Comparing Perindopril and Prestarium | Determining the best

Updated: 04/23/2021 15:13:41

Expert: Abramova Tsilya

With age, the risk of diseases of the cardiovascular system increases significantly; prerequisites for hypertension (high blood pressure) appear even in young people. To prevent this and maintain the condition within normal limits, antihypertensive drugs are used. Our team has analyzed two popular drugs in this group and is ready to conclude which drug is better - Perindopril or Prestarium.

Prestarium - features

The drug Prestarium is an antihypertensive drug. The main active ingredient is perindopril. This substance has a vasodilating effect, acting as a catalyst for a number of chemical processes in the body.

The product is available in tablet form. You can get it with a doctor's prescription. It has strict indications and contraindications, which excludes self-medication. Before prescribing the medicine, the doctor prescribes a series of diagnostic procedures that allow you to determine the most optimal treatment tactics.

Reference!

There is also a drug Bi-Prestarium, which already contains 2 components - perindopril and amlodipine.

Pharmacological properties of the drug Bi-prestarium

Perindopril is an ACE inhibitor that converts angiotensin I into the vasoconstrictor angiotensin II, and also causes the breakdown of the vasodilator bradykinin. ACE inhibition leads to a decrease in the concentration of angiotensin II in the blood plasma, an increase in the activity of renin in the blood plasma and a decrease in the secretion of aldosterone. Also, ACE inhibition leads to an increase in bradykinin levels, the activity of the circulating and local kalikreinin system, as well as activation of the prostaglandin system. This mechanism of action determines a decrease in blood pressure. The action of perindopril is due to its active metabolite - perindoprilat. Other metabolites are inactive. Hypertension (arterial hypertension) Perindopril effectively reduces systolic and diastolic blood pressure in hypertension (arterial hypertension) of any severity: mild, moderate and severe. Perindopril reduces peripheral vascular resistance, which leads to a decrease in blood pressure. As a result, peripheral blood flow increases, but heart rate does not change. Renal blood flow increases, but the glomerular filtration rate does not change. The maximum antihypertensive effect develops 4–6 hours after taking a single dose and persists for at least 24 hours: the T/R ratio (the ratio of the residual effect to the maximum) of perindopril is 87–100%. Blood pressure decreases quickly. In patients who responded to treatment, blood pressure normalizes within a month and persists for a long time without the occurrence of tachyphylaxis. When you stop taking perindopril, there is no withdrawal effect. Perindopril reduces left ventricular hypertrophy. Perindopril has vasodilatory properties, improves the elasticity of large arteries and reduces the wall thickness to lumen ratio of small vessels. Prevention of cardiovascular complications in patients with documented stable coronary artery disease. The 4-year EUROPA study (European Trial on the Reduction of Cardiac Events with Perindopril in Stable Coronary Artery Disease) with the participation of more than 12 thousand patients with coronary artery disease proved that treatment with perindopril significantly reduces probability:

• development of fatal and non-fatal myocardial infarction by 24%;
• development of heart failure, which requires hospitalization, by 39%.

Amlodipine Amlodipine is a calcium ion antagonist (slow calcium channel blocker), which blocks the transmembrane flow of calcium ions to myocardial and vascular smooth muscle cells. The mechanism of the antihypertensive effect of amlodipine is due to a direct relaxing effect on vascular smooth muscle. The antianginal effect of amlodipine is achieved by two mechanisms:

• expansion of peripheral arterioles, and, as a result, a decrease in total peripheral resistance (afterload). Since heart rate does not change, reducing the load on the heart reduces myocardial energy consumption and its oxygen demand;
• expansion of the main coronary arteries and arterioles in both unchanged and ischemic areas of the myocardium. This dilation increases the supply of oxygen to the myocardium in patients with vasospastic angina (Prinzmetal's angina or variant angina).

