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Pharmacology > ANS Cholinergic > Flashcards

ANS Cholinergic Flashcards

1
Q

parasympathetic effect on the eye

A

M3 - Miosis (contraction of sphincter muscle)
M3 - accomodation cyclospasm (near vision contraction of ciliary muscle)
used in opthalmic exams/glaucoma
long term use may lead to cataracts/retinal detachment

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2
Q

Muscarinic Antagonism effect on the eye

A

M3 - Mydriasis (dilation)

M3 - accomodation to far vision leading to cycloplegia

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3
Q

Hemicholinium

A

inhibit choline active transport pp to presynaptic nerve endings.

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4
Q

Botulinum Toxin

A

inhibits Ach exocytosis by interaction with
“clostridum botulinum”
bacterial entersthru recycling vessicle reuptake
synaptobrevin. degrades SNAP-25 preventing vessicle fusion to membrane (protease prevents SNARE complex)
Rx. blepharospasm, strabismus, hyperhydrosis, dystonia, and cosmetics

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5
Q

Acetylcholinesterase inhibitors

A

indirect acting cholinomimetics
Reversible: edrophonium, physostigmine, neostigmine
Irreversible: echothiophate, malathion, parathion

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6
Q

Muscarinic effect on the heart

A

M2 - SA node negative chronotropy
M2 - AV node negative dromotrophy
used in supraventricular tachycardia (SA node M2 receptors via vagus nerve)

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7
Q

Muscarinic effect on the Lungs

A

M3 - bronchioles contraction (bronchospasm)

M3 - gland secretions

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8
Q

Muscarinic effect on the GI tract

A

M3 - increased motility and cramping
M1 - increase secretions
M3 - contraction. diarrhea/involuntary defecation

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9
Q

Muscarinic effect on the Bladder

A

M3 - contraction of detrussor
relaxation of the trigone/sphincter
voiding/urinary incontinence

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10
Q

muscarinic effect on the sphincters

A

M3 - relaxation

lower esophageal contracts!

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11
Q

muscarinic effect on the glands

A

M3 - secretion. sweat thermoregulation, salivation, lacrimation

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12
Q

muscarinic effect blood vessel endothelium

A 
M3 - dilation (NO/endothelial derived relaxing factor
NO innervation (no effect indirect agonists AchE inhibitors)
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13
Q

Cholinergic receptor mechanism

A

M1 and 3 (Gq) phospholipase C (IP3/Dag/Ca+)
M2 (Gi) decrease adenylyl cyclase, cAMP
Nn and Nm are both ionic Na/K channels

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14
Q

AcetylCholine

A

M and N choline ester direct agonist
short half life, no clinical use
quickly metabolized by AchE
intraoccular use for cataract surgery to stimulate rapid miosis

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15
Q

Bethanechol

A

M choline ester direct agonist
no AchE hydrolysis, no CNS
DoA ~2hrs
Rx. ileus (postop/postpardum/neurogenic), urinary retention

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16
Q

Methacholine

A

M>N direct agonist
some AchE hydrolysis (unpredictable magnitude)
Dx bronchial hyperreactivity (asthma)

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17
Q

Pilocarpine

A

M direct agonist
no AchE hydrolysis. uncharged (CNS)
Doa ~2hrs. less potent than Ach itself.
Rx. glaucoma (topical), xerostomia

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18
Q

Edrophonium

A

indirect cholinomimetic - AChE Inhibitor
short acting
Diagnosis Myasthenia gravis from cholinergic crisis

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19
Q

Myasthinia Gravis

A

“autoimmune HSR type II disease acting on the nicotinic cholinergic Ach Receptors (muscular end plates fast inotropic inhibited by curare).
Muscle weakness with prolonged activity, worsening over the day, ptosis, double vision, difficulting swallowing/chewing/speaking,
Tx. With long DoA AChE inhibitor (…stigmine)
DD. Lambert-Eaton wiich is worse in morning when Ca+ is lowest

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20
Q

Cholinergic crisis

A

Organophosphates/carbamates etc.
Rx. with atropine (effects) and pralidoxime (AchE regenerator)
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation (CNS/ nicotinic muscle excitation then paralysis), lacrimation, salivation, sweating.
nicotinic effects: skeletal excitation followed by paralysis, CNS stimulation

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21
Q

lambert-Eaton

A

autoimmune disease HSR type II acting on the presynaptic voltage-gated Ca+2 channels preventing excocytosis of Ach to act on nAchR of the motor end plate.
Muscle weakness worst in the morning when Ca+ is lowest.
dd. Myasthenia Gravis that acts on the AchR themselves and worsens at night with use.”

