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Wap 20

Wap 20 contains the substance alprostadil. It belongs to the group of prostaglandins.

Indications of the wapa 20

It is used to eliminate obliterating pathologies of grade 3-4 of the chronic type (Fontaine's classification is used), not subject to revascularization (or if revascularization in such people has not produced a result).

The drug is not recommended for elimination of obliterating pathologies (chronic type) in the peripheral arteries of the 4th degree.

Release form

Release in the form of a concentrate for the manufacture of infusion in glass ampoules of 1 ml volume (type I Ph.EUR.). Inside a separate pack contains 5 or 10 ampoules of the drug.

Pharmacodynamics

The active ingredient of the drug alprostadil is a vasodilator that promotes blood circulation, performing the process of dilatation of pre-capillary sphincters with arterioles. The drug positively affects the processes of microcirculation, as well as the rheological parameters of the blood.

After infusion into / in the method, an increase in erythrocyte elasticity occurs, as well as inhibition of their aggregation in ex vivo indications. Alprostadil effectively inhibits the process of platelet activation during in vitro action. This effect extends to the properties of the change in the form of platelets, and in addition to aggregation and isolation of components located within the granules, as well as the release of thromboxane (helps aggregation processes). The drug helps to reduce the formation of arterial thrombi in in vivo tests in animals.

The use of drugs activates fibrinolysis processes, increasing its individual internal values (plasmin with plasminogen, and in addition the action of plasminogen activator inside tissues).

Pharmacokinetics

Alprostadil is an artificial analogue of natural PG: E1, which has a short half-life. When oral administration of drugs at a dose of 60 mcg, after 2 hours, the peak plasma level in a healthy person was 6 pg / ml higher than the maximum in the placebo stage (2.4 pg / ml). The half-life in the α-stage is approximately 0.2 minutes (calculated value), and for the β-stage it is about 8 minutes. As a result of this equilibrium level, the drug reaches rather soon after the onset of the infusion.

Metabolism of alprostadil is carried out in the lungs - about 80-90% at the 1st pass. The primary degradation products formed during the first pass are 15-keto-PGE 1, and besides, PGE-0 (the so-called 13,14-dihydro-PGE 1) with the 15-keto-PGE-0 element (which is 13,14 -dihydro-15-keto-PGE 1) - continue to undergo disintegration (among other things, β-oxidation and also ω-oxidation are carried out).

Decay products are excreted in the urine (by 88%), and feces (by 12%). Full excretion takes 72 hours. Of the primary decay products, only the 15-keto-PGE-0 element can be determined by in vitro exposure to pulmonary homogenates.

When receiving alprostadil in the amount of 60 μg, PGE 0 reaches 2 hours of peak plasma level in a healthy person - 11.8 pg / ml after the placebo stage (equal to 1.7 pg / ml), while the half-life is equal to approximately 2 minutes at the α-stage, and also about 33 minutes during the β-stage. The maximum value is observed after 119 minutes. The corresponding values for the 15-keto-PGE-0 element are equal to: the peak level is 151 pg / ml (with a placebo of 8 μg / ml), the α-half-life is about 2 minutes, and the β-elimination half-life is 20 minutes; peak reaches in 106 minutes.

Synthesis of alprostadil with macromolecular elements within the plasma is 93%.

Use of the wapa 20 during pregnancy

The medicine can not be administered to pregnant women, and if it is necessary to use it during lactation, it is necessary to stop breastfeeding at the time of treatment.

Women who are in reproductive age should use effective contraception during the use of medicines to avoid pregnancy.

Information on preclinical tests demonstrates that Wap 20 does not affect fertility in the case of its use in recommended dosage.

