Vasaprostan
Vasaprostan: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Vazaprostan
ATX code: C01EA01
Active ingredient: alprostadil (Alprostadil)
Manufacturer: Bayer Pharma AG (Germany); IDT Biologika, GmbH (Germany)
Description and photo updated: 2019-27-08
Prices in pharmacies: from 6000 rubles.
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Vasaprostan is a drug with antiaggregatory and vasodilating effect, used in the treatment of chronic obliterating arterial diseases.
Release form and composition
Vasaprostan is produced in the form of a lyophilisate for the preparation of a solution for infusion: a hygroscopic white mass (in glass ampoules, 10 ampoules in a cardboard box and instructions for the use of Vasaprostan).
One ampoule of lyophilisate contains 20 μg or 60 μg of the active substance - alprostadil (a clathrate complex with alphadex).
Excipients: Alfadex (α-cyclodextrin), anhydrous lactose.
Pharmacological properties
Pharmacodynamics
Vasaprostan is a prostaglandin E1 (PG E1) drug that has a vasoprotective effect. Thanks to the use of the drug, microcirculation and peripheral circulation are improved. With systemic therapy, relaxation of smooth muscle fibers is observed.
Other effects of the active ingredient of Vazaprostan - alprostadil include:
- Vasodilatory action, reduction of the total peripheral vascular resistance without changing blood pressure. At the same time, a reflex increase in heart rate and cardiac output is noted;
- Decrease in the activity of neutrophils and platelet aggregation, increase in the elasticity of erythrocytes, increase in the fibrinolytic activity of the blood;
- Suppression of gastric acid secretion;
- Stimulating effect on the smooth muscles of the bladder, intestines, uterus.
Pharmacokinetics
Alprostadil is used in combination with alphacyclodextrin (intravenous or intra-arterial). When preparing a solution, the complex decomposes into separate components - PG E1 and alphacyclodextrin.
The therapeutically significant concentration of the active substance when administered intravenously is reached shortly after the start of administration, and C max (maximum concentration) in blood plasma - within 2 hours.
The binding of PG E1 to plasma proteins is at the level of 93%.
Metabolism of PG E1 occurs mainly in the lungs, during the first passage through the lungs, about 60–90% of the active substance is metabolized, with the formation of the main metabolites - 15-keto-PG E0, 15-keto-PG E1 and PG E0.
PG E1 is an endogenous substance that is characterized by an extremely short T 1/2 (half-life). The plasma concentration in the blood returns to the initial level 10 seconds after the termination of the administration. It is excreted in the urine and through the gastrointestinal tract (at 88 and 12%, respectively) within 72 hours in the form of metabolites.
T 1/2 alphacyclodextrin is approximately 7 minutes, excreted unchanged in the urine.
Indications for use
Vasaprostan is indicated for chronic obliterating arterial diseases stage III and IV (according to Fontaine's classification).
Contraindications
The use of Vasaprostan is contraindicated in:
- Severe heart rhythm disturbances;
- Chronic heart failure in the stage of decompensation;
- Exacerbation of ischemic heart disease;
- Myocardial infarction transferred in the last 6 months;
- History of liver disease;
- Liver dysfunction (increased levels of ALT, AST, GGT);
- Pulmonary edema;
- Infiltrative lung diseases;
- Chronic obstructive pulmonary disease;
- Diseases accompanied by an increased risk of bleeding, including gastric ulcer and duodenal ulcer, severe cerebrovascular disease, proliferative retinopathy with a tendency to bleeding, extensive trauma;
- Hypersensitivity to alprostadil and other components of the drug.
Vasaprostan is also not prescribed:
- Simultaneously with anticoagulant and vasodilator drugs;
- Lactating and pregnant women;
- Patients under 18 years of age (safety and efficacy have not been established).
