Equator pills 10mg + 20mg N30
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Active ingredients
Amlodipine + Lizinopril
Release form
Pills
Composition
Active ingredient: Amlodipine (Amlodipine), Lisinopril (Lisinopril) Active ingredient concentration (mg): 30
Pharmacological effect
A combined antihypertensive drug containing lisinopril and amlodipine. Lysinopril is an ACE inhibitor that reduces the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases prostaglandin synthesis. Reduces the OPSS, blood pressure, preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and an increase in myocardial tolerance to stress in patients with chronic heart failure. Expands arteries to a greater extent than veins. Some effects are due to exposure to tissue RAAS. With prolonged use, hypertrophy of the myocardium and the walls of resistive arteries is reduced. It improves blood supply to the ischemic myocardium. ACE inhibitors prolong life expectancy in patients with chronic heart failure, slow down the progression of left ventricular dysfunction in patients who have had a myocardial infarction without clinical manifestations of heart failure. With a sharp withdrawal of the drug, there is no marked increase in blood pressure. Despite the primary effect, which is manifested in the effects on the RAAS, it is also effective in hypertension with low renin activity. In addition to lowering blood pressure, lisinopril reduces albuminuria. Lisinopril does not affect the concentration of glucose in the blood of patients with diabetes mellitus and does not lead to an increase in hypoglycemia. The onset of action is 1 hour after ingestion. The maximum antihypertensive effect is determined after 6 hours and lasts for 24 hours. With arterial hypertension, the effect is observed in the first days after the start of treatment, a stable action develops after 1-2 months. Amlodipine, a slow calcium channel blocker, is a derivative of dihydropyridine. It has antianginal and antihypertensive effects. It blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (to a greater extent in vascular smooth muscle cells than in cardiomyocytes). The antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: in angina pectoris reduces the severity of myocardial ischemia; expanding peripheral arterioles, reduces the round focal disease, reduces the afterload on the heart, reduces the need for myocardium in oxygen.Expanding the coronary arteries and arterioles in the unchanged and ischemic areas of the myocardium, increases the flow of oxygen into the myocardium (especially with vasospastic stenocardia); prevents spasm of the coronary arteries (including caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, slows the development of angina pectoris and ischemic depression of the ST segment, reduces the incidence of angina attacks and consumption of nitroglycerin and other nitrates. antihypertensive effect. The antihypertensive effect is due to the direct vasodilating effect on vascular smooth muscle. In hypertension, a single dose provides a clinically significant reduction in blood pressure for 24 hours (in the position of the patient lying and standing). Orthostatic hypotension with the appointment of amlodipine is quite rare. Does not cause a decrease in exercise tolerance, left ventricular ejection fraction. Decreases the degree of hypertrophy of the left ventricular myocardium. It does not affect myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not have any adverse effect on metabolism and lipid concentration blood plasma and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout. A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours. Amlodipine + Lisinopril The combination of lisinopril with amlodipine in a single drug helps prevent the development of possible adverse effects caused by one of the active substances. Thus, the calcium channel blocker, directly expanding the arterioles, can lead to the retention of sodium and body fluids, and, therefore, can activate the RAAS. An ACE inhibitor blocks this process.
