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Autonomic Drugs- Part 2
Pharmacology Module 3
167
Medical
Graduate
07/07/2009

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Cards

Term
What adrenergic receptor induces contraction of iris, radial m?
Definition
a1
Term
What adrenergic receptor induces relaxation of ciliary mm?
Definition
b2
Term
What adrenergic receptor acts on the sa node to increase heart rate?
Definition
b1
Term
What adrenergic receptor increases contractility of the heart?
Definition
b1
Term
What adrenergic receptor increases velocity by acting on av node?
Definition
b1
Term
What adrenergic receptor increases velocity by acting on purkinje fibers?
Definition
b1
Term
What adrenergic receptor increases velocity, contractility, automaticity by acting on ventricles?
Definition
b1
Term
What adrenergic receptor constricts various arterioles?
Definition
a1
Term
What adrenergic receptor dilates various arterioles?
Definition
b2
Term
What adrenergic receptor constricts systemic vv?
Definition
a
Term
What adrenergic receptor dilates systemic vv?
Definition
b2
Term
What adrenergic receptor relaxes tracheal and bronchial components of the lung?
Definition
b2
Term
What adrenergic receptor decreases activity of glands in the lung?
Definition
a1
Term
What adrenergic receptor increases gland activity in the lungs?
Definition
a2
Term
What adrenergic receptor decreases motility of stomach?
Definition
a1, b2
Term
What adrenergic receptor increases sphincter tone in stomach?
Definition
a1
Term
What adrenergic receptor decreases motility of intestines?
Definition
a, b2
Term
What adrenergic receptor increases sphincter tone in intestine?
Definition
a
Term
What adrenergic receptor decreases secretions in intestines?
Definition
a2
Term
What adrenergic receptor relaxes gallbladder?
Definition
b2
Term
What adrenergic receptor decreases renin from kidney?
Definition
a1
Term
What adrenergic receptor increases renin production in kidney?
Definition
b2
Term
What adrenergic receptor relaxes detrusor m of bladder?
Definition
b2
Term
What adrenergic receptor contracts bladder sphincter?
Definition
a1
Term
What adrenergic receptor contracts prostate?
Definition
a1
Term
What adrenergic receptor induces ejaculation in males?
Definition
a1
Term
What adrenergic receptor contracts pilomotor skin mm?
Definition
a1
Term
What adrenergic receptor relaxes sweat (local) glands in skin?
Definition
a1
Term
What adrenergic receptor decreases secretions from acini glands in pancreas?
Definition
a
Term
What adrenergic receptor decreases b-cell secretion in pancreas?
Definition
a2
Term
What adrenergic receptor increases b-cell gland activity in pancreas?
Definition
b2
Term
What adrenergic receptor primarily acts to contract smooth mm?
Definition
a1
Term
What adrenergic receptor primarily acts to relax smooth mm?
Definition
b2
Term
What adrenergic receptor primarily acts on cardiac tissue?
Definition
b1
Term
What adrenergic receptor acts mostly on sympathetic neurons, producing feedback inhibition of neurotransmitter release?
Definition
a2
Term
Where else are adrenergic receptors found?
Definition
cns
Term
What adrenergic receptor acts to contract vascular smooth mm?
Definition
a1
Term
What adrenergic receptor acts as mydriasis, dilating pupils?
Definition
a1
Term
What adrenergic receptor acts to erect hair via pilomotor smooth mm?
Definition
a1
Term
What adrenergic receptor acts to contract prostate?
Definition
a1
Term
What adrenergic receptor increases force of heart contraction?
Definition
a1
Term
What adrenergic receptor acts to aggregate platelets?
Definition
a2
Term
What adrenergic receptor acts to inhibit transmitter release via adrenergic and cholinergic nn terminals?
Definition
a2
Term
What adrenergic receptor acts to contract some vascular smooth mm?
Definition
a2
Term
What adrenergic receptor acts to inhibit lipolysis in fat cells?
Definition
a2
Term
What adrenergic receptor increases force and rate of contraction in heart?
Definition
b1
Term
What adrenergic receptor promotes smooth mm relaxation via respiratory, uterine, and vascular smooth mm?
Definition
b2
Term
What adrenergic receptor promotes potassium uptake in skeletal mm?
Definition
b2
Term
What adrenergic receptor activates glycogenolysis in liver?
Definition
b2
Term
What adrenergic receptor dilates renal blood vessels?
Definition
d1
Term
What adrenergic receptor occurs in fat cells and activates lipolysis?
Definition
b3
Term
Where are d1 cells found? How does it act?
Definition
smooth mm. act to dilate *renal* blood vessels
Term
Where are d2 (dopamine) receptors found?
Definition
nn endings
Term
What adrenergic receptor modulates neurotransmitter release?
Definition
d2
Term
What is also known as *sympathomimetic* drugs?
Definition
adrenergic receptor agonists
Term
What drugs mimic effect of sns?
Definition
*sympathomimetic* drugs- adrenergic receptor agonists
Term
What type of adrenergic receptors meet the following description: Bind to and activate adrenergic receptors

