Quadropril - instructions for use, dose, side effects, contraindications

Active substanceSpiraprilSpirapril

Similar drugsTo uncover

Quadropril®

pills inwards

Teva Pharmaceutical Enterprises Co., Ltd. Israel

Dosage form: & nbsppills

Composition:

1 tablet contains

active substance: spirapril hydrochloride monohydrate 6.21 mg in terms of spirapril hydrochloride 6.00 mg;

Excipients: lactose monohydrate 99.770 mg, corn starch 22.500 mg, povidone To 30 3,000 mg, glycine hydrochloride 3,000 mg, alginic acid 13,000 mg, silicon dioxide colloid 1,500 mg, magnesium stearate 1,200 mg, iron dye oxide red E 172

Description:From light pink with marble to pink with a touch of orange with marbling, round tablets with chamfers, smooth surface, and risk on one side. On the side of the risks, the plane of the tablet is chamfered inside.

Pharmacotherapeutic group:Angiotensin-converting enzyme (ACE) inhibitor

ATX: & nbsp

C.09.A.A ACE Inhibitors

C.09.A.A.11 Spirapril

Pharmacodynamics:

Angiotensin-converting enzyme (ACE) inhibitor, which catalyzes the conversion of angiotensin I into angiotensin II. Angiotensin II shows a potent vasoconstrictor effect, enhances the excretion of potassium and delays the excretion of sodium. Spirapril has antihypertensive, vasodilating, cardioprotective and natriuretic effect, acting,first of all, on the renin-angiotensin-aldosterone system; it also promotes the release of biologically active substances that have natriuretic and vasodilating effects (prostaglandins E1 and E2, endothelial relaxation factor, atrial natriuretic factor) and reduces the formation of arginine-vasopressin and endothelin-1, which have vasoconstrictive properties.

The effect of the drug develops within an hour after admission, reaches a maximum after 4-8 hours and lasts about 24 hours.

Pharmacokinetics:

Absorption from the gastrointestinal tract is 45%. Due to biotransformation, an active metabolite of spiraprilate is formed in the liver. The maximum concentration of spirapril in the blood plasma is reached 45-90 minutes after administration, and spiraprilata - after 2-3 hours. Absolute bioavailability of spirapril is approximately 50%, spiraprilata - 70%. Spirapril and its active metabolite bind 90% to plasma proteins. Spirapril is excreted by the kidneys (40%) and through the intestine (51%) in unchanged form and in the form of metabolites. The half-life period is 2 hours for the first phase of excretion and 40 hours for the second phase.

Indications:

- Arterial hypertension;

Chronic heart failure (as part of combination therapy).

Contraindications:

Hypersensitivity to the active substance, other components of the drug and other ACE inhibitors: angioedema in the history of taking ACE inhibitors in the anamnesis; hereditary or idiopathic angioedema, aortic stenosis; mitral stenosis; bilateral stenosis of the renal arteries; stenosis of the artery of a single kidney; severe renal dysfunction (creatinine clearance (CK) less than 10 ml / min); hemodialysis or hemofiltration using a membrane containing polyacrylonitrile-metal sulfonate (for example. AN69®); condition after kidney transplantation; hypertrophic obstructive cardiomyopathy; primary hyperaldosteronism; arterial hypotension; simultaneous use with aliskirnym or aliskirezoderzhaschimi drugs in patients with diabetes mellitus and / or renal dysfunction (glomerular filtration rate (GFR) less than 60 ml / min / 1.73 m²) (see the section "Interaction with other medicinal products"); pregnancy; the period of breastfeeding; age to 18 years: lactose intolerance; deficitlactase; syndrome of glucose-galactose malabsorption.

Carefully:

- Bilateral stenosis of the renal arteries,

- stenosis of the artery of a single kidney,

- pronounced impaired renal function (creatinine clearance less than 10 ml / min.),

- conditions after kidney transplantation,

- Stenosis of the aortic or mitral valve,

- hypertrophic obstructive cardiomyopathy,

- primary hyperaldosteronism,

- systemic connective tissue diseases (eg, systemic lupus erythematosus, scleroderma),

- a violation of the liver,

- cerebrovascular and cardiovascular diseases (including cerebral circulatory insufficiency, ischemic heart disease, coronary insufficiency),

- oppression of bone marrow hematopoiesis,

- diabetes,

- Hyperkalemia, a diet with sodium restriction, in conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting),

- elderly age.

Dosing and Administration:

Inside, regardless of food intake, squeezed a sufficient amount of liquid, without chewing.

Arterial hypertension

The initial dose is 1/2 tablet of 6 mg (3 mg / day).If after taking this dose the blood pressure is not normalized, the dose can be increased to 1 tablet (6 mg / day). The maintenance dose is usually 1 tablet (6 mg / day).

The maximum daily dose is 1 tablet (6 mg / day).

Chronic heart failure

The initial dose is 1/2 tablet of 6 mg (3 mg / day).

If necessary, the dose can be increased to 1 tablet (6 mg / day).

