Dipyridamol-FPO, 75 mg 40 pcs

Pharmacotherapeutic group: Vasodilator

ATX code: B01AC07

Pharmacodynamics

Dipyridamole inhibits platelet aggregation and adhesion, improves microcirculation and has a mild vasodilator effect. The mechanism by which dipyridamole has an inhibitory effect on platelet aggregation is related to the inhibition of adenosine reuptake (platelet reactivity inhibitor) by endothelial cells, red blood cells and platelets; activation of adenylate cyclase and inhibition of platelet phosphodiesterases. Thus, dipyridamole prevents the release of aggregation activators from platelets – thromboxane (TxA2), ADP, serotonin and others. Dipyridamole increases synthesis of prostacyclin PgI2 by vascular endothelium, normalizes ratio of PgI2 and TxA2, preventing platelet aggregation and increases synthesis of endothelial nitric oxide (NO).

Dipyridamole reduces platelet adhesiveness, prevents clot formation in vessels and stabilizes blood flow in the focus of ischemia.

Dipyridamole dose-dependently prolongs abnormally shortened platelet lifespan.

Dipyridamole due to its vasodilatory properties helps to decrease total peripheral resistance of blood vessels, improves microcirculation and has angioprotective effect. These effects are due to increased activity of endogenous adenosine (adenosine affects vascular smooth muscle and prevents release of norepinephrine). Dipyridamole has both angiogenic and arteriogenic activity, stimulating the formation of new capillaries and collateral arteries.

Dipyridamole normalizes venous outflow, reduces the incidence of deep vein thrombosis in the postoperative period. It improves microcirculation in the retina and renal glomeruli.

In neurological practice such pharmacodynamic effects of dipyridamole as reduction of cerebral vascular tone and improvement of cerebral circulation are used. According to angiographic studies, the use of dipyridamole in combination with acetylsalicylic acid can slow the progression of atherosclerosis.

In obstetrical practice dipyridamole is used to improve placental blood flow and to prevent dystrophic changes in the placenta, to eliminate hypoxia of fetal tissues and accumulation of glycogen in them.

Pharmacokinetics

Absorption

. When taken orally, dipyridamole is rapidly absorbed from the gastrointestinal tract: Most in the stomach and partly in the small intestine. Bioavailability is 37-66%, the time of reaching maximum concentration in blood plasma is about 2 hours.

Distribution

Dipyridamole is almost completely bound to plasma proteins. After oral administration there is a biphasic pattern of decrease in plasma concentrations of dipyridamole.

Metabolism

Dipyridamole is metabolized in the liver by binding to glucuronic acid.

Elimation

The elimination half-life is 20-30 minutes in the initial phase and 10-12 hours in the final phase of elimination. It is excreted mainly in the bile and is excreted through the intestine as monoglucuronide. A small amount of dipyridamole (1-3 %) is excreted by the kidneys.

Indications

Cerebral Circulatory Disorders, Microcirculatory Disorders, Thrombosis Prevention – Treatment and prevention of cerebral circulation disorders of ischemic type;
– Dyscirculatory encephalopathy;
– Primary and secondary prevention of coronary heart disease (CHD), especially with intolerance to acetylsalicylic acid (for the dosage of 75 mg);
– Prevention of arterial and venous thrombosis and its complications;
– prophylaxis of thromboembolism after cardiac valve replacement;
– prophylaxis of placental insufficiency during difficult pregnancy;
– As a part of complex therapy of any disorders and complications. – As a part of complex therapy for any microcirculation disorders of any genesis;
– As an interferon inductor and immunomodulator for prevention and treatment of flu, acute respiratory viral infections (ARI) (for 25 mg dosage).
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Active ingredient

Dipyridamole

Composition

1 tablet contains:

active ingredient: dipyridamole – 25 mg / 50 mg / 75 mg;

excipients: lactose monohydrate, copovidone, microcrystalline cellulose, magnesium stearate, croscarmellose sodium;
excipients for the shell: hypromellose (hydroxypropyl methyl cellulose), talc, titanium dioxide, macrogol 6000 (polyethylene glycol 6000), quinoline yellow dye.

How to take, the dosage

The tablets are taken orally, on an empty stomach, with a small amount of water, without breaking or biting. The dose of the drug is chosen depending on the indications, the severity of the disease and the patient’s reaction to treatment.

For decrease of platelet aggregation it is recommended to take the preparation in a daily dose of 75-225 mg (3-9 tablets of 25 mg or 1-3 tablets of 75 mg).

In severe cases the daily dose may be increased up to 600 mg (8 tablets of 75 mg).

