Buy Zocardis pills 7.5 pills covered. 7.5 mg, 28 pcs
  • Buy Zocardis pills 7.5 pills covered. 7.5 mg, 28 pcs

Zocardis® [Zofenopril]

Berlin-Chemie / Menarini
1440 Items
2019-09-19
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Clinical Pharmacology

ACE inhibitor, antihypertensive drug. The mechanism of action is associated with a decrease in the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone, while the congestion of systolic and diastolic BP, post- and preload on the myocardium decreases. Expands the arteries to a greater extent than the veins, while the reflex increase in heart rate is not observed. Reduces the degradation of bradykinin, increases prostaglandin synthesis.

The hypotensive effect is more pronounced with a high concentration of plasma renin than with normal or reduced concentration. A decrease in blood pressure in the therapeutic range does not affect cerebral circulation, the blood flow in the brain vessels is maintained at a sufficient level and against the background of low blood pressure. Enhances coronary and renal blood flow.

With prolonged use, the left ventricular hypertrophy of the myocardium and myocytes of the walls of resistive arteries is reduced, it prevents the progression of heart failure and slows down the development of left ventricular dilatation. Improves blood supply to ischemic myocardium. Reduces platelet aggregation. Zofenopril is a prodrug, because activity is free sulfhydryl compound (zofenoprilat), formed as a result of thioester hydrolysis.

After ingestion, the hypotensive effect develops after 1 h, reaches a maximum after 4-6 h and lasts up to 24 h. In some cases, therapy for several weeks is necessary to achieve an optimal decrease in blood pressure. In heart failure, a noticeable clinical effect is observed with prolonged treatment (6 months or more).

Pharmacokinetics

Suction and distribution

After ingestion, zofenopril calcium is rapidly and completely absorbed from the gastrointestinal tract and undergoes almost complete conversion to zofenoplat.

Cmax zofenoprilata in blood plasma is achieved 1.5 hours after taking Zocardis. Binding to plasma proteins for zofenopril is 88%.

Metabolism and excretion

Zofenopril is rapidly metabolized in the liver to form the active metabolite of zofenoprilat. T1/2 zofenoprilat makes 5.5 h, the general clearance makes 1300 ml / min. Zofenoprilat is excreted primarily by the kidneys - 69%, through the intestines - 26%.

Indications

Mild and moderate arterial hypertension.

Acute myocardial infarction with symptoms of heart failure in patients with stable hemodynamic parameters and not receiving thrombolytic therapy.

Composition

1 tablet contains:

Active substances: Zofenopril calcium 7.5 mg.

Excipients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, corn starch, colloidal silicon dioxide.

Shell composition: hypromellose, titanium dioxide, macrogol 400, macrogol 600.

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Zocardis® [Zofenopril]

Dosage and Administration

pills are taken orally, regardless of the meal (before, during or after a meal), drinking plenty of fluids.

Arterial hypertension

Patients with normal liver and kidney function

To achieve an optimal level of blood pressure, adults should begin therapy with a dose of 15 mg (2 pills of 7.5 mg or 1/2 pills of 30 mg) 1 time / day and gradually, with insufficient expression of the hypotensive effect, increase the dose 4 weeks.

The average dose is 30 mg 1 time / day (4 pills of 7.5 mg or 1 tablet of 30 mg).

The maximum daily dose is 60 mg (8 pills of 7.5 mg or 2 pills of 30 mg). Reception frequency - 1-2 times / day.

Patients with impaired water and electrolyte balance

Before the appointment of ACE inhibitors, correction of water and electrolyte metabolism and the cancellation of the therapy with diuretics for 2-3 days before the start of taking the ACE inhibitor. In this case, the initial dose of Zocardis is 15 mg / day. If the abolition of diuretics and the normalization of water and electrolyte balance is impossible, then the initial dose of Zocardis should be 7.5 mg / day.

Patients with impaired renal function or who are on hemodialysis

Correction of the dose of Zocardis is necessary. When QA> 45 ml / min, dose adjustment is not carried out, with QC <45 ml="" min="" the="" dose="" should="" be="" reduced="" to="" 1="" 2="" average="" therapeutic="" time="" day="" p="">

The initial dose for patients on dialysis is 1/4 of the dose used for patients with normal renal function.

Elderly patients

With normal kidney function, dosing regimen adjustment in the elderly is not required. Elderly patients with QA <45 ml="" min="" are="" recommended="" 1="" 2="" of="" the="" average="" therapeutic="" dose="" p="">

Patients with impaired liver function

In patients with mild-to-moderate hepatic insufficiency, the initial dose of Zokardis® is 1/2 the dose used in patients with normal liver function.

Patients with severe hepatic impairment

Zocardis® is not prescribed.

Acute myocardial infarction

Treatment with Zokardis® is started within 24 hours after the onset of the first symptoms of myocardial infarction and continues for 6 weeks, with the following regimen used:

  • The time period of the 1st and 2nd day is 7.5 mg every 12 hours (dosing regimen).
  • The time period of the 3rd and 4th day is 15 mg every 12 hours (dosing regimen).
  • The time period from the 5th day onwards is 30 mg every 12 hours (dosing regimen).

