Magnitor Forte Tablets №30

Author Ольга Кияница

2017-05-11

Amount in a package 30
Product form Pills
Manufacturer Kiev vitamin plant PAT (Ukraine, Kiev)
Registration certificate UA/11211/01/02
The main medicament Magnikor
morion code 155364

Magnicon (Magnicor) instructions for use

Pharmacotherapeutic group

Antithrombotic agents. Platelet aggregation inhibitors, with the exception of heparin.

Storage

active ingredients: 1 tablet contains acetylsalicylic acid 150 mg, magnesium hydroxide 30.39 mg;
excipients: corn starch, microcrystalline cellulose, potato starch, magnesium stearate;
Sheath: a mixture of Ordry II White film (gipromelioz (hydroxypropylmethylcellulose); lactose monohydrate; polyethylene glycol (macrogol); titanium dioxide (E 171); triacetin).

Medicinal form

Tablets coated with a film, forte.

Basic physical and chemical properties:

pills of round shape with a biconvex surface, a rim covered with a film sheath, white or almost white.

Pharmacotherapeutic group

Antithrombotic agents. Thrombocyte aggregation inhibitors, with the exception of heparin. Code АТХ В01А С06.

Pharmacological properties

Pharmacodynamics. Acetylsalicylic acid is analgesic, anti-inflammatory, antipyretic and anti-aggregant. Anti-aggregate properties increase bleeding time.

The main pharmacological effect is the inhibition of the formation of prostaglandins and thromboxanes. The analgesic effect is an additional effect induced by the inhibition of the cyclooxygenase enzyme. The anti-inflammatory effect is associated with reduced blood flow induced by inhibition of PGE2 synthesis.

Acetylsalicylic acid irreversibly inhibits the synthesis of prostaglandins G / H, its effect on platelets lasts longer than acetylsalicylic acid is present in the body. The effect of acetylsalicylic acid on the thromboxane biosynthesis in platelets and on bleeding time lasts for a long time after the cessation of treatment. The action stops only after the appearance of new platelets in the blood plasma.

Salicylic acid (an active metabolite of acetylsalicylic acid) has anti-inflammatory effects, and also has an effect on the processes of breathing, the state of acid-base balance and the mucous membrane of the stomach. Salicylates stimulate breathing, mainly by direct action on the bone marrow. Salicylates have an indirect effect on the mucous membrane of the stomach by inhibition of its vasodilator and cytoprotective prostaglandins and increase the risk of ulceration.

Magnesium hydroxide has an antacid effect and protects the mucous membrane of the digestive tract from the irritant effect of acetylsalicylic acid.

Pharmacokinetics . Absorption. After application internally, acetylsalicylic acid is rapidly absorbed from the digestive tract. After oral administration, absorption of the nonionized form of acetylsalicylic acid occurs in the stomach and intestines. The rate of absorption is reduced with food intake and in patients with migraine attacks, increasing - in patients with achlordia, or in patients who use polysorbates or antacids. The maximum serum concentration is reached in 1-2 hours.

When administered orally, magnesium is in small amounts slowly absorbed from the small intestine.

Distribution. The binding of acetylsalicylic acid to plasma proteins is 80-90%. The volume of distribution for adults is 170 ml / kg body weight. With increased concentration in blood plasma saturation of active centers of proteins occurs, which leads to an increase in the volume of distribution. Salicylates extensively bind to plasma proteins of blood and spread rapidly throughout the body. Salicylases penetrate breast milk and can penetrate the placental barrier.

Magnesium is distributed with bound proteins (about 25-30%). A small amount penetrates breast milk. Magnesium can pass through the placental barrier.

Metabolism. Acetylsalicylic acid hydrolyzes to the active metabolite - salicylic acid in the stomach wall. After absorption of acetylsalicylic acid, it quickly converts to salicylic acid, but during the first 20 minutes after oral administration it is dominant in plasma.

Breeding. Salicylic acid undergoes metabolism predominantly in the liver. Thus, the equilibrium concentration of salicylic acid in the blood plasma increases disproportionately to the administered intradose. At a dose of 325 mg of acetylsalicylic acid, the elimination occurs with the first-order kinetics of the reaction. The half-life is 2-3 hours. At a high dose of acetylsalicylic acid, the half-life is increased to 15-30 hours. Salicylic acid is also excreted unchanged in urine.The volume of salicylic acid released depends on the dose level and pH of the urine. Approximately 30% of the dose of salicylic acid is excreted in urine, if urine is alkaline, only 2% - if acid. The removal through the kidneys is due to processes of glomerular filtration, active secretion of the renal tubules, and passive tubular reabsorption.

