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WorksheetsPharmacology Exam 2 pt 2
Total questions: 104
Worksheet time: 1hrs 8mins
What are the three endogenous monoamine neurotransmitters?
dopamine
norepinephrine
epinephrine
acetylcholine
What is the only neurotransmitter that is synthesized in synaptic vesicles instead of being transported into the vesicle after its synthesis?
epinephrine
norepinephrine
dopamine
Put the steps of monoamine neurotransmitter synthesis in order:
1. dopamine converted to NE
2. tyrosine to dopa by tyrosine hydroxylase (TH)
3. influx of Ca2+ into the nerve terminal trigger the release of MAs
4. dopa to dopamine by dopadecrobxylase
5. dopamine transported from the cytoplasm into vesicles by a vesicular monoamine transporter (VMAT)
6. action termination by reuptake, diffusion, degradation, feedback mechanism
7. action potential arrives at terminal and activates voltage-gated Ca++ channels
2, 4, 5, 1, 7, 3, 6
1, 4, 5, 6, 7, 3, 2
6, 7, 3, 2, 4, 5, 1
What blocks monoamine neurotransmitters via synthesis inhibition?
metyrosine
reserpine
bretylium guanethidine
cocaine and TCAs
What blocks monoamine neurotransmitters via storage inhibition?
metyrosine
reserpine
bretylium guanethidine
cocaine and TCAs
What blocks monoamine neurotransmitters via release inhibition?
metyrosine
reserpine
bretylium guanethidine
cocaine and TCAs
What blocks monoamine neurotransmitters via reuptake inhibitors?
metyrosine
reserpine
bretylium guanethidine
cocaine and TCAs
How are monoamine neurotransmitters released from vesicles?
direct: calcium dependent pathway
indirect: calcium independent pathway
direct: calcium independent pathway
indirect: calcium dependent pathway
What is the MOA of the indirect calcium independent pathway of monamine neurotransmitters being released from vesicles?
displacing NE
displacing epinephrine
displacing dopamine
Most monamine NTs do not bind to adrenergic receptor and some are weak agonists.
true
false
Is the following mechanism of signal termination primary or secondary: reuptake into the presynaptic neurons via NE transporter (NET) or simple diffusion away from the cleft to the circulation then metabolized
primary
secondary
Is the following mechanism of signal termination primary or secondary: catabolism via monoamine oxidase which is highly active in mitochondria in the nerve terminal or methylation via catechol-O-methyltransferase (COMT)
primary
secondary
Which drugs are inhibited by COMT?
entacapone
tolcapone
nitacapone
selegilline
moclobemide
Which drugs are inhibited by MAO?
selegilline
moclobemide
entacapone
tolcapone
nitacapone
Choose the characteristics of alpha 1 adrenoceptors (excitatory):
coupled via Gq proteins to activate PLC
leading to the formation of IP3 and DAG
mobilizes intracellular Ca2+ stores and activates PKC
activate Gi inhibitory proteins to inhibit adenylyl cyclase and decrease cAMP
regulate other ion channels activities
Choose the characteristics of Alph a2 adrenoceptors (inhibitory):
coupled via Gq proteins to activate PLC
leading to the formation of IP3 and DAG
mobilizes intracellular Ca2+ stores and activates PKC
activate Gi inhibitory proteins to inhibit adenylyl cyclase and decrease cAMP
regulate other ion channels activities
alpha 1 receptors (1A, 1B, 1D)
increase IP3 and DAG
widely expressed in vascular beds
Gq protein/ PLC pathway
arterial and venous vasoconstriction
cardiac function is of relatively less importance
alpha 2 receptors (2A, 2B, 2C)
lower cAMP
present in the vasculature: local activation leads to vasoconstriction
CNS centrally: inhibition of sympathetic tone and reduced blood pressure
can be used to treat HTN
increases BP
beta 1 agonists:
increase BP
increase heart rate and contractility
cause vasodilation
lipolysis
beta 2 agonists:
lower peripheral resistance
increase bronchodilation
increase BP
increase heart rate
beta 3 receptor:
lipolysis
mirabegron (induce detrusor muscle relaxation in bladder- overactive bladder)
increase BP
lower heart rate
Where are beta 1 receptors found?
