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Pharmacodynamics and pharmacokinetics

What is Aspirin?

The active substance of the drug - acetylsalicylic acid (sometimes it is mistakenly called "acetyl acid") belongs to the group of nonsteroidal anti-inflammatory drugs, the mechanism of action of which is realized due to the irreversible inactivation of the enzyme COX, which plays an important role in the synthesis of thromboxanes and Pg.
Thus, the question of acetylsalicylic acid is aspirin or not, it can be confidently answered that Aspirin and acetylsalicylic acid are one and the same.
Natural source of Aspirin: bark Salix alba (willow white).
Chemical formula of Aspirin: C₉H₈O₄.


Oral administration of ASA in a dose of 300 mg to 1 g contributes to the relief of pain (including muscular and joint) and conditions accompanied by mild fever (eg, for colds or flu). Similar doses of ASA are prescribed from the temperature.
The properties of ASA make it possible to apply the drug also in acute and chronic inflammatory diseases. The list of indications, from which Aspirin helps, lists osteoarthritis, rheumatoid arthritis, Bekhterev's disease.
In these diseases, as a rule, higher doses are used than, for example, at a temperature or with a cold. To facilitate the condition of an adult, depending on the nature of the course of the disease, appoint 4 to 8 g ASA per day.
By blocking the synthesis of thromboxane A2, ACA inhibits platelet aggregation. This makes it expedient to use it for a large number of vascular diseases. The daily dose for this type of pathology varies from 75 to 300 mg.


After taking the Aspirin tablet, ASA is quickly and completely absorbed from the digestive tract. During and after absorption, it is biotransformed into salicylic acid (SC), the main, pharmacologically active metabolite.
TSAH ASK - 10-20 minutes, salicylates - from 20 minutes to 2 hours. ASA and SC completely bind to the blood plasma proteins and are quickly distributed in the body. SK penetrates the placenta and enters the breast milk.
The liver is involved in the metabolism of SC. The products of the metabolism of the substance are: gentisinic, gentisin-humic, salicylic-uric acids, as well as salicylacyl and salicylphenol glucuronides.
The kinetics of SC excretion depends on the dose, since metabolism is limited by the activity of hepatic enzymes. T1 / 2 is also dose-dependent: in the case of low doses of T1 / 2 - from 2 to 3 hours, in the case of high doses - increases to 15 hours.
Derived SC and the products of its metabolism mainly by the kidneys.
Indications for use Aspirin
Aspirin (ASA) is a symptomatic agent that is used in conditions accompanied by pain, inflammation and fever.

Indications for use:

  • headache;
  • toothache;
  • algodismenorea;
  • sore throat caused by a cold;
  • Muscle and joint pain;
  • backache;
  • SARS and colds;
  • moderate pain with inflammation of the joints.

Contraindications to Aspirin

Contraindications are divided into absolute and relative.
Taking the drug is strictly prohibited for allergy to ASA or any other non-steroidal anti-inflammatory drugs (Analgin, Paracetamol, etc.), as well as in conditions that are characterized by increased propensity to bleed.
The following contraindications are relative:

  • simultaneous reception of anticoagulants;
  • Insufficiency of the cytosolic enzyme G6PD;
  • bronchial asthma;
  • impaired renal function;
  • chronic diseases of the stomach and duodenum;
  • diabetes;
  • gout;
  • children under 12 years;
  • pregnancy;
  • lactation.

If there are relative contraindications, Aspirin Bayer can be taken only after the doctor approves it.

Side effects

  • Side effects:
  • hypersensitivity reactions (skin rash, bronchospasm);
  • decreased platelet count in the blood;
  • pain in the stomach.

Frequent and long-term use of ASA in some cases may be accompanied by the development of bleeding from the digestive tract, which are signs of:

  • tarry stools;
  • anemia;
  • general weakness;
  • persistent abdominal pain.

