Accupro coated pills 10mg N30
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Active ingredients
Hinapril
Release form
Pills
Composition
Active ingredient: Quinapril (Quinapril) Active ingredient concentration (mg): 10
Pharmacological effect
An antihypertensive drug, an ACE inhibitor. The ACP catalyzes the conversion of angiotensin I to angiotensin II, which has a vasoconstrictive effect and increases vascular tone, including by stimulating the production of aldosterone by the adrenal cortex. Quinapril competitively inhibits ACE activity and decreases vasopressor activity and aldosterone production. The elimination of the negative effect of angiotensin II on renin secretion by the feedback mechanism leads to an increase in plasma renin activity. At the same time, a decrease in blood pressure is accompanied by a decrease in OPSS and resistance of the renal vessels, while changes in heart rate, cardiac output, renal blood flow, glomerular filtration rate and filtration fraction are insignificant or absent. Quinapril increases exercise tolerance. With prolonged use contributes to the reverse development of myocardial hypertrophy in patients with arterial hypertension; improves blood supply to ischemic myocardium. Enhances coronary and renal blood flow. Reduces platelet aggregation. After taking a single dose, the antihypertensive effect develops after 1 hour, reaches a maximum after 2-4 hours. The duration of action depends on the size of the dose taken (up to 24 hours). A clinically pronounced effect develops several weeks after the start of therapy.
Pharmacokinetics
Absorption, distribution, metabolism After ingestion of Cmax quinapril in blood plasma is achieved within 1 hour, quinaprilat within 2 hours. Eating does not affect the degree of absorption, but may increase the time to reach the maximum concentration (fatty foods can reduce the absorption of the drug). Taking into account the removal of quinapril and its metabolites by the kidneys, the degree of absorption of the drug is about 60%. Under the action of liver enzymes, quinapril is rapidly metabolized by cleaving the ester group to quinaprilat (the main metabolite is quinapril dibasic acid), which is a powerful ACE inhibitor. About 38% of the ingested dose of quinapril circulates in the blood plasma in the form of quinaprilat. Approximately 97% of quinapril or quinaprilat circulates in the blood plasma in a protein-bound form. Quinapril and its metabolites do not penetrate through the BBB. Excretion: Excreted mainly in the urine - 61% (56% in the form of quinapril and quinaprilat), and also through the intestine - 37%.T1 / 2 quinapril from blood plasma is about 1-2 hours, hinaprilat - 3 hours. Pharmacokinetics in special clinical situations. Patients with renal insufficiency. T1 / 2 quinaprilat increases as CC decreases. Excretion of quinaprilat also decreases in elderly patients (over 65) ) and is closely correlated with impaired renal function, however, in general, differences in efficacy and safety of treatment of elderly and younger patients have not been detected. In patients with alcoholic cirrhosis of the liver, the concentration of hinaprilat decreases due to Rushen deesterification of quinapril.
Indications
Arterial hypertension: (in monotherapy or in combination with thiazide diuretics and beta-blockers). Chronic heart failure: (in combination with diuretics and / or cardiac glycosides).
Contraindications
- Hypersensitivity to any component of the drug. - Angioedema in the history of previous therapy with ACE inhibitors, hereditary and / or idiopathic angioedema. - Age up to 18 years. - Pregnancy and lactation period. - Lactase deficiency, lactose intolerance and glucose syndrome galactose malabsorption.
Precautionary measures
Do not exceed the recommended dose. With caution, you should prescribe the drug to patients with symptomatic hypotension, previously taking diuretics and following a diet with restriction of salt intake; in severe heart failure in patients with a high risk of severe arterial hypotension; with a decrease in the volume of bcc (including vomiting or diarrhea); with hyperkalemia; oppression of bone marrow hematopoiesis; with aortic stenosis, hypertrophic obstructive cardiomyopathy, mitral stenosis; with insufficiency of cerebral circulation, coronary artery disease, coronary insufficiency (a sharp decrease in blood pressure during therapy with ACE inhibitors can worsen the course of these diseases); condition after kidney transplantation, with bilateral renal artery stenosis or arterial stenosis of a single kidney; in violation of renal function; in patients on hemodialysis (CC less than 10 ml / min), because data on the use of Accupro in these patients is not enough; in severe autoimmune systemic diseases of the connective tissue (includingSLE, scleroderma); in violation of liver function (especially when used simultaneously with a diuretic); with combination therapy with potassium-sparing diuretic; diabetes; extensive surgical interventions and general anesthesia; while taking other antihypertensive drugs, as well as inhibitors of the enzymes mTOR and DPP-4.