A small amount of magnesium is excreted in urine, but most of it is reabsorbed and excreted with feces.

Indication

Acute and chronic ischemic heart disease.

Contraindication

  • Hypersensitivity to acetylsalicylic acid, other salicylates or to any component of the medicinal product.
  • Asthma, caused by the use of salicylates or substances with similar effects, especially NSAIDs, in history.
  • Acute peptic ulcer.
  • Hemorrhagic diathesis.
  • Severe renal insufficiency.
  • Hepatic insufficiency of severe degree.
  • Cardiac insufficiency of severe severity.
  • A combination of methotrexate at a dosage of 15 mg / week or more (see section "Interaction with other medicines and other forms of interaction").

Interaction with other drugs and other types of interactions

Contraindications for simultaneous use.

Methotrexate. The use of acetylsalicylic acid and methotrexate in doses of 15 mg / week and more increases the hematologic toxicity of methotrexate (reduction of renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate by salicylates in connection with plasma protein proteins).

ACE inhibitors. Inhibitors of angiotensin converting enzymes in combination with high doses of acetylsalicylic acid cause a decrease in filtration in the glomeruli as a result of inhibiting the vasodilator effect of prostaglandins and reducing the antihypertensive effect.

Acetazolamide. The possible increase in the concentration of acetazolamide may lead to the penetration of salicylates from the blood plasma into the tissue and cause toxicity of acetazolamide (fatigue, lethargy, drowsiness, confusion, hyperchloremic metabolic acidosis) and salicylate toxicity (vomiting, tachycardia, hyperpnea, confusion).

Probenecid, sulfinepirase. When using probenecid and high doses of salicylates (> 500 mg), the metabolism of both drugs is suppressed and excretion of uric acid may decrease.

Combinations to be used with caution.

Methotrexate. In the use of acetylsalicylic acid and methotrexate in doses less than 15 mg / week, the hematological toxicity of methotrexate is increased (decreasing renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate by salicylates in connection with plasma proteins in the blood).

Clopidogrel, ticlopidine. The combined application of clopidogrel and acetylsalicylic acid has a synergistic effect. Such a combination should be used with caution as it increases the risk of bleeding.

Anticoagulants (warfarin, fenprocumone). Possible reduction of thrombin production, resulting in indirect effects on platelet activity (antagonist of vitamin K) and an increased risk of bleeding.

Absiximab, thyrofiban, eptifibatide. Possible inhibition of glycoprotein IIb / IIIa receptors on the platelets, which increases the risk of bleeding.

Heparin It is possible to reduce thrombin production, which results in an indirect effect on the reduction of platelet activity, which leads to an increased risk of bleeding.

If two or more of the above substances are used together with acetylsalicylic acid, this can lead to a synergistic effect of increasing platelet activity inhibition and, as a result, an increase in hemorrhagic diathesis.

NSAIDs and COX-2 inhibitors (celecoxib). Co-administration increases the risk of gastrointestinal disturbances, which can lead to gastro-intestinal bleeding.

Ibuprofen Simultaneous administration of ibuprofen inhibits irreversible aggregation of platelets, due to the action of acetylsalicylic acid. Treatment with ibuprofen in patients at increased risk of cardiovascular effects may limit the cardioprotective effect of acetylsalicylic acid.

Patients who use acetylsalicylic acid once a day to prevent cardiovascular disease and occasionally use ibuprofen should use acetylsalicylic acid at least 2 hours prior to ibuprofen.

Furosemide Possible inhibition of proximal tubular elimination of furosemide, which leads to a decrease in the diuretic effect of furosemide.

Quinidine Possible additive effect on platelets, which leads to prolonged bleeding time.

Spironolactone. A modified renin effect is possible, which reduces the effectiveness of spironolactone.

Selective serotonin reuptake inhibitors. Co-administration increases the risk of gastrointestinal disturbances, which can lead to gastro-intestinal bleeding.

