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Pharm II Exam I > Cholinergic > Flashcards

Cholinergic Flashcards

1
Q

Pilocarpine

A

Cholinergic agonist

Decreases intraocular pressure (narrow angle glaucoma)

SE: blurry vision, brow ache, miosis, SWEATING, SALIVATION

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2
Q

Methacholine

A

Cholinergic agonist

Bronchoconstriction (used to diagnose asthma)

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3
Q

Bethanechol

A

most GI effect; Increase peristalsis, motility, and secretions

Increase Urination

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4
Q

cholinergic GI effect

A

Bethanechol (most)

Pilocarpine (not as much)

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5
Q

Used for underactive bladder

A

Bethanechol

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6
Q

Cause sweating

A

Pilocarpine (MOST)
Muscarine
Acrecoline (betel nuts)

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7
Q

Direct cholinergic drugs

A 
Ach
Bethenachol
Pilocarpine
Cevemiline
Nicotine
Varenicline
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8
Q

Cause significant salivation

A

PILOCARPINE

cevimeline

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9
Q

What effect does IV Ach have that parasympathetics don’t?

A

Vasodilation (NO/EDGF) & Sweating

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10
Q

Bethanechol

A

Quaternary – No CNS
Resistant to AchE
Selective- muscarinic receptors
Urinary/GI effects

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11
Q

Tertiary Nitrogen

A

Pilocarpine- CNS to some degree

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12
Q

Pilocarpine, Muscarine

A

alkaloids
Selective for muscarinic
readily absorbed orally
Pilocarpine- Tertiary N – some CNS penetration
Sweat and salivation glands sensitive to pilocarpine

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13
Q

Cevimeline

A

M1 and M3, but mainly selective for M1; therefore, causes less sweating than pilocarpine

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14
Q

M1

A

salivation

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15
Q

M3

A

sweating, lacrimation, miosiss

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16
Q

Nicotine

A

selective for nicotinic receptors; patches used to quit smoking

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17
Q

Varenicline

A

partial agonist on nicotinic receptor subtype in brain

causes just enough dopamine release to relieve craving, makes smoking less pleasurable

SE: N/V, fatigue, H/a, constipation, FLATULENCE
CNS effects: sleep disturbance, vivid nightmares, pyschosis, mania, suicide

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18
Q

Muscarine

A

found in some mushrooms

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19
Q

Pilocarpine use

A

narrow-angle glaucoma

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20
Q

Tx for postop abdominal distention or gastric atony

A

Bethanechol

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21
Q

Tx for urinary retention

A

Bethanechol

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22
Q

Sjogren’s tx (or dry mouth from radiation)

A

Cevimeline (1st)

Pilocarpine (less so b/c sweating side effect)

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23
Q

Muscarine agonist SE

A 
sweating
salivation
Blurry vision
Abdominal cramping, N/V/D
Cutaneous vasodilation
Bronchoconstriction
bladder tightness
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24
Q

Contraindications for muscarinic agonists

A

PEPTIC ULCER
coronary insufficiency
ASTHMA/COPD
bowel obstruction

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25
Q

Muscarine poisoning from mushrooms

A 
salivation, tears
N/V/D
h/a, visual disturbance
bronchospasm
bradycardia, shock
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26
Q

Tx muscarine poisoning

A

atropine (antagonist) and albuterol (reverse bronchonstriction)

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27
Q

Central effects of nicotine

A

low dose: alertness & attention
High dose: tremor, vomiting, increased respiration
Toxic: convulsions

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28
Q

Peripheral effects of nicotine

A

both sympathetic and parasympathetic

Heart (sym): increase HR, HTN; may alternate w/ vagal bradycardia

GI (parasym): N/V/D, urination

NMJ: initially causes twitches or contraction, progresses to desnsitization of NMJ and flaccid paralysis

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29
Q

Nicotine toxicity

A

Vomiting
CNS: convulsions, coma, respiratory arrest
NMJ block/paralysis
HTN, Cardiac arrhythmia

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30
Q

Tx for nicotine toxicity

A

atropine (blocks muscarinic receptors- dec. parasym effects)
Anticonvulsants
Assist respiration

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31
Q

Why can’t you block nicotinic receptors in nicotine toxicity

A

they are all already block or desensitized

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32
Q

Cholinesterase Inhibitors

A

Carbamates
Edrophonium
Echothiophate
Organophosphate pesticides

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33
Q

Organophosphates

A

DFP, echothiopate, soman, sarin, parathion, malathion

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34
Q

Neostigmine MOA

A

tertiary N is attracted to negative oxygen on AchE; bind the oxygen and blocks enzymes actions; slowly hydrolyzed/released from enzyme

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35
Q

Carbamates

A

Neostigmine
Pyridostigmine
Pysostigmine

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36
Q

Use of cholinesterase inhibitors

A

reverse nerve block after surgery

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37
Q

Carbamate MOA

A

form covalent bond with AchE; last 30 mins-6 hours

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38
Q

Quaternary carbamates

A

Neostigmine and pyridostigmine – not well absorbed orally, DO NOT cross BBB

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39
Q

Tertiary Carbamate

A

Physostigmine – well absorbed orally, will get into brain

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40
Q

Edrophonium

A

Must be injected; VERY SHORT DURATION (5-10 minutes)

