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β-Adrenergic
Blockers
Dr. Hiwa K. Saaed
Ph.D. Pharmacology
& Toxicology
β-Adrenergic Blockers
β-Blockers are effective in treating :
• angina,
• cardiac arrhythmias,
• myocardial infarction,
• congestive heart failure,
• hyperthyroidism,
• and glaucoma,
• prophylaxis of migraine headaches.
Note: The names of all β-blockers end in “olol” except for
labetalol and carvedilol.
β-Blockers
• All are competitive antagonists
• Propranolol is prototype
• Although all β-blockers lower blood pressure
in hypertension, they do not induce postural
hypotension,
• because the α-adrenoceptors remain
functional.
A. Classification and Mechanisms
Selectivity (β1>β2)
Partial agonist activity (Intrinsic
Sympathomimetic Activity “ISA”)
Lipid solubility (CNS effect)
Membrane stabilizing activity (MSA)
(local anesthetic action)
Capacity to block alpha adrenoceptors.
K+ channel blockade (sotalol)
A. Classification: Selectivity (β1>β2)
• β1 selective (cardioselective)
• Atenolol
• Acebutolol
• Bisoprolol
• Esmolol (short t1/2)
• Metoplrolol
Advantage: HTN with asthma, peripheral
vascular disease (coldness of
extremities), NIDDM
A. Classification and Mechanisms
Selective β2
• Butoxamine (experimental)
Nonselective (β1 & β2)
• Nadolol
• Propranolol
• Timolol
Combined (α & β): peripheral vasodilation
• Labetalol
• Carvedilol
• Useful in Rx HTN patients for whom increased
Peripheral resistance is undesirable (elderly or black)
• Labetalol in Rx preeclampsia, pheochromocytoma
• They do not alter serum lipid or blood glucose levels
• Carvedilol also decreasees lipid peroxidation and
vascular wall thickening (benefit in heart failure)
Partial agonist activity ISA
• Pindolol
• Acebutolol
• Labetalol
less bradycardia & diminished effect on COP,
less disturbances of lipid and carbohydrate
metabolism
Advantages:
• HTN with asthma,
• HTN with moderate bradycardia
• HTN+DM
A. Classification and Mechanisms
3. Local anesthetic activity (membrane-stabilizing
activity):
– Is a disadvantage when used topically in the eye
because it decreases protective reflexes and increases
the risk of corneal ulceration
– Timolol, atenolol, carvedilol &nadolol: no Local
anesthetic activity
4. Lipid solubility
– responsible for CNS adverse effects: propranolol
Lipid soluble Pharmacokinetic properties Water soluble Pharmacokinetic properties
Propranolol Highly metabolized
Large Vd
CNS penetration
Shorter t1/2
Acebutolol Excreted unchanged by
kidney
Less 1st pass effect
Small Vd
Longer t1/2 except esmolol
Timolol Atenolol
Pindolol Esmolol
Metoprolol Nadolol
Labetalol
K+ channel blockade: sotalol
• Sotalol is a nonselective β receptor antagonists,
• that lack LA action
• but has marked class III antiarrhythmia effect reflecting k+ channel
blockade
B. Pharmacological Effects and Clinical Uses
1. CVS:
A. Heart: both
– decreased HR, force of contraction (–ve inotropic &
chronotropic effect)
– decreased A-V conduction, ↑PR interval
– Decrease CO, work & O2 consumption
Rx: Angina and Supraventricular tachycardia
Reflex peripheral vasoconstriction!?
B. Vascular system: prevent β2 mediated vasodilation→
reduction in COP (because of cardiac effect) → decrease
BP → reflex vasoconstriction.
• On balance there is gradual reduction of both systolic and
diastolic BP
2. Respiratory: bronchoconstriction; contraindicated in asthma
3. Eye: reduce IOP especially in Glaucomatous eyes decrease
aqueous humor production
B. Pharmacological Effects and Clinical Uses
4. metabolic and endocrine effects:
A. Increased Na+ retention, how?
– Reduced blood pressure causes a decrease in renal perfusion, resulting in
an increase in Na+ retention and ↑plasma volume→
– In some cases, ↑blood pressure.
– For these patients, β-blockers are often combined with a diuretic to
prevent Na+ retention.