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22
Q

Physostigmine

A 
indirect cholinomimetic- AchE inhibitor
enters CNS
DoA ~3hrs (intermediate)
Rx. Glaucoma
Rx. Atropine overdose +/- symptomatic (and antidepressant OD)
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23
Q

Neostigmine

A

indirect cholinomimetic- AchE inhibitor
NO CNS
DoA short acting more potent than physostigmine. Contraction before paralysis.
Rx. Ileus
Rx. urinary retention
Rx. myasthenia
Rx. reversal of nondepolarizing NMJ blockers (curare)

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24
Q

pyridostigmine

A 
indirect cholinomimetic- AchE inhibitor
NO CNS
DoA ~4hrs 
Rx. Ileus
Rx. urinary retention
Rx. myasthenia
Rx. reversal of nondepolarizing NMJ blockers (curare)
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25
Q

Indirect acting cholinomimetics

A 
AChE inhibitors: 
-endrophonium (short acting diagnostic)
-physostigmine (CNS - atropine antidote)
-neostigmine and pyridostigmine (rx ileus, urine ret, myast, reverse NMJ blockes)
-donepezil (CNS -Alz)
-tacrine (CN - Als with hepatic effects)
Irreversible:
organophosphates ( toxin rx glaucoma detox with paralidoxime)
- echothiophate, parathion, malathion
26
Q

Alzheimers

A

late onset dementia with progressive memory loss ad cognitive decline. Neurropathology includes neurofibrillary tangles, amylid plaques, and loss of Ach neurons in the Meynert’s necleus rational for clinical use of AchE inhibitors.

degeneration of neurons in specific regions of cerebral cortex and hippocampus. Most common cause of dementia, incraease with age. Sporatic/ rarely familial. Increased risk in patients with Downs syndrome (ch21) often by 40YOA
4 genes are associated: 9amyloid precursor protein) APP encoding betaAPP, PSEN1 and 2 coding for presenilin.
APOE is not associated with monogenic alzhymers but increases susceptability to nonfamilial (most common form) and influences the age of onset of some monogenetic forms.
* Deposition of two fibrillary proteins (intracellular): Beta-amyloid and Tau (neurofibrillay tangles extracellular) [hirano bodies]
- amyloid/senile plaques which contain amyloid and APOE lipoproteins form in the extracellular spaces
- Tau proteins are microtubule-associated axon structural support proteins abundant in the brain, hyperphosphorylations of which compose the intracellular neurofibrillary tangles found within neurons. Although accumulation of tau fibrillary tangles is one cause of neuro degeneration in alheimers, the actual Tau protein mutations are associated with other neurodegenative deseases such as AD demenia, frontotemporal dimentia.
- The beta-APP amyloid presursor protein (21q21.3) proteolytically cleaved by Alpha, beta, (both cell surface) and gamma (atypical) secretases. 90% betaAPP are cleaved by alpha protease which cleaves within the beta-amyloid (Abeta) domain precluding its formation. The remaining 10% cleaved by beta and gamma protease into Abeta40 and very little Abeta42. Mutations are seen to increase the production of Abeta42 a neurotoxin. Diagnostically Abeta42 elevated in plasma serum. Presenilin 1 and 2 also increase production of Abeta42 as they are critical cofactors for gamma protease. Mutation in PSE1 has earlier onset of symptons than mutations in PSEN2. APOE is a component of the alzhymer amyloid plaques by binding to the Abeta proteins. Three common allleles for APOE gene Echo2,3 and 4. APOEecho4 homozygots have onset before 70yrs, heterozygots after 70yrs. Those with APOEecho2 are shown to have later onset. Carriers of the APOE echo4 allele are also shown to have poorer outcomes of head injury.
* final stages are primive reflexs and death by malnutrition, secondary infections, heart disease.

27
Q

Parathion

A

indirect cholinomimetic - irreversible AChE inhibitor
Organophospates insecticide/military weapons
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation (CNS/ nicotinic muscle excitation then paralysis), lacrimation, salivation, sweating.
RX. atropine/pralidoxime

28
Q

Malathion

A

indirect cholinomimetic - irreversible AChE inhibitor
Organophospates - degraded by UV light.
tx head lice
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation (CNS/ nicotinic muscle excitation then paralysis muscle), lacrimation, salivation, sweating.
RX. atropine/pralidoxime

29
Q

Pralidoxime

A

regeneration of AchE
rx in cholinergic crisis due to AChE Inhibitor overdose
functions by reversing the phosphorylation of AchE and by aging of the organophosphate by cleaving it.
Atropine used for muscarinic management effect.

30
Q

Atropine

A 
muscarinic receptor antagonist (prototype)
CNS activity
management of AchE inhibitor overdose
antisecretory
mydriasis/cycloplegia (short acting)
hyperthermia (vasodilate)
tachycardia
sedation
urinary retention and antidiarrheal
behavioral excitation and hallucinations (antispasmolitic)
C/I  narrow anlge glaucoma,
31
Q

Drugs with antimuscarinic effects

A 
antihistamines
tricyclic antidepressants
quinidine
amantadine
meperidine
C/I  narrow anlge glaucoma,
32
Q

Tropicamide

A

direct muscarinic blocker

opthalmology (topical)

