Adrenergic Drugs Flashcards
MOA phenylephrine and generic name
Alpha agonist direct, neo-synephrine
MOA clonidine and generic name
Alpha agonist direct, catapres
MOA norepinephrine and generic name
mixed alpha and beta direct, levophed
MOA epinephrine and generic name
mixed alpha and beta direct, adrenalin
MOA Dobutamine and generic name
B agonist direct, dobutrex
MOA isoproterenol and generic name
B agonist direct, isuprel
MOA albuterol and generic name
B agonist direct, ventolin
MOA cocaine
inhibit re-uptake DA and NE, indirect
MOA selegiline and generic name
indirect inhibitors of MAO, eldepryl
MOA phenelzine and generic name
indirect inhibitor of MAO, nardil
MOA amphetamines
indirect, reverse NE and DA uptake mechanism and increase their release
MOA methylphenidate and generic name
indirect, reverse NE and Da uptake mechanism and increase their release, ritalin
MOA tyramine
indirect, reverse NE and DA uptake mechanism and increase their release
MOA ephedrine
indirect, increase release of dopamine and NE and a direct receptor agonist
MOA adrenergic drugs
modulate adrenergic transmission and primarily control the function of sympathetic nervous symptoms
G protein and effects for alpha1 receptor
Gq, increase IP3 and DAG
G protein and effects for alpha2 receptor
Gi, decrease cAMP
G protein and effects for B receptor
Gs, increase cAMP
G protein and effects for D1 receptor
Gs, increase cAMP
G protein and effects for D2 receptor
Gi, decrease cAMP
Full response of a1 receptor activation
catecholamine binding leads to activation of GPCR. PLC activated by alpha subunit, leading to production of IP3 and DAG. Results in an increase in Ca and activated protein kinase and activated PKC
Gs activation response
increase cAMP leading to increase PKA
How do direct acting adrenergic drugs produce their effects?
direct interaction with adrenergic receptors
How do indirect acting adrenergic drugs produce their effect?
increasing or reducing concentration of norepinephrine at target receptors, modulate NT concentrations in post-synaptic cleft
Vascular smooth muscle adrenoreceptor and action
alpha 1, contraction
Pupillary dilator muscle adrenoreceptor and action
alpha 1, contraction (DILATION of pupil)
Prostate adrenoreceptor and action
alpha 1, contraction
Heart adrenoreceptor and action
alpha 1, increases force of contraction
Neuron adrenoreceptor and action
alpha 2, modulates transmitter release
Platelets adrenoreceptor and action
alpha 2, aggregation
Adrenergic and cholinergic nerve terminals adrenoreceptor and action
alpha 2, inhibits transmitter release
Fat cells adrenoreceptor and action
alpha 2, inhibits lipolysis
Heart, juxtaglomerular cells adrenoreceptor and action
beta 1, increase force and rate of contraction, increases renin release
Respiratory, uterine adrenoreceptor and action
beta 2, smooth muscle relaxation
Skeletal muscle adrenoreceptor and action
beta 2, promotes potassium uptake
Human liver adrenoreceptor and action
beta 2, activates glycogenolysis and gluconeogenesis
Bladder adrenoreceptor and action
beta 3, relaxes detrussor muscle
Smooth muscle adrenoreceptor and action
D1, dilates renal blood vessels
Epinephrine effect on cardiac function, adrenoreceptor
beta 1, increases force of contraction, HR and conduction velocity at AV node
Epinephrine effect on vascular tone, adrenoreceptor
Beta 2 and alpha 1, increase systolic BP, may decrease diastolic BP and total peripheral resistance
adrenoreceptors in skin vessels
alpha 1
adrenoreceptors in skeletal muscle
alpha 1 and beta 2
adrenoreceptors in renal and cerebral vascular beds
D1 and alpha 1
Epinephrine effect on respiratory system, adrenoreceptor
beta 2: relaxes bronchial muscle
alpha 1: decreases bronchial secretions
Epinephrine effect on skeletal muscle, adrenoreceptor
Beta 2, causes muscle tremor and increases K uptake by skeletal muscle
Epinephrine effect on blood glucose levels, adrenoreceptor
beta 2, enhances liver glycogenolysis and gluconeogenesis
Epinephrine effect on free fatty levels in blood
increases free fatty levels, B1
Epinephrine effect on renin release
increases renin, B1