Agrenox

Agrenox belongs to a group of drugs that have the ability to affect the rheological characteristics of blood. According to the classification, this drug is an inhibitor of platelet aggregation without heparin. The pharmacotherapeutic group of the drug is agents that affect the circulatory system and hematopoiesis.

The drug is widely used to treat diseases whose pathogenesis is associated with increased levels of thrombus formation in the circulatory system. In addition, Agrenox is used to prevent and treat complications of acute and chronic pathological conditions.

Despite the high efficiency of this drug, it is necessary to take into account the possibility of side effects. Before taking Agrenox, contraindications should be taken into account, and the dosage is prescribed exclusively by a doctor.

The drug, when taken in the correct dosage and for the correct duration, is well tolerated and does not cause side effects associated with overdose or the characteristics of each component, including the effect of the main active ingredient.

[ 1 ], [ 2 ]

Indications Agrenoxa

Indications for use of Agrenox include preventive and therapeutic measures. Due to the ability of the drug to prevent platelet aggregation and the formation of conglomerates, it is widely used in pathological conditions, the genesis of which is based on this property of platelets.

Among acute conditions, transient ischemic attack of the brain should be singled out; the pathogenetic explanation for its development lies in the occlusion of the lumen of a blood vessel by a thrombus. Depending on the size of the thrombus, clinical manifestations may vary.

Thus, with a slight closure of the lumen, a decrease in blood flow is observed in a certain vessel that feeds a part of the brain. As a result, dizziness and headaches are possible. However, as the process progresses and the lumen is further occluded, more pronounced clinical symptoms appear with loss of consciousness and impairment of some functions in the body.

Indications for use Agrenox is also used in ischemic stroke, when the nature of the acute condition is confirmed using special instrumental techniques. In addition, the drug is used for preventive purposes in people who already have strokes in their anamnesis. Indications are due to the ability of Agrenox to reduce thrombus formation.

[ 3 ]

Release form

The release form determines the method of using the drug. Thus, Agrenox is released in the form of capsules, which ensures the delivery of their contents to the stomach, bypassing the process of splitting in the oral cavity.

One capsule of the drug consists of dipyridamole with gradual release in the amount of 200 mg and acetylsalicylic acid - 0.025 g. In addition, the capsule has some auxiliary components: gelatin, hypromellose, dimethicone 350, glyceryl triacetate, metacrylate copolymer (type B), titanium dioxide (E 171), acacia, microcrystalline cellulose and many others.

All the listed components are capsules with prolonged activity. The encapsulated form of release prevents the effect of salivary enzymes on the main active components. The drug is released in a polypropylene tube with different quantities: 30 and 60 capsules in each.

Each capsule consists of hard gelatin and is divided into two caps: one is red and opaque, and the other is milky. The capsule is filled with yellow granules and a tablet. The latter is round, biconvex, and has a shell with flat edges.

[ 4 ], [ 5 ]

Pharmacodynamics

The pharmacodynamics of Agrenox is determined by several biochemical mechanisms associated with acetylsalicylic acid and dipyridamole.

Acetylsalicylic acid has the ability to prevent the synthesis of thromboxane A2, which performs the function of activator of platelet adhesion and spasm of blood vessels. This mechanism is based on blocking cyclogenase in platelets.

Dipyradamole affects several mechanisms. It is able to prevent the absorption of adenosine by blood cells and endothelial cells. The activity of this process is reduced by 80% provided that the therapeutic dosage does not exceed 2 mcg/ml.

As a result, there is an increase in the amount of adenosine, which affects the receptor apparatus of platelets A2, which in turn activates the synthesis of adenylate cyclase and increases the content of cAMP in platelets.

As a result of these reactions, a decrease in the rate of platelet adhesion is observed in response to the influence of their activating factor, collagen and adenosine diphosphate.

Reducing platelet aggregation increases their lifespan, resulting in normalization of their number. In addition, dipyradamole is able to dilate blood vessels, as it has vasodilatory activity.

Pharmacodynamics Agrenox, with the help of dipyridamole, reduces the activity of thrombocytogenesis caused by subepithelial structures by increasing the content of the protective mediator.

Thus, the combined effect of dipyridamole and acetylsalicylic acid provides inhibition of platelet aggregation, activation and adhesion.

[ 6 ], [ 7 ]

Pharmacokinetics

The pharmacokinetics of Agrenox is determined by the pathogenetic effects of dipyridamole and acetylsalicylic acid.

The absorption of dipyridamole provides bioavailability of the drug of about 70%. The maximum concentration of the active substance in the bloodstream occurs in the period - 2-3 hours after taking 400 mg (200 mg twice) - this is the daily dose.

The pharmacokinetics of Agrenox with gradual release are not affected by food intake. The distribution of dipyridamole is observed in many organs due to its high lipophilicity. The active phase of distribution with intravenous administration of the drug does not differ from oral administration.