Pharmacokinetics
Lisinopril Absorption After oral administration, lisinopril is absorbed from the gastrointestinal tract, its absorption can vary from 6 to 60%. Bioavailability - 29%. Eating does not affect the absorption of lisinopril.Cmax in plasma is 90 ng / ml and is reached after 6 hours. Distribution Almost does not bind to plasma proteins. The permeability through the BBB and placental barrier is low. Metabolism Lysinopril is not metabolized in the body. Excretion Excreted in the urine unchanged, T1 / 2 - 12.6 hours. Pharmacokinetics in special clinical situations patients of young age. In patients with chronic heart failure, absorption and clearance of lisinopril are reduced. In patients with renal insufficiency, the concentration of lisinopril is several times higher than the concentration in plasma e the blood of healthy volunteers, the marked increase in time achieve Cmax in plasma and an increase in T1 / 2.Lizinopril excreted by gemodializa.AmlodipinVsasyvaniePosle oral amlodipine slowly and almost completely (90%) is absorbed from the gastrointestinal tract. The bioavailability of amlodipine is 64% -80%. Cmax in serum is observed after 6-10 hours. Eating does not affect the absorption of amlodipine. Distribution A large part of amlodipine, which is in the blood (95% -98%), is bound to plasma proteins. Css is achieved after 7-8 days of therapy. The average Vd is 20 L / kg body weight, which indicates that most of the amlodipine is in the tissues, and a smaller part is in the blood. Amlodipine penetrates through a BBB. Metabolism Amlodipine undergoes a slow but active metabolism in the liver in the absence of a significant first-pass effect. Metabolites do not have significant pharmacological activity. Excretion of 10% of amlodipine is excreted in the urine unchanged, 60% - in the form of metabolites; 20-25% - in the form of metabolites with bile through the intestines. Withdrawal has a biphasic character. T1 / 2 of the final phase 30-50 hours. Pharmacokinetics in special clinical situations in elderly patients (over 65 years of age) amlodipine excretion is delayed (T1 / 2 - 65 hours) compared with young patients, but this difference has no clinical significance. In patients with Hepatic insufficiency T1 / 2 lengthening suggests that with prolonged use cumulation of amlodipine in the body will be higher (T1 / 2 - up to 60 h). Renal failure does not have a significant effect on the kinetics of amlodipine. Hemodialysis is not removed. Amlodipine and lisinopril The interaction between the active ingredients that make up the drug is unlikely.AUC, time to reach and Cmax values in plasma, T1 / 2 do not change compared with the performance of each individual active ingredient. Eating does not affect the absorption of active substances.
Indications
Essential hypertension (in patients who are recommended combination therapy).
Contraindications
Hypersensitivity to any of the components of the Equator or to other derivatives of dihydropyridine, a history of angioedema, including caused by the use of other ACE inhibitors, hereditary or idiopathic, hemodynamically significant stenosis of the aorta or mitral valve or hypertrophic cardiomyopathy, severe arterial hypotension, cardiogenic shock, pregnancy, breastfeeding period, age up to 18 years (due to lack of data on the effectiveness and safety of the Equator in this age group).
Precautionary measures
Caution should be used in patients with bilateral renal artery stenosis or stenosis of the artery only kidneys with progressive azotemia, with azotemia, primary hyperaldosteronism, when expressed renal impairment, the condition after kidney transplantation, hyperkalemia, hepatic dysfunction, hypotension, cerebrovascular diseases (in including with cerebral circulatory failure), coronary artery disease, coronary insufficiency, SSS (severe bradycardia, tachycardia), chronic heart disease insufficiency of non-ischemic etiology of III-IV FC according to NYHA classification, with aortic stenosis, mitral stenosis, acute myocardial infarction (and within 1 month after myocardial infarction), autoimmune systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus) , in the oppression of bone marrow hematopoiesis, diabetes mellitus, a diet with restriction of salt, in hypovolemic states (including as a result of diarrhea, vomiting), in elderly patients, in hemodialysis using high GOVERNMENTAL dialysis membranes with high permeability (AN69).
Use during pregnancy and lactation
The drug is contraindicated for use in pregnancy. When diagnosing pregnancy, the drug Equator should be immediately discontinued. Lysinopril crosses the placental barrier.Acceptance of ACE inhibitors in the II and III trimesters of pregnancy has an adverse effect on the fetus (a pronounced decrease in blood pressure, renal failure, hyperkalemia, hypoplasia of the skull bones, fetal death) are possible. There is no data on the negative effect of the drug on the fetus in the case of use in the first trimester of pregnancy. It is recommended to carefully monitor newborns and infants who have undergone intrauterine effects of ACE inhibitors to timely detect a pronounced decrease in blood pressure, oliguria, hyperkalemia. The safety of using amlodipine during pregnancy has not been established, therefore its use is contraindicated in this category of patients. milk There is no evidence of the release of amlodipine in breast milk. However, it is known that other calcium channel blockers derived dihydropyridine are excreted in breast milk. The use of the drug Equator during lactation is not recommended. If necessary, the use of the drug Equator during lactation breastfeeding should be stopped.
