Sotalol
When ATH:
C07AA07
Characteristic.
Sotalol hydrochloride - white crystalline substance, soluble in water, propylene glycol and alcohol, slightly soluble in chloroform. Molecular weight 308,8.
Pharmacological action.
Antiarrhythmic, antianginalnoe, gipotenzivnoe.
Application.
Ventricular arrhythmias: fibrillation, refractory shapes, tachycardia (permanent and paroxysmal, during programmed electrical stimulation of the heart); AV reciprocating tachycardia anomalies of the conducting system of the heart (WPW syndrome, dissociation AV node); supraventricular arrhythmias (incl. prevention); tachycardia, thyrotoxicosis; angina, especially when combined with tachyarrhythmias; arterial hypertension; gipertroficheskaya cardiomyopathy, mitral valve prolapse, prevention and treatment of myocardial infarction (when the patient's condition stable).
Contraindications.
Hypersensitivity, IV heart failure stage according to NYHA, AV block II-III degrees, sinoatrialynaya blockade, sick sinus syndrome, cardiogenic shock, severe hypotension, QT prolongation, sinusovaya bradycardia (less 50 u. / min), expressed by peripheral circulatory disorders, laryngeal edema, severe allergic rhinitis.
Restrictions apply.
Bronchial obstruction (chronic bronchitis, emphysema), psoriasis, diabetes, gipoglikemiâ, pheochromocytoma, renal failure, metabolic acidosis, kaliopenia, gipomagniemiya, advanced age, myocardial infarction, otyahoschennыy allerholohycheskyy history, advanced age, pregnancy, breast-feeding.
Pregnancy and breast-feeding.
Maybe, if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.
Side effects.
Allergic reactions: photosensitivity, erythematous rash (2%), angioedema, anaphylaxis.
From the nervous system and sensory organs: dizziness (7%), headache (4%), asthenia (4%), irritability (2%), depression (1%), sleep disturbance (1%), paresthesia (1%), reduced vision (1%), keratokonъyunktyvyt (1%), decrease in lacrimation (1%), fatiguability, confusion, emotional lability, violation of the sensitivity and coordination, peripheral neuropathy.
Cardio-vascular system and blood (hematopoiesis, hemostasis): vыrazhennaya bradycardia (8%), heartbeat (3%), gipotenziya (3%), heart failure (2%), syncope (1%), the peripheral blood circulation (1%), QT prolongation, pro-arrhythmic effect (incl. arrhythmia type "pirouette") - Less 1%, hypertension (less 1%), OF блокада, collapse, leukopenia, eozinofilija.
From the respiratory system: dyspnoea (5%), chest pain (4%), pulmonary edema, bronchospasm.
From the digestive tract: nausea and vomiting (5%), dyspepsia (2%), diarrhea (2%), appetite disorders (1%), weight change (1%), abdominal pain (less 1%), dry mouth, anorexia.
On the part of the musculoskeletal system: arthralgia (1%), backache (1%), arthritis, muscular weakness, convulsions.
With the genitourinary system: peripheral edema (2%), impotence (1% cases), violation of urogenital functions (1%), decreased libido.
Other: alopecia, prurigo, elevated triglycerides, gipoglikemiâ, withdrawal.
Cooperation.
Hypotension increase Tricyclic antidepressants, barbiturates, phenothiazines, narcotic analgesics, haloperidol, vasodilators, Diuretic. In combination with MAO inhibitors and norepinephrine possible sharp rise in blood pressure, with tubokurarinom - deepening of neuromuscular blockade. Cardiac glycosides, reserpine, klonidin, alpha-methyldopa, guanfacine potentiate slowing heart rate and deceleration of intracardiac conduction, calcium antagonists - blockade of beta-adrenergic receptors, Amiodarone - arrhythmic risk; proizvodnyye sulifonilmochyeviny gipoglikyemiyu; quinolones - increase the bioavailability of. It weakens the effect of theophylline and beta effect2-adrenomimetikov. Increases flecainide and lidocaine plasma.
Overdose.
Symptoms: weakness, midriaz, loss of consciousness, generalized myoclonic jerks, gipotenziya, bronchospasm, bradycardia (with asystole), atypical ventricular tachycardia, symptoms of cardiogenic and hypovolemic shock, heart failure, gipoglikemiâ.
Treatment: gastric lavage, hemodialysis; simptomaticheskaya therapy: atropyn, Dopamine, Isoprenaline, epinephrine, glucagon.
