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Pharm 9 - Sympathomimetics
Pharmacology of adrenoceptor agonists and other sympathomimetic drugs
151
Pharmacology
Professional
02/16/2012

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Term
Where are alpha1 recepts?
Definition
most vascular smooth muscle, pupillary dilator, pilomotor sm musc, prostate, heart
Term
most vascular smooth muscle, pupillary dilator, pilomotor sm musc, prostate, heart - these have which type of alpha receptor?
Definition
alpha1
Term
What would be the effects of alpha 1 stimulation?
Definition
contraction of most vascular smooth muscle, pupil dilation, pilomotor erection, prostate contraction, increased force of heart contraction
Term
contraction of most vascular smooth muscle, pupil dilation, pilomotor erection, prostate contraction, increased force of heart contraction - if I want to achieve these effects, which receptor should I stimulate?
Definition
alpha1
Term
Where are alpha 2 recepts?
Definition
postsyn CNS adrenoreceptors, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth musc, fat cells
Term
postsyn CNS adrenoreceptors, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth musc, fat cells -- which alpha receptor would I find in these locations?
Definition
alpha2
Term
What would be the effects of alpha2 stimulation?
Definition
platelet aggregation, inhibit NT release at adrenergic and cholinergic nerve terminals, contraction of some vascular smooth muscle, inhibition of lipolysis
Term
platelet aggregation, inhibit NT release at adrenergic and cholinergic nerve terminals, contraction of some vascular smooth muscle, inhibition of lipolysis -- if I want to achieve these effects, which receptor should I stimulate?
Definition
alpha2
Term
Where would I find b1 recepts?
Definition
heart, juxtaglomerular cells
Term
Which type of b receptor would I find on heart and juxtaglomerular cells?
Definition
b1
Term
What would be the effects of b1 stimulation?
Definition
increased force and rate of heart contraction, increased renin release
Term
stimulation of which receptor would cause increased force and rate of cardiac contraction and increased renin release?
Definition
b1
Term
Where would I find b2 recepts?
Definition
respiratory, uterine, and vascular sm musc, skeletal muscle and liver
Term
which b receptor would I find on respiratory, uterine, and vascular sm musc, skeletal muscle, and liver?
Definition
b2
Term
what would be the effects of b2 stimulation?
Definition
smooth muscle relaxation (respiratory, uterine, vascular), promotes K+ uptake from skeletal muscle, activates glycogenolysis in liver
Term
I want to achieve these effects: smooth muscle relaxation (respiratory, uterine, vascular), promote K+ uptake from skeletal muscle, activate glycogenolysis in liver. Which receptor should I stimulate?
Definition
b2
Term
Where would I find b3 recepts?
Definition
fat cells
Term
which alpha and which beta receptor is present on fat cells? What are their actions?
Definition
alpha2 - inhibits lipolysis, beta 3 - activates lipolysis
Term
which beta receptor is present on fat cells?
Definition
b3
Term
which receptor mediates the activation of lipolysis?
Definition
b3
Term
Where would I find D1 recepts?
Definition
smooth muscle
Term
smooth muscle has which dopamine receptor?
Definition
D1
Term
What is the effect of D1 stimulation?
Definition
dilates renal blood vessels
Term
Which receptor acts to dilate renal blood vessels?
Definition
D1
Term
Where would I find D2 receptors?
Definition
nerve endings
Term
nerve endings have which type of D recept?
Definition
D2
Term
What is the effect of D2 recepts?
Definition
modulates NT release from nerve endings
Term
which recept modulates NT release from nerve endings?
Definition
D2
Term
name two a1 agonists
Definition
midodrine, phenylephrine
Term
What types of drugs are midodrine and phenylephrine?
Definition
alpha1 agonists
Term
Midodrine: MOA?
Definition
activates PLC -> ^ intracellular Ca+ and vasocontriction
Term
Which drug activates PLC -> ^ intracellular Ca+ and causes vasocontriction?
Definition
midodrine, phenylephrine
Term
effects of midodrine?
