Beta Adrenergic Receptor Antagonists

Question 1

Propranolol (Inderal)

Answer 1

	Beta adrenergic receptor antagonist
	Non-selective
	Lipophilic
	Local anesthetic  properties
	Blockade is activity-  dependent
Pharmacological effects
	Decreased cardiac output and  heart rate
	***Reduced renin release
	Increase VLDL, Decrease HDL
	Inhibit lipolysis
	Inhibit compensatory  glycogenolysis and glucose release in response to  hypoglycemia
	Increase bronchial airway  resistance

Question 2

Nadolol (Corgard)

Answer 2

	***non selective
-***Less lipophilic than propranolol
	Long half-life: ~20 hours
	Mostly excreted unchanged in  urine
	Administered: Oral
	Uses: Hypertension, angina,  migraine

Question 3

Timolol (Timoptic, Blocadren)

Answer 3

 non selective
-Thiadiazole nucleus with morpholine ring
 Administered: Oral, Ophthalmic
 Uses: Hypertension, angina, migraine, glaucoma

Question 4

Pindolol (Visken)

Answer 4

 non selective
-Possesses “Intrinsic sympathomimetic activity (ISA)
 Partial agonist
 Less likely to cause bradycardia and lipid abnormalities
 Administered: Oral
 Uses: Hypertension, angina, migraine

Question 5

Carteolol (Cartrol, Ocupress)

Answer 5

 non selective
-Possesses “Intrinsic sympathomimetic activity (ISA)
 Partial agonist
 Less likely to cause bradycardia and lipid abnormalities
 Administered: Oral, Opththalmic
 Uses: Hypertension, glaucoma

Question 6

Metoprolol (Lopressor, Toprol)

Answer 6

 beta 1
-“Cardioselective”
 Less bronchconstriction
 Moderate lipophilicity
 Half-life: 3-4 hours (Give multiple times a day)
 Significant first-pass metabolism
 Administered: Oral, parenteral
 Uses: Hypertension, angina, antiarrhythmic, congestive heart failure
 Metoprolol: extended release to combat short half life
 FDA indication for heart failure

Question 7

Bisoprolol (Zebeta)

Answer 7

 “Cardioselective”
 Less bronchconstriction
 Moderate lipophilicity
 ***Half-life: 3-4 hours (Give multiple times a day)
 Significant first-pass metabolism
 Administered: Oral, parenteral
 Uses: Hypertension, angina, antiarrhythmic, congestive heart failure
 Metoprolol: extended release to combat short half life
 FDA indication for heart failure

Question 8

Atenolol (Tenormin)

Answer 8

	beta 1
-“Cardioselective”
	Less bronchconstriction
	Low lipophilicity
	Half-life: 6-9 hours
	Administered: Oral, parenteral
	Uses: Hypertension, angina
	On a scale of 1 – 10, this is a ten

Question 9

Esmolol (Brevibloc)

Answer 9

 Very short acting
 **Half-life: 9 minutes
 Rapid hydrolysis by esterases found in red blood cells
 Administered: Parenteral, Note: incompatible with sodium bicarbonate
 **Uses: Supraventricular tachycardia, atrial fibrillation/flutter, perioperative hypertension
 Extremely short, drug cleared in a few half lifes (gone in 45 minutes)

Question 10

Nebivolol (Bystolic)

Answer 10

 β1 selective
 Low lipid solubility
 Vasodilation due to nitric oxide production
 Hypertension
 **1. Beta 1 blockage
 **2. Direct vasodilation due to NO production

Question 11

Labetalol (Normodyne, Trandate)

Answer 11

• Non-selective b receptor antagonist
• ]a1 receptor antagonist
• ]Two asymmetric carbons (1 and 1’)
• (1R, 1’R)-isomer possesses b- blocking activity
• (1S, 1 R)-isomer possesses greatest a1 receptor blocking activity
• b-blocking activity prevents reflex tachycardia normally associated with a1 receptor antagonists
• Administered: Oral, parenteral
• Uses: Hypertension, hypertensive crisis
• ***lowers renin activity

Question 12

Carvedilol (Coreg)

Answer 12

o Non-selective b receptor antagonist
• a1 receptor antagonist
• Both enantiomers antagonize a1 receptors
• Only (S)-enantiomer possesses b- blocking activity
• b-blocking activity prevents reflex tachycardia normally associated with a1 receptor antagonists
• Administered: Oral
• Uses: Hypertension, congestive heart failure (Types II and III)