Tackett 08-30-07 Cholinergic / Anticholinergic Drugs

Front 1

where is nicotinic-g receptor

Back 1

ACh receptor at parasympathetic/sympathetic ganglia

Front 2

type of receptor at parasympathetic organ?

Back 2

muscarinic

Front 3

neurotransmitter at alpha/beta receptors

Back 3

NE

Front 4

neurotransmitter at muscarinic receptors

Back 4

ACh

Front 5

for the most part, nicotic actions create _____ :(

Back 5

side-effects

Front 6

For the most part, indirect acting cholinomimetic drugs inhibit ______

Back 6

Ach-esterase

Front 7

examples of direct acting cholinomimetic drugs

Back 7

Ach
Bethanechol
Pilocarpine

Front 8

examples of indirect acting cholinomimetic drugs

Back 8

Physostigmine
Neostigmine
Edrophonium

Front 9

Acetylcholine is
a) specific
b)nonspecific

Back 9

nonspecific (muscarinic/nicotinic)

Front 10

Why does ACh have a short duration of action?

Back 10

ACh-esterase

Front 11

ACh has nicotinic action: describe its side-effect profile.
a) poor
b) rich
c) no side-effects

Back 11

poor = side-effect prone

Front 12

initial effect of IV Ach on Heart rate and BP

Back 12

increase both initially

(subsequent decrease in both)

Front 13

Direct acting cholinergic drugs

Back 13

Ach (Miochol-E)
Bethanechol (Urecholine)
Carbachol
Cevimeline (Evoxac)
Pilocarpine

Front 14

Side effect of Pilocarpine

Back 14

diarrhea

Pile o' crap-ine

Front 15

cholinergic agonists are more resistant to _______

Back 15

ACh-esterase

Front 16

Cholinergic Agonist directly stimulate ___________receptor

Back 16

muscarinic

Front 17

Cholinergic Agonist effect on the eye

Back 17

miosis
improved near vision

Front 18

Cholinergic Agonist effect on the heart

Back 18

decreased HR
decreased CF
decreased conduction

Front 19

Cholinergic Agonist effect on the lung

Back 19

bronchoconstriction
increased secretion

Front 20

Cholinergic Agonist effect on GI

Back 20

increased motility
relaxed sphincters
increased secretion

Front 21

Cholinergic Agonist effect on urinary bladder

Back 21

contraction
relaxed spinchters

Front 22

Cholinergic Agonist effect on glands

Back 22

secretion

Front 23

Cholinergic agonist used as a test for asthma

Back 23

methanacol (provocholine)

Front 24

Bethanechol is selective for ________and _______

Back 24

GI and urinary tracts

Front 25

Bethanechol is the DOC for postoperative, postpartum, neurogenic _____________

Back 25

urinary retention

Front 26

Bethanechol is used for reflux_________

Back 26

esophagitis

Front 27

Bethanechol is used for postoperative abdominal ________

Back 27

distension

Front 28

Carbachol has a poor side effect profile b/c ________

Back 28

has muscarinic and NICOTINIC actions

Front 29

main usage for carbachol

Back 29

1- treatment of glaucoma

2- for cataract surgery: to reduce intraocular pressure and produc miosis

Front 30

pilocarpine is specific for _______ receptors

Back 30

muscarinic

Front 31

pilocarpine has minimal ________ actions

Back 31

nicotinic

Front 32

Pilocarpine is used to reverse _________

Back 32

mydriasis
and
effects of cyclopegic agents

Front 33

pilocarpine is most commonly used cholinergic agonist to treat _________

Back 33

glaucoma

Front 34

pilocarpine used to treat dry mouth by increasing _______

Back 34

salivation

Front 35

Muscarine is specific for _______ receptors

Back 35

muscarinic

Front 36

side effects of direct acting cholinergic agonists

Back 36

sweating, salivation,
cutaneous vasodilation with flushing,
nausea, vomiting, diarrhea,
HR changes, hypotension

Front 37

contraindication of cholinergic agonists

Back 37

asthma,
peptic ulcer,
Parkinsonism,
Pregnancy,
Severe cardiac disease,
hyperthyroidism (arrhythmias),
mechanical obstruction or impairment of GI or urinary tract

