Lecture 14-16 - Scrogin - Adrenergics (Antagonists) Flashcards
What are the 3 categories of adrenergic beta antagonists?
Non-selective, cardioselective (beta-1), partial agonist
What are the 3 non-selective beta blockers?
Propanolol, nadolol, timolol
What are the indications of non-selective beta blockers?
Hypertension, angina, glaucoma, heart failure, arrhythmia
What is the mechanism of action for non-selective beta blockers in relation to receptors?
Beta-1 = dec HR, dec force of contractility, dec renin release…get reduced vasoconstriction
Beta-2 = inc peripheral resistance
What are the indications for the non-selective beta blockers?
HTN, Angina, HF, Arrhythmia, Glaucoma (timolol)
What are the side effects of the non-selective beta blockers?
Get bronchiole constriction in people with asthma/COPD…bronchospasm
Masks symptoms of hypoglycemia
CNS effects include insomnia and depression
Can raise TAGS
Bradycardia
What are contraindications for non-selective beta-blockers?
BRONCHIAL ASTHMA
Sinus brady
Heart block
Cardiogenic shock
What are the cardioselective beta blockers and what receptor do they bind?
Beta-1 blockers
Metoprolol
Atenolol
Esmolol
What are the indications for the cardioselective beta blockers and which specific drugs are used for each?
Metoprolol = HTN and Angina
Atenolol = MI and HTN and Angina
Esmolol = Arrhythmia and Supraventricular Tachy
Does esmolol last long?
It has a very short half life
What are the effects of cardioselective beta blockers?
They give the same effects on the cardiovascular system as non-selective
What are the side effects of cardioselective beta blockers?
Depression
Insomnia
HYPOtension
Bradycardia
What are the contraindications for cardioselective beta blockers?
Heart block
Cardiogenic shock
Does metoprolol cross the BBB?
Yes
Does atenolol cross the BBB?
No
Name the partial adrenergic agonist
Pindolol
On what receptors does pindolol have activity
Beta-1 and Beta-2
What is the indication for pindolol?
HTN due to high sympathetic output
What is a benefit of pindolol?
As a partial agonist, it will have less bradycardic effect
When would you use pindolol?
For patients who can’t tolerate brady or decreased exercise capacity that’s seen with other beta blockers
What are the effects of pindolol?
It has the same cardio effects as non-selective beta blockers (dec bp/contractility/renin release/symp activation)
What are the side effects for pindolol?
They are the same as non-selective (ex: brady)
What are the contraindications for pindolol?
Same as non-selective…sinus brady, 2nd/3rd degree heart block, cardiogenic shock
What are the two non-selective alpha antagonists?
Phenoxybenzamine
Phentolamine
Which non-selective alpha antagonist is reversible? irreversible?
reversible = phentolamine
irreversible = phenoxybenzamine
What are the indications of the non-selective alpha antagonists?
Peri-operative treatment of pheochromocytoma
Dermal Necrosis
What are the cardio effects of the non-selective alpha antagonists?
inhibition of vasoconstriction
increased inotropy and chronotropy due to alpha-2 presynaptic blockade
reflex inc of NE release
unmasks vasodilatory effect of epi
What are the 3 side effects of the non-selective alpha antagonists?
Prolonged HYPOtension
Reflex Tachy
Nasal Congestion
What are 3 alpha-1 blockers?
Prazosin
Doxazosin
Terazosin
What are the indications for the alpha-1 blockers? Which drugs for each?
HTN (prazosin)
HTN and benign prostatic hyperplasia (doxazosin and terazosin)
What are the side effects of the alpha-1 blockers?
Syncope
Orthostatic hypotension (get dizzy when you stand up)