An effective drug quinapril for heart failure, reviews. Medicinal reference book geotar Results of drug interaction

Means "Khinapril" is a drug that helps in the normalization of blood pressure in hypertension. The medication has its own characteristics of administration, contraindications and side effects, it is taken as prescribed by the doctor.

The drug "Hinapril" is sold in pharmacies in the form of tablets. The pills have a rounded shape and a yellowish tint, they are at risk.

The active ingredient is quinapril hydrochloride. Also in the composition there are additional elements that create the shape of the drug, help the active element to be better absorbed into the blood.

pharmachologic effect

Quinapril tablets are designed to normalize blood pressure. The active ingredient provokes a decrease in the degree of vasopressor activity and aldosterone production, and also affects a person's ability to exercise. When using the drug, a reverse development of hypertrophy of the heart muscle is observed. This is quite important for people who suffer from high blood pressure.

The therapeutic effect of the drug occurs approximately 1-4 hours after the patient has taken the pill. It remains as long as the active substance is in the human body.

Indications for use

Means "Khinapril" is taken in the presence of the following indications:

  • Increased blood pressure.
  • Heart failure.

In case of heart failure, the drug is used as part of a combined treatment.

Mode of application

The drug "Hinapril" is taken orally. It is required to swallow the tablet with a sufficient amount of water. Do not chew it or grind it into powder.

Treatment is carried out, starting with the minimum dosage. If necessary, the concentration of the drug is increased. It is possible to increase the dose every 3 weeks. It is impossible to increase the dosage more often, because the therapeutic effect occurs only after 2-3 weeks after the start of therapy.

Dosage of the drug

The concentration of the active substance is selected for each patient individually. The dosage depends on the specific pathology, the presence of other diseases, the general condition of the sick person and other factors.

Arterial hypertension

If "Hinapril" is used together with diuretics, then it is required to start treatment with 5 mg per day. Gradually, you can also increase the dosage to achieve the desired therapeutic effect.

Heart failure

In case of insufficiency in the activity of the heart, it is recommended to start therapy with a small dose - 5 mg per day. If necessary, it can be increased to 40 mg per day, divided into two doses.

Use during pregnancy and breastfeeding

Women who are carrying and nursing a child are not allowed to take the medicine "Hinapril". It can adversely affect the development and health of the baby.

Reception in violation of the work of the kidneys

If the patient has problems with the work of the kidneys, it is not forbidden to take "Khinapril". However, treatment is required to be carried out strictly under medical supervision. The dosage of the drug is selected depending on the CC indicator (ml / min):

  • Over 60 - recommended dosage of 10 mg
  • From 30 to 60 - 5 mg.
  • From 10 to 30 - 2.5 mg.

If the medication is well tolerated by the patient, the dose can be increased.

Application in childhood and old age

In childhood, it is forbidden to take the remedy "Khinapril" until the age of 18. Elderly people are allowed to be treated with this medicine, but the most optimal dose for them is 10 mg per day.

Side effects

The drug "Hinapril" can cause various side effects in patients. The list of possible reactions of the body is quite extensive, because the drug can affect any internal organs and systems.

The following manifestations are possible:

  • Headache.
  • Attacks of dizziness.
  • Dry cough.
  • Fast fatiguability.
  • Runny nose.
  • Nausea, vomiting.
  • Pain syndrome in muscle tissue.
  • Sleep disorders.
  • Depressive state.
  • Paresthesia.
  • Excessive nervous excitability or, conversely, drowsiness.
  • Violation of visual function.
  • Chair disorders.
  • Soreness in the abdomen.
  • Dryness in the mouth.
  • Increased gas formation.
  • Edema of intestinal tissues.
  • Bleeding of the intestine.
  • Anemia.
  • thrombocytopenia.
  • A strong decrease in blood pressure.
  • Attacks of angina pectoris.
  • Rapid heartbeat.
  • Heart failure.
  • Allergic reaction.
  • Soreness in the chest.
  • Loss of consciousness.
  • Joint pains.
  • Kidney failure.
  • Sexual dysfunction in men.
  • Angioedema.
  • Peripheral edema.

The frequent occurrence of adverse reactions indicates that the drug is not suitable for the patient. Under no circumstances should they be tolerated. You need to contact the doctor and ask to change the remedy to an analogue or adjust the intake regimen.

Contraindications for use

The drug "Hinapril" is not allowed to be taken in the following cases:

  1. Angioedema in history.
  2. Individual intolerance to the components that make up the drug.
  3. Carrying a baby or breastfeeding.
  4. Children's age is less than 18 years.
  5. Lactose deficiency and intolerance.

You can not use the drug together with aliskiren or products containing this substance, as well as with angiotensin II receptor antagonists in the following patients:

  • People who suffer from diabetes.
  • Patients with impaired renal function.
  • Patients with hyperkalemia.
  • Persons with low blood pressure.

It is allowed to take "Hinapril", but only with extreme caution in the following cases:

  1. Arterial hypotension.
  2. Conditions that are accompanied by a strong decrease in BCC.
  3. Hyperkalemia.
  4. Deterioration of blood formation in the bone marrow.
  5. Aortic or mitral stenosis.
  6. Hypertrophic cardiomyopathy.
  7. Violation of blood flow in the brain.
  8. Cardiac ischemia.
  9. coronary insufficiency.
  10. Bilateral form of stenosis of the arteries of the kidneys.
  11. Stenosis of the artery of one kidney, provided that the second organ is removed.
  12. Failure of the functioning of the kidneys and liver.
  13. stay on hemodialysis.
  14. Autoimmune pathologies.
  15. Diabetes.