The appearance of such symptoms requires the cessation of Aspirin and immediate medical attention.
Long-term treatment with high doses of ASA can also provoke:

  • damage to the juxtaglomerular apparatus (near the lump complex) of the kidneys;
  • formation of oxalate and / or urate calculi in the urinary tract and kidneys;
  • kidney failure;
  • damage to the insulin pump in the PJU;
  • violation of glycogen synthesis (in some cases, up to the development of diabetes mellitus);
  • thrombocytosis;
  • myocardial dystrophy;
  • hemolytic anemia, erythrocytopenia, hyperprotrombinemia, neutrophilic leukocytosis;
  • decreased capillary permeability (possible increase in blood pressure and worsening trophism of tissues);
  • hemolysis of erythrocytes (in patients with G6PD deficiency);
  • violation of the exchange of copper and zinc;
  • Dysbacteriosis of the oral cavity.

Aspirin tablets, instructions for use

In the instructions for use Aspirin indicated that the tablet should be taken orally after a meal with a sufficient amount of liquid.
The maximum duration of treatment with the drug without a doctor's consultation is 5 days.
As a single dose, adults are prescribed 300 mg to 1 g ASA. Repeated reception is possible after 4-8 hours. The permissible upper limit of the daily dose is 4 g.
Aspirin: how to drink to prevent heart and vascular disease?
A systematic review of various studies has shown that the use of Aspirin after myocardial infarction can reduce by 31% the incidence of nonfatal heart attacks, 39% - the frequency of nonfatal strokes, 25% - the frequency of recurrent strokes and heart attacks, and 15% - vascular death.
In this case, the positive effect of ASA does not depend on sex, age, the presence of diabetes and blood pressure.
In the course of the research it was found that after myocardial infarction ASA should be administered immediately, and treatment should continue until specific contraindications are revealed. The optimal dosage for vascular prophylaxis is 160-325 mg / day.
Than to wash down Aspirinum?
Aspirin is recommended for drinking tablets with milk, jelly, or hydrogencarbonate-sodium mineral water.

Aspirin for dilution of blood: does the blood of ASA dilute?

ASA is a disaggregant. This property of the drug makes it possible to use it in conditions when it is necessary to create obstacles for induced or spontaneous aggregation of platelets.
There are 2 groups of blood-thinning medications: without ASA and on the basis of this substance. Drugs that dilute blood without ASA are anticoagulants. Drugs, the basis of which is ASA, belong to the group of antiplatelet agents.
When asked if blood is diluted or not Aspirin, doctors respond that the effect of disaggregants (and, in particular, ASA) is that they reduce the ability of platelets to stick together, which in turn reduces the risk of blood clots.
Why do I need Aspirin? In the instructions and in Wikipedia, the following recommendations are given on this score: the drug should be administered to patients with high cardiovascular risk, people who have had myocardial infarction, as well as in an acute period of ischemic stroke, circulatory disorders in the brain and other manifestations of atherosclerosis.
Elena Malysheva about the drug says the following: "Medicine for old age. There are no blood clots in the vessels, good blood flow in the brain, in the heart, in the legs, in the hands. In the skin! ". She also notes that the drug reduces the risk of atherosclerosis and protects the body from cancer.

Tips on how to take Aspirin for the dilution of blood correctly, the following: the optimal dose of the drug in case of its use for the prevention of vascular complications is a dose equal to 75-100 mg / day. It is this dose that is considered the most well balanced in the safety / effectiveness ratio.
Western doctors do not use Aspirin to dilute blood, however, in Russia it is recommended for this purpose quite often. Knowing the benefits of ASA for blood vessels, some people start taking the drug uncontrollably.
Doctors do not get tired of reminding that before you drink Aspirin to cleanse the vascular walls from cholesterol and "soften" the blood, you need to get a doctor's approval.
What is harmful aspirin? Studies carried out by scientists in the 1970s showed that ASA drugs affect the viscosity of the blood, thereby contributing to a decrease in the load on the heart muscle and preventing an increase in blood pressure.
However, to achieve these effects, it is usually sufficient to have 50-75 mg of substance per day. The regular excess of the recommended preventive dose can give directly opposite results and harm the body.
In other words, taking ASA to dilute blood, if there are no signs of heart disease, on the body affects negatively.

How to replace ASC?