Use during pregnancy and lactation
Precautions should be prescribed to patients with symptomatic hypotension, previously taking diuretics and following a diet with restriction of salt intake; in severe heart failure in patients with a high risk of severe arterial hypotension; with a decrease in the volume of bcc (including vomiting or diarrhea); with hyperkalemia; oppression of bone marrow hematopoiesis; with aortic stenosis, hypertrophic obstructive cardiomyopathy, mitral stenosis; with insufficiency of cerebral circulation, coronary artery disease, coronary insufficiency (a sharp decrease in blood pressure during therapy with ACE inhibitors can worsen the course of these diseases); condition after kidney transplantation, with bilateral renal artery stenosis or arterial stenosis of a single kidney; in violation of renal function; in patients on hemodialysis (CC less than 10 ml / min), because data on the use of Accupro in these patients is not enough; in severe autoimmune systemic diseases of the connective tissue (including SLE, scleroderma); in violation of liver function (especially when used simultaneously with a diuretic); with combination therapy with potassium-sparing diuretic; diabetes; extensive surgical interventions and general anesthesia; while taking other antihypertensive drugs, as well as inhibitors of the enzymes mTOR and DPP-4.
Dosage and administration
It is taken orally, without chewing, regardless of the time of eating, drinking water. Arterial hypertension Monotherapy: The recommended initial dose of the drug Accupro in patients not receiving diuretics is 10 mg 1 time per day. Depending on the clinical effect, the dose can be increased (doubled) to a maintenance dose of 20 or 40 mg / day, which is usually prescribed in 1 or 2 doses. As a rule, the dose should be changed at intervals of 4 weeks.In most patients, the use of the drug Accupro 1 time per day allows you to achieve a stable therapeutic response. The maximum daily dose is 80 mg / day. Combination with diuretics: The recommended initial dose of the drug Accupro in patients who continue to receive diuretics is 5 mg 1 time per day; subsequently, it is increased (as indicated above) until the optimum therapeutic effect is achieved (see the section “Interaction with Other Medicines”). Chronic heart failure The recommended initial dose of Accupro is 5 mg 1 or 2 times a day. After taking the drug, the patient should be under medical supervision in order to identify symptomatic arterial hypotension. In the case of good tolerability of the initial dose of the drug Accupro, it can be increased to 10-40 mg / day in 2 equal doses. Use in patients with impaired renal function Considering the clinical and pharmacokinetic data in patients with impaired renal function, the initial dose is recommended to be selected as follows: CC The recommended initial dose (ml / min) (mg) is more than 60 10 30-60 5 10-30 2.5 (1/2 tablet 5 mg) If the tolerance of the initial dose is good, then Accupro can be used 2 times a day. The dose of Accupro can be gradually, not more than once a week, increased taking into account the clinical, hemodynamic effects, and kidney function. The use in elderly patients The recommended initial dose of Accupro in elderly patients is 10 mg 1 time per day; it is subsequently increased until the optimum therapeutic effect is achieved.
Side effects
From the side of the central nervous system and peripheral nervous system: dizziness, weakness, headache are possible; rarely - paresthesia, mood and sleep disorders. From the cardiovascular system: arterial hypotension is possible; rarely, tachycardia. From the digestive system: dyspeptic symptoms are possible (including dry mouth, anorexia); rarely - stomatitis, abdominal pain, pancreatitis, cholestatic jaundice. On the side of metabolism: hyperkalemia, hyponatremia are possible; rarely - proteinuria, increased urea and creatinine levels in the blood (mainly in patients with impaired renal function). On the respiratory system: dry cough, bronchitis, rhinitis are possible. On the hematopoietic system: rarely - neutropenia, agranulocytosis, thrombocytopenia,anemia. From the urinary system: possibly impaired kidney function. From the reproductive system: rarely - impotence. Allergic reactions: skin rash, angioedema and other hypersensitivity reactions are possible. Dermatological reactions: rarely - alopecia. Other: rarely - muscle spasms .
Overdose
Symptoms: marked decrease in blood pressure, dizziness, weakness, visual disturbances. Treatment: symptomatic therapy. The patient should be placed in a horizontal position; It is advisable to / in the introduction of a 0.9% solution of sodium chloride (in order to increase the BCC). Hemodialysis and peritoneal dialysis are not effective.
