Vasaprostan lyophilisate for the preparation of an infusion solution of 20 μg ampoules 10 pcs.
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Active ingredients
Alprostadil
Release form
Powder
Composition
Active ingredient: Alprostadil (Alprostadil) Active ingredient concentration (mg): 20 mcg
Pharmacological effect
The drug is prostaglandin E1. It improves microcirculation and peripheral blood circulation, has an angioprotective effect. With systemic administration, it causes relaxation of smooth muscle fibers, has a vasodilating effect, decreases round congestion, lowers blood pressure. At the same time, there is a reflex increase in cardiac output and heart rate. Improves the rheological properties of blood, enhancing the elasticity of erythrocytes and reducing platelet aggregation and neutrophil activity, increases blood fibrinolytic activity. It has an effect on metabolism, increases glucose utilization and oxygen, inhibits the release of free radicals and lysosomal enzymes from granulocytes and macrophages, stimulates the synthesis of proteins, and gene synthesis Favorable effect on lipid metabolism (suppressing cholesterol synthesis and lowering LDL concentration) inhibits proliferation of smooth chnyh cells. It has a stimulating effect on the smooth muscles of the intestine, bladder, uterus; inhibits the secretion of gastric juice. When administered intracavernously, it blocks α1-adrenoreceptors in the tissues of the penis, has a relaxing effect on the smooth muscles of the cavernous bodies, and increases blood flow and improves microcirculation. The expansion of the cavernous arteries and vessels of the trabecular smooth muscle of the cavernous bodies leads to a rapid increase in blood flow and dilatation of lacunary spaces in the cavernous bodies. Venous outflow through the vessels located under the albuginea is limited, which stimulates the development of erection (corporal veno-exclusion mechanism). Onset of action - 5-10 minutes, duration - 1-3 hours.
Pharmacokinetics
With a / in the introduction of alprostadil rapidly metabolized. With a single passage through the lungs is metabolized to 60-90%. During enzymatic oxidation, 3 biologically active metabolites are formed: 15-keto-PGE1, 15-keto-13,14-dihydro-PGE1 and 13,14-dihydro-PGE1. Keto-metabolites have a lower biological effect compared to alprostadil; the 13,14-dihydro-PGE1 metabolite has an effect comparable to PGE1.The pharmacodynamic effect is mainly due to this biologically active metabolite. T1 / 2 13,14-dihydro-PGE1 is about 1 min. The main metabolites are excreted mainly in the urine and to a lesser extent in the feces. When administered intracavernously, the concentration of alprostadil and its main metabolite, 15-oxo-13,14-dihydro-PgE1, is determined only in the corpus cavernosum. After intracavernous administration of 20 mcg of alprostadil, the content of the main metabolite in the peripheral blood flow increased and reached a maximum 30 minutes after the injection, and then returned to the initial level 60 minutes after the injection, while the alprostadil levels in the peripheral blood flow were slightly higher than the initial levels. Alprostadil is very rapidly metabolized when it enters the systemic circulation during intracavernous administration. It is displayed in the form of metabolites.
Indications
The need to temporarily maintain the functioning of the arterial duct until a corrective operation is performed for congenital duct-dependent heart defects in newborns (including with mitral atresia, atresia of the pulmonary artery, tricuspid atresia, Fallot tetrade). Chronic arterial obliterans of stage III-IV Fontaine's classification). Obliterating endarteritis with severe intermittent claudication (with impossible surgical revascularization of ape vibrations. Treatment of erectile dysfunction of a neurogenic, vascular, psychogenic or mixed etiology; carrying out pharmacological tests in a complex of diagnostic tests for erectile dysfunction.
Contraindications
Chronic heart failure, pulmonary edema, cardiac arrhythmias, myocardial infarction suffered during the last 6 months; infiltrative changes in the lungs, bronchial asthma; abnormal liver function, liver disease (including a history); ulcerative lesions of the gastrointestinal tract in history; hypersensitivity to alprostadil; pregnancy, lactation. For intracavernous administration: diseases predisposing to the occurrence of priapism (sickle cell anemia, myeloma, leukemia); anatomical deformities of the penis (angulation, cavernous fibrosis, Peyronie's disease).Do not use in patients with implants of the penis, as well as in contraindications for sexual intercourse.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Alprostadil is contraindicated during pregnancy and lactation (breastfeeding).
