medicalmeds.eu Medicines Non-steroidal anti-inflammatory drug (NPVP). Acetylsalicylic acid

Acetylsalicylic acid

Producer: JSC Tatkhimfarmpreparaty Russia

Code of automatic telephone exchange: N02BA01

Release form: Firm dosage forms. Tablets.

Indications to use: Hyper thermal syndrome (Fever). Back pain. Dentagra. Headache. Pain syndrome.

General characteristics. Structure:

Active ingredient: acetylsalicylic acid of 250 mg or 500 mg.
Excipients: potato starch, stearic acid, citric acid, talc.

Description. Tablets of white color, slightly marble, ploskotsilindrichesky with risky and a facet, inodorous or with a slight characteristic smell.

Pharmacological properties:

Pharmacodynamics. Drug has anesthetic, febrifugal antiinflammatory effect that is caused by inhibition of enzymes of the cyclooxygenases participating in synthesis of prostaglandins. Acetylsalicylic acid inhibits aggregation of thrombocytes, blocking A2 thromboxane synthesis.

Pharmacokinetics. At intake absorption full. During absorption is exposed to system elimination in a wall of intestines and in a liver it (is deacetylated). The Rezorbirovanny part is quickly hydrolyzed by special esterases therefore T1/2 - no more than 15-20 min.

In an organism circulates (for 75-90% in connection with albumine) and it is distributed in fabrics in the form of anion of salicylic acid.

TCmax is 2 h. Serumal level of salicylates is very variable. Salicylates easily get into many fabrics and liquids of an organism, including into spino-brain, peritoneal and synovial liquids. Penetration into a cavity of a joint accelerates in the presence of a hyperemia and hypostasis and is slowed down in a proliferative phase of an inflammation. In small amounts salicylates are found in brain fabric, traces - in bile, sweat, excrements. When developing acidosis the most part of salicylic acid turns into not ionized acid which is well getting into fabrics including into a brain. Quickly passes through a placenta, in small amounts it is removed with breast milk.

It is metabolized preferential in a liver with formation of 4 metabolites found in many fabrics and urine.

It is removed preferential by active secretion in tubules of kidneys in not changed look (60%) and in the form of metabolites. Removal of not changed salicylate depends on urine pH (when alkalifying urine the ionizirovaniye of salicylates increases, their reabsorption worsens and considerably removal increases). Speed of removal depends on a dose: at reception of small doses of T1/2 - 2-3 h, with increase in a dose can increase up to 15-30 h.

Indications to use:

Symptomatic treatment of a pain syndrome: a headache (including at an abstinence syndrome), a dentagra, a pharyngalgia, a dorsodynia and muscles, a joint pain, pain at periods.

The increased body temperature at catarrhal and other infectious and inflammatory diseases (at adults and children 15 years are more senior).

Route of administration and doses:

Inside, to adults and children 12 years are more senior: the single dose makes 0,25-0,5 g, the maximum single dose - 1,0 g (2 tablets on 0,5 g), maximum daily - a single dose if necessary it is possible to accept 3,0 g (6 tablets on 0,5 g) 3-4 times a day with an interval not less than 4 hours.

To children, except for the acute respiratory diseases caused by viral infections because of risk of development of a syndrome to Reja (encephalopathy and acute fatty dystrophy of a liver with acute development of a liver failure): a single dose for children aged from 3 years - 0,125 g (1/2 tablets of 250 mg), since 6-year age it is possible to appoint in tablets 0,25 g to reception.

Route of administration. Drug should be accepted after food, washing down with water, milk or alkaline mineral water.

Frequency and time of reception: if necessary it is possible to accept a single dose 3-4 times a day with an interval not less than 4 hours. Regular observance of the mode of administration of drug allows to avoid sharp temperature increase and to reduce intensity of a pain syndrome.

Treatment duration (without consultation with the doctor) should not exceed 7 days at appointment as anesthetic and more than 3 days - as an antipyretic.

Features of use:

Acetylsalicylic acid can cause a bronchospasm, an attack of bronchial asthma or other hypersensitivity reactions. Risk factors are existence of bronchial asthma, polyps of a nose, fever, chronic bronchopulmonary diseases, allergy cases in the anamnesis (allergic rhinitises, an enanthesis).

Acetylsalicylic acid can increase tendency to bleeding that is connected with its inhibiting influence on aggregation of thrombocytes. It should be considered in need of surgical interventions, including such small interventions as an odontectomy. Before surgical intervention, for reduction of bleeding during operation and in the post-operational period, it is necessary to cancel administration of drug in 5-7 days and to inform the doctor.

Children cannot appoint the drugs containing acetylsalicylic acid as in case of a viral infection the risk of emergence of a syndrome to Reja increases. Syndrome symptoms to Reja are long vomiting, acute encephalopathy, increase in a liver.

In need of use of drug in the period of a lactation breastfeeding should be stopped.