Contraindications

The main contraindications:

  • the presence of hypersensitivity against alprostadil or other elements of the drug;
  • with disorders in the heart: heart failure decompensated type (3rd and 4th stage according to the NYHA classification); inadequate therapy of cardiac arrhythmia and heart failure; having a different origin of arrhythmia (among them also one that causes the development of hemodynamic disorders); aortic / mitral stenosis / insufficiency; improperly controlled heart pathologies of the coronary type; IHD and transferred in recent time (during the last six months) myocardial infarction;
  • suspicion of the development of pulmonary edema (in chronic or acute form), made after x-rays or clinical examination, and in addition, a history of pulmonary edema or pulmonary infiltration;
  • chronic pulmonary pathologies of the obstructive type in severe degree, and in addition to this PE;
  • Persons with documented hepatic diseases (also those with symptoms of acute liver failure - increased GGT or transaminase) or severe hepatic insufficiency (this includes history);
  • disorders in the work of the kidneys (oligoanuria);
  • presence of a tendency to develop bleeding (polytrauma, and in addition bleeding / erosive ulcer pathology of the duodenum gut or stomach in acute form);
  • presence in the anamnesis for the last half a year of a stroke;
  • decreased blood pressure in severe form;
  • the presence of general contraindications regarding the procedures of infusion (among them, congestive heart failure, cerebral or pulmonary edema, and hyperhydria);
  • children and teenagers under 18 years of age.

Side effects of the wapa 20

The use of medication can cause the following side effects:

  • Disorders from the NA: basically there are paresthesias of the extremity with which the procedure was performed, as well as headaches. Occasionally, there are cerebral cramps and a sense of confusion. Possible development of psychosis or stroke and the appearance of dizziness;
  • disorders in the gastrointestinal tract: occasionally there are pathologies of the gastrointestinal tract, including vomiting with diarrhea and nausea, as well as acceleration of intestinal peristalsis (the effect of alprostadil). Abdominal pain with heartburn, as well as anorexia, may appear;
  • manifestations of the organs of the cardiovascular system: in some cases angina or tachycardia may appear and a decrease in the level of blood pressure may be observed. Occasionally, arrhythmia occurs, or heart failure, which results in acute pulmonary edema, which can cause heart failure of a general type. Blockades and myocardial infarction may occur;
  • reactions of the digestive system: occasionally the index of liver enzymes may be violated;
  • manifestations of the organs of the respiratory system: occasionally there is a pulmonary edema. The appearance of dyspnea;
  • disorders in the hematopoietic system: occasionally anemia or leukocytosis, as well as thrombocyto- or leukopenia;
  • results of laboratory studies: sometimes there is an increase in temperature or the level of transaminases. The values of CRP can also vary, but after the therapy they quickly normalize;
  • reactions of the subcutaneous layer and skin: often there are swelling, redness and hot flashes;
  • systemic disorders and manifestations on the site of infusion: often swelling and an increase in temperature with swelling in the area of administration; In addition, redness of the veins and development of paresthesias are observed. Less often, chills begin with fever and hyperhidrosis. Perhaps the emergence of phlebitis on the site of infusion, and in addition to this thrombosis in the area of introduction into the catheter. There may also be local bleeding, a feeling of malaise and a sensitivity disorder of the mucous membranes with the skin;
  • Immune disorders: sometimes allergies manifest themselves (increased sensitivity of the skin - rashes, swelling, hyperhidrosis, joint discomfort with chills, and pyrogenic reaction). Occasionally - the development of anaphylactoid or anaphylactic signs. Anaphylaxis is possible;
  • disorders in the work of muscles and bones: sometimes there are signs of disorders in the joints (among them pain sensations). A curable hyperostosis is observed in the region of long bones tubular form (when using drugs for more than 1 month);
  • others: there may be increased fatigue, anuria with vasalgia, a feeling of general weakness, kidney failure and orthostatic collapse.

Dosing and administration

You need to inject the medicine into the vein or artery, with the condition that the doctor performing the procedure has experience in the field of angiology, and he is familiar with modern ways of regularly monitoring the values of the SSS and has the equipment required for this purpose. Do not administer the solution by the bolus method intravenously.

In the treatment of / in the method of pathologies of the third degree.

There is the following scheme of intravenous treatment: dissolve the contents of 2 ampoules (equal to 40 micrograms of drug) in a solution of sodium chloride (0.9%, take 50-250 ml), and then inject the obtained substance in a period of 2 hours. This dosage is applied 2 times a day.

