Dipyridamole

Chemical name

2,2',2'',2'''-[(4,8-Ди-1-пипери��инилпиримидо[5,4-d]пири мидин- 2,6-диил)динитрило]тетр акис[этанол]

Gross

C24-H40-N8-O4

Characteristics

Crystalline powder yellow, with a bitter taste and odourless. Rat in the diluted acid, methanol and chloroform and nerastvorim almost in the water.

Of drugs

The drugs-antiagregatine, antiadgezivne, sossoudorasshiratee (артериодилатирующее) . It has an impact on the primary or secondary agregatia platelets. Hindered their adhesion, potenziruet antiagregazionny prostatziklina effect. The mechanism of action is essential fosfodiesterzy inhibition and increasing Zamf in platelets, which leads to halt their aggregation. In addition, stimulated by the release of prostatziklina endotelialnami cages, oppressed education tromboksana A_2, suffered a reverse takeover adenosine cell (perhaps by the influence of the special nukleozidnyi carrier in the cell membrane), and increasing its concentration in blood. Adenosine stimulates adenilatziklazu and, in turn, increases the Zamf in platelets. At the same time, it affects the smooth musculature vessels and prevents the release of Kateholaminov.posle intake of rapidly absorbed. Bioavailability of 37-66%. C_max-75 min. Linking plasma protein-91-99% (mainly from albuminom and acid альфа_1-гликопротеино��). Quickly penetrates the tissues. Pharmacokinetics dwuhfaznaya in the first phase T_1/2 : 40 minutes; In the second stage around 10 am Predominantly metabolized in the liver, 20% of the drug is included in enterogepaticescuu circulation. Excreted with jelchew of monoglukuronida and few diglukuronida. Renal off small. Can drinks (mostly occurs in the liver). As antiagregatingo means more commonly used in combination with aspirin. Adhesion stops platelets in the blood and to a lesser extent agregatia. Antiagregazionny effect occurs when the concentration of plasma 0.1 µ g / J Dozozawisimo lengthens pathologically ahead of the count. Provides vazodilatirtee effect on the coronary vessels through inhibition adenozindezaminaza (this property was used to conduct clinical samples). Increase coronary artery, especially unmodified, it is a phenomenon mezhkoronarnogo victimize. Dipiridamolovaya стресс-эхокардиограф��я in the diagnosis of ischemic heart disease in patients with angiograficski unchanged koronariani arteries is high sensitivity, combined with high specificity (respectively 91 and 83%); sensitivity of the test, above the mnogososudistom defeat in patients with well-developed kollateralami and in patients with reduced regional perfuziei attack. Normalizes venous outflow, reduces the frequency of ankle deep vein in the aftercare period. It improves microcirculation in a mesh coated eyes, kidney clubockah. Impact resistance brain receptacles effective by the dynamic human cerebral circulation. And preventive action against trombirovania implants and coronary venous shunts (in conjunction with antikoagulyantami). Along with aspirin prevents tromboticeskih box for prosthetic heart valves. According to the angiograficski study, a combination of aspirin with dipiridamolom slows progression of peripheral atherosclerosis. In obstetric practice corrigiruet placental blood, warns dystrophic changes in platzente (with the threat of pre-eclampsia), removes tissue hypoxia fruit and contributes to the accumulation of glycogen.

Indications

Prevention tromboamboliceski syndrome after operation prosthetic heart valves prevention occluzii stentov and aortocoronarnah shunts (in combination with aspirin), peripheral vascular damage (including obliterirute chronic diseases of the blood vessels lower limbs, especially if risk factors (arterial hypertension, smoking), prevention platzentarna insufficient to risk pregnancies and treatment and prevention Dvs-sindroma children with infectious toxicosis and septicemia, trejcomponentnoe treatment therapy (complex therapy), the syndrome of suppressing the nine children, �ипиридамол-таллиевой -201 scintigrafii applying physical pressure dipiridamolova �тресс-эхокардиографи и.

Contraindications

Hypersensitivity, acute myocardial infarction expressed ateroskleroticescoe defeated coronary advanced system kollaterley, predisposition to hypotonia, severe violations of the liver, hemorrhagic diateza, obstructive lung diseases expressed violations vnutrijeludockova conductivity, severe arterial hypertension, II and III trimenon, childhood and adolescence (up to 12 years).

Side-Effects

Nausea, eyelid feeling in the stomach, headaches, dizziness, skin person coronary syndrome victimize (worsening IBS), B19, change the functional properties of platelets, bleeding, hypotension, tachycardia, aetiology, weakness, rash.

Patient interaction

Antatsida reduce maximum concentration because of the decline in removals. Aspirin and indirect combined effect increased, derivatives ксантина weaken (especially коронарорасширяющий), heparin increases the risk of bleeding complications.

Overdosing

Symptoms : short гипотензия.Лечение : introduction вазопрессорных agents.

Precautions

If you have coronary syndrome victimize to improve intracardiac blood flow shows aminofillina appointment. Violation of the liver and psoriasis obstruction to require dose reduction.

Dosing and Administration

Inside for 1 hour before meals. As antiagregatingo funds 75-100 mg 3-4 times / den. To prevent tromboamboliceski syndrome trombirovania stenta and aortocoronarnah shunts-on the first day at 50 mg 4 times / day with aspirin, and then on the 100 mg four times per day (cancel within seven days after an operation on the condition of the continuation of receiving aspirin dose to 325 mg / day). Can another scheme : 100 mg drug four times a day for two days before operation, and 100 mg in 1 h after the operation (if necessary in combination with varfarinom). For the treatment of chronic diseases obliteriruth arteries lower limbs-75 mg three times a day; Treated 2-3 months (combination with small doses of aspirin). For diagnostic purposes, 300-400 mg directly at the time of the стресс-эхокардиограф��и or for 45 minutes before injection �адиофармацевтическо��о preparation.

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