Accupro pills 20mg, 30pcs

Composition

Active ingredient:  

10 mg of quinapril hydrochloride;

Auxiliary substances:

magnesium carbonate,

magnesium stearate,

lactose,

gelatin,

crospovidone,

hydroxypropylmethylcellulose,

hydroxypropylcellulose,

titanium dioxide, macrogol 400,

candelilla wax,

Opadry White OY-S-7331.

Pharmacological action

Accupro is an antihypertensive drug, an ACE inhibitor.

ACE 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 reduces vasopressor activity and aldosterone production. 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 renal vascular resistance, 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, it promotes the reverse development of myocardial hypertrophy in patients with arterial hypertension; improves blood supply to the ischemic myocardium. Increases coronary and renal blood flow. Reduces platelet aggregation.

After taking a single dose, the antihypertensive effect develops in 1 hour, reaches a maximum in 2-4 hours. The duration of action depends on the amount of the dose taken (up to 24 hours). A clinically pronounced effect develops a few weeks after the start of therapy.

Pharmacokinetics

Absorption, distribution, and metabolism

After oral use, the Cmax of quinapril in blood plasma is reached within 1 hour, quinaprilat-within 2 hours. Food intake 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 elimination of quinapril and its metabolites by the kidneys, the degree of absorption of the drug is about 60%.

Under the action of hepatic enzymes, quinapril is rapidly metabolized by cleavage of the ester group to quinaprilate (the main metabolite is the dibasic acid of quinapril), which is a powerful ACE inhibitor. About 38% of the oral dose of quinapril circulates in the blood plasma as quinaprilate.

Approximately 97% of quinapril or quinaprilate circulates in the blood plasma in protein-bound form. Quinapril and its metabolites do not cross the BBB.

Deduction

It is mainly excreted in the urine-61% (56% in the form of quinapril and quinaprilat), as well as through the intestine – 37%. T1 / 2 of quinapril from blood plasma is about 1-2 hours, quinaprilat-3 hours

. Pharmacokinetics in special clinical cases

In patients with renal insufficiency, T1 / 2 quinaprilate increases as creatinine clearance decreases.

Elimination of quinaprilate is also reduced in elderly patients (older than 65 years) and is closely correlated with impaired renal function, but in general, there are no differences in the effectiveness and safety of treatment in elderly and younger patients.

In patients with alcoholic cirrhosis of the liver, the concentration of quinaprilate decreases due to impaired deesterification of quinapril.

Indications

Arterial hypertension (in the form of monotherapy or in combination with thiazide diuretics and beta-blockers); various forms of hypertension; chronic heart failure (in combination with diuretics and/or cardiac glycosides).

Use during pregnancy and lactation

Akkupro is contraindicated during pregnancy and lactation

Contraindications

• a history of angioedema associated with treatment with ACE inhibitors, hereditary and/or idiopathic angioedema;
• childhood and adolescence to 18 years;
• pregnancy;
• lactation (breastfeeding);
• lactase deficiency, lactose intolerance syndrome glucose-galactose malabsorption;
• concurrent use with aliskiren and iliskilendirmesi drugs, with antagonists of receptors of angiotensin II, or with other drugs that inhibit the RAAS (double blockade of RAAS), in patients with diabetes mellitus or in patients with diabetes with a lesion of target organs (diabetic nephropathy), with impaired renal function (EGFR less than 60 ml/min/1.73 m 2), with hyperkalemia (>5 mmol/l), with chronic heart failure and hypertension;
• hypersensitivity to any component of the drug.

With caution, the drug should be prescribed to patients with symptomatic arterial hypotension, previously taking diuretics and following a diet with limited salt intake; with severe heart failure in patients with a high risk of severe arterial hypotension; with a decrease in BCC volume (including vomiting or diarrhea); with hyperkalemia; inhibition of bone marrow hematopoiesis; with aortic stenosis, hypertrophic obstructive cardiomyopathy, mitral stenosis; with cerebral insufficiency. blood circulation disorders, coronary heart disease, coronary insufficiency (a sharp decrease in blood pressure on the background of ACE inhibitor therapy can worsen the course of these diseases); condition after kidney transplantation, with bilateral renal artery stenosis or stenosis of the artery of a single kidney; with impaired renal function; in patients on hemodialysis (creatinine clearance less than 10 ml/min), since there are insufficient data on the use of Accupro in such patients; in severe autoimmune systemic connective tissue diseases (including SLE, scleroderma); in case of impaired liver function (especially when used simultaneously with a diuretic); in combination therapy with a potassium-sparing diuretic; in diabetes mellitus; extensive surgical interventions and general anesthesia; while taking other antihypertensive agents, as well as inhibitors of the mTOR and DPP-4 enzymes.

Side effects

From the central nervous system and peripheral nervous system:  possible dizziness, weakness, headache; rarely-paresthesia, mood and sleep disorders.