33
Q

scopolamine

A

direct muscarinic blocker
rx motion sickness
sedation
short term memory block

34
Q

Benztropine

A

direct muscarinic blocker
lipid soluble (CNS)
Rx Parkinsonism
Rx acute extra pyramidal symptoms induced by antipsychotics

35
Q

trihexyphenidyl

A

direct muscarinic blocker
lipid soluble (CNS)
Rx Parkinsonism
Rx acute extra pyramidal symptoms induced by antipsychotics

36
Q

ipratropium

A

direct muscarinic blocker
asthma and COPD (inhalation)
NO CNS
no change in mucus viscosity

37
Q

Donepezil

A 
indirect cholinomimetic- AchE inhibitor
lipid soluble (CNS)
Rx. alzheimers (oral bioavail 100% long DoA)
38
Q

Tacrine

A

indirect cholinomimetic- AchE inhibitor
lipid soluble (CNS)
Rx. alzheimers
no longer used due to liver toxic

39
Q

Organophophates and carbamates

A 
indirect cholinomimetic- AchE inhibitor
irreversible toxin, lipid soluble (CNS)
 rx glaucoma detox with paralidoxime
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation (CNS/ nicotinic muscle excitation then paralysis), lacrimation, salivation, sweating.
40
Q

echothiophate

A

indirect cholinomimetic- AchE inhibitor
irreversible toxin, lipid soluble (CNS)
rx glaucoma
detox with paralidoxime

41
Q

Chronic AchE inhibitor toxicity

A

peripheral neuropathy causing muscle weakness and sensory loss.
demyelination not due to AchE inhibition

42
Q

Parkinsons

A

loss of pigmented dopamine secreting dopaminergic neuronal cells of the substantia nigra. Associated with somatic deletion of mtDNA and subsequent clonal expansion of the deletions in each cell.
Treat with L-dopa (but acts globaly acting on the affect, motivation,and reward center of the brain which can lead to psychosys)
Lewy Bodies

43
Q

ANS pharm on dually innervated tissue

A 
PANS dominates in dual innervation
SA and AV nodes- bradycardia
pupil (miosis constriction/accomodation near vision cyclospasm)
salivation
GI and GU muscles
sphincters

SANS is only dominant in vascular tone (veins and arterioles) and thermoreg sweat glands.

44
Q

hexamethonium

A

Nn nicotinic receptor antagonist (ganglion block SANS or PANS)
reduce predominant autonomic tone (basal)
prevent baroreceptor reflex in HR
toxicity - rarely used

45
Q

mecamylamine

A

Nn nicotinic receptor antagonist (ganglion block SANS or PANS)
reduce predominant autonomic tone (basal)
prevent baroreceptor reflex in HR
toxicity - rarely used

46
Q

Baroreflex

A

increase MAP - increase APs (rate of change)
* Aortic arch thru Vagus (X)
* Carotid Sinuses thru glossopharyngeal (IX)
nucleus tractus solitarius of the medulla
* efferent PANS vagus X to SA node (M2)
* efferent SANS to SA, AV, muscle, Artierioles, Veins. (B1 and a2)
vasodilate (B2)

47
Q

Charbachol

A

M choline ester direct agonist
doa ~1 hr, poor AchE substrate
tx glaucoma

48
Q

Muscarine

A

M direct agonist
Toxic mushroom
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation (CNS/ nicotinic muscle excitation then paralysis), lacrimation, salivation, sweating.

49
Q

Cevimeline

A

M natural alkaloid direct agonist
M1/M3 agonist (M2 is cardio)
tx xerostomia (used with pilocarpine)

50
Q

Rivastigmine

A

indirect cholinomimetic- AchE inhibitor
transdermal patch
tx Alzheimers, dimentia, parkinsons

51
Q

Galantamine

A

indirect cholinomimetic- AchE inhibitor

tx alzeimers. natural OTC sleep aid.

52
Q

propantheline

A

direct muscarinic blocker

rx urge incontinence

53
Q

terodiline

A

direct muscarinic blocker

rx urge incontinence

54
Q

darifenacin

A

direct muscarinic blocker
M3 selective
rx urge incontinence

55
Q

solifenacin

A

direct muscarinic blocker
M3 selective
rx urge incontinence

56
Q

fesoterodine

A

direct muscarinic blocker

rx urge incontinence

57
Q

tolterodine

A

direct muscarinic blocker

rx urge incontinence

58
Q

trospium

A

direct muscarinic blocker

rx urge incontinence

59
Q

cyclopentolate

A

direct muscarinic blocker

opthalmologic produce myadriasis and cycloplegia prior to refraction

60
Q

tiotropium

A

direct muscarinic blocker
NO CNS
DoA long, inhaled solutions
Tx Asthma/COPD, xerostomia nasal spray

61
Q

trimethaphan

A

Nn nicotinic receptor antagonist (ganglion block SANS or PANS)
reduce predominant autonomic tone (basal)
prevent baroreceptor reflex in HR
toxicity - rarely used
Oral, CNS, DoA ~10hrs
Tx Aortic dissection decrease BP in emergency

Pharmacology (18 decks)

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