Acetylsalicylic acid + Magnesium hydroxide - instructions for use, dose, side effects, contraindications

The mechanism of action of acetylsalicylic acid is the inhibition of cyclooxygenase-1, which blocks the synthesis of thromboxane A2 and suppresses platelet aggregation. Think that acetylsalicylic acid has other mechanisms for suppressing platelet aggregation, which expands the area of its use in various vascular diseases. Acetylsalicylic acid has also anti-inflammatory, analgesic, antipyretic effect.

Magnesium hydroxide, which is part of the combined preparation, protects the mucous membrane of the gastrointestinal tract from the effects of acetylsalicylic acid: it neutralizes the hydrochloric acid of the stomach (antacid effect), reducing its damaging effect on the mucous membrane.

Pharmacokinetics:

Acetylsalicylic acid is absorbed from the gastrointestinal tract almost completely. PThe half-elimination period (half-life) acetylsalicylic acid is about 15 minutes. with the participation of enzymes acetylsalicylic acid quickly hydrolyzed into salicylic acid in the intestines, liver and blood plasma. The connection with plasma proteins is high. PThe half-elimination period (half-life) salicylic acid is about 3 hours, but it can significantly increase with simultaneous administration of large doses of acetylsalicylic acid (more than 3 g) as a result of saturation of enzyme systems.

Bioavailability of acetylsalicylic acid is about 70%, but this value largely fluctuates, since acetylsalicylic acid is subjected to pre-systemic hydrolysis (mucosa of the gastrointestinal tract, liver) into salicylic acid under the action of enzymes.

The doses of magnesium hydroxide used do not affect the bioavailability of acetylsalicylic acid. Magnesium is slowly and in small amounts absorbed in the small intestine, bound by plasma proteins by 25-30%. It is able to pass through the placental barrier.Magnesium is excreted mainly in the urine, but some of it is re-absorbed and removed from the body with the feces.

Indications:

Primary prevention of cardiovascular diseases such as thrombosis and acute heart failure in the presence of risk factors (for example, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age).

Prevention of repeated myocardial infarction and thrombosis of blood vessels.

Prevention of thromboembolism after surgical interventions on vessels (aortocoronary bypass, percutaneous transluminal coronary angioplasty).

Unstable angina.

ICD-10

IX.I20-I25.I20.0 Unstable angina

IX.I20-I25.I25.2 Postponed myocardial infarction

IX.I60-I69.I67.9 Cerebrovascular disease, unspecified

IX.I80-I89.I82 Embolism and thrombosis of other veins

IX.I70-I79.I74 Embolism and thrombosis of the arteries

XXI.Z40-Z54.Z40 Prophylactic surgical intervention

Contraindications:

Hypersensitivity to acetylsalicylic acid, drug auxiliaries and other non-steroidal anti-inflammatory drugs, cerebral hemorrhage, a tendency to bleeding (vitamin K deficiency, thrombocytopenia, hemorrhagic diathesis), bronchial asthma induced by the intake of salicylates and non-steroidal anti-inflammatory drug, erosive ulcerative lesions of the gastrointestinal tract (in the exacerbation phase), gastrointestinal bleeding, severe renal failure (Cl creatinine <10 ml per minute), pregnancy (I and III trimesters), lactation period, deficiency of glucose-6-phosphate dehydrogenase , simultaneous reception with methotrexate (> 15 mg per week), children under 18 years of age.

Carefully:

Caution should be given to the drug for gout, hyperuricemia, history of gastrointestinal ulcers or bleeding from the gastrointestinal tract, with kidney and / or liver failure, bronchial asthma, hay fever, nasal polyposis, allergic conditions, in the second trimester pregnancy.

Pregnancy and lactation:

Action category for the fetus by Food and Drug Administration (US Food and Drug Administration) - FROM.

The use of salicylates in high doses in the first trimester of pregnancy is associated with an increased incidence of fetal developmental defects.In the second trimester of pregnancy, salicylates can be administered only in the light of a strict assessment of the risk and benefit. In the third trimester of pregnancy, high-dose salicylates (> 300 mg per day) cause inhibition of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhages, especially in premature infants.

The appointment of salicylates in the first and third trimesters of pregnancy is contraindicated.

Available clinical data are not sufficient to determine whether or not the drug can be used during breastfeeding. Before prescribing acetylsalicylic acid during breastfeeding, the potential benefit of therapy with a drug regarding the potential risk to infants should be assessed.

Acetylsalicylic acid: penetrates into breast milk. When taken in normal doses, complications in humans are not recorded. With prolonged use in high doses acetylsalicylic acid, getting into the body of the child, can cause side effects.

Magnesium hydroxide: magnesium-containing antacids are able to penetrate into the milk, but their concentrations are not enough to affect the newborn. Complications in humans are not documented.

Dosing and Administration:

Tablets should be swallowed whole, washed down with water. If desired, the tablet can be broken in half, chewed or pre-grated.

For primary prevention of cardiovascular diseases, 1 tablet containing acetylsalicylic acid in a dose of 150 mg is prescribed for the first day, then 1/2 tablet once a day.

