VAP 20 - instructions for use, doses, side effects, contraindications

The analogue of natural PGE₁ (prostaglandin E₁), has vasodilator (at the level of arterioles, precapillary sphincters, muscular arteries), antiplatelet and angioprotective action. Improves microcirculation and peripheral blood circulation, contributes to the discovery of collateral vessels. Reduces the overall peripheral vascular resistance,arterial pressure, reflexively increases the heart rate, which leads to an increase in the minute volume of blood.

It improves the rheological properties of blood, promoting the increase of the elasticity of red blood cells and reducing the adhesion / aggregation of platelets. Has a fibrinolytic effect.

Stimulates the smooth muscles of the intestine, bladder and uterus; suppresses the secretion of gastric juice

Pharmacokinetics:

Alprostadil is a synthetic analogue of natural prostaglandin E1 with a short half-life of T1 / 2 (about 10 s). When administered intravenously, it is metabolized in the lungs (at a single passage up to 60-90%). As a result of enzymatic oxidation, biologically active metabolites are formed: 15-KeTO-PgE₁, 15-keto-13,14-dihydro-PgE₁ and 13,14-dihydro-PGE₁ (NGE₀). Keto metabolites have a lower biological effect compared to alprostadil, the PGE metabolite₀ is comparable with PGE₁ action. PGE₀ lasts longer, its T1 / 2 is about 1 min (alpha phase) and 30 min (beta phase). In all likelihood, the pharmacodynamic effect is mainly caused by this biologically active stable metabolite.The main metabolites are excreted by the kidneys - up to 88% and the intestine -12 %.

Indications:

Chronic obliterating diseases of the arteries of the III and IV stages (according to Fontaine's classification).

Contraindications:

Hypersensitivity to alprostadil or other components of the drug.

Chronic heart failure, severe cardiac rhythm disturbances, exacerbation of coronary heart disease, myocardial infarction or stroke in the last 6 months.

Pulmonary edema, infiltrative lung diseases, chronic obstructive pulmonary diseases.

Liver dysfunction (increased activity of aspartate aminotransferase, alanine aminotransferase or gamma-glutamyltransferase) and severe liver disease in the anamnesis, as well as diseases accompanied by an increased risk of bleeding (stomach ulcer, duodenal ulcer, extensive trauma).

Concomitant therapy with vasodilating and anticoagulant drugs.

Pregnancy and lactation.

General contraindications for infusion therapy, such as heart failure in the stage of decompensation, pulmonary or brain edema, functional kidney disorders (oliguria), and hyperhydration.

Children under 18 years.

Carefully:

The use of VAP20 with arterial hypotension, cardiovascular insufficiency, in patients on hemodialysis (treatment should be performed in the postdialysis period), in patients with diabetes mellitus, especially with diabetic angiopathy.

Pregnancy and lactation:

Application in pregnancy is contraindicated, breastfeeding should be abolished.

Dosing and Administration:

Enter intravenously. The solution should be prepared immediately before the introduction. 1-2 ampoules (20 μg or 40 μg) are dissolved in a 0.9% solution of sodium chloride or 5% dextrose solution to a volume of 100-250 ml. The solution ready for use is suitable for 24 hours if stored in a refrigerator (2-8 ° C) in a dark place. Do not use a solution cooked more than 24 hours ago.

50-250 ml of the ready solution for infusions, concentration of alprostadil - 40 μg, administered intravenously for 2 hours (333 ng / min), infusion rate 0.4-2 ml / min. VAP20 is administered Once a day, with severe clinical symptoms of the disease, it is possible to administer VAP20 2 times a day. The duration of treatment on average - 14 days, with a positive effect, treatment with the drug can continue for another 7-14 days. The course of treatment should not exceed 4 weeks.In the absence of a positive effect within 2 weeks from the start of treatment, further use of the drug should be discontinued.

If the renal function is impaired (the concentration of creatinine in the blood serum is more than 1.5 mg / dL) intravenous administration starts with 20 μg. If necessary, after 2-3 days, the single dose is increased to 40-60 μg. For patients with renal insufficiency and heart failure, the maximum volume of injected fluid is 50-100 ml / day. The course of treatment is 4 weeks.

Side effects:

From the central nervous system: headache, convulsive syndrome, dizziness, excessive fatigue, a feeling of malaise, a violation of the sensitivity of the skin and mucous membranes.

From the cardiovascular system: reduction of blood pressure, chest pain, heart rhythm disturbances, atrioventricular blockade.

From the digestive system: a feeling of discomfort in the epigastric region, dyspeptic phenomena - diarrhea, nausea, vomiting

From the musculoskeletal system: reversible hyperostosis of long tubular bones (with continuous continuous administration from 4 weeks).