Definition
vascular smooth muscle contraction increasing BP
Term
which drug causes vascular smooth muscle contraction, increasing BP?
Definition
midodrine, phenylephrine
Term
phenyephrine: MOA?
Definition
activates PLC -> ^ intracellular Ca+ and vasocontriction
Term
effects of phenylephrine?
Definition
vascular sm musc contraction, increasing BP
Term
clinical application of midodrine?
Definition
orthostatic hypotension
Term
which drug is used for orthostatic hypotension?
Definition
midodrine
Term
Tox of midodrine?
Definition
supine hypertension, piloerection, urinary retention
Term
Which drug's toxicity includes supine hypertension, piloerection, urinary retention?
Definition
midodrine
Term
What is phenylephrine used for?
Definition
short term maintenance of BP in acute hypotension and intranasally to produce local vasocontriction as a decongestant
Term
which drug is used for short term maintenance of BP in acute hypotension and intranasally to produce local vasocontriction as a decongestant?
Definition
phenylephrine
Term
Name some a2 agonists
Definition
clonidine, a-methyldopa, dexmedetomidine, tizanidine, apraclonidine, brimonidine
Term
Name the drug class: clonidine, a-methyldopa, dexmedetomidine, tizanidine, apraclonidine, brimonidine
Definition
alpha2 agonist
Term
clonidine: MOA?
Definition
inhibits adenylyl cyclase, interacts with other intracellular pathways
Term
Which drugs inhibit adenylyl cyclase, and interact with other intracellular pathways?
Definition
clonidine (a2 agonists) and bromocriptine (D2 agonist)
Term
effects of clonidine?
Definition
vasocontriction is masked by a central sympatholytic effect, which lowers BP
Term
Which drug causes masking of vasocontriction by a central sympatholytic effect, lowering BP?
Definition
clonidine
Term
clinical applications of clonidine?
Definition
HTN
Term
which drugs are used in HTN?
Definition
clonidine (a2 agonist) and fenoldopam (D1 agonist)
Term
how is clonidine given? tox?
Definition
oral, transdermal, dry mouth and sedation
Term
which drug is given orally and transdermally, and produces dry mouth and sedation?
Definition
clonidine
Term
What is a-methyldopa? How is it used, generally?
Definition
a2 agonist, central sympatholytic
Term
What is guanfacine? How is it used, generally?
Definition
a2 agonist, central sympatholytic
Term
What is guanabenz? How is it used, generally?
Definition
a2 agonist, central sympatholytic
Term
What are a-methyldopa, guanfacine and guanabenz? How are they used, generally?
Definition
a2 agonist, central sympatholytic
Term
name the drugs used as central sympatholytics. What is their MOA?
Definition
clonidine, a-methyldopa, guanfacine, guanabenz. a2 agonists.
Term
What is dexmedetomidine? MOA? What's it used for?
Definition
a2 agonist, prominent sedative effects and used in anesthesia
Term
Which drug is an a2 agonist with prominent sedative effects and is used in anesthesia?
Definition
dexmedetomidine
Term
What is tizanidine? How is it used?
Definition
a2 agonist, used as muscle relaxant
Term
Name an a2 agonist used as a muscle relaxant
Definition
tizanidine
Term
What are apraclonidine and brimonidine? What are they used for?
Definition
Used in glaucoma to reduce IOP
Term
Name two a2 agonist drugs used in glaucoma to reduce IOP
Definition
apraclonidine, brimonidine
Term
Name a b1 agonist.
Definition
dobutamine
Term
what is dobutamine?
Definition
b1 agonist
Term
dobutamine: MOA?
Definition
activates adenylyl cyclase, increases myocardial contractility
Term
name a drug that activates adenylyl cyclase to increase myocardial contractility
Definition
dobutamine
Term
what is the effect of dobutamine?
Definition
positive inotropic effect
Term
name a drug with a positive inotropic effect on the heart
Definition
dobutamine
Term
clinical applications for dobutamine?
Definition
cardiogenic shock, acute heart failure
Term
which drug is used in cardiogenic shock and acute heart failure?