Alternative route: once-daily infusion for 3 hours. Enter 3 ampoules (amount of 60 μg alprostadil), which are dissolved using the same amount of the above solvent.

People with disorders in the work of the kidneys (insufficiency with KK> 1.5 mg / dL) should start IV therapy with the introduction of the 1st ampoule twice a day (twice 20 μg Wap 20 ). Each of the procedures is 2 hours. Taking into account the general clinical picture, it is allowed to increase the dosage to the above standard dose in the period of 2-3 days.

People with kidney failure, and also those who are included in the risk of heart function disorder, need to limit the daily infusion volume to 50-100 ml, and the introduction must necessarily be performed with the help of an infusion device.

Treatment of pathologies of 3rd and 4th degree by the introduction of drugs into the arteries.

Below is indicated the following scheme of the intra-arterial treatment course: dissolve within a solution of sodium chloride (0.9%) 1-ounce ampoule (20 μg of substance). In this case, the volume of the finished solution will be half of the drug ampoule (in 25 ml of this solution - 10 μg of the drug). Infusion is carried out with the help of a special device in the period of 1-2 hours. If the tolerability of the drug remains satisfactory, it is permitted to increase the dose to the 1st ampoule (or 20 μg of the active ingredient), especially if necrosis is present on the body. Often a day requires 1 infusion.

When the infusion is performed by means of an inserted catheter, taking into account the severity of the disease and the tolerability of the drug, a dosage of 0.1-0.6 ng / kg / minute (about a quarter / half of the drug ampoule) is prescribed. In this case, the duration of the infusion using the device is 12 hours.

At the end of 3 weeks of therapy, it is necessary to determine the feasibility of subsequent use of drugs. If there is no result, it is necessary to cancel the drug. The therapeutic course can last no more than 1 month.

Overdose

Manifestations of an overdose - lowering the level of blood pressure, as well as tachycardia of a reflex type due to the expansion of blood vessels. Other likely signs: hyperhidrosis, vomiting, syncopal condition of the vasovagus type, accompanied by pallor, and in addition, heart failure, nausea and myocardial ischemia. Local symptoms may develop: redness and swelling of the extremity, where the infusion is performed, and also the reaction of intolerance.

Therapy should be symptomatic. The medicine does not have a specific antidote. If, when the required dose has been lowered, the blood pressure index has decreased or severe pain has begun, it is necessary to lower the infusion or immediately stop it. In the event of a fall in blood pressure, it is first of all necessary to lay the victim on his back, while lifting his legs slightly. If the manifestations of the violation do not pass, you need to track the CAS indicators. If necessary, the appointment of sympathomimetic drugs is prescribed.

Interactions with other drugs

During the use of VAP 20, potentiation of the properties of antihypertensive drugs may occur, as well as antianginal drugs and vasodilators. The combination of these drugs with alprostadil or the use simultaneously with other vasodilating drugs requires constant monitoring of the CAS indicators (this includes monitoring blood pressure level).

Adrenaline with norepinephrine, as well as sympathomimetic drugs weaken the vasodilating effect of the drug.

Combination with antithrombotic drugs (drugs-inhibitors of platelet aggregation, anticoagulants and thrombolytic drugs) can increase the tendency to bleeding. Given the weak slowing effect of VAP 20 relative to platelet aggregation in indications in vitro, careful use should be made of it in combination with anticoagulants.

Combined use with drugs cefatetan and cefaferazone with cefamendol weakens the effect of alprostadil.

Storage conditions

Wap 20 is required to be kept in a place that is closed from light, and inaccessible to small children. Temperature conditions are within 2-8 ° C.

Shelf life

Wap 20 is allowed to be used in the period of 3 years from the date of manufacture of the medicine.

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Medical expert editor

Portnov Alexey Alexandrovich

Education: Kiev National Medical University. A.A. Bogomolets, Specialty - "General Medicine"

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Attention!

To simplify the perception of information, this instruction for use of the drug "Wap 20" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.

Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.

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