In patients with hypertension (arterial hypertension), taking amlodipine once a day provides a clinically significant decrease in blood pressure over 24 hours. Due to the slow onset of action of amlodipine, a sharp decrease in blood pressure was not observed. In patients with angina pectoris, amlodipine prolongs the total time of physical activity, the time before the onset of an angina attack and increases the time before the onset of depression of the S-T by 1 mm during exercise, and also reduces the frequency of angina attacks and reduces the need for nitroglycerin. Amlodipine does not cause undesirable metabolic effects or changes in plasma lipid levels, so it can be used in patients with asthma, diabetes mellitus and gout. Properties common to perindopril and amlodipine The ASCOT-BLPA study (Anglo-Scandinavian Cardiac outcomes Trial - Blood Pressure Lowering Arm) involving 19,257 patients with hypertension (arterial hypertension) and cardiovascular risk factors proved the advantages of long-term therapy with amlodipine and perindopril compared with therapy with atenolol and a diuretic to reduce the incidence of cardiovascular complications. According to the results of the study, patients in the group that received amlodipine + perindopril had a significantly reduced risk of cardiovascular complications, namely, a reduced risk of:

• coronary complications and interventions - by 16%;
• overall mortality - by 11%;
• cardiovascular mortality - by 24%;
• fatal and non-fatal stroke - by 23%;
• non-fatal myocardial infarction (except silent) and fatal complications of coronary artery disease - by 13%.

The rate and degree of absorption of perindopril and amlodipine, both as single drugs and as part of the drug Bi-Prestarium, do not differ significantly. Perindopril After oral administration, perindopril is rapidly absorbed, the maximum concentration in the blood plasma is reached within 1 hour. The half-life of perindopril in the blood plasma is 1 hour. Perindopril is a prodrug. 27% of the total amount of perindopril taken is determined in the blood in the form of an active metabolite - perindoprilate. In addition to the active metabolite - perindoprilate, the drug forms 5 inactive metabolites. The maximum concentration of perindoprilate in the blood plasma is achieved 3–4 hours after administration. There is a linear relationship between the dose of perindopril and its concentration in the blood plasma. Eating food slightly slows down the conversion of perindopril to perindoprilat, so perindopril should be taken before meals. The volume of distribution of unbound perindoprilate is 0.2 l/kg. The binding of perindoprilate to plasma proteins is 20%, mainly with ACE, this indicator is dose-dependent. Perindoprilat is excreted in the urine. The stage of equilibrium concentration in blood plasma occurs 4 days after the start of treatment. The kinetics of perindopril changes in patients with liver cirrhosis. The hepatic clearance of perindopril is reduced by half. However, the amount of perindoprilate formed does not decrease. Therefore, such patients do not need to adjust the dose. Dialysis clearance of perindoprilate is 70 ml/min. Amlodipine After oral administration in therapeutic doses, amlodipine is well absorbed and reaches maximum concentration in the blood 6-12 hours after administration. Absolute bioavailability is 64–80%. Volume of distribution - 21 l/kg. Food intake does not affect the bioavailability of amlodipine. in vitro study showed that 97.5% of circulating amlodipine is bound to plasma proteins. The half-life from blood plasma is 35–50 hours, which allows the drug to be administered once a day. Amlodipine is metabolized in the liver to form inactive metabolites, 10% of the drug is excreted in the urine unchanged and 60% in the form of metabolites.

Perindopril - features

Perindopril tablets contain the substance of the same name. Auxiliary components are magnesium stearate, cellulose, lactose, primellose. The medicine belongs to ACE inhibitors.

In addition to the main effect, lowering blood pressure, the drug has a positive effect on the condition of arterial vessels. When used systematically, it normalizes the functioning of the heart as a whole.

Perindopril can be prescribed for chronic heart failure to reduce the severity of the disease. According to the bicycle ergometer test, the product increases endurance, that is, tolerance to physical activity.

Overdose of the drug Bi-prestarium

No cases have been reported. Overdose of amlodipine can lead to excessive peripheral vasodilation and, as a result, significant and possibly prolonged systemic hypotension. Amlodipine is not excreted during hemodialysis. Information on perindopril is limited. An overdose of ACE inhibitors may cause arterial hypotension, circulatory shock, electrolyte imbalance, renal failure, hyperventilation, tachycardia, palpitations, bradycardia, dizziness, anxiety, cough, etc. Perindopril can be removed from the systemic circulation using hemodialysis.

Indications for use

The main indication for the use of antihypertensive drugs Perindopril and Prestarium is high blood pressure. Moreover, each drug has several positive effects, which contribute to their use in a number of diseases of the cardiovascular system.

For what diseases and conditions is Prestarium prescribed:

1. arterial hypertension;
2. prevention of complications in coronary heart disease;
3. prevention of repeated ischemia in cerebrovascular disorders;
4. stroke prevention;
5. heart failure.

Regular use of the drug helps delay the progression of the disease in heart failure. Treatment improves survival and reduces hospitalizations.