Definition
dobutamine
Term
How do you give dobutamine?
Definition
IV, need to titrate dose for desire effect
Term
Name a b2 agonist
Definition
albuterol
Term
what is albuterol
Definition
b2 agonist
Term
albuterol: MOA?
Definition
activates adenylyl cyclase
Term
effects of albuterol?
Definition
bronchial sm musc dilation
Term
which drug causes bronchial sm musc dilation?
Definition
albuterol
Term
clinical applications for albuterol?
Definition
asthma
Term
which drug is used for asthma?
Definition
dobutamine
Term
how is albuterol given? tox?
Definition
inhalation, tremors, tachy
Term
Name a D1 agonist
Definition
fenoldopam
Term
What is fenoldopam?
Definition
a D1 agonist
Term
fenoldopam: MOA?
Definition
activates adenylyl cyclase
Term
which drugs in this chapter activate adenylyl cyclase?
Definition
dobutamine (b1 agonist), albuterol (b2 agonist), fenoldopam (D1 agonist)
Term
which drugs in this chapter inhibit adenylyl cyclase?
Definition
clonidine (a2 agonist), bromocriptine (D2 agonist)
Term
effects of fenoldopam?
Definition
vascular smooth muscle relaxation
Term
which drug causes vascular smooth muscle relaxation?
Definition
fenoldopam
Term
what is fenoldopam used for?
Definition
hypertension
Term
What's special about dosing fenoldopam?
Definition
titration is needed
Term
Name a D2 agonist
Definition
bromocriptine
Term
what is bromocriptine?
Definition
a D2 agonist
Term
bromocriptine: MOA?
Definition
inhibits adenylyl cyclase and interacts with other intracellular pathways
Term
effects of bromocriptine?
Definition
restores dopamine actions in the CNS
Term
clinical applications for bromocriptine?
Definition
Parks, prolactinemia
Term
How is bromocriptine given? Tox?
Definition
orally, nausea, HA, ortho hypo
Term
Which receptors use cAMP?
Definition
a2, b, D
Term
Which receptors use ^ IP3, DAG?
Definition
a1
Term
Which intracellular messenger do a2 receptors use? Increase or decrease?
Definition
decrease cAMP
Term
Which intracellular messenger do beta receptors use? Increase or decrease?
Definition
increase cAMP
Term
Which intracellular messenger do D receptors use? Increase or decrease?
Definition
cAMP. D1 and D5 increase cAMP, D2/3/4 decrease cAMP.
Term
Does isoproterenol prefer b1 or b2 recepts?
Definition
they are equal
Term
Which recepts does epi stimulate?
Definition
a1,a2,b1,b2
Term
Which recepts does norepi stimulate?
Definition
a1 = a2, b1 > b2
Term
What's the difference between homologous and heterologous desensitization?
Definition
homologous results in decreased response to only that specific receptor, hetero results in desensitization of another receptor as well
Term
A major mechanism of desensitization that occurs rapidly involves...
Definition
phosphorylation of receptors by members of the GRK family (homologous)
Term
Phosphorylation of an adrenoceptor by GRK enhances their affinity for...
Definition
b-arrestins
Term
Arrestin interacts with...
Definition
clathrin and clathrin adaptor AP2 --> endocytosis of receptor
Term
maximal a and b activity is found with _______s, which have ____ groups on the __ and __ positions of the benzene ring
Definition
catecholamines, -OH, 3, 4
Term
Why aren't catecholamines active orally?
Definition
they are inactivated by COMT, found in the gut and liver
Term
Absence of one of the -OH groups on a catecholamine has what effect?
Definition
improves bioavailability, prolongs DOA, increases distribution to CNS
Term
Absence of one of the -OH groups on a catecholamine has what effect?
Definition
improves bioavailability, prolongs DOA, increases distribution to CNS
Term
Substitution on the amino group of a catecholamine has what effects?
Definition
better at b-receptors, worse at a-receptors
Term
Substitutions on the alpha-carbon of catecholamines has what effect?
