about sotalol as a non selective b blocker drug

1. SOTALOL

2. MODE OF ACTION:
• Non-selective competitive beta-adrenergic receptor
blocker
• class III anti-arrhythmic properties

3. II - PHARMACOKINETICS
1- Absorption
It is well absorbed from the gastrointestinal tract.
Peak plasma concentrations of 1.4 to 1.7 mg/L are
reached at 2-3 hours after a 160mg oral dose.

4. • 2-Distribution
• Total apparent volume of distribution of Sotalol ranges
from 1.6 to 2.4 L/kg.

5. 3-Binding
It does not bind to plasma proteins and does not
significantly cross the blood-brain barrier.
However, it is excreted in breast milk and may cross
the placental barrier.

6. 4-Metabolism:
It is not metabolized by the liver and does not undergo
biotransformation
(no first-pass effect).

7. 5- Excretion
It is excreted by glomerular filtration and to a small
degree by tubular secretion.
After oral administration, about 75% of the dose is
excreted in the urine within 72 hours as unchanged
Sotalol.
Less than 10% is excreted in the feces.
The mean elimination half-life of Sotalol is 12.7 ± 1.6 (SE)
hours

8. III - PHARMACOLOGICAL
ACTION
Beta-receptor
blocked
Decrease in
intracellular
calcium
Decrease in
electrical signals of
contraction
Giving the the time
for pacemaker for
recitification of
contraction.

9. 2- TYPE III ANTI-
ARRHYTHMIC ACTION
It act on
potassium
channels
Blocking
potassium
channel
Increase in the
time before
another
electrical signal
Lengthening the
QT interval and
decreasing
automaticity
Slows (A.V)
nodal
conduction
Decrease the potential for prolonging the frequency of
premature or abnormal + ventricular contraction
contraction
Treat
tachycardia

10. IV - THERAPEUTIC USES
1- Indications
Anti-arrhythmic agent for treatment of ventricular and
supraventricular arrhythmias .
Sotalol is indicated for the maintenance of normal sinus rhythm
[delay in time to recurrence of atrial fibrillation/atrial flutter
(AFIB/AFL)]
in patients with symptomatic AFIB/AFL who are currently in
sinus rhythm.

11. 2- DOSE AND REGIMEN
The recommended initial oral dosing schedule is 160 mg daily,
given in two divided doses 1-2 hours before meal at
approximately 12-hour intervals.
This dose may be increased, if necessary, after appropriate
evaluation to 240 or 320 mg/day.
In most patients, a therapeutic response is obtained at a total
daily dose of 160-320 mg/day, given in 2 divided doses.
Some patients with life-threatening refractory ventricular
arrhythmias may require doses as high as 480-640 mg/day .

12. ADVERSE SIDE EFFECTS:
1- Bradycardia
2- Congestive Heart Failure
3-Hypotension
4-Bronchospasm
5-Hypoglycaemia
6-Fatigue
7-Dizziness
8- Headache

13. TOXICITY
In cases of massive intentional overdosage (2-16
grams) of Sotalol the following clinical findings were
seen:
1-Hypotension
2- Bradycardia
3-Cardiac asystole
4- Prolongation of QT interval
5-Torsade de Pointes
6-Ventricular tachycardia

14. PRECAUTIONS:
1- Not recommended if creatinine clearance is less than 40 mL/min .
2- Not to be taken in nursing mothers
3- Safety and effectiveness have not been established in pediatrics .
4-QT prolongation, bradycardia , AV block, hypotension, worsening
heart
failure: Reduce dose as needed
5- Acute exacerbation of coronary artery disease upon cessation of
therapy:
Do not abruptly discontinue
6- Correct any electrolyte disturbances
7-May mask symptoms of hypoglycemia or worsen hyperglycemia in
diabetic patients

15. VII - DRUG INTERACTIONS
1- Digoxin increases the risk of proarrhythmic events
2- Calcium blocking drugs may have additive effects on decreasing
atrioventricular conduction, ventricular function, and blood pressure
3- Concomitant use of catecholamine-depleting drugs may produce
hypotension, marked bradycardia, and syncope
4- Dosage of insulin or antidiabetic drugs may require adjustment
5- Dose of beta-2 receptor agonists may have to be increased
6- It may potentiate rebound hypertension after discontinuation of
clonidine
7-Aluminum or magnesium-based antacids reduce its exposure
8- It may interact with fingolimod