Aspirin Express - instructions for use, dose, side effects, contraindications

as inactive ingredients: sodium citrate anhydrous 1068 mg, sodium carbonate monosubstituted 1166 mg, citric acid anhydrous 212 mg, sodium carbonate anhydrous 254 mg.

Description:Round, flat, oblique white tablets, engraved in the form of a brand name (Bayer's cross) on one side.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

N.02.B.A Salicylic acid and its derivatives

Pharmacodynamics:

Acetylsalicylic acid (ASA) belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs) and has analgesic, antipyretic and anti-inflammatory effects. The mechanism of action is the irreversible inhibition of the enzyme cyclooxygenase (COX), an enzyme that regulates the synthesis of prostaglandins E2, E12 and thromboxane A2.

Pharmacokinetics:

Absorption is high, after oral administration ASA is rapidly completely absorbed from the gastrointestinal tract. The maximum concentration Cmah ASA for oral administration for the dosage form of the effervescent tablet is achieved after 18 minutes, which is 2 times faster than standard tablets, Cmwhich is equal to 30-45 minutes. During the absorption period and immediately after it, ASA turns into the main active metabolite, salicylic acid. FROMmah salicylic acid for the dosage form effervescent tablets reaches a maximum concentration in the blood plasma after 48 min, and Cmah salicylic acid for standard tablets - after 1.5-2 hours.

About 80% of ASA and salicylic acid binds to plasma proteins and is quickly distributed into tissues. Salicylic acid is metabolized in the liver with the formation of metabolites - salicylurate, salicyl-phenolic glucuronide, salicylacyl glucuronide, gentisin and gentisuric acids. It is excreted in breast milk and penetrates the placenta.

Elimination of salicylic acid is dose-dependent. The half-life period varies from 2-3 hours when the drug is taken in low doses up to about 15 hours when high doses are used. Salicylic acid and its metabolites are excreted mainly by the kidneys.

Indications:

For symptomatic treatment of headache, toothache, sore throat, menstrual pain, back pain, muscles and joints, mild pain in arthritis. Elevated body temperature for colds and other infectious and inflammatory diseases.

Contraindications:

- Ulcerative lesion of the gastrointestinal tract

- Hemorrhagic diathesis

- Hypersensitivity to ASA, other salicylates or any excipients of the drug

- Bronchial asthma induced by the intake of salicylates and NSAIDs

- Combined use with methotrexate at a dose of 15 mg per week

- Severe renal insufficiency

- Severe hepatic impairment

- Severe heart failure in decompensation

- First and third trimester of pregnancy and lactation period

The drug is not prescribed for children under 15 with acute respiratory infections caused by viral infections, because of the risk of developingReye syndrome (encephalopathy and acute fatty liver dystrophy with acute development of hepatic insufficiency).

Carefully:Concomitant treatment with anticoagulants; presence in the anamnesis: ulcers of the gastrointestinal tract,including chronic or recurrent peptic ulcer, as well as gastrointestinal bleeding, allergic reactions to NSAIDs and other drugs, bronchial asthma, hay fever, nasal polyposis, chronic respiratory diseases; impaired renal and hepatic function; gout; hyperuricemia; II trimester of pregnancy.

Pregnancy and lactation:

In the I and III trimesters of pregnancy, the use of all drugs containing ASA is contraindicated.

In II trimester of pregnancy, ASA can be administered occasionally. As a long-term therapy not to use.

The use of ASA in the III trimester of pregnancy at a dose> 500 mg / day, like other inhibitors of prostaglandins, can cause the following anomalies in the fetus:

- Cardiopulmonary (premature closure of the arterial duct and pulmonary hypertension)

- Kidney dysfunction up to the development of renal failure with malnutrition

- Elongation of bleeding time in the mother and fetus by the end of pregnancy. This effect can be observed even with low doses of ASA.

Lactation

Salicylates and their metabolites penetrate into breast milk in small amounts.

When breastfeeding a child, the use of drugs containing ASA is contraindicated.

Dosing and Administration:

Adults and children over 15 years of age should be taken orally after meals, before dissolving in a glass of water.

With a painful syndrome of mild and moderate intensity and fever, a single dose is 1000 mg (corresponding to 2 effervescent tablets of the drug). The maximum single dose is 1000 mg. Intervals between doses of the drug should be at least 4 hours. The maximum daily dose should not exceed 3 g (6 tablets).

The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an anesthetic and more than 3 days - as an antipyretic.

Side effects:

Gastrointestinal tract: stomach ache; nausea; vomiting; heartburn; gastrointestinal bleeding, including latent, leading to the development of iron deficiency anemia; stomach ulcers and duodenal ulcers (including perforating); increased activity of hepatic transaminases.

Central nervous system and sensory organs: dizziness, tinnitus, hearing loss, headache (usually indicative of an overdose)

The system of hematopoiesis: lengthening the time of bleeding with the development of bleeding of different localization (nasal, gum, haemorrhagic purpura, etc.).

Allergic reactions: anaphylactic reactions, bronchial asthma, Quincke's edema, urticaria and other allergic skin reactions.

Overdose:

Overdose should be feared in elderly patients and in young children, for whom it can be fatal.