Dosing and Administration.
Inside, fasting, with a little water. Hypertension - By 80 mg 2 once a day, if necessary, to 160-240 mg / day in 2-3 hours. When arrhythmias - By 80 mg 2 once a day, maintenance - 160-320 mg / day in 2-3 hours. When refractory ventricular arrhythmias - To 640 mg / day. B /, to paroxysms of ventricular tachyarrhythmias (in particular, thyrotoxicosis) first with 20 mg slowly, during 5 m, through 20 m 20 mg at a speed 1 mg / min, then when the effect (through 1 no) You can go to a reception inside. The total dose - 1,5 mg / kg (It can be administered for 5-15 minutes as part of the programmed electrical stimulation). Treatment duration - from several weeks to several months. In patients with renal insufficiency We need to increase the interval between doses and lower dose: the Cl creatinine more 60 ml / min - every 12 no, 30-60 Ml / min - every 24 no, 10-30 Ml / min - every 36-48 hours in half dose, less 10 ml / min - decrease in dose 4 times and administered individually selected intervals (increase the dose only after 5-6 receptions).
Precautions.
The appointment should be canceled other antiarrhythmic drugs - a break in treatment should be at least 2-3 period T1/2 latest. After amiodarone, sotalol may be used only if the normalized QT interval. The highest probability of arrhythmogenic action marked the beginning of treatment and with each increase in dose, so it is recommended to increase gradually, at intervals of 2-3 days. The therapy required monitoring HR, FROM, интервала QT (when more elongation 550 ms receiving end), breath, periodic monitoring of peripheral blood. Diabetic patients need to monitor blood sugar, against the backdrop of diuretics - potassium plasma.
It will be appreciated, Doses 320 mg or more impair psychomotor reactions. It is necessary to dose reduction (until canceled) in elderly patients, the presence of obstructive airways disease or shortness of breath, gipotenzii, ʙradikardii. Cancelling should be gradually, reducing the dose for 1-2 weeks (due to the risk of arrhythmias). When pregnancy sotalol are canceled for 2-3 days before delivery, exceptionally newborn within 48-72 hours after birth should be under medical supervision.
In patients with pheochromocytoma appointment only together with alpha-blockers. Against the background of aggravated allergic history may increase the severity of hypersensitivity reactions and the lack of therapeutic effect of conventional doses of epinephrine.
During the surgery of choice should be the anesthetic with the least negative inotropic effects. It should refrain from the use in pediatric practice, because the safety and efficacy of their use in children is not identified. Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention. It is recommended that the use of alcohol during treatment (likely development ortostaticheskoy gipotenzii).
Cooperation
Active substance | Description of interaction |
Azithromycin | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Akarʙoza | FMR. Against the background of the effect of sotalol enhanced, can mask the early symptoms of hypoglycemia; appointment required the combined control of blood glucose levels. |
Amiodarone | FMR: synergism. Strengthens (mutually) effect and improves (especially when on / in) the chance of developing a deep bradycardia, suppression of sinus rhythm and AV blockade; concomitant use is not recommended. |
Amitriptyline | FMR: synergism. Enhances the hypotensive effect, удлиняет интервал QT; concomitant use is not recommended. |
Amlodipine | FMR: synergism. Strengthens (mutually) effects; possible deepening of hypotension, deterioration of AV conduction and ventricular contractility. |
Verapamil | FMR: synergism. Strengthens (mutually) gipotenziю, It contributes to the negative effects on heart rate, AV conduction and / or cardiac contractility: the possibility of excessive bradycardia, OF блокада, until complete cardiac arrest. |
Haloperidol | FMR: synergism. Enhances the hypotensive effect. |
Glimepiride | FMR. Against the background of the effect of sotalol enhanced, can mask the early symptoms of hypoglycemia; appointment required the combined control of blood glucose levels. |
Glipizide | FMR: synergism. Against the background of the effect of sotalol enhanced, can mask the early symptoms of hypoglycemia (such as tachycardia); the combined appointment required monitoring of blood glucose. |
Guanfaцin | FMR: synergism. Strengthens (mutually) effects, incl. side; y ou usugubitysya bradycardia, develop intracardiac conduction blockade. |
Digoxin | FMR. Worsens (mutually) AV conduction. |
Diltiazem | FMR: synergism. Strengthens (mutually) gipotenziю, It contributes to the negative effects on heart rate, AV conduction and / or cardiac contractility: the possibility of excessive bradycardia, OF блокада, until complete cardiac arrest. |
