Sympatholytic pharmacology Flashcards
What effect would an antagonist alone have on receptor activation?
Nothing without an agonist floating around
Side effects of alpha 1 receptor antagonists?
Orthostatic hypotension
Inhibition of ejaculation
Nasal stuffiness
Tachycardia
B-Haloalkylamines are what kind of antagonist?
Non-selective adrenergic receptor antagonist
Besides alpha receptors what else does B-Haloalkylamines inhibit?
Acetylcholine, histamine, and serotonin receptors
B-Haloalkylamines reversible or irreversible?
Irreversible
What type of antagonist are Imidazolines?
Non-selective alpha receptor antagonist
Imidazolines are competitive reversible or irreversible?
Reversible
Vascular effect of Imidazolines?
Vasodilator
Danger involving Imidazolines?
Reflex tachycardia
What type of antagonist are Quinazolines?
Alpha 1 adrenergic receptor antagonists
Where are quinazolines excreted?
Bile
Function of Quinazolines?
Vasodilator
Relaxation of smooth muscle in enlarged prostate and in bladder base
Blockade of a2 receptors increases what?
Sympathetic discharge
Folklore says that inhibition of a2 adrenergic receptors with Yohimbine treats what?
Male impotence
Suffix to know if a drug is a beta blocker?
OLOL
Most important pharmacological effect of propranolol?
Reduced renin release
Why is there a contraindication of propranolol for diabetics?
Inhibits compensatory glycogenolysis and glucose release in response to hypoglycemia
Difference between Nadolol and propranolol?
Less lipophilic than propranolol
Significant use of nadolol?
Migraines
What type of antagonist is Timolol?
Non-selective B-adrenergic receptor antagonist
Significant use of Timolol?
Glaucoma
How will Beta-Blockers affect pupil size?
It won’t
Main feature of Beta antagonist Pindolol?
Possesses intrinsic sympathomimetic activity and is a partial agonist
Benefit of Pindolol?
Less likely to cause bradycardia and lipid abnormalities
Significance of Carteolol?
Basically the same as Pindolol
Difference between the nonselective beta blockers and the selective B1 blockers?
The selective B1 blockers are “cardioselective” and cause less bronchoconstriction
Which selective B1 blocker is known as 10/10 in quality?
Atenolol
Half life of Esmolol?
9 minutes
Since it has such a short half life what is Esmolol best used for clinically?
Supra-ventricular tachycardia, atrial fib/flutter, perioperative hypertension
3rd generation B1 adrenergic receptor antagonists include?
Nebivolol
What makes up a mixed adrenergic receptor antagonist?
Non-selective B receptor antagonist
alpha 1 receptor antagonist
Benefit of mixed adrenergic receptor antagonist?
The added Beta antagonist will prevent the reflex tachycardia commonly associated with alpha 1 receptor antagonists
Which enantiomer antagonizes B blocking activity for Carvediolol?
S enantiomer
Withdrawal syndrome from Beta blockers involves whaT?
Tachycardia
Hypertension
Increase in sympathetic tone
When do you not use beta blockers?
Asthma
COPD
Type 4 congestive heart failure
What is the catecholamine deplete we talked about in class?
Reserpine
Function of Reserpine?
Block vesicular monoamine transporters
Deplete vesicular pool of NE
Slow onset of activation gives what benefit for Reserpine?
Won’t activate baroreceptors
How long does Reserpine last?
Sustained effect (weeks)
Reserpine is used to treat what?
Hypertension
Reserpine led to the discovery of what through its ability to precipitate depression?
Discovery of anti-depressants
