the case of regular use of high doses (> 300 mg/day).

Ability to influence reaction speed when driving vehicles or other mechanisms

No research was conducted.

Method of administration and doses

The drug should be taken orally, 30-60 minutes before meals, without chewing, with sufficient liquid.

* - Continue to take a maintenance dose of 75-300 mg per day for 30 days after the infarction. After 30 days, further prevention of recurrent myocardial infarction should be considered. The initial dose should be chewed to achieve rapid absorption.

** - use one of the treatment regimens.

Elderly patients

In general, acetylsalicylic acid should be used with caution in elderly patients, who are more prone to adverse reactions (see section "Special warnings and precautions for use"). In the absence of severe renal or hepatic insufficiency, the usual adult dose is recommended. Treatment should be reviewed at regular intervals.

Children.

According to the indications (see the "Indications" section), the drug Lospirin® should not be used in children.

The use of acetylsalicylic acid in children under 18 years of age may cause serious side effects (including Reye's syndrome, one of the signs of which is persistent vomiting). Please read the information provided in the "Special instructions" section.

Overdose

Symptoms of severe poisoning may develop slowly, for example within 12–24 hours after administration. After oral administration of ASA doses up to 150 mg/kg body weight, moderate intoxication may develop, and at doses > 300 mg/kg body weight, severe intoxication may develop.

Chronic salicylate poisoning can be latent because its symptoms are nonspecific. Moderate chronic intoxication usually occurs only after repeated ingestion of large doses.

Acute intoxication is indicated by a pronounced change in acid-base balance, which may vary depending on the age of the patient and the severity of intoxication. Its most common manifestation in children is metabolic acidosis. The severity of the condition cannot be assessed solely on the basis of the concentration of salicylates in the plasma. The absorption of acetylsalicylic acid may be slowed down due to delayed gastric release, the formation of concrements in the stomach or when the drug is taken in the form of tablets coated with an enteric coating.

Reservation.

Local signs of irritation that usually dominate in ASA overdose, such as nausea, vomiting, and stomach pain, may be absent because this dosage form of ASA has an enteric coating and resorption occurs only in the small intestine.

Symptoms.

Headache, nausea, hypocalcemia or hypoglycemia, skin rash, dizziness, gastrointestinal bleeding, inhibition of thromboembolism to coagulopathy, cardiovascular disorders (from arrhythmia, arterial hypotension to cardiac arrest), tinnitus, visual and hearing impairment, tremor, confusion, hyperthermia, increased sweating, hyperventilation, acid-base and electrolyte imbalance, dehydration, coma and respiratory failure.

Tinnitus is possible at plasma salicylate concentrations above 150–300 μg/mL. More serious adverse reactions are observed at plasma salicylate concentrations above 300 μg/mL.

Therapy.

Due to life-threatening conditions due to severe intoxication, all necessary precautions should be taken immediately: prevention or reduction of absorption, gastric lavage in the early stages (up to one hour after ingestion), activated charcoal, monitoring and appropriate correction of electrolytes. Use of glucose. Sodium bicarbonate to correct acidosis and to accelerate excretion (urine pH > 8). Glycine: initial dose - 8 g orally, then - 4 g every 2 hours for 16 hours. Hemoperfusion or hemodialysis is possible (the need for use can be established in the poison control center).

Side effects

From the blood and lymphatic system: thrombocytopenia, agranulocytosis, pancytopenia, leukopenia, anemia (posthemorrhagic/iron deficiency, aplastic) with corresponding laboratory parameters and clinical manifestations; hemolysis and hemolytic anemia (in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency), prolongation of bleeding time.

Immune system: hypersensitivity reactions, including asthmatic status, skin reactions, respiratory, gastrointestinal and cardiovascular disorders, rash, edema, pruritus, cardiorespiratory failure, anaphylactic shock; erythematous/eczematous skin reactions, severe skin reactions, including exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis; angioedema, allergic edema, rhinitis, nasal congestion, shock-like hypotension.

Metabolic disorders: hyperuricemia with corresponding laboratory indicators and clinical manifestations (gout attacks), hypoglycemia, acid-base imbalance.

From the nervous system: headache, dizziness, disorientation, confusion.

On the part of the organs of vision: visual impairment.

On the part of the auditory organs: hearing impairment, ringing in the ears (tinnitus).

Gastrointestinal: microbleeds (70%), dyspepsia, nausea, vomiting, diarrhea; epigastric pain, abdominal pain, heartburn, anorexia, gastrointestinal inflammation, gastrointestinal bleeding, gastrointestinal ulcers, which very rarely can lead to hemorrhage and perforation, with corresponding clinical symptoms and changes in laboratory parameters.

Vascular disorders: hemorrhagic vasculitis, bleeding (intraoperative hemorrhages, hematomas, bleeding from the genitourinary system, epistaxis, bleeding from the gums, gastrointestinal hemorrhages, hematemesis, melena, occult gastrointestinal hemorrhages, cerebral hemorrhages (especially in patients with uncontrolled hypertension and/or concomitant use of anticoagulants) with corresponding clinical symptoms, including: asthenia, pallor of the skin, hypoperfusion.

Liver and biliary tract disorders: hepatic dysfunction, transient hepatic failure, increased liver transaminases.

Renal and urinary disorders: renal dysfunction, acute renal failure.

From the respiratory system: rhinitis, shortness of breath, bronchospasm, asthma attacks.

From the reproductive system: menorrhagia.

Skin and subcutaneous tissue disorders: purpura, erythema nodosum, erythema multiforme.

Others: Reye's syndrome (see section "Special warnings and precautions for use").

Expiration date

4 years.

Storage conditions

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging

10 tablets in a strip; 3, 8 or 10 strips in a cardboard box.

30 tablets in a strip; 1, 2, 3 or 4 strips in a cardboard box.

Vacation category

Without a prescription.

Producer

"KUSUM FARM" LLC.

or

KUSUM HEALTHCARE PVT LTD/KUSUM HEALTHCARE PVT LTD.

Location of the manufacturer and address of its place of business.

40020, Ukraine, Sumy region, Sumy city, Skryabina st., 54.

or

Plot No. M-3, Indore Special Economic Zone, Phase-II, Pithampur, Distt. Dhar, Madhya Pradesh, Pin 454774, India.