Sotalol

Chemical name

N-[4-[1-Гидрокси-2-[(1-мети��этил)амино]этил]фенил ]метансульфонамид (as hydrochloride)

Gross

C12-H20-N2-O3-S

Characteristics

Sotalol hydrochloride-white TNT substance soluble in water, propilenglikole alcohol and slightly soluble in chloroform.

Of drugs

The drugs-antiaritmicescoe, antianginalnoe, gipotenzivne. Selectivity blocks beta-adrainoretseptora and potassium channels (in high doses), does not have the internal and simpatomimeticescoy мебраностабилизирующ ей activity. Beta-blokiruty effect is the one receiving 25 mg, becoming clinically meaningful dose of 160 mg / day and the maximum, with the admission of more than 320 mg / sut. Increases the repolarization predserdy and testing (current slows potassium) and the length of the building, while elongation effective and absolute refrakternah periods (Class III medical complications). Decreases Patient, airway diseases (inotroponoe negative effect), and Sad Dad slows AV conduction weakens renin activity плазмы.Антиаритмичес��ое Effects begins in one hour after taking the inside reaches a maximum 2.5-4 hours and lasts 24 hours The on / in a dose of 40 mg is effective in five minutes and lasts for 90 minutes. Effective in aritmiah with a re-entry, especially with atrial fibrillation. As the dose is proaritmogennoe act, the risk of arrhythmias, including Letalnah.v experimental studies was not carcinogenic action in a 24 months rats doses of 137-275 mg / kg / day (approximately 30-kratnaya MRDC), and mice doses 4141-7122 mg / kg / day (450-750 NHDRs) within 24 months. The male and female rats using doses of up to 1000 mg / kg / day (100 MRDC) is not adversely action on fertility. In imposing krolikam dose of 160 mg / kg / day (16 MRDC), a marginal increase mortality Plodov.bystro and completely absorbed from the digestive tract. Material-89%, eating, especially dairy products, reduces it to 18-20%. C_max is 2-4 hour equilibrium concentration after a 5-6 receptions (within 2-3 days). It binds to plasma proteins. Poor passes through GEB (vsokogidrofilen) in the spinal fluid of only 5-28% of the plasma. Penetrates through the placental barrier and in breast milk. There is metabolized in the liver (less than 1%). T_1/2 7-18 hours (average 15 hours), and renal failure-to 48 hours. Patients who are older can koumoulirovati. Report mostly kidneys (90%), largely due to clubockova filtering.

Indications

Jeludockove adults : fibrillace, refrakternae form tachycardia (permanent and paroxizmale form in the programmed electrical stimulation of the heart); AV retiprokne tachycardia with anomalies out of the heart (WPW syndrome, dissociation AV node); Najeludockove adults (including prevention); tachycardia in tireotoxicose; Drinking voltage, especially when combined with tahiaritmiami; Arterial Hypertension; gipertrofica cardiomyopathy, mitral prolapse valve prevention and treatment of myocardial infarction (with a stable condition patient).

Restrictions on the use of

Bronchoobstructive syndrome (chronic bronchitis, emphysema light), psoriasis, diabetes mellitus, hypoglycaemia, feohromotsytoma, renal failure, metabolic acidosis, gipokaliemia, gipomagniemia, old age, myocardial infarction in history, coupled allergic history, old age, pregnancy, breast-feeding.

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

Hypersensitivity, cardiac insufficiency IV of the NYHA, AV blockade II extent sinoatrialnaya blockade syndrome weakness sinusnogo unit cardiogenny shock expressed arterial gipotenzia lengthening the QT interval, sinusova aetiology (less than 50 u. / min), expressed human peripheral blood circulation, swelling the larynx, severe allergic rhinitis.

Side-Effects

Allergic reactions : photosensitization, eritematosnaya rash (2%), swelling angioneuroticeski, Anaphylaccia.so the nervous system and sensory organs : dizziness (7%), headache (4%), fatigue (4%), irritability (37%), depression (1%), insomnia (1.0%), parestesia (1%), a decline of (1%), keratokongunguit (1%) slezootdelenia reduction (1%), fatigue, sputannosti consciousness, emotional lability, the sensitivity and coordination of movements, peripheral Neiropatia.so the circulatory system and blood (blood, gemostaz) : expressed aetiology (8%), heart (3%), gipotenzia (3%), heart failure (2%), sincope (1%), the peripheral blood (1%), elongation QT interval, proaritmicski effect (including automatic type "pirouette"), less than 1% hypertension (less than 1%), AV blockade collapsed lakopenia, Eozinofilia.so the respiratory system : despnoe (5%), pain in the chest (4%), healthy lungs, Bronhospazm.so part of the intestine : nausea and vomiting (5%), neuralgia (2%), diarrhea (2%), the appetite (1%) changing body mass index (1%), stomachache (less than 1%), dry mouth, Anorexia.so the musculoskeletal system : artralgia (1%) pain in the back (1%), arthritis, muscle weakness, Sudorogi.so the urogenital system : peripheral edema (2%), impotence (1% of cases), violation of urinary functions (1%), lower Libido.prochie : alopecia, prurigo, raising triglycerides, hypoglycaemia, the syndrome.

