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

Excipients: potato starch 16.2 mg or 81.0 mg, stearic acid 1.2 mg or 6.0 mg, silicon dioxide colloid (aerosil) 1.2 mg or 6.0 mg, povidone-K25 1.4 mg or 7, 0 mg.

Description:Tablets are flat-cylindrical white, light "marbling" and weak characteristic odor are allowed.

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

ATX: & nbsp

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

Pharmacodynamics:Has anti-inflammatory, analgesic and antipyretic effects associated with the suppression of cyclooxygenase 1 and 2, regulating the synthesis of prostaglandins. As a result, prostaglandins are not formed, which provide the formation of edema and hyperalgesia. Reduction of the content of prostaglandins (mainly E1) in the center of thermoregulation leads to a decrease in body temperature due to expansion,vessels of the skin and increased sweating. The analgesic effect is due to both central and peripheral action.

Pharmacokinetics:

At intake the absorption is complete. During absorption, it undergoes systemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is rapidly hydrolyzed by plasma cholinesterases and albumin esterase, so T1 / 2 is no more than 15-20 minutes. In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. FROMmah is reached in about 2 hours. Easily penetrates into many tissues and body fluids, including. into the cerebrospinal fluid, peritoneal and synovial fluid. Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. In small amounts, salicylates are found in the nervous tissue, traces in bile, sweat, feces. When acidosis occurs, most of the salicylate is converted to a non-ionized acid that penetrates well into the tissue, incl. in the brain. Rapidly passes through the placenta, in small quantities is excreted in breast milk.

Metabolized mainly in the liver with the formation of 4 metabolites, found in many tissues and urine.

It is excreted mainly by active secretion in the renal tubules in the form of actually salicylic acid (60%) and its metabolites. Removal of unchanged salicylate depends on the pH of the urine (with alkalization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). The rate of excretion depends on the dose: for small doses of T1 / 2 2-3 hours, with an increase in the dose may increase to 15-30 hours. Newborn salicylate elimination is much slower than in adults.

Indications:

- Moderately or mildly expressed pain syndrome of various origins (headache, toothache, migraine, neuralgia, arthralgia, lumbago, radicular syndrome, muscle pain, algodismenorea).

- The raised temperature of a body at cold and other infectious-inflammatory diseases (at adults and children is more senior 15 years).

Contraindications:

- Hypersensitivity to acetylsalicylic acid, acid and other non-steroidal anti-inflammatory drugs (NSAIDs) or other components of the drug;

- erosive-ulcerative lesions of the gastrointestinal tract (GIT) (in the phase of exacerbation);

- gastrointestinal bleeding;

- hemorrhagic diathesis;

- simultaneous reception of methotrexate in a dose of 15 mg per week or more;

- a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid;

- The bronchial asthma, induced by the intake of salicylates and other NSAIDs;

- pregnancy (I and III trimester), the period of breastfeeding;

- children under 3 years for tablets of 100 mg, up to 6 years for tablets of 500 mg.

The drug is not prescribed for children under 15 with acute respiratory infections caused by viral infections, because of the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute development of liver failure).

Carefully:With concomitant anticoagulant therapies, gout, peptic ulcer and / or duodenal ulcer (in the anamnesis), including chronic or recurrent peptic ulcer disease, or episodes of gastrointestinal bleeding; with renal and / or hepatic insufficiency, deficiency of glucose-6-phosphate dehydrogenase; hyperuricemia, bronchial asthma, chronic obstructive pulmonary disease, hay fever,polyposis of the nose, drug allergy, simultaneous reception of methotrexate in a dose of less than 15 mg per week, pregnancy (II trimester).

Pregnancy and lactation:

Acetylsalicylic acid has a teratogenic effect; when applied in the first trimester leads to the development of cleavage of the upper palate; in the III trimester causes inhibition of labor (inhibition of the synthesis of prostaglandins), premature closure of the arterial duct in the fetus; hyperplasia of pulmonary vessels and hypertension in the "small" circle of blood circulation. The drug is contraindicated for use in I and III trimester of pregnancy. Reception of the drug in the II trimester is possible if the potential benefit to the mother exceeds the risk to the fetus.

