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^® нельзя применять для гемодиализа или гемофильтрации мембраны, содержащие полиакрилнитрил-металлилсульфонат (eg, “AN 69”), as there is a risk of hypersensitivity reactions until development of shock, threatening the life of the patient. В случае необходимости неотложного диализа или гемофильтрации, перед проведением этих процедур больному либо назначают другой антигипертензивный препарат (не ингибитор АПФ), or apply another dializnuju membrane.

Во время проведения плазмафереза с сульфатом декстрана при сопутствующей терапии ингибитором АПФ могут возникать реакции повышенной чувствительности, угрожающие жизни больного.

During desensibilizirujushhej therapy, aimed at addressing the symptoms, caused by poison insects (stings of bees or wasps), на фоне приема ингибитора АПФ могут развиваться анафилактические реакции, иногда угрожающие жизни больного (decrease in blood pressure, breathlessness, vomiting, allergic skin rashes).

Лечение проводят под постоянным врачебным контролем.

У больных со сниженным ОЦК в организме (conditioned, eg, vomiting, diarrhea, приемом диуретиков), ослаблением сократительной способности сердца или злокачественной артериальной гипертензией в начале лечения Квадроприлом^® может отмечаться резкое падение АД. По возможности перед началом лечения Квадроприлом^® следует восполнить дефицит ОЦК в организме или ограничить проводимую терапию диуретиками и, 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, возможно появление данной побочной реакции и при приеме Квадроприла^®. В этом случае лечение Квадроприлом^® следует немедленно прекратить и установить наблюдение за состоянием пациента вплоть до полного исчезновения отека. Даже в случае отека языка без нарушения дыхания может потребоваться длительное наблюдение за состоянием пациента и принятие экстренных мер, так как в очень редких случаях при отеках языка и гортани отмечали смертельный исход.

При отеке тканей с вовлечением гортани, глотки и/или языка следует срочно ввести эпинефрин п/к в дозе 0.3-0.5 мг или медленно в/в в дозе 0.1 мг под контролем ЭКГ и АД, затем назначают ГКС. После этого рекомендуется в/в введение антигистаминных средств (blokatorov gistaminovyh N₁-receptors).

У больных со злокачественной артериальной гипертензией или с сердечной недостаточностью терапию Квадроприлом^® начинают в стационаре.

В период лечения необходимо воздерживаться от приема этанола.

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, назначение адсорбирующих веществ). In severe cases, – госпитализация и поддержание жизненно-важных функций организма в условиях стационара.

Для выведения препарата из организма можно провести сеанс гемодиализа. If hypotension, primarily, восполняют ОЦК в/в вливанием физиологического раствора. При необходимости дополнительно в/в вводят катехоламины. При выраженной брадикардии, которая не купируется с помощью лекарственных средств, имплантируют искусственный водитель ритма. Необходим контроль концентрации электролитов и креатинина в крови.

Drug Interactions

Antihypertensive drugs (особенно в сочетании с диуретиками), sleeping pills, средства для общего наркоза усипивают гипотензивное действие Квадроприла^®.

NSAIDs (eg, acetylsalicylic acid, Indomethacin), incl. и ингибиторы ЦОГ-2, могут ослаблять гипотензивный эффект Квадроприла^®.

При одновременном применении Квадроприла^® with potassium preparations, potassium-sparing diuretics (eg, spironolactone, amiloridom, Triamteren), а также гепарином повышается риск развития гиперкалиемии.

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).

При совместном применении Квадроприла^® with allopurinol, prokaynamydom, а также лекарственными средствами, подавляющими защитные реакции организма (цитостатические, иммунодепрессивные средства, SCS for systemic use) повышается риск развития лейкопении.

Kvadropril^® усиливает гипогликемическое действие инсулина, oral hypoglycemic agents (бигуанидов, sulfonylureas).

При одновременном применении с эстрогенами или поваренной солью ослабляется антигипертензивное действие Квадроприла^®.

Одновременный прием Квадроприла^® 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.