Renitek
Renitek: 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: Renitec
ATX code: C09AA02
Active ingredient: Enalapril maleate (Enalaprili maleates)
Producer: Merck Sharp & Dohme (Netherlands)
Description and photo update: 2018-22-10
Prices in pharmacies: from 50 rubles.
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Renitek is a drug used for arterial and renovascular hypertension.
Release form and composition
The dosage form of Renitek is tablets: triangular, on one side with a risk; 5 mg each - white, with engraving on the other side "MSD 712"; 10 mg each - pink, engraved on the other side "MSD 713"; 20 mg each - light pink with a yellowish tinge with splashes, engraved on the other side "MSD 714" (7 pcs. in blisters, in a cardboard box 1, 2 or 4 blisters; 100 pcs. in dark glass bottles, in cardboard box 1 bottle).
Composition of 1 tablet:
- active substance: enalapril maleate - 5, 10 or 20 mg;
- auxiliary components (5/10/20 mg): sodium bicarbonate - 2.5 / 5/10 mg; lactose monohydrate - 198.1 / 164.1 / 153.9 mg; pregelatinized starch - 5.06 / 2.2 / 2.2 mg; corn starch - 22.77 / 22/22 mg; magnesium stearate - 0.9 / 1 / 1.1 mg; yellow iron oxide (E172) - 0/0 / 0.13 mg; red iron oxide (E172) - 0 / 0.5 / 0.05 mg.
Pharmacological properties
Pharmacodynamics
Renitek is one of the ACE inhibitors (angiotensin converting enzyme) - drugs that affect the renin-angiotensin-aldosterone system (RAAS). The drug is used in the treatment of essential hypertension - primary hypertension (arterial hypertension) of any severity, as well as renovascular hypertension. It can be used as a monopreparation or in combination with other antihypertensive drugs, mainly with diuretics. In addition, Renitek is used to treat or prevent the development of heart failure (heart failure).
Enalapril is a derivative of L-proline and L-alanine (amino acids). After oral administration, the substance is rapidly absorbed, followed by hydrolysis into enalaprilat. It is a highly specific and long acting ACE inhibitor that does not contain a sulfhydryl group.
ACE (peptidyl dipeptidase A) catalyzes the conversion of angiotensin I to the angiotensin II pressor peptide. Enalaprilat inhibits ACE, which leads to a decrease in the plasma concentration of angiotensin II in the blood and the secretion of aldosterone, as well as an increase in renin activity.
ACE is identical to the enzyme kininase II, and therefore enalapril can also block the destruction of bradykinin, a peptide that has a pronounced vasodilating effect (the meaning of this effect needs to be clarified).
Despite the fact that the main mechanism for lowering blood pressure (blood pressure) is the suppression of the RAAS activity, Renitek also exhibits an antihypertensive effect in patients with hypertension and with reduced renin activity.
The use of enalapril in patients with hypertension leads to a decrease in blood pressure in the standing and lying position without a significant increase in heart rate (heart rate).
Symptomatic postural hypotension is uncommon. In some patients, it may take several weeks of use to achieve an optimal reduction in blood pressure. Interruption of therapy does not lead to a sharp rise in blood pressure.
Effective inhibition of ACE activity, as a rule, develops within 2-4 hours after taking a single dose. The antihypertensive effect develops within 1 hour, the maximum decrease in blood pressure is observed 4–6 hours after taking Renitek. The duration of action depends on the dose. Hemodynamic effects and antihypertensive effects when using the recommended doses persist for 24 hours.
Antihypertensive therapy with enalapril leads to significant regression of left ventricular hypertrophy and contributes to the preservation of its systolic function.
When conducting clinical studies of hemodynamics in patients with essential hypertension, a decrease in blood pressure was accompanied by a decrease in total peripheral vascular resistance, an increase in cardiac output and insignificant changes or no changes in heart rate. After taking enalapril, an increase in renal blood flow is observed. At the same time, there are no signs of fluid or sodium retention and changes in GFR (glomerular filtration rate). However, in patients with initially decreased glomerular filtration, its rate, as a rule, increases.
Long-term therapy for essential hypertension and renal failure can lead to improved renal function, as evidenced by an increase in GFR.
In short clinical studies in patients with renal failure with / without diabetes mellitus, after taking enalapril, there was a decrease in albuminuria, renal excretion of IgG, as well as a decrease in total protein in the urine.
With the combined use of Renitek and thiazide diuretics, the antihypertensive effect is enhanced. Enalapril reduces / prevents the occurrence of hypokalemia caused by taking thiazides.
Enalapril does not have an undesirable effect on the plasma concentration of uric acid in the blood.