Interaction with other drugs
Tetracycline and other drugs that interact with magnesium. Simultaneous use of tetracycline with quinapril was accompanied by a decrease in tetracycline absorption by about 28-37% due to the presence of magnesium carbonate as an auxiliary component of the drug. With the simultaneous appointment of quinapril and tetracycline, the possibility of such interaction should be considered. Lithium preparations In patients simultaneously receiving lithium preparations and ACE inhibitors, an increase in serum lithium concentrations and signs of lithium intoxication were observed due to increased sodium excretion. It is necessary to appoint the specified drugs at the same time carefully; the treatment shows the regular determination of lithium in the serum. Simultaneous use of diuretic can increase the risk of lithium intoxication. salts containing potassium, then they should be used carefully under the control of the content of potassium in the blood serum. Hypoglycemic drugs for taking and inside and insulin therapy, ACE inhibitors are sometimes accompanied by the development of hypoglycemia in patients with diabetes, receiving insulin or hypoglycemic drugs for oral administration.Hinapril enhances the effect of hypoglycemic drugs for ingestion and insulin. Other drugs Signs of clinically significant pharmacokinetic interaction of quinapril with propranolol, hydrochlorothiazide, digoxin or cimetidine were not detected. The use of quinapril 2 times / day did not significantly affect the anticoagulant effect of warfarin when administered once (assessed on the basis of prothrombin time). With simultaneous repeated use of atorvastatin at a dose of 10 mg with quinapril at a dose of 80 mg, there were no significant changes in the equilibrium pharmacokinetic parameters of atorvastatin. Quinapril increases the risk of developing leukopenia with simultaneous use with allopurinol, cytotoxic drugs, immunosuppressants, procainamide. Hypotensive drugs, narcotic analgesics, drugs for general anesthesia enhance the antihypertensive effect of quinapril. Estrogens, NSAIDs (including selective COX-2 inhibitors) weaken the antihypertensive effect of quinapril due to fluid retention. In addition, in elderly patients, in patients with reduced BCC (including patients receiving diuretic therapy) or in patients with impaired renal function, the simultaneous use of NSAIDs (including selective COX-2 inhibitors) with ACE inhibitors, including with quinapril, can lead to impaired renal function, including possible acute renal failure. The state of renal function in patients receiving both NSAIDs and quinapril should be monitored regularly. The use of angiotensin II receptor antagonists, ACE inhibitors or aliskiren can lead to a double blockade of RAAS activity. This effect may manifest as a decrease in blood pressure, hyperkalemia, and changes in renal function (including acute renal failure) compared with monotherapy. It is not necessary to simultaneously use quinapril with aliskiren and aliskiren containing drugs, with antagonists of angiotensin II receptors or with other drugs that inhibit PAAS (double block RAAS) in patients with diabetes mellitus or in patients with diabetes mellitus with target organ damage (diabetic nephropathy), in patients with renal impairment (GFR less 60 ml / min / 1.73 m2),in patients with hyperkalemia (more than 5 mmol / l), in patients with chronic heart failure and arterial hypertension. Drugs that inhibit bone marrow function, increase the risk of developing neutropenia and / or agranulocytosis. When ACE inhibitors and gold preparations (sodium aurothiomalate, in / in) a symptom complex is described, including facial flushing, nausea, vomiting and a decrease in blood pressure. Patients simultaneously receiving therapy with inhibitors of mTOR enzymes (for example, temsirolimus) or DP inhibitors P-4 (glyptines) or estramustine may be at greater risk of developing angioedema. Caution should be exercised while using these drugs with the drug Accupro. Ethanol (drinks containing alcohol) Ethanol enhances the antihypertensive effect of quinapril.
special instructions
In case of treatment with ACE inhibitors, cases of angioedema in the head and neck area are described, incl. and in 0.1% of patients receiving Accupro. When a guttural whistle or angioedema of the face, tongue or vocal folds appears, it is necessary to immediately stop the treatment with Accupro. The patient must be prescribed adequate treatment and observe it until the edema is relieved. Antihistamines can be used to reduce symptoms. Angioedema involving the larynx can be fatal. If edema of the tongue, vocal folds or larynx threatens the development of airway obstruction, emergency treatment is needed, including subcutaneous injection of 1: 1000 (0.3-0.5 ml) administration of epinephrine (adrenaline) solution. In cases of treatment with ACE inhibitors, angioedema . Patients had abdominal pain (with / without nausea and vomiting); in some cases without prior angioedema of the face and normal C1-esterase level. The diagnosis was established using computed tomography of the abdominal area, ultrasound or at the time of surgical intervention. Symptoms disappeared after discontinuation of ACE inhibitors. Therefore, in patients with abdominal pain, taking ACE inhibitors, when conducting a differential diagnosis, it is necessary to consider the possibility of the development of angioedema. Intestinal patients.who have a history of angioedema, not associated with taking an ACE inhibitor, may increase the risk of its development in the treatment of this group. Patients receiving ACE inhibitors during desensitizing therapy with hymenoptera may develop life-threatening anaphylactic reactions. In these patients, it was possible to avoid these reactions by temporarily canceling ACE inhibitors, but they developed again after accidental use of drugs. Anaphylactic reactions when treated with ACE inhibitors may also develop in patients who have simultaneously undergone LDL apheresis with dextran sulfate