Vasaprostan

Drug medication Vasaprostan can be attributed to a number of antispasmodics, which help to relax the smooth muscles of the walls of blood supply vessels.

Indications Vasaprostan

There are the following possible indications for the use of medication Vazoprostan:

• severe forms of obliterating arterial pathology (stage III or IV according to Fontaine's classifications);
• syndrome of intermittent claudication due to endarteritis in the vessels of the legs (in cases where surgical intervention is impossible for some reason);
• diabetic angiopathy;
• manifestations of a syndrome or Raynaud's disease;
• systemic vasculitis;
• in the palliative treatment of patients with so-called ductus-dependent heart defects.

[1], [2], [3]

Release form

Vazaprostan is available in the form of ampoules with lyophilizate to make a solution - it is a white hygroscopic mass consisting of alprostadil (clathrate complex and alfadex). Lactose is an additional substance.

The cardboard package contains 10 ampoules with lyophilizate.

[4], [5], [6]

Pharmacodynamics

The active substance of the preparation is an analogue of natural PGE1. This causes vasodilatation, antiaggregation and angioprotective properties of the drug.

Vasodilatation processes occur in the arterioles. Microcirculation and dynamics of collateral circulation are activated.

The degree of general peripheral resistance decreases, the periodicity of cardiac muscle contractions and cardiac ejection increases. The indices of blood pressure do not increase.

The influence of Vazaprostana medication on the rheological abilities of blood is based on the improvement of its quality, the reduction of platelet adhesion and the increase in erythrocyte elasticity.

Vazaprostan gently stimulates the activity of the muscular fibers of the uterus, the smooth muscles of the intestine and the bladder.

Pharmacokinetics

Intravenous infusion of Vazaprostana provides achievement of a therapeutic level in the blood for two to three minutes, and maximum concentration - for 1.5-2 hours.

Metabolic processes occur in the lung tissue, where a different active and inactive form of metabolites is formed, which is then excreted by the kidneys and partly by the liver.

[7], [8]

Dosing and administration

Preparation of the solution should be started immediately before the introduction. The powder should dissolve instantly after the addition of saline. Sometimes there may be some turbidity in the solution, which soon disappears.

It is inadmissible to use a solution that was diluted more than 12 hours ago.

• Intraarterial infusion - a substance from a single ampoule is diluted in 50 ml of saline. After that, half of the ampoule is administered intra-arterially with the aid of a device for intra-arterial infusion. With endarteritis, taking place in severe form, with the development of necrotic tissue damage, the dosage can be increased to one ampoule (20 μg). The solution is administered gradually, for one to two hours, once a day.
• Intravenous infusion - requires the dissolution of two ampoules (40 μg) of the drug in saline (from 50 to 250 ml). The solution is administered extremely gradually, for two hours, usually 2 times a day. Sometimes the following scheme of administration is also used: three ampoules (60 μg) are administered for three hours once a day.

The duration of therapy is about two weeks. The doctor can prescribe and continue treatment for up to one month (if necessary). If the use of the drug for 14 days did not bring the desired effect, the drug is canceled because of its inadvisability.

Patients with impaired renal function should start the drug with 20 μg (1 time per day), gradually increasing the dosage, if there is such a need.

With pathologies of the heart and kidneys, the amount of physiological solution for diluting the medication is reduced to 50-150 ml. For such patients, the treatment course should take at least one month.

Therapy with vasaprostane is carried out along with constant monitoring of blood pressure, pulse rate, and coagulation characteristics.

Treatment of patients with vasaprostane is usually carried out in a hospital.

[12], [13]

Use Vasaprostan during pregnancy

Treatment with the use of the drug Vazaprostan during pregnancy is prohibited.

If treatment is necessary for the period of breastfeeding, the child should be transferred to artificial mixtures.

Contraindications

Among the contraindications to the use of medication Vazaprostan identified as follows:

• decompensated stage of chronic heart failure;
• cardiac conduction abnormalities;
• acute stage of ischemic heart disease;
• presence in the anamnesis of myocardial infarction during the last six months;
• signs of pulmonary edema, as well as infiltrative pathology of pulmonary tissue;
• obstruction of the lungs;
• a violation of the functional capacity of the liver, previously transferred liver pathology;
• associated diseases with increased risk of bleeding (gastrointestinal ulcers, damage to the vascular walls in the brain, traumatic lesions, diagnosed cases of proliferative retinopathy);
• simultaneous treatment with anticoagulant and vasodilating medications;
• the entire period of pregnancy;
• breast feeding of the child;
• childhood;
• allergic sensitivity to any of the components of the drug.

Taking medication Vazaprostan requires caution under reduced pressure, in patients with signs of heart failure, with type 1 diabetes, as well as hemodialysis.

[9]

Side effects Vasaprostan

Side effects from the use of medication Vazaprostan can be as follows:

• Migraine, convulsions, decreased efficiency, weakness, sensitivity disorders of the skin;
• hypotension, pain in the heart, arrhythmias, signs of AV blockade;
• nausea, upset of the chair, a feeling of discomfort in the stomach;
• allergy in the form of itchy skin rashes;
• redness, swelling, phlebitis at the injection site;
• increased sweating, fever, swelling;
• pain in the joints, febrile conditions, disruption of the kidneys, pulmonary edema.

Less common can be the development of shock, bleeding, the development of cardiac and renal insufficiency, hematuria, respiratory function disorders.

The listed side effects are reversible and, as a rule, disappear after lowering the dosage or discontinuing the drug.

[10], [11]

Overdose

Symptoms of an overdose of the drug:

• hypotension;
• tachycardia;
• blanching of the skin;
• increased sweating;
• bouts of nausea.

Such signs may occur along with ischemia of the heart muscle and symptoms of heart failure.

At initial signs of an overdose it is necessary to lower a dose of Vasaprostan or to cancel treatment. At the expressed deterioration of state of health it is recommended to apply symptomatic therapy with application of sympathomimetics.

Interactions with other drugs

Simultaneous use of vasoprostane enhances the effect of drugs that reduce blood pressure, dilate the peripheral vessels, as well as funds for the treatment of angina pectoris.

Use of the drug along with blood thinning and preventing its coagulability increases the risk of bleeding.

The vasodilating property of epinephrine or norepinephrine can be disrupted by joint administration with vasaprostan.

Such interactions are observed in those cases when the listed drugs were used immediately before or during therapy with vasaprostane.

[14]

Storage conditions

Medication Vazaprostan is to be stored in a place difficult for children, at room temperature.

If the powder inside the ampoule became much smaller and stuck together - it means that the ampoule is damaged. To use such a drug is unacceptable.

Shelf life

Shelf life Vazaprostan - up to 4 years.