Renitek has a beneficial effect on the ratio of lipoprotein fractions in blood plasma. There is also a beneficial / no effect on total cholesterol concentration.
In patients with heart failure, against the background of the use of cardiac glycosides and diuretics, taking Renitek leads to a decrease in the total peripheral resistance and blood pressure. There is an increase in cardiac output, while heart rate (usually increased in HF patients) decreases. The pressure of wedging in the pulmonary capillaries also decreases. According to New York Heart Association (NYHA) criteria, HF severity and exercise tolerance are improving. These effects are observed with long-term treatment.
In mild to moderate heart failure, enalapril slows down the progression of heart dilatation and heart failure (confirmed by an improvement in left ventricular ejection fraction and a decrease in left ventricular systolic and end-diastolic volumes).
Clinical data indicate that enalapril reduces the incidence of ventricular arrhythmias in patients with heart failure, although the clinical significance and underlying mechanisms of this effect are not known.
Pharmacokinetics
Absorption: after oral administration, enalapril is rapidly absorbed in the gastrointestinal tract. The maximum serum concentration in the blood is reached within 1 hour. The degree of absorption of the substance is approximately 60%. Food intake has no effect on the absorption of enalapril. After absorption, the substance is rapidly hydrolyzed, the formation of an active metabolite - enalaprilat, which is a potent ACE inhibitor, occurs. The maximum serum concentration of the substance in the blood is observed approximately 4 hours after oral administration. The duration of absorption and hydrolysis of enalapril is similar for various recommended therapeutic doses. Equilibrium serum concentration of the substance in the blood is reached by the fourth day of application of Renitek.
Distribution: binding of enalaprilat with blood plasma proteins in the range of therapeutic doses - no more than 60%.
Metabolism: there is no information on other significant pathways of metabolism of enalapril, in addition to hydrolysis to enalaprilat.
Excretion: excreted mainly through the kidneys. The main metabolites determined in urine are enalaprilat (about 40% of the dose) and unchanged enalapril (about 20%).
The plasma concentration curve of enalaprilat in the blood has a long final phase. The half-life of the substance during course use is 11 hours.
The AUC (area under the concentration-time curve) of enalaprilat and enalapril increases in patients with renal failure. With creatinine clearance of 40-60 ml / min after taking Renitek in a daily dose of 5 mg, the equilibrium value of AUC of enalaprilat is approximately 2 times higher than in patients with intact renal function. In severe renal failure (creatinine clearance no more than 30 ml / min), the AUC value increases by about 8 times, the effective half-life after repeated administration of the drug increases, and the onset of the equilibrium state of the concentration of enalaprilat is delayed. Enalaprilat can be removed from the general bloodstream using the hemodialysis procedure. With hemodialysis, the clearance is 62 ml / min.
The average maximum concentration of enalapril in breast milk after a single dose of 20 mg of enalapril is 1.7 mcg / l 4-6 hours after administration. The estimated maximum intake of a substance by a fully breastfed infant is 0.16% of the dose based on the mother's weight.
Indications for use
- renovascular hypertension;
- essential hypertension;
- any stage of heart failure.
In the presence of clinical manifestations of HF, Renitek is also prescribed to achieve the following goals:
- increased patient survival;
- reducing the frequency of hospitalizations associated with heart failure;
- slowing down the progression of heart failure.
In the absence of clinical symptoms of HF in patients with impaired left ventricular function, Renitek is prescribed to achieve the following goals (prevention of the development of clinically severe HF):
- reducing the frequency of hospitalizations associated with heart failure;
- slowing down the onset of clinical manifestations of heart failure.
With left ventricular dysfunction, Renitec is prescribed to achieve the following goals (prevention of coronary ischemia):
- a decrease in the frequency of hospitalizations associated with unstable angina pectoris;
- reducing the incidence of myocardial infarction.
Contraindications
Absolute:
- idiopathic / hereditary angioedema, aggravated history of angioedema associated with the use of ACE inhibitors;
- syndrome of glucose-galactose malabsorption, lactase deficiency, hereditary lactose intolerance;
- combined therapy with aliskiren-containing drugs or aliskiren in patients with diabetes mellitus / impaired renal function (GFR less than 60 ml / min / 1.73 m 2);
- age up to 18 years;
- pregnancy and lactation;
- individual intolerance to the components of the drug.