Valproat When simultaneous use with valproate acetylsalicylic acid displaces it from the connection with proteins of blood plasma, increasing the toxicity of the latter (suppression of the central nervous system, disorders of the gastrointestinal tract).

Systemic glucocorticosteroids (excluding hydrocortisone, used for substitution therapy in Addison's disease) reduce the level of salicylates in the blood and increase the risk of overdose after treatment.

Antidiabetic medicines. Simultaneous administration of acetylsalicylic acid and anti-diabetic drugs increases the risk of hypoglycaemia.

Antacids It is possible to increase renal clearance and decrease renal absorption (due to an increase in urine pH), which leads to a decrease in the effect of acetylsalicylic acid. The clinical value of the interaction of acetylsalicylic acid and magnesium is minimal due to the small amount of magnesium that is included in the medicinal product.

Vaccine against chickenpox. Co-administration increases the risk of developing Ray's syndrome.

Ginkgo biloba A co-administration with gingko biloba prevents platelet aggregation, which increases the risk of bleeding.

Digoxin When co-administered with digoxin, the concentration of the latter in plasma is increased due to a decrease in renal excretion.

Alcohol contributes to damage to the mucous membrane of the gastrointestinal tract and prolongs bleeding time due to the synergism of acetylsalicylic acid and alcohol.

Application features

Medicines should be used with caution in the following situations:

  • Hypersensitivity to analgesic, anti-inflammatory, anti-rheumatic drugs, as well as in the presence of allergies to other substances;
  • ulcers of the gastrointestinal tract, including chronic and recurrent peptic ulcer or gastrointestinal bleeding in history;
  • simultaneous application of anticoagulants;
  • in patients with impaired kidney function or patients with cardiovascular disorders (eg renal vascular pathology, congestive heart failure, hypovolemia, extensive surgery, sepsis or severe bleeding), since acetylsalicylic acid may also increase the risk of renal dysfunction and acute renal failure ;
  • in patients with severe deficiency of glucose-6-phosphate dehydrogenase, acetylsalicylic acid can cause hemolysis or hemolytic anemia. Especially in the presence of factors that may increase the risk of hemolysis, such as high doses of the drug, fever or acute infectious process;
  • disturbance of liver function.

Ibuprofen may reduce the inhibitory effect of acetylsalicylic acid on platelet aggregation. If a medicinal product is used before the use of ibuprofen as an analgesic, the patient should consult a physician.

Acetylsalicylic acid can cause the development of bronchospasm or bronchial asthma attack, or other reactions of high sensitivity. Risk factors include asthma in history, hay fever, nasal polyposis or chronic respiratory disease, allergic reactions (eg, skin reactions, itching, urticaria) to other substances in the history.

Due to the inhibitory effect of acetylsalicylic acid on platelet aggregation, which persists for several days after application, the use of drugs containing acetylsalicylic acid may increase the likelihood / severity of bleeding in surgical operations (including minor surgical interventions such as tooth extraction).

With the use of small doses of acetylsalicylic acid, the withdrawal of uric acid may decrease. This can lead to an attack of gout in patients who are prone to it.

Medicines containing acetylsalicylic acid should not be used in children and adolescents with acute respiratory viral infection (ARI), which is accompanied or not accompanied by an increase in body temperature, without consulting a physician. In some viral diseases, especially with influenza A, influenza B and chickenpox, there is a risk of Ray syndrome, which is a very rare but life-threatening illness requiring urgent medical intervention. The risk may be increased if acetylsalicylic acid is used as an adjunct to the drug, but the cause-effect relationship is not proved in this case. If these conditions are accompanied by constant vomiting, this may be a manifestation of Ray's syndrome.

Use during pregnancy or breastfeeding.

The inhibition of prostaglandin synthesis may adversely affect pregnancy and / or embryo / fetal development. Available data from epidemiological studies indicate the risk of miscarriage and fetal malformations after the use of prostaglandin synthesis inhibitors at the beginning of pregnancy. The risk increases depending on the increase in dose and duration of therapy. According to available data, the association between the use of acetylsalicylic acid and the increased risk of miscarriage has not been confirmed.

Available epidemiological data on developmental malformations are not consistent, but the increased risk of gastroschisis can not be excluded in the use of acetylsalicylic acid. Available data on its effects in early pregnancy (1-4 months) do not indicate any association with the increased risk of malformations.