Perindopril has the following indications:

1. arterial hypertension;
2. chronic heart failure;
3. prevention of stroke recurrence and micro-stroke;
4. reducing the risk of complications in persistent ischemic disease.

Patients who have suffered a stroke can use this antihypertensive medication in the comprehensive prevention of complications. In this case, it is combined with indapamide.

Interactions of the drug Bi-prestarium

All warnings associated with each of the components of the drug apply to the drug Bi-Prestarium. For perindopril, simultaneous use with:

• potassium-sparing diuretics, potassium supplements, or potassium salt substitutes, as these may significantly increase serum potassium levels. Their simultaneous use with Bi-Prestarium is not recommended. If concomitant use is indicated due to the presence of documented hypokalemia, they should be used with caution. It is necessary to monitor blood plasma potassium levels;
• lithium Concomitant use of lithium and ACE inhibitors is not recommended due to the possible occurrence of a reverse increase in the concentration of lithium in the blood serum and, accordingly, an increase in its toxicity (severe neurotoxicity). However, if this is truly necessary, serum lithium concentrations should be carefully monitored;
• estramustine - increased risk of angioedema.

Drugs that require monitoring when co-administered: NSAIDs, including acetylsalicylic acid at a dose of ≥3 g/day, may increase the risk of renal impairment, including acute renal failure, and increased serum potassium levels, especially in patients with existing impairment kidney function. Prescribe with caution, especially for elderly patients. Periodic monitoring of renal function is necessary. Antidiabetic agents (insulin, hypoglycemic sulfonamides): when used simultaneously with ACE inhibitors, the hypoglycemic effect may be enhanced (possibly due to increased glucose tolerance). Diuretics: to reduce the risk of arterial hypotension, it is recommended to stop taking diuretics and restore water and electrolyte balance before starting treatment with ACE inhibitors. Sympathomimetics may reduce the antihypertensive effects of ACE inhibitors. Gold : with the simultaneous use of ACE inhibitors, including perindopril, and injectable gold preparations (sodium aurothiomalate), reactions similar to those with the use of nitrates (facial redness, hot flushes, nausea, vomiting and hypotension) may rarely occur. For amlodipine, simultaneous administration of: Dantrolene (infusion): simultaneous administration of dantrolene and calcium antagonists is not recommended due to the risk of ventricular fibrillation. Drugs for which simultaneous use requires caution Inducers of CYP 3A4 (rifampicin, hypericum perforatum, anticonvulsants such as carbamazepine, phenobarbital, fosphenytoin, phenytoin, primidone): simultaneous use may lead to a decrease in the concentration of amlodipine in the blood plasma. Amlodipine should be prescribed in combination with CYP3A4 inducers with caution; if necessary, the dose of amlodipine can be adjusted. CYP3A4 inhibitors (itraconazole, ketoconazole): simultaneous use may increase the plasma concentration of amlodipine and the incidence of its side effects. Amlodipine should be prescribed in combination with these drugs with caution; if necessary, the dosage of amlodipine can be changed. β-receptor blockers used for heart failure (bisoprolol, carvedilol, metoprolol): risk of arterial hypotension, cardiac weakness in patients with heart failure (both latent and uncontrolled). Co-administration of amlodipine is safe with thiazide diuretics, ACE inhibitors, β-receptor blockers, long-acting nitrates, sublingual nitroglycerin, digoxin, warfarin, atorvastatin, sildenafil, drugs to reduce gastric acidity (aluminum hydroxide gel, magnesium hydroxide, simethicone), cimetidine, NSAIDs , antibiotics and oral hypoglycemic drugs. Consuming grapefruit juice does not significantly affect the pharmacokinetics of amlodipine. General properties of perindopril and amlodipine Drugs whose simultaneous administration requires monitoring: baclofen - may enhance the antihypertensive effect; antihypertensive drugs (such as beta-receptor blockers) and vasodilators : the simultaneous use of these drugs may enhance the hypotensive effect of perindopril and amlodipine; α-receptor blockers (prazosin, alfuzosin, doxazosin, tamsulosin, terazosin): enhance the antihypertensive effect and increase the risk of orthostatic hypotension; GCS, tetracosactide : weakening of the antihypertensive effect (through the retention of water and salts of GCS); amifostine : may enhance the hypotensive effect; tricyclic antidepressants/antipsychotics/anesthetics : increased antihypertensive effect and increased risk of orthostatic hypotension.