Also, with caution, take the drug with extensive surgery and the use of anesthesia.

special instructions

Treatment with the drug "Hinapril" is carried out taking into account the following rules:

  • If a patient has a failure in the water-electrolyte balance, it is necessary to first eliminate it, only then begin therapy.
  • When taken simultaneously with diuretics, it is required to reduce the dosage of "Khinapril".
  • During treatment, it is necessary to regularly monitor the readings of the tonometer in order not to miss an excessive decrease in blood pressure, which is possible when taking the medication in question.

Do not take "Hinapril" with alcohol. Ethanol aggravates the effect of the drug, so blood pressure can drop sharply and severely.

Features of interaction with other drugs

With the joint use of "Hinapril" with lithium preparations, an increase in the concentration of its active substance in the blood is observed. As a result of this, the likelihood of side effects in the patient increases significantly, because the toxic effect of the drug is enhanced.

With the simultaneous administration of "Hinapril" with hypoglycemic agents, there is a risk of developing hypoglycemia. This is also possible if the patient takes insulin together with an antihypertensive medication.

Estrogens, non-steroidal anti-inflammatory drugs help to reduce the effectiveness of "Khinapril".

Overdose

An overdose of the drug "Hinapril" is very rare. It occurs with a significant increase in the maximum allowable dosage. In case of an overdose, symptoms such as:

  • Attacks of dizziness.
  • Severe drop in blood pressure.
  • Failure of the visual organs.
  • General weakness.

In the event of an overdose, it is required to wash the stomach, take a sorbent. It is advisable to call an ambulance, because more serious therapy may be needed in a hospital setting.

Analogues and price

If necessary, the attending physician can change "Hinapril" to an analogue. You can choose a remedy with the same active substance, or you can use a different component, but with the same therapeutic effect.

The following analogues are popular:

  • Quinapril.
  • "Cordaflex".
  • "Metoprolol".

The cost of the medicine is small - about 150 rubles. Tablets are released only with a prescription from a doctor.

In order to purchase Quinapril in a pharmacy, you must present a prescription.

Storage conditions

It is necessary to store the drug "Hinapril" in a place protected from children and penetration of sunlight and moisture. The recommended storage temperature is 25 degrees. The shelf life of the drug is 3 years.

Thus, the drug "Hinapril" is used to treat arterial hypertension, as it helps in lowering pressure. It can only be taken as prescribed by a specialist.

pharmachologic effect

ACE is an enzyme that catalyzes the conversion of angiotensin I to angiotensin II, which has a vasoconstrictive effect and increases vascular tone, including by stimulating the secretion of aldosterone by the adrenal cortex. Quinapril competitively inhibits ACE and causes a decrease in vasopressor activity and aldosterone secretion.

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 (BP) is accompanied by a decrease in total peripheral vascular resistance (OPVR) and renal vascular resistance, while changes in heart rate (HR), cardiac output, renal blood flow, glomerular filtration rate and filtration fraction are insignificant or absent. .

Quinapril increases exercise tolerance. With prolonged use, it contributes to the regression of myocardial hypertrophy in patients with arterial hypertension; improves blood supply to ischemic myocardium. Enhances coronary and renal blood flow. Reduces platelet aggregation.

The onset of action after taking a single dose - after 1 hour, 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 a few weeks after the start of therapy.

Pharmacokinetics

The concentration of quinapril in the blood plasma after oral administration reaches a maximum within 1 hour, quinapril -2 hours. Eating does not affect the degree of absorption, but may increase the time to reach the maximum concentration (T max) (fatty food can reduce the rate and degree of absorption of quinapril) . Taking into account the excretion of quinapril and its metabolites by the kidneys, the degree of absorption is approximately 60%. Under the action of "liver" enzymes, quinapril is rapidly metabolized to quinapril by cleavage of the ester group (the main metabolite is the dibasic acid of quinapril), which is an ACE inhibitor. Approximately 38% of an oral dose of quinapril circulates in plasma as quinapril. The half-life (T 1 / 2) of quinapril from blood plasma is about 1-2 hours, quinaprilata - 3 hours. Excreted by the kidneys - 61% (56% in the form of quinapril and quinaprilata) and through the intestines - 37%. Approximately 97% of quinapril and quinaprilate circulate in the blood plasma in protein-bound form. Quinapril and its metabolites do not cross the blood-brain barrier.

In patients with renal insufficiency, T 1/2 of hinaprilat increases as creatinine clearance (CC) decreases. Quinaprilat excretion also decreases in elderly patients (over 65 years of age) and closely correlates with impaired renal function, however, in general, no differences in the efficacy and safety of treatment in elderly and younger patients have been identified.

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

Indications

- arterial hypertension (in monotherapy or in combination with thiazide diuretics and beta-blockers);

- chronic heart failure (as part of combination therapy).

Dosing regimen

It is taken orally, without chewing, regardless of the time of the meal, washed down with water.

Arterial hypertension:

Monotherapy: The recommended initial dose of Quinapril-SZ in patients not receiving diuretics is 10 mg 1 time per day. Depending on the clinical effect, the dose can be increased (doubling) 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 Quinapril-SZ 1 time per day allows you to achieve a stable therapeutic response. The maximum daily dose is 80 mg/day.

With simultaneous use with diuretics: the recommended initial dose of the drug Quinapril-SZ in patients who continue to take diuretics is 5 mg 1 time per day; subsequently, it is increased (as indicated above) until the optimal therapeutic effect is achieved (see the section "Interaction with other drugs").

Chronic heart failure

After taking the drug, the patient should be under medical supervision in order to detect symptomatic arterial hypotension. In the case of good tolerance of the initial dose of the drug Quinapril-SZ, it can be increased to 10-40 mg / day divided into 2 doses.