The maintenance dose is usually 1 tablet (6 mg / day).

The maximum daily dose is 1 tablet (6 mg / day).

In patients with impaired renal function (QC from 10-30 ml / min.) The recommended dose of the drug Quadropril® is 1/2 tablet of 6 mg (3 mg / day), which is taken in the morning. Treatment begins with the establishment of careful clinical observation of the patient. Depending on the indices of kidney function in single reasonable cases, the dose of the drug Quadropril® can be increased to a maximum of 1 tablet (6 mg / day), which is taken in the morning.

In patients with impaired renal function (CK 30-60 ml / min) or liver, as well as in elderly patients no dose reduction is required.

The duration of the course of treatment is determined by the doctor.

Side effects:

From the side of the cardiovascular system: contraction of AD, orthostatic hypotension, rarely - a syncope, in isolated cases - tachycardia, arrhythmias, angina pectoris, myocardial infarction, increased manifestations of peripheral circulatory insufficiency.

From the genitourinary system: development or strengthening of chronic renal failure, proteinuria, decreased potency.

From the central nervous system: cerebral stroke, dizziness, headache, weakness, exacerbation of Raynaud's disease; when used in high doses - insomnia, anxiety, depression, confusion, paresthesia, sleep disorders, imbalance.

From the sense organs: violations of the vestibular apparatus, hearing and vision impairment, tinnitus; changes in taste or temporary loss of taste.

From the digestive system: nausea, diarrhea, cholestatic jaundice, dyspepsia, constipation, decreased appetite, stomatitis, glossitis, dry mouth, in single cases - intestinal obstruction; single cases of liver dysfunction, hepatitis, pancreatitis were described. In a few cases, there was a progressive necrosis of the liver, sometimes with a fatal outcome.

From the respiratory system: "dry" cough, pulmonary infiltrates, bronchospasm, dyspnea, rhinitis, rhinorrhea, sinusitis, pharyngitis, dysphonia.

Allergic reactions: skin rash, itching, hives, photosensitivity; angioneurotic edema of facial, limb, lip, tongue, vocal cracks and / or larynx, polymorphic erythema, exfliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). In very rare cases with angiotensin-converting enzyme inhibitors angioedema was noted.

On the part of the organs of hematopoiesis: anemia, leukopenia, thrombocytopenia, rarely - eosinophilia, in isolated cases - agranulocytosis, pancytopenia and hemolysis, increased titer of antinuclear antibodies.

Laboratory indicators: hypercreatininaemia, increased urea levels, increased activity of "hepatic" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia.

Influence on the fetus: impaired fetal kidney development, decreased blood pressure in newborns, impaired renal function, hyperkalemia, skull hypoplasia, oligohydramnia, limb contracture, skull deformity, lung hypoplasia. Other: alopecia, onycholysis.

Overdose:

Symptoms: marked decrease in blood pressure, bradycardia, collapse, shock, disturbance of water electrolyte balance, acute renal failure.

Treatment: symptomatic (gastric lavage, the appointment of adsorbent substances). In severe cases - hospitalization and maintenance of vital body functions.

To remove the drug from the body, you can conduct a hemodialysis session.

With arterial hypotension, first of all, replenish the volume of circulating blood by intravenous infusion of physiological solution.

If necessary, additional intravenous catecholamines are administered.

With a pronounced bradycardia, which is not stopped with the help of drugs, an artificial pacemaker is implanted.

It is necessary to control the concentration of electrolytes and creatinine in the blood.

Interaction:

The double blockade of the renin-hyotezine-aldosteron system (RAAS) with the use of angiotensin II receptor antagonists (APA II), ACE inhibitors or aliskiren (renin inhibitor) is associated with an increased risk of arterial hypotension, syncope, hyperkalemia and renal dysfunction number of acute renal failure) compared with monotherapy.Regular monitoring of blood pressure, kidney function and electrolyte content in blood in patients taking both spirapril and other drugs that affect RAAS.

Spirapril should not be used concomitantly with aliskiren or ACE inhibitors and dipeptidyl peptidase inhibitors of the 4th type (eg, vildaglptia) may increase the risk of developing Quincke's edema.

Hypotensive drugs, hypnotics, drugs increase antihypertensive effect of the drug Quadropril ®, especially with simultaneous use with diuretic drugs. Non-steroidal anti-inflammatory drugs, incl. inhibitors of cyclooxygenase-2 (COX-2) (for example, acetylsalicylic acid, indomethacin , etc.), can weaken the antihypertensive effect of the drug Quadropril®.

When used with potassium preparations, potassium-sparing diuretics (e.g., eplersonom (spironolactone derivative), spironolactone, amiloride. triamterene), as well as heparin, the risk of developing hyperkalemia increases;

When taken simultaneously with lithium salts, the concentration of lithium in the blood serum increases (it is necessary systematic control of concentration lithium in the blood serum!).

In the appointment of ACE inhibitors to patients receiving infusion preparations of gold (sodium aurotomy malate), nitrate-like reactions (hyperemia of the facial skin, nausea, vomiting, arterial hypotension) were noted.