Often, patients wonder what dilutes blood other than Aspirin. As an alternative to drugs, you can use individual products that dilute the blood, -analogues of antiplatelet agents.
The main ones are those containing salicylic acid, vitamin E and iodine. Vegetable substitutes for Aspirin are licorice, sage, aloe, horse chestnut. Also, for dilution of blood, it is good to introduce cherries, oranges, cranberries, raisins, grapes, mandarins, blueberries, thyme, mint, ginger and curry into the diet.

Meat, fish and dairy products are not conducive to liquefaction of blood, but regular consumption of fish improves the picture of blood. Blood becomes less viscous even when the body receives a sufficient amount of vitamin D.
Pregnant women should be liquefied with eggplants, courgettes, cabbage, onions, horseradish, capsicum, lemons, pomegranates, currants, cranberries, and viburnum.

Lowers or increases pressure Aspirin? Aspirin for headache

Aspirin for headache is particularly effective if the cause of pain is increased intracranial pressure (ICP). This is due to the fact that ASA has a blood-thinning effect and thus contributes to the reduction of ICP.
Adults with headache (depending on its intensity) are usually prescribed to take from 0.25 to 1 g ASA every 6-8 hours.

How to take Aspirin for varicose for prophylaxis?

The action of ASA is aimed at suppressing the function of platelets. As a consequence, with varicose, regular use of the drug helps reduce the risk of thrombosis.
Nevertheless, doctors on the question "Is it possible to drink every day Aspirin?" Reply that it is not worthwhile to abuse this drug with varicose veins. The optimal way of using the product is special medical compresses.
To prepare a compress it is recommended to pour 200 ml of alcohol (vodka) to ground Aspirin tablets (10 pieces) and to insist the medication within 48 hours. Compresses are applied to the area of ​​dilated veins daily, at night. This procedure for varicose veins helps to eliminate pain syndrome.

How useful is Aspirin in cosmetology?

In cosmetology, ASA is used for hair (in particular, as a remedy for dandruff), to treat acne and improve the skin. The effectiveness of the drug is confirmed by a large number of positive reviews and pictures, on which it is possible to assess the appearance of the face before and after applying Aspirin.
For facial skin, ASA is used in creams for daily care, as well as in masks. The benefit of this treatment for the face is that the skin quickly enough - within a few hours - the inflammation and redness disappear and the tissue swelling subsides.
In addition, face masks with Aspirin help exfoliate the layer of dead cells and clean the pores from subcutaneous fat.
On the question of how to help acne on the face of Aspirin, cosmetologists say that the property of clearing the pores is due to the drying effect and good solubility in fats, thanks to which the ASA can penetrate deep enough into the pores sealed with sebum.
Light peeling is guaranteed due to the granular structure of the dissolved preparation. In this case, the product does not injure healthy areas of the skin. This is due to the fact that ASK works a little differently than abrasive scrubs, the exfoliating effect of which is realized due to the presence of coarse particles in their composition.

The action of ASA, unlike such remedies, is aimed at weakening the adhesive bonds between the cells, which in turn helps to remove dead cells from the skin surface without damaging young healthy cells in deeper layers.
The simplest recipe for acne is to put half the tablet of the drug on the inflamed area.
You can also add crushed Aspirin tablets to the cream. To prepare the formulation, 4 tablets of the drug are placed in a bowl and dripped on them with water. When the drug begins to dissolve, it is rubbed with fingers to a gruel-like consistency and then mixed with a spatula with 2 tbsp. tablespoons of cream.
That the agent from spots had more thin structure, it is possible to pour to a mixture up to 1 tbsp. spoons of warm water. The cream is applied to the face, and after 15 minutes washed off with warm water.
Aspirin for acne can also be used in combination with freshly squeezed lemon juice.
The recipe for this mask of Aspirin against acne is simple: 6 tablets of the drug are ground with lemon juice and juice until a homogeneous mass is obtained (reviews suggest that the process of dissolving tablets may last for 10 minutes), and then the resulting paste is applied pointwise to the pimples and left to dry.
Remove the paste from the skin to neutralize the acid recommended solution of drinking soda.
Good reviews of the face mask with Aspirin and honey. For the preparation of the medicinal composition, you need to put 3 tablets in the bowl (use not effervescent Aspirin UPSA, but usual tablets) and drop on them with water. When the tablets become loose, add 0.5-1 teaspoon of honey to them and mix thoroughly.
If the honey is too thick, you can add a few drops of water to the mixture. The mask is applied to dry skin for 15 minutes, and then gently, in a circular motion, wash your face with warm water.
Most suited to the mask of honey and Aspirin for fading, oily and porous skin, but cosmetologists say that you can use a mask with honey and acne.