Relative (diseases / conditions in the presence of which caution is required when prescribing Renitek):
- conditions after kidney transplantation;
- bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney;
- mitral / aortic stenosis;
- hypertrophic obstructive cardiomyopathy;
- cerebrovascular disease or ischemic heart disease;
- renal failure;
- oppression of bone marrow hematopoiesis;
- hyperkalemia;
- renovascular hypertension;
- liver failure;
- combined use with potassium-sparing diuretics, potassium preparations, potassium-containing substitutes for table salt and lithium preparations;
- Low-density lipoprotein apheresis (LDL-apheresis) procedure using dextran sulfate;
- conditions that are accompanied by a decrease in the volume of circulating blood (including during dialysis, diuretic therapy, adherence to a diet with limited salt, vomiting or diarrhea);
- aggravated allergic history or a history of angioedema;
- dialysis with high-flow membranes (such as AN 69);
- systemic connective tissue diseases (scleroderma, systemic lupus erythematosus, etc.), therapy with procainamide or allopurinol, immunosuppressive therapy, or a combination of these complicating factors;
- diabetes;
- desensitization with an allergen from hymenoptera venom;
- belonging to the Negroid race;
- conditions after major surgical interventions or general anesthesia;
- age over 65.
Instructions for use of Renitek: method and dosage
Renitek tablets are taken orally. The effectiveness of therapy does not depend on food intake.
Arterial hypertension
The drug is prescribed in an initial dose of 10 (for mild disease) to 20 mg (in other cases) per day in 1 dose, but not more than 40 mg per day. The maintenance dose is 20 mg once a day.
Renovascular hypertension
The initial dose of Renitek is 5 mg or less (due to the fact that blood pressure and renal function in this group of patients may be especially sensitive to ACE inhibition). Then the dose is selected in accordance with the needs of the patient.
Typically, when taken daily, the effective dose is 20 mg per day.
Patients who received diuretic treatment shortly before starting Renitec should be careful.
Concomitant therapy of hypertension with diuretics
After taking the first dose of Renitek, arterial hypotension may develop. This effect is most likely in patients who use diuretics.
Prescribing the drug requires caution, since such patients may have sodium / fluid deficiency. Diuretics must be discontinued 2-3 days before starting Renitek use. If this is not possible, a reduced dose (5 mg or less) should be given to determine the primary effect. In the future, the dosage is selected taking into account the patient's condition.
In case of renal failure, it is necessary to increase the interval between doses of the drug and / or reduce the dose.
Initial daily dose of Renitek depending on creatinine clearance:
- 30–80 ml / min (minor disturbances): 5–10 mg;
- 10-30 ml / min (moderate disturbances): 2.5-5 mg;
- <10 ml / min (severe disorders; such patients, as a rule, are on hemodialysis): 2.5 mg on dialysis days (dose adjustment on days when hemodialysis is not performed should be carried out depending on the level of blood pressure).
HF / asymptomatic left ventricular dysfunction
The appointment of Renitek should be carried out under close medical supervision in order to establish the primary effect of the drug on blood pressure. The starting dose is 2.5 mg. The drug can be used for the treatment of HF with severe clinical manifestations in conjunction with diuretics and, if necessary, with cardiac glycosides.
In the absence of symptomatic hypotension (associated with taking Renitek) or after its appropriate correction, the dose is gradually increased to the usual maintenance dose - 20 mg in 1 or 2 doses (depending on tolerance).
Dose titration can be done over 2–4 weeks or less (if residual signs and symptoms of heart failure are present). This therapeutic regimen is effective in reducing mortality rates in patients with clinically severe HF.
Before and after starting therapy, it is necessary to carefully monitor blood pressure and renal function in patients with heart failure, since there is information about the occurrence of arterial hypotension as a result of taking Renitec, followed (which is much less common) the appearance of renal failure. In patients receiving diuretics, their dose, if possible, should be reduced before taking the drug. The development of arterial hypotension after taking the first dose of the drug does not mean that it will persist with prolonged treatment, and does not indicate the need to stop taking the drug. Serum potassium levels in the blood should also be monitored while treating Renitek.
Side effects
In general, Renitek is well tolerated. The total frequency of adverse reactions when using the drug does not exceed that when using placebo. Usually, adverse reactions are minor, temporary, and do not lead to discontinuation of therapy.
Headache and dizziness are most common. Asthenia and increased fatigue are observed in 2-3% of patients. The development of arterial hypotension, orthostatic hypotension, fainting, nausea, diarrhea, muscle cramps, skin rash and cough occurs in less than 2% of patients. There are rare reports of side effects such as renal failure, oliguria, proteinuria, and impaired renal function.
Hypersensitivity reactions appear in rare cases in the form of angioedema of the tongue, face, lips, extremities, larynx and / or glottis, in very rare cases - as intestinal angioedema.