heart
juxtaglomerular cells
respiratory smooth muscle
human liver
fat cells
Where are beta 2 receptors found?
respiratory, uterine, and vascular smooth muscle
juxtaglomerular cells
skeletal muscle
human liver
fat cells
Where are beta 3 receptors found?
fat cells
heart
skeletal muscle
human liver
What do beta 1 receptors in the heart and juxtaglomerular cells do?
increase force and rate of contraction
increase renin release
promote smooth muscle relaxation
promote potassium uptake
activates glycogenolysis
What do beta 2 receptors in the respiratory, uterine, and vascular smooth muscle do?
promote smooth muscle relaxation
promote potassium uptake
activates glycogenolysis
activates lipolysis
What do beta 2 receptors in the skeletal muscle do?
promote potassium uptake
activates glycogenolysis
activates lipolysis
promotes smooth muscle relaxation
What do beta 2 receptors in the human liver do?
activates glycogenolysis
activates lipolysis
promotes smooth muscle relaxation
increases force and rate of contraction; increases renin release
What do beta 3 receptors in the fat cells do?
activates lipolysis
activates glycogenolysis
promote smooth muscle relaxation
promotes potassium uptake
Norepinephrine
agonist at a1, a2, b1 receptors
positive inotropic
the baroreflex activation compensate for the chrontropic effect
activates both alpha and beta receptors
Epinephrine
activate both alpha and beta receptors
agonist at both a1, a2, b1 receptors
Where are D1 receptors?
smooth muscle
nerve endings
What do D1 receptors do?
dilates renal blood vessels
modulates transmitter release
Where are D2 receptors?
nerve endings
smooth muscle
What do D2 receptors do?
dilate renal blood vessels
modulates transmitter release
Choose the alpha agonists with a higher affinity for alpha 1
phenylephrine
methoxamine
clonidine
methylnorepinephrine
Choose the alpha agonists with a higher affinity for alpha 2
phenylephrine
methoxamine
clonidine
methylnorepinephrine
Choose the mixed alpha and beta agonists that are equal affinity in alpha receptors but beta 1 is greater than beta 2
norepinephrine
epinephrine
Choose the mixed alpha and beta agonists that are equal affinity in alpha AND beta receptors
norepinephrine
epinephrine
Choose the beta agonist with greater affinity for beta 1
dobutamine
isoproterenol
albuterol
dopamine
Choose the beta agonist with equal affinity in the beta receptors
dobutamine
isoproterenol
albuterol
dopamine
Choose the beta agonists with greater affinity for beta 2 receptors
albuterol
terbutaline
metaproterenol
ritodrine
dopamine
Choose the dopamine agonist with equal affinity between D receptors, and greater beta affinity than alpha
dopamine
fenoldopam
Choose the dopamine agonist with greater D1 affinity than D2
dopamine
fenoldopam
Direct-Acting Sympathomimetics: Phenylephrine
almost pure alpha 1 agonist
not a catechol derivative- resistant to inactivation by COMT, longer duration of action than catecholamines
can be used as: mydriatic (pupil dilator), decongestant, BP increase
treats orthostatic hypotension
pro-drug
Direct-Acting Sympathomimetics: Midodrine (oral)
pro-drug
selective alpha 1 receptor agonist
treats orthostatic hypotension
almost pure alpha 1 agonist
not a catechol derivative
Choose the alpha 2 selective agonists (centrally acting)
clonidine
methyldopa (preferred in pregnancy)
guanfacine
guanabenz
midodrine
How do alpha 2-selective agonists (centrally acting) work?