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41
Q

Echothiophate

A

IRREVERSIBLE bond w/ AchE

42
Q

Echothiophate use

A

occasionally used for narrow angle glaucoma b/c of long-lasting effect

43
Q

Physostigmine use

A

not used orally;

topically to decrease intraocular pressure

44
Q

Organophosphate MOA

A

phosphorylate AChE to form long-lasting bond; becomes irreversible w/ “aging”

45
Q

Aging

A

breaking one phosphorous-oxygen bond increases the strength of bond until it becomes irreversible

46
Q

Pralidoxime

A

aka 2-PAM;

prevents aging; MUST be used with 3-4 hours

47
Q

2-PAM MOA

A

strong nucleophile, which attracts the organophosphate and irreversible bind to them – prevents attachment to AChE or pulls it off enzyme if used before aging; fatal if aging is not prevented

48
Q

SE of 2-PAM

A

HTN

49
Q

Effects of AChE inhibitors

A

(Parasym effects)
CNS: alertness, improve memory; convulsions, respiratory arrest w/ poisoning
Eye: miosis, near vision
GI, Bladder: stimulation, diarrhea, urination
Resp: salivation, secretion, bronchoconstriction
CV: bradycardia, dec. force of contraction, decreased CO
- little effect on BP: no cholinergic innervation
Low conc: increase muscle strength
Higher conc: twitches, fasiculations, neuromuscular blockade, paralysis

50
Q

Neotstigmine

A

~4 hours
quaternary - no CNA, poorly absorbed orally, but still used
some direct NMJ effect

51
Q

Use of neostigmine

A

increase bladder motility
reverse neuromuscular blockade in surgery
treat myasthenia gravis

52
Q

Edrophonium use

A

diagnosis of myathenia gravis: if myathenic, muscle strength will improve for 5 min;

used to see if AChE inhibitor dose is right: edrophonium decreases strength if dose too high, increase strength if dose too low

53
Q

Physostigmine use

A

glaucoma (eye drops)

muscarinic antagonist poisoning (only systemic use b/c it is the only agonist that gets into CNS)

54
Q

Organophosphates

A

Diisopropyl fluorophosphate (DFP) - prototype

Soman, Sarin, Tabun (nerve gases, fast acting)

Malathion (thiophosphate, lipid soluble – not activated well by birds and mammals– used to overspray for mosquito control)

Parathion-many poisonings, taken off market

55
Q

Fast acting organophosphates

A

soman, sarin, tabun

56
Q

Tx for organophosphate poisoning

A

Atropine-until pupils dilate
2-PAM (if w/i 3-4 hrs)
Diazepam for seizures
respiration

57
Q

Prophylaxis (troops) for organophosphates

A

Pyridostigmine

58
Q

AChE inhibitor toxicity

A

SLUDGE:
Salivation, lacrimation, urination, defecation, gastric distress, emesis

also: miosis, sweating, bronchoconstriction, nausea, vomiting diarrhea, bradycardia, hypotension
CNS: confusion, atazia, slurring, convulsions, coma, NMJ stimulation followed by blockade, causing paralysis

59
Q

Antimuscarinic (anticholinergic) MOA

A

bind to muscarinic receptor; don’t activate receptor but displace Ach or agonist from receptor

60
Q

Prototype antimuscarinic

A

Atropine

61
Q

Muscarinic antagonists

A

atropine- enters CNS only at very high dose
Scopolamine (more lipid soluble, into brain easily)
Tropicamide/Homatropine (eyes)
Glycopyrrolate (surgery)
Ipratropium, tiotropium (asthma, COPD)

62
Q

Scopolamine

A

into brain easily (euphoria, sedation, amnesia);

used as transdermal patch for motion sickness

63
Q

Use of scopolamine

A

motion sickness

64
Q

Effects of atropine

A

salivary, sweat glands, bronchioles affected at low dose
heart and eye
GI, urinary tract at high doses

65
Q

Effects of atropine

A 
DRY MOUTH!, decreased sweating
increased HR
Blurred vision, tachy, palpitation
urinary retention, hot/dry skin, fatigue
weak pulse, hallucination, delirium, coma
66
Q

Drugs that block muscarinic receptors

A 
older antihistamines (benedryl)
antidepressant
antipychotics
GI meds
(poisoning common)
67
Q

CNS effects of antimuscarinics

A

atropine: little, except at toxic doses; stimulation follow by depression, can cause confusion/coma
scopolamin: drowsiness, memory loss; relieves motion sickness, dries up secretions, pre-anesthesia; toxic: hallucination, agitiation, coma

68
Q

eye antimuscarinics

A

mydriasis, lens flattens; angle gets smaller (bad in narrow-angle glaucoma); photophobia; dry eyes

69
Q

cycloplegia

A

loss of accommodation for near vision (inhibit ciliary muscle)