Based on clinical and pharmacokinetic data in patients with impaired renal function the initial dose is recommended to be selected as follows:

If the tolerance of the initial dose is good, then the drug Quinapril-SZ can be used 2 times / day. The dose of the drug Khinapril-SZ can be gradually increased, not more than once a week, taking into account the clinical, hemodynamic effects, as well as kidney function.

Side effect

Adverse events with the use of quinapril are usually mild and transient. The most commonly reported headache (7.2%), dizziness (5.5%), cough (3.9%), fatigue (3.5%), rhinitis (3.2%), nausea and/or vomiting (2.8%) and myalgia (2.2%) . It should be noted that in a typical case, the cough is non-productive, persistent and disappears after treatment is stopped.

The frequency of cases of withdrawal of quinapril as a result of side effects was observed in 5.3% of cases.

Below is a list of adverse reactions distributed by organ systems and frequency of occurrence (classification of the World Health Organization):

Very often - more than 1/10; often - from more than 1/100 to less than 1/10; infrequently - from more than 1/1000 to less than 1/100; rarely - from more than 1/10000 to less than 1/1000; very rarely - from less than 1/10000, including individual messages.

From the nervous system: often - headache, dizziness, insomnia, paresthesia, increased fatigue; infrequently - depression, irritability, drowsiness, vertigo.

From the digestive tract: often - nausea and / or vomiting, diarrhea, dyspepsia, abdominal pain. Uncommon: dryness of the mucous membrane of the mouth or throat, flatulence, pancreatitis*, angioedema of the intestine, gastrointestinal bleeding; rarely - hepatitis.

General disorders and disorders at the injection site: infrequently - edema (peripheral or generalized), malaise, viral infections.

From the circulatory and lymphatic systems: infrequently - hemolytic anemia *, thrombocytopenia *.

From the side of the cardiovascular system: often - a pronounced decrease in blood pressure; infrequently - angina pectoris, palpitations, tachycardia, heart failure, myocardial infarction, stroke, increased blood pressure, cardiogenic shock, postural hypotension *, syncope *, symptoms of vasodilation.

From the respiratory system, chest organs and mediastinum: often - cough, dyspnea, pharyngitis, chest pain.

From the skin and subcutaneous tissues: infrequently - alopecia*, exfoliative dermatitis*, increased sweating, pemphigus*, photosensitivity reactions*, pruritus, rash.

From the side of the musculoskeletal and connective tissue: often - back pain; infrequently - arthralgia.

From the side of the kidneys and urinary tract: infrequently - urinary tract infections, acute renal failure.

From the genitals and mammary gland: infrequently - a decrease in potency.

From the side of the organ of vision: infrequently - visual impairment.

From the immune system: infrequently - anaphylactic reactions *, rarely - angioedema.

Others: rarely - eosinophilic pneumonitis.

Laboratory indicators: very rarely noted agranulocytosis and neutropenia, although a causal relationship with the use of quinapril has not yet been established.

Hyperkalemia:(see "Special Instructions").

Creatinine and blood urea nitrogen: an increase (more than 1.25 times compared with the upper limit of the norm) in the concentration of creatinine in the blood serum and blood urea nitrogen was observed in 2% and 2% of patients receiving quinapril monotherapy, respectively. The likelihood of an increase in these indicators in patients receiving diuretics at the same time is higher than with the use of quinapril alone. With further therapy, the indicators often return to normal.

* - less frequent adverse events or noted during post-marketing studies.

Contraindications for use

- hypersensitivity to any component of the drug;

- angioedema in history as a result of previous therapy with AG1F inhibitors, hereditary and / or idiomatic angioedema;

- age up to 18 years;

- pregnancy and breastfeeding period;

- lactase deficiency, lactose intolerance and glucose-galactose malabsorption syndrome;

- simultaneous use with aliskiren and aliskiren-containing agents or with angiotensin II receptor antagonists (ARA II) or with other drugs that inhibit the renin-angiotensin-aldosterone system (RAAS) (double blockade of RA AS):

In patients with diabetes mellitus or in patients with diabetes mellitus with damage to target organs (diabetic nephropathy);

In patients with impaired renal function (glomerular filtration rate (GFR) less than 60 ml / min / 1.73 m 2);

In patients with hyperkalemia (more than 5 mmol / l);

In patients with chronic heart failure and arterial hypotension.

Carefully: symptomatic arterial hypotension in patients who have previously taken diuretics and are on a diet with limited salt intake; severe heart failure in patients at high risk of arterial hypotension; severe chronic heart failure; conditions accompanied by a decrease in circulating blood volume (BCC) (including vomiting and diarrhea); hyperkalemia; oppression of bone marrow hematopoiesis; aortic stenosis, hypertrophic obstructive cardiomyopathy, mitral stenosis; cerebrovascular insufficiency, coronary heart disease, coronary insufficiency - a sharp decrease in blood pressure during therapy with ACE inhibitors can worsen the course of these diseases; bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, condition after kidney transplantation; impaired renal function; in patients on hemodialysis (CC less than 10 ml / min) (data on the use of quinapril in such patients is not enough); autoimmune systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma); abnormal liver function (especially when used simultaneously with diuretics); when used simultaneously with potassium-sparing diuretics; diabetes; major surgery and general anesthesia; concomitant use of other antihypertensive drugs, as well as inhibitors of mTOR and DPP-4 enzymes.

Use during pregnancy and lactation

The use of the drug Quinapril-SZ is contraindicated during pregnancy, in women planning a pregnancy, as well as in women of reproductive age who do not use reliable methods of contraception.

Women of reproductive age taking Quinapril-SZ should use reliable methods of contraception.

