Prestilol
Prestilol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Prestilol
ATX code: C09BX02
Active ingredient: bisoprolol (bisoprolol) + perindopril (perindopril)
Producer: Laboratories Servier Industry (France)
Description and photo updated: 17.07.2018
Prices in pharmacies: from 440 rubles.
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Prestilol is an antihypertensive drug that is a combination of a selective beta 1 -adrenergic blocker and an angiotensin-converting enzyme (ACE) inhibitor.
Release form and composition
The drug is available in the form of film-coated tablets: oblong, biconvex, orange-pink in color, with a dividing line, engraved on two sides: on one side - in the form of two inverted triangles and an asterisk on the side of one of them, on the other - “5 / 5 "," 5/10 "," 10/5 "or" 10/10 "(29 pcs. Or 30 pcs. In polypropylene bottles with a dispenser, in a cardboard box with first opening control 1 bottle; for hospitals - by 30 pcs. In polypropylene bottles with a dispenser, in a cardboard box with first opening control 3 bottles; each box also contains instructions for the use of Prestilol).
In 1 tablet, the content of active ingredients can be (it corresponds to the engraving on the tablet):
- tablets at a dose of 5 mg + 5 mg: bisoprolol fumarate - 5 mg (equivalent to the content of 4.24 mg of bisoprolol) + perindopril arginine - 5 mg (equivalent to the content of 3.39 mg of perindopril);
- tablets at a dose of 5 mg + 10 mg: bisoprolol fumarate - 5 mg (equivalent to the content of 4.24 mg of bisoprolol) + perindopril arginine - 10 mg (equivalent to the content of 6.79 mg of perindopril);
- tablets at a dose of 10 mg + 5 mg: bisoprolol fumarate - 10 mg (equivalent to the content of 8.49 mg of bisoprolol) + perindopril arginine - 5 mg (equivalent to the content of 3.39 mg of perindopril);
- tablets at a dose of 10 mg + 10 mg: bisoprolol fumarate - 10 mg (equivalent to the content of 8.49 mg of bisoprolol) + perindopril arginine - 5 mg (equivalent to the content of 6.79 mg of perindopril).
Excipients: pregelatinized starch, microcrystalline cellulose, croscarmellose sodium, calcium carbonate, sodium carboxymethyl starch, magnesium stearate, anhydrous colloidal silicon.
The composition of the film shell: macrogol 6000, glycerol, titanium dioxide, hypromellose, iron dye yellow oxide, magnesium stearate, iron dye red oxide.
Pharmacological properties
Pharmacodynamics
Prestilol is a combined antihypertensive drug consisting of a selective beta 1- blocker and an ACE inhibitor (bisoprolol + perindopril).
Bisoprolol is a highly selective blocker of beta 1 -adrenergic receptors, does not have a stimulating and corresponding membrane stabilizing effect. In general, it does not affect airway resistance and metabolic processes, since it has only a slight affinity for beta 2 -adrenergic receptors involved in metabolic regulation, as well as beta 2 -adrenergic receptors of bronchial and vascular smooth muscles. Bisoprolol retains selective activity to beta 1 -adrenergic receptors and outside the range of therapeutic doses.
Perindopril is an ACE inhibitor that converts angiotensin I to the vasoconstrictor substance angiotensin II. In addition, ACE (kinase II) promotes the breakdown of bradykinin, which has a vasodilating effect, to heptapeptide. As a result of ACE inhibition, a decrease in the concentration of angiotensin II in the blood plasma occurs, causing an increase in plasma renin activity and a decrease in aldosterone secretion.
Suppression of ACE against the background of inactivation of bradykinin is accompanied by an increase in the activity of the prostaglandin system, circulating and tissue kallikrein-kinin system. It is assumed that this effect is responsible for the antihypertensive effect of ACE inhibitors and is part of the mechanism for the development of cough and some other side effects.
The therapeutic effect of perindopril is due to the active metabolite of perindoprilat, while other metabolites do not have an inhibitory effect on ACE in vitro.
Bisoprolol has no significant negative inotropic effects. After oral administration, its maximum effect occurs in 3-4 hours. The half-life (T 1/2) is 10-12 hours, so bisoprolol continues to act for 24 hours. The maximum antihypertensive effect is achieved after 14 days of use.
