Acetilsalicylic kislota-Darnitsa

General characteristics. Structure:

Active ingredient: acetylsalicylic acid;

1 tablet contains 500 mg of acetylsalicylic acid (in terms of 100% dry matter);

excipients: potato starch; citric acid, monohydrate.

Pharmacological properties:

Acetylsalicylic acid – the non-steroidal anti-inflammatory drug derivative of salicylate. The main mechanism of effect of acetylsalicylic acid is the inactivation of TsOG enzyme (cyclooxygenase) thereof products of mediators of an inflammation decrease: prostaglandins, prostacyclins and thromboxane. Decrease in synthesis of prostaglandins leads to reduction of their influence on the centers of thermal control that leads to decrease in temperature increased owing to an inflammation. Reduces the sensibilizing influence of prostaglandins on nerve terminations, sensitive to pain, that reduces their sensitivity to pain mediators. Irreversible oppression of synthesis of A2 thromboxane in thrombocytes predetermines antiagregantny effect of acetylsalicylic acid.

The pharmacodynamics to acetilsalicylic acid depends on a daily dose:

small doses – 30-325 mg – cause braking of aggregation of thrombocytes;

average doses – 1,5-2 g – have analgeziruyushchy and febrifugal effect;

high doses – 4 g – render antiinflammatory effect.

In a dose less than 4 g acetylsalicylic acid detains excretion of uric acid.

At intake it is almost completely absorbed from digestive tract. Time of achievement of the maximum concentration in a blood plasma (Tmax) makes 10-20 min. Tmax of the general salicylate which is formed owing to metabolism, makes 0,3-2 hours. Extent of linkng with proteins of a blood plasma makes 49-70%. For 50% it is metabolized at primary passing through a liver. The glycylconjugate of salicylic acid is formed. It is brought out of an organism through kidneys in the form of metabolites. The elimination half-life (T1/2) makes 20 min. T1/2 for salicylic acid – about 2 h. Gets into breast milk, synovial fluid, into liquor.

Indications to use:

Symptomatic treatment of a pain syndrome of weak and average intensity of various genesis (including inflammatory); feverish states; rheumatic diseases.

Route of administration and doses:

Acetilsalicylic kislotu-Darnitsa apply to adults and children aged from 12 years. Drug is accepted inside, after food. An interval between administrations of drug – not less than 4-8 hours.

At a feverish and pain syndrome accept 500-1000 mg (1-2 tablets) 3-4 times a day. The daily dose should not exceed 4 g (8 tablets).

Not to apply more than 3-5 days without consultation with the doctor.

Features of use:

Acetilsalicylic kislotu-Darnitsa it is necessary to apply with extra care in the following cases: individual hypersensitivity to other analgetics / to anti-inflammatory drugs and existence of other types of an allergy; gastrointestinal ulcers in the anamnesis, and also a chronic or recurrent peptic ulcer or gastrointestinal bleedings; at the accompanying treatment by anticoagulants; deterioration in function of kidneys; deterioration in function of a liver.

Because acetylsalicylic acid oppresses aggregation of thrombocytes, and this effect remains for several days after use, it can increase tendency to bleedings in time and after surgical interventions (including small operative measures, for example, an odontectomy). Before planned surgical interventions it is necessary to stop administration of drug in 5-7 days prior to operation.

In low doses acetylsalicylic acid reduces removal of uric acid therefore can provoke a gout attack at inclined patients.

Patients with a functional hepatic unsufficiency and kidneys a dose of drug need to reduce or increase an interval between receptions.

As acetylsalicylic acid, as well as all non-selective non-steroidal anti-inflammatory drugs, causes irritation of a mucous membrane of digestive tract, drug should be accepted only after food, washing down with water, alkaline mineral waters, Natrii hydrocarbonas solution (it is the best of all – milk).

At prolonged use of acetylsalicylic acid it is necessary to check availability of blood in Calais for identification of ulcerogenic action and to do blood tests (influence on aggregation of thrombocytes, some anticoagulating activity).

With care use drug for treatment of patients with allergic rhinitis, polipozy a nose, a small tortoiseshell.

