Accupro, 40 mg 30 pcs.

Excipients:

magnesium carbonate,

gelatin,
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Lactose,

Crosspovidone,

Magnesium stearate.

Pharmgroup:

Angiotensin-converting enzyme (ACE) inhibitor

Pharmic action:

The ACE is an enzyme that catalyzes the conversion of angiotensin I to angiotensin II, which has a vasoconstrictor effect and increases vascular tone, including by stimulating aldosterone secretion by the adrenal cortex. Quinapril competitively inhibits ACE and causes reduction of vasopressor activity and aldosterone secretion. Elimination of the negative effect of angiotensin II on renin secretion by a feedback mechanism leads to an increase in plasma renin activity. At the same time, a decrease in blood pressure (BP) is accompanied by a decrease in total peripheral vascular resistance (TPR) and renal vascular resistance, while changes in heart rate (HR), cardiac output, renal blood flow, glomerular filtration rate and filtration fraction are negligible or absent.

Hinapril increases exercise tolerance. With long-term use, it promotes inverse development of myocardial hypertrophy in patients with arterial hypertension; it improves blood supply to the ischemic myocardium. Enhances coronary and renal blood flow. Reduces platelet aggregation. Onset of action after a single dose – 1 hour, maximum – 2-4 hours, the duration of action depends on the size of the dose taken (up to 24 hours). A clinically pronounced effect occurs several weeks after the start of therapy.

Pharmacokinetics: The concentration of quinapril in blood plasma after oral administration reaches a maximum within 1 hour, quinaprilat – 2 hours. Food intake does not affect the degree of absorption, but may increase the time to reach maximum concentration (TCmax) (fatty foods may reduce absorption). Taking into account the excretion of quinapril and its metabolites by the kidneys, the degree of absorption is about 60%. Under the action of hepatic enzymes quinapril is rapidly metabolized to quinaprilate by chipping off the ester group (the main metabolite is quinapril bivalent acid), which is a potent ACE inhibitor.

About 38% of the oral dose of quinapril circulates in blood plasma as quinaprilate. The elimination half-life (T1/2) of quinapril from blood plasma is about 1 hour, of quinaprilat 3 hours. Renal excretion is 61% (56% as quinapril and quinaprilat) and intestinal excretion is 37%. T1/2 of quinapril is 1-2 hours, of quinaprilat 3 hours. Approximately 97% of quinapril and quinaprilat circulate in blood plasma in protein-bound form. Quinapril and its metabolites do not penetrate the blood-brain barrier.

In patients with renal insufficiency, the T1/2 of quinaprilat increases as creatinine clearance (CK) decreases. Quinaprilat excretion is also decreased in elderly patients (over 65 years) and closely correlates with impaired renal function, but in general there are no differences in efficacy and safety in elderly and younger patients.
In patients with alcoholic liver cirrhosis quinaprilat concentration is reduced due to impaired deetherification of quinapril.

Indications

Arterial hypertension, chronic heart failure.

Active ingredient

Composition

1 coated tablet contains 40 mg quinapril hydrochloride.

accompaniments:

magnesium carbonate,

magnesium stearate,

p> lactose,

gelatin,

crospovidone,

hydroxypropyl methylcellulose,

hydroxypropylcellulose,

titanium dioxide,

macrogol 400,

candelilla wax,

Opadry White OY-S-7331.

How to take, the dosage

In arterial hypertension monotherapy, the recommended starting dose of quinapril in patients not receiving diuretics is 10 mg or 20 mg once daily.

Depending on clinical effect, the dose may be increased to a maintenance dose of 20 mg or 40 mg/day, which is usually administered in 1 dose or divided into 2 parts.

As a rule, the dose should be changed at 4 week intervals.

In most patients, it is possible to get adequate BP control with prolonged treatment by taking the drug once daily.

In some patients, the quinapril dose has reached 80 mg/day.

Interaction

Hypotensive drugs, diuretics, opioid analgesics, drugs for general anesthesia increase the hypotensive effect. NSAIDs, table salt – weaken the effect.

Potassium preparations, potassium-saving diuretics (amiloride, spironolactone, triamterene) – increase the risk of hyperkalemia. It enhances the effect of ethanol, slows the excretion of Li+.

It increases the hypoglycemic effect of sulfonylurea derivatives, insulin.

It increases the risk of leukopenia when used concomitantly with allopurinol, cytostatics, immunosuppressants, procainamide.

Estrogens weaken the hypotensive effect due to fluid retention.

The drugs that cause bone marrow suppression increase the risk of neutropenia and/or agranulocytosis up to fatal.

