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66 Cards in this Set

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two types of cholinergic receptor agonist
1. direct acting agonist
2. Indirect acting agonist
Direct acting cholinergic receptor agonist

examples:
bind and activate cholinergic receptors

i.e. choline esters
Ach, bethanecol,carbachol
Indirect acting cholinergic receptor agonsit do what?
increase levels of Ach at synapse:
-inhibit cholinesterase
-inhibit breakdown of Ach
-inhibit release of Ach
General Properties of cholinergic agonist
-similar to Ach
-do NOT cause CNS effects
-are non specific for M receptors, stimulate all, thus cause wide variety of effects
Cholinergic agonist ocular effects
-increase lacrimal gland secretions
-stimulate contraction of iris sphincter muscle and ciliary muscle (miosis)
-enhance near vision
-decrease night vision
cholinergic agonist toxic doses/overdoses can cause:
-diarrhea
-salivates
-cramps
-shortness of breath
-urniary incontinence
cholinergic agonist respiratory effects:
-increase bronchial smooth muscle contraction
-increase secretions of mucus
-contradicted in patients with uncontrolled asthma and COPD
Cholinergic agonsit cardiac effects:
-reduced peripheral vascular reistance
-reduced HR
-slows HR by decreasing sinus rhythm
-increase PR interval by slowing conduction thru AV node
Cholinergic agonsit GI effects:
-stimulate gastric motility via stimulus ENS

-stimulat salivary and gastric secretions

-increase GI contractions; except sphincters
Cholinergic agonsit Urinary tract effects:
-stimulate detrusor muscle; layer of muscle in the uterus that when contracted expels urine

-relax urinary sphincter and trigone

-promotes micturition
Two types of indirect acting cholinergic agonsit
1. reversible=short acting
*used to treat myasthenia
graves- autoimmune

2.Irreversible=long lasting
*used as nerve gases and
pesticides
Cholinergic antagonist general effects:
-relax smooth muscle
-decrease secretions

-decrease lacrimination

-increase heart rate

-increase cardiac conduction
cholinergic antagonist ocular effects:
-relax iris sphincter=pupil
dilation (mydriasis)

-relax ciliary muscle
causing cycloplegia(paralysis of accomodation)

-decreases lacrimation=
dry eyes
cholinergic antagonist cardiac effects:
-increase HR

-icrease AV conduction
Cholinergic antagonist respiratory effects:
-bronchial smooth muscle
relaxation

-bronchial dilation

-inhibit secretions of upper
and lower resp tract
cholinergic antagonist GI effects
-reduces LES tone and may promote reflux

-relaxes smooth muscles
(except sphincters)

-reduces motility

-inhibit gastric secretions

-lead to prolonged emptying time and consitpation
cholinergic antagonist Urinary tract effects
-retract detrusor muscle leading to urinary retention

-CNS effects

-sedation; across blood-brain barrier

-acute confusional (delirium)

-high doses cause hallucinations
cholinergic antagonsit inhibit_______ and causes___ ___ skin
sweating;

hot;dry
cholinergic antagonist overdose causes
Dry as bone
hot as pepper
red as a beet
mad as a hatter
adrengic receptors include
3 main types
alpha 1 and alpha 2

beta 1 and beta 2

dopamine 1and 2
alpha 1 primary function

i.e.
smooth muscle contraction

bladder sphincter
iris dilator
vascular vasoconstriction increase peripheral vascular resistance
increases BP

mydriases

urniary retetion
alpha 2 primarily pre-synaptic; functions to
-inhibition of NE release

-decrease secretion of aqueous humor

-decrease insulin secretion

-mediates platelet aggregation
Beta-1 functions primarily
caridac
beta-1 functions
-increase HR chronotropic effect

-increase contractility
(inotropic)

-increase heart conduction
(dromotrpic)