With ischemic heart disease (coronary artery disease) without CHF (chronic heart failure), a single dose of bisoprolol reduces heart rate (heart rate) and stroke volume, which causes a decrease in cardiac output and oxygen consumption. Regular intake of Prestilol helps to reduce the initially increased peripheral vascular resistance. Suppression of renin activity in blood plasma is considered as the main mechanism of action, providing beta-blockers with an antihypertensive effect.
Bisoprolol, blocking the beta-adrenergic receptors of the heart, reduces the sympathoadrenergic reaction, which results in a decrease in heart rate and myocardial contractility, which leads to a decrease in myocardial oxygen demand in angina pectoris caused by coronary artery disease.
In the treatment of hypertension of any severity, perindopril lowers systolic and diastolic blood pressure (BP) in the supine and standing positions.
A decrease in blood pressure is achieved as a result of a decrease in the total peripheral vascular resistance (OPSR), which leads to an improvement in peripheral blood flow without disturbing the heart rate.
Taking perindopril usually increases only renal blood flow, while the glomerular filtration rate (GFR) remains unchanged.
The clinical efficacy and safety of bisoprolol in CHF III – IV functional class according to NYHA classification (New York Heart Association) are confirmed by the results of the studies. In patients with ejection fraction less than 35%, there was a decrease in overall mortality from 17.3% to 11.8%. In addition, Prestilol helps to reduce the number of sudden deaths, the number of episodes requiring hospitalization, and a significant improvement in the functional status of CHF according to the NYHA classification.
After a single oral administration of perindopril, the maximum antihypertensive effect develops within 4-6 hours and lasts for at least 24 hours. The decrease in blood pressure occurs quickly. In patients with an adequate response to treatment, taking Prestilol for 30 days can normalize blood pressure, which persists without the development of tachyphylaxis. Abrupt withdrawal of the drug does not cause a rebound effect.
Perindopril reduces left ventricular hypertrophy, has a vasodilating effect, helps to restore the elasticity of large arteries and reduce the ratio of wall thickness and lumen of small arteries.
The simultaneous use of thiazide diuretics contributes to the mutual enhancement of the effects, reduces the risk of hypokalemia associated with diuretic therapy.
In the treatment of stable coronary artery disease without clinical symptoms of CHF, the addition of perindopril to patients taking a beta-blocker can significantly reduce the absolute risk of cardiovascular mortality, non-fatal myocardial infarction and / or cardiac arrest.
The results of clinical studies of combination therapy with an angiotensin II receptor antagonist (ARA II) indicate that in patients with diabetic nephropathy, ACE inhibitors and ARA II should not be combined.
The safety and efficacy of Prestilol in patients under the age of 18 have not been established.
Pharmacokinetics
The rate and degree of absorption of active substances in the composition of Prestilol does not significantly differ from the pharmacokinetics of bisoprolol and perindopril when used as monotherapy.
After oral administration, absorption of bisoprolol from the gastrointestinal tract occurs almost completely (more than 90%), its bioavailability is about 90%.
Perindopril is rapidly absorbed after oral administration. The maximum concentration (C max) of the substance is achieved in blood plasma within 1 hour, T 1/2 from blood plasma - 1 hour. The relationship between dose and plasma concentration of perindopril is linear.
The volume of distribution (V d) of bisoprolol is 3.5 l / kg, binding to blood plasma proteins is approximately 30%.
V d of free perindoprilat is about 0.2 l / kg, the connection with blood plasma proteins (to a greater extent with ACE) is dose-dependent and is 20%.
50% of bisoprolol is metabolized in the liver with the formation of inactive metabolites. Bisoprolol is excreted through the kidneys: 50% - in the form of inactive metabolites and 50% - unchanged. Its total clearance is 15 l / h, T 1/2 from blood plasma - 10-12 hours.
Perindopril is a prodrug. It is metabolized to form the active metabolite of perindoprilat and five inactive metabolites. The bloodstream receives 27% of the amount taken orally in the form of perindoprilat. The maximum concentration of the active metabolite in blood plasma is reached within 3-4 hours. Simultaneous food intake reduces the rate of biotransformation and bioavailability of perindopril, so it is recommended to take it in the morning before meals.
Perindoprilat is excreted through the kidneys. The final T 1/2 of the free fraction is 17 hours, the equilibrium state is reached within 96 hours.
