Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Preparation of prostaglandin E 1 . Improves microcirculation and peripheral circulation, has an angioprotective effect. With systemic administration causes relaxation of smooth muscle fibers, has a vasodilating effect, reduces OPSS, reduces blood pressure. At the same time there is a reflex increase in cardiac output and heart rate. It improves the rheological properties of blood, contributing to the increase in the elasticity of red blood cells and reducing platelet aggregation and neutrophil activity, increases the fibrinolytic activity of the blood.
It has an effect on metabolism, increases utilization of glucose and oxygen, suppresses the release of free radicals and lysosomal enzymes from granulocytes and macrophages, stimulates protein synthesis, has a beneficial effect on lipid metabolism (suppressing the synthesis of cholesterol and lowering the concentration of LDL), inhibits the proliferation of smooth muscle cells.
Has a stimulating effect on the smooth muscles of the intestine, bladder, uterus; suppresses the secretion of gastric juice.
When an intracavernous injection blocks? 1- adrenoreceptors in the tissues of the penis, has a relaxing effect on the smooth musculature of the cavernous bodies, contributes to increased blood flow and improved microcirculation. Expansion of the cavernous arteries and vessels of the trabecular smooth muscles of the cavernous bodies leads to a rapid increase in blood flow and dilatation of the lacunar spaces in the cavernous bodies. Venous outflow through the vessels, located under the belly, is limited, which stimulates the development of erection ("corporal veno-occlusive mechanism"). The onset of action is 5-10 minutes, duration - 1-3 hours.
PHARMACOKINETICS
With iv injection, alprostadil is rapidly metabolized. At a single passage through the lungs, it is metabolized to 60-90%. During enzyme oxidation, 3 biologically active metabolites are formed: 15-keto-PGE 1 , 15-keto-13,14-dihydro-PGE 1 and 13,14-dihydro-PGE 1 . Keto metabolites have a lower biological effect compared to alprostadil, the metabolite 13,14-dihydro-PGE 1 has a comparable action with PGE 1 . The pharmacodynamic effect is mainly due to this biologically active metabolite. T 1/2 13,14-dihydro-PGE 1 is about 1 minute. The main metabolites are excreted mainly with urine and, to a lesser extent, with feces.
With intracavernous injection, the concentration of alprostadil and its main metabolite, 15-oxo-13,14-dihydro-PgE 1, is determined only in cavernous bodies. After intracavernous injection of 20 Ојg 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 baseline 60 minutes after the injection, while the levels of alprostadil in the peripheral blood flow were slightly higher than the baseline. Alprostadil on admission to a large circle of circulation during intracavernous injection is very quickly metabolized. It is excreted in the form of metabolites.
INDICATIONS
The need for temporary maintenance of the functioning of the arterial duct until the corrective operation is performed with congenital ductus-dependent heart defects in newborns (including mitral atresia, pulmonary atresia, tricuspid atresia, tetralogy of Fallot).
Chronic obliterating diseases of arteries of III-IV stage (according to Fontaine's classification). Obliterating endarteritis with severe degree of intermittent claudication (with impossible surgical revascularization of the lower limb), obliterating atherosclerosis, diabetic angiopathy, obliterating thromboangiitis (Burger's disease), Reynaud's syndrome with trophic disorders, vasculitis, scleroderma, spasms of the calf muscles, damaging the influence of physical factors, especially the overlimit vibration.
Treatment of erectile dysfunction of neurogenic, vascular, psychogenic or mixed etiology; conducting a pharmacological test in a complex of diagnostic tests for erectile dysfunction.
DOSING MODE
Individual, depending on the indications and the dosage form used.
SIDE EFFECT
On the part of the digestive system: diarrhea, nausea, vomiting, increased activity of transaminases; rarely - hyperbilirubinemia, peritoneal symptoms.
From the cardiovascular system: arterial hypotension, tachycardia, pain in the heart; rarely - heart failure, heart rhythm disturbances, AV blockade, acute pulmonary edema.
From the central nervous system and peripheral nervous system: headache, psychosis, convulsions of the central genesis, paresthesia; rarely - retardation.
On the part of the respiratory system: rarely - tachypnea, respiratory distress syndrome.
