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SOTALOL 120

Product Name:
SOTALOL 120
Composition:

Sotalol HCL 120 mg.

Pharmaceutical Form:

Tablets

Packing:

20 Tabs.

Public Price:

 65 sp

Pharmacist Price:

 50.45 sp

Pharmacologic Category:

Cardiac

Properties:

SOTALOL is an antiarrhythmic drug with Class II (beta-adrenoreceptor blocking) and Class III (cardiac action potential duration prolongation) properties.

<B>Mechanism of action:</B>
Sotalol is beta – blocker which contains both beta-adrenorecptor-blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation(Vaughan Williams Class II) properties.
Class II effects: Increased sinus cycle length, slowed heart rate, decreased A-V nodal refractoriness.
Class III effects: Prolongation of the atrial and ventricular monophasic action potentials, and effective refractory prolongation of atrial muscle, ventricular muscle, and atrioventricular accessory pathways in both the antegeade and retrograde directions.

Sotalol is a racemic mixture of d-and l-sotalol; both isomers have similar Class III antiarrhythmic effects while the l-isomer is responsible for virtually all of the beta-blocking activity.

The beta-blocking effect of Sotalol is a noncardioselective. Siginificant beta-blocked occurs at oral doses as low as 25 mg/day. The Class III effects are seen only at oral doses 160 mg/days.

</B>Pharmacodynamics/Kinetics:</B>
Onset of action: Rapid, 1-2 hours.
Absorption: Deceased 20% to 30% by meals compared to fasting.

Didtribution: Low lipid solubility; Sotalol is excreted in the milk of laboratory animals and reported to be present in human milk.

Elimination: Unchanged through kidney.

Indications:

1- SOTALOL (Sotalol hydrochloride) is indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that in the judgment of the physician are life-threatening.

Initiation of SOTALOL treatment or increasing doses, as with other should be carried out in the hospital. The response to treatment should then be evaluated by a suitable method prior to continuing the patient on chronic therapy.

2- It is also indicated for the prophylaxis of paroxysmal atrial tachycardia or fibrillation, paroxysmal AV reentrant tachycardias (both nodal and involving accessory pathways), paroxysmal supraventricular tachycardia after cardiac surgery, maintenance of since rhythm following cardioversion of atrial fibrillation or flutter.

Antiarrhythmic drugs have not been show to enhance survival in patients with ventricular arrhythmias.

Contraindications:

SOTALOL is contraindicated in patients with bronchial asthma, sinus bradycardia, second and third degree AV block, unless a functioning pacemaker is present, congenital or acquired long QT syndromes, cardiogenic shock, uncontrolled condestive heart failure, and previous evidence of hypersensitivity to SOTALOL.

Side Effects:

1- Cardiovascular: Bradycardia, chest pain, palpitions.
2- Central nervous system: Fatigue, dizziness.
3- Neuromusclar and skeletal: Weakness.

And there are some rare side effects, which are:
1- Cardiovascular: Congestive heart failure, reduced peripheral circulation, edema, abnormal EKD, hypotension, proaahythmia, syncope.
2- Central nervous system: Mental confusion, anxiety, headache, sleep problems, depression.
3- Dermatologic: Itching/ rash.
4- Endocrine and metabolic: Decreased sexual ability.
5- Gastrointinal: Diarrhea, nausea/ vomiting, stomach discomfort.
6- Hematologic: Bleeding.
7- Neuromuscular and skeletal: Paresthesia.
8- Ocular:Visual problems.
9- Respiratory: Upper repiratory problems, asthma.

Other very rare side effects are:
Raynaud\'s phenomenon, red, crusted skin, skin necrosis after extravasation; leucopenia, phlebitis, diaphoresis, cold extremities.

Precautions:

SOTALOL should be cautiously used in patients with: Sick sinus syndrome, CHF, left ventricular dysfunction, recent MI, diabetes, thyroid disorders.
Correct electrolyte imbalances and withdraw other antiarrhythmics before starting. Avoid abrupt cessation if possible.

Famales, excessive QT prolongation, history of cardiomegaly, CHF increase risk of arrhythmias.

<B>Pregnancy and lactation:</B>
Although there are no adequate and well controlled studies in pregnant women, SOTALOL has been shown to cross the placenta, and id found in amniotic fluid. Therefore, Sotalol should be used during pregnancy only if the potential benefit outweighs the potential risk.

SOTALOL is not recommended to nursing mothers.
Proarrhythima: Like other antiarrhythmic agents, SOTALOL can provoke newor worsened ventricular arrhythmias in some patients, including sustained ventricular tachycardia or ventricular fibrillation, with potentially fatal consequences. Because of its effect on cardiac repolarization (QTc interval prolongation), torsade de pointes, a polymorphic ventricular tachycardia with prolongation of the QT interval and a shifting electrical axis is the most common form of proarrhythmia associated with SOTALOL, occurring about 4% of high risk (history of sustained VT/VF) patients. The risk of torsade de pointes progressively increases with prolongation of the QT interval, and is worsened also by reduction in heart rate and reduction in serum potassium.

