7 Adrenergic Agonists Flashcards
describe noncatecholamine:
- administration
- potency
- lipid solubility
- duration of action
compared to catecholamines
- effective as PO
- decreased potency compared to catecholamines
- lipophilic; can cross BBB
- longer duration of action due to COMT/MAO resistances
name the NE releasers
tyramine, ephedrine, amphetamine
describe the interaction between MAOI and dietary tyramine(and other NE releasers)
tyramine is usually degraded by MAO in the intestines
when MAO is inhibited, mass amounts of NE can be released by ingestion of tyramine rich foods: aged/fermented foods
leads to HYPERTENSIVE CRISIS
peripheral uses for ephedrine
b2AR agonist in combination w/NE-releasing
**decongestant - **closes of blood to nose(a1/2) but opens throat (b2)
vasopressor
stress urinary incontinence
cocaine mechanism of action
systemic effects?
NET is blocked
NE cannot return from synapse
-
increased BP, HR = increased O2 demand; coronary spasm = less O2 available
- leads to ischemia, infarction
- also causes persistent hyperthermia and rhabdomyolysis
5-HT2b agonists
significance?
amphetamine, ergot, DA derivatives
can cause drug-induced valvular heart disease
a1AR agonist
phenylephrine
a2AR agonist
clonidine
describe the mechanism of clonidine action
inhibits NE release
low dose: CNS effects
therapeutic dose: anti-hypertensive, lower IOP
high dose: becomes a1AR agonist
respiratory b2AR agonists?
respiratory b1/2AR agonist/non-selective b-agonist?
b2AR: albuterol**, **salmeterol
nonselective: isoproteronol
stepped-care approach to asthma treatment
- SABA
- leukotriene-receptor antagonist
- leukotriene modifier
- LABA
**b2AR agonist **used to delay pre-term labor
ritodrine
tolerance dvelops fast(48 hrs) and systemic b2 effects are prominent
clenbuterol
b2AR used to gain muscle mass(usually illegally)
“build muscle, burn fat”
long term adverse CV effects - cardiac hypertorophy
