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Drugs Affecting
The Autonomic Nervous System(ANS)
β-Adrenergic Blockers
ANS Pharmacology
Lecture 7
Dr. Hiwa K. Saaed
College of Pharmacy/University of Sulaimani
2017-2018
β-Adrenergic Blockers
• β-Blockers are effective in treating:
• angina,
• cardiac arrhythmias,
• myocardial infarction,
• congestive heart failure,
• hyperthyroidism,
• and glaucoma,
• as well as serving in the prophylaxis of migraine headaches.
• Note: The names of all β-blockers end in “olol” except for labetalol and carvedilol.
• 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)
1. 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
Selective β2
• Butoxamine (experimental)
Nonselective (β1 & β2)
• Nadolol
• Propranolol
• Timolol
2, 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)
3. Partial agonist activity ISA
Pindolol, Acebutolol & Labetalol
less bradycardia & diminished effect on CO,
less disturbances of lipid and carbohydrate metabolism
Advantages:
• HTN with asthma,
• HTN with moderate bradycardia
• HTN+DM
4. 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
5. Lipid solubility
Lipid soluble
• Propranolol. Timolol. Pindolol
Metoprolol. Labetalol
Pharmacokinetic properties
• Highly metabolized
• Large Vd
• CNS penetration
• Shorter t1/2
WATER SOLUBLE
• Acebutolol, Atenolol, Esmolol,
Nadolol
Pharmacokinetic properties
• Excreted unchanged by kidney
• Less 1st pass effect
• Small Vd
• Longer t1/2 except esmolol
6. K+ channel blockade: sotalol
• Sotalol is a nonselective β receptor antagonists,
• that lack Local Anesthetic 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
B. Vascular system: prevent β2 mediated vasodilation→ reduction in CO
(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
4. metabolic and endocrine effects:
A. Increased Na+ retention, how?
• Reduced BP causes a decrease in renal perfusion, resulting in an increase in Na+
retention and ↑plasma volume → In some cases, ↑BP.
• 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..
4. metabolic and endocrine effects:
B. Pharmacological Effects and 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,? may increase diastolic pressure
Labetalol is effective in emergency HTN
-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. 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. Pharmacological Effects and 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?? Independent of β blockade
• CNS effects: sedation, fatigue, sleep alterations
L7 ans pharmacology 17 18

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L7 ans pharmacology 17 18

  • 1. Drugs Affecting The Autonomic Nervous System(ANS) β-Adrenergic Blockers ANS Pharmacology Lecture 7 Dr. Hiwa K. Saaed College of Pharmacy/University of Sulaimani 2017-2018
  • 2.
  • 3. β-Adrenergic Blockers • β-Blockers are effective in treating: • angina, • cardiac arrhythmias, • myocardial infarction, • congestive heart failure, • hyperthyroidism, • and glaucoma, • as well as serving in the prophylaxis of migraine headaches. • Note: The names of all β-blockers end in “olol” except for labetalol and carvedilol. • 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.
  • 4. 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)
  • 5. 1. 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 Selective β2 • Butoxamine (experimental) Nonselective (β1 & β2) • Nadolol • Propranolol • Timolol
  • 6. 2, 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)
  • 7. 3. Partial agonist activity ISA Pindolol, Acebutolol & Labetalol less bradycardia & diminished effect on CO, less disturbances of lipid and carbohydrate metabolism Advantages: • HTN with asthma, • HTN with moderate bradycardia • HTN+DM 4. 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
  • 8. 5. Lipid solubility Lipid soluble • Propranolol. Timolol. Pindolol Metoprolol. Labetalol Pharmacokinetic properties • Highly metabolized • Large Vd • CNS penetration • Shorter t1/2 WATER SOLUBLE • Acebutolol, Atenolol, Esmolol, Nadolol Pharmacokinetic properties • Excreted unchanged by kidney • Less 1st pass effect • Small Vd • Longer t1/2 except esmolol
  • 9. 6. K+ channel blockade: sotalol • Sotalol is a nonselective β receptor antagonists, • that lack Local Anesthetic action • but has marked class III antiarrhythmia effect reflecting k+ channel blockade
  • 10. 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 B. Vascular system: prevent β2 mediated vasodilation→ reduction in CO (because of cardiac effect) → decrease BP → reflex vasoconstriction. On balance there is gradual reduction of both systolic and diastolic BP
  • 11. 2. Respiratory: bronchoconstriction; contraindicated in asthma 3. Eye: reduce IOP especially in Glaucomatous eyes decrease aqueous humor production 4. metabolic and endocrine effects: A. Increased Na+ retention, how? • Reduced BP causes a decrease in renal perfusion, resulting in an increase in Na+ retention and ↑plasma volume → In some cases, ↑BP. • 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
  • 12. 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.. 4. metabolic and endocrine effects:
  • 13. B. Pharmacological Effects and 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,? may increase diastolic pressure Labetalol is effective in emergency HTN -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*
  • 14. 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. Pharmacological Effects and Clinical Uses
  • 15. 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?? Independent of β blockade • CNS effects: sedation, fatigue, sleep alterations