In patients with a history of sustained ventricular tachycardia, the incidence of torsade de pointes was 4% and worsened VT in about 1%; in patients with other,less serious, ventricular arrhythmias and supraventricular arrhythmias, the incidence of torsade de pointes was 1% and 1.4% respectively.

Drug Interactions:

Decreased effect of beta-blockers with aluminum salts, barbiturates, calcium salts, cholestyramine, colestipol, NSAIDs, penicillins(ampiciline), rifampin, salicylates and sulfinpyrazone due to decreased bioavailability and plasma levels.

Beta-blockers may decrease the effect of sulfonylureas and beta agonists. Increased effect/toxicity

if beta-blockers with calcium blockers (diltiazem, felodipine, nicardipine),contraceptives, flecainide, quinidine (in extensive metabolizers), ciprofloxacin.

Beta-blockers may increase the effect/toxicity of digoxin, flecainide, and other antiarrhythmics ( especially class IA), haloperidol, phenothiazines, acetaminophen, clonidine (hypertensive crisis after or during withdrawal of either agent),epinephrine (initial hypertensive episode followed by bradycardia),nifedipine and verapamil, lidocaine, ergots (peripheral ischemia),prazosin (postural hypotension),and catecholamine- depleting agents (reserpine and guanethidine).

Beta-blockers may affect the action or levels of ethanol, disopyramide, nondepolarizing muscle relaxants and theophylline although the effects are difficult to predict.

Avoid use of SOTALOL with sparfloxacin, terfenadine, and astemizole since risk of cardiotoxicity may be increased.

Dosage:

As with other antiarrhythmic agents, SOTALOL should be initiated and doses increased in a hospital with facilities for cardiac rhythm monitoring and assessment.

SOTALOL should be administered only after appropriate clinical assessment, and the dosage of SOTALOL must be individualized for each patient on the basis of therapeutic response and tolerance. Proarrhythmic events can occur not only atinitiation of therapy, but also witheach upward dosage adjustment.

Dosage of SOTALOL should be adjusted gradually, allowing 2-3 days between dosing increments in order to attain steady-state plasma concentrations, and to allow monitoring of QT intervals.

Graded dose adjustment will help prevent the usage of doses which are higher than necessary to control the arrhythmia. The recommended initial dose is 80 mg twice daily.

This dose may be increased, if necessary, after appropriate evaluation to 240 or 320 mg/day (120-160 mg twice daily). In most patients, a therapeutic response is obtained at a total daily dose of 160 to 320 mg/day, given in two or three divided dose. Some patients with life-threatening refractory ventricular arrhythmias may require dose as high as 480-640 mg/day; however,

these doses should only be prescribed when the potential benefit outweighs the increased risk of adverse events, in particular proarrhthmia. Because of the long terminal elimination half-life of SOTALOL, dosing on more than a BID regimen is usually not necessary.

Dosage in renal impairment: Because sotalol is excreted predominantly in urine and is terminal elimination half-life is prolonged in conditions of renal impairment,

Since the terminal elimination half-life of SOTALO is increased in patients with renal impairment,a longer duration of dosing is requiredto reach steady-state. Dose escalations in renal impairment should be done after administration of at least 5-6 doses at appropriate intervals (see table above).

Extreme caution should be exercised in the use of SOTALOL in patients with renal failure undergoing hemodialysis. The half-life of SOTALOL is prolonged (up to 69 hours) in anuric patients. SOTALOL, however, can be party removed by dialysis with subsequent partial rebound in concentrations

when dialysis is completed. Both safety (heart rate, QT interval)and efficacy (arrhythmia control) must be closely monitored.

Transfer to SOTALOL: Before starting SOTALOL, previous antiarrhythmic therapy should generally be withdrawn under careful monitoring for a minimum of 2-3 plasma half-lives if the patient\\\\\\\\\\\\\\\'s clinical condition permits. Treatment has ben initiated in some patients receiving I.V. lidocaine without ill effect. After discontinuation of amiodarone, SOTALOL should not be initiated until the QT interval is normalized.

Over Dosage:

Intentional or accidental overdosage with SOTALOL (Sotalol hydrochloride) has rarely resulted in death.

Symptoms and treatment of overdosage: The most common signs to be expected are bradycardia, congestive heart failure, hypotension, bronchospasm and hypoglycardia.

In cases of massive intentional overdosage (2-16 grams)of SOTALOL the following clinical findings were seen: hypotension, bradycardia, cardiac asystole, prologation of QT interval, torsade de pointes, ventricular tachycardia, and premature ventricular complexes.

If overdosage occurs, therapy with SOTALOL should be discontinued and the patient observed closely. Because of the lack of protein binding, hemodialysis is useful for reducing SOTALOL plasma concentrations. Patients should be carefully observed until QT intervals are normalized and the heart rate returns to levels >50 bpm.