Dipyridamole in small quantities can penetrate the blood-brain and transplacental barriers. The active substance is transported in a complex with blood proteins. Metabolism occurs to a greater extent in the liver due to its complex with glucuronic acid with the formation of mono- and diglucuronides.

The elimination process of dipyridamole is divided into two phases. The predominant half-life is 40 minutes, and the final half-life is 13 hours. Repeated use of the drug does not cause its accumulation in the body.

Another component of Agrenox is acetylsalicylic acid, which is quickly absorbed in the gastrointestinal tract when used orally. The maximum blood level is reached within 30 minutes when taking 50 mg twice daily.

Acetylsalicylic acid is transformed into salicylate, which combines with albumin and is transported to all organs and tissues, including breast milk, CNS structures and fetal tissues. The concentration of salicylate decreases rapidly, and its metabolism occurs with the help of specific esterases.

Almost 100% of acetylsalicylic acid is excreted in a metabolized form by the kidneys. The unchanged form of this substance is excreted in greater volumes with increasing doses.

[ 8 ]

Dosing and administration

Agrenox is taken regardless of meals twice a day. A certain interval must be observed between doses, so Agrenox is used in the morning and evening.

In order for the capsule contents to be delivered to the stomach unchanged, the capsule must be swallowed whole, without chewing it. To facilitate the intake of Agrenox, the capsule is washed down with a glass of water.

The method of administration and dosage for each person should be selected individually, as some may experience cephalgia at the beginning of therapy with Agrenox. To reduce the manifestation of side effects, it is necessary to reduce the dosage taken and leave one capsule per day, preferably before bedtime. In the morning, a small dose of acetylsalicylic acid should be taken.

However, it should be remembered that to obtain the desired result, it is necessary to follow the method of application and dosage, so as soon as the headache stops bothering, it is recommended to resume the dosage of two capsules. The duration of the therapeutic course is determined individually, based on the severity of the disease and the presence of concomitant pathology.

[ 12 ], [ 13 ], [ 14 ], [ 15 ]

Use Agrenoxa during pregnancy

The use of Agrenox during pregnancy is limited due to insufficient data on its use during this period. Due to the content of acetylsalicylic acid in this drug, it may have a negative effect on the fetus.

Taking the drug after the second trimester of pregnancy may cause premature birth of a premature baby, the appearance of intracranial hemorrhages in the substance and spaces of the fetal brain, as well as the birth of a stillborn fetus or death in the first hours after birth.

Based on the above, the use of Agrenox during pregnancy in the 3rd trimester of pregnancy should be prohibited due to the negative impact of the drug on the fetus in the form of cardiovascular pathology - closure of the arterial duct.

Studies have not been conducted on pregnant women using this drug, so its use should not be recommended during this period. In addition, if a fetus is conceived while taking Agrenox, the pregnant woman should be warned about the possible pathological effect of the drug on the fetus.

As for the breastfeeding period, the main active ingredients of the drug - dipyridamole and salicylates can penetrate into breast milk. As a result, the use of Agrenox during this period is not recommended.

Contraindications

Contraindications to the use of Agrenox are based on the individual characteristics of the body and the presence of concomitant pathological conditions. From the genetic intolerance of the components of Agrenox, it is worth highlighting allergic reactions to dipyridamole and acetylsalicylic acid, as well as additional components. It is not recommended to use the drug in the third trimester of pregnancy and in childhood.

Contraindications to the use of Agrenox also include certain diseases, such as ulcerative lesions of the gastric mucosa and duodenum, pathology of the blood coagulation system - hemophilia, hemorrhagic diseases or diathesis, which may be complicated by bleeding.

Due to the presence of acetylsalicylic acid in the composition of the drug, it is not recommended for people with diseases of allergic genesis - bronchial asthma or polyps in the nasal cavities.

Renal, hepatic and cardiac failure in the decompensation stage are contraindications to the administration of Agrenox. In addition, it is not advisable to take this drug simultaneously with methotrexate in a dosage of more than 15 mg/week.

[ 9 ], [ 10 ]

Side effects Agrenoxa

All side effects of Agrenox are divided according to disorders in certain body systems. From the circulatory and lymphatic systems, it is necessary to highlight a decrease in the level of platelets and erythrocytes in the blood. In addition, due to constant bleeding into the stomach cavity, iron deficiency anemia may develop.

The immune system may react to the drug with a hypersensitivity reaction, causing rash, severe bronchospasm, angioedema, or urticaria.

Side effects of Agrenox caused by the nervous system are manifested by hemorrhages in the tissue or spaces of the brain, cephalgia, dizziness similar to migraine.

Bleeding may occur in the eyes, nasal cavities, gastrointestinal tract organs, skin, and it may be difficult to stop it during surgical operations or other manipulations.