Dosage and administration
Inside, regardless of the meal. It is recommended in cases when taking medications separately containing the active components of the Equator in the same doses does not provide adequate control of blood pressure. The daily dose for patients not taking antihypertensive drugs is 1 tab. For 2-3 days before the start of therapy, diuretic should be stopped. if such treatment is carried out. In the case when the cancellation of the diuretic is impossible, the initial dose of the Equator is 1/2 table. per day, after which a patient should be monitored for several hours due to the possible development of symptomatic hypotension. In case of heart failure and severe arterial hypertension, the maintenance dose is 1 table. In renal failure, with creatinine clearance 30-70 ml / min prescribed 1/2 of the usual initial dose, because Lisinopril is excreted by the kidneys. The maintenance dose of the Equator depends on the individual response of the patient, treatment requires regular monitoring of kidney function, the level of potassium and sodium in the blood.
Side effects
Occurring adverse reactions are usually unexpressed and transient in nature, the cancellation of treatment is required in rare cases. Side effects caused by a combination drug, occur no more often than in cases of taking each component separately. The most common are: headache (8%), dry cough (5%) and dizziness (3%). Possible: weakness, diarrhea, nausea, vomiting, orthostatic hypotension, pruritus, skin rash, swelling of the ankles of the legs, facial flushing, chest pain, arthralgia (1-3%). The frequency of other side effects is less than 1%. In case of hypersensitivity, angioedema of the face, extremities, lips, tongue, epiglottis and larynx may develop (0.1%). In such cases, you should immediately stop treatment and observe the patient until all symptoms disappear. From the laboratory indicators: hyperkalemia, increased creatinine, urea nitrogen, liver enzyme activity and blood bilirubin, especially with kidney disease, diabetes mellitus, and renovascular hypertension. hematopoietic organs: leukopenia, neutropenia, agranulocytosis (the effects of an ACE inhibitor), thrombocytopenia, erythrocytopenia, a slight decrease in concentration is possible with prolonged treatment Hemoglobin and hematocrit trauma. Other, rare side effects: Cardiovascular system: arrhythmias, heart palpitations, tachycardia, probably as a result of an excessive decrease in blood pressure in patients with a high risk of myocardial infarction, cerebrovascular stroke. intestinal, dry mouth, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, gum hyperplasia, loss of appetite. From the side of the skin: urticaria, increased sweat separation, itching, alopecia. From the urogenital system: renal dysfunction, frequent urination, oliguria, anuria, acute renal failure, uremia, proteinuria, impotence. From the immune system: syndrome with the appearance of antinuclear antibodies, accelerated ESR and arthralgia; myalgia; erythema multiforme; fever. On the CNS side: increased drowsiness, muscle fasciculation of the extremities and lips, asthenia, mood lability, confusion.
Overdose
Amlodipine Symptoms: pronounced decrease in blood pressure with possible development of reflex tachycardia and excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including with the development of shock and death). Treatment: gastric lavage, the appointment of activated carbon, maintaining cardiovascular function systems, control of functions of the cardiovascular and respiratory systems, giving the patient a horizontal position with raised legs, control of BCC and diuresis. To restore vascular tone - the use of vasoconstrictor agents (in the absence of contraindications to their use); in order to eliminate the effects of calcium channel blockade - in / in the introduction of calcium gluconate. Hemodialysis is ineffective. Lysinopril Symptoms: marked reduction in blood pressure, dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability. Treatment: gastric lavage, taking activated charcoal, giving the patient a horizontal position with elevated legs, replenishment of BCC - in / in the introduction of plasmas solutions, symptomatic therapy, control functions of the cardiovascular and respiratory systems, BCC, urea, creatinine and electrolytes in the blood serum, as well as diuresis. Lisinopril can be removed from the body through hemodialysis.