The pharmacokinetics of bisoprolol does not depend on age and is linear. In case of impaired liver function or renal failure, its dose adjustment is not required. In patients with CHF, the pharmacokinetics of impaired liver or kidney function has not been established. It should be borne in mind that in patients with CHF class III (NYHA classification), the level of bisoprolol concentration in the blood plasma is higher, and T 1/2 is from 12 to 22 hours.
With renal and heart failure in elderly patients, the excretion of perindoprilat is slowed down. In this regard, in patients with renal insufficiency, it is recommended to adjust the dose taking into account the degree of impaired renal function or creatinine clearance (CC).
The clearance of perindoprilat during dialysis is 70 ml / min.
In patients with liver cirrhosis, dose adjustment of Prestilol is not required.
Indications for use
The use of Prestilol is indicated in patients with stable coronary artery disease and / or arterial hypertension, and / or stable chronic heart failure with reduced systolic function of the left ventricle in cases where therapy involves the simultaneous administration of bisoprolol and perindopril in appropriate doses.
Contraindications
- cardiogenic shock;
- acute heart failure;
- episodes of decompensation of heart failure, requiring intravenous (IV) administration of inotropic drugs;
- sick sinus syndrome;
- AV block (atrioventricular block) of II and III degrees in the absence of a pacemaker;
- sinoatrial blockade;
- severe arterial hypotension (systolic blood pressure less than 100 mm Hg);
- severe bradycardia (heart rate less than 60 beats per minute);
- severe violations of peripheral arterial circulation;
- Raynaud's syndrome in severe form;
- untreated pheochromocytoma;
- severe form of chronic obstructive pulmonary disease;
- severe bronchial asthma;
- metabolic acidosis;
- hereditary or idiopathic angioedema;
- Quincke's edema (angioneurotic edema) while taking ACE inhibitors in history;
- concomitant therapy with aliskiren-containing agents in patients with diabetes mellitus or with impaired renal function (GFR less than 60 ml / min per 1.73 m 2 of body surface area);
- collapse;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- established hypersensitivity to ACE inhibitors;
- individual intolerance to the components of the drug.
Prestilol should be prescribed with caution in patients with a high risk of severe arterial hypotension, hypovolemia and hyponatremia (adherence to a salt-free diet, prior diuretic therapy, dialysis, vomiting and / or diarrhea), the presence of risk factors for the development of hyperkalemia, cerebrovascular diseases (including cerebrovascular insufficiency), coronary insufficiency, a history of angioedema, restrictive cardiomyopathy, congenital heart defects, with hemodynamically significant organic lesions of the heart valves, myocardial infarction (postponed in the last 3 months), bradycardia, AV-blockade of the 1st degree, mitral stenosis, aortrophic stenosis, hyper cardiomyopathy, Prinzmetal angina, renovascular hypertension, impaired renal function (GFR less than 90 ml / min),bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, hemodialysis using high-flow membranes, in the period after kidney transplantation, in type 1 diabetes mellitus, significant fluctuations in blood glucose levels in type 2 diabetes mellitus, bronchial asthma, obstructive respiratory diseases, neutropenia, agranulocytosis, thrombocytopenia, anemia, peripheral arterial occlusive disease, pheochromocytoma, hyperthyroidism, psoriasis, severe liver dysfunction, glucose-6-phosphate dehydrogenase deficiency, connective tissue diseases (including systemic lupus erythematosus, scleroderma, anemia), depression, treatment of black patients, abrupt withdrawal of therapy.hemodialysis using high-flow membranes, in the period after kidney transplantation, with type 1 diabetes mellitus, significant fluctuations in blood glucose levels in type 2 diabetes mellitus, bronchial asthma, obstructive respiratory diseases, neutropenia, agranulocytosis, thrombocytopenia, anemia, occlusive peripheral arterial disease, pheochromocytoma, hyperthyroidism, psoriasis, severe liver dysfunction, glucose-6-phosphate dehydrogenase deficiency, connective tissue diseases (including systemic lupus erythematosus, scleroderma), depression (including history), adherence to a strict diet, treatment of black patients, abrupt withdrawal of therapy.hemodialysis using high-flow membranes, in the period after kidney transplantation, with type 1 diabetes mellitus, significant fluctuations in blood glucose levels in type 2 diabetes mellitus, bronchial asthma, obstructive respiratory diseases, neutropenia, agranulocytosis, thrombocytopenia, anemia, occlusive peripheral arterial disease, pheochromocytoma, hyperthyroidism, psoriasis, severe liver