Other side reactions (in very rare cases):
- digestive system: pancreatitis, intestinal obstruction, liver failure, dry mouth, vomiting, constipation, dyspepsia, stomatitis, anorexia, cholestatic / hepatocellular hepatitis, jaundice, abdominal pain;
- cardiovascular system: stroke or myocardial infarction, possibly secondary to severe arterial hypotension in patients at risk, Raynaud's syndrome, palpitations, chest pain, angina pectoris, rhythm disturbances;
- respiratory system: rhinorrhea, hoarseness, sore throat, pulmonary infiltrates, bronchial asthma / bronchospasm, shortness of breath;
- central nervous system: anxiety, sleep disturbances, increased nervousness, depression, dizziness, confusion, insomnia, drowsiness, paresthesia;
- skin: pemphigus, toxic epidermal necrolysis, urticaria, pruritus, baldness, increased sweating, exfoliative dermatitis, erythema polymorphism, Stevens-Johnson syndrome;
- metabolism: hypoglycemia (with diabetes mellitus during therapy with oral hypoglycemic agents or insulin);
- others: blurred vision, facial redness, impotence, taste disturbances, glossitis, tinnitus.
There is evidence of the development of a complex symptom complex, which may include some or all of the following symptoms: myositis / myalgia, vasculitis, fever, arthralgia / arthritis, serositis, increased erythrocyte sedimentation rate (ESR), a positive test for antinuclear antibodies, leukocytosis and eosinophilia. Rash, photosensitivity and other skin reactions can also occur as side reactions.
There is information about an increase in serum creatinine, the level of urea in the blood, the activity of liver enzymes and / or bilirubin in the blood serum (as a rule, they are reversible and normalize after the termination of Renitek intake). The development of hyperkalemia and hyponatremia is sometimes noted.
There is evidence of a decrease in the concentration of hematocrit and hemoglobin. There are isolated reports of thrombocytopenia, neutropenia, bone marrow suppression, and agranulocytosis.
Side effects noted as a result of post-marketing surveillance: urological infection, pneumonia, herpes zoster, upper respiratory tract infection, cardiac arrest, bronchitis, atrial fibrillation, melena, thromboembolism of the pulmonary artery branches, ataxia, hemolytic anemia, including cases of hemolysis in patients with deficiency of glucose-6-phosphate dehydrogenase. The causal relationship with the reception of Renitek has not been reliably established.
Overdose
Overdose data are limited.
The main symptoms: a marked decrease in blood pressure, which usually begins about 6 hours after taking the drug, stupor. Plasma concentration of enalaprilat in the blood, which is 100-200 times higher than the concentration observed with the use of therapeutic doses, is observed after taking 300 and 440 mg of enalapril (respectively).
Therapy: intravenous infusion with isotonic sodium chloride solution, if possible - angiotensin II infusion; provoking vomiting. Elimination of enalaprilat is possible by hemodialysis.
special instructions
The development of clinically severe arterial hypotension in patients with uncomplicated arterial hypertension is rare. During therapy, in patients with arterial hypertension, this disease often develops against the background of hypovolemia, which is associated with diuretic therapy, restriction of salt intake, in patients on hemodialysis, and also with diarrhea or vomiting. Clinically pronounced arterial hypotension can also be observed in patients with heart failure with / without renal failure. In the case of arterial hypotension, the patient must take a lying position, if necessary, physiological sodium chloride solution is injected intravenously.
When taking Renitek, transient arterial hypotension is not a contraindication to further treatment; after replenishing the volume of fluid and normalizing blood pressure, the drug can be continued. In some patients with heart failure and normal / low blood pressure, the use of Renitek can cause an additional decrease in blood pressure. Such a reaction to taking the drug is expected, and there is no need to regard it as a reason for stopping therapy. In cases where arterial hypotension becomes stable, dose reduction and / or withdrawal of the diuretic / Renitec are indicated.
In patients with a history of angioedema, which is not associated with the use of ACE inhibitors, the likelihood of its occurrence may increase with the use of Renitek. The incidence of angioedema in patients of the Negroid race is higher than in representatives of other races.
There is information about rare cases of the development of life-threatening anaphylactic reactions during hyposensitization with an allergen from the venom of Hymenoptera. Such reactions can be avoided if Renitek is temporarily canceled before the onset of hyposensitization.
There is information about the appearance of a cough during the use of the drug. In most cases, the cough is unproductive, persistent, and after the cancellation of Renitek it stops (it must be taken into account when conducting a differential diagnosis of cough).