From the cardiovascular system:  hypotension is possible; rarely-tachycardia.

From the digestive system:  possible dyspeptic symptoms (including dry mouth, loss of appetite); rarely-stomatitis, abdominal pain, pancreatitis, cholestatic jaundice.

From 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).

Respiratory system disorders:  possible dry cough, bronchitis, rhinitis.

From the hematopoietic system:  rarely-neutropenia, agranulocytosis, thrombocytopenia, anemia.

From the urinary system:  kidney function may be impaired.

From the side of the reproductive system:  rarely-impotence.

Allergic reactions:  skin rash, angioedema, and other hypersensitivity reactions are possible.

Dermatological reactions:  rarely-alopecia.

Other services:  rarely-muscle spasms.

Interaction

Antihypertensive drugs, diuretics, opioid analgesics, and general anaesthetics enhance the antihypertensive effect. NSAIDs, table salt-weaken the effect.

Potassium supplements, potassium-sparing diuretics (amiloride, spironolactone, triamterene) – increase the risk of hyperkalemia. Enhances the effect of ethanol, slows down the elimination of Li+.

Increases the hypoglycemic effect of sulfonylureas and insulin derivatives. Increases the risk of leukopenia when used concomitantly with allopurinol, cytostatic agents, immunosuppressants, procainamide.

Estrogens weaken the hypotensive effect due to fluid retention. Drugs that cause bone marrow suppression increase the risk of developing neutropenia and / or agranulocytosis up to a fatal outcome.

How to take it, course of use and dosage

When conducting monotherapy for arterial hypertension, the recommended initial dose of quinapril in patients who do not receive diuretics is 10 mg or 20 mg 1 time/day.

Depending on the clinical effect, the dose can be increased to a maintenance dose of 20 mg or 40 mg / day, which is usually prescribed in 1 dose or divided into 2 parts. As a rule, the dose should be changed at intervals of 4 weeks.

In most patients, adequate blood pressure control can be achieved with long-term treatment by using the drug 1 time / day. In some patients, the dose of quinapril reached 80 mg / day.

Overdose

Symptoms: marked decrease in blood pressure, dizziness, weakness, visual disturbances.

Treatment: – symptomatic. The patient should take a horizontal position, it is advisable to conduct an intravenous infusion using 0.9% sodium chloride solution (in order to increase the BCC).

Hemodialysis and peritoneal dialysis are not effective.

Special instructions

Caution should be exercised when prescribing to patients with reduced BCC (including as a result of diuretic therapy, with limited NaCl intake, hemodialysis, diarrhea and vomiting) because of the increased risk of developing a sudden decrease in blood pressure after even the initial dose of ACE.

Transient hypotension is not a contraindication for continuing treatment with the drug after blood pressure stabilization (the dose should be reduced). In case of an excessive decrease in blood pressure, the patient is transferred to a horizontal position with a low headboard, if necessary, saline solution is infused (to increase the volume of BCC).

Prior diuretic therapy should be discontinued 2-3 days before starting treatment, except in patients with malignant or difficult-to-treat hypertension. In these patients, the use of quinapril can be started immediately, at a reduced dose, under close medical supervision (within 2 hours after use and an additional 1 hour until blood pressure stabilizes) and a careful increase in the dose.

Patients with malignant arterial hypertension or concomitant severe heart failure should start treatment in a hospital setting. Before starting therapy with ACE inhibitors, it is necessary to count the total number of white blood cells, as well as monitor the leukocyte formula 1 time per month for the first 3-6 months of treatment, and at periodic intervals of up to 1 year in patients with an increased risk of neutropenia (with impaired renal function, systemic connective tissue diseases, high-dose patients, at the first signs of infection).

Before and during treatment, it is necessary to monitor blood pressure, kidney function, K+ content in plasma, control of Hb content in peripheral blood, creatinine, urea, control of the concentration of electrolytes and “liver” enzymes in the blood. The use of AN69 dialysis membranes in combination with ACE inhibitors is not recommended (due to the possibility of developing anaphylactoid reactions in patients). Newborns who have been exposed to ACE inhibitors in utero should be closely monitored for hypotension, oliguria, and hyperkalemia.

With oliguria, it is necessary to maintain blood pressure and renal perfusion by introducing appropriate fluids and vasoconstrictors. In newborns and infants, the risk of developing oliguria and neurological disorders is associated with a decrease in renal and cerebral blood flow due to a decrease in blood pressure caused by ACE inhibitors; in this case, use at lower initial doses and careful monitoring is recommended.

Caution should be exercised when driving vehicles or performing other work that requires increased attention, as dizziness may occur, especially after the initial dose of an ACE inhibitor in patients taking diuretics.

Caution should be exercised when exercising or in hot weather due to the risk of dehydration and hypotension due to reduced fluid volume. Before surgery (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Quinapril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Heart Failure