Excreted in breast milk. If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside. The drug should be taken after meals, washed down with water, milk or alkaline mineral water.

Adults and children over 12 years of age: a single dose of 250-500 mg, a maximum single dose of 1000 mg (2 tablets of 500 mg), a maximum daily dose of 3000 mg (6 tablets of 500 mg), a single dose, if necessary, can be taken 3-4 once a day with an interval of at least 4 hours.

Children aged 3 years, with the exception of acute respiratory infections caused by viral infections, because of the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute development of liver failure), single dose is 100 mg; from the age of 6 can be prescribed in tablets of 250 mg (1/2 tablet of 500 mg) per reception.

Frequency and time of admission: a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Regular adherence to the regimen allows you to avoid a sharp increase in temperature and reduce the intensity of the pain syndrome.

The duration of treatment (without consulting a doctor) should not exceed 5 days with an appointment as an anesthetic and more than 3 days - as an antipyretic.

Side effects:

From the gastrointestinal tract: nausea, decreased appetite, gastralgia, diarrhea.

On the part of the hematopoiesis system: thrombocytopenia, anemia, leukopenia, increased coagulation time.

Allergic reactions: skin rash, angioedema, bronchospasm.

Other: impaired liver and / or kidney function; Reye syndrome (encephalopathy and acute fatty liver dystrophy with rapid development of liver failure). Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, an increase liver.

With prolonged use, dizziness, headache, vomiting, erosive and ulcerative lesions of the digestive tract, hypocoagulation, bleeding (including in the gastrointestinal tract), visual impairment, decreased ear aches, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with hypercreatininemia and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of chronic heart failure, edema, increased activity of "liver" transaminases.

If you experience "similar symptoms, it is recommended that you stop taking the medication and contact your doctor immediately.

Overdose:

May occur after a single dose of a large dose or with prolonged use. If a single dose is less than 150 mg / kg, acute poisoning is considered easy, 150-300 mg / kg - moderate and with higher doses - heavy.

Symptoms:

With mild poisoning - salicylism syndrome (nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache, general malaise, fever - a poor prognostic sign in adults). Severe poisoning - hyperventilation of the lungs of the central genesis, respiratory alkalosis, metabolic acidosis, confused consciousness, drowsiness, collapse, convulsions, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis - dyspnea, choking, cyanosis, cold sticky sweat; With increased intoxication, paralysis of respiration and disconnectionoxidative phosphorylation causing respiratory acidosis. In chronic overdose, the concentration in the plasma is poorly correlated with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly with more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicylism are not always noticeable, so it is advisable to periodically determine the salicylate content in the blood: a concentration above 70 mg% indicates moderate or severe poisoning; above 100 mg% - about extremely severe, prognostically unfavorable.With moderate and severe poisoning, hospitalization is necessary.

Treatment:

Provocation of vomiting, the appointment of activated carbon, laxatives, constant monitoring of acid-base state and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate solution or sodium lactate. The increase in reserve alkalinity increases the excretion of acetylsalicylic acid due to alkalinization of urine.

The alkalinization of urine (shown at the level of salicylates above 40 mg%, is provided by intravenous infusion of sodium bicarbonate - 88 mEq in 1 L of 5% glucose solution, at a rate of 10-15 ml / kg / h), recovery of circulating blood volume and induction of diuresis is achieved by the introduction of bicarbonate in the same dose and dilution, repeated 2-3 times); it should be borne in mind that intensive fluid infusion of the elderly can lead to pulmonary edema. It is not recommended to use acetosolamide for alkalinization of urine (can cause acidemia and enhance the toxic effect of salicylates). Hemodialysis is indicated at a salicylate level of more than 100-130 mg%, and in patients with chronic poisoning - 40 mg% and lower in the presence of indications (refractory acidosis, progressive deterioration of the condition, severe central nervous system damage, pulmonary edema and renal failure). With pulmonary edema, artificial ventilation of the lungs with a mixture enriched with oxygen is shown in the positive pressure mode at the end of the exhalation; To treat edema of the brain, hyperventilation and osmotic diuresis are used.

