Dipyridamole - instructions for use, dose, side effects, contraindications

Excipients: corn starch - 67.75 mg, lactose monohydrate 28,50 mg, sodium starch glycolag - 3.75 mg, povidone K-30 - 2.50 mg, silicon dioxide colloid hydrophobic - 1.25 mg, magnesium stearate - 1.25 mg;

film sheath: [hypromellose - 2,500 mg, giprolose (hydroxypropylcellulose) 0.9700 mg, talc 0.9630 mg, titanium dioxide 0.5435 mg, iron oxide oxide yellow (iron oxide) 0.0235 mg] or [dry mixture for film coating containing hipromellose (50%), giprolose (hydroxypropylcellulose) (19.4%), talc (19.26%), titanium dioxide (10.87%), iron oxide oxide yellow (iron oxide) (0.47% )] 5.0 mg.

Dosage of 75 mg

active substance: dipyridamole 75.00 mg;

Excipients: corn starch - 33.75 mg, lactose monohydrate 12,50 mg, sodium starch glycolate - 3.75 mg, povidone K-30 - 2.50 mg, silicon dioxide colloid hydrophobic - 1.25 mg, magnesium stearate - 1.25 mg;

film sheath: [hypromellose - 2,500 mg, giprolose (hydroxypropyl cellulose) 0.9700 mg, talc 0.9630 mg, titanium dioxide 0.4520 mg, iron oxide oxide yellow (iron oxide) 0.1150 mg] or [dry mixture for film coating containing hipromellose (50%), giprolose (hydroxypropyl cellulose) (19.4%), talc (19.26%), titanium dioxide (9.04%), iron oxide oxide yellow (iron oxide) (2.30% )] - 5.0 mg.

Description:

Round biconvex tablets coated with a filmy coating of light yellow (for a dosage of 25 mg) and yellow (for a dosage of 75 mg) of color. On the cross section, the core is bright yellow.

Pharmacotherapeutic group:Vasodilator

ATX: & nbsp

B.01.A.C.07 Dipyridamole

Pharmacodynamics:

Dipiridamole inhibits aggregation and adhesion of platelets, improves microcirculation, has a mild vasodilating action. The mechanism by which dipyridamole has a retarding effect on platelet aggregation, is associated with inhibition of adenosine reuptake (platelet reactivity inhibitor)cells of the endothelium, erythrocytes and platelets; activation of adenylylcyclase and inhibition of platelet phosphodiesterases. In this way, dipyridamole prevents the release of platelets aggregation activators - thromboxane (ТхА₂), ADP, serotonin and others. Dipyridamole increases the synthesis of prostacyclin PgI₂ endothelium of the vascular wall, normalizes the ratio PgI₂ and ТхА₂, preventing the aggregation of platelets; enhances the synthesis of endothelial nitric oxide (N0). Dipiridamol reduces the adhesiveness of platelets, prevents the formation of blood clots in the vessels and stabilizes the blood flow in the source of ischemia.

Dipiridamole dose-dependent extends the pathologically shortened life time of platelets.

Dipiridamole, due to vasodilating properties, contributes to a reduction in overall peripheral vascular resistance, improves microcirculation, and has an angioprotective effect. These effects are due to the increased activity of endogenous adenosine (adenosine affects the smooth musculature of the vessels and prevents the release of norepinephrine). Dipyridamole has both angiogenic and arteriogenic activity, stimulating the formation of new capillaries and collateral arteries.

Dipiridamole normalizes venous outflow, reduces the incidence of deep vein thrombosis in the postoperative period. Improves microcirculation in the retina of the eye and kidney glomeruli.

In neurological practice, such pharmacodynamic effects of dipyridamole as a decrease in the tone of cerebral vessels 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 used to improve placental blood flow and prevent dystrophic changes in the placenta, eliminate hypoxia of the fetal tissues and accumulate glycogen in them.

Pharmacokinetics:

Absorption

Ingestion dipyridamole quickly absorbed from the gastrointestinal tract: most in the stomach and partially in the small intestine. Bioavailability is 37-66%, the time to reach the maximum concentration in the blood plasma is about 2 hours.

Distribution

Dipyridamole almost completely binds to blood plasma proteins. After oral administration, there is a two-phase character of a decrease in the concentration of dipyridamole in the blood plasma.

Metabolism

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

Excretion

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

Indications:

- Treatment and prevention of cerebral circulation disorders according to the ischemic type;

- encephalopathy;

- primary and secondary prevention of coronary heart disease (CHD), especially with intolerance to acetylsalicylic acid (for a dosage of 75 mg);

- prevention of arterial and venous thromboses and their complications;

- prophylaxis of thromboembolism after the operation of prosthetic heart valves;

- prevention of placental insufficiency in complicated pregnancies;

- as part of complex therapy for any violations of microcirculation of any genesis;

- as an inducer of interferon and immunomodulator for the prevention and treatment of influenza, acute respiratory viral infections (ARI) (for a dosage of 25 mg).

Contraindications:

- Hypersensitivity to the components of the drug;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;

acute myocardial infarction;

- unstable angina;

- widespread stenosing coronary artery atherosclerosis;

- Subaortic stenosis;

Decompensated heart failure;

- severe arterial hypotension;

- severe arterial hypertension;

- severe disturbances of the heart rhythm;

- chronic obstructive pulmonary disease;

Decompensated renal failure;

- liver failure;

- hemorrhagic diathesis;

- diseases with a tendency to bleeding (peptic ulcer of the stomach and duodenum, etc.);

- Children under 12 years of age (efficacy and safety not studied).