A good mask for acne with Aspirin and clay. To prepare it you need to take 6 tablets ASA, 2 tsp cosmetic clay (blue or white) and a small amount of warm water.
All the ingredients are mixed in a convenient container until the gruel is obtained, after which the composition is applied by a cotton disc to the face for 15 minutes. At occurrence of unpleasant sensations (burning, an itch) the mask can be washed off earlier. After the procedure, it is recommended to wipe the skin with soaked chamomile or sponge.
To eliminate small acne and black dots Aspirin is used in combination with carbonated mineral water and black cosmetic clay. At 1 tbsp. A clay spoon needs to take 1 ASA tablet. First, the clay is diluted with mineral water, then Aspirin is added to the resulting gruel.
The composition is applied to the skin with a thin layer. The exposure time is 20 minutes. The cream after the procedure is recommended to be applied not earlier than in 10-15 minutes (this will give the skin "breathe").
Effective against acne Levomycetin, calendula and Aspirin in the form of a talker. To prepare the preparation for 40 ml of calendula tincture, add 4 tablets of each preparation and shake the bottle well. The solution is used to rub the face.
Purification of the face with Aspirin is carried out using only tablets in pure form. It should be remembered that there are different types of ASA on sale. However, for peeling should use tablets without additional coating, Aspirin in the shell for these purposes do not use.
A wettable tablet of the drug is placed on a cotton pad, and then circular movements are applied to the face skin for 3 minutes and then rinsed off with warm water.
From black dots, against acne (comedones) and to prevent the appearance of acne, you can use Aspirin as part of a mask with coffee and clay. At 2 tbsp. spoons of white or blue cosmetic clay is recommended to use 1 h.

a spoon of natural medium-grind coffee and 4 tablets of ASA.
To the finished mixture in small portions poured carbonated mineral water in an amount necessary to produce a thick slurry. The skin is applied to the skin with slow, massaging movements, covering all areas except the upper and lower eyelid regions. The exposure time is 20 minutes, after which the mask is washed off. To enhance the effect, problem areas can be wiped with an ice cube.
Aspirin for hair is used mainly as a remedy for dandruff. The easiest way to treat hair diseases is to use a shampoo with ASA.
To prepare the medicinal composition, the amount of shampoo necessary for a single shampoo (preferably if it contains a minimum of dyes and fragrances) is measured in a separate container, and then 2 crushed ACK tablets are added (uncoated).


Symptoms of an overdose of moderate severity are: noise in the ears, nausea, hearing loss, vomiting, confusion, dizziness, headache. The listed phenomena disappear when the dose of the drug decreases.
Severe overdose Aspirin is accompanied by hyperventilation, fever, metabolic acidosis, respiratory alkalosis, ketosis, cardiogenic shock, coma, severe hypoglycaemia, respiratory failure.
In such cases, the patient is hospitalized. Treatment includes reception of activated charcoal, lavage, control of KChR, forced alkaline diuresis to obtain pH values ​​of urine within 7.5-8.0, compensation for fluid loss, hemodialysis, symptomatic therapy.


ASA enhances the effects of non-steroidal anti-inflammatory drugs (for this reason, doctors do not recommend taking Aspirin with other drugs of this group, for example, concurrently with Paracetamol), non-narcotic analgesics, oral hypoglycemic drugs, indirect anticoagulants, heparin, thrombolytic agents that inhibit platelet aggregation, triiodothyronine, sulfonamides.
Reduces the effects of diuretics, uricosuric drugs, antihypertensive drugs.
SCS, alcohol and ethanol-containing drugs increase the damaging effect of ASA on the mucosa of the digestive canal, increase the risk of developing gastric and intestinal bleeding.
ASA increases the plasma concentration of drugs Li, barbiturates and digoxin.
Absorption of ASA worsens and slows down while taking the drug with Al and / or Mg-containing antacids.