Interaction:

With the combined use of acetylsalicylic acid with methotrexate at a dose of 15 mg per week or more, the hemolytic cytotoxicity of methotrexate (decreased renal clearance of methotrexate and methotrexate is replaced by salicylates in association with blood plasma proteins).

With the combined use of acetylsalicylic acid with anticoagulants, for example, heparin, the risk of bleeding increases due to impaired platelet function, damage to the mucosa of the gastrointestinal tract, and the displacement of anticoagulants (indirect) from binding to plasma proteins.

With the combined use of acetylsalicylic acid with other non-steroidal anti-inflammatory drugs as a result of synergistic interaction, the risk of ulcers and bleeding from the stomach and duodenum increases.

With the combined use of acetylsalicylic acid with uricosuric drugs, for example, benzbromarone, the uricosuric effect of the latter decreases.

With the combined use of acetylsalicylic acid with digoxin, the concentration of digoxin is increased due to a decrease in renal excretion.

When combined use of acetylsalicylic acid with hypoglycemic drugs increases the hypoglycemic effect of the latter due to hypoglycemic action of acetylsalicylic acid.

With the combined use of acetylsalicylic acid with drugs of the thrombolytics group, the fibrinolytic effect of the latter increases and the risk of bleeding increases.

When combined use of acetylsalicylic acid with glucocorticosteroids, except hydrocortisone, used as a substitute therapy for Addison's disease, reduces the concentration of salicylates in the blood by increasing the excretion of the latter.

With the combined use of acetylsalicylic acid with angiotensin converting enzyme inhibitors, glomerular filtration is reduced by inhibiting the synthesis of prostaglandins and, as a consequence, the antihypertensive effect is reduced.With the combined use of acetylsalicylic acid with valproic acid, the toxicity of valproic acid increases.

With the combined use of acetylsalicylic acid with glucocorticosteroids, ethanol (alcoholic beverages) and ethanol-containing drugs, the risk of damaging effects on the gastrointestinal mucosa increases, and the risk of developing gastrointestinal bleeding increases.

Acetylsalicylic acid enhances the effects of narcotic analgesics, indirect anticoagulants and antiaggregants, sulfonamides (including co-trimoxazole - increases their activity and toxicity), triiodothyronine (increases activity and increases the risk of side effects of the latter).

Acetylsalicylic acid reduces the effect of antihypertensive drugs, diuretics (spironolactone, furosemide).

Acetylsalicylic acid increases the concentration of barbiturates and lithium salts in plasma.

Antatsida containing magnesium and / or aluminum, slow down and worsen the absorption of acetylsalicylic acid.

Myelotoxic drugs increase the manifestation of hematotoxicity of acetylsalicylic acid.

Special instructions:

Currently, the use of acetylsalicylic acid as an anti-inflammatory drug in a daily dose of 5-8 g is limited due to the high probability of side effects from the gastrointestinal tract (NSAIDs). Acetylsalicylic acid can cause bronchospasm, an attack of bronchial asthma, or other reactions of hypersensitivity. Risk factors are the presence of bronchial asthma, polyps of the nose, fever, chronic bronchopulmonary diseases, cases of allergy in the anamnesis (allergic rhinitis, rashes on the skin). Acetylsalicylic acid can increase the tendency to bleeding, which is due to its inhibitory effect on platelet aggregation. This should be considered when surgical interventions are required, including, such small interventions as tooth extraction. Before surgery, to reduce bleeding during surgery and in the postoperative period, you should cancel taking the drug for 5-7 days and inform the doctor.

Acetylsalicylic acid reduces the excretion of uric acid from the body,which can cause an acute attack of gout in predisposed patients.

During treatment should refrain from taking ethanol.

Effect on the ability to drive transp. cf. and fur:There was no evidence of the effect of drug administration on vehicle management and other mechanisms.

Form release / dosage:Tablets of 100 mg and 500 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

1 circuit cell pack together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LS-000994

Date of registration:19.05.2011

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp27.09.2017

Illustrated instructions

Instructions

Aspinate® (Aspinat®)