Imipramine | FMR. Удлиняет интервал QT; combined use is not recommended. |
Indomethacin | FMR: antagonizm. Reduces hypotensive effect (It inhibits the synthesis of prostaglandins in the kidneys and inhibits sodium and fluid). |
Insulin aspart | FMR: synergism. Against the background of the effect of sotalol enhanced, possible masking of the earliest manifestations of hypoglycemia; the combined appointment required constant monitoring of blood glucose. |
Insulin dvuhfaznыy [human genetic engineering] | FMR: antagonizm. Against the background of the effect of sotalol enhanced, can disguise the early symptoms of hypoglycemia; the combined appointment required constant monitoring of blood glucose. |
Clarithromycin | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Clomipramine | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Klonidin | FMR. Strengthens (mutually) effects, incl. side: more significant decreases in blood pressure, compounded bradycardia and AV block increases the probability. |
Lidokain | FKV. Against the backdrop of increased plasma levels of sotalol. |
Magnesium oxide | FKV. FMR. It slows down and reduces the absorption of its completeness, reduces Cmax and AUC - the effect falls; the combined appointment interval between doses should be at least 2 no. |
Maprotilin | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Methyldopa | FMR: synergism. Strengthens (mutually) hypotensive effect, exacerbates bradycardia, It increases the likelihood of AV block. |
Metformin | FMR: synergism. Against the background of the effect of sotalol enhanced, possible masking of the early symptoms of hypoglycemia, in particular, tachycardia; the combined appointment is necessary to control the level of glucose in the blood. |
Nimodipine | FMR: synergism. Strengthens (mutually) effects, incl. negative (possible deterioration of AV conduction and ventricular contractility, development of hypotension); combined use is not recommended. |
Nifedipine | FMR: synergism. Strengthens (mutually) effects, incl. negative (possible deterioration of AV conduction and ventricular contractility, development of hypotension); combined use is not recommended. |
Norepinephrine | FMR. The joint appointment raises blood pressure, may develop excessive bradycardia. |
Octreotide | FMR: synergism. May enhance the therapeutic and side (usugublenie bradycardia, Arrhythmia, conduction disorders) effects; with a joint appointment needed dose reduction. |
Perfenazyn | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Pioglitazone | FMR. Against the background of the effect of sotalol enhanced, can mask the early symptoms of hypoglycemia (tachycardia); the combined appointment required monitoring of blood glucose concentration. |
Prokaynamyd | FMR: synergism. Against the background of sotalol significantly prolonged refractory period; concomitant use is not recommended. |
Promethazine | FMR. Increases (mutually) plasma levels, It increases the likelihood of adverse effects on the cardiovascular system (QT prolongation, ventricular arrhythmias, excessive hypotension et al.); concomitant use is not recommended. |
Repaglinide | FMR: synergism. Against the background of the effect of sotalol enhanced, possible masking of the early symptoms of hypoglycemia, in particular, tachycardia; with a joint appointment requires constant monitoring of blood glucose. |
Risperidone | FMR: synergism. Enhances the hypotensive effect. |
Rifampicin | FKV. Intensifies biotransformation (while the appointment of sotalol metabolites are not more than 1%) and decreases blood levels. |
Rosiglitazone | FMR. Against the background of the effect of sotalol enhanced, may mask the symptoms of hypoglycemia early (tachycardia); the combined appointment requires monitoring of blood glucose. |
Salmeterol | FMR: antagonizm. Against the background of weakened bronchodilator effect of sotalol; the combined appointment may require higher doses. |
Theophylline | FMR: antagonizm. Against the background of the effect of sotalol is reduced. |
Tioridazin | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Trifluoperazine | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Felodipine | FMR: synergism. Strengthens (mutually) gipotenziю, slows AV conduction and ventricular contractility deterioration. |
Flufenazin | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Quinidine | FMR: synergism. Against the background of sotalol significantly prolonged refractory period; concomitant use is not recommended. |
Chlorpromazine | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Epinephrine | FMR: antagonizm. Against the background of the effect of sotalol is reduced; It requires the combined use of high doses. |
Erythromycin | FMR. Удлиняет интервал QT; concomitant use is not recommended. |
Ephedrine | FMR: antagonizm. Against the background of the effect of sotalol is reduced; It requires the combined use of high doses. |