Teva-Sotalol

Uses

Arrhythmias, Cardiac arrhythmias, Supraventricular and ventricular arrhythmias

Teva-Sotalol is also used to associated treatment for these conditions: Atrial Fibrillation, Flutter, Atrial, Severe ventricular arrhythmias

How Teva-Sotalol works

Teva-Sotalol inhibits beta-1 adrenoceptors in the myocardium as well as rapid potassium channels to slow repolarization, lengthen the QT interval, and slow and shorten conduction of action potentials through the atria. The action of sotalol on beta adrenergic receptors lengthens the sinus node cycle, conduction time through the atrioventricular node, refractory period, and duration of action potentials.

Dosage

Teva-Sotalol dosage

Oral (Adult)-

Supraventricular and ventricular arrhythmias: Initial: 80 mg/day in 1 -2 divided doses, increase gradually every 2-3 days. Usual: 160-320 mg/day in 2 divided doses. Max: 640 mg/day.

Life-threatening ventricular arrhythmias: 480-640 mg/day.

Acute arrhythmias: 20-120 mg, may repeat 6 hrly if needed.

For programmed electrical stimulation (to test antiarrhythmic efficacy): Initial: 1.5 mg/kg, then 0.2-0.5 mg/kg/hr infusion

Side Effects

Dyspnea, Dizziness, Fatigue, Bradycardia, Chest pain, Palpitation, Weakness, Lightheadedness, Nausea/vomiting, Edema, Headache, Sleep disturbances, Abnormal ECG, Diarrhea, Extremity pain, Hypotension, Mental confusion, Congestive heart failure, ltching/rash, Syncope, Anxiety, Depression, Torsades de pointes or new ventricular tachycardia / fibrillation in patients with supraventricular arrhythmia, Peripheral vascular disorders, Impotence, Proarrhythmic effect, Torsades de pointes with history of sustained ventricular tachycardia, Catechol hypersensitivity after abrupt withdrawal, Increased insulin requirement in diabetics

Toxicity

Patients experiencing an overdose may present with bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia. Larger intentional overdoses may present as hypotension, bradycardia, cardiac asystole, prolonged QT interval, torsade de pointes, ventricular tachycardia, and premature ventricular complexes. Stop administering sotalol and observe the patient until the QT interval returns to normal and the heart rate rises above 50 beats per minute. Hemodialysis may help lower plasma concentrations of sotalol as it is not bound to plasma proteins. Bradycardia and cardiac asystole may be treated with atropine, other anticholinergic drugs, beta adrenergic agonists, or transvenous cardiac pacing.. Second or third degree heart block may be treated with a transvenous cardiac pacemaker. Hypotension may be treated with epinephrine or norepinephrine. Bronchospasm may be treated with aminophylline or a beta-2 agonist, possibly at higher than normal doses. Torsade de pointes may be treated with DC cardioversion, transvenous cardiac pacing, epinephrine, or magnesium sulfate.

The oral LD50 for rats is 3450mg/kg, intraperitoneal LD50 for rats is 680mg/kg, oral LD50 for mice is 2600mg/kg, and intraperitoneal LD50 for mice is 670mg/kg.

Pregnant rabbits given 6 times the maximum recommended human dose showed an increase in fetal death and maternal toxicity, while rats given 18 times the maximum recommended human dose had an increased number of fetal resorptions. Teva-Sotalol is present in human breast milk so patients taking sotalol should not breast feed.

Teva-Sotalol has not been found to be carcinogenic. No studies have been performed regarding mutagenicity or clastogenicity. In animal studies, sotalol was not associated with a reduction in fertility aside from smaller litter sizes.

Further information regarding adverse reactions can be found here.