Local reactions: pain, edema, erythema, impaired sensation, phlebitis (proximal to the site of intravenous administration).

Laboratory indicators: leukocytosis, leukopenia, an increase in the titer of C-reactive protein, an increase in the activity of transaminases.

Other: increased sweating, hyperthermia, puffiness of the extremity, in the vein of which the infusion is performed.

Rarely: pain in the joints, confusion, convulsions of the central genesis, fever, chills, bradypnoe, arthralgia, psychosis, renal failure, anuria. Several cases of pulmonary edema and acute left ventricular failure were reported.

Allergic reactions: skin rash, itching.

The side effects associated with the use of the drug or with the procedure itself of the catheterization disappear after a dose reduction or discontinuation of the infusion.

Overdose:

An overdose of the drug can be manifested by lowering blood pressure (BP) and increasing heart rate (heart rate). Possible development of vasovagal reactions with pallor of the skin, increased sweating, nausea and vomiting, which can also be accompanied by myocardial ischemia and symptoms of heart failure, as well as pain,swelling and redness of the tissue at the site of infusion.

If symptoms of an overdose need to reduce the dose of the drug or stop the infusion. With a marked decrease in blood pressure, the patient in the prone position should raise his legs.

Interaction:

Alprostadil can enhance the effect of antihypertensive drugs, vasodilators and antianginal drugs. The simultaneous use of alprostadil in patients, taking drugs that prevent blood clotting (anticoagulants, antiaggregants), may increase the chance of bleeding. AT combinations with cefamandol, cefoperazonom, cefotetan and thrombolytic - increases the risk of bleeding. Adrenomimetics - epinephrine, norepinephrine - reduce the vasodilating effect.

It should be taken into account that drug interactions are possible if the above-mentioned drugs were used shortly before the drug therapy was started.

Special instructions:

Alprostadil can be prescribed only by physicians with experience in angiology, familiar with modern methods of continuous monitoring of the cardiovascular system and having for this purpose appropriate equipment.

The prepared solution is recommended to be used immediately after preparation, it is possible to temporarily store the resulting solution for not more than 24 hours at a temperature of 2 to 8 ° C.

During the period of treatment, it is necessary to control blood pressure and heart rate, biochemical parameters of the blood, coagulation system (for violations of the blood coagulation system or for simultaneous therapy with drugs that affect the coagulation system). Patients with coronary heart disease, renal insufficiency (serum creatinine more than 1.5 mg / dL) should be monitored. in the hospital during treatment with alprostadil and within 1 day after discontinuation of treatment. In order to avoid the appearance of symptoms of hyperhydration in such patients, the volume of injected liquid should not exceed 50-100 ml per day, if possible. It requires dynamic monitoring of the patient's condition (control of blood pressure and heart rate), if necessary - control of body weight, fluid balance, measurement of central venous pressure or echocardiography (echocardiography).

In patients with chronic obliterating diseases of lower extremity arteries, infusion therapy is a necessary part of complex treatment.The clinical effect is long-term and may occur with a certain delay after the completion of the course of treatment.

Phlebitis (proximal to the injection site), as a rule, is not a reason to stop therapy, signs of inflammation disappear after a few hours after stopping the infusion or changing the place of administration, no specific treatment is required in such cases. Central vein catheterization can reduce the incidence of this side effect.

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

The drug may affect the ability to actively participate in street traffic or management mechanisms, especially at the beginning of treatment, with increasing doses and withdrawal of the drug, as well as with the simultaneous intake of alcohol.

Form release / dosage:

Concentrate for the preparation of a solution for infusions of 20 mcg / ml.

Packaging:

For 1.0 ml in ampoules of brown neutral glass (type I Ph. Eur.) with a ring of white color.

For 5 or 10 ampoules together with the instructions for use, in a cardboard box with a special holder for ampoules.

Storage conditions:

List B.

At a temperature of 2 to 8 ° C (in the refrigerator), in a place protected from light. Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date!

Terms of leave from pharmacies:On prescription

Registration number:LSR-005103/10

Date of registration:01.06.2010

Expiration Date:Unlimited

The owner of the registration certificate:SEM Pharmaceuticals LimitedSEM Pharmaceuticals Limited Cyprus

Manufacturer: & nbsp

DREHM Pharma GmbH, Austria Austria

Representation: & nbspSEM Pharmaceuticals LimitedSEM Pharmaceuticals LimitedRussia

Information update date: & nbsp22.01.2017

Illustrated instructions

Instructions

VAP® 20 (Vap® 20)