Terms of sale

The recipe in Latin for the drug (sample): Rp .: Tab. Acidi acetylsalicylici 0,1 №10 D. S. If you suspect of AMI, take 1 tablet 2 times a day.

Storage conditions

Tablets should be kept out of the reach of children, protected from light and moisture.
Shelf life
Five years.

Special instructions

ASA can cause reactions of hypersensitivity (for example, an attack of bronchial asthma (BA) or bronchospasm). Risk factors are the presence in the history of asthma, polyps of the nose, fever, broncho-pulmonary diseases in chronic form, allergy cases (cutaneous manifestations of allergy, allergic rhinitis).
ASA can increase the tendency to bleeding, which is due to its inhibitory effect on platelet aggregation. This must be taken into account when prescribing the drug to patients who are undergoing surgery (including a small one, for example, tooth extraction).
The drug is stopped for 5-7 days before the operation. The doctor should be informed that before the surgery the patient was taking Aspirin.
ASA reduces the excretion of uric acid from the body, which can predispose an acute attack of gout in predisposed patients.

Aspirin - good or bad?

ASA is widely used as an anesthetic, antipyretic and anti-inflammatory drug. In lower doses, it is used to prevent the development of vascular complications.
To date, ASA is the only disaggregant whose effectiveness when used in an acute period of ischemic stroke (cerebral infarction) is supported by evidence-based medicine.
With the regular administration of ASA, the risk of colorectal cancer, as well as prostate, lung, esophagus and throat cancer, is significantly reduced.
An important feature of ASA is that it irreversibly suppresses the COX-enzyme, which is involved in the synthesis of thromboxanes and Pg. Acting as an acetylating agent, ASA joins the remainder of the serine in the active center of the COX acetyl group. This distinguishes the drug from other NSAIDs (in particular, from ibuprofen and diclofenac), which belong to the group of reversible inhibitors of COX.
Bodybuilders use the combination "Aspirin-Caffeine-Broncholitin" as a fat burner (this mixture is considered the progenitor of all fat burners). Housewives found the use of ASA and in everyday life: the remedy is often used to remove stains of sweat from white clothes and to water the affected soil.
You can use ASA and for flowers: a chopped Aspirin tablet is added to the water when you want to keep the cut plants longer.
Some women use Aspirin tablets as a contraceptive: the tablet is administered intravaginally 10-15 minutes before PA or dissolved in water and then douched with the resulting solution.
The effectiveness of this method of protection from pregnancy has not been investigated, however, the right to its existence by gynecologists is not denied. At the same time, doctors note that the effectiveness of contraception with the use of ASA is only about 10%.

Also there is an opinion that with the help of Aspirin, pregnancy can be interrupted. Doctors of such methods, of course, do not welcome, and advise in case if pregnancy is not planned and undesirable, nevertheless it is timely to seek help from medical institutions.
Despite a large number of useful properties, the drug has a bad name. Suppression of COX activity provokes a violation of the integrity of the walls of the digestive canal and is a factor in the development of peptic ulcer.
Also dangerous ASA can be for children under 12 years old. If used in the presence of a child with a viral infection, the drug may cause Reye's syndrome, a disease that threatens the lives of young patients.

Can I give Aspirin to children?

Children Aspirin is recommended to be given from the age of 12 years.
To give children at a temperature rising against the background of a viral infection, drugs containing ASA are prohibited, since ASA acts on the same structures of the liver and brain as some viruses.
Thus, the combination of Aspirin and viral infection can cause the development of Ray's syndrome, a disease in which the brain and liver are affected, and about one in five small patients die.
The risk of developing Ray's syndrome increases in cases where ASA is used as a concomitant drug, but there is no evidence of a causal relationship in such cases. One of the signs of Ray's syndrome is prolonged vomiting.
As a single dose for children under three years is usually given 100 mg, children of four to six years -200 mg, and children of seven to nine years - 300 mg ASA.
The recommended dose for a child is 60 mg / kg / day, divided into 4-6 receptions, or 15 mg / kg every 6 hours or 10 mg / kg every 4 hours. In children under the age of three, the drug in this dosage form is not used.

