Alprostan

Alprostan – _{the E1 prostaglandin} drug having vasodilating and angioprotektorny effect, improving peripheric circulation.

Form of release and structure

Dosage form – a concentrate for preparation of solution for infusions: transparent colourless solution (on 0,2 ml in ampoules, on 5 ampoules in PVC containers, 2 containers in a pack cardboard).

Contains in 1 ampoule:

• Active agent: alprostadit – 100 mkg;
• Auxiliary component: ethanol.

Indications to use

Alprostan – means for treatment of chronic obliterating diseases of arteries of the III-IV stage (according to Fontaine's classification).

Contraindications

Absolute:

• Unstable or severe form of stenocardia;
• Dekompensirovanny chronic heart failure, disturbances of a cordial rhythm;
• Acute and subacute myocardial infarction;
• The expressed abnormal liver functions;
• Fluid lungs, heavy bronkhoobstruktivny syndrome with signs of respiratory insufficiency, the infiltrative changes in lungs confirmed at clinical and radiological inspection;
• Overhydratation, oliguria, brain hypostasis;
• The diseases which are followed by risk of developing of bleeding (severe defeat of vessels of a brain, stomach ulcer or a 12-perstny gut, an extensive injury, a proliferative retinopathy with tendency to bleedings, etc.);
• Period of pregnancy and lactation;
• The age up to 18 years is also more senior than 75 years;
• Simultaneous use of vasodilators and/or anticoagulants;
• Hypersensitivity to components of Alprostan.

Relative (to apply with care):

• Cardiovascular insufficiency;
• Arterial hypotension;
• Diabetes mellitus of 1 type, diabetic angiopatiya;
• Hemodialysis.

Route of administration and dosage

Alprostan is entered intravenously. Just before introduction from lyophilisate prepare infusion solution.

The recommended cultivation: to dissolve contents of 1 ampoule with lyophilisate (0,2 ml) in 9,8 ml of solvent (5% or 10% of solution of glucose, normal saline solution). After cultivation concentration of an alprostadil in 10 ml of solution makes 100 mkg. The received solution if necessary can be dissolved in the bigger volume of solvent.

To adult patients appoint 50-200 mkg of 1 times a day. In hard cases the dose is increased to 50-100 mkg by 2 times a day. Lyophilisate is usually dissolved in 200-500 ml. Infusion duration – is not less than 2 hours.

The average duration of treatment – 14 days. In case of positive effect therapy is continued within 7-14 days. The general duration of use of drug should not exceed 28 days.

In case of lack of effect during the first 14 days of treatment Alprostan is cancelled.

For patients with renal failures (concentration of creatinine in blood serum it is more than 1,5 ml/dl) the initial dose makes 20 mkg. In 2-3 days if in it there is a need, the dose is increased to 40-60 mkg.

At a heart and renal failure the maximum volume of the entered liquid makes 50-100 ml a day.

Treatment duration for these categories of patients – 28 days.

Side effects

• From cardiovascular system: disturbances of a cordial rhythm, tachycardia, lowering of arterial pressure, stenocardia attacks;
• From a musculoskeletal system: at long therapy (of 4 weeks) – a hyperostosis of tubular bones (reversible);
• From the alimentary system: nausea, a sensation of discomfort in epigastriums, diarrhea, vomiting;
• From an urinary system: availability of blood in urine (hamaturia);
• From a nervous system: dizziness, headache;
• Allergic reactions: itch, skin rash;
• Laboratory indicators: a leukocytosis, a hyperbilirubinemia, a leukopenia, tranzitorny increase in activity of hepatic transaminases in blood serum; in individual cases – increase in a caption of S-reactive protein;
• Others: an indisposition, increased fatigue, a hyperthermia, an overhydratation, puffiness of an extremity to which vein drug infusion is carried out;
• Local reactions: symptoms of phlebitis proksimalny injection sites (disappear in several hours after the end of infusion or change of an injection site, specific treatment is not demanded; catheterization of the central vein allows to reduce the frequency of manifestation of this side effect).

The number of undesirable reactions depends on volume, concentration and the speed of performing infusions.

Special instructions

Only medical specialists having experience in angiology, conditions of cardiovascular system, familiar with modern methods of continuous control, and having for this purpose the corresponding equipment have to apply Alprostan.

During treatment it is necessary to control hemodynamic indicators of acid-base balance, biochemical indicators of blood and coagulant system of blood (patients with disturbances of coagulant system have blood or receiving simultaneous therapy by drugs which exert impact on system of hemocoagulation).

In case of side effects it is recommended to lower a drug dose.

Patients with a renal failure and coronary heart disease during treatment and within 1 day after its termination have to be in a hospital under observation of the doctor. In order to avoid development of an overhydratation it is desirable that the volume of the entered liquid at such patients did not exceed 50-100 ml a day. It is necessary to watch a condition of patients carefully: to control the arterial pressure and heart rate, if necessary – the body weight, balance of liquid, the central venous pressure or an echocardiography. At newborns Alprostan should be applied under constant control of arterial pressure, in the presence of conditions for carrying out artificial ventilation of the lungs.

Treatment of patients on a hemodialysis should be carried out in the post-dialysis period.

At patients with chronic obliterating diseases of arteries of the lower extremities use of Alprostan is a part of complex therapy, the clinical effect of treatment has long character and can be shown with a certain delay after the termination of a therapeutic course.

Alprostan can cause system effects in the form of dizziness, weaknesses or hypotensions which usually disappear soon after the termination of infusions therefore patients should be careful when driving and performing the types of activity demanding the increased speed of psychomotor reactions and concentration of attention.

Medicinal interaction

Alprostadil strengthens action of vasodilating and anti-hypertensive means.

At simultaneous use of antiagregantny and anticoagulating drugs, trombolitik, a tsefamandola, a tsefotetana, the tsefoperazona increases risk of bleeding.

Adrenomimetiki (Epinephrinum, Norepinephrinum) reduce vazodilatiruyushchy effect of drug.

Terms and storage conditions

To store in dry, protected from light, the place, unavailable to children, at a temperature of 1-5 °C. Not to freeze!

Period of validity – 2 years.

The solution prepared from lyophilisate can be stored at a temperature of 2-8 °C no more than 24 watch.