Animal studies indicate reproductive toxicity.

During the 1st and 2nd trimester of pregnancy, medicinal products containing acetylsalicylic acid should not be prescribed without a clear clinical need. For women who are likely to be pregnant or during the 1st and 2nd trimester of pregnancy, the dose of drugs containing acetylsalicylic acid should be as low as possible and the duration of treatment as short as possible.

During the third trimester of pregnancy, all inhibitors of prostaglandin synthesis can affect the fetus as follows:

  • cardio-pulmonary toxicity (with premature closure of arterial duct and pulmonary hypertension);
  • disturbance of renal function with possible subsequent development of renal failure with oligohydroamniosis;
  • on the woman and the child at the end of pregnancy the inhibitors of prostaglandin synthesis can be influenced as follows:
  • the possibility of lengthening the time of bleeding, antiplatelet effect, which may occur even after the application of very low doses;
  • inhibition of uterine contractions, which can lead to a delay or increase in the duration of childbirth.

In view of this, acetylsalicylic acid is contraindicated in the third trimester of pregnancy.

Salicylas and their metabolites penetrate breast milk in small quantities.

Since no harmful effects of the drug have been identified on the child after the use of women in the period of lactation, the abortion of breastfeeding is usually not required. However, in case of regular use or when using high doses, breastfeeding should be stopped at an early stage.

Ability to influence the reaction rate when driving with motor vehicles or other mechanisms.

Does not affect

Method of administration and dose

Recommended dose for adults - 1 tablet (150 mg / 30.39 mg) per day.

Pills to swallow whole, if necessary, to drink with water. To ensure rapid absorption, the tablet can be chewed or dissolved in water.

Violation of liver function. Medicines should not be used in patients with severe liver function abnormalities. Correction of dosage may be necessary in patients with impaired liver function.

Renal dysfunction. The drug is not used to treat patients with severe renal insufficiency (glomerular filtration rate <0.2 mL / sec (10 ml / min)). Correction of dosage may be necessary in patients with renal dysfunction.

Children.

According to the testimony (see. Section "Dosage and Administration") drug not apply to children.

The use of aspirin to children under 15 years can cause severe side effects (including Reye syndrome, one of the signs of which are constant vomiting).

Overdose

Toxicity. Dangerous dose. Adults: 300 mg / kg body weight.

Chronic poisoning by salicylates can be hidden because its signs and symptoms are nonspecific. Moderate chronic intoxication caused by salicylates or salitsylizm occurs usually only after repeated uses high doses.

Symptoms.

Symptoms of chronic poisoning moderate (the result of prolonged use of high doses of the drug): dizziness, vertigo, deafness, sweating, fever, rapid breathing, tinnitus, respiratory alkalosis, metabolic acidosis, lethargy, mild dehydration, headache, confusion, nausea and vomiting.

About acute intoxication indicates marked changes in acid-base balance, which varies depending on the age and severity of intoxication. The most common manifestation in children is metabolic acidosis. The severity of the condition can be evaluated only on the basis of data on concentrations of salicylates in blood plasma. Absorption of aspirin may slow down due to the delayed release of the stomach, forming concretions in the stomach or in the case of its application in the form of tablets, enteric coated shell.

Symptoms of severe and acute poisoning (due to overdose), hypoglycaemia (especially in children), encephalopathy, coma, hypotension, pulmonary edema, convulsions, coagulopathy, cerebral edema, cardiac arrhythmias.

More pronounced toxic effects observed in patients with chronic overdose or drug abuse, as well as the elderly or children.

Treatment.

In case of acute overdose necessary gastric lavage and use of activated carbon. If you suspect that the use of doses over 120 mg / kg body weight necessary to use activated carbon again.

The level of salicylate in serum should be measured at least every 2 hours after the dose application until salicylate levels will be consistently lowered and recovered acid-base balance.

Prothrombin time and / or INR (international normalized ratio) should be checked, especially if there is a suspicion of bleeding.

It is necessary to restore the balance of fluids and electrolytes. Effective method of removal of plasma salicylate is alkaline diuresis and hemodialysis. Hemodialysis should be used in case of severe intoxication, because this method significantly speeds up the withdrawal of salicylate and restores acid-base and water-salt balance.

Because of the complex pathophysiological effects of salicylates poisoning signs and symptoms / test results may include:


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