Precaution

Patients with well-compensated heart failure, myasthenia gravis, DM, 1 st degree AV block. May mask symptoms of hyperthyroidism and hypoglycaemia. May worsen psoriasis. Patients undergoing major surgery requiring general anaesth. Avoid abrupt withdrawal as it may precipitate thyroid storm and exacerbate angina and Ml. Renal impairment. Pregnancy and lactation. Monitoring Parameters Monitor BP, heart rate, serum creatinine; Mg and K levels.

Interaction

May increase risk of bradycardia with digoxin. May increase risk of arrhythmias with diuretics. May potentiate rebound HTN with clonidine. May prolong refractoriness with disopyramide, quinidine, procainamide, amiodarone and bepridil. May prolong QT interval with TCAs, phenothiazines, terfenadine and astemizole. Increased risk of torsades de pointes with K-depleting diuretics, erythromycin IV, halofantrine, pentamidine, and quinolones. May prolong neuromuscular blockade of tubocurarine. May reduce response to insulin and oral hypoglycaemics.

Food Interaction

• Take with or without food. Oral sotalol with a meal reduces absorption by 20%.

Teva-Sotalol Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Teva-Sotalol Cholesterol interaction

[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.

Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.

Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.

Teva-Sotalol multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.

The exact mechanism of interaction is unknown.

In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.

The elimination half-life increased by 44%.

Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.

However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.

The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.

It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.

Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.

Teva-Sotalol Drug Interaction

Moderate: furosemide, alprazolamMinor: aspirin, aspirin, levothyroxineUnknown: ubiquinone, warfarin, rosuvastatin, apixaban, omega-3 polyunsaturated fatty acids, atorvastatin, metoprolol, esomeprazole, clopidogrel, dabigatran, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, rivaroxaban

Teva-Sotalol Disease Interaction

Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hypersensitivity, ischemic heart disease, PVD, asthma/COPD, hemodialysis, QT interval prolongation, renal dysfunctionModerate: cerebrovascular insufficiency, glaucoma, hyperlipidemia, hyperthyroidism, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, Prinzmetal's variant angina

Volume of Distribution

The apparent volume of distribution is 1.2-2.4L/kg.

Elimination Route

Teva-Sotalol is 90-100% bioavailable. When taken with a meal, adsorption is lowered by 18%. In patients with a creatinine clearance >80mL/min, the maximum concentration is 6.25±2.19.

Half Life

The terminal elimination half life is 10-20 hours in healthy patients. In patients with a creatinine clearance >80mL/min, the half life is 17.5±0.97h. In patients with a creatinine clearance 30-80mL/min, the half life is 22.7±6.4h. In patients with a creatinine clearance 10-30mL/min, the half life is 64±27.2h. In patients with a creatinine clearance 1

Clearance

In patients with a creatinine clearance >80mL/min, the plasma clearance is 6.78±2.72L/h and the renal clearance is 4.99±1.43L/h. In patients with a creatinine clearance 30-80mL/min, the plasma clearance is 2.74±0.53L/h and the renal clearance is 2.00±0.67L/h. In patients with a creatinine clearance 10-30mL/min, the plasma clearance is 1.56±0.44L/h and the renal clearance is 0.65±0.31L/h. In patients with a creatinine clearance 1

Elimination Route

80-90% of a given dose is excreted in the urine as unchanged sotalol. A small fraction of the doses is excreted in the feces as unchanged sotalol.

Pregnancy & Breastfeeding use

Pregnancy Category- D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Contraindication

Bronchial asthma or history of COPD, sick sinus syndrome, symptomatic sinus bradycardia, cardiogenic shock. 2nd and 3rd degree AV block, untreated phaeochromocytoma, torsades de pointes, congenital or acquired long QT syndromes, uncontrolled cardiac failure, cardiogenic shock, metabolic acidosis, hypotension, severe peripheral arterial disease, Raynaud's disease, anaesthesia that causes myocardial depression. Renal impairment (CrCI <10 mL/min). Concomitant use with Ca channel blockers (e.g. verapamil and diltiazem).

Innovators Monograph

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