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
Norepinephrine effects on body, adrenoreceptors
a1, a2, b1; cardiac stimulant but reduces heart rate, potent vasoconstrictor, increase peripheral vascular resistance and BP
What receptor does norepinephrine not act on that epinephrine does act on?
Beta 2
Phenylephrine adrenoreceptor
alpha 1 and 2
Phenylephrine action
effective mydriatic and decongestant; severe vasoconstriction, BP elevation, severe bradycardia
Clonidine adrenoreceptor
selective alpha 2 agonist
Clonidine action
central effect on presynaptic alpha 2 receptors in lower brainstem, decreases sympathetic outflow and reduces BP, bradycardia
Isoproterenol adrenoreceptor
beta 1 and 2
Isoproterenol actions
B1: positive inotropic and chronotropic, increases CO
B2: vasodilator, decrease arterial pressure, bronchodilation
Dobutamine adrenoreceptor
selective B1
Dobutamine action
positive inotropic action
Albuterol adrenoreceptor
selective B2 agonist
Albuterol action
bronchodilation
Important characteristics of indirect-acting adrenomimetics
lipophilic, easily penetrate BBB, significant central effects
Tyramine characteristics and effects
hydrophilic, does not cross BBB, metabolized by liver and causes elevation of systolic BP
Clinical uses of norepinephrine
hypotensive emergencies, hemorrhagic shock, overdose of antihypertensives
Clinical uses of phenylephrine
hypotensive emergencies, hemorrhagic shock, overdose antihypertensives
Clinical uses of ephedrine
chronic hypotension
Clinical uses of dobutamine
cardiogenic shock
Adrenomimetic for heart failure
dobutamine
adrenomimetic for hypertension
alpha 2 agonists
adrenomimetic fo complete AV block and cardiac arrest
epinephrine and isoproterenol
Adrenomimetic for depression
phenelzine and selegiline
adrenomimetic for narcolepsy
amphetamines, methylphenidate
adrenomimetic for ADHD
methylphenidate
adrenomimetic for obesity
ephedrine and amphetamines
adrenomimetic for bronchial asthma
albuterol
adrenomimetic for decongestion of mucous membranes
phenylephrine, ephedrine
adrenomimetic for anaphylaxis
epinephrine
adrenomimetic for induction of mydriasis
phenylephrine
adrenomimetic for glaucoma
alpha 2 selective agonists
adrenomimetic for stress urinary incontinence
ephedrine
CV adverse effects of adrenomimetics
elevated BP, increased cardiac work, sinus tachycardia and ventricular arrhythmias
CNS toxicity AE of adrenomimetics
insomnia, lack of appetite, anxiety, restlessness, psychoses, convulsions and hemorrhagic stroke
MOA phentolamine and generic name
non-selective alpha 1 and 2 antagonist, oraverse
MOA phenoxybenzamine and generic name
non-selective alpha 1 and 2 antagonist, dibenzyline
MOA prazosin and generic name
alpha 1 direct antagonist, minipress
MOA tamsulosin and generic name
alpha 1 direct antagonist, flomax
MOA Labetalol and generic name
Beta and a1 direct antagonist, trandate
MOA carvedilol and generic name
Beta and a1 direct antagonist, Coreg
MOA propranolol and generic name
B1 and B2 direct blocker, Ineral
MOA pindolol and generic name
B1 and B2 direct blocker, visken
MOA nadolol and generic name
B1 and B2 direct blocker, corgard
MOA metoprolol and generic name
direct B1 blocker, toprol
MOA betaxolol and generic name
direct B1 blocker, kerlone
MOA acebutolol and generic name
direct B1 blocker, sectral
MOA atenolol and generic name
direct B1 blocker, tenormin
MOA guanethidine and generic name
indirect antiadrenergic, NE release inhibitor; ismelin
MOA metyrosine and generic name
indirect antiadrenergic, inhibitor of tyrosine hydroxylase; demser
Phentolamine vs. Phenoxybenzamine response to NE
phentolamine is a reversible competitive a antagonist that is shorter acting, phenoxybenzamine is an irreversible non-competitive a antagonist
Alpha antagonists on CV system
decreased peripheral vascular resistance and BP, postural hypotension, reflex tachycardia
Alpha antagonists on GU system
relaxation of smooth muscle in prostate, decreased resistance to flow of urine
Alpha antagonists of eye
relaxation of pupillary dilator muscle, miosis
Alpha antagonists used for pheochromocytoma
phentolamine, phenoxybenzamine, metyrosine
Alpha antagonist used for chronic hypertension
prazosin and doxazosin
Alpha antagonist used for erectile dysfunction
phentolamine
Alpha antagonist used for BPH
Tamsulosin, relieves urinary obstruction
AE of alpha antagonist
postural hypotension, nasal stuffiness, tachycardia, retention of fluid and salt, impaired ejactulation
Beta blocker antagonists
atenolol, nadolol, propranolol
Beta blocker partial agonists
acebutolol, labetalol, pindolol
Beta blocker inverse agonists
betaxolol, metoprolol
Beta blocker with ISA are…
partial agonists that produce a blunted sympathetic response, resulting in less risk for bradycardia
B blocker effect on CV system
negative inotropic and chronotropic effect, slow conduction via AV node; initially increases peripheral vascular resistance but will decrease with chronic use; inhibits renin release
B blocker effect on respiratory system
increase airway resistance
B blocker effect on eye
reduce intraocular pressure
B blocker effects on metabolism
inhibition of lipolysis, increase VLDL and decrease HDL, inhibition of glycogenolysis and gluconeogensis in liver
B blocker used for hypertension
beta blockers and mixed a and B blockers are used; labetalol
B blockers used for MI
propranolol and metoprolol
Clinical uses for B blockers
cardiac arrhythmias, MI, angina pectoris, hypertension, heart failure, glaucoma, hyperthyroidism
B blocker used for heart failure
metoprolol and carvedilol
B blocker used for glaucoma
betaxolol
B blocker used for hyperthyroidism
propranolol
AE of beta blockers
sedation, sleep disturbances, depression, increased airway resistance, trigger bronchospasm, depressed heart rate and contractility, increase VLDL and decrease HDL, hypoglycemic episodes
Abrupt discontinuation of B blocker therapy can cause…
increased responsiveness to beta receptors, enhanced cardiac stimulation and arrhythmias