When diagnosing pregnancy, the drug Quinapril-SZ should be discontinued as early as possible.

The use of ACE inhibitors during pregnancy is accompanied by an increased risk of developing abnormalities in the cardiovascular and nervous systems of the fetus. In addition, against the background of taking ACE inhibitors during pregnancy, cases of oligohydramnios, premature births, the birth of children with arterial hypotension, kidney pathology (including acute renal failure), hypoplasia of the bones of the skull, contractures of the limbs, craniofacial deformities, pulmonary hypoplasia, delayed intrauterine development, open ductus arteriosus, as well as cases of intrauterine death of the fetus and death of the newborn. Often, oligohydramnios is diagnosed after the fetus has been irreversibly damaged.

Neonates exposed to ACE inhibitors in utero should be monitored for hypotension, oliguria, and hyperkalemia. When oliguria appears, blood pressure and renal perfusion should be maintained.

The drug Quinapril-SZ should not be prescribed during breastfeeding due to the fact that ACE inhibitors, including quinapril, pass into breast milk to a limited extent. Given the possibility of developing serious adverse events in a newborn, the drug Quinapril-SZ must be discontinued during lactation or breastfeeding should be stopped.

Use in children

Contraindicated in children and adolescents under 18 years of age.

Overdose

Symptoms: pronounced decrease in blood pressure, dizziness, weakness, visual impairment.

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

drug interaction

Tetracycline and other drugs that interact with magnesium: the simultaneous use of tetracycline with quinapril reduces the absorption of tetracycline by about 28-37% due to the presence of magnesium carbonate as an auxiliary component of the drug. With simultaneous use, the possibility of such an interaction should be taken into account. Lithium: in patients who simultaneously received lithium preparations and ACE inhibitors, an increase in the content of lithium in the blood serum and signs of lithium intoxication due to increased sodium excretion were observed. Use of these drugs at the same time should be done with caution; during treatment, regular determination of the content of lithium in the blood serum is shown. Concomitant use of diuretics may increase the risk of lithium intoxication.

Diuretics: with the simultaneous use of quinapril with diuretics, an increase in the antihypertensive effect is noted (see section "Special Instructions").

Drugs that increase the content of potassium in the blood serum: if a patient receiving quinapril is shown potassium-sparing diuretics (for example, spironolactone, triamterene or amiloride), potassium preparations and salt substitutes containing potassium, then they should be used carefully under the control of serum potassium.

Ethanol (drinks containing alcohol): ethanol enhances the antihypertensive effect of quinapril.

Oral hypoglycemic agents and insulin: therapy with ACE inhibitors is sometimes accompanied by the development of hypoglycemia in patients with diabetes mellitus receiving insulin or oral hypoglycemic agents. Quinapril enhances the effect of oral hypoglycemic agents and insulin.

Other drugs: there were no signs of a clinically significant pharmacokinetic interaction of quinapril with propranolol, hydrochlorothiazide, digoxin or cimetidine. The use of hinapril 2 times a day did not significantly affect the anticoagulant effect of warfarin with its single use (estimated 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 did not lead to significant changes in the equilibrium pharmacokinetic parameters of atorvastatin.

Quinapril increases the risk of developing leukopenia when used simultaneously with allopurinol, cytostatic agents, immunosuppressants, procainamide.

Antihypertensive drugs, narcotic analgesics, drugs for general anesthesia enhance the antihypertensive effect of quinapril.

Estrogens, non-steroidal anti-inflammatory drugs (NSAIDs) (including selective inhibitors of cyclooxygenase-2 (COX-2)) 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 NG1VP (including selective COX-2 inhibitors), with ACE inhibitors, including quinapril, may lead to deterioration of renal function, including possible acute renal failure. The state of kidney function should be regularly monitored in patients receiving both NSAIDs and quinapril.

The use of ARA II, 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.

Quinapril should not be used simultaneously with aliskiren and aliskiren-containing agents or with ARA II or other drugs that inhibit the RAAS (double blockade of the RAAS):

- in patients with diabetes mellitus or in patients with diabetes mellitus with damage to the target organs (diabetic nephropathy);

- in patients with impaired renal function (glomerular filtration rate (GFR) less than 60 ml / min / 1.73 m 2);

- in patients with hyperkalemia (more than 5 mmol / l);

- in patients with chronic heart failure and arterial hypertension.

Drugs that cause bone marrow suppression increase the risk of developing neutropenia and / or agranulocytosis.

With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate, intravenously), a symptom complex is described, including facial flushing, nausea, vomiting, and a decrease in blood pressure.

Patients concomitantly receiving therapy with mTOR enzyme inhibitors (eg, temsirolimus) or DPP-4 inhibitors (sitagliptin, vildagliptin, alogliptin, saxagliptin, linagliptin) or estramustine may be at greater risk of developing angioedema. Caution should be exercised while using these drugs with the drug Quinapril-SZ.

Terms of dispensing from pharmacies

On prescription.

Terms and conditions of storage

Store in a dry, dark place and out of the reach of children, at a temperature not exceeding 25 °C.

Shelf life - 3 years.

Application for violations of liver function

Take with caution in case of impaired liver function.

Application for violations of kidney function

Taking into account clinical and pharmacokinetic data in patients with impaired renal function, it is recommended to select the initial dose according to the formula (see section "Dosage regimen").

special instructions

In the treatment of ACE inhibitors, cases of angioedema in the head and neck are described, including in 0.1% of patients treated with quinapril. If a laryngeal whistle or angioedema of the face, tongue, or vocal folds occurs, quinapril should be discontinued immediately. The patient should be given adequate treatment and observed until the symptoms of edema regress. Antihistamines may be used to reduce symptoms. Angioedema involving the larynx can be fatal. If swelling of the tongue, vocal folds, or larynx threatens to develop airway obstruction, adequate emergency therapy is necessary, including subcutaneous administration of a 1:1000 (0.3-0.5 ml) solution of epinephrine (adrenaline).