Contraindications and adverse reactions

A common contraindication for the two drugs is intolerance to perindopril and allergy to auxiliary components. Otherwise, the drugs have a number of contraindications, which must be taken into account when choosing the best drug for treatment.

What are the contraindications for the drug Prestarium:

1. angioedema of hereditary type, including idiopathic;
2. aortic stenosis;
3. severe autoimmune collagenosis, scleroderma;
4. intolerance to drugs of the ACE inhibitor group;
5. coronary and cerebral insufficiency bleeding;
6. diabetes;
7. elderly age;
8. chronic renal failure, which is accompanied by hypercalcemia.

Medicines are not prescribed to women during pregnancy, during pregnancy planning and during breastfeeding. The drugs have a systemic effect, the components are able to penetrate the placenta and into breast milk.

The drug Perindopril has the following contraindications:

1. previous angioedema while taking ACE inhibitors;
2. idiopathic and hereditary angioedema;
3. severe autoimmune connective tissue diseases;
4. kidney transplantation;
5. chronic renal failure;
6. impaired blood circulation in the bone marrow while taking immunosuppressants;
7. dehydration of the body;
8. condition after general anesthesia;
9. a diet with reduced sodium intake;
10. childhood, pregnancy and lactation.

There are conditions in which an antihypertensive drug may be prescribed with caution. In particular, these are diseases associated with circulatory disorders.

The prescription of medication for coronary insufficiency, acute ischemic disease, when there is a risk of a strong decrease in blood pressure, is considered individually. The medicine is used with caution in cases of cerebrovascular accident.

Special instructions for the use of the drug Bi-prestarium

All warnings associated with each of the components of the drug apply to the drug Bi-Prestarium. For perindopril Arterial hypotension. ACE inhibitors can cause a sharp decrease in blood pressure, which occurs more often in patients with hypovolemia or in patients with severe renin-dependent hypertension. In patients at high risk of symptomatic hypotension, as well as patients with coronary artery disease or cerebrovascular disease in whom an excessive decrease in blood pressure may cause the development of myocardial infarction or stroke, blood pressure, renal function, and serum potassium concentrations should be carefully monitored. Aortic and mitral valve stenosis/hypertrophic cardiomyopathy ACE inhibitors should be prescribed with caution to patients with mitral valve stenosis and/or left ventricular outflow tract obstruction (aortic stenosis, hypertrophic cardiomyopathy). Neutropenia/agranulocytosis/thrombocytopenia/anemia. Perindopril should be prescribed with caution to patients with collagen diseases, during therapy with immunosuppressants, allopurinol or procainamide, especially in the presence of renal impairment, due to the risk of neutropenia/agranulocytosis, thrombocytopenia and anemia. In patients with impaired renal function and in elderly patients, the excretion of perindoprilate is reduced. Therefore, frequent monitoring of creatinine and potassium levels is necessary during treatment. While taking ACE inhibitors, some patients with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney may experience a reversible increase in blood urea and serum creatinine concentrations. The presence of renovascular hypertension increases the risk of severe arterial hypotension and renal failure. Liver dysfunction . If a patient develops jaundice or significantly elevated liver enzyme levels while taking an ACE inhibitor, the ACE inhibitor should be discontinued and the patient should be monitored closely medically. Anaphylactoid reactions during LDL apheresis. Rarely, life-threatening anaphylactoid reactions may occur in patients taking ACE inhibitors during LDL apheresis with dextran sulfate. The development of anaphylactoid reactions can be avoided by temporarily stopping the use of ACE inhibitors before starting plasmapheresis. Anaphylactoid reactions during desensitizing therapy. Patients who take ACE inhibitors during desensitization treatment with drugs containing bee venom may experience anaphylactoid reactions. These reactions can be avoided by temporarily stopping the use of ACE inhibitors. If the patient is about to undergo surgery or requires anesthesia , treatment with the ACE inhibitor should be discontinued the day before surgery (see INTERACTIONS WITH OTHER MEDICINES). Hyperkalemia may occur in patients taking ACE inhibitors. Risk factors for hyperkalemia include renal failure or deterioration of renal function, age (over 70 years), diabetes mellitus, intercurrent conditions such as dehydration, acute cardiac decompensation, metabolic acidosis. For amlodipine Patients with impaired liver function. As with other calcium antagonists, the half-life of amlodipine is prolonged in patients with impaired liver function. Therefore, amlodipine should be prescribed to such patients with caution, with careful monitoring of liver enzyme levels. Amlodipine should be prescribed with caution in patients with heart failure For elderly patients, the recommended dosage is the same as for other patients, but dose increases should be done with caution. For Bi-Prestarium, Bi-Prestarium can be prescribed to patients with creatinine clearance ≥60 ml/min. For patients with creatinine clearance ≤60 ml/min, individual dose selection is recommended for each of the components of the drug separately. The drug contains lactose , therefore patients with congenital galactose intolerance, glucose and galactose malabsorption syndrome, Lapp lactase deficiency are not recommended to prescribe the drug. Children Bi-Prestarium is not recommended for use in children under 18 years of age due to the lack of studies in this group of patients. Pregnancy and breastfeeding The drug Bi-Prestarium is not recommended for use in the first trimester of pregnancy. If pregnancy is established, alternative therapy should be started as soon as possible. Bi-Prestarium is contraindicated in the second and third trimester of pregnancy. It is not recommended to take Bi-Prestarium while breastfeeding. The ability to influence the reaction rate when driving vehicles or other mechanisms When driving a car or when working with various mechanisms, the possibility of developing such adverse drug reactions as dizziness or weakness should be taken into account.