May be selective or non-selective for αand β
receptors

Catecholamines vs noncatecholamines?
Definition
direct acting agonists
Term
Which adrenergic receptor agonists are not metabolized by MAO and COMT
and can be given orally and have longer duration of action
Definition
noncatecholamines
Term
Which adrenergic receptor agonists 
metabolized by monoamine oxidase
inhibitor (MAO) and catechol-o-methyltransferase (COMT)?
Definition
catecholamines
Term
Which type of adrenergic receptor agonist 
Increase concentration of norepinephrine at synapse
by several different mechanisms ?
Definition
indirect-acting agonists
Term
Which adrenergic receptor agonist acts in Combination of direct-and indirect-action ?
Definition
mixed-acting agonists
Term
What is the receptor affinity of epinephrine?
Definition
α
= α; β= β
Term
How is epinephrine administered? To what class does it belong?
Definition
Catecholamine given IV or SC, non-selective (a and b) direct acting adrenergic agonist
Term
Which effect predominates when epinephrine is given in higher or lower doses?
Definition
Low doses: βeffects predominate

High doses: α
effects predominate
Term
What drug can be used for anaphylactic shock, cardiac arrest, topical
vasoconstriction?
Definition
epinephrine
Term
What adrenergic agonists has the following adrs: tremor, palpitations, headache,
arrhythmias?
Definition
epinephrine, norepinephrine, dopamine in high doses
Term
How is norepinephrine administered? To what class does it belong?
Definition
iv, catecholamine, non-selective (a and b) direct acting adrenergic agonists
Term
What is the receptor affinity for norepinephrine?
Definition
: α
= α; β>> β
Term
Which has greater peripheral vascular resistance: epinephrine or norepinephrine?
Definition
norepinephrine
Term
What is the indication for norepinephrine?
Definition
hypotension
Term
How is isoproterenol administered? To what class does it belong?
Definition
iv, catecholamine- nonselective b1 *and* b2 direct acting adrenergic agonist
Term
To what class does dobutamine belong and how is it administered?
Definition
Selective (β
1orβ2)
Direct Acting Adrenergic Agonists

Selective β
1-agonist

Dobutamine

Catecholamine given IV
Term
What is the receptor affinity for isoproterenol?
Definition
β
= β
Term
What is a
Potent vasodilator

Potent inotropic agent (increases force of
contraction)?
Definition
isoproterenol
Term
What are the adrs of isoproterenol?
Definition
tachycardia, arrhythmias
Term
What is the receptor affinity of dobutamine?
Definition