With an excessive 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 the drug.

After 6 weeks of treatment, therapy may be discontinued in patients without signs of left ventricular failure or heart failure. For the correction of left ventricular failure or heart failure, as well as hypertension, treatment can be continued for a long time.

Dosage in elderly patients with acute myocardial infarction

Zokardis® should be used with caution in patients with myocardial infarction older than 75 years.

Adverse reactions

Since the cardiovascular system: excessive blood pressure reduction, orthostatic collapse; rarely - chest pain, stenocardia, myocardial infarction (usually associated with a pronounced decrease in blood pressure), arrhythmias (atrial brady- or tachycardia, atrial fibrillation), palpitations, pulmonary embolism, pain in the heart, fainting.

From the side of the central nervous system and peripheral nervous system: dizziness, headache, weakness, insomnia, anxiety, depression, confusion, fatigue, drowsiness (2-3%); very rarely (when used in high doses) - nervousness, paresthesias.

From the senses: rarely - vestibular disorders, hearing and vision disorders, tinnitus.

From the digestive system: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), increased activity of hepatic transaminases, hyperbilirubinemia, intestinal obstruction, pancreatitis, abnormal liver function, disorders of the biliary tract, hepatitis, jaundice

On the part of the respiratory system: unproductive dry cough; very rarely - interstitial pneumonitis, bronchospasm, shortness of breath, rhinorrhea, pharyngitis.

From the hemopoietic system: in some cases, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.

From the urinary system: increased levels of creatinine and urea, renal dysfunction, proteinuria.

From the laboratory indicators: hypercreatinemia, increased urinary level, increased activity of AST, ALT, hyperbilirubinemia, hyperkalemia, hyponatremia, in some cases decrease in hematocrit and decrease in hemoglobin, increased ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases, patients with autoimmune diseases, idiopathic cases), eutropenia (agonulocytosis)

Allergic reactions: rarely, skin rash, angioedema (face, extremities, lips, tongue, glottis and / or larynx), dysphonia, erythema polymorphic, exfoliative dermatitis; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), pemphigus, pruritus, urticaria, photosensitization, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

Contraindications

Caution should be used Zokardis®: in primary hyperaldosteronism, bilateral renal artery stenosis, single kidney artery stenosis, hyperkalemia, condition after kidney transplantation, aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, connective tissue diseases, cerextra, in case of cerebral injury proteinuria more than 1 g / day), liver failure, while used with immunosuppressants, in the elderly (st Arshe 75 years), with psoriasis.

Care must be taken when prescribing the drug to patients with reduced BCC (as a result of diuretic therapy, while limiting salt intake, hemodialysis, diarrhea and vomiting), because increased risk of sudden and pronounced decrease in blood pressure after the use of an ACE inhibitor, even in the initial dose.

Drug interactions

When combined, the hypotensive effect of ACE inhibitors can be enhanced by other antihypertensive agents, diuretics, general anesthesia drugs, analgesics, antipyretics, ethanol.

With simultaneous appointment with NSAIDs may decrease the hypotensive effect of zofenopril.

With simultaneous appointment with potassium-sparing diuretics may develop hyperkalemia.

With simultaneous appointment with lithium salts, a slowdown in the elimination of lithium is noted.

When used together, immunosuppressants, allopurinol, and cytostatics increase the hematotoxicity of zofenopril.

With simultaneous appointment with hypoglycemic agents increases the risk of hypoglycemia.

Pregnancy and Lactation

Zocardi® is contraindicated for use during pregnancy and lactation (breastfeeding).

When using the drug, women of childbearing age should use reliable methods of contraception. Zofenopril calcium is excreted in breast milk.

Special instructions

A transient pronounced decrease in blood pressure is not a contraindication for the continuation of drug treatment after stabilization of blood pressure. In case of repeated pronounced decrease in blood pressure, reduce the dose or discontinue the drug.

With the development of an excessive decrease in the patient's blood pressure, the patient is transferred to a horizontal position with a low headboard; if necessary, a 0.9% solution of sodium chloride and plasma substitutes are injected.

The use of high-flow dialysis membranes increases the risk of anaphylactic reactions. Correction of the dosing regimen on dialysis-free days should be carried out depending on the level of blood pressure. Before and after treatment with ACE inhibitors, it is necessary to control blood pressure, blood parameters (hemoglobin, potassium, creatinine, urea, AST, ALT), and urine protein levels.

It should be carefully monitored for patients with severe heart failure, coronary artery disease and cerebrovascular disease, in which a sharp decrease in blood pressure can lead to myocardial infarction, stroke or impaired renal function. Sudden cancellation of treatment does not lead to the syndrome of "cancellation" (a sharp rise in blood pressure).

In patients with angioedema in the history of anamnesis there is an increased risk of its development when taking ACE inhibitors.

In patients with reduced kidney function, reduce the single dose or increase the intervals between doses of the drug. The patient should be warned about the need to be careful when performing physical exercises in hot weather (the risk of dehydration and excessive blood pressure due to lower BCC).