Vazaprostan is prescribed with caution:
- With arterial hypotension;
- Patients on hemodialysis (therapy should be carried out in the post-dialysis period);
- In case of cardiovascular insufficiency (it is necessary to control the load of the volume of the carrier solution);
- Patients with type 1 diabetes mellitus, especially with extensive vascular lesions.
Vasaprostan, instructions for use: method and dosage
The solution is prepared just prior to infusion. The use of a solution prepared more than 12 hours ago is not allowed.
Intra-arterial administration
For intra-arterial administration, the contents of the ampoule (20 μg of alprostadil) are dissolved in 50 ml of saline.
Unless otherwise prescribed, 10 mcg of alprostadil (half an ampoule) is administered intra-arterially over 60-120 minutes using an infusion device. If necessary, especially in the presence of necrosis, the dose can be increased to 20 μg of alprostadil (under strict tolerance control). This dose is usually given as a single daily infusion.
If intra-arterial administration of Vazaprostan is carried out through an installed catheter, depending on the severity of the disease and tolerance, a dose of 0.1-0.6 ng / kg per minute is recommended with the introduction of the drug within 12 hours when using an infusion device.
Intravenous administration
For intravenous administration, 40 μg of alprostadil (2 ampoules of 20 μg) are diluted in 50-250 ml of saline and injected intravenously for 2 hours 2 times a day or 60 μg of alprostadil (3 ampoules of 20 μg) for 3 hours 1 time day.
The average duration of therapy is 2 weeks. In the absence of positive dynamics, treatment is stopped, with improvement, it is possible to extend therapy for another 7-14 days.
In patients with renal insufficiency (serum creatinine greater than 1.5 mg / dL), intravenous administration of Vazaprostan should be started with 20 μg (1 ampoule of 20 μg) for 2 hours. If necessary, after 2-3 days, a single dose can be increased to 40-60 mcg.
For patients with heart and renal failure, the maximum volume of injected fluid is 50-100 ml per day. The duration of therapy is 4 weeks.
Side effects
With the use of Vazaprostan, the development of disorders from various body systems is possible:
- Central and peripheral nervous system: headache, convulsions, dizziness, general weakness, increased fatigue, impaired sensitivity of the mucous membranes and skin;
- Cardiovascular system: cardiac arrhythmias, lowering blood pressure, chest pain, AV block;
- Musculoskeletal system: hyperostosis of long bones (with a duration of therapy more than 28 days);
- Digestive system: nausea, epigastric discomfort, diarrhea, vomiting;
- Local reactions: edema, erythema, impaired sensitivity, pain, phlebitis;
- Allergic reactions: itching, skin rash;
- Laboratory indicators: leukopenia, leukocytosis, increased transaminase levels, increased C-reactive protein titer;
- Others: hyperthermia, increased sweating;
- Rarely: confusion, arthralgia, fever, seizures of central origin, bradypnea, chills, renal failure, psychosis, anuria;
- Extremely rare (less than 1% of cases): acute heart failure, shock, bleeding, hyperbilirubinemia, bradypnea, drowsiness, tachypnea, decreased respiratory function, impaired renal function, anuria, ventricular fibrillation, hypoglycemia, supraventricular arrhythmia, II degree AV block, increased irritability, neck muscle tension, hypercapnia, hypothermia, hematuria, skin hyperemia, tachyphylaxis, anemia, thrombocytopenia, hyperkalemia.
Side effects associated with the use of Vasaprostan or with the catheterization procedure are reversible after lowering the dosage or stopping the infusion.
Overdose
The main symptoms: a decrease in blood pressure, an increase in heart rate, vasovagal reactions may develop (manifested in the form of increased sweating, pallor of the skin, nausea, vomiting); this may be accompanied by symptoms of heart failure and myocardial ischemia; swelling, tissue redness, and pain at the infusion site are also possible.
Therapy: reducing the dose of Vasaprostan or stopping the infusion. With a pronounced decrease in blood pressure, the patient is transferred to the supine position with raised legs. If symptoms persist, sympathomimetics are prescribed.
special instructions
Vasaprostan can only be used by doctors with experience in angiology and familiar with the methods of modern continuous monitoring of the cardiovascular system, as well as having the necessary equipment.
