Pcol Test 2 Cholinergics Part 1

Front 1

what kind of Rc is on the neuromuscular junction

Back 1

Nicotinic

Front 2

what are the Rc subtypes of the nicotinic Rc

Back 2

N (neurological)
M (neuromuscular)

Front 3

what are the properties of the Nicotinic Receptor

Back 3

ligand gated ion channel
influx of Na and Ca
5 polypeptide units
two subtypes N/M

REGARDLESS OF WHAT SUBTYPE OF NICOTINIC RC THERE HAS TO BE 5 POLYPETIDES 2 OF WHICH MUST BE ALPHA

Front 4

what are the properties of the N subtype of Nicotinic Rc

Back 4

alpha and beta

2 alpha minimum

Front 5

what are the properties of the M subtype of the Nicotinic Rc

Back 5

alpha/beta/gamma/delta

2 alpha minimum

Front 6

how can nicotinic Rc become refractory

Back 6

since its an ion channel it can be depolarized and the membrane will be refractory until repolarized

Front 7

what would happen in the heart and to your BP as a reflex to a surge of nicotine

Back 7

BP and HR would increase

Front 8

what happens @ the neuromuscular endplates with a low dose, moderate dose, and high dose of nicotine/nicotinic agonist

Back 8

low dose: muscle contraction
moderate dose: depolarization blockade
high dose: paralysis

Front 9

how does varenicline work

Back 9

partial agonist @ nicotinic Rc

so it partially activates the nicotinic Rc and as a result less dopamine is released but enough dopamine to take the edge off withdraw symptoms but not enough to reinforce (addictive properties)

PREVENTS BINDING OF NICOTINE BY COMPETITIVE INHIBITION by sitting on the Rc and proventing other agonist/nicotine from binding

Front 10

what is the brand name of varenicline

Back 10

chantix

Front 11

what nicotinic subtype does chantix work at

Back 11

N type

Front 12

what are the two subtypes of cholinomimetic drugs

Back 12

direct (receptor agonist)
indirect (AChE-I)

Front 13

why are AChE-I indirect cholinomimetic drugs

Back 13

because they inhibit AChE and thereby indirectly increase the amount of ACh in the synapse

Front 14

where do direct receptor agonist bind

Back 14

MUSCARINIC RC ONLY!

Front 15

how can giving someone a cholinomimetic drug cause sweating

Back 15

since the sweat glands has muscarinic Rc we will be able to stimulate sweat secretions

Front 16

what are the properties of AChE-I

Back 16

indirectly cause stimulation of nicotinic Rc on SNS and PSNS ganglia and neuromuscular junction

indirectly cause stimulation of muscarinic Rc at all post junctional sites innervated by PSNS

Front 17

do Muscarinic agonist stimulate ACh release

Back 17

no

Front 18

what Muscarinic Rc subtypes are associated w/ Gi

Back 18

2,4

Front 19

what Muscarinic Rc subtypes are associated w/ Gq

Back 19

1,3,5

Front 20

what are the steps in Gq signaling

Back 20

agonist binds to GPCR

alpha GPCR activates PLC

PLC activates PIP2

PIP2 gets cleaved into IP3 and DAG (diacylglycerol)

IPE mobilizes Ca
Ca binds to CAM (calmodulin)
CAM binds to CAM-E(CAM Kinase)

RESPONSE

DAG activates PKC
PKC phosphorylates other proteins
RESPONSE

Front 21

what kind of kinase is PKC

Back 21

serine threonine

Front 22

what are the steps in Gs signaling

Back 22

agonist binds to GPCR

alpha GPCR activates AC (adenolyl cyclase)

AC converts ATP to cAMP

cAMP activates PKA (regulatory sites bind to cAMP)

catalytic unit then goes on to phosphorylate a protein

RESPONSE

Front 23

what are the steps in Gi signaling

Back 23

inhibits activation of AC (adenolyl cyclase) thereby inhibiting Gs signaling

Front 24

what kind of muscles in the eye are controlled by the SNS and contraction of them does what to the pupil

