Vazaprostan

Vazaprostan – the drug with anti-aggregation and vasodilating action applied at treatment of chronic obliterating diseases of arteries.

Form of release and structure

Vazaprostan is released in the form of lyophilisate for preparation of solution for infusions (hydroscopic mass of white color), in glass ampoules, on 10 ampoules in a cardboard pack.

20 mkg or 60 mkg of active agent – an alprostadil are a part of one ampoule of lyophilisate (a klatratny complex with alfadeksy).

Excipients: альфадекс (α-cyclodextrin), anhydrous lactose.

Indications to use

Vazaprostan is shown at chronic obliterating diseases of arteries of III and IV stages (on Fontaine's classification).

Contraindications

Use of Vazaprostan is contraindicated at:

• The expressed disturbances of a heart rhythm;
• Chronic heart failure in a decompensation stage;
• Exacerbation of coronary heart disease;
• The myocardial infarction postponed to the last 6 months;
• Liver diseases in the anamnesis;
• Liver dysfunctions (increase in the ALT, nuclear Heating Plant, GGT level);
• Fluid lungs;
• Infiltrative diseases of lungs;
• Chronic obstructive lungs of a disease;
• The diseases which are followed by the increased risk of developing of bleedings including a peptic ulcer of a stomach and duodenum, severe defeat of vessels of a brain, a proliferative retinopathy with tendency to bleedings, extensive injuries;
• Hypersensitivity to an alprostadil and other components of drug.

Drug is also not appointed:

• Along with anticoagulating and vasodilating drugs;
• To the feeding and pregnant women;
• To patients of age up to 18 years (safety and efficiency are not established).

With care Vazaprostan is appointed:

• At arterial hypotension;
• To the patients who are on a hemodialysis (therapy should be carried out in the post-dialysis period);
• At cardiovascular insufficiency (control of loading of volume of solution carrier is necessary);
• The patient with a diabetes mellitus of 1 type, especially with extensive defeats of vessels.

Route of administration and dosage

Solution is prepared just before infusion performance. Use of the solution prepared more than 12 hours ago is not allowed.

Intra arterial introduction:

For intra arterial introduction ampoule contents (20 mkg of an alprostadil) are dissolved – in 50 ml of normal saline solution.

If other instructions are absent, 10 mkg of an alprostadil (a half of an ampoule) enter vnutriarterialno within 60-120 minutes by means of the device for infusion. In case of need, especially in the presence of necroses, it is possible to increase a dose to 20 mkg of an alprostadil (under strict control of portability). Such dose is usually applied to single daily infusion.

If intra arterial introduction of Vazaprostan is carried out through the established catheter, depending on severity of a disease and portability, the dose 0,1-0,6 ¡ú/kg in a minute with administration of drug within 12 hours is recommended when using the device for infusions.

Intravenous administration:

For intravenous administration of 40 mkg of an alprostadil (2 ampoules on 20 mkg) part in 50-250 ml of normal saline solution and enter intravenously within 2 hours 2 times a day or 60 mkg of an alprostadil (3 ampoules on 20 mkg) within 3 hours once a day.

The average duration of therapy - 2 weeks. In the absence of positive dynamics treatment is stopped, at improvement extension of therapy for 7-14 days is possible.

At patients with a renal failure (serumal creatinine is more than 1,5 mg/dl) intravenous administration of Vazaprostan should be begun with 20 mkg (1 ampoule on 20 mkg) within 2 hours. If necessary in 2-3 days it is possible to increase a single dose to 40-60 mkg.

For patients with a heart and renal failure the maximum volume of the entered liquid – 50-100 ml a day. Therapy duration – 4 weeks.

Side effects

At use of Vazaprostan development of disturbances from various systems of an organism is possible:

• Central and peripheral nervous system: a headache, spasms, dizziness, the general weakness, the increased fatigue, disturbance of sensitivity of mucous membranes and skin;
• Cardiovascular system: disturbances of a cordial rhythm, lowering of arterial pressure, pains behind a breast, AV blockade;
• Musculoskeletal system: hyperostosis of long tubular bones (lasting therapy more than 28 days);
• Alimentary system: nausea, feeling of discomfort in epigastriums, diarrhea, vomiting;
• Local reactions: hypostasis, erythema, sensitivity disturbance, pain, phlebitis;
• Allergic reactions: itch, skin rash;
• Laboratory indicators: leukopenia, leukocytosis, increase in level of transaminases, increase in a caption of S-reactive protein;
• Others: a hyperthermia, the increased sweating;
• Seldom: confusion of consciousness, arthralgia, fever, spasms of the central genesis, брадипноэ, fever, renal failure, psychosis, anury;
• Extremely seldom (less than 1% of cases): acute heart failure, shock, bleeding, hyperbilirubinemia, брадипноэ, drowsiness, tachypnea, breath depression of function, renal failure, anury, fibrillation of ventricles, hypoglycemia, supraventricular arrhythmia, AV blockade of the II degree, acrimony, neck muscle tension, hypercapnia, hypothermia, hamaturia, hyperemia of integuments, tachyphylaxis, anemia, thrombocytopenia, hyperpotassemia.

The side effects connected using Vazaprostan or with the procedure of catheterization are reversible after decrease in a dosage or the termination of infusion.

Special instructions

Vazaprostan can be applied only by the doctors having experience in angiology and familiar with methods of modern continuous control of cardiovascular system, and also having the equipment necessary for this purpose.

When performing therapy it is important to control the arterial pressure, biochemical indicators of blood, heart rate, indicators of coagulability of blood (at emergence of disturbances of coagulant system of blood or at simultaneous use with the drugs influencing coagulant system).

In order to avoid emergence of symptoms of an overhydratation in patients with a renal failure the volume of the entered liquid needs to be limited to 50-100 ml a day. It is necessary to make dynamic observation of a condition of patients (control of arterial pressure and heart rate), if necessary – control of balance of liquid, body weight, carrying out an echocardiographic research or measurement of the central venous pressure.

Patients with coronary heart disease, renal failures and peripheral hypostases (serumal creatinine is more than 1,5 mg/dl) during use of Vazaprostan and within 1 day after the termination of therapy have to be in a hospital under observation of the doctor.

As a rule, phlebitis (proksimalny injection sites) is not the reason for the treatment termination, symptoms of an inflammation pass in several hours after change of an injection site of drug or the termination of infusion. Specific treatment in similar cases is not carried out. Catheterization of the central vein allows to reduce the frequency of manifestation of this side effect of drug.

Vazaprostan can exert impact on ability to control of mechanisms and to driving of motor transport in the period of an initiation of treatment, increase in a dosage and drug withdrawal, and also at alcohol intake.

Analogs

Analog of Vazaprostan are lyophilisate of Kaverdzhekt.

Terms and storage conditions

To protect from children. To store at a temperature not above 25 °C. A period of validity – 4 years.

At damage of an ampoule lyophilisate considerably decreases in volume and becomes sticky. In this case it is impossible to use drug.