Acebutolol

Chemical name

({+})-N-[3-Aцетил-4-[2-гидрок си-3-[(1-метилэтил)амино ]пропокси]фенил]бутан��мид (as hydrochloride)

Gross

C18-H28-N2-O4

Characteristics

White or almost white powder. It is soluble in water, however, in spirit.

Of drugs

The drugs-gipotenzivne, antianginalnoe, antiaritmicescoe. Does beta_1-adrainoretseptora, has its own simpatomimeticescuu activity and мембраностабилизирую щие properties. Normalizes increased Sad and Dad while preserving curves and minutes of the heart. Gipotenzia made through 1.5 h after administration reaches its peak in 3-8 h, until 24-30 h stabilize by the end of two weeks of treatment. Antihypertensive effect of oppression CNS, a decrease heart emission synthesis and renin activity, the restoration of the sensitivity baroretseptorov and eventually reduced peripheral sympathetic influences. Antiarrhythmic properties linked to the suppression of automaticity sinusnogo unit elongation of refrakternogo period, the slower the AV node. There is a negative action at the London Obmen.v pilot studies in a rat and mice aceboutolola in doses up to 300 mg / kg / day (15 MRDC), and diazetolola in doses up to 1800 mg / kg / day carcinogenicity signs were found. The test at Ames mutagenicity received negative results. The male and female rats using doses aceboutolola to 240 mg / kg / day and diazetolola 1000 mg / kg / day of the adverse action on fertility was observed in rats and rabbits exposed to 31.5 and 6.8 times respectively over MRDC, tertogennogo action is not supported; aceboutolol dose of 135 mg / kg / day delayed growth fruit and diazetolol (450 mg / kg / day) raised postimplantatinuyu loss of Krolikov.pocti entirely (97%) of the skin glands (eating slows induction). Bioavailability is about 40% because under intense biotransformation in "first pass" through the liver, where in part, into a more active metabolite - diazetolol. Bioavailability aceboutolola increases twice the elderly, owing to a decrease in metabolism in "first pass" through the liver and reducing renal function. C_max aceboutolola achieved through 2.5 hour diazetolola, after 3.5 hours The blood aceboutolol (26%), diazetolol (6-9%) relate to the protein. T_1/2-12 h and 16 h, respectively (kidney failure T_1/2 diazetolola grew 2-3 times). Aceboutolol and diazetolol pass through gistogematicalkie barriers, including placental infiltrates the breast milk. Report the news-40% (mostly diazetolol) and the blood-50-60% (aceboutolol).

Indications

Arterial hypertension, stenocardia (preventing attacks), myocardial infarction, and najeludochkovaya ventricular tahiaritmia, blinking predserdy, gipertrofica cardiomyopathy, mitral prolapse valve headache vascular genesis, tremor, anxiety, thyrotoxicosis.

Restrictions on the use of

Bronchial asthma, obstructive respiratory disease, the liver or kidney disease peripheral vessels (illness Reynaud, etc.) Heart failure (asthma phase), feohromotsytoma, diabetes mellitus, Ray, depression, male, psoriasis, pregnancy, breast-feeding, elderly and child.

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Chronic heart failure in the process of decompensation, cardiogenny shock syndrome weakness sinusnogo hub, AV blockade II and III degree expressed aetiology (less than 50 u. / min), gipotenzia (including the infarct infarction).

Side-Effects

From the nervous system and sensory organs : insomnia (11%), insomnia (6%), dizziness (6%), headache (6%), drowsiness (3%), nightmares (2%), depression (2%), a violation of (2%), fatigue, weakness, anxiety, paresthesia, convulsions, Reducing product slezna liquids (dry mucous membranes eye), the pain in Glazah.so the circulatory system and blood (blood, gemostaz) : pain in the chest (2%), the deterioration of peripheral blood circulation, decompensation heart failure, AV blockade aetiology, Gipotenzia.so part of the intestine : neuralgia (4%), diarrhea (4%), constipation (4%), nausea (4%), flatulence (3%), anorexia, giperlipidemia, human liver (increase LDG, cium, alkalinovh phosphatases and other enzymes). From the respiratory system : dizziness (4%), vazomotornyi rhinitis (2%), cough (1%), bronhospazm, asthma status (rarely). From the urogenital system : edema (2%), dizuriceskie disorders, dark urine, nictoria weakening Libido.prochie : allergic reaction (rash-2%), and artralgia mialgia (2%), hypoglycaemia.

Specific guidance

The treatment may change the results of tests in the laboratory (growth titra antinuclearnah antibodies, etc.).

Patient interaction

Verapamil, diltiazem, quinidine, snow for narcosis, amiodaron reinforce negative foreign and / or hronotropony effect. Gipotenzia potenziruetsa other hypotensive drugs. Quick depletion kateholaminovykh depot amidst simpatolitikov (rezerpin). In the same time the application of insulin and oral medications protivodiabeticakih increases gipoglikemii symptoms. Incompatible with MAO inhibitors. It increases the likelihood of a severe systemic reactions (up to arginine) in the face of the allergens (immunotherapy, skin samples).

Overdosing

Symptoms : aetiology expressed Arterial gipotenzia, bronhospasticskie reaction cardiac Nedostaternsti.lechenie : symptomatic : introduction atropine (in / with 1-3 mg), glukagona, vazopressornah funds (dobutamin, epinephrine, dopamine), izoprenalina, diazepam, bronhodilatatorov (theofillin, aminofillin, terbutalin), cardiac glycosides, dioreticakih products; a kidney dialysis.

Precautions

Before treatment should be compensated for heart disease, in the future need to be monitored HR, AD and the early identification of the symptoms of heart failure. There is a need to reduce the dose in older patients with obstructive airways disorders, bradikardii. In feohromotsytome appointment only, in conjunction with альфа-адреноблокатор��м. It should be borne in mind that in patients with diabetes mellitus in the face of hypoglycaemia treatment is not accompanied by palpitations. Admission aceboutolola possible two weeks after the lifting of MAO inhibitors. During treatment should be deleted alcohol (risk of Orthostatic hypotension). The rapid intervention with the use of general anesthesia for the choice should be an anaesthetic with the least negative inotrope Actiem.otmente aceboutolol it is for a period of not less than two weeks, as sudden cessation can cause severe arrhythmia, myocardial infarction. It should refrain from the use in paediatric practice, since safety and efficacy of their use in children has not been quantified. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside. In hypertension - 400 mg 1-2 admission (morning and evening), which supports the dose-800 mg, the strokes on the 200 mg twice a day, with inefficiency, 300 mg three times a day. In violation of the kidney dose dependent on the Cl creatinine : Cl with less than 50 ml/min/1 .73 m ^ 2 is not more than 50% of the normal dose below 25 ml/min/1 .73 m ^ 2-25% of the normal dose; Older patients maximum dose of 800 mg.

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