Back 24

radial muscle

contraction opens the pupil

Front 25

what kind of muscles in the eye are controlled by the PSNS and contraction of them does what to the pupil

Back 25

iris sphincter

cotnraction makes the pupil get smaller

Front 26

what stimulates miosis and what occurs

Back 26

PSNS activity stimulates miosis

miosis is constriction of the pupil of the eye

Front 27

what stimulates mydriasis and what occurs

Back 27

SNS activity stimulates mydriasis

mydriasis is dilation of the pupil

Front 28

what happens in closed angle glaucoma

Back 28

pressure dislocates the iris and decreases the ocular angle thereby limiting drainage

there is acute and chronic

Front 29

what kind of cholinomimetics can be used to treat glaucoma

Back 29

direct and indirect because there is PSNS innervation

Front 30

how do you treat closed angle glaucoma

Back 30

give cholinomimetic to contract the iris sphincter pulling the iris back to a more normal position therefore increasing ocular angle

Front 31

what happens in open angle glaucoma

Back 31

ocular angle is open but abnormalties in trabecular meshwork and/or canal of schlemm impede flow of aqueous humor

Front 32

in closed/narrow angle glaucoma what muscles do you want to contract

Back 32

iris sphincter and cilliary muscle to decrease pressure and improve outflow

Front 33

in open angle glaucoma what muscles do you want to contract

Back 33

cilliary muscles to improve outflow

Front 34

in secondary glaucoma what muscles do you want to contract

Back 34

cilliary muscles to clear any obstructions @ canal of schlemme

Front 35

what causes secondary glaucoma

Back 35

occurs after surgery/trama, infections etc

Front 36

what are the causes of overflow incontinence

Back 36

defect in innervation (poor contractility)
obstruction
constipation
drugs

Front 37

what happens in overflow incontinence

Back 37

bladder becomes full and we don't get the right signals to stimulate the contraction of the detrusor muscles and relaxation of the sphincter and results in leakage

Front 38

what are some things that have a direct effect in causing overflow incontinence

Back 38

alpha adrenergic agonist (they would keep sphincter tight)

anticholinergics (this would decrease PSNS tone to bladder therefore no contraction)

calcium channel blockers (need Ca to contract smooth muscle)


antipsychotics/TCA-antidepressants/narcotics ALL HAVE ANTICHOLINERGIC EFFECTS

Front 39

what are some things that have a indirect effect in causing overflow incontinence

Back 39

narcotics (opiods) they cause constipation which might block passage of urine out the bladder

Front 40

what is the main thing we want to achieve in overflow incontinence

Back 40

we want to have a contraction

Front 41

which type of cholinomimetic would you use to treat overflow incontinence

Back 41

direct or indirect cholinimimetic since there is PSNS innervation

Front 42

what is Myasthenia gravis

Back 42

muscle weakness in skeletal muscle due to the body making an antibody that blocks the N TYPE NICOTINIC RECEPTOR AT THE MOTOR ENDPLATE

ultimately we have a decrease in the # of N type nicotinic Rc therefore we have less muscles that can contract at one time

Front 43

what resembles paralysis induced by d-tubocurarine

Back 43

myasthenia gravis

Front 44

how do you treat MG

Back 44

AChE-I are used b/c if you increase local concentration of ACh you can stimulate more muscles more often

Front 45

why are direct cholinomimetics not used in MG

Back 45

because MG is caused by blockage of the nicotinic Rc and direct cholinomimetics can only stimulate the muscarine Rc

Front 46

what drugs are commonly used to treat MG

Back 46

neostignmine
pyridostigmine
ambenonium

Front 47

what is used to treat the side effects from MG treatment

Back 47

atropine (anticholinergic) blocks all the other responses we might see at muscarinic Rc doesn't bind @ nicotinic Rc