stimulates alpha 2 adrenoceptors in the brain stem activating inhibitory neuron which result in reduced sympathetic outflow from the CNS
topical decongestant
Dobutamine (beta 1 selective agents)
positive inotropic
positive chronotopic
negative inotropic
negative chronotropic
Choose the short acting beta 2 selective drugs (direct-acting sympathomimetics):
albuterol (salbutamol)
terbutaline
metaproterenol
indacterol
salmeterol
Choose the long acting beta 2 selective drugs (direct-acting sympathomimetics):
formoterol
salmeterol
terbutaline
indacterol
Choose the ultralong acting beta 2 selective drugs:
indacterol
olodaterol
vilanterol
formoterol
salmeterol
How are indirect-acting sympathomimetics amphetamine-like?
they enter the sympathetic nerve ending and displace stored catecholamine
stimulant effect
Which drugs are amphetamine-like indirect-acting sympathomimetics?
amphetamine
methamphetamine
methylphenidate
modafanil
tyramine
Which of the following drugs are catecholamine reuptake inhibitors used for ADD?
atomoxetine
reboxetine
sibutramine
duloxetine
venlafaxine
Which of the following drugs is a catecholamine reuptake inhibitor and used to be used as an appetite suppressant?
sibutramine
duloxetine
venlafaxine
desvenlafaxine
Which of the following drugs are catecholamine reuptake inhibitors and SNRIscused for depression and treatment of pain in fibromyalgia?
duloxetine
venlafaxine
desvenlafaxine
atomoxetine
sibutramine
Which of the following drugs is a catecholamine reuptake inhibitors can be used as a local anesthetic and inhibits transmitter reuptake at noradrenergic synapses?
cocaine
levodopa
fenoldopam
Which of the following dopamine agonists (catecholamine reuptake inhibitors) is converted to dopamine in the body and used in the treatment of Parkinson's disease and prolactinemia?
levodopa
fenoldopam
Which of the following dopamine agonists (catecholamine reuptake inhibitors) is a D1-receptor agonist that selectively leads to peripheral vasodilation in some vascular beds and is used as an IV treatment of severe HTN?
levodopa
fenoldopam
Which sympathomimetic drugs are used to treat acute hypotension and shock?
norepinephrine
dopamine
midodrine
dobutamine
Which sympathomimetic drug treats chronic orthostatic hypotension?
midodrine
epinephrine
dobutamine
phenylephrine
Which sympathomimetic drug treats cardiac arrest?
epinephrine
dobutamine
phenylephrine
brimonidine
Which sympathomimetic drug is used in cardiac stress tests?
dobutamine
epinephrine
apraclonidine
brimonidine
Which sympathomimetic drugs are used to treat glaucoma?
apraclonidine
brimonidine
phenylephrine
midodrine
What are some examples of reversible alpha receptor antagonists?
phentolamine
prazosin
terazosin
phenoxybenzamine
Choose the example of an irreversible alpha receptor antagonist
phenoxybenzamine
phentolamine
prazosin
terazosin
Which alpha antagonists have strong alpha 1 affinity vs alpha 2?
prazosin
terazosin
doxazosin
phentolamine
yohimbine
Which alpha antagonists have a weak alpha 1 affinity over alpha 2?
phenoxybenzamine
phentolamine
yohimbine
tolazoline
Which alpha antagonists have equal alpha 1 and 2 affinity?
phentolamine
yohimbine
tolazoline
labetolol
Which alpha antagonists have stronger alpha 2 vs alpha 1 affinity?
yohimbine
tolazoline
labetalol
carvedilol
Which mixed antagonists have equal b1 and b2 receptor affinity; b2 affinity is greater than or equal to alpha 1 which is greater than alpha 2?
labetalol
carvedilol
metoprolol
acebutolol
Which alpha antagonists have strong b1 vs b2 affinity?
metoprolol
acebutolol
atenolol
betaxolol
esmolol
Which alpha antagonists have equal b1 and b2 affinity?
propranolol
carteolol
penbutolol
pindolol
timolol
Which alpha antagonist has strong b2 vs b1 affinity?
butoxamine
metoprolol
labetolol
propranolol
Does phenoxybenzamine bind covalently or nah?
hell yeah brother
nope, dope
What does phenoxybenzamine block?