Interaction with other drugs
LisinoprilKaliyisberegayuschie diuretics (for example, spironolactone, amiloride and triamterene), dietary supplements with potassium, potassium-containing salt substitutes and other drugs that can increase the level of potassium in the blood serum (eg, heparin), can lead to hyperkalemia when combined with ACE inhibitors, especially patients with renal failure and other kidney diseases in history. When prescribing a drug that affects the concentration of potassium, simultaneously with lisinopril, the concentration of potassium in the blood serum should be monitored. Therefore, the simultaneous appointment should be carefully justified and made with extreme caution and regular monitoring of both the level of potassium in the blood serum and kidney function. Potassium-sparing diuretics can be taken in conjunction with Equator only under medical control. In the case of diuretic administration to a patient receiving Equator, the hypotensive effect is usually enhanced. It is therefore necessary with extreme caution to take the Equator in combination with diuretics.Lisinopril softens the potassium uretic effect of diuretics. With the simultaneous use of other antihypertensive drugs, the hypotensive effect of the Equator drug may be enhanced. If it is taken simultaneously with nitroglycerin, other nitrates or vasodilators, a more pronounced decrease in blood pressure can be expected. for general anesthesia, opioid analgesics may have a more pronounced decrease in blood pressure. Ethanol will increase em hypotensive effect of the drug. Allopurinol, procainamide, cytotoxic drugs or immunosuppressants (systemic corticosteroids) may increase the risk of leukopenia while being used with ACE inhibitors. It is necessary to carefully monitor the achievement of the desired effect. If you take ACE inhibitors and hypoglycemic drugs (insulin and hypoglycemic agents for oral administration) at the same time, you may increase the probability of reducing the glucose concentration in the blood and the risk of hypoglycemia. Most often this phenomenon is observed during the first week of combined treatment and in patients with renal insufficiency. With prolonged use of NSAIDs, including acetylsalicylic acid in high doses, a decrease in the effectiveness of ACE inhibitors is possible. The additive effect when taking NSAIDs and ACE inhibitors is manifested by an increase in the level of potassium in the blood serum and can lead to a deterioration in renal function. These effects are usually reversible. Very rarely, the development of acute renal failure is possible, especially in elderly patients and patients in a state of dehydration. Excretion of lithium can be slowed down during simultaneous use with ACE inhibitors and therefore lithium concentration in the blood serum should be monitored during this period. When used in combination with lithium preparations, it is possible to increase the manifestation of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). With simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate), the symptom complex, including facial flushing, nausea ,vomiting and arterial hypotension. Amlodipine Studies in elderly patients have shown that diltiazem inhibits amlodipine metabolism, probably due to inhibition of the CYP3A4 isoenzyme (plasma concentration rises by almost 50% and the effect of amlodipine increases). It is impossible to exclude the possibility that stronger inhibitors of the isoenzyme CYP3A4 (ie, ketoconazole, itraconazole, ritonavir) can increase the concentration of amlodipine in the blood plasma to a greater extent than diltiazem. Simultaneous use should be carried out with caution. If used simultaneously with inducers of CYP3A4 isoenzyme - with antiepileptic drugs (for example, carbamazepine, phenobarbital, phenytoin, fenfenitoin, primidone), rifampicin, herbal preparations, containing amber beefaulum, reduction may be applied; Clinical control was shown with possible dose adjustment of amlodipine during treatment with inducers of the CYP3A4 isoenzyme and after their withdrawal. Simultaneous use should be carried out with caution. As a monotherapy, amlodipine was well combined with thiazide and loop diuretics, general anesthesia drugs, beta adrenoblockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, digoxin, warfarin, орв vorstastin, i have no patterns, and I have no delay. hydroxide, magnesium hydroxide), simethicone, cimetidine, NSAIDs, antibiotics and oral hypoglycemic drugs. It is possible to increase antianginal and ntihypertensive action of slow calcium channel blockers when combined with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as enhancing their antihypertensive