dysfunction, deficiency of glucose-6-phosphate dehydrogenase, connective tissue diseases (including systemic lupus erythematosus, scleroderma), depression (including history), adherence to a strict diet, treatment of black patients, abrupt withdrawal of therapy.obstructive respiratory diseases, neutropenia, agranulocytosis, thrombocytopenia, anemia, occlusive peripheral arterial disease, pheochromocytoma, hyperthyroidism, psoriasis, severe liver dysfunction, glucose-6-phosphate dehydrogenase deficiency, connective tissue diseases (including systemic lupus erythematosus) including history), adherence to a strict diet, treatment of black patients, abrupt withdrawal of therapy.obstructive respiratory diseases, neutropenia, agranulocytosis, thrombocytopenia, anemia, occlusive peripheral arterial disease, pheochromocytoma, hyperthyroidism, psoriasis, severe liver dysfunction, glucose-6-phosphate dehydrogenase deficiency, connective tissue diseases (including systemic lupus erythematosus) including history), adherence to a strict diet, treatment of black patients, abrupt withdrawal of therapy.treatment of black patients, abrupt discontinuation of therapy.treatment of black patients, abrupt discontinuation of therapy.
The doctor should be informed about taking Prestilol during the procedure of apheresis of LDL (low density lipoproteins), the simultaneous appointment of desensitizing therapy, lithium preparations, potassium-sparing diuretics, angiotensin receptor blockers, aliskiren-containing drugs, blockers of slow calcium channels, antiarrhythmics of class I, antiarrhythmics potassium salt preparations, surgical intervention using general anesthesia.
Prestilol, instructions for use: method and dosage
Prestilol tablets are taken orally, in the morning before meals, once a day.
The dose of the drug is determined by the doctor based on clinical indications, including taking into account the doses of bisoprolol and perindopril of the previous monotherapy.
If the administration of 2.5 mg of bisoprolol and 2.5 mg of perindopril is indicated, 1/2 tablet of Prestilol 5 mg + 5 mg once a day should be taken.
When prescribing the drug in a dose of 2.5 mg of bisoprolol and 5 mg of perindopril, 1/2 tablet should be taken with a dosage of 5 mg + 10 mg once a day.
In case of impaired renal function, a single dose of Prestilol is prescribed taking into account the individual CC in the blood and may be the following amount of active components (bisoprolol + perindopril):
- CC 60 ml / min and above: initial dose - 2.5 mg + 5 mg. In the absence of the desired therapeutic effect and good tolerance, the dose of bisoprolol can be increased and Prestilol tablets 5 mg + 5 mg or 10 mg + 5 mg can be used;
- CC 30-60 ml / min: 2.5 mg + 2.5 mg (1/2 tablet at a dose of 5 mg + 5 mg);
- CC less than 30 ml / min: the drug should not be taken. It is recommended to use the selection of doses of each component separately.
For the treatment of elderly patients, doses should be prescribed in accordance with the recommendations for patients with impaired renal function; dose titration should be performed under close medical supervision.
Side effects
Adverse reactions established against the background of bisoprolol monotherapy during clinical trials and / or in the post-registration period:
- infections and invasions: rarely - rhinitis;
- mental disorders: infrequently - sleep disorders, depression; rarely - terrible dreams, hallucinations;
- from the nervous system: often - headache, dizziness; rarely - fainting;
- on the part of the organ of vision: rarely - reduced lacrimation; very rarely - conjunctivitis;
- from the organ of hearing: rarely - hearing impairment;
- from the side of the heart: very often - bradycardia; often - worsening of the course of heart failure; infrequently - violation of AV conduction;
- on the part of the vessels: often - lowering blood pressure (including accompanying effects), feeling of numbness or coldness of the extremities; infrequently - orthostatic hypotension;
- from the gastrointestinal tract: often - abdominal pain, nausea, vomiting, constipation, diarrhea;
- from the hepatobiliary system: rarely - cytolytic or cholestatic hepatitis;
- from the respiratory system, chest and mediastinal organs: infrequently - bronchospasm;
- dermatological reactions: rarely - hypersensitivity reactions in the form of itching, redness, rash; very rarely - alopecia, development of psoriasis or worsening of its course, the appearance of a psoriasis-like rash;
- on the part of the musculoskeletal system and connective tissue: infrequently - muscle spasms, muscle weakness;
- from the reproductive system and mammary glands: rarely - violation of potency;
- general disorders: often - increased fatigue, asthenia;
- laboratory indicators: rarely - an increase in the activity of hepatic transaminases, an increase in triglyceride levels.