From the hemopoietic system and the coagulating system of blood: leukocytosis, leukopenia; rarely bleeding, hypochromic anemia, thrombocytopenia.
From the urinary system: rarely - anuria, kidney failure, hematuria.
From the side of metabolism: rarely - hypoglycemia, hypercapnia.
From the musculoskeletal system: joint pain, neck muscle strain, reversible hyperostosis of tubular bones.
Allergic reactions: skin rash, itching.
Other: possible hyperthermia, redness of the skin, increased sweating, swelling of the extremity into which the infusion is performed.
With intracavernous injection , pain in the penis, prolonged erection and priapism are possible; rarely - fibrosis, swelling, heat, numbness, eruptions on the penis, balanitis, hemorrhages, itching and swelling of the injection site, bleeding from the urethra, fungal infection, phimosis, painful erection and ejaculation, pain in the testicles, swelling of the testicles, pain and tension of the scrotum, frequency of urination, urinary incontinence, pain in the buttocks, legs, abdomen, pelvic pain, lower back, flu-like syndrome, hypoesthesia, myasthenia gravis.
CONTRAINDICATIONS
Chronic heart failure, pulmonary edema, cardiac arrhythmias, myocardial infarction suffered during the last 6 months; infiltrative changes in the lungs, bronchial asthma; violations of liver function, liver disease (including in history); ulcerative lesions of the gastrointestinal tract in anamnesis; hypersensitivity to alprostadil;pregnancy, lactation.
For intracavernous administration: diseases predisposing to the occurrence of priapism (sickle-cell anemia, myeloma, leukemia); anatomical deformations of the penis (angulation, cavernous fibrosis, Peyronie's disease). Do not use in patients with an implant of the penis, as well as contraindications for sexual intercourse.
PREGNANCY AND LACTATION
Alprostadil is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: liver dysfunction, liver disease (including in history).
APPLICATION FOR CHILDREN
In newborns should be used under constant monitoring of blood pressure, with the mandatory availability of conditions for ventilation.
At present, there is no experience of intracavernous administration to patients younger than 18 years of age.
APPLICATION IN ELDERLY PATIENTS
At present, there is no experience of intracavernous administration to patients older than 75 years.
C use caution in / a and / in cases of extensive vascular lesions in diabetes mellitus (in elderly patients).
SPECIAL INSTRUCTIONS
C use caution in / a and / in acute and subacute myocardial infarction, with myocardial infarction, transferred during the last 6 months, with severe or unstable angina, decompensated chronic heart failure, with arterial hypotension, cardiovascular failure, with pulmonary edema, severe arrhythmias, bronchoobstructive syndrome (severe with signs of respiratory failure), with infiltrative changes in the lungs, liver failure (including in the history), with increased (including ulcers of the stomach or duodenum, severe cerebral vascular disease, proliferative retinopathy with a tendency to bleeding, extensive trauma), hemodialysis, type 1 diabetes mellitus, especially with extensive vascular lesions (in elderly patients age); on the background of the use of vasodilators or anticoagulants; in newborns (risk of developing bradypnoea, arterial hypotension, tachycardia, or hyperthermia).
C caution should be given intracavernously with thrombocytopenia, polycythemia, thrombophlebitis, venous thrombosis (including in case of predisposition), increased blood viscosity, balanitis, urethritis.
Do not use in patients with a tendency to addiction and / or mental or intellectual disorders.
In case of violations of the blood coagulation system or with simultaneous therapy with drugs that affect the coagulation system, during treatment with alprostadil, the blood coagulation indicators should be regularly monitored. With systemic administration, it is necessary to control the parameters of central hemodynamics, the biochemical parameters of the blood.
With prolonged continuous administration, apnea may develop, a negative effect on the wall structure of the arterial duct, with an increased risk of rupture, thinning of the muscle layer of the pulmonary artery. With a treatment duration of more than 4 weeks, reversible cortical proliferation of tubular bones is possible.
In newborns should be used under constant monitoring of blood pressure, with the mandatory availability of conditions for ventilation.
At present, there is no experience of intracavernous administration to patients younger than 18 years and older than 75 years.
Alprostadil is not intended for 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 with specific indications for its use.
DRUG INTERACTION
With the simultaneous use of alprostadil enhances the effect of antihypertensive agents and vasodilators, anticoagulants, antiaggregants.
