Aspinat

General characteristics. Structure:

Active agent: acetylsalicylic acid of 500 mg; 100 mg; 300 mg.

Pharmacological properties:

NPVS. Has antiinflammatory, analgeziruyushchy and febrifugal effect, and also oppresses aggregation of thrombocytes. The mechanism of action is connected with oppression of activity of TsOG - the main enzyme of metabolism of arachidonic acid, being the predecessor of prostaglandins which play a major role in a pathogeny of an inflammation, pain and fever. Decrease in content of prostaglandins (E1 is preferential) in the center of thermal control leads to decrease in body temperature owing to vasodilatation of skin and increase of sweating. The Analgeziruyushchy effect is caused by both the central, and peripheral action. Reduces aggregation, adhesion of thrombocytes and a thrombogenesis due to suppression of synthesis of A2 thromboxane in thrombocytes.
Reduces a lethality and risk of development of a myocardial infarction at unstable stenocardia. It is effective at primary prevention of diseases of cardiovascular system and at secondary prevention of a myocardial infarction. In a daily dose of 6 g and more suppresses synthesis of a prothrombin in a liver and increases a prothrombin time. Increases fibrinolitic activity of plasma and vitamin of K-dependent factors of coagulation reduces concentration (II, VII, IX, X). Speeds up hemorrhagic complications when carrying out surgical interventions, increases risk of development of bleeding against the background of therapy by anticoagulants. Stimulates removal of uric acid (breaks its reabsorption in renal tubules), but in high doses. Blockade of TsOG-1 in a mucous membrane of a stomach leads to braking of gastroprotektorny prostaglandins that can cause an ulceration of a mucous membrane and the subsequent bleeding.

Pharmacokinetics. At intake it is quickly absorbed preferential from proximal department of a small bowel and to a lesser extent from a stomach. Presence of food at a stomach considerably changes absorption of acetylsalicylic acid.
It is metabolized in a liver by hydrolysis with formation of salicylic acid with the subsequent conjugation with glycine or a glucuronide. Concentration of salicylates in a blood plasma is variable.
About 80% of salicylic acid contact proteins of a blood plasma. Salicylates easily get into many fabrics and liquids of an organism, including into spinal, peritoneal and synovial liquids. In small amounts salicylates are found in brain fabric, traces - in bile, sweat, Calais. Quickly gets through a placental barrier, in small amounts it is allocated with breast milk.
At newborns salicylates can force out bilirubin from communication with albumine and promote development of bilirubinovy encephalopathy.
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.
When developing acidosis the most part of salicylate turns into not ionized acid which is well getting into fabrics including into a brain.

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). T1/2 of acetylsalicylic acid makes about 15 min. T1/2 of salicylate at reception in low doses makes 2-3 h, with increase in a dose can increase up to 15-30 h. At newborns salicylate elimination much slower, than at adults.

Indications to use:

Rheumatism, pseudorheumatism, infectious and allergic myocarditis; fever at infectious and inflammatory diseases; pain syndrome of weak and average intensity of various genesis (including neuralgia, mialgiya, headache); prevention of thromboses and embolisms; primary and secondary prevention of a myocardial infarction; prevention of disturbances of cerebral circulation on ischemic type.

In clinical immunology and allergology: in gradually accruing doses for a long "aspirinovy" desensitization and formation of resistant tolerance to NPVS at patients with "aspirinovy" asthma and "an aspirinovy triad".

Route of administration and doses:

Individual. For adults the single dose varies from 40 mg to 1 g, daily - from 150 mg to 8 g; frequency rate of use - 2-6 times/days.

Features of use:

With care apply at patients with diseases of a liver and kidneys, at bronchial asthma, erosive cankers and bleedings from a GIT in the anamnesis, at the raised bleeding or at simultaneous performing anticoagulative therapy, dekompensirovanny chronic heart failure.
Acetylsalicylic acid even in small doses reduces removal of uric acid from an organism that can become the reason of a bad attack of gout at predisposed patients. During the performing long therapy and/or use of acetylsalicylic acid in high doses observation of the doctor and regular control of level of hemoglobin is required.
Use of acetylsalicylic acid as anti-inflammatory drug in a daily dose of 5-8 g is limited in connection with high probability of development of side effects from a GIT.
Before surgical intervention, for reduction of bleeding during operation and in the postoperative period it is necessary to cancel reception of salicylates in 5-7 days.
During long therapy it is necessary to conduct the general blood test and a research a calla on the occult blood.
Use of acetylsalicylic acid in pediatrics is contraindicated as in case of a viral infection at children under the influence of acetylsalicylic acid the risk of development of a syndrome to Reja increases. Syndrome symptoms to Reja are long vomiting, acute encephalopathy, increase in a liver.
Treatment duration (without consultation with the doctor) should not exceed 7 days at appointment as analgeziruyushchy means and more than 3 days as febrifugal.
During treatment the patient has to abstain from alcohol intake.