In the treatment of ACE inhibitors, cases of angioedema of the intestine are also described. Patients reported abdominal pain (with/without nausea or vomiting); in some cases without previous angioedema of the face and normal C1-esterase activity. Diagnosis was established by computed tomography of the abdominal region, ultrasound, or at the time of surgery. Symptoms disappeared after discontinuation of ACE inhibitors. Therefore, in patients with abdominal pain taking ACE inhibitors, when establishing a differential diagnosis, it is necessary to take into account the possibility of developing angioedema of the intestine.

Patients with a history of angioedema unrelated to an ACE inhibitor may be at an increased risk of developing it when treated with this group of drugs.

Life-threatening anaphylactoid reactions may develop in patients receiving ACE inhibitors during desensitization therapy with hymenoptera venom. By temporarily stopping the use of ACE inhibitors, these reactions could be avoided, but they reappeared when these drugs were accidentally taken.

Anaphylactoid reactions can also develop with the use of ACE inhibitors in patients undergoing low-density lipoprotein apheresis by absorption with dextran sulfate or in patients undergoing hemodialysis using high-flow membranes such as polyacrylonitrile (for example, AN69). Therefore, such combinations should be avoided by using either other antihypertensive drugs or alternative hemodialysis membranes. Symptomatic arterial hypotension is rare in the treatment of quinapril in patients with uncomplicated arterial hypertension, however, it can develop as a result of therapy with ACE inhibitors in patients with reduced BCC, for example, when following a diet with limited salt intake, hemodialysis. In the event of symptomatic arterial hypotension, it is necessary to carry out symptomatic therapy (the patient should take a horizontal position and, if necessary, give him an intravenous infusion using 0.9% sodium chloride solution). Transient arterial hypotension is not a contraindication to further use of the drug, however, in such cases, its dose should be reduced or the advisability of simultaneous therapy with diuretics should be evaluated.

Other causes of a decrease in 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 use of quinapril can also lead to the development of symptomatic arterial hypotension. It is advisable for such patients to temporarily stop taking the diuretic 2-3 days before the start of treatment with quinapril, except for patients with malignant or difficult-to-treat arterial hypertension. If monotherapy with quinapril does not provide the desired therapeutic effect, then diuretic treatment should be resumed. If it is impossible to cancel the diuretic, then quinapril is used at a low initial dose.

In patients with chronic heart failure who have an increased risk of severe arterial hypotension, treatment with quinapril should be started at the recommended dose under close medical supervision; patients should be observed during the first two weeks of treatment, as well as in all cases when the dose of quinapril is increased.

When treated with ACE inhibitors, patients with uncomplicated arterial hypertension rarely developed agraulocytosis, which was more common in patients with impaired renal function and connective tissue diseases. In the treatment of quinapril, agranulocytosis developed rarely. When using quinapril (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 RAAS activity can lead to impaired renal function. In patients with severe chronic heart failure, in whom renal function may depend on RAAS activity, treatment with ACE inhibitors, including quinapril, may be accompanied by oliguria and / or progressive azotemia, and in rare cases, acute renal failure and / or death. The use of ARA II, 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, renal function and plasma electrolytes should be carefully monitored in patients taking quinapril and other drugs that affect the RAAS. The simultaneous use of RAAS-active agents and quinapril should be avoided. If it is necessary to use this combination, it is necessary to evaluate the ratio of the expected benefit to the possible risk of using the combination in each individual case and regularly monitor kidney function and potassium levels.

In patients with chronic heart failure or arterial hypertension with unilateral or bilateral renal artery stenosis, in the treatment of ACE inhibitors, in some cases, an increase in the concentration of urea nitrogen in the blood 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, during the first few weeks of treatment, renal function should be monitored.

The half-life of hinaprilat increases with a decrease in CC. In patients with CC less than 60 ml / min, quinapril should be used at a lower initial dose. In such patients, the dose of the drug should be increased taking into account the therapeutic effect, with regular monitoring of renal function, although in clinical studies there was no further deterioration in renal function during treatment with the drug.

Quinapril in combination with diuretics should be used with caution in patients with impaired function or progressive liver disease, since small changes in the water and electrolyte balance can cause the development of hepatic coma.

ACE inhibitors, including quinapril, may increase serum potassium levels.

Quinapril can reduce hypokalemia caused by thiazide diuretics when used simultaneously. The use of quinapril in combination therapy with potassium-sparing diuretics has not been studied. Given the risk of a further increase in serum potassium, combination therapy with potassium-sparing diuretics should be carried out with caution, under the control of serum potassium.

Patients with diabetes mellitus may require more careful monitoring and dose adjustment of oral hypoglycemic agents and insulin, and glycemic control, especially during the first month of therapy with an ACE inhibitor, including quinapril.

In the treatment of ACE inhibitors, including quinapril, the development of cough was noted. It is typically non-productive, persistent, and resolves upon discontinuation of therapy. In the differential diagnosis of cough, its possible association with ACE inhibitors should be taken into account.

Before surgery (including dentistry), it is necessary to warn the surgeon / anesthesiologist about the use of ACE inhibitors.

If any symptoms of infection (eg, acute tonsillitis, fever) appear, the patient should immediately consult a doctor, as they may be a manifestation of neutropenia.

