ASPIRIN 1000

Active material: Acetylsalicylic acid
When ATH: N02BA01
CCF: NPVC, used when experiencing migraines
ICD-10 codes (testimony): G43
When CSF: 05.01.01.01
Reg. room: P # 016188/01
Registration Date: 08.12.06
Manufacturer: BAYER CONSUMER CARE AG (Switzerland)

Pharmaceutical form, composition and packaging

◊ Effervescent tablets white, round, flat, beveled to the edge, engraved in the form of the logo (“Bayero” cross) one side.

Excipients: sodium citrate, anhydrous, sodium carbonate monosubstituted, Citric acid anhydrous, anhydrous sodium carbonate,.

2 PC. – strips of paper laminated (6) – packs cardboard.
2 PC. – strips of paper laminated (12) – packs cardboard.

Pharmacological action

NSAIDs. Has analgesic, antipyretic and anti-inflammatory effect. The mechanism of action is irreversible inhibition of COX – enzyme, regulating the synthesis of prostaglandins (e)₂, I₂ and thromboxane and₂. One of the main mechanisms of headaches when migrenoznom fit is aseptic neurogenic inflammation of blood vessels and the dura mater. Acetylsalicylic acid, inhibiting the synthesis of prostaglandins, which are mediators of inflammation, reduces pain receptors irritation of the trigeminal nerve. On the other hand, acetylsalicylic acid inhibits in endotelia receptacles nitric oxide synthesis, who is involved in the mechanism of initiation and maintenance of attack of headache and migraines.

Pharmacokinetics

Absorption

After intake of acetylsalicylic acid is rapidly and completely absorbed from the digestive tract. In the period immediately following the absorption and acetylsalicylic acid turns into a major active metabolite – salicylic acid. ASK PRICE reaches maximum concentration in the blood plasma through 10-20 minutes, and salicylic acid – through 0.3-2 no.

Distribution

Plasma protein binding of acetylsalicylic acid and salicylic acid is about 80%. Distribution in the tissues quick.

Metabolism

Salicylic acid is metabolized in the liver with the formation of metabolites – salicilurata, salicilovofenol'nogo glucuronide, salicilacilovogo glucuronide, gentizinovoj and gentizurovoj acids. Provided with breast milk, It crosses the placental barrier.

Deduction

Elimination of salicylic acid is dozozawisimy nature. T_1/2 It varies between 2-3 h when taking the drug at low doses to approximately 15 h when administered in high doses. Salicylic acid and its metabolites excretiruyutza, mainly, kidney.

Testimony

-symptomatic treatment headache bouts with migraines.

Dosage regimen

The drug is taken orally after meal, before taking to dissolve in a glass of water.

Appoint one dose 1 g (matches 2 Fizzy tablets.). If necessary, you can repeat the reception via 4-8 no. The maximum daily dose is 3 g (6 tab.).

Patients should not take the drug more 3 days without consulting a doctor. If frequent migraine attacks, and their frequency increases or the symptoms persist for a long time, the patient should consult a doctor, can optionally be assigned alternative treatment.

Side effect

From the digestive system: stomach ache, nausea, vomiting, heartburn, gastrointestinal bleeding (incl. hidden, leading to the development of iron-deficiency anaemia), ulcers stomach and duodenal ulcers (including perforativnye), increase in liver transaminases.

From the central and peripheral nervous system: dizziness, noise in ears, hearing disorder, headache (are usually signs of overdose).

From the hematopoietic system: prolonged bleeding with the development of the bleeding of various localization (bow, gums, gemorragicheskaya purpura).

Allergic reactions: anaphylactic reactions, bronchial asthma, angioedema, urticaria and other allergic skin reactions.

Contraindications

- Ulcerative lesions GIT;

- Gyemorragichyeskii diatyez;

- Bronchial asthma, induced intake of salicylates, and NSAIDs;

- The combined use with methotrexate 15 mg per week;

- Severe renal insufficiency;

- Severe hepatic impairment;

— severe cardiac insufficiency of the decompensation;

- I and III trimesters of pregnancy;

- Lactation;

children and adolescents under the age of 15 years with a viral URTI, because of the risk of Reye's syndrome (acute encephalopathy and fatty degeneration of the liver with the development of acute liver failure);

- Hypersensitivity to the drug;

-hypersensitivity to other salicylates.

FROM caution the drug should be used in patients, receiving concomitant treatment with anticoagulants; with indications in history to defeat ulcerous STOMACH, including chronic or recurrent ulcer disease, on gastro-intestinal bleeding, allergic reactions to NSAIDS and other drugs, on bronchial asthma, hay fever, nasal polyposis, chronic respiratory diseases; in patients with impaired kidney and liver, gout, hyperuricemia; in the II trimester of pregnancy.

Pregnancy and lactation

In II and III trimestrah pregnancy use of all drugs, containing acetylsalicylic acid is contraindicated. In the second trimester of pregnancy can be assigned sporadically acetylsalicylic acid. As a long-term therapy does not apply.