histamine H1
Ach
serotonin receptors
norepinephrine
epinephrine
Alpha receptor antagonist phenoxybenzamine:
low oral bioavailability
high oral bioavailability
long duration of action (14-48 hours)
short duration of action (5-10 minutes)
distribute to CNS
What is phenoxybenzamine used for?
pheochromocytoma: tumor of the adrenal medulla or sympathetic ganglion
increase NE and epinephrine secretion
reverse vasoconstriction in local anesthesia
Alpha receptor antagonist phentolamine:
potent competitive antagonist
non-selective a1 and a2 receptors
little inhibitory effects of serotonin receptors
agonistic activity on muscarinic, H1 and H2 receptors
relaxes smooth muscle in the prostate
Alpha receptor antagonist prazosin:
relaxes both arterial and venous vascular smooth muscle
relaxes smooth muscle in the prostate
highly metabolized by the liver
used for HTN
used for BPH
Alpha receptor antagonists terazosin and doxazosin:
a1 receptors selective antagonist
relaxes both arterial and venous vascular smooth muscle
relaxes smooth muscle in the prostate
used for HTN
used for BPH
Alpha receptor antagonist tamsulosin:
a1A and a1D >>> a1B subtype
less effect on standing BP in patients
used for BPH
used for HTN
Alpha receptor antagonist yohimbine:
a2-selective antagonist
a1-selective antagonist
promotes NE release in both the CNS and the periphery
increase BP and HR
hepatotoxic
Choose the highly bioavailable beta-receptor antagonist drugs:
propranolol
betaxolol
penbutolol
pindolol
sotalol
Why does propranolol have low bioavailability?
extensive hepatic (first-pass) metabolism
extensive hydrolysis reaction in GI tract
Which 2 beta receptor antagonists are the most lipophilic and readily cross the BBB?
propranolol
penbutolol
esmolol
nadolol
Which beta receptor antagonist has the shortest half life?
esmolol
metoprolol
carvedilol
nadolol
Which beta receptor antagonists are extensively metabolized in the liver by CYP2D6?
propranolol
metoprolol
carvedilol
nadolol
Which beta receptor antagonist is excreted unchanged into the urine and has the longest half life compared to the other drugs in this class?
esmolol
metoprolol
nadolol
carvedilol
Which beta receptor antagonist is non selective?
propranolol
carvedilol
metoprolol
nebivolol
When is propranolol contraindicated?
asthma
COPD
glaucoma
Which beta receptor antagonists have strong b1 affinity?
metoprolol
atenolol
bisoprolol
betaxolol
nebivolol
Which beta receptor antagonist is the most highly selective for b1?
nebivolol
propranolol
metoprolol
atenolol
Which beta receptor antagonists have partial beta agonist activity (intrinsic sympathomimetic activity (ISA)?
pindolol
acebutolol
carteolol
celiprolol
penbutolol
Is timolol a selective or non selective beta receptor antagonist?
selective
non selective
Which beta receptor antagonist is available in a racemic mixture?
labetalol
timolol
pindolol
acebutolol
Which beta receptor antagonist is non selective for beta receptor antagonists with some ability to block a1 adrenergic receptors?
metoprolol
carvedilol
betaxolol
Which beta receptor antagonist is the drug of choice in chronic heart failure?
carvedilol
metoprolol
acebutolol
atenolol
The action of beta receptor antagonists for treatment of HTN is less effective in:
elderly
individuals of African ancestry
children
Asians
What are the clinical applications of beta receptor antagonists?
HTN
ischemic heart disease
myocardial infarction
arrhythmia
hyperthyroidism
Which beta receptor antagonists are the most studied in treatment of MI?
timolol
propranolol
metoprolol
carvedilol
betaxolol
Sotalol is generally used for anti arrhythmic properties- how does it work?
K+ ion channel blocker
Na+ ion channel blocker
Ca+ channel blocker
How do beta receptor antagonists affect hyperthyroidism?
blockade of adrenoreceptors
inhibition of peripheral conversion of thyroxine to triiodothyronine
propranolol is most commonly used