To prevent repeated myocardial infarction and thrombosis of blood vessels, one tablet containing acetylsalicylic acid in a dose of 75-150 mg, once a day, is prescribed.

For the prophylaxis of thromboembolism after surgical interventions on vessels (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty) one tablet containing acetylsalicylic acid in a dose of 75-150 mg, once a day, is prescribed.

With unstable angina, 1 tablet containing acetylsalicylic acid in a dose of 75-150 mg, once a day, is prescribed.

Side effects:

Allergic reactions: urticaria, angioedema.

From the side of the immune system: anaphylactic reactions.

From the gastrointestinal tract: nausea, heartburn, vomiting, pain in the abdomen, ulcers of the mucous membrane of the stomach and duodenum, incl. perforated, gastrointestinal hemorrhages, increased activity of hepatic enzymes, stomatitis, esophagitis, erosive lesions of the upper gastrointestinal tract, stricture, colitis, irritable bowel syndrome.

From the respiratory system: bronchospasm.

From the hemopoietic system: increased bleeding, anemia, hypoprothrombinemia, thrombocytopenia, neutropenia, aplastic anemia, eosinophilia, agranulocytosis.

From the central nervous system: dizziness, headache, insomnia, drowsiness, tinnitus, intracerebral haemorrhage (rarely).

Overdose:

Symptoms of an overdose of moderate severity: nausea, vomiting, tinnitus, hearing impairment, dizziness, confusion.

Treatment: should wash the stomach, appoint Activated carbon, to carry out symptomatic therapy.

Symptoms of a severe overdose: fever, hyperventilation, ketoacidosis, respiratory alkalosis, coma, cardiovascular and respiratory failure, severe hypoglycemia.

Treatment: immediate hospitalization in specialized departments for emergency therapy - gastric lavage, determination of acid-base balance, alkaline and forced alkaline diuresis, hemodialysis, administration of saline solutions, Activated carbon, symptomatic therapy. When carrying out alkaline diuresis, it is necessary to achieve hydrogen values between 7.5 and 8. The forced alkaline diuresis should be performed when the concentration of salicylates in the plasma is more than 500 mg / l (3.6 mmol / l) in adults and 300 mg / l (2 , 2 mmol / L) in children.

Interaction:

With simultaneous application acetylsalicylic acid enhances the effect of the following drugs:

- methotrexate (by reducing renal clearance and displacing it from the bond with proteins);

- heparin and indirect anticoagulants (due to disruption of platelet function and displacement of indirect anticoagulants from binding to proteins);

- thrombolytic and antiplatelet agents and anticoagulant drugs (ticlopidine);

- Digoxin (due to a decrease in its renal excretion);

- hypoglycemic agents for oral administration (derivatives of sulfonylureas) and insulin (due to hypoglycemic properties of acetylsalicylic acid itself in high doses and displacement of sulfonylurea derivatives from binding to plasma proteins);

- Valproic acid (due to its displacement from the bond with proteins).

Simultaneous use of acetylsalicylic acid with ibuprofen leads to a decrease in the cardioprotective effects of acetylsalicylic acid.

Additive effect is observed with simultaneous administration of acetylsalicylic acid with ethanol (alcohol).

Acetylsalicylic acid reduces the effect of uricosuric agents (benzbromaron) due tubular competitive elimination of uric acid.

By enhancing the elimination of salicylates, systemic glucocorticosteroids weaken their action.

Antacids and colestramine with simultaneous use reduce the absorption of the drug.

Special instructions:

The drug should be used after the appointment of a doctor.

Acetylsalicylic acid can provoke bronchospasm, as well as cause attacks of bronchial asthma and other reactions of hypersensitivity. Risk factors are the availability of a history of asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system as well as of allergic reactions to other drugs (e.g., skin reactions, pruritus, urticaria).

Acetylsalicylic acid can cause bleeding of varying severity during and after surgical interventions. A few days before the planned surgery, the risk of bleeding should be assessed compared with the risk of developing ischemic complications in patients taking low doses of acetylsalicylic acid. If the risk of bleeding is significant, the intake of acetylsalicylic acid should be temporarily discontinued.

The combination of acetylsalicylic acid with anticoagulants, thrombolytics and antiplatelet drugs is accompanied by an increased risk of bleeding.

Acetylsalicylic acid in low doses can provoke the development of gout in predisposed individuals (having decreased uric acid excretion).

High doses of acetylsalicylic acid have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents.

When combined appointment of glucocorticosteroids and salicylates should be remembered that during treatment, the level of salicylates in the blood is reduced, and after the abolition of glucocorticosteroids, an overdose of salicylates is possible.

It is not recommended combination of acetylsalicylic acid with ibuprofbecause the latter worsens the beneficial effect of acetylsalicylic acid on life expectancy.

Excess dose of acetylsalicylic acid is associated with a risk of gastrointestinal bleeding.

Overdose is especially dangerous in elderly patients.

When combined with acetylsalicylic acid and alcohol, the risk of damage to the mucous membrane of the gastrointestinal tract and prolong the bleeding time.

Instructions

Acetylsalicylic acid + Magnesium hydroxide (Acidum acetylsalicylicum + Magnesii hydroxydum)