– Also by inhibiting β receptors, renin production is also prevented,
contributing to Na+ retention.
B. Pharmacological Effects and Clinical Uses
B. inhibit lipolysis: ↑ plasma VLDL, ↓ HDL, ─LDL
↓ HDL/LDL ratio→ coronary heart disease
C. partially inhibit glycogenolysis and decrease glucagon secretion
• Great caution in IDDM (Type 1)?
• Because pronounce hypoglycemia may occur after insulin injection,
β blockers also attenuate the normal physiologic response to
hypoglycemia, furthermore they mask signs of hypoglycemia; tremor,
palpitation..
B. Pharmacological Effects and Clinical Uses
B. Clinical Uses
Cardiovascular and ophthalmic applications are extremly important
A. CVS:
-angina pectoris ↓cardiac work & O2 demand,
-Chronic hypertension, ↓CO, ↓ TPR, inhibition of renin
release
NB: β blockers are not used for acute or emergency Rx of HTN,? ma y
increase diastolic pressure
Labetalol is effective in emergency
-Arrhythmia (supraventricular tachycardias),
-prophylaxis after MI:
1) early use within 6-12 hrs for 3-4 wks
2) Late use within 4 days- 4 wks after onset of infarction and
continued for at least 2 years useful for secondary prevention
from another MI
- congestive heart failure*
B. Clinical Uses
B. Eye: Glaucoma: reduce aqueous humor secretion (timolol)
C. Endocrine use: Thyroid storm, thyrotoxicosis: propranolol
D. CNS: propranolol
1. Anxiety with somatic symptoms
2. Migraine headache prophylaxis:
3. Famillial tremor, other types of tremor, “stage fright”:
4. Alcohol, opioids acute withdrawal symptoms
B. Clinical Uses
C. Adverse effects
• CVS: bradycardia, A-V blockade, CHF
• Arrhythmias: never stop Rx with β blockers
suddenly
• Bronchoconstriction: Patients with airway
disease: asthmatic attack
• Sexual dysfunction?? Indep of β blockade
• CNS effects: sedation, fatigue, sleep
alterations
Thank You

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L8: B-adrenergic blockers

  • 1. β-Adrenergic Blockers Dr. Hiwa K. Saaed Ph.D. Pharmacology & Toxicology
  • 2.
  • 3. β-Adrenergic Blockers β-Blockers are effective in treating : • angina, • cardiac arrhythmias, • myocardial infarction, • congestive heart failure, • hyperthyroidism, • and glaucoma, • prophylaxis of migraine headaches. Note: The names of all β-blockers end in “olol” except for labetalol and carvedilol.
  • 4. β-Blockers • All are competitive antagonists • Propranolol is prototype • Although all β-blockers lower blood pressure in hypertension, they do not induce postural hypotension, • because the α-adrenoceptors remain functional.
  • 5. A. Classification and Mechanisms Selectivity (β1>β2) Partial agonist activity (Intrinsic Sympathomimetic Activity “ISA”) Lipid solubility (CNS effect) Membrane stabilizing activity (MSA) (local anesthetic action) Capacity to block alpha adrenoceptors. K+ channel blockade (sotalol)
  • 6. A. Classification: Selectivity (β1>β2) • β1 selective (cardioselective) • Atenolol • Acebutolol • Bisoprolol • Esmolol (short t1/2) • Metoplrolol Advantage: HTN with asthma, peripheral vascular disease (coldness of extremities), NIDDM
  • 7. A. Classification and Mechanisms Selective β2 • Butoxamine (experimental) Nonselective (β1 & β2) • Nadolol • Propranolol • Timolol
  • 8. Combined (α & β): peripheral vasodilation • Labetalol • Carvedilol • Useful in Rx HTN patients for whom increased Peripheral resistance is undesirable (elderly or black) • Labetalol in Rx preeclampsia, pheochromocytoma • They do not alter serum lipid or blood glucose levels • Carvedilol also decreasees lipid peroxidation and vascular wall thickening (benefit in heart failure)
  • 9. Partial agonist activity ISA • Pindolol • Acebutolol • Labetalol less bradycardia & diminished effect on COP, less disturbances of lipid and carbohydrate metabolism Advantages: • HTN with asthma, • HTN with moderate bradycardia • HTN+DM
