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Talliton

See also Carvedilol

Roman name

Talliton

Characteristics

Carvedilol is a non - бета-адреноблокаторо�� sosudorasshiratmi the properties (from the blockade alfa_1-adrainoretseptorov) and the secondary antioxidant substances Aguostew.aguna Tallitona ® is a mixture razemical two enantiomers carvedilola.

Pharmacokinetics

After intake of rapidly absorbed from the digestive tract. Treated with metobolizmu <pervom prokhojdenia> through the liver, bioavailability of approximately 25%. C_max in plasma is about one hour after admission внутрь.Фармакокинети��а carvedilola is linear (concentration in plasma is proportional to the dose). Collateral eating no influence on the bioavailability and C_max, but may increase T_max.carvedilol is lipofilnam connection tying him with blood plasma proteins reaches 98-99%. The apparent mass of the distribution is approximately 2 l / kg, and to a large extent be increased by cirrhosis печени.Метаболизируе��ся mainly in the liver, primarily through education glukuronidov. Demethylation and gidrauxilirovnie phenyl ring leads to the formation of three active metabolites of бета-адреноблокирующ��й activity. 4-gidroksi-metabolit beta-adrenoblokator as 13 times more carvedilola. At the same time, active metabolites are weaker sosudorasshiratmi means and two gidroksicarbazolovykh metabolita are stronger antioxidants compared to the reference compound. Average T_1/2 carvedilola - 6-10 h, and plasma klirens approximately 590 ml / Min.vwoditsa mainly jelchew. Carvedilol and its metabolites can cross the placenta, as well as the provision of breast milk. Carvedilol little removed from the blood in Gemodialize.u older patients carvedilola concentration in plasma were 50% higher than Young.bole-impaired kidney : carvedilol story appears mainly through blood, of the kidney is not accompanied by his Koumoulyatsiei.bole with liver disease : cirrhosis of the liver bioavailability carvedilola four times, and S_max in plasma-five times higher than the norm.

Farmakodinamika

As sossoudorasshiratee of carvedilol reduces force on vascular resistance, but as beta-adrenoblokator he was oppressing ренин-ангиотензин-аль достероновую system. Carvedilol reduced renin activity in plasma, and at the time of the delay of the liquid in the body, is a rare Fenomenom.carvedilol, a competitive blokatorom beta-adrainoretseptorov has negative chrono, dromo-, batmo- and inotrope effect. The drug slows conductivity in the AV node. Carvedilol or internal simpatomimeticescoy activity has been мембраностабилизирую щий Effect.sovokupnosti and sosudorasshirath �ета-адреноблокирующи х carvedilola properties is the following clinical Effectami.pri a drug in arterial hypertension antigipertenzivny its effects have not been matched by improvements in total peripheral resistance, as is the case in other �ета-адреноблокаторов . Carvedilol significantly reduces elapsed, but perfuzia kidneys and their function remain unchanged. Since the force on the blood did not change, a sense of cooling off in the application carvedilola is rare, unlike the бета-адреноблокаторо�� without sosudorasshiratei �ктивности.Антигиперт ензивный effect quick-by 2-3 h after a single injection and lasts 24 hours Leaving the treatment of the maximum effect through the 3-4 Ned.pri ischemia carvedilol has antiishemicakim and antianginalnam effects that persist long term treatment. Hemodynamics Studies have shown that carvedilol reduces pre - and the postnagruzku Serdze.blagopriatny effect carvedilola hemodinamics at heart, faction release left chamber is both dilatation cardiomyopathy, and in the form of coronary heart failure. In heart failure carvedilol reduces конечно-систолически�� and �онечно-диастолически й volume, as well as force on lung and vascular resistance. Faction release and cordial index in the normal heart functions not Izmenautxia.v case of a breach of the left heart альфа_1-адреноблокиру��щее carvedilola effect resulting in an increase in arterial and to a lesser extent venous pressure. In clinical studies, it was found that the additional appointment in the face of the cardiac glycosides, ACE inhibitors and dioretikov kaverdilol reduces mortality, slowing the progression of the disease and improving the general condition of the patient, regardless of the gravity of Zabolevania.vo treatment carvedilolom cholesterol ratio LPVP / engineers not change.