Adverse reactions established during monotherapy with perindopril during clinical trials and / or in the post-registration period:
- infections and invasions: very rarely - rhinitis;
- on the part of the blood and lymphatic system: infrequently - eosinophilia; very rarely - agranulocytosis, leukopenia, pancytopenia, thrombocytopenia, neutropenia, with congenital insufficiency of glucose-6-phosphate dehydrogenase - hemolytic anemia;
- on the part of metabolism and nutrition: infrequently - hypoglycemia, transient hyperkalemia, hyponatremia;
- mental disorders: infrequently - sleep disorders, mood disorders; very rarely - confusion of consciousness;
- from the nervous system: often - headache, paresthesia, dizziness, dysgeusia, vertigo; infrequently - drowsiness, fainting;
- on the part of the organ of vision: often - visual impairment;
- from the organ of hearing: often - tinnitus;
- from the heart: infrequently - palpitations, tachycardia; very rarely - arrhythmia, angina pectoris, myocardial infarction;
- on the part of the vessels: often - lowering blood pressure (including accompanying effects); infrequently - vasculitis; very rarely - stroke (more often in high-risk patients, possibly due to a significant decrease in blood pressure);
- from the respiratory system, chest and mediastinal organs: often - cough, shortness of breath; infrequently - bronchospasm; very rarely - eosinophilic pneumonia;
- from the gastrointestinal tract: often - abdominal pain, nausea, vomiting, dyspepsia, constipation, diarrhea; infrequently - dryness of the oral mucosa; very rarely - pancreatitis;
- from the hepatobiliary system: very rarely - cytolytic or cholestatic hepatitis;
- dermatological reactions: often - itching, rash; infrequently - angioedema (face, lips, mucous membranes, tongue, glottis and / or larynx, extremities), urticaria, pemphigoid, photosensitivity reactions, hyperhidrosis; rarely - worsening of the course of psoriasis; very rarely - erythema multiforme;
- from the musculoskeletal system and connective tissue: often - muscle spasms; infrequently - arthralgia, myalgia;
- from the urinary system: infrequently - impaired renal function; very rarely - acute renal failure;
- on the part of the reproductive system and mammary glands: infrequently - erectile dysfunction;
- general disorders: often - asthenia; infrequently - malaise, chest pain, peripheral edema, hyperthermia;
- laboratory indicators: infrequently - an increase in the concentration of urea in the blood, an increase in the content of creatinine in the blood; rarely - an increase in the activity of hepatic transaminases, an increase in the level of bilirubin in the blood; very rarely - a decrease in hemoglobin and hematocrit;
- others: infrequently - falls.
Overdose
When taking an increased dose of Prestilol, it is necessary to take into account the symptoms associated with an overdose of beta-blockers and ACE inhibitors.
Symptoms in case of an overdose of beta-blockers: arterial hypotension, bradycardia, acute heart failure, bronchospasm, hypoglycemia.
Treatment: the appointment of symptomatic therapy. Careful monitoring of the patient's condition is necessary. In the case of a sharp deterioration in the course of heart failure, the patient should be prescribed intravenous administration of a diuretic, inotropic and vasodilators. With the development of bradycardia, intravenous administration of atropine is indicated. In the absence of a sufficient clinical effect, an agent with a positive chronotropic effect (isoprenaline) can be administered; if necessary, a transvenous installation of an artificial pacemaker is recommended. With severe arterial hypotension - in / in the introduction of fluids, vasoconstrictor drugs, glucagon. If careful monitoring of the patient's condition indicates the development of grade II – III AV block, isoprenaline infusion or transvenous installation of an artificial pacemaker is required. In case of bronchospasm, the administration of bronchodilators (including isoprenaline, beta2 -sympathomimetics and / or aminophylline), with hypoglycemia - intravenous glucose. The use of hemodialysis is ineffective.
Symptoms of an overdose of ACE inhibitors: arterial hypotension, palpitations, tachycardia, bradycardia, cough, dizziness, anxiety, imbalance in water and electrolyte balance, renal failure, hyperventilation, circulatory shock.