effect when used in conjunction with alpha-blockers, neuroleptics. hypertension does not affect the pharmacokinetic parameters of amlodipine. The repeated use of amlodipine in a dose of 10 mg and atorvastatin in a dose of 80 mg is not accompanied pharmacokinetic performance by a significant change atorvastatina.Protivovirusnye means (ritonavir) increase the plasma concentrations of calcium channel blockers slow, includingamlodipine. Neuroleptics and isoflurane increase the antihypertensive effect of dihydropyridine derivatives. Amlodipine does not have a significant effect on ethanol pharmacokinetics. Calcium preparations can reduce the effect of slow calcium channel blockers. When combined with amlodipine with lithium preparations, it is possible to increase the effect of neurotoxicity (acacia). tremor, tinnitus). Amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine. It does not affect the serum concentration of digoxin and its renal clearance. It does not significantly affect the effect of warfarin (prothrombin time). with estrogens, sympathomimetics. Procainamide, quinidine, and other drugs that prolong the QT interval can contribute to its significant Amlodipine has no effect on protein binding of digoxin blood, phenytoin, warfarin and indometatsina.Priem amlodipine with grapefruit juice is not suitable udlineniyu.V in vitro studies, because some patients this may lead to increased bioavailability of amlodipine, thereby increasing its antihypertensive effect.
special instructions
Arterial hypotension A pronounced decrease in blood pressure with the development of clinical symptoms can be observed in patients with reduced BCC and / or sodium content due to diuretic administration, fluid loss, or for other reasons, such as excessive sweating, prolonged vomiting and / or diarrhea. In case of arterial hypotension, the patient should be laid down and the fluid loss (intravenous infusion of a 0.9% sodium chloride solution) should be added if necessary. Preferably, the restoration of fluid and / or sodium loss was carried out before the treatment of the Equator. It is necessary to monitor blood pressure after taking the initial dose. This is especially true for patients with coronary artery disease or cerebrovascular diseases, when a pronounced decrease in blood pressure can lead to myocardial infarction or stroke. Aortic and mitral stenosis As with all vasodilators, the Equator should be used with caution in patients with left ventricular outflow tract obstruction and mitral stenosis. Kidney In some patients with arterial hypertension without pronounced manifestations of renovascular diseases, an increase in creatinine and urine levels was observed. in serum,in most cases, the minimum or transient, more pronounced, while taking ACE inhibitors and diuretic. This is most characteristic of patients with kidney disease in history. To determine the optimal maintenance dose, it is necessary to determine the dosing regimen individually, using lisinopril and amlodipine separately, with simultaneous monitoring of renal function. In the event of a decrease in kidney function, taking Equator should be discontinued and replaced with monotherapy with drugs in adequate doses. In addition, a dose reduction or diuretic withdrawal may be necessary. Angioedema The angioedema of the face, extremities, lips, tongue, vocal folds and / or larynx is registered in patients taking an ACE inhibitor, including lisinopril. In these cases, the Equator should be stopped immediately and the patient should be carefully monitored until the symptoms disappear. The swelling of the face, lips and extremities usually go away on their own, however, antihistamines should be used to reduce the severity of the symptoms. can be fatal. If you detect edema of the tongue, pharynx, or larynx, which are the cause of airway obstruction, it is necessary to urgently start emergency measures. Appropriate measures include: subcutaneous injection of 0.3-0.5 mg or slow intravenous administration of 0.1 mg 0.1% solution of epinephrine (adrenaline), followed by intravenous administration of GCS and antihistamines and simultaneous monitoring of vital functions. In patients ACE inhibitors, intestinal angioedema of the intestine was rarely seen. These patients complained of abdominal pain (with or without nausea and vomiting); in some cases, no previous edema of the face was observed, and C-1 esterase activity was within the normal range. Intestinal angioedema of the intestines was diagnosed by computed tomography of the gastrointestinal tract, or after an ultrasound examination, or during surgery, the symptoms disappeared after discontinuation of the ACE inhibitor. When conducting a differential