Symptoms

For a moderate overdose characteristic of noise in the ears, a sense of hearing loss, headache, dizziness, inhibition.

Symptoms can be controlled by lowering the dose of the drug.

For a severe overdose fever, hyperventilation, ketosis, respiratory alkalosis, metabolic acidosis, coma, cardiovascular shock, respiratory failure, severe hypoglycemia.

Emergency services

Urgent hospitalization in a specialized department for emergency therapy - gastric lavage, the appointment of activated charcoal, the determination of acid-base balance, alkaline diuresis to obtain pH values of urine within 7.5-8, forced alkaline diuresis,when the concentration of salicylate in blood over 500 mg / l (3.6 mmol / l) in adults and 300 mg / l (2.2 mmol / l) in children compensation fluid losses, symptomatic treatment.

With severe poisoning, hemodialysis is possible.

Interaction:

Combination with Methotrexate in a dose> 15 mg per week is contraindicated.

Combinations of drugs that are used with caution

Methotrexate in a dose of less than 15 mg / week: With simultaneous use of drugs, the hematological toxicity of methotrexate is increased because NSAIDs generally decrease the renal clearance of methotrexate, and salicylates in particular are displacing it from the bond with plasma proteins.

Anticoagulants (coumarin, heparin): with the simultaneous administration of ASA and indirect anticoagulants increases the risk of bleeding due to the suppression of platelet function, damage to the mucous membrane of the stomach and duodenum and the displacement of oral anticoagulants from their association with plasma proteins.

Other NSAIDs with salicylates in a high dose (> 3 g / day): while the use of drugs because of synergies increased risk of ulceration of the mucous membrane of the gastrointestinal tract and bleeding.

Urikozuric drugs (benzbromarone, probenecid): the therapeutic effect of uricosuric drugs decreases due to competitive tubular elimination of uric acid.

Digoxin: with simultaneous use of drugs increases the concentration digoxin in the plasma by reducing its excretion.

Antidiabetic drugs (insulin, sulfonylurea): is increasing hypoglycemic effect due to the fact that ASA in high dose has hypoglycemic properties and displaces sulfonylurea from the connection with plasma proteins.

Thrombolytics / antiplatelet drugs of other classes (ticlopidine): increased risk of bleeding.

Diuretics in combination with ASA in a dose of 3 g / day or more: the glomerular filtration decreases, due to a decrease in the synthesis of prostaglandins in the kidneys.

Systemic glucocorticosteroids (GCS) excluding hydrocortisone (used to treat Addison's disease): with simultaneous use of drugs the concentration of salicylates in the blood decreases, as the GCS enhances the elimination of salicylates

Angiotensin-converting enzyme (ACE) inhibitors: while simultaneous use of ACE inhibitors and ASA at a dose of 3 g / day or more, a decrease in the hypotensive effect of ACE inhibitors is noted, due to a decrease in glomerular filtration.

Valproic Acid: ASA disrupts the association of valproic acid with plasma proteins, resulting in increased toxicity.

Alcohol: when combined with ASA, the damaging effect on the mucous membrane of the gastrointestinal tract increases and the bleeding time is prolonged.

Special instructions:

Children should not be prescribed drugs containing acetylsalicylic acid, since In case of a viral infection, the risk of developing Reye syndrome increases. Symptoms Reye syndrome is a prolonged vomiting, acute encephalopathy, an increase liver.

ASA can provoke the development of bronchospasm and cause an attack of bronchial asthma or other allergic reactions. Risk factors are the patient's history of bronchial asthma, hay fever, nasal polyposis, chronic respiratory diseases, and allergic reactions to other drugs (eg, itching, urticaria, other skin reactions).

The ability of ASA to inhibit platelet aggregation can lead to increased bleeding during and after surgery (including minor surgical interventions, such as tooth extraction). The risk of bleeding increases with the use of ASA in a high dose. The haemorrhagic effect of ASA persists for 4-8 days after its withdrawal.

In low doses, ASA reduces uric acid excretion, which can cause gout in patients with an initially low level of excretion.

Long-term use of analgesics can lead to the formation of a headache of addiction, which occurs during the withdrawal of analgesics.

The usual use of analgesics (especially combinations of various analgesics) can lead to the development of severe kidney damage - analgesic nephropathy.

In 1 dose of the drug contains 1086 mg of sodium, which should be borne in mind when using the drug in patients on a diet that requires the restriction of salt intake.

Effect on the ability to drive transp. cf. and fur:Does not affect.

Form release / dosage:Tablets effervescent 500 mg.

Packaging:

2 tablets per strip of paper, laminated with aluminum foil.For 6 and 12 strips together with instructions for use in cardboard pack.

Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N016188 / 01

Date of registration:10.12.2009 / 09.06.2016

Expiration Date:Unlimited

The owner of the registration certificate:BAYER, AO BAYER, AO Russia

Manufacturer: & nbsp

BAYER, CJSC Russia

Representation: & nbspBAYER, AOBAYER, AO

Information update date: & nbsp27.09.2017

Illustrated instructions

Instructions

Aspirin® Express (Aspirin® Express)