Treatment: the appointment of symptomatic therapy. It is necessary to control the concentration of electrolytes and creatinine in the blood serum, indicators of the basic vital functions of the body. With severe arterial hypotension, the patient should be placed on his back and his legs raised. Assign intravenous infusion of 0.9% sodium chloride solution, if necessary - intravenous administration of a solution of catecholamines and / or angiotensin II. An artificial pacemaker may be required.
special instructions
When prescribing Prestilol, the mechanism of action of each of the active substances of the drug and possible undesirable effects due to concomitant pathologies and interactions with other drugs should be taken into account.
As an ACE inhibitor, perindopril can cause a sharp decrease in blood pressure. Patients with reduced blood volume, which may result from diarrhea / vomiting, concurrent use of diuretics, adherence to a strict salt-free diet, hemodialysis, or patients with severe arterial hypertension with high renin activity, are at a higher risk of an excessive decrease in blood pressure. In patients with clinical manifestations of heart failure, the occurrence of severe arterial hypotension can be observed both with and without renal failure. In addition, an excessive decrease in blood pressure in cerebrovascular diseases and ischemic heart disease can cause the development of myocardial infarction or acute cerebrovascular accident. In this regard, in patients with an increased risk of developing symptomatic arterial hypotension, it is recommended to start treatment and make dose adjustments under close medical supervision. In the event of arterial hypotension, the patient should take a horizontal position. To replenish the volume of fluid in the body, intravenous infusion of 0.9% sodium chloride solution is indicated. After replenishing the volume of circulating blood and increasing blood pressure, Prestilol can be continued. After replenishing the volume of circulating blood and increasing blood pressure, Prestilol can be continued. After replenishing the circulating blood volume and increasing blood pressure, Prestilol can be continued.
In some cases with CHF in patients with normal or low blood pressure, it is advisable to prescribe individual components of the drug as monotherapy.
It should be borne in mind that the risk of developing angioedema while taking an ACE inhibitor increases with the simultaneous use of sirolimus, temsirolimus, everolimus, or if the patient has a history of indications of angioedema of any genesis.
It has been established that angioedema occurs more often in patients of the Negroid race. In addition, in this category of patients, the therapeutic efficacy of perindopril is low.
When carrying out the differential diagnosis of dry persistent cough, it should be taken into account as a possible side effect of Prestilol.
Factors that increase the risk of developing hyperkalemia are: renal failure, impaired liver function, diabetes mellitus, age over 70 years, dehydration, metabolic acidosis, acute decompensation of cardiac activity, concomitant use of drugs that increase serum potassium levels (for example, heparin), potassium preparations, potassium-sparing diuretics (including spironolactone, triamterene, amiloride, eplerenone), salt substitutes, or food supplements containing potassium. Heart rhythm disturbances caused by hyperkalemia can be fatal. In this regard, if it is necessary to combine Prestilol with the above agents, the potassium content in the blood serum should be regularly monitored.
With caution, only if absolutely necessary, the simultaneous use of perindopril with angiotensin II receptor blockers or aliskiren is allowed. This combination is not recommended due to the increased risk of arterial hypotension, renal dysfunction and hyperkalemia.
Abrupt withdrawal of Prestilol, especially in patients with coronary artery disease, can cause a temporary deterioration in cardiac activity. If it is necessary to discontinue treatment, the dose should be reduced gradually (over 14 days or more) using separate components, and replacement therapy should be started in parallel.
If, against the background of the use of Prestilol in a patient at rest, a decrease in heart rate to 50–55 beats per minute or less is observed, causing the development of symptoms associated with bradycardia, it is necessary to consider lowering the dose of the drug while maintaining an acceptable dose of bisoprolol.
Carrying out hemodialysis using high-flow membranes while taking an ACE inhibitor is associated with the risk of developing anaphylactoid reactions; therefore, it is recommended to use a different type of dialysis membrane.
There is a risk of thrombocytopenia, anemia, neutropenia, or agranulocytosis. In patients with normal renal function and in the absence of aggravating factors, neutropenia rarely develops. The use of perindopril in patients with severe infections is recommended to be accompanied by periodic monitoring of the leukocyte count in the blood.
