Dt, Cholinergic Pharm

Front 1

this drug prevents the uptake of choline into the presynaptic terminal of a cholinergic neuron

Back 1

hemicholinium

Front 2

this drug inhibits ACH release into the synapse?

Back 2

botulinum toxin

Front 3

these drugs inhibit acetylcholine breakdown by acetylcholine esterase into --> choline and acetate

Back 3

ACHE inhibitors

Front 4

Choline acetyl transferase does what ?

Back 4

takes CHOLINE and ACETYL COA and forms ACETYLCHOLINE

Front 5

BOTULISM toxin interacts w/ what protein to prevent ACH release?

Back 5

synaptobrevin

Front 6

what conditions are drugs that prevent ACH release used for?

Back 6

- blepharospasm
- strabismus/hyperhydrosis
- dystonia
-cosmetics

Front 7

this muscarinic receptor is located -->
- eye (sphincter/ciliary muscle)
- lungs (bronchioles/glands)
- gi tract (stomach/intestines)
- bladder
- sphincters, glands, endothelium of blood vessels

Back 7

M3 muscarinic receptor

Front 8

stimulation of pupillary sphincter and ciliary muscle in the eye via the m3 receptor does what?

Back 8

- sphincter contraction --> miosis (pinpoint pupils)
- contraction of ciliary muscle --> accomodation for near vision

Front 9

these muscarinic receptors are located on the heart ?

Back 9

M2 receptors
- sa node
- av node

Front 10

M2 stimulation in heart causes what?

Back 10

- enhances parasympathetic tone on the heart
--> Sa node --> dcrse heart rate
--> av node --> dcrse condctn velocity

Front 11

does m2 receptor stimulation have any effect on the ventricles of the heart?

Back 11

no effects on the ventricles or the purkinje system of the heart

Front 12

M3 receptor stimulation of the lungs causes what?

Back 12

bronchioles contract --> bronchospasm
+secretions from the glands in the lungs (incrsd edema)

Front 13

M1 receptors are responsible for what affects in the gi?

Back 13

- m1 stimulation --> increases GI secretion

Front 14

m3 stimluation in the stomach and intestines causes what?

Back 14

stomach --> increase motlity and cramps
- contraction of intestines --> diarrhea and involuntary defecation

Front 15

M3 bladder stimulation?

Back 15

-contraction of detrusor
- relaxation of trigone/sphincter
- --> causes voiding and urinary incontinence

Front 16

m3 receptor stimulation of sphincters?

Back 16

all RELAX except for the Lower esophageal sphincter (contracts)

Front 17

m3 stimulation of glands?

Back 17

increased sweating , salivation and lacrimation

Front 18

m3 stimulation of the blood vessels (endothelial cells)

Back 18

dilation of the blood vessels via NO release

Front 19

Nn stimulation in the adrenal medulla produces what catecholamines?

Back 19

NE and E

Front 20

autonomic ganglia stimulation does what ?

Back 20

Nn Receptor --> net fx depends on overall combined fx of sympathetic and parasympathetic dominance

Front 21

neuromuscular junction has what types of receptors? and respond to which stimulatory molecules?

Back 21

- Nicotinic muscle receptors
- respond to NE and E
--> twitches --> hyperactive skeletal muscle

Front 22

M1 and M3 are coupled with what g-protein?

Back 22

Gq --> incrse IP3, DAG, Ca2+

Front 23

M2 coupled to which g-protein?

Back 23

Gi-inhibitory protein
- dcrses a.cyclase --> dcrse cAMP

Front 24

NN and NM...any second messengers?

Back 24

no second messengers... activation and opening of Na/K channels

Front 25

name 4 muscarinic agonists

Back 25

Ach, Betanechol, metacholine, pilocarpine

Front 26

this drug has only MUSCARINIC activity, and is used for
- post op ileus
- urinary retention

Back 26

BETHANECOL

Front 27

this drug prefers M>N and stimulates AChE hydrolysis...used in the diagnosis of BRONCHIAL HYPERACTIVITY

Back 27

Methacholine

Front 28

this drug stimulates the M RECEPTORS only, and does NOT cause any ACHE hydrolysis... used topically for glaucoma and xerostomia

Back 28

Pilocarpine

Front 29

acetylcholinesterase inhibitors cause what to happen in the synapse?