Dosage and administration
In / a introduction. Dissolve the contents of 1 ampoule of Vasaprostan lyophilisate (corresponding to 20 mcg of alprostadil) in 50 ml of physiological saline. In the absence of other prescriptions, half of the contents of the ampoule of Vasaprostan (corresponding to 10 mcg of alprostadil) are injected within 60–120 min when using an infusion device. If necessary, especially in the presence of necrosis, under strict control of tolerance, it is possible to increase the dose to 20 μg of alprostadil (the contents of 1 ampoule). This dosage is usually used for a single daily infusion. If intravenous infusion is performed through the inserted catheter, depending on tolerance and severity of the disease, a dose of 0.1–0.6 ng / kg / min is recommended with the introduction of the drug for 12 hours while using devices for infusion (corresponds to 0.25–1.5 ampoules of Vazaprostan).
Side effects
On the part of the digestive system: diarrhea, nausea, vomiting, increased transaminase activity; rarely - hyperbilirubinemia, peritoneal symptoms. From the cardiovascular system: arterial hypotension, tachycardia, pain in the region of the heart; rarely - heart failure, heart rhythm disturbances, AV-blockade, acute pulmonary edema. On the side of the central nervous system and peripheral nervous system: headache, psychosis, convulsions of central origin, paresthesia; rarely - lethargy. From the respiratory system: rarely - tachypnea, respiratory distress syndrome. From the side of the hemopoietic system and the blood coagulation system: leukocytosis, leukopenia; rarely - bleeding, hypochromic anemia, thrombocytopenia. From the urinary system: rarely - anuria, renal failure, hematuria. From the metabolic side: rarely - hypoglycemia, hypercapnia. From the musculoskeletal system: pain in the joints, neck muscle tension, reversible hyperostosis of tubular bones. Allergic reactions: skin rash, itching. Other: possible hyperthermia, redness of the skin, increased sweating, swelling of the limb,in which infusion is carried out. In case of intracavernous administration, pain in the penis, prolonged erection and priapism are possible; rarely - fibrosis, swelling, feeling of heat, numbness, rash on the penis, balanitis, hemorrhages, itching and swelling of the injection site, bleeding from the urethra, fungal infection, phimosis, painful erection and impaired ejaculation, pain in the testicles, testicular swelling, pain and tension of the scrotum, increased urination, urinary incontinence, pain in the buttocks, legs, abdomen, pain in the pelvic region, lower back, flu-like syndrome, hypesthesia, myasthenia gravis.
Overdose
Overdose of the drug is not described.
Interaction with other drugs
With the simultaneous use of alprostadil enhances the action of antihypertensive agents and vasodilators, anticoagulants, antiplatelet agents.
special instructions
C caution is used in / and and / in acute and subacute myocardial infarction, in myocardial infarction, postponed during the last 6 months, in severe or unstable form of angina, decompensated chronic heart failure, in case of arterial hypotension, cardiovascular failure, edema of the lungs, severe arrhythmias, broncho-obstructive syndrome (severe with signs of respiratory failure), with infiltrative changes in the lungs, liver failure (including anamnesis), with increased the lawsuit of bleeding (including with gastric ulcer or duodenal ulcer, severe damage to the brain vessels, proliferative retinopathy with a tendency to bleeding, extensive injury), hemodialysis, type 1 diabetes mellitus, especially with extensive lesions of the vessels (in elderly patients age); against the background of the use of vasodilators or anticoagulants; in newborns (risk of developing bradypnea, arterial hypotension, tachycardia, or hyperthermia). To be cautious to drive intracavernous for thrombocytopenia, polycythemia, thrombophlebitis, venous thrombosis (including in case of predisposition), increased viscosity of the blood, balance, venous thrombosis, including increased blood viscosity, balancing viscosity, increased viscosity, balanitis in patients with a tendency to drug addiction and / or mental or intellectual disorders. In cases of coagulation disorders or with simultaneous therapy with drugs that affect the coagulation system, during the treatment of alprostadi scrap should be regularly monitored for blood coagulation.With systemic administration, it is necessary to control the parameters of central hemodynamics and blood biochemical parameters. With prolonged continuous administration, apnea may develop, a negative effect on the structure of the arterial duct wall with an increased risk of rupture, and a thinning of the muscle layer of the pulmonary artery. With a duration of treatment of more than 4 weeks, reversible cortical proliferation of the tubular bones is possible. In newborns, it should be used under the constant control of blood pressure, with mandatory conditions for IVL. simultaneous use with other drugs for the treatment of erectile dysfunction. It is necessary to strictly observe the compliance of the used dosage form of alprostadil con specific indications for its use.