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Pharma > 06 - Autonomic, 07 - Cholinoreceptor-activating and cholinesterase inhibiting drugs > Flashcards

06 - Autonomic, 07 - Cholinoreceptor-activating and cholinesterase inhibiting drugs Flashcards

1
Q

Spinal roots of origin SANS

A

Thoracic T1-12
Lumbar L1-5
segments of SC

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2
Q

Spinal roots of origin PANS

A

CN III, VII, IX, and X

sacral segments of spinal cord

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3
Q

Location of ganglia SANS

A

paravertebral chains that lie along the spinal column, some along the anterior aspect of the abdominal aorta

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4
Q

Location of ganglia PANS

A

most are located in the organs innervated, more distant from the spinal cord

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5
Q

Preganglionic fibers SANS

A

short

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6
Q

Preganglionic fibers PANS

A

long

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7
Q

postganglioni fibers SANS

A

long

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8
Q

postganglioni fibers PANS

A

short

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9
Q

Pupils sympathetic effect/receptor

parasympathetic effect/receptor

A

mydriasis a1

miosis m3

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10
Q

Heart rate sympathetic effect/receptor

parasympathetic effect/receptor

A

tachycardia B1

bradycardia M2

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11
Q

Heart contractility sympathetic effect/receptor

parasympathetic effect/receptor

A

increased b1

decreased m1

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12
Q

Blood vessels skin, splanchnic sympathetic effect/receptor

parasympathetic effect/receptor

A

constriction a1

no effect

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13
Q

Blood vessels skeletal sympathetic effect/receptor

parasympathetic effect/receptor

A

dilation b2, m3

no effect

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14
Q

bronchi sympathetic effect/receptor

parasympathetic effect/receptor

A

dilation b2

constriction m3

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15
Q

GIT walls sympathetic effect/receptor

parasympathetic effect/receptor

A

relaxation a2, b2

contraction m3

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16
Q

GIT spincters sympathetic effect/receptor

parasympathetic effect/receptor

A

contraction a1

relaxation m3

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17
Q

GIT secretion sympathetic effect/receptor

parasympathetic effect/receptor

A

no effect

increased m1, m3

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18
Q

bladder wall sympathetic effect/receptor

parasympathetic effect/receptor

A

relaxation b2

contraction m3

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19
Q

bladder sphincter sympathetic effect/receptor

parasympathetic effect/receptor

A

contraction a1

relaxation m3

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20
Q

uterus sympathetic effect/receptor

parasympathetic effect/receptor

A

contraction a1, relaxation b2

contraction m3

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21
Q

penis sympathetic effect/receptor

parasympathetic effect/receptor

A

ejaculation a

erection m

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22
Q

sweat glands sympathetic effect/receptor

parasympathetic effect/receptor

A

increased sweating a

no effect

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23
Q

liver sympathetic effect/receptor

parasympathetic effect/receptor

A

gluconeogenesis, glycogenolysis a,b2

no effect

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24
Q

fat cells sympathetic effect/receptor

parasympathetic effect/receptor

A

lipolysis b3

no effect

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25
Q

kidney sympathetic effect/receptor

parasympathetic effect/receptor

A

increased renin b1

no effect

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26
Q

PLASMA mnemonic

A 
for parasympathetic nervous system
P-NS
L-ong preganglionic fibers
A-cetylcholine
S-hort postganglionic fibers
A-cetylcholine
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27
Q

Point and shoot mnemonic

A

point (erection) = PNS

shoot (ejaculation) = SNS

28
Q

primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic neurons and their effector cells
primary transmitter at the somatic (voluntary) skeletal muscle neuromuscular junction

A

acetylcholine

29
Q

ACh is synthesized from acetyl CoA and choline by

A

ChAT

choline acetyltransferase

30
Q

choline transport is inhibited by

A

hemicholinium

31
Q

ACh is actively transported into vesicles for storage by

A

VAT

vesicle associated transporter

32
Q

VAT is inhibited by

33
Q

entry of calcium triggers interaction among

A

SNARE proteins

VAMPs and SNAPs

34
Q

toxin that alters synaptobrevins to prevent release of ACh

35
Q

degradation of ACh into choline and acetate by

A

acetylcholinesterase

36
Q

degradation of ACh is inhibited by

A

inderect actin cholinomimetics

neostigmine, carbamates, and organophosphates

37
Q

Cholinomimetic drug types

A

direct acting

  • muscarinic (choline esters, alkaloids)
  • nicotinic

indirect

  • edrophonium (short acting)
  • carbamates (intermediate to long)
  • organophosphates (very long)
38
Q 
BETANECHOL
class
similar drug
MOA
uses
SE
A
  • cholinomimetic (direct-acting, muscarinic)
  • carbachol (act on both M and N receptors)
  • activates muscarinic M1-M3 receptors (act on M receptors only)
  • bladder and bowel atony (post-surgery or spinal cord injury)
  • cyclospasm, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating
39
Q 
PILOCARPINE
class
similar drug
MOA
uses
SE
A
  • cholinomimetic (direct-acting, muscarinic)
  • cevimeline (m3 selective)
  • activates muscarinic M3 receptors in ciliary muscle (increasing aqueous humor outflow) and salivary glands (increasing salivation)
  • glaucoma, sjorgren syndrome, sicca syndrome
  • miosis, blurring of vision (due to cyclospasm)
40
Q

Sjogren syndrome triad

A

xerostomia (dry mouth)
xerophthalmia (dry eyes)
RA

41
Q 
NICOTINE
class
similar drug
MOA
uses
SE
A
  • cholinomimetic (direct-acting, nicotinic)
  • varenicline
  • activates nicotinic Ach receptors (Nn and Nm)
  • smoking cessation
  • generalized ganglionic stimulation (hypertension, tachycardia, nausea, vomiting, diarrhea)

overdose leads to convulsions, paralysis, and coma

42
Q

Muscarinic toxicity CNS stimulation or depression?