Definition
block oxidation by MAO, prolong action - e.g. ephedrine and amphetamine
Term
Substitution at the beta carbon of a catecholamine has what effect?
Definition
facilitates activation of adrenoreceptors, may be important for storage in vesicles
Term
phenylephrine ____s BP and ___s heart rate
Definition
increases, decreases (baroreceptor-vagal reflex)
Term
The important effect for a2 receptors is...
Definition
to produce CENTRAL inhibition of sympathetic tone and BP, which overrides the local effects to constrict blood vessels
Term
In patients with autonomic failure, clonidine may ____ BP
Definition
increase
Term
beta receptor activation results in increased ____ influx in cardiac cells
Definition
calcium
Term
IV administration of dopamine promotes...
Definition
vasodilation of renal, splanchnic, coronary, cerebral, and perhaps other resistance vessels
Term
Dopamine actives ___ recepts in the heart
Definition
b1
Term
At higher rates of infusion, dopamine activates vascular ___ recepts, leading to ___
Definition
a, vasoconstriction
Term
In the eye, the radial pupillary dilator muscle contains ___ recepts
Definition
a
Term
a-agonists increase the outflow of aqueous humor and can be used to...
Definition
reduce IOP
Term
b-ANTAGONISTS have what effect in glaucoma?
Definition
decrease production of aqueous humor
Term
the bladder base, urethral sphincter and prostate contain ___ recepts that mediate ____
Definition
a, contraction and continence
Term
which is a centrally acting a2 agonist useful for sedation of intubated pts during treatment in the ICU, and also reduces requirements for opioids in pain control?
Definition
dexmedetomidine
Term
xylometazoline and oxymetazoline are direct ___ agonists
Definition
a
Term
when used in large doses, oxymetazoline can cause ____ due to central effect
Definition
hypotension
Term
Which drug is a potent vasodilator, causes increased cardiac output, fall in diastolic, lesser decrease or slight increase in systolic?
Definition
isoproterenol
Term
what is a partial b1 agonist?
Definition
prenalterol
Term
What is found in ma huang?
Definition
ephedrine
Term
___ is a racemic mixture of phenylisopropylamine
Definition
amphetamine
Term
Which drug is like amphetamine, has been promoted as an anorexiant and is a popular drug of abuse?
Definition
phenmetrazine
Term
Which drug is a psychostimulant with effects on NE, D, serotonin, glutamate, and decreases GABA, and is used in narcolepsy?
Definition
Modafinil
Term
Atomoxetine and reboxetine are...
Definition
NE reuptake inhibitors
Term
Which drug is an inhibitor of serotonin and NE reuptake, and is the only appetite suppressant approved by the FDA for long term tx of obesity?
Definition
sibutrimine
Term
____ is a local anesthetic with peripheral sympathomimetic action that results from inhibition of transmitter reuptake at noradrenergic synapses
Definition
cocaine
Term
the major action of cocaine in the CNS is...
Definition
inhibit dopamine reuptake in the pleasure centers
Term
For acute hypotension, which drugs have been used?
Definition
norepi, phenylephrine, methoxamine
Term
b2-selective agents relax the pregnant uterus, so drugs like ___ and ____ suppress premature labor
Definition
ritodrine, terbutaline
Term
Epinephrine and dipivefrin are used for
Definition
glaucoma
Term
longer acting b2 agonist for prevention of asthma attacks?
Definition
salmeterol
Term
___ agonists may be useful in acute heart failure
Definition
b1
Term
These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
Definition
Alpha1 agonists
Term
Shock due to septicemia or myocardial infarction is made worse by
Definition
Increasing afterload and tissue perfusion declines
Term
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
Definition
Terbutaline
Term
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
Definition
Ephedrine
Term
Alpha 1 agonist toxicity
Definition
HTN
Term
Beta 1 agonist toxicity
Definition
sinus tachy and arrhythmias
Term
Beta 2 agonist toxicity
Definition
skeletal muscle tremor
Term
The selective agents lose their selectivity at
Definition
high doses
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