Special Instructions

Caution should be exercised when prescribing in patients with decreased blood pressure (including as a result of diuretic therapy, restriction of NaCl intake, hemodialysis, diarrhea and vomiting) due to increased risk of sudden BP decrease after administration of even the initial dose of ACE.

Transient hypotension is not a contraindication to continue treatment with the drug after BP stabilization (the dose should be reduced). In case of excessive BP decrease the patient should be transferred to supine position with low head rest, if necessary, the physiological solution should be infused (to increase the blood circulation volume).

Before starting treatment it is necessary to cancel 2-3 days prior therapy with diuretics, except for patients with malignant or difficult to treat hypertension. In these patients, quinapril can be started immediately, in a reduced dose, under close medical supervision (for 2 h after administration and an additional 1 h before BP stabilizes) and cautiously increasing the dose. Patients with malignant arterial hypertension or concomitant severe heart failure should begin treatment in a hospital setting.

Before starting therapy with ACE inhibitors it is necessary to count the total number of leukocytes and to monitor the leukocyte formula once a month during the first 3-6 months of treatment, and at periodic intervals up to 1 year in patients with increased risk of neutropenia (with renal dysfunction, systemic connective tissue diseases, in those receiving high doses, at first signs of infection).

Before and during treatment it is necessary to monitor BP, renal function, plasma K+ content, control of peripheral blood Hb, creatinine, urea, control of electrolyte and “liver” enzymes concentration in blood. It is not recommended to use dialysis membranes AN69 in combination with ACE inhibitors (because of the possibility of anaphylactoid reactions in patients).

In newborns who have had intrauterine exposure to ACE inhibitors are recommended to be closely monitored for hypotension, oliguria and hyperkalemia.

In oliguria, BP and renal perfusion should be maintained by administration of appropriate fluids and vasoconstrictors. In newborns and infants, the risk of oliguria and neurological disorders is associated with decreased renal and cerebral blood flow due to the decrease in BP caused by ACE inhibitors; in this case, use at lower initial doses and close monitoring is recommended.

Caution should be exercised when driving vehicles or performing other work requiring increased attention because dizziness is possible, especially after the initial dose of ACE inhibitor in patients taking diuretics.

Perhaps caution should be exercising or in hot weather because of the risk of dehydration and hypotension due to decreased fluid volume. A surgeon/anesthesiologist should be advised of the use of ACE inhibitors before surgical procedures (including dentistry).

Contraindications

– Hypersensitivity to any component of the drug.
– Angioneurotic edema in the history as a result of previous therapy with ACE inhibitors, hereditary and/or idiopathic angioedema.
– Age under 18 years.
– Pregnancy and lactation.
– Lactase deficiency, lactose intolerance and glucose-galactose malabsorption syndrome.

With caution.

Symptomatic arterial hypotension in patients who have previously taken diuretics and are on a salt restricted diet; severe heart failure in patients at high risk of arterial hypotension; conditions accompanied with decreased circulating blood volume (CBC) (including vomiting and diarrhea); hyperkalemia; inhibition of bone marrow hematopoiesis; aortic stenosis; cerebral insufficiency, coronary heart disease, coronary insufficiency – a sharp decrease in BP during therapy with ACE inhibitors may worsen the course of these diseases; bilateral renal artery stenosis or artery stenosis of a single kidney, state after renal transplantation; renal impairment; in patients on hemodialysis (IQ less than 10 ml/min) (data on Accupro® use in such patients are insufficient); autoimmune systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma); liver dysfunction (especially in concurrent use with diuretics); in concurrent use with potassium-saving diuretics; diabetes mellitus; extensive surgical procedures and performing general anesthesia.

Side effects

CNS and peripheral nervous system disorders: dizziness, weakness, headache are possible; paresthesias, mood and sleep disorders are rare.

Cardiovascular system: arterial hypotension possible; rarely – tachycardia.

Gastrointestinal system: dyspeptic symptoms (including dry mouth, poor appetite) are possible; stomatitis, abdominal pain, pancreatitis, cholestatic jaundice are rare.

Metabolism disorders: hyperkalemia, hyponatremia; rarely – proteinuria, increased level of urea and creatinine in blood (especially in patients with renal dysfunction).

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

Hematopoietic system disorders: rarely – neutropenia, agranulocytosis, thrombocytopenia, anemia.

Urinary system disorders: possibly impaired renal function.

Reproductive system disorders: rarely – impotence.

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

Dermatological reactions: rarely – alopecia.

Others: rare – muscle cramps.

Overdose

Symptoms: marked BP decrease, dizziness, weakness, visual disturbances.

The treatment is symptomatic.

The patient should take the horizontal position, it is advisable to perform intravenous infusion with 0.9% sodium chloride solution (in order to increase the blood circulation).

Hemodialysis and peritoneal dialysis are not effective.