-increase renin secretion

-tachycardia
beta-2 acts on which muscle
smooth
beta-2 functions to do what?
-relaxation of smooth muscle:
*vascular
*bronchial
*uterine
-glycogenolysis
relax
breakdown of what?
Ach effects
dopainne acts primarily in the ______
brain
dopamine functions to
mediate vascular smooth muscle relaxation

modualte neruotransmitter relase in sympathetic and CNS

*D receptors only st. by dopamine
vascular ___ muscle _____

modulate _____release in sympathetic and CNS

act only on
catecholamines ____ -OH group

natural
synthetic
have;

epi, NE , dopamine
isoproterenol, dobutamine
non-catecholamines____-OH group

types
lack;


phenylephrine, pseudoephedrine,amphetamine
adernergic agonist epinephrine potent at ___&____

constricts vessels in___ ____ and ____

dilates vessels to ____&____
-potent agonist at both A and B sites


-constricts vessles in skin,mucus membranes and visera

-dilates vessels to liver and muscle
Adrenergic receptor antagonists consist of what 2 groups?
Alpha 1&2 blockers
Beta 1&2 blockers
what are alpha blockers generally used to treat?
used mainly to treat hypertension, cardiac dysrhythmias, angina and myocardial infarction. Also used to treat anxiety.
effects of Alpha-1 blocker?
cause smooth muscle relaxtion in vascular and uriary tissue

causes vasodilation and lower BP

less reflex tachycardia then phentolamine

can cause fast reduction in BP,dose low to start, prevent syncope
Alpha-1 blocker
-no change in _____ and ____
-improves _______
Use for ____&_____
cardiac output; renal flow
urinary flow;
BPH; HTN
Side effects of Alpha-1 blockers?
Dizziness
syncope
othrostasis
nasal congestion
headache
Beta-1 blocker decreases HR by having negative effects on _____,_____,_____
Chronotropic (change HR)
inotropic (contractility)
dromotropic (conductivity of cardiac muscle fibers)
Beta-1 blocker
decreases_____ ____ from the kidneys
renin secretion
Beta-1 blocker
decreases____ ____ formation in the eyes
lowers ____ _____ pressure
aqueous humor;

intra ocular
Beta-2 blockers cause
-bronchial______

-_____ gylcogenolysis and glucagon secretion

-masks signs of _____ in DM

-decreased _____ _____
constriction

inhibits

hypoglycemia

renal perfusion
Therapeutic uses of beta blockers
hypertension
hyperthyroidism
angina
glaucoma
migraine HA
MI prevention
palpatations
performance anxiety
tremor
pheochromocytoma
SE of beta blockers
brochospasm
bradycardia
heart block due to high doses
Erectile dysfunction
Epinephrine Adrenergic agonist:
_________bronchial smooth muscle

relieves ______ induced bronchospasm

_______ tidal volume

stimualtes ________
dilates;

histamine;

increases;

glycogenolysis
ephinephrine therapeutic uses include:
*asthma
*glaucoma
*anaphylaxis(epi pen)
*anaphylactic shock
*use to prolong effects of
local anesthetics
*reduce bleeding in surgery
*in actue MI w/ cardiac arrest
Norepinephrine is more receptive to ____ then ____ receptors
B1; B2
NE
strong agonist at alpha receptors =
vasoconstriction of most all vessels
NE:
increase ___
BP
Dopamine activates
___,___,&___ receptors
D1; B1; alpha
dopamine stimulates release of ____ from synaptic neurons
NE
Dopamine selectively dilates vessels in _____ and ____ vessels
renal; sphlanchic
Dopamine increases
HR
contractility
cardiac output
Dopamine is dose ______
dependent
Low dose of dopamine cause:
renal failure; vasodilates and increase renal blodd flow
(D1 receptor)
medium dose of dopamine cause:
Increase HR and CO so used in shock (B1 receptor)
High dose of dopamine cause:
stimulates alpha 1 and causes vasoconstriction and increases periperal resistance
Dopamine side effects:
short-lived
rapid metabolism
HTN
nausea
disrhythmia
NE:
increase ___
BP
Dopamine activates
___,___,&___ receptors
D1; B1; alpha
dopamine stimulates release of ____ from synaptic neurons
NE
Dopamine selectively dilates vessels in _____ and ____ vessels
renal; sphlanchic
Dopamine increases
HR
contractility
cardiac output
similar to B1 effects
Dopamine is dose ______
dependent
Low dose of dopamine cause:
renal failure; vasodilates and increase renal blodd flow
(D1 receptor)
medium dose of dopamine cause:
Increase HR and CO so used in shock (B1 receptor)
High dose of dopamine cause:
stimulates alpha 1 and causes vasoconstriction and increases periperal resistance
Dopamine side effects:
are ____
have a ___ ___
consist of:
____
____
____
short-lived
rapid metabolism
HTN
nausea
disrhythmia