β
> β>>>> α
Term
What drug is used in acute heart failure –potent *inotropic* agent?
Definition
dobutamine
Term
What are the adrs of dobutamine?
Definition
hypertension and tachycardia
Term
To what class do the following belong:
Albuterol, levalbuterol (Xopenex), salmeterol
(Serevent) ?
Definition
Selective (β
1orβ2)
Direct Acting Adrenergic Agonists

Selective β
2-adrenergic agonists
Term
What drug is used for the following: 
PO –bronchodilation for asthma (but more
systemic effects)

IV –relaxation of uterus in late pregnancy to delay
premature labor?
Definition
terbutaline
Term
To what class does terbutaline belong?
Definition
Selective (β
1orβ2)
Direct Acting Adrenergic Agonists

Selective β
2-adrenergic agonists
Term
To what class do phenylephrine and oxymetazoline belong?
Definition
Selective (α
1orα2)
DirectActing Adrenergic Agonists

Selective α
1-adrenergic agonists
Term
What drug causes 
Vasoconstriction with increased vascular
resistance and increased blood pressure ?
Definition
phenylephrine
Term
What drug is used for the following purposes:
IV –for hypotension and shock

PO –popular OTC decongestant?
Definition
phenylephrine
Term
What drug is a
Nasal decongestant

Causes rebound congestion (tachyphylaxis) if used for
more than several days?
Definition
oxymetazoline (afrin)
Term
To what class do clonidine and alpha-methyldopa belong?
Definition
Selective (α
1orα2)
DirectActing Adrenergic Agonists

Selective α
2-adrenergic agonists
Term
What is 
Centrally acting antihypertensive agent

Also used for attenuating substance withdrawal
symptoms

Given orally or as transdermal patch?
Definition
clonidine
Term
What is a Centrally acting antihypertensive agent

Still useful during pregnancy?
Definition
alpha-methyldopa
Term
To what class do the following belong: amphetamine and methamphetamine, and methylphenidate (ritalin)?
Definition
Indirect Acting Adrenergic Agonists
Term
What drugs
Stimulate release of norepinephrine and dopamine
from presynaptic vesicles?
Definition
amphetamine and methamphetamine
Term
Are amphetamine and methamphetamine aq or lipid soluble?
Definition

Very lipid soluble and easily enter CNS
Term
What drug has
Stimulant effects on mood and alertness and an
appetite depressant?
Definition
amphetamine and methamphetamine
Term
How do amphetamine and methamphetamine act?
Definition
Amphetamine derivative with similar action
Term
What drug 
Inhibits reuptake of norepinephrine ,
dopamine , and serotonin (similar in action to
antidepressants)?
Definition
cocaine
Term
What drug is 
Peripherally vasocontrictive and a cardiac
stimulant?
Definition
cocaine
Term
What drug has
Effects similar to amphetamine but shorter
acting and more intense?
Definition
cocaine
Term
What drug 
Also has local anesthetic effects (used in
ocular surgery)?
Definition
cocaine
Term
To what drug class does cocaine belong?
Definition
indirect acting adrenergic agonist
Term
What compound is Naturally occurring amine found in fermented
products such as cheese and sausage as well
as red wine, beer, bananas, avocados,
canned meats, sardines, and yeast
supplements?
Definition
tyramine
Term
Board ?: What is the adr associated w/tyramine?
Definition
Levels can increase if foods taken with MAO
inhibiting drugs (used for depression)
Term
What compound
Increases norepinephrine release and can
cause hypertensive crisis?
Definition
tyramine
Term
To what class does dopamine belong and how is it administered?
Definition
Mixed Acting Adrenergic Agonists

Dopamine

Catecholamine given IV
Term
What is the receptor affinity of dopamine?
Definition
D
1= D2>> β1>> α1
Term
What receptors are activated in low, medium, and high doses of dopamine?
Definition
Low doses: D receptor activation increases renal
blood flow