70
Q

Use of scopolamine

A

pre-anesthetic, motion sickness

71
Q

Contraindication of anticholinergics

A

narrow angle glaucoma

72
Q

CV effects of anticholinergics

A

tachycardia (dec. vagal tone- blocks M2 receptors leading to inc. NE release); little vagal tone in babies or elderly so atropine will have little CV effect;

little blood vessel effect (no inputs) – may block NO release;

Atropine @ high dose: vasodilation in face to decrease heat

73
Q

Respiratory use of antimuscarinics

A

reverse bronchoconstriciton, cause broncodilation (useful in ACUTE asthma attacks, COPD) (ipratropium, tiotropium)

74
Q

Respiratory antimuscarinics

A

tiotropium, ipratropium

75
Q

GI antimuscarinics

A

Dicyclomine

Atropine-Diphenoxylate (Lomotil)

76
Q

Dicyclomine use

A

decrease motility and GI secretions (antispasmodic)

77
Q

Atropine-diphenoxylate (lomotil) use

A

diarrhea

78
Q

GU antimuscarinics

A

(tinkling frequently on toilets during summer)

Tolterodine
Fesoterodine
Oxybutynin
Trospium
Darifenacin
Solifenacin
79
Q

Atropine use

A

decrease bradycardia

reverse AV block

80
Q

Glycopyrrolate use

A

surgery to decrease vagal tone (brady and secretions);

decrease muscarinic side effects when neotigmine or other cholinesterase inhibitors are used to reat myathenia gravis

81
Q

Side effects of antimuscarinics

A 
dry mouth
dry eyes
tachycardia
mydriasis
decrease GI motility
Urinary retention
Hot, dry skin (high doses)
82
Q

Contraindication of antimuscarinics

A

glaucoma

BPH

83
Q

Atropine overdose

A

dry as a bone, blind as a bat, red as a beet, mad as a hatter

tx: supportive, phystogimine (gets into CNS)

84
Q

NMJ blockade

A

block nicotinic receptor on skeletal muscle:

85
Q

Depolarizing NMJ blocker

A

stimulates, densensitizes, leads to paralysis (Succinylcholine)

86
Q

Non-depolarizing NMJ Blocker

A

competitive antagonist for nicotinic receptor; can be overcome by increasing Ach concentration (D-Tubocurarine); highly ionized – must be injected

87
Q

non-depolarizing drug used in surgery

A

D-Tubocurarine
Rocuronium
Vecuronium
Cisatracurium

88
Q

Reversal of non-depolarizing NMJ block

A

AChE inhibitor – Neostigmine (or edrophonium)

89
Q

non-depolarizing blocking order

A

Onset: 1-6 minutes
small muscles –> trunk –> respiratory last

Respiratory first to cover –> thumb last to recover

(if thumb is recovered, they know lungs have recovered so they can take off ventilator)

90
Q

Succinylcholine facts

A

worst VERY FAST – used for intubation

Depolarizes before blocking, very brief action w/ rapid onset

91
Q

Hydrolysis of succinylcholine

A

pseudocholiesterase
genetic differences in hydrolysis - expressed in terms of dibucaine number; dibucaine is a local anesthetic that causes inhibition of cholinesterase; normal dibucaine inhibition (80%), 20% means cholinesterase is abnormal and effects of succinylcholne can last hours, instead of minutes; AchE inhibitor will prolong action

92
Q

Low dibucain (20%)

A

succinylcholine will last hours instead of minutes

93
Q

Succinylcholine times

A

onset: 1 minutes
duration: 5-10 minutes (unless low dibucaine)

94
Q

Side effect of succinylchline

A

Hyperkalemia: K+ released when nicotinic receptors stimulated; may lead to cardiac arrest - most common w/ denervated muscle or burns (nicotinic receptors upregulated)

95
Q

Contraindications of succinylcholine

A 
extensive soft tissue damage
severe burns
nontraumatic rhabdo
quadriplegia, paraplegia
muscular dystrophy
in children < 8 (unless emergency)
96
Q

NMJ blocker interactions

A

inhaled anesthetics (halothane) - uncontrolled release of caclium from SR leading to muscle rigidity and high temperature (MALIGNANT HYPERTHERMIA)

97
Q

Tx for malignant hyperthermia

A

dantrolene

98
Q

Ganglion Blockers

A

Hexamethonium; mecamylamine

not used clinically

99
Q

Effects of ganglion blockade

A

effects dependent on dominant tone:

Eye: cycloplegia, mydriasis
Blood vessels: dilation, orthostatic hypotension

Heart: contractility blocked, decreased vagal tone- tachycardia

GU: decreased bladder tone, retention w/ BPH, erection/ejaculation reduced

No sweating

Reflex responses to brain blocked – no ability of ganglion to send messages to brain

100
Q

Hexamethonium man

A 
pink, pale (can't constrict veins)
warm, dry
placid, can't cry
doesn't blush or get pale
no sweat
dry mouth
far-sighted
urinary retention, impotence
constipated

Pharm II Exam I (3 decks)

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