In patients with bronchial asthma and other chronic obstructive pulmonary pathologies, the use of beta-blockers can increase airway resistance, in these cases, an increase in the dose of beta 2 -adrenomimetics is required.
Patients with diabetes should be aware that the effects of beta-blockers can mask the symptoms of hypoglycemia.
Patients with psoriasis (including a history) should be prescribed beta-blockers after a careful assessment of the balance between the benefits of therapy and the associated potential risks.
With pheochromocytoma (or suspicion of it), the use of bisoprolol is indicated only in combination with an alpha-adrenergic receptor blocker.
Bisoprolol may mask the symptoms of hyperthyroidism.
Before carrying out major operations involving the use of anesthetic agents, it is necessary to inform the anesthesiologist about taking Prestilol. This will avoid drug interactions that can cause bradyarrhythmia, attenuation of reflex tachycardia, and a decrease in the reflex ability to compensate for blood loss-related effects. The use of the drug must be discontinued 48 hours before anesthesia.
With the development of depression, drug therapy is recommended to be canceled.
Influence on the ability to drive vehicles and complex mechanisms
Prestilol does not have a direct effect on the patient's ability to drive a vehicle and work with mechanisms, but individual reactions should be taken into account, especially at the initial stage of use or when changing the drug, associated with a decrease in blood pressure.
Application during pregnancy and lactation
The use of Prestilol is contraindicated during the period of gestation and breastfeeding.
When planning a pregnancy, it is necessary to switch to the use of an alternative antihypertensive drug with an established safety profile.
Pediatric use
Due to the lack of information on the safety and efficacy of the drug for the treatment of children and adolescents, Prestilol is contraindicated in patients under the age of 18 years.
With impaired renal function
A combined antihypertensive agent should be prescribed with caution in case of impaired renal function (GFR less than 90 ml / min).
A single dose of Prestilol is prescribed taking into account the individual CC in the blood and may be the following amount of active components (bisoprolol + perindopril):
- CC 60 ml / min and above: initial dose - 2.5 mg + 5 mg. In the absence of the desired therapeutic effect and with good tolerance, the dose of bisoprolol can be increased and tablets of 5 mg + 5 mg or 10 mg + 5 mg can be used;
- CC 30-60 ml / min: 2.5 mg + 2.5 mg (1/2 tablet at a dose of 5 mg + 5 mg);
- CC less than 30 ml / min: the drug should not be taken. It is recommended to use the selection of doses of each component separately.
For violations of liver function
Prestilol should be taken with caution in severe liver dysfunction.
If hepatic function is impaired, dose adjustment is not required.
Use in the elderly
For the treatment of elderly patients, the dose of Prestilol should be determined in accordance with the recommendations for patients with impaired renal function and titrated under close medical supervision.
Drug interactions
With the simultaneous use of Prestilol:
- aliskiren, potassium-sparing diuretics, ACE inhibitors, non-steroidal anti-inflammatory drugs (NSAIDs), angiotensin II receptor blockers, heparins, immunosuppressants (cyclosporin, tacrolimus and similar drugs), trimethoprim, drugs containing potassium salts: increase the risk of hyperkalemia;
- antihypertensive drugs of central action (including clonidine, methyldopa, rilmenidine, moxonidine): contribute to the worsening of heart failure, cause a decrease in heart rate, a decrease in cardiac output and vasodilation. Abrupt withdrawal of therapy without a previous dose reduction of the beta-blocker significantly increases the risk of developing rebound arterial hypertension;
- quinidine, disopyramide, phenytoin, flecainide, lidocaine, propafenone and other class I antiarrhythmics: can affect AV conduction and enhance the negative inotropic effect;
- blockers of slow calcium channels (verapamil, diltiazem): negatively affect contractility and AV conduction. IV administration of verapamil during therapy with beta-blockers can cause severe arterial hypotension and AV blockade;
- angiotensin II receptor blockers and aliskiren: the combination of ACE inhibitors with angiotensin II receptor blockers or aliskiren causes double blockade of the renin-aldosterone-angiotensin system (RAAS), caused by arterial hypotension, hyperkalemia or decreased renal function (including acute renal failure), often this combination;
- estramustine: increases the risk of developing angioedema and similar adverse events;
- lithium preparations: promote a reversible increase in the concentration of lithium in the blood and the associated toxic effects;