A

stimulation

43
Q

Muscarinic toxicity eye

A

miosis, spasm of accomodation

44
Q

Muscarinic toxicity lungs

A

bronchoconstriction

45
Q

Muscarinic toxicity GIT/GUT

A

excessive GI and genitourinary smooth muscle activity

46
Q

Muscarinic toxicity increased secretory activity in

A

sweat glands
airway
GI tract
lacrimal glands

47
Q

Muscarinic toxicity blood vessels

A

vasodilation

48
Q

Nicotinic toxicity ganglionic stimulation or depression?

A

stimulation

49
Q

Nicotinic toxicity blockade of

A

neuromuscular end plate depolarization leading to fasciculations and paralysis

50
Q

Nicotinic toxicity CNS stimulation or depression?

A

CNS stimulations (convulsions) followed by CNS depression

51
Q

MOA of indirect-acting cholinomimetics

A
  • bind to cholinesterase and undergo prompt hydrolysis
  • alcohol portion released, acidic portion retained and released slowly
  • – prevents binding and hydrolysis of endogenous ach
  • – amplify ach effects wherever ach is released
  • no significant actions at uninnervated sites where ach is not normally released
52
Q 
EDROPHONIUM
class
similar drug
MOA
uses
SE
A
  • cholinomimetic (indirect) [alcohol]
  • none
  • inhibits acetylcholinesterase, amplifies endogenously released ach
  • myasthenia gravis (tensilon test)
  • miosis, salivation, nausea, vomiting, diarrhea

very short acting upon IV administration

53
Q

EDROPHONIUM

tensilon test

A

for differentiation of cholinergic crisis and myasthenic crisis

improves muscle strength in myasthenic crisis
weakens muscle strength in cholinergic crisis

54
Q 
NEOSTIGMINE
class
similar drug
MOA
uses
SE
A
  • cholinomimetic (indirect)
  • pyridostigmine, physostigmine, ambenonium, demecarium (carbamates), echothiophate (organophosphate)
  • inhibits acetylcholinesterase, amplifies endogenously released ach
  • myasthenia gravis treatment, reversal of nondepolarizing neuromuscular blockade, glaucoma (physostigmine, echothiophate, demecarium)
  • miosis, salivation, nausea, vomiting, diarrhea, bradycardia
55
Q

NEOSTIGMINE

muscarinic effects are blocked by

56
Q

Other organophosphates:

insecticides

A

malathion

parathion

57
Q

Other organophosphates:

nerve gases

A

sarin
tabun
soman

58
Q

myasthenia gravis

A 
autoimmune destruction of nicotinic ach receptors
characterized by:
- fluctuating muscle
- weakness
- ocular symptoms
- bulbar symptoms
- proximal muscle weakness
59
Q

differentiate myasthenic crisis from cholinergic crisis

A

myaesthenic crisis - acute worsening of symptoms due to infection, stress, or undermedication

cholinergic crisis - excessive activation of cholinoreceptors (skeletal muscle weakness and parasymapthetic signs) due to overmedication

60
Q 
RIVASTIGMINE
class
similar drug
MOA
uses
SE
A
  • cholinomimetic (indirect)
  • galantamine, donepezil, tacrine
  • inhibits acetylcholinesterase, amplifies endogenously released acetylcholine
  • alzheimer’s disease
  • miosis, salivation, nausea, vomiting, diarrhea, bradycardia
61
Q

organophosphate poisoning signs and symptoms

A

DUMBBELSS

diarrhea
urination
miosis
bronchospasm
bradycardia
excitation (skeletal muscle and CNS)
lacrimation
sweating
salivation
62
Q

treatment of organophosphate poisoning

A

atropine

pralidoxime

63
Q 
ATROPINE
class
similar drug
MOA
uses
SE
A
  • cholinergic antagonist (muscarinic)
  • blah
  • competitively blocks all muscarinic receptors
  • mydriatic, cyclopegic, antidote for organophosphate poisoning (first choice), bradycardia, hypersalivation, decrease airway secretion during general anesthesia
  • tachycardia, mydriasis, cyclopegia, skin flushing, delirium, hallucinations, urinary retention, constipation

no effect on nicotinic signs of toxicity; notorious for causing hyperthermia

64
Q 
PRALIDOXIME
class
similar drug
MOA
uses
SE
A
  • cholinesterase regenerator, antidote
  • blah
  • binds phosphorus of organophosphate, breaks organophosphate bond with cholinesterase
  • antidote for organophosphate poisoning and nerve gas poisoning (sarin, tabun)
  • muscle weakness
  • must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs
65
Q

Cholinoreceptor blocker types

A

anticholinergic drugs

  • antimuscarinic
  • –M1-selective (pirenzepine)
  • –non-selective (atropine)
  • antinicotinic
  • –ganglion blockers (hexamethonium)
  • –neuromuscular blockers (tubocurarine)

cholinesterase regenerators
- oximes (pralidoxime)

Pharma (7 decks)

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