Vasaprostan lyophilisate for infusions 60mcg N10
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Description
The white lyophilisate is collected at the bottom of the ampoule and forms a layer about 3 mm thick. After complete dissolution of the lyophilisate in saline, a clear, colorless liquid.
Active ingredients
Release form
Pharmacological effect
Pharmacological action - vasodilator, antiaggregatory.
The preparation PGE1 improves microcirculation and peripheral circulation, has a vasoprotective effect. With systemic administration, it causes relaxation of smooth muscle fibers, has a vasodilating effect, reduces round focal disease without changing blood pressure. At the same time, there is a reflex increase in cardiac output and heart rate. It helps to improve the elasticity of red blood cells, reduces platelet aggregation and neutrophil activity, increases blood fibrinolytic activity. It has a stimulating effect on the smooth muscles of the intestine, bladder, uterus; inhibits the secretion of gastric juice.
Pharmacokinetics
PGE1 is used in combination with alpha-cyclodextrin in / in or in / a. During the preparation of the solution, the complex of the drug breaks down into its constituent parts - PGE1 and alpha cyclodextrin. With the on / in the introduction of a therapeutically significant concentration of the active substance is reached soon after the start of the drug, and Cmax in the blood plasma - within 2 hours from the start of the introduction. PGE 1 is an endogenous substance with an exceptionally short T1 / 2 — plasma concentration returns to its initial level 10 seconds after stopping the administration. The process of biotransformation of PGE 1 occurs mainly in the lungs, with the “first pass” through the lungs, 60–90% of the active substance is metabolized with the formation of the main metabolites - 15-keto –PGE1, 15-keto –PGE0 and PGE0. The main metabolic products are excreted by the kidneys - 88% and through the gastrointestinal tract - 12% within 72 hours. 93% PGE1 binds to plasma proteins. Alpha-cyclodextrin has a T1 / 2 of about 7 minutes, excreted by the kidneys in unchanged form.
Indications
Chronic obliterating diseases of arteries of III and IV stages (according to Fontaine's classification).
Contraindications
Hypersensitivity to alprostadil and other components of the drug, chronic heart failure, marked cardiac arrhythmias, exacerbation of coronary artery disease, myocardial infarction (within the next 6 months),pulmonary edema, infiltrative pulmonary disease, chronic obstructive pulmonary disease, liver dysfunction (elevated AST, ALT or GGT) and a history of liver disease, as well as diseases accompanied by an increased risk of bleeding and hemorrhage (gastric ulcer or duodenal ulcer, severe lesion cerebral vessels, proliferative retinopathy with a tendency to bleeding, extensive trauma, etc.), concomitant therapy of vasodilators and anticoagulants and, pregnancy, breastfeeding.
Precautionary measures
Vazaprostan® is used with caution in case of arterial hypotension, cardiovascular insufficiency (special attention should be paid to controlling the load with the volume of the carrier solution), in patients on hemodialysis (drug treatment should be carried out in postdialysis period), in patients with diabetes mellitus type 1, especially with extensive vascular lesions.
Vazaprostan® may affect the ability to actively participate in traffic or control mechanisms, especially at the beginning of treatment, with increasing doses and discontinuation of the drug, as well as while taking alcohol.
Use during pregnancy and lactation
Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.
Dosage and administration
In / a introduction. Dissolve the contents of 1 ampoule of Vazaprostan® 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 Vapaprostan® ampoule (corresponding to 10 mcg of alprostadil) are injected into a / a 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 the 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 when using an infusion device (corresponding to 0.25– 1.5 ampoules of Vazaprostan).
In / in infusion. Dissolve the contents of 2 ampoules of Vazaprostan® lyophilisate (corresponding to 40 mcg of alprostadil) in 50–250 ml of saline and inject the resulting solution intravenously for 2 hours 2 times a day or 3 ampoules (60 mcg of alprostadil) for 3 hours 1 time. day.
In patients with impaired renal function (renal failure with a creatinine level of more than 1.5 mg / dL), intravenous injection begins with 20 μg for 2 hours. If necessary, after 2-3 days a single dose is increased to 40–60 μg.
For patients with renal and heart failure, the maximum volume of fluid injected is 50–100 ml / day. The course of treatment is 4 weeks.
The duration of treatment is an average of 14 days, with a positive effect, drug treatment can be continued for 7–14 days. In the absence of a positive effect within 2 weeks from the start of treatment, further use of the drug should be discontinued.
