Vazaprostan

Description overdue on 08/12/2014

• Latin name: Vazaprostan
• ATC code: C01EA01
• Active substance: Alprostadil (Alprostadil)
• Manufacturer: Bayer HealthCare AG (Germany)

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use vazaprostan (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

1 vial contains 20 micrograms vazaprostan or 60 mcg alprostadil   (active ingredient in combination with   alfadeksom ).

Auxiliary ingredients: alfadeks lactose.

Product form

Available in the form of freeze-dried product (powder) for solution for infusion. 1 pack contains 10 ampoules.

Pharmacological action

It has antiaggregant and vasodilating action.

Pharmacodynamics and pharmacokinetics

The drug Vazaprostan improves peripheral circulation and microcirculation Thereby exhibiting vasoprotective action. Systemic administration of the drug leads to relaxation smooth muscle fibers , Vasodilatation, reduced PR , Without affecting blood pressure. At the same time there is a reflex gain Emergency   and cardiac output.   The drug reduces the platelet aggregation , Enhances erythrocyte elasticity It reduces the activity of neutrophils, amplifies fibrinolytic activity blood. Alprostadil   characterized by a stimulating effect on the smooth muscles of the uterus, bladder and bowel, and also inhibits the secretion of gastric juice.

The drug is administered intramuscularly, or in combination with intra- alpha-cyclodextrin . In preparing the solution it is separated complex PGE1   and alpha-cyclodextrin. Therapeutic concentrations of the active substance, when administered intravenously, is observed within a few minutes after administration, reaching a maximum after 100-120 minutes. So how PGE 1   this endogenous substances , Its half-life is very short, and the concentration in the blood after administration, already after 10 seconds comes to the original value.

Contact PGE1   plasma proteins is - 93%.

Biotransformation PGE 1   mainly takes place in the lungs, to form a staple metabolism (15-keto - PGE1; 15- keto - PGE0 and PGE0) . Metabolism   undergoes 60-90% of active ingredient.

Main metabolites   for 72 hours appear through the digestive tract (12%) and urine (88%).

The half-life alpha-cyclodextrin is approximately 7 minutes. In unaltered state excreted in the urine.

Indications

Vazaprostan used for the treatment of severe stages (3-4 stages of Fontaine) obliterating chronic arterial disease :

• angiopathy , because of diabetes;
• endarteriit   lower limbs, in case of failure of surgery to restore blood flow;
• vasculitis , Systemic diseases;
• disease and Raynaud's syndrome;
• as a therapy for patients with temporary heart defects,   that are open ductus arteriosus.

Contraindications

• Individual sensitivity to other substances vazaprostan;
• CHF (congestive heart failure);
• expressed pathology of heart rate;
• exacerbation Coronary artery disease;
• pulmonary edema;
• recent myocardial infarction   (Within 6 months);
• infiltrative and chronic obstructive pulmonary disease;
• liver disease Including a history;
• disease, which can lead to bleeding and hemorrhage (cerebrovascular disease, gastrointestinal ulcer, proliferative retinopathy, injury, etc.) ;
• current treatment with anticoagulants   and vasodilators   tools;
• period breast-feeding ;
• during pregnancy.

Side effects

Nervous system :

• convulsions;
• headache ;
• fatigue;
• dizziness ;
• malaise;
• lowering the sensitivity of the mucous membranes and skin.

Cardiovascular system :

• cardiac arrhythmias;
• lowering blood pressure;
• pain behind the breastbone;
• AV block.

Digestive system :

• discomfort epigastric;
• dyspeptic disorders .

Locomotor apparatus :

• long-term therapy possible   hyperostosis   long bones.

Local reactions :

• pain;
• erythema;
• swelling;
• phlebitis;
• the weakening of sensitivity.

Laboratory findings :

• leukopenia;
• leukocytosis;
• level increase transaminases;
• increase titer of C-reactive protein.

Others:

• increased sweating;
• puffiness ;
• hyperthermia ;
• joint pain.

In rare cases, we observed:

• confusion;
• fever;
• seizures of central origin ;
• bradypnea;
• chills;
• arthralgia;
• renal insufficiency;
• psychosis;
• anuria.

Present data on the number of cases of acute left ventricular failure and pulmonary edema.

Rarely:

• congestive heart failure;
• shock;
• bleeding ;
• hyperbilirubinemia;
• reduction in respiratory function;
• tachypnea;
• hypoglycemia;
• violation of the kidneys;
• ventricular fibrillation;
• supraventricular arrhythmia;
• AV blockade II degree;
• irritability;
• tension of the neck muscles;
• hypothermia;
• dermahemia ;
• hypercapnia;
• peritoneal signs;
• hematuria;
• tachyphylaxis;
• thrombocytopenia;
• hyperkalemia;
• anemia.

Allergic reactions:

• itching;
• skin rash.

Side effects that are associated with the procedure of administration disappear on their own, or at lower doses at the end of infusion.

Instructions for use vazaprostan (method and dosage)

Instructions on Vazaprostan involves intravenous or intra-arterial administration of a drug.