Before performing surgical interventions (including dental) it is necessary to warn the surgeon / anesthesiologist about the use of ACE inhibitors.

Newborns and infants who have undergone intrauterine effects of ACE inhibitors are recommended to be closely monitored for the timely detection of pronounced reduction in blood pressure, oliguria, hyperkalemia and neurological disorders, possible due to a decrease in renal and cerebral blood flow while reducing blood pressure caused by ACE inhibitors. When oliguria, it is necessary to maintain blood pressure and renal perfusion by injecting appropriate fluids and vasoconstrictor agents.

During the use of the drug is not recommended to drink alcohol, because alcohol enhances the hypotensive effect of the drug.

The simultaneous use of hypoglycemic agents increases the risk of hypoglycemia.

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

In the period of selection of a therapeutic dose, it is necessary to refrain from driving vehicles and practicing potentially hazardous activities that require increased concentration and psychomotor speed, because dizziness is possible (especially after taking the initial dose of an ACE inhibitor in patients taking diuretics).

Overdosage

Symptoms: pronounced decrease in blood pressure (up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications), convulsions, stupor.

Treatment: the patient is transferred to a horizontal position with a low head. In mild cases - gastric lavage and ingestion of saline, in more severe cases - measures aimed at stabilizing blood pressure (in / in the introduction of a 0.9% sodium chloride solution, plasma substitutes); if necessary, the introduction of angiotensin II, hemodialysis.

  • Brand name: Zocardis
  • Active ingredient: Zofenopril
  • Dosage form: pills, coated.
  • Manufacturer: Berlin-Chemie / Menarini
  • Country of Origin: Germany

Studies and clinical trials of Zofenopril (Click to expand)

  1. An unusual rearrangement of Zofenopril, a new ACE inhibitor drug: mass spectrometric and conformational studies
  2. HPLC-DAD method for the simultaneous determination of zofenopril and hydrochlorothiazide in oral pharmaceutical formulations
  3. Temperature, pH and agitation rate as dissolution test discriminators of zofenopril calcium tablets
  4. Development and validation of a liquid chromatography–tandem mass spectrometry method for the determination of zofenopril and its active metabolite zofenoprilat in human plasma
  5. Assay of zofenopril and its active metabolite zofenoprilat by liquid chromatography coupled with tandem mass spectrometry
  6. Effect of Zofenopril on regeneration of sciatic nerve crush injury in a rat model
  7. The effects of oral pretreatment with zofenopril, an angiotensin-converting enzyme inhibitor, on early reperfusion and subsequent electrophysiologic stability in the pig
  8. Antihypertensive efficacy of zofenopril plus hydrochlorothiazide fixed combination for treatment in metabolic syndrome
  9. Differences between zofenopril and ramipril, two ACE inhibitors, on cough induced by citric acid in guinea pigs: role of bradykinin and PGE2
  10. Effect of acute and chronic zofenopril administration on cardiac gene expression
  11. Serum cholesterol levels on admission and survival in patients with acute myocardial infarction treated with zofenopril: a post hoc analysis of the Survival of Myocardial Infarction Long-term Evaluation trial
  12. Cardiovascular changes in spontaneously hypertensive rats are improved by chronic treatment with zofenopril
  13. Preclinical Profile of Zofenopril: An Angiotensin Converting Enzyme Inhibitor with Peculiar Cardioprotective Properties
  14. The Role of Zofenopril in Myocardial Protection During Cardioplegia Arrest: An Isolated Rat Heart Model
  15. Comparison of zofenopril and lisinopril to study the role of the sulfhydryl-group in improvement of endothelial dysfunction with ACE-inhibitors in experimental heart failure
  16. The effects of atenolol and zofenopril on plasma atrial natriuretic peptide are due to their interactions with target organ damage of essential hypertensive patients
  17. Sites of First-Pass Bioactivation (Hydrolysis) of Orally Administered Zofenopril Calcium in Dogs
  18. Simultaneous Analysis of Zofenopril and Its Active Metabolite Zofenoprilat in Human Plasma by LC–ESI-MS Using Pre-Column Derivatization withp-Bromophenacyl Bromide
  19. Comparison Between Zofenopril and Ramipril in Combination With Acetylsalicylic Acid in Patients With Left Ventricular Systolic Dysfunction After Acute Myocardial Infarction: Results of a Randomized, Double-Blind, Parallel-Group, Multicenter, European Study (SMILE-4)
  20. LES IEC dans le post-infarctus : gros plan sur le zofénopril
  21. Hydrochlorothiazide increases plasma or tissue angiotensin-converting enzyme-inhibitor drug levels in rats with myocardial infarction: Differential effects on lisinopril and zofenopril
  22. Effects of the Early Administration of Zofenopril on Onset and Progression of Congestive Heart Failure in Patients With Anterior Wall Acute Myocardial Infarction
  23. Cardioprotective effects of zofenopril, a new angiotensin-converting enzyme inhibitor, on doxorubicin-induced cardiotoxicity in the rat
  24. Beneficial effects of ACE-inhibition with zofenopril on plaque formation and low-density lipoprotein oxidation in watanabe heritable hyperlipidemic rabbits

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