primobolan

This reduces the total peripheral vascular resistance, systolic and diastolic blood pressure (BP), fasting -. And preload on the myocardium
Extends the artery to a greater extent than the veins, with the reflex increase of heart rate frequency is not marked. Reduces degradation of bradykinin, prostaglandin synthesis increases.
Hypotensive effect is more pronounced at high plasma renin concentration than under normal or reduced concentrations. Lowering blood pressure in the therapeutic primobolan range has no effect on cerebral blood flow, cerebral blood flow in the vessels is maintained at a sufficient level and on the background of decreased blood pressure. Enhances coronary and renal blood flow.
With prolonged use reduces hypertrophy of the left ventricle myocytes and resistive walls of arteries, preventing the progression of heart failure and slowing the development of left ventricular dilatation. It improves blood flow to ischemic myocardium. Reduces platelet aggregation.
Calcium Zofenopril is a prodrug as an active inhibitor is the Link-free sulfhydryl zofenoprilat- thioether which primobolan result from hydrolysis.
Onset of the antihypertensive effect vnutr- reception time is 1 hour, reaching a maximum after 4-6 hours and lasts up to 24 hrs. some patients to achieve optimal blood pressure therapy is required for several weeks. In heart failure, a significant clinical benefit observed with long-term treatment – 6 months or more.

Pharmacokinetics
calcium Zofenopril is rapidly and completely absorbed from the gastrointestinal tract after oral administration and undergoes nearly complete conversion to zofenoprilat, whose maximum concentration is achieved in the blood at 1.5 hours after receiving the oral dose Zokardisa ®
Approximately 88% of zofenopril calcium is bound to plasma proteins. Zofenopril is rapidly metabolized in the liver to the active metabolite zofenoprilata.
The half-life is 5.5 hours zofenoprilata, and its total body clearance is 1300 ml / min following oral zofenopril calcium. Zofenoprilat Displayed mostly kidneys – 69% -26% through the intestines.

Indications for use:

 

  • Hypertension mild to moderate moderate.
  • Acute myocardial infarction with signs or symptoms of heart failure in patients with stable hemodynamics and not receiving thrombolytic therapy.

    Contraindications:

    Hypersensitivity to zofenopril and other ACE inhibitors, a history of angioedema associated with treatment with ACE inhibitors, porphyria, age 18 years (effectiveness and safety have not installed), severe hepatic impairment.
    Caution should be used Zokardis ® 30 with primary hyperaldosteronism, bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, hyperkalemia, condition after kidney transplantation; aortic stenosis, mitral stenosis (with impaired hemodynamics), idiopathic hypertrophic subaortic stenosis, connective tissue diseases, cerebrovascular diseases, diabetes, renal disease (proteinuria greater than 1 g / day), liver failure, patients on a diet with restriction of salt or under on hemodialysis, at simultaneous reception with immunosuppressants and saluretikami in the elderly (over 75 years), psoriasis.
    caution should be exercised when administered to patients with reduced volume of circulating blood (as a result of diuretic therapy, while limiting intake of salt, hemodialysis, diarrhea and vomiting) – are at increased risk of sudden and pronounced reduction in blood pressure after the application of even the initial dose of the ACE inhibitor.

    Pregnancy and breast-feeding

    The drug Zokardis ® 30 should not be used during pregnancy and should not be used in women of childbearing age in the absence of effective contraception.Because zofenopril calcium is released in breast milk, the drug should not be used to nursing mothers.

    Dosage and administration:

    Zokardis ® 30 appointed interior regardless of meal times (before, during or after a meal), drinking plenty of fluids. Hypertension Patients with normal renal and hepatic function to achieve optimal blood pressure treatment should start with the 1/2 tablet formulation Zokardis ® 30 , 1 time a day, and gradually, with the lack of severity of the hypotensive effect, increase the dose at intervals of 4 weeks.Typically, the effective dose is 1 tablet of the drug Zokardis ® 30, 1 time per day. The maximum daily dose is 2 tablets of the drug Zokardis ® 30 per day taken once or divided into two doses (1 tablet).Patients with impaired water – salt balance Initial ACE inhibitor therapy requires adjusting salt and / or water deficit termination ongoing diuretic therapy for 2-3 days prior to initiation of an ACE inhibitor and begins with a dose of 1/2 tablet formulation Zokardis ® January 30 times per day. If this is not possible, you should start treatment with 1/4 tablet Zokardis ® 30 per day. Patients with impaired renal function or are on hemodialysis in patients with impaired renal function (creatinine clearance (CC) more than 45 ml / min) no dose reduction is required . Patients with moderate to severe renal impairment (creatinine clearance less than 45 ml / min) should be given a therapeutic dose of 1 1/2 times a day. The starting dose for patients on hemodialysis, is 1/4 of the dose used for patients with normal renal function. dosage in elderly patients in elderly patients with normal CK does not require dose adjustment. In elderly patients with CC less than 45 ml / min is recommended to take half the daily dose.Dosage in hepatic dysfunction in patients with mild to moderate dysfunction of the liver initial dose of the drug Zokardis ® 30 is half the dose used for patients with normal liver function . In patients with severe liver dysfunction Zokardis ® 30 should not be used.

     

    Acute myocardial infarction (as part of combination therapy)
    Treatment should be started within 24 hours after the first symptoms of myocardial infarction and continued for 6 weeks.