Medium dose: D + β
1receptors activated

High doses: D + β
+ αreceptors activated
Term
What drug has
Dose related activation of D, β
1, and α1
receptors as well as release of norepinephrine
Definition
dopamine
Term
To what class do ephedrine and pseudoephedrine (sudafed) belong?
Definition
Mixed Acting Adrenergic Agonists
Term
What is a 
Natural product found in ma-huang?
Definition
ephedrine
Term
How is ephedrine absorbed and how long does it act?
Definition

Well absorbed and long acting
Term
In high doses, what is ephedrine similar to?
Definition
epinephrine
Term
How can you get ephedrine-containing dietary supplements?
Definition
As of August, 2006 the sale of ephedrine-containing dietary
supplementsis prohibited in the U.S.
Term
What drug is a stereoisomer of ephedrine?
Definition
pseudoephedrine (sudafed)
Term
What is a Popular OTC decongestant but distribution now restricted
because it is primary ingredient for illegal methamphetamine
manufacture?
Definition
pseudoephedrine
Term
What do most OTC brands with “PE” on label now contain?
Definition
Most OTC brands with “PE” on label now contain phenyephrine
Term
What pts should avoid pseudoephedrine (sudafed)?
Definition
Should avoid in patients with hypertension or cardiomyopathies
Term
To what class does phenoxybenzamine belong?
Definition
Nonselective α-Blockers
Term
Does phenoxybenzamine bind reversibly or irreversibly?
Definition
Irreversiblereceptor blockade –lasts 4 days
Term
What is the receptor affinity of phenoxybenzamine?
Definition
α
1> α2
Term
What is used for catecholamine excess, such as for
pheochromocytoma, a tumor of the adrenal medulla
Definition
phenoxybenzamine
Term
What are the adrs of phenoxybenzamine and phenoxybenzamine?
Definition
Adverse effects: postural hypotension and reflex
tachycardia
Term
To what class does phentolamine belong?
Definition
Nonselective α-Blockers

Phentolamine

Competitive antagonist
Term
What is the receptor affinity of phentolamine?
Definition
α
1= α2
Term
What has the following uses: Pheochromocytoma

Reversal of ischemia from extravasation or injection of
adrenergic agonists such as epinephrine
Definition

Phentolamine
Term
To what class do the following belong: Prazosin

Terazosin (Hytrin)

Doxazosin (Cardura)
Definition
Selective α
1-Blockers
Term
What drug has the following uses: Relax vascular smooth muscle
Relax smooth muscle of bladder neck and prostate?
Definition
doxazosin
Term
What drug has the following uses: 3rdline agents for hypertension because increased morbidity
compared to other antihypertensive agents

Benign prostatic hypertrophy (BPH)?
Definition
doxazosin (cardura)
Term
What drug has the following adrs: 
1st dose syncope (must use small doses and have patient lie down)

Reflex tachycardia?
Definition
doxazosin (cardura)
Term
To what class does tamsulosin (flomax) belong?
Definition
Selective α
-Blockers
Term
What drug is a 
Specific antagonist of α
1A receptor in prostate gland

Causes less vasodilation than other α
1-blockers?
Definition
tamsulosin (flomax)
Term
Does tamsulosin cause more or less vasodilation than other alpha1-blockers?
Definition
Causes less vasodilation than other α
1-blockers
Term
What is 
Indicated for decreasing urinary obstruction from BPH?
Definition
tamsulosin (flomax)
Term
What is the effect of tamsulosin (flomax) on bp?
Definition
 Little effect on blood pressure at normal doses
Term
What is the prototypic agent of nonselected beta-blockers?
Definition
propranolol (inderal)
Term
To what class does propranolol (inderal) belong?
Definition
Nonselective β-Blockers
Term
What is the receptor affinity of
Propranolol (Inderal)?
Definition
β
1= β2
Term
What drug has the highest lipid solubility- more penetration in cns?
Definition
Propranolol (Inderal)
Term
What is the 1st pass effect for
Propranolol (Inderal)?
Definition
high; oral dose>>iv
Term
What drug has