Back 29

increases levels of ACh due to inhibition of the enzyme that breaks down ACh (acetylcholinesterase)

Front 30

- dx of myasthenia gravis
- differentiate from myasthenia and cholinergic crisis

Back 30

Edrophonium - short acting

Front 31

Rx of glaucoma, and is antidote for atropine overdose

Back 31

Physostigmine (enters the cns)

Front 32

Rx of ileus, urinary retention and myasthenia
- used to reverse the fx of NON-DEPOLARIZING NM blockers

Back 32

Neostigmine, pyridostigmine
- no cns entry b/c quaternary amine

Front 33

rx of alzheimers disease

Back 33

Donepezil, tacrine
- lipid solube = cns entrance

Front 34

rx of glaucoma and often used as insecticides

Back 34

organophosphates
- ecothiophate (glaucoma)
- malathion,parathion (insecticides)
- sarin (nerve gas)

Front 35

DUMBBELSS ?

Back 35

ACHE inhibitor overdose --> poisoning effects seen in someone who overdosed
--> fx of having too much ACh in the synpase --> overload of muscarinic effects

Front 36

DUMBBELSS?

Back 36

D= DIARRHEA
u= urination
m=miosis
b= bradycardia
b= bronchoconstriction
e= excitation (mscle and cns) --> leads to paralysis
l= lacrimation
s= salivation
s= sweating

Front 37

antidote for ache overdose? regeneration of ache?

Back 37

atropine (muscarinic receptor antagonist)
- pralidoxime

Front 38

name the prototype drug for MUSCARINIC RECEPTOR ANTAGONISTS

Back 38

Atropine

Front 39

what type of amine must atropine be in order to enter the cns?

Back 39

tertiary amine

Front 40

atropine fx on the body?

Back 40

- dcrsed secretion
- mydriasis and cycloplegia (paralysis of accomodation)
- hyperthermia (via vasodilation = red face)
- tachycardia (incrsd risk for arrythmias)
- sedation --> sleepppy
- urnry retention and constipation (dcrsd gi motility )

Front 41

what is a major sidefx of atropine?

Back 41

dry mouth due to dcrsd gland secretion

Front 42

what is the hallmark side effect of muscarinic blockade?

Back 42

- tachycardia

Front 43

give 6 other drugs that have atropine like fx in their pharm?

Back 43

-antihistamines - all of them have some atropine like fx
- tca's
- antipsychotics
- quinidine
- amantadine (antiviral y parks rx)
- meperidine

Front 44

tca's and antipsychotic overdose can lead to ?

Back 44

the 3 c's...
- coma
- convulsions
- cardiotoxicity

Front 45

what do u use to treat an overdose of atropine?

Back 45

if symptomatic --> physostigmine
- 3* amine that blocks AChE --> thus increasing the breakdown of Ach in the cleft and causing a dcrse --> less Muscarinic stimulation

Front 46

clinical uses of this drug are --> antispasmodic, antisecretory prior to intubation, management of ACHE overdose, antidarrheal, mydriasis of the eye (long acting 36-48 hours)

Back 46

Atropine

Front 47

this drug is a opthamological topical M-blocker with a few hours of fx

Back 47

Tropicamide

Front 48

used in asthma and COPD
- no cns entry and causes no change in mucus viscosity

Back 48

Ipratropium
- causes bronchodilation via blockage of the Muscarinic M3 receptors in the lung

Front 49

muscarinic blocker used in motion sickness
- causes sedation and short term memory loss

Back 49

Scopolamine

Front 50

these m-blockers are lipid soluble, and used in parks
- also used to manage the EPS symptoms caused by antipsychotics

Back 50

Benztropine
- trihexyphenidyl

Front 51

when is the SANS dominant in the body?

Back 51

- vascular tone
- thermoregulatory sweat glands

Front 52

when is PANS dominant in the body?

Back 52

sa node
av node
pupil
gi/ gu muscles
sphincters

Front 53

name 2 drugs that are used as Ganglion blocking agents (Nicotinic receptor antagonists)

Back 53

hexamethonium
mecamylamine

Front 54

moa of hexamethonium or mecamylamine?

Back 54

reduce predominant autonomic tone
- prevent baroreceptor changes in heart rate