Comparison of side effects by frequency

The risk of side effects from Prestarium and Perindopril increases if the instructions for use are not followed. Important

strictly follow the course of treatment and dosage prescribed by your doctor.

Price and analogues

You can buy the drug Prestarium at a price of 370 rubles, Perindopril - from 90 rubles, the average cost from different manufacturers is about 250 rubles.

When choosing analogues, a doctor may consider the following options:

1. Prilamide;
2. Bi-Prestarium;
3. Prestarium-Combi;
4. Promepril;
5. Triplix;
6. Triveram.

The drugs Prestarium and Perindopril are analogues. The choice of medication depends on the underlying disease and associated disorders.

Dosage and method of administration

Prestarium 2.5 and 10 mg cannot be divided and are taken in one dose. 5 mg tablets can be divided into two doses. It is recommended to take 1 time per day at the same time. The dosage is selected by the doctor individually, taking into account the underlying disease and associated disorders. Prestarium can be used both independently and in complex therapy.

Perindopril should be taken in the morning on an empty stomach. The initial standard dosage is 4 mg/day. Gradually the dose can be increased to 8 mg/day. In elderly patients, the initial dose may be 2 mg/day with further increases. For kidney disease, the dosage may be reduced depending on blood and urine test results.

Which medicine is better - the opinion of doctors and patients

Perindopril and Prestarium contain a similar main component in the composition. Tablets have different dosages and excipients. Each antihypertensive drug is prescribed according to strict indications specified in the instructions.

When choosing a treatment, it is impossible to say which medicine is better, because each has advantages and disadvantages. Prestarium is more expensive and has been showing its effectiveness for more than 20 years. Perindopril is a similar drug, but with other auxiliary components.

Medicines have the same indications and contraindications. This takes into account the effect of additional components on the body, which can be decisive when choosing a drug.

Risks and Precautions

It's important to remember the risk

development of severe arterial hypotension, especially when the water-salt balance in the body is disturbed. During the treatment period, you need to undergo regular tests in order to notice and prevent sodium loss in time.

You cannot combine Prestarium and Perindopril with a diuretic

. For the period of treatment, the latter are canceled at least 3 days before the start of the course of treatment. Patients at risk with severe systemic diseases undergo therapy under the supervision of medical personnel.

Due to the risk of dizziness and hypotension, driving and engaging in activities requiring increased attention are limited for the entire treatment period. The drugs may affect concentration and motor activity.

Both drugs cope with their task and are widely used to treat arterial hypertension. If one medicine is poorly tolerated by the patient, the doctor may prescribe another. The means have more in common than differences. If you follow your doctor's instructions, each medication is well tolerated with minimal chance of adverse reactions. Be aware of the risks of self-medication and always tell your doctor about unusual symptoms that occur during treatment.

Contraindications to the use of the drug Bi-prestarium

Hypersensitivity to perindopril (or any other ACE inhibitors), amlodipine (or other dihydropyridines) or to any excipient; history of angioedema associated with previous treatment with ACE inhibitors; congenital or idiopathic angioedema; During pregnancy and breastfeeding; severe arterial hypotension; shock, including cardiogenic; obstruction of the exit from the left ventricle (for example, clinically significant aortic stenosis); unstable angina (with the exception of Prinzmetal angina); heart failure after acute myocardial infarction (during the first 28 days).