At treatment of vascular diseases the daily dose of acetylsalicylic acid makes from 75 to 300 mg.

Acetylsalicylic acid reduces removal of uric acid from an organism that can become the reason of a bad attack of gout at predisposed patients.

Influence of administration of drug on control of the vehicle and other mechanisms is not revealed.

Side effects:

From digestive tract: abdominal pains, heartburn, nausea, vomiting, explicit (vomiting with blood, a tar-like chair) or the hidden symptoms of gastrointestinal bleeding which can lead to an iron deficiency anemia, erosive cankers (including with perforation) digestive tract, isolated cases - abnormal liver functions (increase in hepatic transaminases).
From the central nervous system: dizziness, a sonitus (usually are overdose signs).
From system of a hemopoiesis: increase in risk of bleeding that is a consequence of influence of acetylsalicylic acid on aggregation of thrombocytes.

Interaction with other medicines:

Combined use:

with a methotrexate in a dose of 15 mg a week or more: hemolitic cytotoxicity of a methotrexate increases (the renal clearance of a methotrexate decreases and the methotrexate is replaced with salicylates in connection with proteins of a blood plasma);
with anticoagulants, for example, heparin: the risk of bleeding owing to inhibition of function of thrombocytes, damages mucous digestive tract, replacement of anticoagulants (peroral) of communication with proteins of a blood plasma increases;
with other non-steroidal anti-inflammatory drugs: as a result of synergy interaction, the risk of developing of an ulcer and bleeding of a stomach increases;
with uricosuric medicines, for example бензбромарон: reduces uricosuric effect;
with digoxin: concentration of digoxin increases owing to decrease in renal excretion;
with hypoglycemic drugs, for example insulin: hypoglycemic effect of hypoglycemic drugs owing to hypoglycemic effect of acetylsalicylic acid increases;
with drugs of group of trombolitik: the risk of developing of bleeding increases;
with system glucocorticosteroids, excepting the hydrocortisone used as replacement therapy at Addison's disease: at use of glucocorticosteroids the level of salicylates in blood due to increase in removal of the last decreases;
with angiotensin-converting enzyme inhibitors: glomerular filtering at the expense of inhibition of prostaglandins decreases and, as a result, the anti-hypertensive effect decreases;
with valproic acid: toxicity of valproic acid increases;
with ethanol (alcoholic beverages): the risk of the damaging influence on mucous digestive tract increases and the risk of GIT bleeding increases;
strengthens effects of narcotic analgetics, trombolitik and inhibitors of aggregation of thrombocytes, streptocides (including co-trimoxazole);
increases concentration of barbiturates, lithium salts in plasma;
the antacids containing magnesium and/or aluminum slow down and worsen absorption of acetylsalicylic acid;
myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

hypersensitivity to acetylsalicylic acid and other NPVP or other components of drug;
digestive tract erosive cankers (in an aggravation phase);
hemorrhagic diathesis;
the combined use of a methotrexate in a dose of 15 mg a week and more;
combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid;
pregnancy (I and III trimester), breastfeeding period.
children's age up to 3 years for tablets on 250 mg, up to 6 years for tablets on 500 mg.

Drug is not appointed to children up to 15 years with the acute respiratory diseases caused by viral infections because of risk of development of a syndrome to Reja (encephalopathy and acute fatty dystrophy of a liver with acute development of a liver failure). With care - at the accompanying therapy by anticoagulants, gout, a peptic ulcer of a stomach and/or a duodenum (in the anamnesis), including a chronic or recurrent current of a peptic ulcer, or episodes of gastrointestinal bleedings; renal and/or liver failure, deficit glyukozo-6-fosfatdegidrogenazy; a hyperuricemia, bronchial asthma, a chronic obstructive pulmonary disease, hay fever, nose polyposes, a medicinal allergy, a concomitant use of a methotrexate in a dose of 15 mg/week, pregnancy (the II trimester).

Overdose:

Symptoms: Overdose of moderate severity: nausea, vomiting, sonitus, hearing disorder, headache, dizziness and confusion of consciousness. These symptoms pass at a drug dose decline.

Heavy overdose: fever, a hyperventilation, ketoacidosis, a respiratory alkalosis, a metabolic acidosis, a coma, cardiogenic shock, respiratory insufficiency, the expressed hypoglycemia.

Treatment: hospitalization, gastric lavage, reception of absorbent carbon, monitoring of acid-base balance, an alkaline diuresis to receive рН urine between 7,5-8 (the forced alkaline diuresis is considered reached if concentration of salicylate in a blood plasma makes more than 500 mg/l (3,6 mmol/l) at adults or children have 300 mg/l (2,2 mmol/l)), a hemodialysis, compensation of loss of liquid, symptomatic therapy.

Storage conditions:

To store in the dry place, at ^{a temperature not higher than 25 ° C}. To store in the place, unavailable to children.
Period of validity - 4 years. Not to use after the term specified on packaging.