Influence on the ability to drive vehicles and control mechanisms

When using the drug Quinapril-SZ, care should be taken when driving vehicles or performing other work that requires increased attention, especially at the beginning of treatment, due to the risk of arterial hypotension and dizziness.

  • Tablets, film-coated, yellow, round, biconvex. On a transverse section, the core of the tablet is white or almost white.

Pharmacokinetics

The concentration of quinapril in the blood plasma after oral administration reaches a maximum within 1 hour, quinapril - 2 hours. Eating does not affect the degree of absorption, but may increase the time to reach the maximum concentration (TCmax) (fatty food can reduce the speed and degree of absorption of quinapril). Taking into account the excretion of quinapril and its metabolites by the kidneys, the degree of absorption is approximately 60%. Under the action of "liver" enzymes, quinapril is rapidly metabolized to quinapril by cleavage of the ester group (the main metabolite is the dibasic acid of quinapril), which is an ACE inhibitor. Approximately 38% of an oral dose of quinapril circulates in plasma as quinapril. The half-life (T1 / 2) of quinapril from blood plasma is about 1-2 hours, quinaprilata - 3 hours. Excreted by the kidneys - 61% (56% in the form of quinapril and quinaprilata) and through the intestines - 37%. Approximately 97% of quinapril and quinaprilate circulate in the blood plasma in protein-bound form. Quinapril and its metabolites do not cross the blood-brain barrier. In patients with renal insufficiency, T1 / 2 of quinaprilata increases as creatinine clearance (CC) decreases. Quinaprilat excretion also decreases in elderly patients (over 65 years of age) and closely correlates with impaired renal function, however, in general, no differences in the efficacy and safety of treatment in elderly and younger patients have been identified. In patients with alcoholic cirrhosis of the liver, the concentration of quinapril is reduced due to impaired deesterification of quinapril.

Special conditions

in 0.1% of patients treated with quinapril. If a laryngeal whistle or angioedema of the face, tongue, or vocal folds occurs, quinapril should be discontinued immediately. The patient should be given adequate treatment and observed until the symptoms of edema regress. Antihistamines may be used to reduce symptoms. Angioedema involving the larynx can be fatal. If swelling of the tongue, vocal folds or larynx threatens to develop airway obstruction, adequate emergency therapy is necessary, including subcutaneous administration of a 1:1000 (0.3-0.5 ml) solution of epinephrine (adrenaline). In the treatment of ACE inhibitors, cases of angioedema of the intestine are also described. Patients reported abdominal pain (with/without nausea or vomiting); in some cases without previous angioedema of the face and normal C1-esterase activity. Diagnosis was established by computed tomography of the abdominal region, ultrasound, or at the time of surgery. Symptoms disappeared after discontinuation of ACE inhibitors. Therefore, in patients with abdominal pain taking ACE inhibitors, when establishing a differential diagnosis, it is necessary to take into account the possibility of developing angioedema of the intestine. Patients with a history of angioedema unrelated to an ACE inhibitor may be at an increased risk of developing it when treated with this group of drugs. Life-threatening anaphylactoid reactions may develop in patients receiving ACE inhibitors during desensitization therapy with hymenoptera venom. By temporarily stopping the use of ACE inhibitors, these reactions could be avoided, but they reappeared when these drugs were accidentally taken. Anaphylactoid reactions may also develop with the use of ACE inhibitors in patients undergoing low-density lipoprotein apheresis by absorption with dextran sulfate or in patients undergoing hemodialysis using high-flow membranes such as polyacrylonitrile (eg, AN69). Therefore, such combinations should be avoided by using either other antihypertensive drugs or alternative hemodialysis membranes. Symptomatic arterial hypotension is rare in the treatment of quinapril in patients with uncomplicated arterial hypertension, however, it can develop as a result of therapy with ACE inhibitors in patients with reduced BCC, for example, when following a diet with limited salt intake, hemodialysis. In the event of symptomatic arterial hypotension, it is necessary to carry out symptomatic therapy (the patient should take a horizontal position and, if necessary, give him an intravenous infusion using 0.9% sodium chloride solution). Transient arterial hypotension is not a contraindication to further use of the drug, however, in such cases, its dose should be reduced or the advisability of simultaneous therapy with diuretics should be evaluated. Other causes of a decrease in 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 use of quinapril can also lead to the development of symptomatic arterial hypotension. It is advisable for such patients to temporarily stop taking the diuretic 2-3 days before the start of treatment with quinapril, except for patients with malignant or difficult-to-treat arterial hypertension. If monotherapy with quinapril does not provide the desired therapeutic effect, then diuretic treatment should be resumed. If it is impossible to cancel the diuretic, then quinapril is used at a low initial dose. In patients with chronic heart failure who have an increased risk of severe arterial hypotension, treatment with quinapril should be started at the recommended dose under close medical supervision; patients should be observed during the first two weeks of treatment, as well as in all cases when the dose of quinapril is increased. When treated with ACE inhibitors, patients with uncomplicated arterial hypertension rarely developed agranulocytosis, which was more common in patients with impaired renal function and connective tissue diseases. In the treatment of quinapril, agranulocytosis developed rarely. When using quinapril (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 RAAS activity can lead to impaired renal function. In patients with severe chronic heart failure, in whom renal function may depend on RAAS activity, treatment with ACE inhibitors, including quinapril, may be accompanied by oliguria and / or progressive azotemia, and in rare cases, acute renal failure and / or death. The use of ARA II, 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, renal function and plasma electrolytes should be carefully monitored in patients taking quinapril and other drugs that affect the RAAS. The simultaneous use of RAAS-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 assessed in each individual case and the kidney function and potassium content should be regularly monitored. In patients with chronic heart failure or arterial hypertension with unilateral or bilateral renal artery stenosis, in the treatment of ACE inhibitors, in some cases, an increase in the concentration of urea nitrogen in the blood 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, during the first few weeks of treatment, renal function should be monitored. The half-life of hinaprilat increases with a decrease in CC. In patients with CC less than 60 ml / min, quinapril should be used at a lower initial dose. In such patients, the dose of the drug should be increased taking into account the therapeutic effect, with regular monitoring of renal function, although in clinical studies there was no further deterioration in renal function during treatment with the drug. Quinapril in combination with diuretics should be used with caution in patients with impaired function or progressive liver disease, since small changes in the water and electrolyte balance can cause the development of hepatic coma. ACE inhibitors, including quinapril, may increase serum potassium levels. Quinapril can reduce hypokalemia caused by thiazide diuretics when used simultaneously. The use of quinapril in combination therapy with potassium-sparing diuretics has not been studied. Given the risk of a further increase in serum potassium, combination therapy with potassium-sparing diuretics should be carried out with caution, under the control of serum potassium. Patients with diabetes mellitus may require more careful monitoring and dose adjustment of oral hypoglycemic agents and insulin, and glycemic control, especially during the first month of therapy with an ACE inhibitor, including quinapril. In the treatment of ACE inhibitors, including quinapril, the development of cough was noted. It is typically non-productive, persistent, and resolves upon discontinuation of therapy. In the differential diagnosis of cough, its possible association with ACE inhibitors should be taken into account. Before surgery (including dentistry), it is necessary to warn the surgeon / anesthesiologist about the use of ACE inhibitors. If any symptoms of infection (eg, acute tonsillitis, fever) appear, the patient should immediately consult a doctor, as they may be a manifestation of neutropenia. Influence on the ability to drive vehicles and control mechanisms When using the drug Quinapril-SZ, care should be taken when driving vehicles or performing other work that requires increased attention, especially at the beginning of treatment, due to the risk of arterial hypotension and dizziness.

