Vasaprostan, powder for solution for infusion, 60mcg, 10 ampoules — Made in Germany — Free Delivery

Pharmacological properties:

Pharmacodynamics. Alprostadil, the active ingredient in Vasaprostan, is a vasodilator. It increases blood flow by dilating arterioles and precapillary sphincters. The preparation improves microcirculation and blood rheological properties. After i.v. use in healthy volunteers or in patients, an increase in the elasticity of erythrocytes and inhibition of their ex vivo aggregation are noted. Alprostadil effectively inhibits platelet activation in vitro. This effect also extends to the parameters of shape change, aggregation, secretion of substances contained in the granules, and the release of thromboxane, a substance that promotes aggregation. The preparation leads to a decrease in the formation of arterial blood clots.

The use of the preparation stimulates fibrinolysis and an increase in certain indicators of endogenous fibrinolysis (plasminogen, plasmin, tissue plasminogen activator activity).

Pharmacokinetics. The complex, consisting of alprostadil and alfadex, when preparing a solution for infusion, dissociates into separate components. So, pharmacokinetics does not depend on the presence of the complex in the lyophilisate. After i.v. use of alprostadil at a dose of 60 μg / 2 h, the average Cmax in blood plasma in healthy volunteers is 5.2 pkg / ml higher than the average Cmax in the placebo phase (2.4 pkg / ml). The T½ during the alpha phase is approximately 0.2 minutes and during the beta phase approximately 8 minutes. Thus, steady-state concentration is reached shortly after the start of the infusion. Alprostadil is metabolized mainly in the lungs - 80–90% during the first passage. The primary metabolites are 15-keto-PGE1, PGE0 (13,14-dihydro-PGE1) and 15-keto-PGE0 (13,14-dihydro-15-keto-PGE1), which, in turn, undergo further degradation, into particularly by beta-oxidation and omega-oxidation. Metabolites are excreted in urine (88%) and feces (12%). Complete excretion is carried out in 72 hours. Alprostadil is 93% bound to macromolecular components of blood plasma. In animal experiments, it was found that the T½ of alphadex is approximately 7 minutes; it is excreted in the urine unchanged.

Indications:

treatment in adults with chronic obliterating diseases of the arteries stage III and IV (according to Fontaine's classification).

Application:

intravenous infusion. The contents of 1 ampoule (20 μg alprostadil) are dissolved in 50 ml of 0.9% sodium chloride solution. IV therapy is carried out according to the following dosage regimen.

The volume of the obtained solution, which corresponds to the contents of half of the ampoule of the preparation (25 ml of solution contains 10 μg of alprostadil), should be injected intravenously for 60–120 minutes using an infusion device. With satisfactory tolerance, the dose can be increased to 1 ampoule (20 μg alprostadil), especially in the presence of necrosis. Usually 1 infusion is given per day.

If the intravenous infusion is carried out through an inserted catheter, then, depending on the tolerance of the preparation and the severity of the disease, a dose of 0.1–0.6 ng / kg of body weight per minute is recommended; infusion with the use of an infusion device lasts 12 hours (corresponds to the contents of a ¼ – ½ ampoule of the preparation).

After a 3-week course of treatment, the question of the expediency of further use of the preparation is decided. If the patient does not have a therapeutic effect, treatment should be discontinued. The course of treatment should not exceed 4 weeks.

IV infusion. IV therapy is carried out according to the following dosage regimen.

Dissolve the contents of 1 ampoule (20 μg alprostadil) of the preparation in 50–250 ml of 0.9% sodium chloride solution and inject the resulting solution intravenously for 2 hours. This dose is applied 2 times a day. Alternatively: once a day intravenous infusion for 3 hours 3 ampoules (60 μg alprostadil), which are dissolved in 50–250 ml of 0.9% sodium chloride solution.

In patients with impaired renal function (renal failure with creatinine values> 1.5 mg / dl), intravenous administration of the preparation begins with 1 ampoule 2 times a day (20 μg alprostadil 2 times a day), each infusion lasts 2 hours. Depending on the general clinical picture, the dose can be increased to the above-mentioned usual dose (40-60 mcg of alprostadil per day) for 2-3 days. For patients with renal insufficiency and patients at risk of cardiac dysfunction, the infusion volume should be limited to 50–100 ml / day and it is imperative to use infusion devices.

Contraindications:

hypersensitivity to alprostadil or other components of the preparation;

decompensated heart failure;

arrhythmias of various etiologies;

severe insufficiency or aortic or mitral stenosis;

uncontrolled coronary heart disease;

Ischemic heart disease;

recent myocardial infarction (within the last 6 months);

pulmonary edema or infiltration (as determined by clinical or x-ray examination);

severe COPD;

a history of pulmonary edema in patients with heart failure;

veno-occlusive lung disease;

hepatic dysfunction (increased levels of transaminases or gamma-glutamyl transferase);

history of liver disease;

the threat of bleeding (patients with acute gastrointestinal ulcers, polytrauma);

During pregnancy and breastfeeding;

childhood.