When carrying out therapy, it is important to control blood pressure, blood biochemical parameters, heart rate, blood coagulation indicators (in the event of disorders of the blood coagulation system or when used simultaneously with drugs that affect the coagulation system).
In order to avoid the appearance of symptoms of overhydration in patients with renal insufficiency, the volume of injected fluid should be limited to 50-100 ml per day. It is necessary to carry out dynamic monitoring of the patient's condition (control of blood pressure and heart rate), if necessary, control of fluid balance, body weight, echocardiographic examination or measurement of central venous pressure.
Patients with ischemic heart disease, impaired renal function and peripheral edema (serum creatinine greater than 1.5 mg / dL) while using Vasaprostan and within 1 day after stopping therapy should be in the hospital under medical supervision.
As a rule, phlebitis (proximal to the injection site) is not a reason for stopping treatment, the symptoms of inflammation disappear a few hours after changing the injection site or stopping the infusion. Specific treatment in such cases is not carried out. Central vein catheterization can reduce the incidence of this side effect of Vasaprostan.
Influence on the ability to drive vehicles and complex mechanisms
Vasaprostan may affect the ability to control mechanisms and drive vehicles during the period of starting treatment, increasing the dosage and discontinuing the drug, as well as when taking alcohol.
Application during pregnancy and lactation
Vasaprostan is not prescribed during pregnancy / lactation.
Pediatric use
For patients under 18 years of age, Vasaprostan is not prescribed.
With impaired renal function
In patients on hemodialysis, Vazaprostan is used with caution, therapy should be carried out in the post-dialysis period.
For violations of liver function
In case of impaired liver function (in patients with elevated levels of aspartate aminotransferase, alanine aminotransferase and gamma-glutamyltransferase), as well as with a burdened history of liver disease, the use of Vasaprostan is contraindicated.
Drug interactions
- Antihypertensive and antianginal drugs, peripheral vasodilators: their effect is enhanced;
- Epinephrine (adrenaline), norepinephrine (norepinephrine): vasodilating effect decreases;
- Anticoagulants, platelet aggregation inhibitors, cefamandol, cefoperazone, cefotetan, thrombolytics: the likelihood of bleeding increases.
It should be borne in mind that interaction can develop if the above drugs were used shortly before the start of therapy with Vasaprostan.
Analogs
The analogs of Vasaprostan are: VAP 20, Vasostenon, Muse, Alprostadil, Alprostan, Kaverjekt, Edex, etc.
Terms and conditions of storage
Keep out of the reach of children. Store at a temperature not exceeding 25 ° C. Shelf life is 4 years.
If the ampoule is damaged, the lyophilisate significantly decreases in volume and becomes sticky. In this case, the drug cannot be used.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Vasaprostan
According to reviews, Vasaprostan is isolated as an effective drug for the treatment of severe vascular pathologies. Patients note that the action of the drug develops quickly. There are reports of side effects, most often headaches. The cost is assessed as high.
The price of Vazaprostan in pharmacies
The approximate price for Vazaprostan (10 ampoules of 20 mcg) is 8199–9834 rubles.
Vazaprostan: prices in online pharmacies
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Drug name Price Pharmacy |
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Vasaprostan 20 μg lyophilisate for preparation of solution for infusion 10 pcs. RUB 6000 Buy |
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Vasaprostan lyof. for prig solution for inf. 20 mcg amp 10 pcs. RUB 8314 Buy |
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Vasaprostan lyof. for prig solution for inf. 20μg amp. 10 pieces. 8633 RUB Buy |
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Vasaprostan 60 mcg lyophilisate for preparation of solution for infusion 10 pcs. RUB 13,899 Buy |
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Vasaprostan lyof. for prig solution for inf. 60mcg amp. 10 pieces. RUB 14169 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