Negative inotropic (cardiac contractility) and
chronotropic (heart rate) effect?
Definition
Propranolol (Inderal)
Term
Which should you use for pts w/ copd: porpranolol (inderal) or metoprolol (lopressor, toprol xl)?
Definition
metroprolol
Term
What can be used for hypertension, arrhythmias, angina, migraine headache, essential tremor?
Definition
propranolol
Term
What are the adrs/cautions of propranolol (inderal)?
Definition

Adverse effects/cautions: bradycardia, insomnia,
heart failure, asthma, diabetes
Term
Which has more adrs: nadolol (corgard) or propranolol?
Definition
propranolol
Term
To what class do nadolol (corgard), timolol, and pindolol belong?
Definition
Nonselective β-Blockers
Term
How is nadolol (corgard) excreted?
Definition
renal
Term
Does nadolol (corgard) have a long or short t1/2?
Definition
long
Term
What is the primary use of timiolol?
Definition
topical agent for glaucoma
Term
What drug is 
Also partial agonist of β
1and β2 receptors

Intrinsic sympathomimetic activity –causes less
bradycardia?
Definition
pindolol
Term
What is the prototypical selective β1 blocker agent?
Definition
metoprolol (lopressor, toprol xl)
Term
To what class does 
Metoprolol (Lopressor, Toprol XL belong?
Definition
Selective β1
-Blockers
Term
What is the receptor affinity of Metoprolol (Lopressor, Toprol XL)?
Definition
: β
1>> β2
Term
What is known as 
Known as cardioselectiveβ-blockers?
Definition
Metoprolol (Lopressor, Toprol XL)- Selectivity is lost with higher doses!
Term
With what drug is Selectivity is lost with higher doses?
Definition
Metoprolol (Lopressor, Toprol XL)
Term
What drug is Primarily used for hypertension (higher doses), heart
failure (lower doses), and angina?
Definition
Metoprolol (Lopressor, Toprol XL
Term
What drug is Safer for asthma and diabetes than nonselective β-
blockers but still must use caution?
Definition
Metoprolol (Lopressor, Toprol XL)
Term
What is the lipophilicity of atenolol (tenormin)?
Definition
Low lipophilicity -less CNS adverse effects than propranolol
Term
How is atenolol (tenormin) excreted and what is its t1/2?
Definition
Renal excretion

Long T 1⁄2
Term
To what class do the following belong: atenolol (tenormin), bisprolol (zebeta), esmolol, and acebutolol?
Definition
Selective β
1-Blockers
Term
What is the lipophilicity of bisoprolol (zebeta)?
Definition
moderate
Term
What selective b1-blockr is iv only?
Definition
esmolol
Term
What drug is a Partial agonist of β
1 receptor

Intrinsic sympathomimetic activity?
Definition
acebutolol
Term
To what class do labetalol and carvediol (coreg) belong?
Definition
α-and β-Adrenergic Antagonists
Term
What is teh receptor affinity of Labetalol and carvedilol (Coreg)?
Definition

β
1= β2 ;α1> α2
Term
What has More pronounced vasodilation than other β-
blockers due to α
1blockade?
Definition
Labetalol and carvedilol (Coreg)
Term
Labetalol and carvedilol (Coreg) have the same cautions as what other class?
Definition

Same cautions as nonselective β-blockers
Term
For what is labetalol (iv, po) useful?
Definition
useful for rapid reduction of
blood pressure
Term
For what is carvedilol primarily used?
Definition
heart failure
Term
What 4 things should be considered when choosing β-Blockers?
Definition
Receptor selectivity

If using selective agent, selectivity tends to be
lost at higher doses

Lipid solubility

If too high, can have CNS adverse effects

Half-life

Determines doses per day

Elimination route (renal vs liver)
Term
3 drugs that are reversible cholinesterase inhibitors for alzheimer's
Definition
donepezil (aricept)-1/day. galantamine (rizatidine). rivastigmine (exelon).
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