Indications

Essencialnaya hypertension, in the form alone or in combination with any other antigipertenzivei means; Stable stenocardia; chronic heart failure II and IV class NYHA, in combination with dioretikami, digoxinom or ACE inhibitors (NYHA-New York Heart Association-II : in patients in this stage alone no symptoms, moderate physical activity is accompanied by fatigue, palpitations and breathing difficulties (short breath); NYHA-IV : symptoms of heart failure at rest, a physical load sharply increases the symptoms listed above).

Pregnancy and lactation

The Tallitona ® during pregnancy and breast-feeding infants is not recommended because of the lack of clinical data. If necessary, the use of drugs during lactation should stop breastfeeding.

Patient interaction

It is a caution at the same time : to the tools drain stocks catecholamines (rezerpin, MAO inhibitors), as possible heavy aetiology and arterial gipotenzia; from BAC (verapamil, diltiazem), and protiwaritmicakimi means (especially Class I), since they may provoke expressed hypotension hypertension and heart disease. In / in the introduction of these products in conjunction with the reception counter carvedilola .- with Alpha and бета-адреномиметикам�� (because of the potential for hypertension expressed laser bradikardii asistolia and, as well as reduce the �ета-адреноблокирующе го carvedilola actions); - Clonidine and carvedilol may increase the ability of one another to reduce AD and curves. In joint application removal should be done : first excluded carvedilol, then in a few days can be gradually stopped receiving clonidine; from digoxinom (down AV conduction); on the insulin and gipoglikemicakimi facilities for the reception inside (because increase gipotenzivnogo actions and masking symptoms gipoglikemii); from nitrates and hypotensive Programme (clonidine, guanetidin, alfa-metildofa, guanfation, etc.) as a result of increased gipotenzivnogo actions and reduce variation; with the means to narcosis (because of their negative actions inotroponogo and gipotenzivnogo effect); with the means affecting the central nervous system (sedatives, tranquilizers, Tricyclic antidepressants and ethyl alcohol), because of the possibility of mutual reinforcement effects; from NPVS (due to a decrease gipotenzivnogo action as a result of reduced production NG); From ergotaminom (to be taken into account sossoudossouerveshchee of ergotamine); On the derivative xantina (aminofillin, theofillin) - due to a decrease �ета-адреноблокирующе го Actia.poscolku carvedilol is oxidative metabolizmu, his farmakokinetika may change with the induction or repression of the enzyme zitohroma P450, it should take into account the impact of :-rifampitina (a 70% decline carvedilola concentration in the serum); - barbiturates (reduce the carvedilola); - inhibitors izoenzima CYP2D6 (quinidine, fluoxetin, paroxetin, propafenon; it is increasing the concentration of R (+) Enantioselectivity carvedilola); - zimetidina (increases bioavailability carvedilola 30%). Carvedilol delaying metabolism of cyclosporine, increases the concentration of digoxin in plasma.

Precautions

Patients with severe heart failure (more III degree NYHA), and numerous electro balance reconstruction of the AD (less than 100 mm Hg), or in old age should be kept under close medical supervision during the 2 hours after the first dose, or after receiving the first dose increased, at the risk of a sudden fall AD Orthostatic Hypotension and sinkope. The danger of these complications can be reduced by a drug in small doses primary, and his reception during early Eda.v treatment and an increase in each dose patients should be monitored because possibly worsening heart failure. Could develop delay liquid, and the effect sossoudorasshiratm-arterial gipotenzia and weakness. The fluid should raise dioretikov dose, in addition, it may be necessary to temporarily reduce the dose Tallitona ®. In some cases, treatment Tallitonom ® should temporarily Priostanoviti.dozu drug to be reduced if the patient is aetiology (HR least 55 u. / min). Appointment carvedilola patients receiving heart glycosides, dioretiki and / or ACE inhibitors in heart failure, requires special Ostorozhnosti.u patients with heart failure, if they back Sad less than 100 mm Hg or are associated with the disease, coronary heart disease, peripheral defeated receptacles or violation of the kidneys, should frequently check on the health of the urinary system, as treatment may affect kidney function (usually temporarily). If the oppression of the kidneys, dose Tallitona ® should be reduced or therapy should be Prekreatmeno.u stroke patients Prinzmetala indiscriminate beta-adrenoblokatora may cause pain in the chest ( альфа_1-адреноблокиру��щий effect can prevent the act). Appointment drug during a lightning strokes, as well as AV blockade degree I requires attention frequent registration exercise and careful medical monitoring Ballam.lechenie patients with disease peripheral arteries requires attention and Ostorozhnosti.kak and other beta-adrenoblokatora, carvedilol can mask symptoms gipoglikemii and affect carbohydrate exchange. The carvedilolom treatment of diabetes mellitus requires special attention and more frequent measurements of sugar Krovi.carvedilol may mask the symptoms of hyperthyroidism. The sudden removal of the drug might increase tireotoxicoza and possible tireotoksicski Kriz.lechenie Tallitonom ® patients with the feohromotsytoma should not start until the therapeutic blockade �льфа-адренорецепторо в.Лечение Tallitonom ® patients psoriazom requires an assessment of the benefits / risk because carvedilol can strengthen disease or provoke a Simptomov.kajdaya tablet Tallitona ® contains 50 mg lactose. This amount should be taken into account in lactaza insufficient, and galactose syndrome violations intake глюкозы/галактозы.Каж дая tablet Tallitona ® contains 12.5 mg sucrose. This may be relevant in diabetes, the hereditary rejecting fruktozy, violation learning glucose / galactose or deficit сахаразы/изомальтазы. Прекращать treatment should be gradually reducing Dozu.ballah using contact lenses should warn that carvedilol reduces products slezna Jidkosti.v early treatment Tallitonom ® patients may experience dizziness, fatigue, in this case they should refrain from driving vehicles and Occupation potentially hazardous activities requiring more concentration and psychomotor speed reactions. In the future, the safe dose is individually.