Compound

  • active substance: quinapril hydrochloride - 10.832 mg
  • in terms of quinapril - 10 mg;
  • excipients (core): lactose monohydrate (milk sugar) - 46.168 mg; magnesium hydroxycarbonate pentahydrate (magnesium carbonate basic water) - 125.0 mg; croscarmellose sodium (primellose) - 5.0 mg; povidone (medium molecular weight polyvinylpyrrolidone) - 10.0 mg; colloidal silicon dioxide (aerosil) - 1.0 mg; magnesium stearate - 2.0 mg;
  • excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 2.4 mg; talc - 0.888 mg; titanium dioxide E 171 -
  • 1.3122 mg; macrogol (polyethylene glycol 3350) - 1.212 mg; aluminum varnish based on quinoline yellow dye - 0.1806 mg; aluminum varnish based on sunset yellow dye - 0.0042 mg; iron dye oxide (II) yellow - 0.0018 mg; aluminum varnish based on indigo carmine dye - 0.0012 mg);

Quinapril indications for use

  • Arterial hypertension
  • (in monotherapy or in combination with thiazide diuretics and beta-blockers).
  • Chronic heart failure
  • (as part of combination therapy).

Quinapril contraindications

  • Hypersensitivity to any component of the drug.
  • Angioedema in history as a result of previous therapy with ACE inhibitors, hereditary and / or idiopathic angioedema.
  • Age up to 18 years.
  • Pregnancy and the period of breastfeeding.
  • Lactase deficiency, lactose intolerance and glucose-galactose malabsorption syndrome.
  • Simultaneous use with aliskiren and aliskiren-containing agents or with angiotensin II receptor antagonists (APA II) or with other drugs that inhibit the renin-angiotensin-aldosterone system (RAAS) (double blockade of the RAAS):
  • in patients with diabetes mellitus or in patients with diabetes mellitus with damage to target organs (diabetic nephropathy);
  • in patients with impaired renal function (glomerular filtration rate (GFR) less than 60 ml / min / 1.73 m2);
  • in patients with hyperkalemia (more than 5 mmol / l);
  • in patients with chronic heart failure and arterial hypotension.
  • Carefully
  • Symptom