  • 10. A. Classification and Mechanisms 3. Local anesthetic activity (membrane-stabilizing activity): – Is a disadvantage when used topically in the eye because it decreases protective reflexes and increases the risk of corneal ulceration – Timolol, atenolol, carvedilol &nadolol: no Local anesthetic activity
  • 11. 4. Lipid solubility – responsible for CNS adverse effects: propranolol Lipid soluble Pharmacokinetic properties Water soluble Pharmacokinetic properties Propranolol Highly metabolized Large Vd CNS penetration Shorter t1/2 Acebutolol Excreted unchanged by kidney Less 1st pass effect Small Vd Longer t1/2 except esmolol Timolol Atenolol Pindolol Esmolol Metoprolol Nadolol Labetalol
  • 12. K+ channel blockade: sotalol • Sotalol is a nonselective β receptor antagonists, • that lack LA action • but has marked class III antiarrhythmia effect reflecting k+ channel blockade
  • 13. B. Pharmacological Effects and Clinical Uses 1. CVS: A. Heart: both – decreased HR, force of contraction (–ve inotropic & chronotropic effect) – decreased A-V conduction, ↑PR interval – Decrease CO, work & O2 consumption Rx: Angina and Supraventricular tachycardia
  • 14. Reflex peripheral vasoconstriction!? B. Vascular system: prevent β2 mediated vasodilation→ reduction in COP (because of cardiac effect) → decrease BP → reflex vasoconstriction. • On balance there is gradual reduction of both systolic and diastolic BP
  • 15. 2. Respiratory: bronchoconstriction; contraindicated in asthma 3. Eye: reduce IOP especially in Glaucomatous eyes decrease aqueous humor production B. Pharmacological Effects and Clinical Uses
  • 16. 4. metabolic and endocrine effects: A. Increased Na+ retention, how? – Reduced blood pressure causes a decrease in renal perfusion, resulting in an increase in Na+ retention and ↑plasma volume→ – In some cases, ↑blood pressure. – For these patients, β-blockers are often combined with a diuretic to prevent Na+ retention. – Also by inhibiting β receptors, renin production is also prevented, contributing to Na+ retention. B. Pharmacological Effects and Clinical Uses
  • 17. B. inhibit lipolysis: ↑ plasma VLDL, ↓ HDL, ─LDL ↓ HDL/LDL ratio→ coronary heart disease C. partially inhibit glycogenolysis and decrease glucagon secretion • Great caution in IDDM (Type 1)? • Because pronounce hypoglycemia may occur after insulin injection, β blockers also attenuate the normal physiologic response to hypoglycemia, furthermore they mask signs of hypoglycemia; tremor, palpitation.. B. Pharmacological Effects and Clinical Uses
  • 18. B. Clinical Uses Cardiovascular and ophthalmic applications are extremly important A. CVS: -angina pectoris ↓cardiac work & O2 demand, -Chronic hypertension, ↓CO, ↓ TPR, inhibition of renin release NB: β blockers are not used for acute or emergency Rx of HTN,? ma y increase diastolic pressure Labetalol is effective in emergency
  • 19. -Arrhythmia (supraventricular tachycardias), -prophylaxis after MI: 1) early use within 6-12 hrs for 3-4 wks 2) Late use within 4 days- 4 wks after onset of infarction and continued for at least 2 years useful for secondary prevention from another MI - congestive heart failure* B. Clinical Uses
  • 20. B. Eye: Glaucoma: reduce aqueous humor secretion (timolol) C. Endocrine use: Thyroid storm, thyrotoxicosis: propranolol D. CNS: propranolol 1. Anxiety with somatic symptoms 2. Migraine headache prophylaxis: 3. Famillial tremor, other types of tremor, “stage fright”: 4. Alcohol, opioids acute withdrawal symptoms B. Clinical Uses
  • 21. C. Adverse effects • CVS: bradycardia, A-V blockade, CHF • Arrhythmias: never stop Rx with β blockers suddenly • Bronchoconstriction: Patients with airway disease: asthmatic attack • Sexual dysfunction?? Indep of β blockade • CNS effects: sedation, fatigue, sleep alterations