Patient interaction

Hypotension increase Tricyclic antidepressants, barbiturates, derivatives fenotiazina, narcotic analgesics, haloperidol, vazodilatatora, dioretiki. Coupled with MAO inhibitors and norapinefrinom possible surge in the AD with tubokurarinom-deepening neiromyshecna blockade. Heart glycosides, rezerpin, clonidine, alfa-metildofa, guanfation potenziruut ischemia curves and braking vnutriserdecna conductivity, calcium antagonists, beta-adrainoretseptorov blockade, amiodaron-risk arrhythmias; sulfonylureas derivative-gipoglikemia; hinolona-increase bioavailability. Ters effect theofillina and Effects бета_2-адреномиметико��. Increases the flekainida lidocaine and epinephrine.

Overdosing

Symptoms : weakness, midriaz, loss of consciousness, mioclauniceskie Generalized convulsions, gipotenzia, bronhospazm, aetiology (with asistoliei), acute ventricular tachycardia, cardiogennogo symptoms and hypovolemic shock, cardiac failure, Gipoglikemia.lechenie : washing stomach, Hepatology; symptomatic therapy : atropine, dopamine, izoprenalin, epinephrine, glukagon.

Precautions

The appointment should be lifted so antiaritmicescie to break in the treatment must be at least 2-3 years T_1/2 past. After kordarona sotalol can be applied only if normal QT interval. The chances of aritmogennogo noted at the beginning of treatment and at each increasing dose, and its recommended to increase gradually, at intervals of 2-3 days. The therapy required monitoring HR, AD QT interval (if it gets more than 550 ms receiving end), breathing apparatus periodic monitoring picture peripheral blood. The diabetes mellitus, there is a need to control blood sugar amidst dioreticakih products, the content of potassium in Plazme.sleduet bear in mind that the dose of 320 mg or more affect psychomotor reaction. There is a need to reduce the doses (up to cancellation) in older patients with obstructive respiratory disease, or difficulty breathing, hypotension, bradikardii. Remove should be gradual, reducing the dose for 1-2 weeks (at the risk of arrhythmias). When pregnancy sotalol to abolish 2-3 day before, exceptionally newborn within 48 to 72 hours after birth should be under medical Controlem.u patients feohromotsytoma appointment only together with �льфа-адреноблокатора ми. Against the backdrop of aggravated allergologicaki history may increase symptoms reaction гиперчувствительност и and the lack of therapeutic effect of conventional doses Epinefrina.pri a rapid intervention vehicle of choice should be an anaesthetic with the least negative inotrope action. 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. Recommended that the use of alcohol during the course of treatment (probably the Orthostatic hypotension).

Dosing and Administration

Inside, erh, squeezed small amounts of water. In hypertension, 80 mg twice a day, if necessary, to 160-240 mg / day 2-3 reception. In aritmiah on 80 mg twice a day, supporting-160-320 mg / day 2-3 reception. In refrakternah jeludockovh aritmiah-up to 640 mg / sut. In / in, for cupping paroxizmov jeludockovh tachiarrhythmia (in particular, tireotoxicose) at the 20 mg slowly for 5 minutes, 20 min 20 mg at the rate of 1 mg / min, then when the effect (after one hour), you can get to ingesting. The total dose of 1.5 mg / kg (can be within 15 minutes as part of the programmed ES). Duration of treatment, ranging from a few weeks to several months. Against the backdrop of kidney failure it is necessary to increase the interval between meals and lower dose : in the Cl creatinine greater than 60 ml / min, every 12 hours, 104 ml / min, every 24 hours, 10-30 ml / min, every 48 hours in half dose, less than 10 ml / min-dose reduced fourfold, to be individually selected intervals (more dose is possible only after 5-6 receptions).

Literature

J. Baumann Class III antiarrythmic agents : the next wave / / Pharmacotherapy .- 1997 .- V. 17-N 2 (Pt.2) .- P. 76S-83S; 89S-91S discussion.

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