Alprostan (alprostadil) concentrate for infusions 0.1 mg/0.2 ml. 0.2 ml. ampoules №10

Description

Ingredients

active substance: alprostadil;

1 ampoule (0.2 ml of solution) contains 0.1 mg of alprostadil;

excipient: anhydrous ethanol. 

Pharmacotherapeutic group

Cardiological drugs. Prostaglandins. ATX code C01E A01. 

Pharmacodynamics

Alprostadil is a synthetic analogue of prostaglandin E1, which is present in the human body under normal conditions. Its effect is complex and is based on the promotion of microcirculation and the opening of collateral vessels. In the systemic and pulmonary blood circulation, alprostadil causes vasodilatation (at the level of arterioles and precapillary sphincters and/or also in muscular arteries), relaxes the smooth muscles of the cavernous bodies, and in the fetal blood circulation, alprostadil maintains the open state of the ductus arteriosus. It affects blood coagulation, acting as an anti-adhesive and anti-aggregation substance on platelets. Alprostadil improves the rheological properties of blood by increasing the flexibility of erythrocytes and reducing the aggregation ability of platelets. It exerts an antiatherogenic effect by inhibiting the activation of neutrophils and excessive proliferation of vascular wall cells, as well as by reducing cholesterol synthesis and its deposition in vessel walls. Alprostadil also has a fibrinolytic effect.

Indication

• Chronic ischemia of the lower extremities at the stage of pain at rest and trophic changes (stages III and IV).
• Critical congenital heart defects in newborns associated with non-union of the ductus arteriosus, in which surgical reconstruction is indicated (in order to temporarily ensure the functioning of the ductus arteriosus before corrective surgery).

Contraindication

Hypersensitivity to the active substance or to any of the excipients.

With chronic ischemia of the lower extremities:

• pregnancy and/or breastfeeding;
• class III and IV heart failure according to the classification of the New York Heart Association (NYHA), arrhythmias with significant hemodynamic disturbances, insufficiently controlled coronary heart disease, insufficiency of the mitral and/or aortic valves and/or stenosis of these valves, the presence of a history of myocardial infarction (MI ) during the last 6 months;
• acute pulmonary edema or a history of pulmonary edema in patients with heart failure;
• severe chronic obstructive pulmonary disease or veno-occlusive disease of the lungs, the presence of a pulmonary infiltrate, confirmed by chest X-ray examination or clinically;
• cerebral edema and hyperhydration;
• acute liver failure (increased levels of transaminases or gamma-glutamyltransferase) or clinical manifestations or history of severe liver failure;
• the risk of hemorrhagic complications (stroke, gastric or duodenal ulcer, proliferative retinopathy with a tendency to bleeding/hemorrhages, polytrauma, etc.);
• violation of cerebral blood circulation in the anamnesis during the last 6 months;
• severe arterial hypotension; renal dysfunction (oligoanuria);
• general contraindications for infusion therapy (for example, decompensated heart failure, pulmonary or cerebral edema, and hyperhydration).

Preservation of patency of the ductus arteriosus:

• respiratory distress syndrome;
• spontaneous permanent non-occlusion of the ductus arteriosus.

Directions

The doses prescribed for each of the two indicated indications for use differ significantly.

Chronic ischemia of the lower extremities

In adults, for the treatment of ischemia of the lower extremities, the drug is used intravenously for several weeks. The recommended dose is from 50 to 200 μg/day, which is administered once a day or in the form of two separate doses of 200–500 ml of the drug solution each during at least a two-hour infusion.

An isotonic solution of sodium chloride (physiological solution), 5% or 10% glucose solution is used as a solvent. Such a solution should be prepared immediately before the infusion.

The course of treatment should last at least two weeks; in the case of a positive effect, the treatment should be carried out for another 7–14 days. However, the course of treatment should not exceed four weeks. If the desired effect is not achieved during the first two weeks of treatment, the drug should be discontinued.

Preservation of ductus arteriosus patency

It is preferable to use alprostadil in newborns by continuous intravenous infusion (as an alternative, by introducing into the ductus arteriosus through the umbilical artery). The recommended starting dose is 0.01–0.05 mcg/kg/min; if a therapeutic response is registered, that is, signs of opening or re-opening of the ductus arteriosus, the dose of the drug should be reduced to the minimum effective therapeutic dose (usually 0.01–0.02 μg/kg/min). In exceptional cases, if the initial dose is not effective, the dose of the drug can be increased to 0.1 mcg/kg/min. Serious adverse reactions to the drug are a reason to reduce the dose.

During the use of the drug, monitoring of the main indicators of vital activity, hemodynamic indicators and acid-alkaline balance (blood gas composition) should be carried out.

Recommendations for diluting the concentrate for use by newborns

The contents of 1 ampoule of the drug Alprostan® (0.2 ml) are dissolved in 9.8 ml of a suitable solvent (for example, physiological saline, 5% or 10% glucose solution), which makes it possible to achieve a concentration of 100 μg of alprostadil in 10 ml of solution. The resulting solution should be further made up to a larger volume with a suitable solution suitable for the application.

Children. This medicine is used by newborns according to the indications.