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Adrenergic system - Coggle Diagram
Adrenergic system
agonists
indirect acting agojnists
mixed acting agonists
direct acting agonists
selective a1 adrenergic agonists
Phenylephrine,metarminol,methoxamine
selective to a1 (strong vasoconstrictors for severe hypertension) minimal caradic side affects. not substrates for COMT > long duration of action.
2-Arylimidazoline family
(potent vasoconstrictor) for eye/nasal drops
a adrenergic nonselective
epinephrine for anaphylatic shock
Ephedrine
Dont have phenolic group > avoid metabolism
can cross BBB (uncharged)
Psuedoephedrine
indirect action/ no direct action on adrenergic receptor
cause release of endogenous noradrenaline from storage vesicles in presynaptic neurons
selective a2 adrenergic agonists
switch Ch2 of arlimidazoline to NH will get you Clonidine (dramatic hypotensive effect). imidazoline ring and Has two Cl groups in a benzene that act as steric blockers
inhibit sympathetic output pre synaptic
Guanfacine (Tenex) as a result of removing imidazoline ring
Methyldopa
Prodrug can cross BBB with carrier, give us a-methyldopamine
False neurotransimmer replace norepinpherine in nerve terminal
selective b1 adrenergic agonists
dobutamine
has a chiral center,S enantiomer exhibit a1 agonist activity and b1 agonist activity, R enantiomer exhibit a1 antagonist. they cancel each other leaving the wanted B1-effect
Isoprenaline
selective for b receptors but shows no selectiveity for different subtypes (b1,b2)
attemps to modfify phenolic group so it is not recognized by COMT , increase duration
Soterenol, Salbutamol(albuterol
salbutamol(albuterol)
longer duration, same potency as isoprenaline, 2000 timesless active on the heart
Result of introduction of sulfonamide group to isoprenaline
Soterenol
Salmeterol
long and lipophilic group, twice duration of albuterol up to 12 hours