Preparation of the solution. It is necessary to prepare the solution immediately before performing the infusion. The lyophilisate is dissolved immediately after the addition of saline. At the beginning, the solution may turn milky. This effect is created by air bubbles and does not matter. After a short time, the solution becomes clear. Do not use the solution prepared more than 12 hours ago.
Side effects
From the nervous system: headache, convulsive syndrome, dizziness, increased fatigue, feeling unwell, impaired sensitivity of the skin and mucous membranes.
Since the cardiovascular system: decrease in blood pressure, chest pain, cardiac arrhythmias, AV blockade.
From the digestive system: feeling of discomfort in the epigastric region, dyspeptic phenomena - diarrhea, nausea, vomiting.
From the musculoskeletal system: hyperostosis of long tubular bones (with treatment for more than 4 weeks).
Local reactions: pain, swelling, erythema, impaired sensitivity, phlebitis (proximal to the place of injection).
Laboratory values: leukocytosis, leukopenia, an increase in the C-reactive protein titer, an increase in the level of transaminases.
Other: increased sweating, hyperthermia, swelling of the limb, into which the vein is infused.
Rarely: pain in the joints, confusion, convulsions of central origin, fever, chills, bradypnea, arthralgia, psychosis, renal failure, anuria. Several cases of pulmonary edema and acute left ventricular failure have been reported.
Extremely rare (up to 1% of cases): shock, acute heart failure, hyperbilirubinemia, bleeding, drowsiness, bradypnea, decreased respiratory function, tachypnea, anuria, impaired renal function, hypoglycemia, ventricular fibrillation, AV block II degree, supraventricular arrhythmia, tension neck muscles, irritability, hypothermia, hypercapnia, skin hyperemia, hematuria, peritoneal symptoms, tachyphylaxis, hyperkalemia, thrombocytopenia, anemia.
Allergic reactions: skin rash, itching.
The side effects associated with the use of the drug or with the catheterization procedure itself disappear after dose reduction or cessation of the infusion.
Overdose
Symptoms: decrease in blood pressure, increased heart rate. Vasovagal reactions may develop with pale skin, increased sweating, nausea and vomiting, which may be accompanied by myocardial ischemia and symptoms of heart failure, as well as pain, swelling and redness of the tissue at the site of infusion.
Treatment: it is necessary to reduce the dose of the drug or stop the infusion. With a marked decrease in the patient in a prone position, it is necessary to raise the legs. Sympathomimetics should be used when symptoms persist.
Interaction with other drugs
Vazaprostan® can enhance the effect of antihypertensive drugs, vasodilators and antianginal drugs. The simultaneous use of Vazaprostan® in patients taking drugs that prevent blood clotting (anticoagulants, platelet aggregation inhibitors) may increase the likelihood of bleeding. In combination with cefamundol, cefoperazone, cefotetan and thrombolytic agents - increases the risk of bleeding. Sympathomimetics - adrenaline, norepinephrine, - reduce the vasodilating effect.
It must be borne in mind that drug interactions are possible even if the above preparations were used shortly before Vapaprostan® therapy was started.
special instructions
Alprostadil can be used only by doctors who have experience in angiology, are familiar with modern methods of continuous monitoring of the cardiovascular system and have the appropriate equipment for this.
During the period of treatment, control of blood pressure, heart rate, biochemical parameters of blood, blood coagulation system is necessary (for violations of the blood coagulation system or for simultaneous therapy with drugs that affect the coagulation system).
Patients with coronary artery disease, as well as patients with peripheral edema and renal dysfunction (serum creatinine> 1.5 mg / dL) should be monitored in the hospital during treatment with Vazaprostan® for 1 day after discontinuation of its use.
In order to avoid the onset of symptoms of hyperhydration in patients with renal insufficiency, the volume of injected fluid should not exceed 50–100 ml / day. Be sure to dynamically monitor the patient's condition: control of blood pressure and heart rate, if necessary - control of body weight, fluid balance, measurement of central venous pressure or an echocardiographic study.
Phlebitis (proximal to the injection site), as a rule, is not a reason to stop therapy, signs of inflammation disappear several hours after the cessation of the infusion or changes in the injection site, specific treatment in such cases is not required. Catheterization of the central vein can reduce the incidence of this side effect of the drug.
When the ampoule is damaged, the lyophilisate becomes wet and sticky, and is greatly reduced in volume. In this case, the drug can not be used.
Storage conditions
At temperatures not above 25 ° C.
Keep out of the reach of children.