KVADROPRIL

Active material: Spirapril
When ATH: C09AA11
CCF: ACE inhibitor
ICD-10 codes (testimony): I10, I50.0
When CSF: 01.04.01.03
Manufacturer: AWD.pharma GmbH & Co.KG (Germany)

DOSAGE FORM, COMPOSITION AND PACKAGING

Pills from light pink to mramornostju to pink with a touch of Orange from mramornostju, round, with chamfers, with a smooth surface and scored on one side; on the side of the plane risks pills beveled inside.

Excipients: lactose monohydrate, corn starch, povidone K30, glycine hydrochloride, alginic acid, colloidal silicon dioxide, magnesium stearate, iron oxide red dye (E172).

10 PC. – blisters (3) – packs cardboard.

Pharmacological action

ACE inhibitor – enzyme, catalysing making angiotenzina I angiotenzin II. Angiotensin II exerts powerful sosudossoujiwati effect, increases withdrawal potassium and retards the excretion of sodium.

Spirapril provides antihypertensive, vasodilator, cardioprotective and natriyureticescoe effect, acting, primarily, the Renin-angiotensin-aldosteronovuju system; He also contributes to the release of biologically active substances, an natriyureticescoe and sossoudorasshiratee effect (Prostaglandins E1 and E2, endothelial relaxation factor, predserdi natriyureticeski factor) and reduces the formation of arginine-vasopressin and endothelin-1, possessing sossoudossoujiwatmi properties.

Drug effect develops over 1 h after administration, reaches through 4-8 h and lasts for about 24 no.

Pharmacokinetics

Absorption

After taking the drug inside the absorption from the digestive tract is 45%. Absolute bioavailability is approximately spiraprila 50%, spiraprilata – 70%. C_max in plasma achieved through spiraprila 45-90 m, spiraprilata – through 2-3 no.

Distribution

Linking blood plasma spiraprila and its active metabolite is 90%.

Metabolism

Biotransformiroetsa in the liver with the formation of the active metabolita – spiraprilata.

Deduction

Excreted in the urine (40%) and feces (51%) in unmodified form and in the form of metabolites. T_1/2 is 2 h for the first phase and excretion 40 no – for the second phase.

Testimony

- Arterial hypertension;

- Congestive heart failure (in a combination therapy).

Dosage regimen

The drug is taken orally, regardless of the meal, drinking plenty of fluids, without chewing.

At hypertension and chronic heart failure initial daily dose 3 mg (1/2 tab.). If necessary, the daily dose can be increased up to 6 mg (1 tab.). The maintenance dose is, average, 6 mg (1 tab.) per day. The maximum daily dose – 6 mg.

Duration of treatment is determined by the physician individually.

To patients with impaired renal function (CC 10-30 ml / min) The recommended daily dose is 3 mg (1/2 tab.), you take in the morning. Treatment begin only with careful medical observation of patients. Depending on the indicators of kidney daily dose of the drug, you can maximize in single justified cases to 6 mg (1 tab.), you take in the morning.

In patients from moderate impaired kidney (CC 30-60 ml / min), impaired liver function, and y elderly patients reducing the dose is not required.

Side effect

Cardio-vascular system: decrease in blood pressure, orthostatic hypotension; rarely – fainting; in a few cases – tachycardia, Arrhythmia, angina, myocardial infarction, the increasing incidence of failure of peripheral blood circulation, exacerbation of Raynaud's disease.

From the urinary system: giperkreatininemiя, the development or strengthening of the chronic renal failure, proteinuria.

From the central and peripheral nervous system: cerebral stroke, dizziness, headache, weakness; when used in high doses – insomnia, anxiety, depression, confusion, paresthesia, sleep disorders, disequilibrium.

From the senses: vestibular disorders, hearing and visual impairment, noise in ears, changes in taste, or a temporary loss of taste.

From the digestive system: nausea, diarrhea, cholestatic jaundice, dyspepsia, constipation, decreased appetite, stomatitis, glossitis, dry mouth, increase in liver transaminases, giperʙiliruʙinemija; in a few cases – ileus, abnormal liver function, hepatitis, pancreatitis and progressive hepatic necrosis (until death).

The respiratory system: dry cough, pulmonary infiltrates, bronchospasm, breathlessness, rhinitis, rhinorrhea, sinusitis, pharyngitis, disfonija.

Allergic reactions: skin rash, itch, hives, photosensitivity, angioedema facial tissues, limbs, lips, language, glottis and / or larynx, erythema multiforme, exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome); in a few cases – intestinal angioedema.

From the hematopoietic system: anemia, leukopenia, thrombocytopenia; rarely – eozinofilija; in a few cases – agranulocytosis, pancytopenia, gemoliz.

Metabolism: increase of urea, hyperkalemia, giponatriemiya.

Other: alopecia, onycholysis, reduced potency; in a few cases – raised titer of antinuclear antibodies.

Contraindications

— swelling angioneuroticeski in history against the backdrop of the admission of ACE inhibitors;

- Hereditary or idiopathic angioedema;

- Pregnancy;

- Lactation (breast-feeding);

- Up to 18 years (efficacy and safety have not been established);

- Hypersensitivity to the drug.

FROM caution should designate product with bilateral stenosis of the renal arteries, stenosis of the artery to a solitary kidney, expressed violation of the kidney (CC < 10 ml / min), condition after kidney transplantation, stenosis of the aortic or mitral valve, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, systemic connective tissue diseases (eg, SLE, scleroderma), abnormal liver function, cerebro- and cardiovascular diseases (incl. cerebrovascular insufficiency, CHD, coronary insufficiency), suppression of bone marrow hematopoiesis, diabetes, hyperkalemia, diet with restriction of sodium, under conditions, accompanied by a decrease in the bcc (incl. diarrhea, vomiting), and elderly patients.