or in patients on hemodialysis using high-flow membranes such as polyacrylonitrile. Therefore, such combinations should be avoided by using either other antihypertensive drugs or alternative membranes for hemodialysis. Symptomatic arterial hypotension is rare in patients with uncomplicated arterial hypertension receiving Accupro, but it is a possible complication of therapy with ACE inhibitors in patients with reduced BCC, for example, compliance with a diet with limited consumption of table salt, hemodialysis. If symptomatic hypotension occurs, the patient should be placed and, if necessary, start / infusion of a 0.9% sodium chloride solution. Transient arterial hypotension is not a contraindication to the further use of the drug, but in such cases the dose should be reduced or the feasibility of concurrent therapy with diuretics should be evaluated. Other reasons for lowering BCC, such as vomiting or diarrhea, can also lead to a pronounced decrease in blood pressure. In such cases, patients should consult a doctor. In patients receiving diuretics, the appointment of Accupro can lead to the development of symptomatic arterial hypotension. It is advisable for such patients to temporarily stop taking diuretic 2-3 days before starting treatment with Accupro (except for patients with malignant or difficult to treat arterial hypertension). If Quinapril monotherapy does not provide a sufficient antihypertensive effect, diuretic treatment should be resumed.If it is impossible to cancel the diuretic, then Accupro is prescribed in a low initial dose. In patients with chronic heart failure who have an increased risk of severe arterial hypotension, treatment with Accupro should begin with the recommended dose under close medical supervision; Patients should be monitored during the first 2 weeks of treatment, as well as in all cases when the Accupro dose rises. Treatment of ACE inhibitors in patients with uncomplicated arterial hypertension was rarely accompanied by agranulocytosis, which was more common in patients with impaired renal function and connective tissue diseases. When treated with the drug Accupro, agranulocytosis rarely developed. When using this drug (as well as other ACE inhibitors) in patients with connective tissue diseases and / or kidney disease, the number of leukocytes in the blood should be monitored. In susceptible patients, suppression of the RAAS can lead to impaired renal function. In patients with severe chronic heart failure, in whom renal function may depend on the activity of the RAAS, treatment with ACE inhibitors, including quinapril, may be accompanied by oliguria and / or increasing azotemia and, in rare cases, acute renal failure and / or death. Antagonists use angiotensin II receptors, ACE inhibitors or aliskiren can lead to a double blockade of RAAS activity. This effect may be manifested by a decrease in blood pressure, hyperkalemia, and changes in renal function (including acute renal failure) compared with monotherapy. Blood pressure, kidney function and electrolyte levels in the blood plasma of patients taking Accupro and other drugs that affect the RAAS should be carefully monitored. The simultaneous use of PAAC-active agents and quinapril should be avoided. If it is necessary to use this combination, the ratio of the expected benefit to the possible risk of using the combination should be evaluated in each individual case and the kidney function and potassium content should be regularly monitored. In patients with chronic heart failure or arterial hypertension who have unilateral or bilateral stenosis of the renal artery when treated with ACE inhibitors in some cases, an increase in blood urea nitrogen and serum creatinine was observed. These changes were almost always reversible and disappeared after discontinuation of the ACE inhibitor and / or diuretic.In such cases, kidney function should be monitored during the first few weeks of treatment. T1 / 2 quinapril increases with decreasing CC. Patients with CC <60 ml / min should be given quinapril at a lower initial dose. In these patients, the dose should be gradually increased taking into account the therapeutic effect under the control of kidney function, although clinical studies have not shown any further deterioration in kidney function when treated with the drug. Akkpro in combination with a diuretic should be used with caution in patients with impaired function or progressive liver disease because small changes in water and electrolyte balance can cause the development of hepatic coma. ACE inhibitors, including quinapril, can increase the content of potassium in the blood serum. Accupro can reduce the hypokalemia caused by thiazide diuretics while simultaneous use. The use of the drug Accupro as part of combination therapy with potassium-sparing diuretic has not been studied. Given the risk of a further increase in serum potassium, a combination therapy with a potassium-saving diuretic should be carried out with caution, under the control of potassium in the serum. Patients with diabetes mellitus may need more careful monitoring and dose adjustment of hypoglycemic drugs for oral administration and insulin, especially the first month of treatment with an ACE inhibitor, including quinapril. When treating with an ACE inhibitor, including quinapril, cough development was noted. In the typical case, it is unproductive, persistent and passes after cessation of therapy. When differential diagnosis of cough, its possible relationship with the use of ACE inhibitors should be considered. Before surgery (including dental), the surgeon / anesthesiologist should be warned about the use of ACE inhibitors. If any symptoms of infection (eg, acute tonsillitis, fever) occur, the patient should immediately consult a doctor because they can be a manifestation of neutropenia. Effect on the ability to drive motor vehicles and control mechanisms. When using the drug Accupro, care should be taken when driving or doing other work that requires increased attention, especially at the beginning of treatment.