Quinapril dosage

  • 10 mg

Quinapril side effects

  • Adverse events with the use of quinapril are usually mild and transient. The most common headache
  • (7.2%), dizziness (5.5%), cough (3.9%), fatigue (3.5%), rhinitis (3.2%), nausea and/or vomiting (2.8% ) and myalgia (2.2%). It should be noted that in a typical case, the cough is non-productive, persistent and disappears after treatment is stopped.
  • The frequency of cases of withdrawal of quinapril as a result of side effects was observed in 5.3% of cases.
  • Below is a list of adverse reactions distributed by organ systems and frequency of occurrence (classification of the World Health Organization):
  • very often - more than 1/10,
  • often - from more than 1/100 to less than 1/10,
  • infrequently - from more than 1/1000 to less than 1/100,
  • rarely - from more than 1/10000 to less than 1/1000,
  • very rarely - from less than 1/10000, including individual messages.
  • From the side of the nervous system
  • Often: headache, dizziness, insomnia, paresthesia, fatigue.
  • Uncommon: depression, irritability, drowsiness, vertigo.
  • From the digestive tract
  • Often: nausea and / or vomiting, diarrhea, dyspepsia, abdominal pain.
  • Infrequently: dryness of the mucous membrane of the mouth or throat, flatulence, pancreatitis *, angioedema of the intestine, gastrointestinal bleeding.
  • Rare: hepatitis.
  • General disorders and disorders at the injection site
  • Uncommon: edema (peripheral or generalized), malaise, viral infections.
  • From the circulatory and lymphatic systems
  • Uncommon: hemolytic anemia*, thrombocytopenia*.
  • From the side of the cardiovascular system
  • Often: a pronounced decrease in blood pressure.
  • Uncommon: angina pectoris, palpitations, tachycardia, heart failure, myocardial infarction, stroke, increased blood pressure, cardiogenic shock, postural hypotension*, syncope*, symptoms of vasodilation.
  • From the respiratory system, chest organs and mediastinum
  • Often: cough, dyspnea, pharyngitis, chest pain.
  • From the skin and subcutaneous tissues
  • Uncommon: alopecia*, exfoliative dermatitis*, increased sweating, pemphigus*, photosensitivity reactions*, pruritus, rash.
  • From the musculoskeletal and connective tissue
  • Often: back pain.
  • Uncommon: arthralgia.
  • From the side of the kidneys and urinary tract
  • Uncommon: urinary tract infections, acute renal failure.
  • From the genital organs and mammary gland
  • Infrequently: decreased potency.
  • From the side of the organ of vision:
  • Uncommon: blurred vision.
  • From the immune system:
  • Uncommon: anaphylactic reactions*.
  • Rare: angioedema.
  • Others:
  • Rare: eosinophilic pneumonitis.
  • Laboratory indicators:
  • very rarely noted agranulocytosis and neutropenia, although a causal relationship with the use of quinapril has not yet been established.
  • Hyperkalemia: (see "Special Instructions").
  • Creatinine and blood urea nitrogen: an increase (more than 1.25 times compared with the upper limit of normal) in serum creatinine and blood urea nitrogen was observed in 2% and 2% of patients receiving quinapril monotherapy, respectively. The likelihood of an increase in these indicators in patients receiving diuretics at the same time is higher than with the use of quinapril alone. With further therapy, the indicators often return to normal.
  • * - less frequent adverse events or noted during post-marketing studies.
  • With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate, intravenously), a symptom complex is described, including facial flushing, nausea, vomiting, and a decrease in blood pressure.

drug interaction

Tetracycline and other drugs that interact with magnesium: the simultaneous use of tetracycline with quinapril reduces the absorption of tetracycline by approximately 28-37% due to the presence of magnesium carbonate as an auxiliary component of the drug. With simultaneous use, the possibility of such an interaction should be taken into account. Lithium: in patients who simultaneously received lithium preparations and ACE inhibitors, an increase in the content of lithium in the blood serum and signs of lithium intoxication due to increased sodium excretion were observed. Use of these drugs at the same time should be done with caution; during treatment, regular determination of the content of lithium in the blood serum is shown. Concomitant use of diuretics may increase the risk of lithium intoxication. Diuretics: with the simultaneous use of quinapril with diuretics, an increase in the antihypertensive effect is noted (see section "Special Instructions"). Drugs that increase the content of potassium in the blood serum: if a patient receiving quinapril is shown potassium-sparing diuretics (for example, spironolactone, triamterene or amiloride), potassium preparations and salt substitutes containing potassium, then they should be used carefully under the control of potassium content in the blood serum. Ethanol (drinks containing alcohol): ethanol enhances the antihypertensive effect of quinapril. Hypoglycemic agents for oral administration and insulin: Therapy with ACE inhibitors is sometimes accompanied by the development of hypoglycemia in patients with diabetes mellitus receiving insulin or hypoglycemic agents for oral administration. Quinapril enhances the effect of oral hypoglycemic agents and insulin. Other drugs: there were no signs of a clinically significant pharmacokinetic interaction of quinapril with propranolol, hydrochlorothiazide, digoxin or cimetidine. The use of hinapril 2 times a day did not significantly affect the anticoagulant effect of warfarin with its single use (estimated 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 did not lead to significant changes in the equilibrium pharmacokinetic parameters of atorvastatin. Quinapril increases the risk of developing leukopenia when used simultaneously with allopurinol, cytostatic agents, immunosuppressants, procainamide. Antihypertensive drugs, narcotic analgesics, drugs for general anesthesia enhance the antihypertensive effect of quinapril. Estrogens, non-steroidal anti-inflammatory drugs (NSAIDs) (incl. selective inhibitors of cyclooxygenase-2 (COX-2)) 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 quinapril, may lead to deterioration of renal function, including possible acute renal failure. The state of kidney function should be regularly monitored in patients receiving both NSAIDs and quinapril. The use of ARA II, 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. Quinapril should not be used simultaneously with aliskiren and aliskiren-containing agents or with ARA II or with other drugs that inhibit the RAAS (double blockade of the RAAS): in patients with diabetes mellitus or in patients with diabetes mellitus with target organ damage (diabetic nephropathy); in patients with impaired renal function (glomerular filtration rate (GFR) less than 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 cause bone marrow suppression increase the risk of developing neutropenia and / or agranulocytosis. With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate, intravenously), a symptom complex is described, including facial flushing, nausea, vomiting, and a decrease in blood pressure. Patients receiving concomitant therapy with mTOR enzyme inhibitors (eg, temsirolimus) or DPP-4 inhibitors (sitagliptin, vildagliptin, alogliptin, saxagliptin, linagliptin) or estramustine may be at greater risk of developing angioedema. Caution should be exercised while using these drugs with the drug Quinapril-SZ.

Overdose

Symptoms: pronounced decrease in blood pressure, dizziness, weakness, visual impairment. Treatment: symptomatic. The patient should take a horizontal position, it is advisable to conduct intravenous infusion using 0.9% sodium chloride solution (in order to increase BCC). Hemodialysis and peritoneal dialysis are ineffective.

Storage conditions

  • store in a dry place
  • keep away from children
  • store in a place protected from light
Information provided
Similar posts