- insulin, oral hypoglycemic agents: their hypoglycemic effect is enhanced;
- NSAIDs, including acetylsalicylic acid (at a dose of 3 g per day and above), cyclooxygenase 2 (COX-2) inhibitors, non-selective NSAIDs: they can weaken the hypotensive effect of Prestilol, cause deterioration of renal function, including the development of acute renal failure. Patients with initially reduced renal function and in old age are at particular risk;
- vasodilators and antihypertensive drugs (nitroglycerin and other nitrates, tricyclic antidepressants, phenothiazines, barbiturates and other drugs that lower blood pressure): can enhance the antihypertensive effect of Prestilol;
- tricyclic antidepressants, antipsychotics, drugs for general anesthesia: cause an increased risk of arterial hypotension;
- isoprenaline, dobutamine and other beta-sympathomimetics: the therapeutic effect of each drug decreases. Sympathomimetics that activate alpha- and beta-adrenergic receptors (including norepinephrine, adrenaline) increase intermittent claudication;
- felodipine, amlodipine and other blockers of slow calcium channels of the dihydropyridine series: increase the risk of hypotension, further deterioration of the pumping function of the ventricles of the heart in heart failure;
- class III antiarrhythmics (including amiodarone): enhance the effect on AV conduction;
- parasympathomimetics: cause a decrease in AV conduction and an increase in the risk of developing bradycardia;
- local beta-blockers (for example, eye drops): may increase the systemic effects of bisoprolol;
- digitalis preparations: help to decrease heart rate and slow down AV conduction;
- baclofen: causes an increase in the antihypertensive effect of perindopril;
- potassium-sparing diuretics: in patients with reduced BCC and / or salt content, the use of potassium-sparing diuretics may cause an excessive decrease in blood pressure in the initial stages of therapy with an ACE inhibitor. In this regard, it is recommended to avoid the combination with potassium-sparing diuretics, to replenish the BCC before starting therapy with perindopril, or to increase salt intake and start taking perindopril with a low initial dose. In patients with CHF, the dose of a potassium-sparing diuretic should be reduced before starting therapy with an ACE inhibitor. Treatment should be accompanied by careful monitoring of renal function;
- potassium-sparing diuretics (spironolactone, eplerenone): a combination of eplerenone or spironolactone in the dose range of 12.5–50 mg per day with low doses of ACE inhibitors in patients with functional class II – IV heart failure (according to NYHA classification) who have previously taken ACE inhibitors and " loop "diuretics, increases the risk of hyperkalemia (up to death). Therefore, before the appointment of combination therapy, the presence of hyperkalemia and impaired renal function should be excluded, and during the treatment period, regularly (once every 7 days for the first 30 days, then once every 30 days) monitor the concentration of creatinine and potassium in the blood;
- racecadotril: an antidiarrheal agent may contribute to the development of angioedema;
- sirolimus, temsirolimus, everolimus: taking mTOR inhibitors (mammalian target of rapamycin) increases the likelihood of developing angioedema;
- mefloquine: the risk of developing bradycardia increases;
- monoamine oxidase (MAO) inhibitors, except for MAO type B inhibitors: it is possible to increase the effects of beta-blockers and the risk of hypertensive crisis;
- linagliptin, saxagliptin, vildagliptin, sitagliptin (gliptins): cause an increased risk of angioedema;
- gold preparations (sodium aurothiomalate): the administration of gold preparations may be accompanied by flushing, nausea, vomiting, arterial hypotension.
Analogs
The analogue of Prestilol is Kosirel.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Prestilol
There are no patients and doctors about Prestilol.
Price for Prestilol in pharmacies
The price of Prestilol for a package containing 30 tablets at a dose of 5 mg + 5 mg can be from 531 rubles, at a dose of 5 mg + 10 mg - from 580 rubles, at a dose of 10 mg + 10 mg - from 707 rubles.
Prestilol: prices in online pharmacies
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Drug name Price Pharmacy |
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Prestilol 5 mg + 10 mg tablets 30 pcs. 440 RUB Buy |
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Prestilol 5 mg + 5 mg tablets 30 pcs. 494 r Buy |
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Prestilol tablets p.p. 5mg + 5mg 30 pcs. 495 RUB Buy |
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Prestilol 10 mg + 10 mg tablets 30 pcs. RUB 680 Buy |
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Prestilol tablets p.p. 10mg + 10mg 30 pcs. 707 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!