Side effects:

- From the alimentary system: nausea, vomiting, anorexia, pains in epigastriums, diarrhea; seldom - emergence of erosive cankers, bleedings from a GIT, an abnormal liver function.
- From TsNS: at prolonged use dizziness, a headache, reversible vision disorders, a sonitus, aseptic meningitis are possible.
- From system of a hemopoiesis: seldom - thrombocytopenia, anemia.
- From system of a blood coagulation: seldom - a hemorrhagic syndrome, lengthening of a bleeding time.
- From an urinary system: seldom - a renal failure; at prolonged use - an acute renal failure, a nephrotic syndrome.
- Allergic reactions: seldom - skin rash, a Quincke's edema, a bronchospasm, "an aspirinovy triad" (a combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid and medicines of a pyrazolon row).
- Other: in some cases - a syndrome to Reja; at prolonged use - strengthening of symptoms of chronic heart failure.

Interaction with other medicines:

At simultaneous use the antacids containing magnesium and/or aluminum hydroxide slow down and reduce absorption of acetylsalicylic acid.

At simultaneous use of blockers of the calcium channels, the means limiting intake of calcium or increasing removal of calcium from an organism the risk of development of bleedings increases.

At simultaneous use with acetylsalicylic acid effect of heparin and indirect anticoagulants, hypoglycemic means of derivatives of sulphonylurea, insulin, a methotrexate, Phenytoinum, valproic acid amplifies.

At simultaneous use with GKS the risk of ulcerogenic action and developing of gastrointestinal bleedings increases.

At simultaneous use efficiency of diuretics (Spironolactonum, furosemide) decreases.

At simultaneous use of other NPVS the risk of development of side effects increases. Acetylsalicylic acid can reduce concentration in a blood plasma of indometacin, piroxicam.

At simultaneous use with gold drugs acetylsalicylic acid can induce injury of a liver.

At simultaneous use efficiency of uricosuric means decreases (including a probenetsida, Sulfinpyrazonum, a benzbromaron).

At simultaneous use of acetylsalicylic acid and an alendronat of sodium development of a heavy esophagitis is possible.

At simultaneous use of griseofulvin disturbance of absorption of acetylsalicylic acid is possible.

The case of spontaneous hemorrhage in an iris of the eye at reception of extract of a ginkgo of a bilob against the background of prolonged use of acetylsalicylic acid in a dose of 325 mg it is described / Believe that it can be caused by the additive inhibiting effect on aggregation of thrombocytes.

At simultaneous use of Dipiridamolum increase in Cmax of salicylate in a blood plasma and AUC is possible.

At simultaneous use with acetylsalicylic acid concentration of digoxin, barbiturates and salts of lithium in a blood plasma increase.

At simultaneous use of salicylates in high doses with inhibitors of a karboangidraza intoxication salicylates is possible.

Acetylsalicylic acid in doses less than 300 mg / exerts insignificant impact on efficiency of captopril and enalapril. At use of acetylsalicylic acid in high doses reduction of efficiency of captopril and enalapril is possible.

At simultaneous use caffeine increases the absorption speed, concentration in a blood plasma and bioavailability of acetylsalicylic acid.

At simultaneous use метопролол can raise salicylate Cmax in a blood plasma.

At use of pentazocine against the background of long reception of acetylsalicylic acid in high doses there is a risk of development of heavy side reactions from kidneys.

At simultaneous use phenylbutazone reduces the uricosuria caused by acetylsalicylic acid.

At simultaneous use ethanol can strengthen effect of acetylsalicylic acid on a GIT.

Contraindications:

GIT erosive cankers in an aggravation phase, gastrointestinal bleeding, "an aspirinovy triad", existence in the anamnesis of instructions on the urticaria, rhinitis caused by reception of acetylsalicylic acid and other NPVS, hemophilia, hemorrhagic diathesis, a prothrombinopenia, the stratifying aortic aneurysm, portal hypertensia, deficit of vitamin K, a liver and/or renal failure, deficit glyukozo-6-fosfatdegidrogenazy, a syndrome to Reja, children's age (up to 15 years - risk of development of a syndrome to Reja at children with a hyperthermia against the background of viral diseases), I and III trimesters of pregnancy, the lactation period, hypersensitivity to acetylsalicylic acid and other salicylates.

Use at pregnancy and feeding by a breast
It is contraindicated to use in I and III trimesters of pregnancy. In the II trimester of pregnancy one-time reception according to strict indications is possible.
Possesses teratogenic action: at use in the I trimester leads to development of splitting of the upper sky, in the III trimester - causes braking of patrimonial activity (inhibition of synthesis of prostaglandins), premature closing of an arterial channel in a fruit, a hyperplasia of pulmonary vessels and hypertensia in a small circle of blood circulation.
Acetylsalicylic acid is emitted with breast milk that increases risk of developing of bleedings at the child owing to dysfunction of thrombocytes therefore it is not necessary to apply acetylsalicylic acid at mother in the period of a lactation.

Use at abnormal liver functions
Contraindication: liver failure.
With care apply at patients with liver diseases.

Use at renal failures
Contraindication: renal failure.
With care apply at patients with diseases of kidneys.

Use for children
Contraindication: children's age (up to 15 years - risk of development of a syndrome to Reja at children with a hyperthermia against the background of viral diseases).

Overdose:

There are no data.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Tablets of 500 mg; 100 mg; 300 mg: 10 or 20 pieces.