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Type of Drug CV effects Respiratory effects GI effects Genitourinary Effects Misc.

effects
Cholinergic
agonists
K
+
current in atria and
SA/AV nodes
incoming Ca
2+
hyperpolarizing
currents

overall pacemaker
firing rate
less PSNS control of
vesicles
Smooth muscle
constriction
trachebronchial
gland secretion
bronchioconstrictio
secretion and motor
activity of gut
salivary and gastric
gland secretion
relaxation of sphincters
stimulation of detrusor
muscle relaxation of
bladder sphincter
no effects on uterine
smooth muscle

Cholinesterase
inhibitors
(same as
direct-acting
muscarinic
agonists:
DUMBBELSS)
Dominated by PSNS
activation=>chronotropic
effects
Bradychardia, cardiac
output, little/no change
in BP
Myosis
contraction of
ciliary body to
enhancy aqueous
humor outflow
Cholinergic
Antagonists
SA node effected =>
tachychardia

Bronchodilation and
reduced mucus
production
Salivation/dry mouth
GI secretions
Relaxation of GI tract
smooth muscle

Relaxation of smooth
muscle
GI motility

heat induced hand
sweating
Low dose sedative effects
(more by scopolamine)
High dose excitation,
agitation, hallucination
Reduction in essential or
Parkinsons tremor
N/V prevention
Mydriasis/cyclopegia:
Pupil dilation used for
measurements of refractive
errors in eye exams
Adrenergic
agonists
(alpha 1)
Bradychardia
(vasomotor centre
activates PSNS and shuts
down SNS)
heart rate BP, constriction of
arteries, vagus nerve
activity, sympathetic
nerve activity
Adrenergic
agonists
(alpha 2)
bradychardia BP/Hypotensio
n, sedation;
Inhibit SNS
activity
Adrenergic
agonists (beta
1)
Contraction of heart and
accelerated heart rate
Decreased SNS activity
Negligible BP
effects
Stimulates PSNS
Adrenergic
agonists (beta
2)
Promote relaxation by
phosphorylation and
inactivation of MLCK by
cAMP
bronchodilation glycogenolysis and
glucogenesis
Act on smooth
muscle
vasculature,
bronchial tree and
uterus
Adrenergic
agonists (beta
3)
Promote lipolysis in
adipose tissue and
negative ionotropy in the
heart

Adrenergic
antagonist
(alpha
receptor)
Peripheral
resistance/lowered BP
-Postural/orthostatic
hypotension can occur
b/c of the inability to
change pressure from
sitting to standing
-reflex tachychardia: BP
drop activates the SNS
=> NE released
-nasal congestion

Adrenergic
antagonist
(beta
receptor)
-BP for hypertensive
pts
-negative ionotropic and
chronotropic effects on
the heart by slowing AV
node conduction
-nonselective blockers
increase peripheral
resistance by preventing
B2 receptor vasodilation
- Beta2
blockers:bronchcon
striction
(evident in
asthmatics)
-beta1 blockers no
significant
constriction at
normal doses

-B2 antagonists block
glycogenolysis
-non-selective
antagonists interfere
with glucose homeostasis
-inhibition of SNS
stimulation of lipolysis









Class Drug Effects
Nicotonic cholinergic agonist Nicotine
Lobeline
Acetyl-alpha-methylcholine?
Muscarinic cholinergic agonist Pilocarpine Salivation via PSNS, sweating via SNS,
myosis for glaucoma
Muscarine
Methacholine Equal activity as ACh but muscarinic selectivity
Bethanechol Smooth muscle effects, GI/urinary motility
post surgery
carbachol Urinary + GI tract stimulation, myosis
Cholinergic partial agonist (nicotinic) Varenicline aka Champix Binds selectively to alpha4-beta2-nicotinic ACh
receptors => dopamine release
Cholinesterase inhibitors reversible
AChE antagonist
neostigmine
Cholinesterase inhibitors - irreversible Dichlorvos 3.7 hour aging rate
melathion 3.7 hour aging rate
Diazinon 33 hours aging rate
parathion 33 hours aging rate
Soman (warfare agent) 2-6 min
Cholinergic antagonist Atropine Reduces heat induced sweating
Reverse drug-induced bradychardia
Reverses excess vagal nerve discharge due to MI
Depresses SA/AV node firing
Ipratropium (atropine analog) Used to stimulate resp effects in COPD/asthma
Antihistamine (diphenhydramine) Anti-nausea and non-vestibular-induced nausea
(morning sickness)
Antipsychotic
antidepressant
scopolamine
Cholinesterase regenerator compound Pralidoxime (PAM) Used after organophosphate poisoning, usually
in conjuction with atropine to block over-
activation of muscarinic receptors
Adrenergic agonist L-noradrenaline/norepinephrine
L-adrenaline/epinephrine
Adrenergic agonists (alpha) Phenylephrine, methoxamine Receptor affinity: a1, a2 >>> B
Clonidine, methylnorepinephrine Receptor affinity: a2>a1>>>>>B
Adrenergic agonists (mixed alpha/beta) norepinephrine a1 = a2; B1 >> B2 causes bradychardia;
BP/peripheral resistance=>SNS turned off,
PSNS turned on
epinephrine a1=a2; B1=B2 causes tachychardia via B1; no
change in peripheral resistance
Adrenergic agonists (beta) Dobutamine B1>B2 >>>>a
isoproterenol B1 = B2>>>a tachychardia via B1; dilation of
skeletal muscle vasculature via
B2=>peripheral resistance
Terbutaline, metaproterenol, albuterol,
ritodrine
B2>>>B1>>>>>>>>a
Adrenergic agonists (indirect) Amphetamine Promomtes catecholamine release => release of
norepinephrine
Cocaine Inhibits catecholamine reuptake at synapses =>
prevents norepinephrine reuptake
tyramine Found in fermented foods, metabolized by MAO
enzymes in the liver, stimulates release of
catecholamines
Pts taking MAO-inhibitors (ie MAO-A)should
avoid tyramine-containing foods
Adrenergic antagonist (B-
adrenoreceptor antagonist)
Oxprenolol (has partial agonist activity) Increased heart rate
Adrenergic antagonist (a-receptor) Phentolamine (competitive a1+2
antagonist)

Adrenergic antagonist (a1-receptor) Phenoxybenzamine Covalently binds a1 receptor; irreversible =>
long duration of action
-tachychardia, decreased BP, nasal congestion
-azosin (prazosin, terazosin, tamsulosin) -same effects as above
Adrenergic antagonist (a2) Alpha-methyldopa
Adrenergic antagonist (B-receptor) Lols
Adrenergic antagonist (mixed a/B) Labetolol Used for hypertensive emergencies, alpha
receptor antagonists also used
Adrenergic antagonist (type not
specified?)
reserpine Catecholamine storage in nerve
terminals=>BP=>hypersensitivity to
adrenergic agonists
Rarely used, occasionally for hypertension
ADR: excessive bradycardia, flushed skin,
congestion, postural hypotension, parkinsonism
(depletion of dopamine), depression (depleted
5HT), abdominal cramps, diarrhea

Adrenergic antagonist (a2) Alpha-methyldopa Safe for htn in pregnancy
Converted to methyldopamine and
methylnoradrenaline
Inhibits catecholamine rls

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