For prophylaxis of placental insufficiency it is recommended to take Dipyridamole-FPO® in dose of 25 mg or 75 mg (1 tablet of 25 mg or 75 mg 3 times daily).

The maximum recommended daily dose is 225 mg (9 tablets of 25 mg or 3 tablets of 75 mg).

For prevention and treatment of cerebral circulation disorders the daily dose of Dipyridamole is 225-450 mg (1 tablet of 75 mg 3-6 times a day).

In patients with CHD it is recommended to take the preparation Dipyridamole-FPO® 75 mg 3 times a day.

If necessary, the dose may be increased under medical supervision.

For prevention of influenza and other acute respiratory infections, especially during epidemics, it is recommended to take the drug Dipyridamol-FPO® according to the following scheme: 50 mg (2 tablets of 25 mg) once a week during 4-5 weeks.

For prophylaxis of relapses in patients who have often had respiratory viral infections it is recommended to take the preparation Dipyridamol-FPO® under the following scheme: 100 mg (2 tablets of 25 mg twice a day with 2-hour interval) once a week during 8-10 weeks.

Dipyridamol-FPO® is suitable for long-term treatment course.

Interaction

Xanthine derivatives (coffee, tea, theophylline derivatives) may weaken the vasodilator effect of dipyridamole.

Dipyridamole may increase the effect of anticoagulants and acetylsalicylic acid when used simultaneously.

Dipyridamole increases the effect of hypotensive drugs.

Dipyridamole weakens cholinesterase inhibitors, which may worsen the course of myasthenia gravis.

The cephalosporins increase the antithrombic effect of dipyridamole.

Antacids decrease the maximum concentration of dipyridamole due to reduced absorption.

Special Instructions

Dipyridamole-FPO® is not recommended for children under 12 years of age.

Coffee and tea should be avoided during treatment.

In patients with myasthenia gravis after changing the dose of dipyridamole may require adjustment of doses of drugs used in the complex therapy of myasthenia gravis.

Patients who regularly take dipyridamole orally should not be prescribed additional intravenously. If it is necessary to conduct an intravenous dipyridamole loading test to diagnose coronary artery disease, oral administration of the drug should be stopped 24 hours before the procedure.

In coronary bypass syndrome to improve intracardiac blood flow, aminophylline is indicated.

Influence on the ability to drive vehicles, mechanisms
Due to the possibility of decreased blood pressure and dizziness during the drug administration, the ability to concentrate and speed of psychomotor reactions in patients may be reduced. Therefore, during the treatment with dipyridamole, caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require high concentration and quick psychomotor reactions.

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Synopsis

Round biconvex, yellow film-coated tablets. On the cross section the core is yellow.

Contraindications

– Hypersensitivity to the drug components;
– Lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
– Acute myocardial infarction;
– Unstable angina;
– widespread stenotic atherosclerosis of coronary arteries;
– subaortic stenosis;
– decompensated heart insufficiency;
– Severe arterial hypotension;
– Severe arterial hypertension;
– Severe heart rhythm disorders;
– Chronic obstructive pulmonary disease;
– Decompensated renal insufficiency;
– Liver insufficiency;
– Hemorrhagic diathesis;
– Diseases with propensity to bleeding (gastric and duodenal ulcer and others).
– children under 12 years of age (effectiveness and safety has not been studied).

With caution

Elderly patients (may cause orthostatic hypotension).

Side effects

Classification of the frequency of side effects according to the World Health Organization (WHO) recommendations: very frequently (≥ 1/10); frequently (≥ 1/100 to < 1/10); infrequently (≥ 1/1000 to < 1/100); rarely (≥ 1/10000 to < 1/1000); very rarely (< 1/10000, including individual reports; frequency is unknown – according to the available data it is impossible to determine the incidence.

Cardiac disorders:

infrequent – tachycardia, “flushes” of blood to the face, coronary bypass syndrome (when used at a dose greater than 225 mg/day).

Vascular disorders:

infrequent – decreased blood pressure (especially when combined with other vasodilators).

Gastrointestinal tract:

infrequent – nausea, vomiting, diarrhea, epigastric pain.

Usually these side effects, having appeared at the beginning of treatment, disappear with longer use of the drug.

Blood and homeostasis system:

infrequent – thrombocytopenia, changes in the functional properties of platelets, bleeding;

very rare – increased bleeding after surgical interventions.

An immune system side:

rarely – allergic reactions such as skin rash, urticaria.

Others:

frequency unknown – weakness, dizziness, headache, facial skin hyperemia, arthritis, myalgia, rhinitis, worsening of CHD symptoms such as angina, myocardial infarction.