Use during pregnancy or feeding by a breast.

Drug in this dosage is not used in Ι and ΙΙΙ pregnancy trimesters in view of threat of a perenashivaniye of pregnancy and weakening of pains at the time of delivery, and also the increased risk of development of cardiopulmonary toxicity (premature closing of ductus arteriosus), congenital anomalies and intracranial bleedings (especially at premature children).

Use of drug in ΙΙ a trimester of pregnancy is admissible only on doctor's orders taking into account a ratio advantage for mother/risk for a fruit, in the smallest effective doses and throughout perhaps shorter span.

As certain amounts of acetylsalicylic acid are distinguished in breast milk and can cause Ray's syndrome and dysfunctions of thrombocytes in babies, for a while treatment it is necessary to stop feeding by a breast.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

Influence is improbable, however it is necessary to consider a possibility of dizziness.

Children.

Drug in this dosage form and a dosage is applied to children aged from 12 years. There is a possible communication between use of acetylsalicylic acid to children and a syndrome to Reja. The syndrome to Reja represents quite rare disease which influences a brain and a liver and can be fatal (one of its signs vomiting which does not stop throughout a long time is). For this reason children cannot apply acetylsalicylic acid at the diseases which are followed by a hyperthermia if other is directly not specified by the doctor (for example, a disease of Kawasaki).

Side effects:

From the central nervous system: dizziness, headache, aseptic meningitis.

From sense bodys: sonitus, hearing loss.

From digestive tract: nausea, vomiting, pain in epigastric area, diarrhea, ulcerogenic action, erosive and cankers of a mucous membrane of a stomach and duodenum, gastrointestinal bleedings, gastrointestinal perforation, microhemorrhages, a melena.

From a liver and biliary tract: an abnormal liver function, hepatogenous encephalopathy, a tranzitorny liver failure with increase in level of transaminases of a liver.

Metabolic disturbances: hypoglycemia.

From blood: thrombocytopenia, anemia, leukopenia, eosinophilia, hemorrhagic syndrome, prothrombinopenia.

From a respiratory organs: asthma, a triad (the eosinophilic rhinitis recuring nose polyposes, hyperplastic sinusitis), not cardiogenic fluid lungs.

From an urinary system: renal failure.

Allergic reactions: a small tortoiseshell, various a dieback, skin rashes, an itch, a Quincke's disease, asthma, an acute anaphylaxis, a bronchospasm, at patients with bronchial asthma is observed increase and strengthening of attacks.

Interaction with other medicines:

Anticoagulants, peroral gipoglikemiziruyushchy drugs (sulphonylurea derivatives), non-steroidal anti-inflammatory drugs, antirheumatic means, triiodothyronine, antiepileptic drugs (Phenytoinum) – at simultaneous use with acetylsalicylic acid effect of these drugs amplifies (the probability of development of side reactions increases).

The methotrexate – use  together with acetylsalicylic acid of a methotrexate in a dose of 15 mg a week and more increases hematologic toxicity of a methotrexate (decrease in renal clearance of a methotrexate by antiinflammatory agents and replacement by methotrexate salicylates from communication with blood plasma proteins).

Caffeine, Metoclopramidum – raises absorption of acetylsalicylic acid in digestive tract.

Glucocorticoids, methotrexate and ethanol – the probability of ulcerogenic effect of acetylsalicylic acid and risk of developing of gastrointestinal bleedings increases.

Digoxin, barbiturates and salts of lithium – at simultaneous use with acetylsalicylic acid raises concentration of these drugs in a blood plasma.

Diuretics (Spironolactonum, furosemide), uricosuric means (Sulfinpyrazonum, пробенецид, Aethamidum), anti-hypertensive drugs (captopril, тенорик, анаприлин) – at simultaneous use the effect of these drugs is weakened.

It is not recommended to apply together with antiacid drugs.

Acetylsalicylic acid blocks zhelodochny alcohol dehydrogenase, than increases ethanol level in an organism.