Use in the third trimester of pregnancy in a dose of acetylsalicylic acid 500 mg / day, like other inhibitors of prostaglandin synthesis, can cause the fetus following anomalies: cardiopulmonary (premature closure of the ductus arteriosus and pulmonary hypertension); kidney dysfunction up to development of renal failure with malovodiem; prolonged bleeding in the mother and fetus to the end of pregnancy. This effect can be observed even when applied at low doses of acetylsalicylic acid.

Salicylates and their metabolites in small amounts are excreted in breast milk. During breastfeeding supplementation, containing acetylsalicylic acid is contraindicated.

Cautions

Acetylsalicylic acid can provoke development of bronchospasm and trigger an attack of bronchial asthma or other allergic reactions. Risk factors is the presence of the patient of bronchial asthma in history, hay fever, nasal polyposis, chronic respiratory diseases, and allergic reactions to other drugs (eg, itch, hives, other skin reactions). Acetylsalicylic acid's ability to suppress agregatia platelets may cause excessive bleeding during and after surgery (including small surgical intervention, eg, tooth extraction). The risk of bleeding is increased by the use of acetylsalicylic acid in high dose. Hemorrhagic effect of acetylsalicylic acid is stored within 4-8 days after its abolition.

In the low-dose acetylsalicylic acid reduces the excretion of uric acid, What can cause the development of gout in patients with initially low levels of its excretion. The long-term prescription of analgesics may lead to headaches addiction, that occurs during the repeal of analgesics. Habitual use of analgesics (especially combinations of different analgesics) can lead to severe kidney failure – analgetic nephropathy.

IN 1 Dose Aspirin^®1000 contains 1086 mg of sodium, that should be considered when applying the drug in patients, staying on a diet with salt restriction.

Use in Pediatrics

Contraindicated medications use in children, containing acetylsalicylic acid, because in case of a virus infection increases the risk of getting Reye's syndrome (prolonged vomiting, acute encephalopathy, enlargement of the liver).

Effects on ability to drive vehicles and management mechanisms

Aspirin^®1000 does not affect the ability to drive vehicles and Office moving mechanisms.

Overdose

In patients older and younger children acetylsalicylic acid overdose can be deadly.

Symptoms: moderate overdose – noise in ears, feeling a decrease in hearing, headache, dizziness, lethargy. Severe overdose – fever, hyperventilation, ketosis, respiratory alkalosis, metabolic acidosis, coma, cardiovascular shock, respiratory insufficiency, severe hypoglycemia.

Treatment: moderate overdose symptoms can be controlled dose drug.

Severe overdose require urgent hospitalization in a specialized ITD – gastric lavage, appointment of activated carbon, Determination of acid-base balance, alkaline diuresis up to getting urine pH values within the 7.5-8, forced alkaline diuresis, When the concentration in the blood salicilatov more 500 mg / l (3.6 mmol / l) adults and 300 mg / l (2.2 mmol / l) children, reimbursement loss of fluids, symptomatic therapy. In severe poisoning may have a kidney dialysis.

Drug Interactions

Is a combination of aspirin^®1000 in a dose of methotrexate 15 mg per week.

The caution should be applied to Aspirin^®1000 If the following combinations.

Together with the use of methotrexate dose of less than 15 mg a week increases the hematological toxicity methotrexate because the, that NSAIDS as a whole reduces kidney klirens methotrexate, and salicylates, in particular, displace it from the blood plasma.

Together with other salicilatami due to synergy of education increases the risk of ulcerative lesions of mucous membrane STOMACH and bleeding.

Acetylsalicylic acid reduces the therapeutic effect of urikozuricheskih drugs (ʙenzʙromaron, probenecid) due to the competitive tubuljarnogo uric acid.

If you are applying to concentrations of Digoxin in plasma by reducing its excretion.

There has been a strengthening of hypoglycemic action of insulin and a hypoglycemic drugs sulfonylureas derivatives due to the fact, that acetylsalicylic acid in high dose has hypoglycemic properties and displaces sul'fonilmochevinu from the blood plasma.

Together with the use of thrombolytic drugs/drugs antitrombocitarnymi other classes (ticlopidine) increased risk of bleeding.

When combined with diuretic acetylsalicylic acid dose 3 g/d and more reduced glomeruljarnaja filtering, due to inhibition of prostaglandin synthesis in the kidneys.

Together with the use of systemic CORTICOSTEROIDS, with the exception of hydrocortisone (applied for the treatment of Addison disease), concentrations of Salicylates in plasma reduced, because the SCS reinforce eliminatiu salicylates.

Together with the use of ACE inhibitors and acetylsalicylic acid in the dose 3 g/d and more declining gipotenzivnogo effect of ACE inhibitors, as a result of reduced glomeruliarna filtering.

Acetylsalicylic acid violates tying valproeva acid plasma protein, which leads to the strengthening of its toxicity.

With a combination of acetylsalicylic acid with ethanol intensifies the damaging effect on the mucous membrane of the stomach and increases bleeding time.

Conditions of supply of pharmacies

The drug is resolved to application as an agent Valium holidays.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.