Pregnancy and lactation

Kvadropril^® contraindicated during pregnancy.

If you must use Kvadroprila^® lactation breastfeeding should be discontinued.

If treatment with Kvadroprilom^® pregnancy was achieved, therapy should be discontinued, tk. When taking Kvadroprila^® intrauterine fetal damage may occur (violation of kidney, reduction in blood pressure of the fetus and newborn, impairment of renal function, hyperkalemia, skull hypoplasia, oligogidramnion, contracture of limbs, deformation of the skull, pulmonary hypoplasia).

Cautions

Hypotension, After the first dose, is not a contraindication to further use of Kvadroprila^® (after normalization of HELL, the subsequent regular intake does not lead to arterial hypotension).

In patients with renovascular hypertension there is a need to systematically monitor the content of creatinine and urea in plasma.

In patients with autoimmune diseases requires regular monitoring of the number of leukocytes in the blood.

The appointment amid giperkaliemii should be under the control of the concentration of potassium in the blood plasma.

When conducting surgical procedures using general anesthesia patients, host Kvadropril^®, perhaps marked reduction of blood pressure. Before the general anesthesia must notify anesthesiologist about the application of ACE inhibitors.

During treatment Kvadroprilom^® cannot be used for hemodialysis or hemofiltration of the membrane, containing polyacrylnitril-metallil sophulosfonat (eg, “AN 69”), as there is a risk of hypersensitivity reactions until development of shock, threatening the life of the patient. If necessary, emergency dialysis or hemofiltration, Before carrying out these procedures, a patient is prescribed by another antihypertensive drug (Not an ACE inhibitor), or apply another dializnuju membrane.

During plasmapheresis with Dexstran sulfate with concomitant therapy for the ACE inhibitor, reactions of increased sensitivity may occur, threatening the patient's lives.

During desensibilizirujushhej therapy, aimed at addressing the symptoms, caused by poison insects (stings of bees or wasps), Anaphylactic reactions may develop against the background of the reception of the ACE inhibitor, sometimes threatening the patient's lives (decrease in blood pressure, breathlessness, vomiting, allergic skin rashes).

Treatment is carried out under constant medical control.

In patients with reduced BCC in the body (conditioned, eg, vomiting, diarrhea, reception of diuretics), weakening of the contractile ability of the heart or malignant arterial hypertension at the beginning of the treatment with a quadropril^® A sharp drop in blood pressure may be noted. If possible, before the treatment of quadropril^® It should be replenished with the deficiency of the BCC in the body or limit the therapy carried out by diuretics and, if necessary, cancel them.

To avoid unexpected sharp fall ad after the first dose, as well as after raising dose dioretikov and/or increase the dose of Kvadroprila^® for these patients, establish medical supervision for at least 6 no.

Because, that in rare cases when taking ACE inhibitors indicated angioedema of the face, limbs, lips, language, the larynx or pharynx, this adverse reaction is possible when taking a quadropril^®. In this case, the treatment of quadropril^® should immediately stop and monitor the patient's condition until the swelling disappears completely. Even in the case of tongue swelling without breathing problems, long-term monitoring of the patient’s condition and emergency measures may be required, since in very rare cases, death has been reported due to swelling of the tongue and larynx.

For tissue swelling involving the larynx, pharynx and/or tongue, epinephrine should be urgently administered subcutaneously in a dose 0.3-0.5 mg or slow IV dose 0.1 mg under ECG and blood pressure control, then GCS is prescribed. After this, intravenous administration of antihistamines is recommended. (blokatorov gistaminovyh N₁-receptors).

In patients with malignant arterial hypertension or heart failure, therapy with Quadropril^® start in hospital.

During the treatment period it is necessary to refrain from taking ethanol.

Effects on ability to drive vehicles and management mechanisms

In the period of treatment should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: marked reduction in blood pressure, bradycardia, collapse, shock, violations of water-electrolyte balance, acute renal failure.

Treatment: symptomatic (gastric lavage, purpose of adsorbents). In severe cases, – hospitalization and maintenance of vital body functions in a hospital setting.

To remove the drug from the body, you can perform a hemodialysis session.. If hypotension, primarily, replenish blood volume with intravenous infusion of saline solution. If necessary, additional catecholamines are administered intravenously. With severe bradycardia, which is not controlled with medications, implantation of an artificial pacemaker. It is necessary to control the concentration of electrolytes and creatinine in the blood.

Drug Interactions

Antihypertensive drugs (especially in combination with diuretics), sleeping pills, General anesthesia enhances the hypotensive effect of Quadropril^®.

NSAIDs (eg, acetylsalicylic acid, Indomethacin), incl. and COX-2 inhibitors, may weaken the hypotensive effect of Quadropril^®.

With simultaneous use of Quadropril^® with potassium preparations, potassium-sparing diuretics (eg, spironolactone, amiloridom, Triamteren), and heparin increases the risk of developing hyperkalemia.

Kvadropril^® together with the use of lithium salts increases concentration of lithium in the blood plasma (a systematic monitoring of the concentration of lithium in the blood serum).

When used together with Quadropril^® with allopurinol, prokaynamydom, as well as drugs, suppressing the body's defense reactions (cytostatic, immunosuppressive drugs, SCS for systemic use) the risk of developing leukopenia increases.

Kvadropril^® enhances the hypoglycemic effect of insulin, oral hypoglycemic agents (biguanidov, sulfonylureas).

When used simultaneously with estrogens or table salt, the antihypertensive effect of Quadropril is weakened^®.

Simultaneous use of Quadropril^® and ethanol leads to increased activity of ethanol.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.