When used with allopurinol, procainamide, as well as drugs that suppress the protective reactions of the body (cytostatic, immunosuppressive drugs, glucocorticosteroids (GCS)), the risk of developing leukopenia increases. AT combination with the preparation Quadropril® enhances the hypoglycemic effect of insulin and sulfonylurea derivatives.

Cooking salt and estrogens weaken the antihypertensive effect of the preparation Quadropril®.

Simultaneous administration of the drug QuadroprilAnd ethanol leads to an increase in the action of ethanol.

Special instructions:

Arterial hypotension, which occurred after taking the first dose, is not a contraindication for the further use of the drug Quadropril® (after normalization of blood pressure, subsequent regular administration does not lead to hypotension).

In patients with reninvascular hypertension, the concentration of creatinine and urea must be systematically monitoredblood plasma.

Simultaneous application of inhibitors ACE, ARA II or aliskiren increases the risk of developing

arterial hypotension, hyperkalemia and renal dysfunction (including acute renal failure). Double blockade of RAAS with the use of ACE inhibitors. ARA II or aliskiren is not recommended (see section "Interaction with other medicinal products"). If a double blockade of RAAS is considered absolutely necessary, the treatment should only take place under the supervision of specialists and should be accompanied by a thorough and regular monitoring of kidney function, electrolyte content and blood pressure. ACE inhibitors and ARA II should not be used simultaneously in patients with diabetic nephropathy.

Patients with autoimmune diseases need regular monitoring of the number of leukocytes in the blood. Use on the background of hyperkalemia should be carried out under the control of the potassium content in the blood plasma.

When conducting surgical interventions with the use of general anesthesia in patients taking the drug Quadropril®, there may be a marked decrease in blood pressure.

Before general anesthesia, an anesthesiologist should be warned about the use of inhibitors ACE.

During treatment with Quadropril®, hemodialysis or hemofiltration membranes containing polyacrylonitrile-metallosulfonate (for example, AN69®), since there is a danger of reactions of hypersensitivity up to the development of shock, which threatens the life of the patient. In case of emergency dialysis or hemofiltration, before carrying out these procedures, the patient is either replaced by a drug Quadropril® for another antihypertensive drug is not an ACE inhibitor. or use another dialysis membrane.

During the conduct of plasmapheresis with dexgran sulfate with concomitant therapy with an ACE inhibitor, hypersensitivity reactions that threaten the patient's life may occur. During desensitizing therapy aimed at eliminating the symptoms caused by the poison of insects (bee or wasp stings) and the simultaneous use of an ACE inhibitor, anaphylactic reactions can sometimes develop, sometimes threatening the life of the patient (lowering blood pressure, dyspnea, vomiting, allergic skin rash).

The treatment is carried out under constant medical supervision.

In patients with reduced circulating blood volume (BCC) (for example,caused by vomiting, diarrhea, diuretics), weakening of the contractility of the heart or malignant arterial hypertension at the beginning of treatment with the drug Quadropril® there may be a sharp drop in blood pressure. If possible, before starting treatment with the drug Quadropril® should compensate for the deficiency of BCC in the body or limit the ongoing therapy with diuretics and, if necessary, cancel them.

To avoid an unpredictable sharp decrease in blood pressure after taking the first dose, as well as after increasing the dose of diuretics and / or increasing the dose of the drug Quadropril® these patients are monitored by a doctor for at least 6 hours. Due to the fact that in rare cases with angiotensin converting angiotensinergic swelling of the face, extremities, lips, tongue, larynx or pharynx, the appearance of this adverse reaction is possible and when taking the drug Quadropril®. In this case, the drug treatment Quadropril® should immediately stop and establish monitoring of the patient's condition until the complete disappearance of the edema. Even in case of edema of the tongue without disturbing breathing,it may take a long time to monitor the patient's condition and take emergency measures. because in very rare cases with swelling of the tongue and larynx, a fatal outcome was noted.

When swelling of tissues involving the larynx, pharynx and / or tongue, urgently enter subcutaneously eninephrine (adrenaline) at a dose of 0.3-0.5 mg or slowly intravenously (iv) epinephrine (epinephrine) in a dose of 0.1 mg under the control of the electrocardiogram and blood pressure, then use GCS. After this, the administration of antihistamines and H2-receptor antagonists is recommended.

In patients with malignant hypertension or with heart failure, drug therapy Quadropril® begin in the hospital.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from drinking alcohol and from practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions

Form release / dosage:

Tablets of 6 mg.

Packaging:

10 tablets per blister (PA / aluminum foil / PVC and aluminum foil).

For 3 blisters with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

In a place inaccessible to children.

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N015520 / 01

Date of registration:29.10.2008 / 26.04.2013

Expiration Date:Unlimited

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

KLOCKE PHARMA-SERVICE, GmbH Germany

Representation: & nbspPliva of Hvartska dooPliva of Hvartska doo

Information update date: & nbsp26.12.2017

Illustrated instructions

Instructions

Quadropril® (Quadropril®)