Universal reference book for medicines
Product name: TASPIR (TASPIR)

Active substance: acetylsalicylic acid

Type: NSAIDs

Manufacturer: TATHIMFARMPREPARATY (Russia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
NSAIDs.
Has anti-inflammatory, analgesic and antipyretic effect, and also inhibits platelet aggregation. The mechanism of action is associated with oppression of the activity of COX, the main enzyme of arachidonic acid metabolism, which is the precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Decrease in the content of prostaglandins (predominantly E 1 ) at the center of thermoregulation leads to a decrease in body temperature due to the expansion of the vessels of the skin and increased sweating. The analgesic effect is due to both central and peripheral action. Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A 2 in platelets.
Reduces the mortality and risk of myocardial infarction with unstable angina.
Effective in the primary prevention of diseases of the cardiovascular system and in the secondary prevention of myocardial infarction. In a daily dose of 6 g or more suppresses the synthesis of prothrombin in the liver and increases prothrombin time.Increases the fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent clotting factors (II, VII, IX, X). It increases hemorrhagic complications during surgical interventions, increases the risk of bleeding on the background of therapy with anticoagulants. Stimulates the excretion of uric acid (violates its reabsorption in the renal tubules), but in high doses. Blockage of COX-1 in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which can cause ulceration of the mucosa and subsequent bleeding.
PHARMACOKINETICS
When ingested quickly absorbed mainly from the proximal part of the small intestine and to a lesser extent from the stomach.
The presence of food in the stomach significantly alters the absorption of acetylsalicylic acid.
Metabolised in the liver by hydrolysis with the formation of salicylic acid, followed by conjugation with glycine or glucuronide.
The concentration of salicylates in the blood plasma is variable.
About 80% of salicylic acid binds to blood plasma proteins.
Salicylates easily penetrate into many tissues and body fluids, including. in spinal, peritoneal and synovial fluid. In small amounts, salicylates are found in the brain tissue, traces - in bile, sweat, feces. Rapidly penetrates the placental barrier, in small quantities excreted in breast milk.
In newborns, salicylates can displace bilirubin from bonding with albumin and promote the development of bilirubin encephalopathy.

Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation.

When acidosis occurs, most of the salicylate is converted to a non-ionized acid that penetrates well into the tissue, incl.
in the brain.
It is excreted mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites.
Removal of unchanged salicylate depends on the pH of the urine (with alkalinization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). T 1/2acetylsalicylic acid is approximately 15 minutes. T 1/2 salicylate when taken in low doses is 2-3 hours, with an increase in the dose may increase to 15-30 hours. In newborns, the elimination of salicylate is much slower than in adults.
INDICATIONS
Rheumatism, rheumatoid arthritis, infectious-allergic myocarditis;
fever in infectious and inflammatory diseases; pain syndrome of mild and moderate intensity of various genesis (including neuralgia, myalgia, headache); prevention of thrombosis and embolism; primary and secondary prevention of myocardial infarction;prevention of cerebral circulation disorders by ischemic type.
In clinical immunology and allergology: in gradually increasing doses for prolonged "aspirin" desensitization and the formation of stable tolerance to NSAIDs in patients with "aspirin" asthma and "aspirin triad."

DOSING MODE
Individual.
For adults, a single dose varies from 40 mg to 1 g, daily from 150 mg to 8 g; multiplicity of application - 2-6 times / day.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, anorexia, epigastric pain, diarrhea;
rarely - the occurrence of erosive-ulcerative lesions, bleeding from the gastrointestinal tract, a violation of liver function.
From the side of the central nervous system: with prolonged use, dizziness, headache, reversible visual impairment, tinnitus, aseptic meningitis are possible.

From the hemopoietic system: rarely - thrombocytopenia, anemia.

On the part of the blood coagulation system: rarely - hemorrhagic syndrome, lengthening bleeding time.

From the urinary system: rarely - a violation of kidney function;
with prolonged use - acute renal failure, nephrotic syndrome.
Allergic reactions: rarely - skin rash, Quincke's edema, bronchospasm, "aspirin triad" (combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and pyrazolone drugs).