Compatibility with alcohol

Is it possible to drink with alcohol Aspirin?

Aspirin and alcohol are incompatible. There are descriptions of cases when taking even 40 g of alcohol in combination with the drug was accompanied by the development of gastric bleeding and severe allergic reactions.

Does Aspirin help with a hangover?

Aspirin in a hangover is very effective, due to the ability of ASA to prevent platelet aggregation (both spontaneous and induced).
On the question whether it is possible to drink from a hangover Aspirin, doctors respond that the drug is better not to drink after alcohol, but about 2 hours before the planned feast. This will prevent microthrombin in the small blood vessels of the brain and, in part, swelling of the tissues.
With a hangover, it is best to take a rapidly soluble Aspirin, for example, Uppsarin UPCA. The latter less irritates the gastrointestinal mucosa, and the citric acid contained in it activates the processing of under-oxidized alcohol decomposition products. The optimal dosage is 500 mg for every 35 kg of body weight.

Aspirin during pregnancy

Is it possible to drink Aspirin during pregnancy in the early stages?

The use of salicylates in the first three months in individual retrospective epidemiological studies was associated with an increased risk of developing congenital defects (including heart defects and cleavage of the hard palate).
Nevertheless, with prolonged use of the drug in therapeutic doses that do not exceed 150 mg / day, this risk was low. At 32 thousand pairs "mother-child" during researches there was no connection between application of Aspirin and an increase in the number of congenital malformations.
During pregnancy, ASA should only be taken after assessing the risk for the child / benefit for the mother. In case of long-term use of Aspirin, the daily dose of ASA should not exceed 150 mg.

Aspirin for pregnant women in the 3rd trimester

In the last months of pregnancy, the intake of high (more than 300 mg / day.) Doses of salicylates can cause pregnancy overweight and weakening of labor during labor.
In addition, treatment with Aspirin in such doses can lead to premature closure in the child of ductus arteriosus (cardiopulmonary toxicity).
The use of high doses of ASA shortly before birth can provoke intracranial bleeding, especially in premature infants.
Proceeding from this, except for exceptional cases caused by obstetric and cardiological medical indications using special monitoring, the use of ASA in the last trimester of pregnancy is contraindicated.

Is it possible to breast-feed Aspirin?

Salicylates and the products of their metabolism penetrate into milk in small amounts. Since side effects in infants after accidental use of the drug were not noted, interruptions of GV are usually not required.
If you need long-term treatment with the drug in high doses, you need to decide whether to stop breastfeeding.

Reviews about Aspirin

Aspirin is a medicine familiar to everyone. Its effectiveness has been clinically tested, and the safety profile and the mechanism of action have been thoroughly studied. WHO included ASC in the list of essential drugs.
The properties of ASA make it possible to use Aspirin for the relief of pain and inflammation, to reduce the elevated temperature and ICP, as well as for the prevention of vascular complications.
Along with the feedback on the use of ASA for their intended purpose, women also give good feedback on cleaning the face with Aspirin and reviews about the use of the drug for the hair. Much positive feedback about the mask "Aspirin with honey," which is used in cosmetics as a means of acne.

Aspirin well cures inflamed elements, relieves swelling of tissues and helps exfoliate dead skin cells, honey for facial skin is useful in that, penetrating into deep layers, perfectly nourishes and cleanses the skin, prevents evaporation of moisture from the skin, and has astringent, tightening and toning action.

Composition of Aspirin

The tablet contains 500 mg of acetylsalicylic acid (ASA), as well as corn starch and microcrystalline cellulose.

Form of issue

The form of the preparation is a tablet.

Pharmachologic effect

The drug removes inflammation and pain, and also acts as an antipyretic and disaggregant.
Pharmacological group: NSAIDs are derivatives of salicylic acid.


Coment read

Alexandra 17:27 | 02/13/2018
Many thanks to you for your valuable, practically, exhaustive publications about medicines! Success to you in everything! Health!