Flashcards in Adrenergic Agonists Deck (45):
? is the parent compound from which all catecholamines and sympathomimetic drugs are derived
increased size of alkyl substitutions increase ? activity
removal of one or both of the ? on the benzene ring reduces the activity of the enzyme and increases the bioavailability and DOA of the drug
alpha adrenergic increase arterial resistance in ? and ?
catecholamine are excluded and enter only with ?
high rates of infusion
non-catecholamines i.e. ? or ? readily enter the CNS
activation of alpha 2 receptors in the ? decreases sympathetic outflow and causes ?
epinephrine acts on ? receptors
both alpha, both beta
epi treats ? by increaseing aqueous humor ? and decreasing its ?
OPEN angle GLC, outflow, production
hypovolemia, cardiac insufficiency, altered vascular resistance?
three major mechanisms responsible for shock
? is preferred for NON-anaphylactic shock- dilates renal vasculature
only use of NE is to ? in an ? state
-metabolized rapidly by ? and ?- very short 1/2 life
increase BP, acute hypotensive
NE has no effect on ?
Isoproterenol only acts on ?
potent vasoconstrictor and rapid IV can lead to reverse HR due to reflex effect?
use isoproterenol for acute ? and emergency ?; also heart block, torsades pointes
dopamine only give ?
dopamine treatment of severe ?
*also beneficial in septic or cardiogenic shock
D1 dopamine receptor- lowers BP in ?
-moderate affinity for ? receptors
full B1 agonist
-short term treatment of ? that may occur after surgery, in CHF, in acute myocardial infarction
dobutamine- LUB DOB ;)
alpha one selective agonists? (3)
ArAmine- off market
resistant to COMT metabolism?
-causes ? and an increase in BP with associated sinus ?
-IV- can be used as a potent ? w/ no direct inotropic or chronotropic effects on the heart
-due to reflex bradycardia- useful in treating ?
-commonly used as a ?
-in eye- effective ? in solutions
vasoconstriction, bradycardia (reflex)
treats postural hypotension?
alpha 2 agonists (5)
primarily used for hypertension?
also used to Dx phaeochromocytoma
*also useful in treating Ca patients, ADHD, nicotine/alcohol withdrawal, vascular HA, diabetic diarrhea, GLC, ulcerative colitis, Tourette's, etc.
alpha 2 that decreases IOP by decreasing aqueous humor production?
alpha 2 decreases IOP and is used for open angle GLC or ocular htn
B2 selective agonists (some action at B1 receptors)
B2 selective useful for bronchospasm & ? as well as ? due to the uterus relaxation
50 fold more selective than albuterol?
used for asthma, bronchospasm, & COPD?
B3 agonist- relaxes the detrusor muscle during storage phase increasing ?
indirect acting sympathomimetics main action is to increase synaptic conc of ? and ?
amphetamin & dextroamphetamine:
1. increased ? release of NT
2. ? transport
d-isomer is 3-4 times more potent at stim the CNS than the ? and is available as ? (ADHD)
CNS- increased ? activity
PNS- increase ? release which can lead to?
increased systolic&diastolic pressure
only CNS effects and no peripheral effects?
*this is why it is preferred for ADHD
Tx for obesity- decrease food intake but doesn't increase metabolism
do NOT give indirect agonists with ? >> massive increases of peripheral NE that could cause a ? and death
all indirect work by stim NE release by ? blocks reuptake of ?
? is more potent than ritalin; d-isomer of ritalin
first orally active sympathomimetic?
relief of nasal congestion?
combats fall in BP during epidural anesthesia?
raises Bp/CO/peripheral vasoconstriction?
decongestant, stereoisomer of ephedrine, less potent