The main risk factors for the development of hyperkalemia are renal failure, diabetes mellitus, combined use with potassium-sparing diuretics (spironolactone, triamterene or amiloride). Also, the risk increases with the use of potassium supplements and salts. It must be borne in mind that hyperkalemia can lead to serious (in some cases fatal) heart rhythm disturbances. In cases of the need for combined use with the above potassium-containing or potassium-increasing drugs, care must be taken and regular monitoring of the serum potassium content in the blood should be carried out.
Influence on the ability to drive vehicles and complex mechanisms
Due to the likelihood of dizziness (especially after taking the initial dose of Renitek in patients taking diuretics), care must be taken when driving a motor vehicle during therapy.
Application during pregnancy and lactation
Renitek is contraindicated for pregnant and lactating women.
In case of pregnancy, the drug should be stopped immediately, since its use in the II and III trimesters of pregnancy can lead to the development of diseases or the death of the fetus / newborn. Possible consequences of continuing therapy during this period: arterial hypotension, renal failure, hyperkalemia / hypoplasia of the skull, oligohydramnios (can lead to deformation of the skull, contracture of the extremities, hypoplasia of the lungs). These complications, apparently, are not observed in cases of using Renitek during the first trimester of pregnancy.
The condition of newborns whose mothers took Renitek should be carefully monitored for a decrease in blood pressure, hyperkalemia and oliguria. Enalapril, which has crossed the placenta, can be partially removed from the circulation of the newborn using peritoneal dialysis; theoretically it can be removed by exchange transfusion.
Pediatric use
Renitek tablets are not prescribed for children under 18 years of age, which is due to the lack of information confirming the effectiveness / safety of the drug.
With impaired renal function
In some patients, arterial hypotension that occurs after the start of the use of Renitec can lead to a deterioration in renal function. In some cases, acute renal failure has been reported, usually reversible.
In renal insufficiency, it may be necessary to adjust the dose and / or frequency of the drug. In some patients with bilateral renal artery stenosis or stenosis of an artery of a solitary kidney, an increase in blood urea and serum creatinine was noted. In most cases, the changes were reversible.
Sometimes, in the absence of kidney disease before starting the drug, therapy in combination with diuretics usually caused a transient and slight increase in blood urea and serum creatinine (dose reduction and / or withdrawal of Renitek / diuretic may be required).
For violations of liver function
In hepatic impairment, Renitec should be used with caution.
Use in the elderly
According to reviews, Renitek patients over 65 years of age should be prescribed with caution.
Drug interactions
With the combined use of Renitek with some drugs / substances, the following interactions may develop:
- diuretics that cause loss of potassium: the combination requires caution, therapy should be carried out with regular monitoring of serum potassium in the blood, which is associated with the likelihood of hypokalemia;
- other drugs with antihypertensive effects: summation of the effect;
- lithium salts: a decrease in the excretion of lithium by the kidneys and an increase in the likelihood of lithium intoxication (monitoring of the serum lithium level in the blood is required);
- hypoglycemic drugs (insulin, oral hypoglycemic agents): an increase in their hypoglycemic effect and an increase in the risk of hypoglycemia (most often during the first weeks of joint use, as well as in renal failure); patients with diabetes mellitus require careful monitoring of blood glucose levels, especially during the first month of combination therapy;
- gold preparations for parenteral use (sodium aurothiomalate): development in rare cases of a symptom complex, including facial flushing, arterial hypotension, vomiting and nausea;
- nonsteroidal anti-inflammatory drugs, including selective COX-2 inhibitors: a decrease in the effect of Renitek, further deterioration of renal function in patients with impaired renal function (as a rule, it is reversible).
Analogs
Renitek's analogues are: Berlipril, Renipril, Enam, Enapharm, Enalapril, Ednit, Enap.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 2.5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Renitek
According to reviews, Renitek is an affordable and effective drug. There is a convenient dosing regimen (1 time per day), a mild effect on the body, the possibility of long-term use without the need to increase the dose. In the first week of admission, minor side effects (in the form of weakness and dizziness) may be observed. With continued therapy, these symptoms go away on their own.
Price for Renitek in pharmacies
The approximate price for Renitek is:
- 14 tablets per pack (5, 10 or 20 mg, respectively) - 60-80, 70-90 or 120-140 rubles;
- 100 pieces. in a package (10 or 20 mg, respectively) - 75 or 130 rubles.
Renitek: prices in online pharmacies
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Drug name Price Pharmacy |
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Renitek 10 mg tablets 14 pcs. RUB 50 Buy |
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Renitek tab. 10mg No. 14 RUB 60 Buy |
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Renitek 20 mg tablets 14 pcs. 83 rbl. Buy |
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Renitek tab. 20mg No. 14 113 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
