Adrenergic Antagonists

Question 1

Nonselective alpha blockers

Answer 1

Phenoxybenzamine
Phentolamine
Ergotamine

Question 2

Selective Alpha 1 blockers

Answer 2

Prazosin
Doxazosin
Terazosin 
Alfuzosin
Tamsulosin (alpha1-A)

Question 3

Selective alpha 2 blockers

Answer 3

Yohimbine

Question 4

Phenoxybenzamine

Answer 4

• Nonselective irreversible noncompetitive alpha antagonist
• (a1)Prevents vasoconstriction -> DEC PVR -> DEC BP
• (a2) INC HR + CO
• NOT successful in maintaining lower BP
• Clinical: Pheochromosytoma
• AE: Orthostatic hypotension; Inhibits erection; Reflex Tachy

Question 5

Phentolamine

Answer 5

• Reversible Nonselective antagonist
• Very similar to phenoxybenzamine
• Clinical: ST PCCytoma; Hypertesive crisis; clonidine withdrawal; Tyramine OD; Dermal necrosis; Reversal of anesthesia
• Same AE as Phenoxybenzamine

Question 6

Prazosin

Answer 6

• Selective a1 blocker
• DEC SVR -> DEC BP
• Clinical: Hypertension; BPH
• AE: Orthostatic hypotension
• NO reflex Tachy

Question 7

Terazosin/ Doxazosin

Answer 7

• Selective a1 antagonist
• Longer T1/2
• Clinical: Hypertension + BPH
• AE: Intraoperative floppy Iris Syndrome; Priapism

Question 8

Tamsulosin/Alfuzosin/Silodosin

Answer 8

• Selective alpha1A antagonist
• Less affect on Hypertension
• Clincal: BPH
• AE: Retinal detachment; Priapism; Abnml Ejaculation

Question 9

Yohimbine

Answer 9

• Selective a2 blocker
• Obsolete clinical use; Research
• OTC fat burning

Question 10

Alpha antagonist Contra/Interactions

Answer 10

• Tricyclics (Hypotension)
• Concurrent use w/ strong 3A4 inhibitors
• Contra: Hypersensitivity; Hepatic impairment; Renal impairment; QT prolongation

Question 11

Cardioselective Beta Blockers (B1)

Answer 11

New Exclusive Beta Blockers Are Acting Mainly Cardioselectively

Nebivolol
Esmolol
Bisoprolol
Betaxolol
Acebutolol
Atenolol
Metoprolol
Celiprolol

Question 12

Partial agonist Beta Blockers

Answer 12

Contain Partial Agonist Like Property

Carteolol
Pindolol
Acebutolol
Labetalol
Penbutolol

Question 13

Local anesthetic B blockers

Answer 13

Possess Local Anesthetic Membrane-stabilizing Property

Propanalol 
Labetalol
Acebutolol
Metoprolol
Pindolol

Question 14

Propanolol

Answer 14

• Nonselective B Blocker; Crosses BBB
• Pharm: Depress SA/AV Node; DEC CO + BP; Blocks Vasodilation (reflex constriction) mediated by B2; DEC PVR; DEC Renin
• Bronchoconstriction (Asthma)
• DEC glycogenolysis
• Clinical: HT; Angina; MI; Migraine; HyperThy; HF; Variceal bleeding; Arrhythmias; tremors; Glaucoma

Question 15

Other non-selective B antagonists (besides Prop)

Answer 15

Nadolol: More potent; Less CNS; Stevens-Johnson Syndrome

Timolol: DEC aqueous humour-> Glaucoma + heart conditions

Penbutolol: Partial agonist w/ sympathomimetic activity; More potent

Acebutolol: Same as Pen

Pindolol: Same as Pen; Safer in asthma

Question 16

Labetalol

Answer 16

• Additional alpha 1 blocking
• Clinical: Hypertensive crisis
• AE: Hepatotoxicity, Orthostatic hypotension

Question 17

Carvedilol

Answer 17

• Also has a1 blocking
• Clinical: HF; Hypertension
• AE: IFIS; Stevens-Johnson syndrome
• Take w/ food for absorption + Orthostatic hypertension

Question 18

Nonselective B antagonist interactions/contra

Answer 18

Interactions: drugs which inhibit metabolism potential employers affects (Cimetidine, fluoxetine); Prevent rescue affects of EP; NSAIDS attenuate antihypertensive action;

Contra: Asthma/COPD; Bradycardia; AV Block; CHF; Diabetes + Hyperthyroidism; CNS depression

Question 19

Atenolol/Metoprolol

Answer 19

• Competitive B1 blocker
• Clinical: HyperT; Angina; AMI; HF; SupraV Tachy
• AE: CNS less likely; Hypotension;

Question 20

other B1 selective antagonist

Answer 20

Esmolol: IV; Thyroid storm; HT emergency;

Betazolol: Glaucoma

Nebivolol: ONCE DAILY; Vasodilation via NO release to delay atherosclerosis; Contra Severe Liver impairment