When intra-arterial administration of the contents of one vial of the drug (20 mg alprostadil ) Dissolved in saline (50 ml).

If there are no other recommendations, spend half of intra-arterial injection vials (10 mg) as a vazaprostan infusion over 60 - 120 minutes. With endarteriite   in severe forms with necrosis   may increase the dose by half (20 mg). This dosage is generally a single daily dose infusion.

In the case of intra-arterial infusion administration using a catheter, the recommended dose alprostadil   can be 0, 1 ng / kg / min (0, 25 ampoules) 0 to 6 ng / kg / min (1, 5 ampoules), depending on the severity of disease and drug tolerability. Infusion is performed over 12 hours.

When assigning the contents of two intravenous infusions vazaprostan ampoules (40 mg) was dissolved in 50 ml - 250 ml of saline. The resulting solution as an infusion is administered twice a day for two hours. At the recommended dose - 3 vials (60 mg), a one-time infusion carried out for 3 hours.

If the kidney function (level creatinine   greater than 1, 5 mg / dL) begin intravenous infusion at a dose of 20 micrograms and was carried out for 2 hours. If required, you can increase the dose to 40 - 60 g, 2-3 days.

Patients with heart   and renal failure   reduce the amount of the injected solution to 50 ml / day - 100 ml / day. The course of treatment is 4 weeks.

The recommended duration of therapy an average of two weeks. In case of positive dynamics can continue treatment for another 14 days. A negative effect of the introduction of vazaprostan for two weeks of therapy, should renounce the use of this drug and find another drug.

Preparation of the solution is carried out directly prior to use. Powder, by adding physiological saline, and quickly dissolves first may acquire milky turbid color, because it got in the air bubbles. After some time the solution must obtain uniformity and transparency. It does not use a solution prepared more than 12 hours ago.

Overdose

If overdose Vazaprostan possible decrease in blood pressure, development reflex tachycardia , and hyperemia   skin, nausea and vomiting, increased sweating. It may be myocardial ischemia   and symptoms Heart Failure . Of the local reactions - swelling, pain, redness at the injection site.

Is recommended to reduce the dose or interrupt infusion administration. The patient is shown to take a horizontal position with raised legs. With the progression of the symptoms of an overdose of prescribed sympathomimetics.

Cooperation

Alprostadil   able to enhance the effect of antihypertensive drugs, antianginal drugs, and vasodilators.

Joint reception with drugs that prevent blood clotting ( platelet aggregation inhibitors, anticoagulants ) And with thrombolytics, cefoperazone, cefamandole, tsefotetanom   increases the risk of bleeding.

Vasodilating effect is reduced by the concomitant use of sympathomimetics.

Keep in mind that possible pharmaceutical interactions when taking the above medications shortly before the start of therapy Vazaprostanom.

Terms of sale

Vazaprostan drug prescription.

Storage conditions

The drug belongs to the list B. Store at temperatures not above 25 ° C.

Shelf life

4 years.

Cautions

Introduction vazaprostan may make only an experienced medical staff with appropriate knowledge Angiology   and suitable equipment.

During therapy, you need to constantly monitor the biochemical parameters of blood, Blood pressure, heart rate, blood clotting ability,   especially when violations blood clotting   held or treatment affecting her preparations.

Patients suffering Coronary artery disease, renal dysfunction, peripheral edema   Vazaprostanom during infusion should be in a hospital, under constant supervision of the attending physician during the days after injection.

With renal failure,   to avoid overhydration,   recommend administering fluids to patients in an amount not exceeding 50-100 ml per day. It is mandatory for the dynamic monitoring of the general state of the patient, control Blood pressure and heart rate.

Should also monitor changes the fluid balance and body weight, to measure central venous pressure and, if necessary, echocardiography .

Developing   phlebitis   usually it is not grounds for termination of the infusion. Signs vascular inflammation   disappear on their own within a few hours after the change of the site of administration or discontinuation of the infusion. In such cases, a specific treatment is not required. Setting catheter   a central vein can significantly reduce the incidence of this side effect.

The contents of the ampule vazaprostan which becomes sticky and wet, says about the damage of the primary packaging of the drug. In this case the drug can not be used.

Analogs vazaprostan

Among the many unique product Vazaprostan are:

• Plavix;
• Tiklid;
• Curantil;
• Vases;
• Trental;
• Tanakan;
• Clexane;
• Fraksiparin;
• Aktovegin;
• Vessel Due   etc.

During pregnancy and lactation

Do not use during pregnancy and lactation.

Reviews Vazaprostane

Among doctors Vazaprostan considered the most effective drug, especially in atherosclerosis. It noted its high efficiency and quick action, leading to the positive dynamics of the disease. However, it is worth noting that in some severe forms of disease can be very difficult to achieve positive results without surgery.

Also on the internet - forums have a lot of positive feedback about Vazaprostane, despite its cost.

Price vazaprostan where to buy

In Russia, the approximate price vazaprostan 60 micrograms of №10 - 15,000 rubles; 20 g №10 - 9000 rubles.

Vazaprostan drug you can buy in Kiev in about 3000 hryvnia - 20 g №10 and 7,000 hryvnia - 60 g №10.

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