    In case of abnormal decrease in blood pressure at the beginning of treatment or during the first 3 days after myocardial infarction, the initial dose does not increase or cancel.
    To correct for left ventricular failure or congestive heart failure, and hypertension treatment can be continued for a long time.
    After 6 weeks of therapy may be discontinued in patients without signs of left ventricular failure or congestive heart failure. Dosage in elderly patients Zokardis ® 30 should be used with caution in myocardial infarction patients who are older than 75 years.

    Side effect:

    Since the cardiovascular system: an excessive fall in blood pressure, orthostatic collapse, rarely – chest pain angina, myocardial infarction (usually associated with a marked reduction of blood pressure), arrhythmia (atrial or bradi- tachycardia, atrial fibrillation), palpitations, thromboembolism of pulmonary artery branches , pain in the heart, faint. On the part of the central nervous system: dizziness, headache, fatigue, insomnia, anxiety, depression, confusion, fatigue, somnolence (2 – 3%), is very rare in the application of high doses of -nervoznost, depression, paresthesia. From the sensory organs: rarely disorders of the vestibular apparatus, hearing and visual impairment, tinnitus. on the part of the digestive tract: dry mouth, anorexia, dyspepsia (nausea, diarrhea or constipation, vomiting, abdominal pain ), very rare: ileus, pancreatitis, liver dysfunction and biliary excretion, hepatitis, jaundice. The respiratory system: nonproductive cough, very rare: interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, sore throat.Allergic reactions: rare: skin rash , angioedema face, extremities, lips, tongue, glottis and / or larynx, hoarseness, erythema multiforme, exfoliative dermatitis, very rare: Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, pruritus, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis. From the laboratory parameters: giperkreatinemiya, increased urea, increased activity of “liver” transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia. There have been, in some cases, decrease in hematocrit and hemoglobin, increased erythrocyte sedimentation rate, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia. From the urinary system: renal dysfunction, proteinuria.

     

    Overdose:

    Symptoms: marked reduction of blood pressure until the development of collapse, myocardial infarction, acute stroke or thromboembolic complications, convulsions, stupor. Treatment: the patient is transferred to a horizontal position with a low headboard. In mild cases shows gastric lavage and ingestion of saline, in more severe cases – measures aimed at stabilizing the blood pressure: intravenous infusion of 0.9% sodium chloride solution, plasma substitutes, at necessity administration of angiotensin II of, hemodialysis.

    Interaction with other drugs

    The antihypertensive effect may be enhanced when taken with other antihypertensive agents, diuretics, general anesthetics, analgesics and antipyretics, ethanol.
    When concomitant administration of zofenopril with nonsteroidal anti-inflammatory drugs may reduce the hypotensive effect of zofenopril; kalisberegatmi diuretikami- hyperkalemia; with lithium salts -. slowdown lithium excretion
    immunosuppressants, allopurinol, cytostatics reinforce haematotoxicity.
    Hypoglycemic agents – increase the risk of hypoglycemia.

    special instructions

    Transient marked reduction of blood pressure is not a contraindication for continuation of treatment after stabilization of blood pressure (BP). In the case of re-pronounced reduction in blood pressure, reduce the dose or stop the drug.
    With the development of excessive blood pressure lowering the patient is transferred to a horizontal position with a low headboard, if necessary, introduce 0.9% chloride and plasma substituting drugs sodium solution.
    The use of vysokoprotochnyh dialysis membranes increases the risk of an anaphylactic reaction. Correction of the dosing regimen on the days free from dialysis should be performed depending on the level of blood pressure. Before and after treatment with ACE inhibitors is necessary to monitor blood pressure, blood parameters (hemoglobin, potassium, creatinine, urea), the activity of “liver” enzymes), protein in the urine.
    It is necessary to carefully monitor the bolnmi with severe heart failure, coronary heart disease and diseases of the brain vessels in which a sharp decrease in blood pressure can lead to heart attack, stroke, or renal dysfunction. The sudden cancellation of treatment does not lead to the syndrome of “lifting” (a sharp rise in blood pressure).
    In patients with an indication for the development of angioedema in history, there is an increased risk of developing cancer while taking ACE inhibitors.
    For newborns and babies who were in utero effects of ACE inhibitors, should be closely monitored for timely detection of significant decrease in blood pressure, oliguria, hyperkalemia, and neurological disorders, possible due to the decrease in renal and cerebral blood flow while reducing blood pressure, called ACE inhibitors. If oliguria need to maintain blood pressure and renal perfusion through the introduction of appropriate fluids and vasoconstrictor.
    In patients with impaired renal function should be to reduce the single dose or increase the interval between doses of the drug.
    During the selection of a therapeutic dose should refrain from driving motor vehicles and activities potentially hazardous activities, require high concentration and speed of psychomotor reactions, becausedizziness, especially after the initial dose of ACE inhibitor in patients taking diuretics.
    Use caution when exercising in hot weather (risk of development of dehydration and excessive reduction of blood pressure due to a decrease in blood volume). Before surgery (including dental) must notify the surgeon / anesthetist on the use of ACE inhibitors.
    During treatment is not recommended to drink alcoholic beverages, as Alcohol enhances the hypotensive effect of the drug.
    The simultaneous use of hypoglycemic agents, increases the risk of hypoglycemia.

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