Side effects:

when assessing side effects, the following frequency criteria were taken as a basis:

very often:> 10%;

often:> 1 to <10%;

sometimes:> 0.1 to <1%;

rarely:> 0.01 to <0.1%;

very rare: <0.01%, including isolated cases.

Changes at the injection site: very often - pain, erythema or edema of the limb with intravenous administration; often - hyperemia at the injection site and along the vein. After reducing the dose or stopping the infusion, these side effects, due to the characteristics of the preparation or administration, disappear.

The following symptoms may occur regardless of the injection site.

Neurological disorders: often - headache, impaired sensitivity of the limb on which the manipulation was performed; sometimes - confusion of consciousness; rarely - cerebral convulsions.

Gastrointestinal disorders: sometimes - disruption of the gastrointestinal tract, including diarrhea, nausea, vomiting.

Cardiac disorders: often - sudden redness of the face, neck, fever; sometimes - a decrease in blood pressure, tachycardia, angina pectoris; rarely - arrhythmia, acute pulmonary edema, or severe heart failure.

From the hepatobiliary system: sometimes - an increase in the level of liver enzymes (transaminases).

On the part of the blood and lymphatic system: rarely - leukopenia, leukocytosis, thrombocytopenia.

From the immune system: sometimes - allergic reactions (skin rash, feeling of swelling); very rarely - the development of anaphylaxis / anaphylactic shock.

From the musculoskeletal system and connective tissue: sometimes - joint pain; very rarely - reversible hyperostosis of long bones after using the preparation for> 4 weeks.

General disorders: sometimes - an increase in body temperature, increased sweating, chills, fever, changes in the C-reactive protein index. After completion of treatment, a rapid normalization occurs.

Special instructions:

Vasaprostan 20 mcg is intended for intravenous administration. Solution must be prepared immediately before infusion. Solution prepared> 12 hours ago should not be administered.

The ampoule does not require further filing: the fracture site is under the blue dot.

The content of the ampoule is a dry white powder that forms a hard layer 3 mm thick at the bottom of the ampoule. Small cracks and crumbs are possible on this layer. When the ampoule is damaged, the usually dry substance becomes wet and sticky and loses very much in volume. In this case, the preparation cannot be used.

The dry matter dissolves immediately after adding 0.9% sodium chloride solution. At first, the solution may turn out to be a little cloudy, which is explained by the formation of air bubbles. After a short time, the solution becomes transparent.

In patients at risk, preparation therapy should be carried out with caution. Persons predisposed to heart failure by age, and patients with coronary artery disease should be monitored in a hospital during and for 1 day after stopping treatment with the preparation. The preparation is prescribed with caution for arterial hypotension. To prevent the onset of symptoms of overhydration, infusion volumes should not exceed 50-100 ml / day (administration using an infusion device). It is necessary to constantly monitor the parameters of the patient's cardiovascular system: blood pressure and heart rate, control of body weight and fluid balance, central venous pressure or echocardiography.

The same observation is necessary for patients with peripheral edema or renal dysfunction (serum creatinine> 1.5 mg / dL).

The preparation is prescribed with caution to patients on hemodialysis (treatment is carried out in the post-dialysis period), to persons with type I diabetes mellitus, especially with severe vascular lesions. The influence of high temperatures, humidity and light can cause the cleavage of the OH-group in the 11th position and lead to the formation of prostaglandin A1.

Use during pregnancy and lactation. Do not use the preparation during pregnancy. If it is necessary to use the preparation, breastfeeding should be discontinued.

Children. Do not use in children.

The ability to influence the reaction rate when driving and operating other mechanisms. Like all preparations acting on the cardiovascular system, the preparation can adversely affect the ability to drive vehicles and work with mechanisms, especially at the beginning of treatment, with an increase in the dose, discontinuation of the preparation, alcohol consumption.

Interactions:

during treatment with the preparation, the effect of antihypertensive preparations, vasodilators, and antianginal preparations may be enhanced. With the simultaneous use of these preparations with alprostadil, careful monitoring of the state of the cardiovascular system is necessary.

Sympathomimetics, epinephrine, norepinephrine reduce the vasodilating effect of the preparation. The simultaneous use of the preparation and antithrombotic agents (anticoagulants, platelet aggregation inhibitors, thrombolytic agents) may increase the tendency to bleeding.

Concomitant use with cefamandol, cefaperazone, cefatetan reduces the effectiveness of Vasaprostan.

The incompatibility is unknown.

Overdose:

overdose of the preparation can lead to a decrease in blood pressure and reflex tachycardia due to the effect of vasodilation. Other possible symptoms: vasovagus reactions, pallor, increased sweating, nausea, vomiting, myocardial ischemia, heart failure. Local reactions are possible: pain, swelling and redness of the limb into which the infusion is carried out, manifestations of hypersensitivity.

Treatment is symptomatic. There is no specific antidote. In cases of overdose (severe pain, lowering blood pressure), the dose of the preparation should be reduced; discontinue infusion if necessary. With a decrease in blood pressure, an urgent measure is to raise the lower extremities of the patient, who is lying on his back, up; sympathomimetics can be used.

Storage conditions:

at a temperature not higher than 25 ° С.

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