Contraindications:

–       Hypersensitivity to acetylsalicylic acid, other salicylates or to any auxiliary component of drug;

–       existence in the anamnesis of instructions on asthma, urticaria or rhinitis which are caused by use of salicylates or substances with similar action, especially non-steroidal anti-inflammatory drugs;

–       active round ulcer of a stomach and duodenum;

–       hemorrhagic diathesis, hemophilia, the increased tendency to bleedings;

–       heavy abnormal liver functions and kidneys, heavy heart failure;

–       deficit glyukozo-6-fosfatdegidrogenazy;

–       the combined use with a methotrexate in a dose of 15 mg a week or is more (see the section "Interaction with Other Medicines and Other Types of Interactions");

–       Ι and ΙΙΙ pregnancy trimesters, feeding period breast;

–       children's age up to 12 years.

Overdose:

Toxicity of salicylates can be result of intoxication owing to prolonged use    of therapeutic  doses  or   acute  intoxication   (at  use  > 100 mg/kg/days more than two days) that potentially threatens life, from an accidental proglatyvaniye children to accidental poisoning.

Chronic poisoning with salicylates can pass asymptomatically as has no specific symptoms. Intoxication salicylates of moderate severity, or a salitsilizm, as a rule develops only after repeated use of high doses. Symptoms: dizziness, a sonitus, deafness, perspiration, nausea, vomiting, a headache and oppression of consciousness, can be controlled by a dose decline. The sonitus can arise at plasmatic concentration from 150 to 300 mkg/ml. Heavier side effects arise at concentration Bol of 300 mkg/ml.

The main feature of acute poisoning is heavy disturbance of acid-base balance which can differ with age and weight of intoxication. The most widespread sign at children is the metabolic acidosis. Weight of poisoning cannot be estimated, using only data of plasmatic concentration.

Absorption of acetylsalicylic acid can be slowed down because of braking of gastric emptying, formation of concrements in a stomach or owing to use of the drugs covered with a kishechnorastvorimy cover.

Acute management at poisoning with acetylsalicylic acid is defined by severity, a stage and clinical symptoms and answers standard methods of rendering acute management at poisonings. Priority actions have to be allocated for removal acceleration of medicine, and also recovery of electrolytic and acid-base balance.

Owing to complex pathophysiological effects, at poisoning with salicylates there can be following symptoms and laboratory changes.

Poisoning easy and moderate severity: tachypnea, hyperventilation, respiratory alkalosis, perspiration, nausea, vomiting. Datas of laboratory: alkalosis, alkali reaction of urine. Acute management: a gastric lavage, repeated purpose of absorbent carbon, the forced alkaline diuresis.

Serious poisoning: a respiratory alkalosis with a compensatory metabolic acidosis, a hyper pyrexia, feeling of a sonitus, deafness.

Respiratory system: from a hyperventilation, not cardiogenic fluid lungs to an apnoea and asphyxia; datas of laboratory – an alkalosis, alkali reaction of urine.

Cardiovascular system: from disturbances of a cordial rhythm, arterial hypotension to a cardiac standstill. Loss of liquid and electrolytes: dehydration, oliguria, renal failure. Datas of laboratory – a hypopotassemia, a hypernatremia, a hyponatremia, change of function of kidneys.

Disturbance of exchange of glucose, a ketosis is laboratory shown in the form of a hyperglycemia, a hypoglycemia (especially at children), increases in level of ketonic bodies.

Digestive tract: gastrointestinal bleedings. Changes from blood: from oppression of function of thrombocytes to coagulopathies. Datas of laboratory – lengthening of a prothrombin time, a prothrombinopenia. Neurologic: toxic encephalopathy and oppression of TsNS from weakness, oppressions of consciousness to a coma and an attack of spasms.

Acute management: a gastric lavage, repeated purpose of absorbent carbon, the forced alkaline diuresis, a hemodialysis in hard cases, infusion of liquid and electrolytes.

Storage conditions:

Period of validity. 4 years. To store in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in a blister strip packaging, on 1 blister strip packaging in a pack. On 10 tablets in a blister strip packaging without investment in a pack.