Dosing and Administration

Inside pills to swallow whole and zapiwati enough Jidkosti.pri essencialna hypertension : Recommended starting dose of 12.5 mg Tallitona ® once a day for 2 days (1 table. 12.5 mg morning , or at one table. 6.25 mg twice a day, morning and evening). Recommended supporting dose, 25 mg Tallitona ® (1 table. 25 mg morning, or at one table. 12.5 mg twice on the day in the morning and evening). If �еудовлетворительног�� result, but not earlier than 14 days of treatment, dose can be increased to a maximum of 50 mg per day (1 tab. 25 mg twice a day. morning and evening). The maximum single dose of 25 mg daily dose should not exceed 50 Mg.hronica stable stenocardia : Recommended starting dose, 12.5 mg twice a day (morning and evening) for the first two days. Recommended supporting dose 25 mg twice a day (morning and evening). If неудовлетворительног о result, but not earlier than 14 days of treatment, dose can be increased to the maximum of 50 mg twice a day (table 2. 25 mg morning and 2 table. evening). Chronic heart failure : dose should be compiled individually at the time of the dose to carry out a thorough grid. It is to monitor the patient for a period of two to three hours after the first admission or after the first dose increased. Supplementary application Tallitona ® requires a stable clinical condition. Dose, and the appointment of other property, such as digoxin, and dioretiki ACE inhibitors should be recorded prior to the appointment Tallitona ®. Patients must take pills at the time of delivery (to reduce the risk Orthostatic гипотензии).Рекоменду емая initial dose, 3.125 mg twice a day for 14 days (1 / 2 table. 6.25 mg morning and evening). If treatment is postponed patient well, and there is a need, dose can be increased to 205 mg twice a day (1 tab. 6.25 mg morning and one in the afternoon). The subsequent increase in dose to 12.5 mg twice a day (1 tab. 12.5 mg morning and evening) then to 25 mg twice a day (1 tab. 25 mg morning and evening). Patients designated as transported dose. The maximum recommended dosage for the 25 mg twice a day (1 tab. 25 mg morning and one evening, for patients weighing up to 85 kg and 50 mg twice a day (2 table. to 25 mg morning and two in the afternoon) for patients weighing more than 85 kg. Patients with heart failure to prevent Orthostatic hypotension to take medication at the time of delivery.

Storage conditions

List B. In the dark place at a temperature of 15-25 ° C

Shelf life

2

The registration

015970/01

The drug forms

Answers to 6.25 mg-bledno-jeltae flat round with 2-storonney panel, with the mark on the same side and the initials "E 341" on the other, with no or little Zapaha.tabletki 12.5 mg-bledno-orangeve flat round with 2-storonney panel, with the mark on the same side and the initials "E 342" - to another, with no or little Zapaha.tabletki to 25 mg-white flat round with 2-storonney panel, with the mark on the same side and the initials "E 343" to the other without, or almost odourless.

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