Brand name: Sota Hexal
Active ingredient (generic name): Sotalol
Manufacturer: Hexal
Importer: Behestan Darou
Pharmacotherapeutic group: anti arrhythmia
Pharmaceutical form: 80mg tablets
,l-sotalol is a non-selective hydrophilic β-adrenergic receptor blocking agent, devoid of intrinsic sympathomimetic activity or membrane stabilising activity.
sotalol has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. Sotalol has no known effect on the upstroke velocity and therefore no effect on the depolarisation phase.
Sotalol uniformly prolongs the action potential duration in cardiac tissues by delaying the repolarisation phase. Its major effects are prolongation of the atrial, ventricular and accessory pathway effective refractory periods.
The Class II and III properties may be reflected on the surface electrocardiogram by a lengthening of the PR, QT and QTc (QT corrected for heart rate) intervals with no significant alteration in the QRS duration
Pharmacokinetic:
The bioavailability of oral sotalol is essentially complete (greater than 90%). After oral administration, peak levels are reached in 2 to 4 hours, and steady-state plasma levels are attained within 2-3 days. The absorption is reduced by approximately 20% when administered with a standard meal, in comparison to fasting conditions. Distribution occurs to a central (plasma) and a peripheral compartment, with an elimination half-life of 10-20 hours. Sotalol does not bind to plasma proteins and is not metabolised. There is very little inter-subject variability in plasma levels. Sotalol crosses the blood brain barrier poorly, with cerebrospinal fluid concentrations only 10% of those in plasma. The primary route of elimination is renal excretion.
Therapeutic indication:
Sotalol 80mg Tablets are indicated for:
1. Ventricular arrhythmias:
• Treatment of life-threatening ventricular tachyarrhythmias;
• Treatment of symptomatic non-sustained ventricular tachyarrhythmias
2. Supraventricular arrhythmias:
• Prophylaxis of paroxysmal atrial tachycardia, paroxysmal atrial fibrillation, paroxysmal A-V nodal re-entrant tachycardia, paroxysmal A-V re-entrant tachycardia using accessory pathways, and paroxysmal supraventricular tachycardia after cardiac surgery;
• Maintenance of normal sinus rhythm following conversion of atrial fibrillation or atrial flutter
Dosage and administration:
The initial dose is 80 mg, administered either singly or as two divided doses.
Oral dosage of Sotalol should be adjusted gradually allowing 2-3 days between dosing increments in order to attain steady-state, and to allow monitoring of QT intervals. Most patients respond to a daily dose of 160 to 320 mg administered in two divided doses at approximately 12 hour intervals. Some patients with life-threatening refractory ventricular arrhythmias may require doses as high as 480 - 640 mg/day. These doses should be used under specialist supervision and should only be prescribed when the potential benefit outweighs the increased risk of adverse events, particularly proarrhythmias.
Adverse reaction:
The most frequent adverse effects of sotalol arise from its beta-blockade properties. Adverse effects are usually transient in nature and rarely necessitate interruption of, or withdrawal from treatment. If they do occur, they usually disappear when the dosage is reduced. The most significant adverse effects, however, are those due to proarrhythmia, including torsades de pointes (see Warnings).
The following are adverse events considered related to therapy, occurring in 1% or more of patients treated with sotalol.
Cardiovascular
Bradycardia, dyspnoea, chest pain, palpitations, oedema, ECG abnormalities, hypotension, proarrhythmia, syncope, heart failure, presyncope.
Dermatologic
Rash
Gastro-intestinal
Nausea/vomiting, diarrhoea, dyspepsia, abdominal pain, flatulence
Musculoskeletal
Cramps
Nervous/psychiatric
Fatigue, dizziness, asthenia, lightheadedness, headache, sleep disturbances, depression, paraesthesia, mood changes, anxiety
Urogenital
Sexual dysfunction
Special Senses
Visual disturbances, taste abnormalities, hearing disturbances
Body as a whole
Fever
In trials of patients with cardiac arrhythmia, the most common adverse events leading to discontinuation of sotalol were fatigue 4%, bradycardia ( <50 bpm) 3%, dyspnoea 3%, proarrhythmia 2%, asthenia 2%, and dizziness 2%.
Cold and cyanotic extremities, Raynaud's phenomenon, increase in existing intermittent claudication and dry eyes have been seen in association with other beta-blockers.
Pharmacokinetic interactions:
Class 1a antiarrhythmic drugs, such as disopyramide, quinidine and procainamide and other antiarrhythmic drugs such as amiodarone and bepridil are not recommended as concomitant therapy with sotalol, because of their potential to prolong refractoriness
Sota Hexal Tablets should be given with extreme caution in conjunction with other drugs known to prolong the QT-interval such as phenothiazines, tricyclic antidepressants, terfenadine and astemizole. Other drugs that have been associated with an increased risk for torsades de pointes include erythromycin IV, halofantrine, pentamidine, and quinolone antibiotics.
The concomitant use of other beta-blocking agents with sotalol may result in additive Class II effects.Concurrent administration of beta-blocking agents and calcium channel blockers has resulted in hypotension, bradycardia, conduction defects, and cardiac failure.
Contraindication:
Contraindicated Combination:
sick sinus syndrome , second and third degree AV heart block unless a functioning pacemaker is present , congenital or acquired long QT syndromes , torsades de pointes , symptomatic sinus bradycardia , uncontrolled congestive heart failure , cardiogenic shock , anaesthesia that produces myocardial depression , untreated phaeochromocytoma , hypotension (except due to arrhythmia), Raynaud's phenomenon and severe peripheral circulatory disturbances , history of chronic obstructive airway disease or bronchial asthma, hypersensitivity to any of the components of the formulation , metabolic acidosis , renal failure (creatinine clearance < 10 ml/min).
Sotalol should not be administered in combination with drugs like class Ia antiarrhythmics, class II antiarrhythmics such as amiodarone, dofetilide, ibutilide etc; neuroleptics such as trimipramine, phenobarbitone, chlorpromazine etc; and antibiotics such as erythromycin IV and moxifloxacin
Special warnings:
In patients already receiving sotalol caution should be used if the QTc exceeds 500msec whilst on therapy, and serious consideration should be given to reducing the dose or discontinuing therapy when the QTc-interval exceeds 550 msec. Due to the multiple risk factors associated with torsades de pointes, however, caution should be exercised regardless of the QTc-interval.
In view of its β-adrenergic blocking properties, treatment with sotalol should not be discontinued suddenly, especially in patients with ischaemic heart disease (angina pectoris, prior acute myocardial infarction) or hypertension, to prevent exacerbation of the disease.
As with other beta-blocking agents, Sota Hexal Tablets should be used with caution in patients undergoing surgery.
Pregnancy and lactation:
Sota Hexal should be used in pregnancy only if the potential benefits outweigh the possible risk to the foetus. Most beta-blockers, particularly lipophilic compounds, will pass into breast milk although to a variable extent. Breast feeding is therefore not recommended during administration of these compounds.
Storage temperature:
Do not store above 25°C. Store in original package.
Products