Front 48

what are the properties of edrophonium

Back 48

very short acting AChE inhibitor

Front 49

what do we use to see if the pt is getting enough AChE-I to treat MG

Back 49

edrophonium

Front 50

what happens is someone already getting AChE-I gets edrophonium and a contraction occurs

Back 50

they aren't getting enough AChE-I

Front 51

what happens if you give someone too much AChE-I

Back 51

muscle weakness due to over stimulation of nicotinic Rc @ neuromuscular junction

Front 52

what happens in Alzheimers

Back 52

progessive memory loss and loss of cholinergic nerves

Front 53

what is the strategy to treat Alzheimers

Back 53

increase level of ACh by using AChE-I but they must cross BBB

Front 54

what are the AChE-I that can be used to treat Alzheimers

Back 54

tacrine
donepezile

Front 55

what is the drug of choice to treat alzheimers

Back 55

donepezile

Front 56

what happens in congenital megocolon and how do you treat it

Back 56

accumulate waste in colon which gets stretched out and large

have to use direct cholinomimetic because no PSNS innervation

Front 57

what do cholinergic antagonist (anticholinergics do)

Back 57

block cholinergic agonist from binding and activating either muscarinic or nicotinic Rc

Front 58

what are the properties of Atropine

Back 58

anticholinergic

not selective and will bind to the Rc subtypes of muscarinic Rc

more effective at blocking exogenous cholinoceptor agonist than endogenous (ACh)

Front 59

what is scopolarmine mainly used for

Back 59

motion sickness
decreases secretions for surgery

Front 60

what is scopolamine

Back 60

an anticholinergic

Front 61

why must you use a anticholinergic along with an agonist when dealing with the eye

Back 61

to prevent adhesions

Front 62

what increases intraocular pressure opening or closing the iris

Back 62

opening the iris

Front 63

what can happen if you block the ciliary muscle from contracting

Back 63

open angle glaucoma

Front 64

what drugs can be used to treat the eyes

Back 64

atropine
scopolamine
tropicamide
cyclopentolate
homatropine

Front 65

what happens in congenital megocolon and how do you treat it

Back 65

accumulate waste in colon which gets stretched out and large

have to use direct cholinomimetic because no PSNS innervation

Front 66

what do cholinergic antagonist (anticholinergics do)

Back 66

block cholinergic agonist from binding and activating either muscarinic or nicotinic Rc

Front 67

what are the properties of Atropine

Back 67

anticholinergic

not selective and will bind to the Rc subtypes of muscarinic Rc

more effective at blocking exogenous cholinoceptor agonist than endogenous (ACh)

Front 68

what is scopolarmine mainly used for

Back 68

motion sickness
decreases secretions for surgery

Front 69

what is scopolamine

Back 69

an anticholinergic

Front 70

why must you use a anticholinergic along with an agonist

Back 70

to prevent adhesions

Front 71

what increases intraocular pressure opening or closing the iris

Back 71

opening the iris

Front 72

what can happen if you block the ciliary muscle from contracting

Back 72

open angle glaucoma

Front 73

what drugs can be used to treat the eyes

Back 73

atropine
scopolamine
tropicamide
cyclopentolate
homatropine

Front 74

what happens in urge incontinence

Back 74

involuntary detrusor muscle contractions

Front 75

why are postmenopausal women and women who have had children suceptible to urge incontinence

Back 75

post menopausal women due to their lack of estrogen which controls the sphincters

women with children due to loss of muscle tone down there

Front 76

what must you beware of when treating men for urge incontinence

Back 76

if he has an inlarged prostate

this is because if we inhibit bladder contraction and maintain tone in the sphincter he'll end up with overflow incontinence

Front 77

what drugs will make overflow incontinence worse

Back 77

anticholinergics (opiods, alpha adrenergic agonists, calcium channel blockers, TCA-antidepressants, antipsychotics)

Front 78

what drugs will make urge incontinence worse

Back 78

diuretics
soda
alcohol
caffeine

Front 79

why are anticholinergics used for intubation before surgery

Back 79

they cause the airway to relax