Ch 10: Adrenergic Blockers Flashcards
Adrenergic Blockers (Sympatholytics)
- Alpha-1 blockers:
phenoxylbenzamine, prazosin, terazosin
- For hypertensive crisis, high catechize hypertension, some migraines
** Inhibits vasoconstriction, allows Beta-induced vasodilation - Alpha-2 blockers:
yohimbine (phentolamine is non-selective… alpha-1 = alpha-2)
- allows increased NE from terminals (only used experimentally)
Phentolamine
- blocks aplha-1 adrenoceptors
- epinephrine activated both alpha and beta receptors
Beta Blockers
1.
Beta-1: metoprolol, atenolol
- slows HR, reduces contractility, inhibit renin
* For: arrhythmias, hypertension, heart failure, anxiety
Side effects: bradycardia, B-receptor super-sensitivity
- B-1 = B-2: propanolol, nadolol, timolol
- labetolol (also blocks alpha receptors)
3.
B-2: butoxamine –> No therapeutic indications
- B-2 blocking can cause bronchoconstriction (no asthmatics) and inhibit glycogenolysis (no diabetics)
Cardiac effects of Beta-Blockers
- decrease contractility (negative inotrophy)
- decrease relaxation rate (negative chronotrophy)
- decrease heart rate (negative chronotrophy)
- decrease conduction velocity (negative dromotrophy)
Vascular effects of Beta-Blockers
- smooth muscle contraction (mild vasoconstriction)
Action- Blocks Beta receptors in the Heart causing:
decrease in heart rate
decrease in force of contraction
decrease in rate of A-V conduction
Side effects of B-Blockers
bradycardia lethargy GI disturbance CHF decrease in BP depression
Abuse of Beta-blockers in sports
- calm down heart beat and circulation
- avoid excitement, stage fright and Hand tremor
- ***** increased tranquilization
Side effects of Adrenergic Antagonists B-Blockers
Hypotension
symptoms in CHF
bradycardia (AV-block)
drowsiness, depression
Adrenergic transmission blockers
- Reserpine
- depletes catechize stores by blocking uptake; causes transient sympathomimetic effect, then sympatholytic.
For hypertensive crisis/ hypertension
- can cause lethargy and depression - Guanethidine
- taken up then prevents NE release; leads to prolonged hypotension
- can cause hypotension, bradycardia, sexual dysfunction - Guanadrel
- similar to guanethidine, but also blocks NE release from adrenal medulla