The cardiovascular system may react to Agrenox with increased heart rate, fainting, decreased blood pressure, or a feeling of “heat.”

The gastrointestinal tract may react to the drug with nausea, vomiting, intestinal disorders and abdominal pain. Myalgia is a symptom of damage to the musculoskeletal system.

[ 11 ]

Overdose

An overdose of the drug is mostly manifested by clinical symptoms of excessive accumulation of dipyridamole. This is due to the fact that the capsule contains 200 mg of dipyridamole and only 0.025 g of acetylsalicylic acid. As a result, the manifestations of an overdose may be expressed by hot flashes, increased sweating, nervousness and general weakness.

In addition, there may be pain behind the breastbone, decreased blood pressure and increased heart rate.

An overdose of acetylsalicylic acid is less intense, but dizziness, frequent shallow breathing, digestive disorders, tinnitus (especially in old age), decreased visual and auditory perception, and loss of consciousness are still observed. In case of taking a large dose, hyperthermia with an increase in temperature to 39 degrees, as well as symptoms of hypovolemia are possible. Lack of fluid in the body contributes to the development of life-threatening conditions.

However, these clinical manifestations may occur only in a small number of cases due to the small amount of acetylsalicylic acid in one capsule of Agrenox.

If symptoms of overdose appear, symptomatic treatment should be carried out. This includes gastric lavage, administration of xanthine derivatives (aminophylline), which can reduce the severity of overdose. Other methods for accelerating the elimination of the drug are not of particular importance, since Agrenox is transformed in the liver and tissues, which causes its long-term presence in the body.

Interactions with other drugs

Interactions of Agrenox with other drugs are based on the enhancement or inhibition of certain therapeutic effects of drugs taken simultaneously.

Acetylsalicylic acid can increase the activity of anticoagulants, antithrombotic agents, valproic acid and phenytoin, which may increase the likelihood of developing side effects.

Combination with non-steroidal anti-inflammatory drugs (paracetamol and ibuprofen), hormones and alcohol can provoke complications from the digestive system. Acetylsalicylic acid increases the effect of drugs that lower blood sugar, as well as the toxic properties of methotrexate, especially in dosages above 15 mg/week.

This acid inhibits the activity of prostaglandins and leads to a decrease in renal blood flow with subsequent retention of fluid and salts. As a result, the therapeutic effect of beta-blockers and diuretics (spironolactone) may decrease.

Dipyridamole can increase the concentration of adenosine in the blood, so the dosage of the latter should be reviewed. Combined use with warfarin does not lead to the development of complications, including bleeding, to a greater extent than warfarin alone.

Dipyridamole enhances the activity of drugs whose mechanism of action is based on lowering blood pressure, and inhibits the effect of anticholinesterase inhibitors, which are used in malignant myasthenia.

Interactions of Agrenox with other drugs in a dosage of acetylsalicylic acid greater than 3 g/day may lead to a decrease in the therapeutic effect of ACE inhibitors due to the effect of the acid on the reaction of converting renin to angiotensin.

The simultaneous use of acetylsalicylic acid and acetazolamide may provoke an increase in the concentration of the latter in the blood and the development of side effects.

[ 16 ]

Storage conditions

Storage conditions for Agrenox, like any other drug, require compliance with certain rules, which include temperature, humidity and avoiding direct sunlight on the drug packaging.

The temperature of the room where this medicine will be stored should not exceed 30 degrees. In addition, it is necessary to monitor the integrity of the packaging of the drug.

The manufacturer was concerned about children who could reach Agrenox and take a large dose or the capsule could close the lumen of the upper respiratory tract, so the bottle has a special cap. As a result, it can be opened only by applying force.

The storage conditions of Agrenox ensure the preservation of the therapeutic properties specified in the instructions for a certain period. The date of the last day of taking the drug is also indicated on the outer cardboard packaging and the inner bottle. Due to such packaging, the active substance is not affected by environmental factors.

[ 17 ], [ 18 ], [ 19 ], [ 20 ]

Shelf life

The expiration date is information about the drug that is mandatory for each medicine. It is a certain period of time that has a specific date of the last dose. During this period, the manufacturer of the drug guarantees the doubt of the main therapeutic properties, subject to the above storage conditions.

The shelf life of Agrenox is 3 years. After this period, it is prohibited to use the drug, as it may not only lose its medicinal properties, but also have a negative effect on the body with varying intensity.

Agrenox is a proven effective drug based on dipyridamole and acetylsalicylic acid. Due to their combination, this drug has an antithrombotic effect. It is achieved by preventing platelet aggregation in the bloodstream. Its therapeutic property is used for treatment and prevention of transient ischemic attacks or ischemic strokes.

[ 21 ], [ 22 ], [ 23 ]