5. Questions
1. What is happening when β1 receptor is
activated?
2. What is happening when β2 receptor is
activated?
6. Answers
1. Activation of the β1 receptor leads to
increases in contraction force and heart
rate (In Heart).
2. Activation of the β2 receptor leads to
smooth muscle relaxation (In Lung).
8. Non selective Selective
Causes bronchoconstriction
So not safe for asthma patients
Does not cause bronchoconstriction
So safe for asthma patients
Decreases insulin secretion &
impairs insulin sensitivity.
Thus Increases blood sugar
level, even may causes new
onset of diabetes
Not safe for Diabetes patients
Does not decrease insulin secretion &
impair insulin sensitivity
Does not increase blood sugar level
,does not cause new onset of diabetes
Safe for Diabetes patients
Has unfavorable effect on
Blood lipid profile
Has no effect on blood lipid profile
9. Generatio
n
Selectivity Generic
1st Non selective beta blocker (blocks both
β1 & β2)
Propanolol
2nd Selective beta blocker (blocks only β1 )
cardioselective
Atenolol ( Tenoloc),
Metoprolol,
Bisoprolol
3rd Beta blocker + Vasodilatory activity
1. Non selective beta blocker (blocks
both β1 & β2) and α blocker activity
(Vasodilation)
2. Selective beta blocker (blocks only
β1) and α blocker activity
(Vasodilation)
1. Carvedilol
(Carvipress)
2. Nevibolol
10. Indications
Indicated in the management of
Hypertension
Angina.
It may be used alone or in combination with other
antihypertensive agents
11. Mechanism of Action
Bisoprolol is the most potent β1-selective β-blocker. It has
the highest level of β1-selectivity and by blocking the
heart’s β1 adrenergic receptors it reduces heart rate &
force of contraction of the heart, thus lowers blood
pressure.
13. The dose of Betabis must be individualized to the needs of the
patient. The usual starting dose is Betabis 5 mg once daily. In
some patients, Betabis 2.5 mg may be an appropriate starting
dose. If the antihypertensive effect of Betabis 5 mg is
inadequate, the dose may be increased to Betabis 10 mg and
then, if necessary, to 20 mg once daily.
Patients with renal or Hepatic Impairment : In patients with
hepatic impairment (hepatitis or cirrhossis) or renal dysfunction
(creatinine clearance <40 mL/min), the initial daily dose should be
2.5 mg and caution should be used in dose-titration Since limited
data suggest that Bisopolol hemifumarate is not dialyzable, drug
replacement is not necessary in patients undergoing dialysis.
14. Geriatric Patients: It is not necessary to adjust the dose in the
elderly, unless there is also significant renal or hepatic
dysfunction.
OR AS DIRECTED BY THE PHYSICIAN.
15. Side effects
Fatigue, dizziness, headache, sleep disturbance,
bronchospasm, peripheral vasoconstriction, gastro-
intestinal disturbances, bradycardia and worsening
of heart failure.
16. USE IN PREGNANCY &
LACTATION
There are no adequate and well controlled studies
of safety evidence in pregnant women. Therefore,
Bisoprolol should be used during pregnancy only if
the potential benefit justifies the potential risk to the
fetus.
It is not known whether this drug is excreted in
human milk and therefore caution should be
exercised when Bisoprolol is administered to
nursing women.
19. Highlighting Points
Betabis…
◙ Possesses the highest β1-selectivity
◙ Effectively controls high blood pressure and angina
◙ Shows no impact on lipid parameters
◙ Does not effect blood glucose level
◙ Safe for asthma patients
20.
21.
22.
23.
24. Ohm's law (For calculation of Airway resistance)
R = resistance
Pmouth = Maximum airway pressure in cm H2O pressure
Palveoli = Static airway pressure in cm H2O pressure
V = Volume rate L/sec
25. Positioning of Beta blockers
Tenoloc (Atenolol) Betabis (Bisoprolol) Betaone (Metoprolol)
Cardioselective beta blocker Cardioselective beta blocker possesses Highest β1
selectivity
Cardioselective beta blocker
Effective in hypertension and angina
pectoris
Controls high BP and angina pectoris better than
Tenoloc and Betaone
Effective in hypertension & angina
Shows no impact on Lipid parameters
Does not effect on blood glucose level
(Better for Diabetic hypertensive patients)
Controls arrhythmia effectively
Comparatively Safe for asthma patients Ensure post infarct protection & lowers the
risk of reinfarction
Effective beta blocker for heart failure
patients
Cost effective
Unit price
Atenolo 50 – 0.77tk
Atenolo 100 – 1.34tk
Unit price
Betabis 2.5 – 6.00tk
Betabis 5 – 10.00tk
Unit price
Betaone 50 – 2.00tk