diagnosis of abdominal pain in patients taking ACE inhibitors,intestinal angioedema of the intestinal edema should be considered. Anaphylactic reactions in patients on hemodialysis Patients who underwent hemodialysis through polyacrylonitrile membranes (for example, AN69) and who simultaneously received ACE inhibitors have reported cases of anaphylactic shock, so this combination should be avoided. Patients are advised to use either another type of dialysis membrane or a hypotensive drug of another pharmacotherapeutic group. Anaphylactic reactions in patients during LDEF apheresis Rare in patients who received ACE inhibitors during apheresis of LDL dextran sulfate, life-threatening anaphylactic reactions developed. Such reactions were prevented by discontinuing the use of ACE inhibitors before each apheresis procedure. Desensitization with wasp or bee venom Sometimes anaphylactic reactions developed in patients who took ACE inhibitors during desensitization with hymenoptera (eg wasps or bees). Such life-threatening situations can be avoided with the timely cancellation of ACE inhibitors. Hepatotoxicity In rare cases, the use of ACE inhibitors was accompanied by a syndrome that started with cholestatic jaundice or hepatitis and developed into fulminant necrosis of the liver and in several cases was fatal. The mechanism of this syndrome is unclear. In patients receiving Equator, with the development of jaundice or increased activity of liver enzymes, Equator should be canceled with subsequent monitoring of their condition. Hepatic insufficiency In patients with impaired liver function, amlodipine T1 / 2 is extended. Currently, dosing regimen recommendations have not been developed, therefore the Equator should be prescribed with caution, having previously evaluated the expected benefit and potential risk of treatment. Hematologic toxicity In rare cases, patients receiving ACE inhibitors have neutropenia, agranulocytosis, thrombocytopenia and anemia. In patients with normal renal function and in the absence of other aggravating factors, neutropenia is rare. Neutropenia and agranulocytosis are reversible and disappear after discontinuation of the ACE inhibitor.The equator should be used with extreme caution in patients with collagen vascular disease, during immunosuppressive therapy, during treatment with allopurinol or procainamide, or with a combination of these aggravating factors, especially in the presence of a previous renal dysfunction. Some of these patients developed serious infectious diseases, which in several cases were not corrected with antibiotic therapy. During treatment with the Equator, it is recommended to periodically monitor the level of white blood cells in these patients, as well as to warn them about the need to report the first signs of an infectious disease. Cough During the use of ACE inhibitors, cough was often recorded. As a rule, cough is unproductive, persistent and stopped after discontinuation of the drug. A differential diagnosis of cough should also include cough caused by the use of ACE inhibitors. Surgical intervention / general anesthesia In patients undergoing extensive surgery or during general anesthesia with drugs leading to hypotension, lisinopril can block the formation of angiotensin II after compensatory renin release. If arterial hypotension develops, probably as a result of the above mechanism, an increase in BCC can be performed. Elderly patientsPatients of advanced age with impaired renal function should be adjusted dose of the drug Equator. The risk group for the development of hyperkalemia consists of patients with renal insufficiency, diabetes, acute heart failure, dehydration, metabolic acidosis, or while taking potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or any other medical drugs that increase serum potassium. blood (for example, heparin). If necessary, simultaneous use with the above drugs should be monitored for the concentration of potassium in the blood serum. Patients with reduced body weight,patients with short stature and patients with severely impaired liver function may require a dose reduction. The equator does not have any adverse effect on the metabolism and blood plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout. body and observation at the dentist (to prevent soreness, bleeding and gingival hyperplasia). Effect on the ability to drive vehicles and control mechanisms. Apply the preparation Equator so care must be taken (risk of significant decrease in blood pressure and dizziness). Therefore, at the beginning of treatment, it is recommended to avoid driving, working with mechanisms and doing other work that requires high concentration of attention.