Other: in some cases - Reye's syndrome;
with prolonged use - increased symptoms of chronic heart failure.
CONTRAINDICATIONS
Erosion-ulcerative lesions of the gastrointestinal tract in the acute phase, gastrointestinal bleeding, aspirin triad, history of urticaria, rhinitis caused by taking acetylsalicylic acid and other NSAIDs, hemophilia, hemorrhagic diathesis, hypoprothrombinemia, exfoliating aortic aneurysm, portal hypertension, vitamin K deficiency, hepatic and / or renal insufficiency, glucose-6-phosphate dehydrogenase deficiency, Reye's syndrome, children's age (under 15 years - the risk of developing Reye syndrome in children with hyperthermia against a background of viral diseases
), I and III trimester of pregnancy, lactation period, hypersensitivity to acetylsalicylic acid and other salicylates.
PREGNANCY AND LACTATION
Contraindicated in the I and III trimesters of pregnancy.
In the II trimester of pregnancy, one-time administration is possible on strict indications.
Has a teratogenic effect: when applied in the first trimester leads to the development of cleavage of the upper palate, in the third trimester - causes inhibition of labor (inhibition of prostaglandin synthesis), premature closure of the arterial duct in the fetus, hyperplasia of the pulmonary vessels and hypertension in the small circulation.

Acetylsalicylic acid is excreted in breast milk, which increases the risk of bleeding in the child due to impaired platelet function, so do not use acetylsalicylic acid in the mother during lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication: renal failure.

Use with caution in patients with kidney disease.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: liver failure.

Use with caution in patients with liver disease.

APPLICATION FOR CHILDREN
Contraindication: children's age (under 15 years - the risk of developing Reye syndrome in children with hyperthermia in the background of viral diseases) .

SPECIAL INSTRUCTIONS
They are used with caution in patients with liver and kidney disease, with bronchial asthma, erosive and ulcerative lesions and bleeding from the gastrointestinal tract in an anamnesis, with increased bleeding or concomitant anticonvolution therapy, decompensated chronic heart failure.

Acetylsalicylic acid even in small doses reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients.
When performing long-term therapy and / or using acetylsalicylic acid in high doses, it is necessary to observe the doctor and regularly check the level of hemoglobin.
The use of acetylsalicylic acid as an anti-inflammatory agent in a daily dose of 5-8 g is limited due to a high probability of side effects from the gastrointestinal tract.

Before surgical intervention, to reduce bleeding during surgery and in the postoperative period, it is necessary to cancel the intake of salicylates for 5-7 days.

During prolonged therapy, a general blood test and examination of feces for latent blood should be performed.

The use of acetylsalicylic acid in pediatrics is contraindicated, since in the case of viral infection in children under the influence of acetylsalicylic acid, the risk of developing the Reye syndrome increases.
Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, enlargement of the liver.
Duration of treatment (without consulting a physician) should not exceed 7 days with an appointment as an analgesic and more than 3 days as an antipyretic.

During treatment, the patient should refrain from drinking alcohol.

DRUG INTERACTION
With simultaneous use of antacids containing magnesium and / or aluminum hydroxide, slow down and reduce the absorption of acetylsalicylic acid.

With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.

With simultaneous use with acetylsalicylic acid, the action of heparin and indirect anticoagulants, hypoglycemic agents of sulfonylurea derivatives, insulins, methotrexate, phenytoin, valproic acid increases.

With simultaneous application with GCS, the risk of ulcerogenic action and the occurrence of gastrointestinal bleeding increases.

With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.

With the simultaneous use of other NSAIDs, the risk of side effects increases.
Acetylsalicylic acid can reduce plasma concentrations of indomethacin, piroxicam.
When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.

With the simultaneous use, the effectiveness of uricosuric agents decreases (including probenecid, sulfinpyrazone, benzbromarone).

With the simultaneous use of acetylsalicylic acid and alendronate sodium, the development of severe esophagitis is possible.

With the simultaneous use of griseofulvin, absorption of acetylsalicylic acid may be impaired.

A case of spontaneous hemorrhage into the iris was described when taking an extract of ginkgo biloba against the background of prolonged use of acetylsalicylic acid in a dose of 325 mg / day.
It is believed that this may be due to an additive inhibitory effect on platelet aggregation.
With the simultaneous use of dipyridamole, an increase in C max of salicylate in the blood plasma and AUC is possible.

With simultaneous use with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in blood plasma increase.

With the simultaneous use of salicylates in high doses with inhibitors of carbonic anhydrase, intoxication with salicylates is possible.

Acetylsalicylic acid in doses less than 300 mg / day has a negligible effect on the efficacy of captopril and enalapril.
With the use of acetylsalicylic acid in high doses, a decrease in the efficacy of captopril and enalapril is possible.
With simultaneous use of caffeine increases the rate of absorption, concentration in the blood plasma and bioavailability of acetylsalicylic acid.

With the simultaneous use of metoprolol can increase C max salicylate in blood plasma.

When pentazocine is used against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing serious adverse reactions from the kidneys.

With simultaneous use of phenylbutazone reduces uricosuria caused by acetylsalicylic acid.

With the simultaneous use of ethanol can increase the effect of acetylsalicylic acid on the digestive tract.


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