Carefully:

Patients of advanced age (may cause orthostatic hypotension).

Pregnancy and lactation:

The use of the drug during pregnancy and during breastfeeding is possible only if the intended benefit to the mother exceeds the possible risk to the fetus and the baby. The duration of the course of treatment is determined by the doctor.

Dosing and Administration:

Tablets are taken orally, on an empty stomach, washed down with a small amount of water, without breaking and not cracking. The dose of the drug is selected depending on the indications, the severity of the disease and the patient's response to treatment. The duration of treatment is determined by the doctor.

To reduce aggregation of platelets, it is recommended to take the drug 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 can be increased to 600 mg (8 tablets of 75 mg).

For the prevention of placental insufficiency, it is recommended to take the drug Dipyridamole in a dose of 25 mg or 75 mg (1 tablet of 25 mg or 75 mg 3 times a day). The maximum recommended daily dose is 225 mg (9 tablets of 25 mg or 3 tablets of 75 mg).

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

Patients with ischemic heart disease are recommended to take the drug Dipyridamole 75 mg 3 times a day. If necessary, the dose may be increased under the supervision of a doctor.

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

For the prevention of relapse in patients with respiratory viral infections, who are often ill, it is recommended to take the drug Dipyridamole according to the following scheme: 100 mg (2 tablets of 25 mg twice a day at intervals of 2 hours) once a week for 8-10 weeks.

Dipyridamole is suitable for long-term treatment.

Side effects:

Classification of the incidence of adverse events according to recommendations

World Health Organization (WHO):

very often ≥ 1/10;

often from ≥ 1/100 to <1/10;

infrequently from ≥ 1/1000 to <1/100;

rarely from ≥ 1/10000 to <1/1000;

very rarely <1/10000, including individual messages;

the frequency is unknown - it is not possible to establish the frequency of occurrence from the available data.

Heart Disease:

infrequently - a tachycardia, "flushes" of blood to the face, a syndrome of a coronary stealing (at application in a dose more than 225 mg / day)

Vascular disorders:

infrequently - lowering blood pressure (especially when combined with other vasodilators).

From the gastrointestinal tract: infrequently - nausea, vomiting, diarrhea, epigastric pain.

Usually these side effects, appearing at the beginning of the course of treatment, disappear with a longer application of the drug.

On the part of the blood and the system of homeostasis:

infrequently - thrombocytopenia, changes in the functional properties of platelets, bleeding;

very rarely - increased bleeding after surgical interventions.

From the immune system:

rarely - allergic reactions, such as a skin rash, hives.

Other:

frequency unknown - weakness, dizziness, headache, skin flushing, arthritis, myalgia, rhinitis, increased symptoms of IHD, such as angina pectoris, myocardial infarction.

Overdose:

Symptoms

Pronounced decrease in blood pressure, development or exacerbation of angina attacks, tachycardia, a feeling of heat, "tides" of blood to the face, increased sweating, anxiety, weakness and dizziness.

Measures to help with overdose

Induction of vomiting, gastric lavage, the use of adsorbents to reduce absorption (Activated carbon etc.). The undesirable vasodilating effect of the drug can be suppressed with a slow (50-100 mg / min) intravenous injection of aminophylline.In case of symptoms of angina pectoris, sublingual application of nitroglycerin is indicated.

Interaction:

Xanthine derivatives (coffee, tea, theophylline derivatives) can weaken the vasodilating effect of dipyridamole.

Dipyridamole, when used at the same time, can enhance the effect of anticoagulants and acetylsalicylic acid.

Dipyridamole enhances the effect of antihypertensive drugs.

Dipiridamole weakens the properties of cholinesterase inhibitors, which can lead to an aggravation of myasthenia flow gravis.

Cephalosporins increase the antithrombotic effect of dipyridamole.

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

Special instructions:

A drug Dipyridamole not recommended for children under 12 years.

During treatment, you should avoid drinking coffee and tea.

In patients with myasthenia gravis gravis after changing the dose of dipyridamole, you may need to adjust the dosage of the drugs used in the complex therapy of myasthenia gravis.

Patients who receive dipyridamole orally, it is not possible to additionally administer it intravenously.If it is necessary to conduct a dipyridamole intravenous load test for the diagnosis of coronary artery disease, oral administration of the drug should be discontinued 24 hours before the procedure.

With the syndrome of coronary stealing to improve intracardiac blood flow, the use of aminophylline is indicated.

Effect on the ability to drive transp. cf. and fur:

In connection with the possibility of lowering blood pressure and dizziness during the period of taking the drug, the ability to concentrate and speed of psychomotor reactions in patients can be reduced. Therefore, during treatment with dipyridamole, caution should be exercised when administering vehicles and occupations of potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets, 25 mg and 75 mg.

Packaging:

10, 15, 20 or 30 tablets in a planar cell packaging made of a polyvinylchloride film and aluminum foil.

40 or 100 tablets in a can of high-density polyethylene.

4 or 6 contour cell packs of 10 tablets, 4 contour packs of 15 tablets, 2, 3,5 or 6 out-of-round cell packs of 20 tablets, 2 or 4 out-of-round packs of 30 tablets or one can, together with instructions for use in a pack of cardboard.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004559

Date of registration:27.11.2017

Expiration Date:27.11.2022

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp09.01.2018

Illustrated instructions

Instructions

Dipyridamole (Dipiridamol)