Front 38

Indirect acting drugs potentiate the effects of ACh by inhibiting ________

Back 38

hydrolysis

Front 39

Indirect acting drug effects are due to ACh stimulating __________

Back 39

muscarinic and nicotinic receptors

Front 40

Reversible Anticholinesterases

Back 40

Physostigmine, Pyridostigmine, Neostigmine,
Demecarium, Ambenoenium, Edrophonium

Front 41

Irreversible Anticholinesterases

Back 41

Isoflurophate, Echothiophate,
Malathion, Parathion,
Tabun,
Paraoxon

Front 42

Physostigmine can be used to treat _______, but pilocarpine is preferred

Back 42

glaucoma

Front 43

Physostigmine is used for treatment of ___________, but be careful to avoid seizures, bradycardia

Back 43

anticholinergic intoxication (ex. curare overdose)

Front 44

Neostigmine has ACh-esterase action and direct _____-like action

Back 44

ACh

Front 45

Neostigmine has muscarinic effects due to ___________ inhibition

Back 45

cholinesterase

Front 46

Neostigmine has nicotinic effects at neuromuscular sites due to _____________

Back 46

direct stimulation

Front 47

Neostigmine's muscarinic action are used to treat ________

Back 47

postoperative distension and urinary retention

Front 48

Neostigmine' nicotinic actions can be used to reverse ________

Back 48

paralysis induced by neuromuscular blocking agents

Front 49

Side effects of neostigmine

Back 49

Elevation of skin temperature,
Sweating,
Salivation,
Bradycardia with hypotension
Skeletal muscle fasciculations

Front 50

Neostigmine Substitutes

Back 50

Pyridostigmine
Ambenonium
Demecarium

Front 51

Pyridostigmine used for _____

Back 51

-used for chronic management of myasthenia gravis

Front 52

Ambenonium used for______

Back 52

- used also for management of myasthenia

Front 53

Demecarium used for _______

Back 53

-used for glaucoma

Front 54

Edrophonium has a _____ duration of action

Back 54

short

Front 55

Edrophonium is Used as a diagnostic tool for ______

Back 55

myasthenia

Front 56

Edrophonium produces ________ in untreated myasthenia patient

Back 56

rapid, transient increase in muscular strength

If strength improves, increase therapy
If response is unfavorable, decrease therapy

Front 57

Edrophonium Used as an antidote to

Back 57

curare

Front 58

Irreversible organophosphorus anticholinesterases Bind _____

Back 58

irreversibly with the enzyme - enzyme becomes permanently phosphorylated

Front 59

Irreversible organophosphorus anticholinesterases Effects remain until ________

Back 59

new enzyme is regenerated

Front 60

Irreversible organophosphorus anticholinesterases Effects may persist for ______

Back 60

weeks or months

Front 61

Measurement of RBC Achase can be used to assess _______

Back 61

severity of intoxication of Irreversible organophosphorus anticholinesterases

Front 62

Isoflurophate and echothiophate are used for ______ therapeutically

Back 62

glaucoma

Front 63

Malathion can be used to treat _________

Back 63

head lice

Front 64

Organophosphates Most commonly used as ____________

Back 64

insecticides

Front 65

Organophosphates Developed as _________

Back 65

chemical warfare agents

Front 66

Organophosphates Toxicology is significant due to___________

Back 66

High lipid solubility
Absorbed through skin, ingestion or inhalation
Readily enter CNS

Front 67

Most common symptoms of Organophosphate Toxicity include __________________

Back 67

nausea, dizziness, vomiting, abdominal pain, weakness, blurred vision and headache

Front 68

Plasma cholinesterase is regenerated in _______

Back 68

2 weeks

Front 69

Neural cholinesterase may require _____ months to completely restore the enzyme

Back 69

1-3

Front 70

Organophosphate Toxicity Vision disturbances and headache can persist for ________

Back 70

more than a month

Front 71

Muscarinic manifestations of Organophosphate Toxicity

Back 71

bronchoconstriction, increased bronchial secretions, sweating, salivation, lacrimation, bradycardia, miosis, blurred vision, urinary incontinence

Front 72

Nicotinic manifestations of Organophosphate Toxicity

Back 72

muscular fasciculations, tachycardia, hypertension

Front 73

CNS manifestations of Organophosphate Toxicity

Back 73

restlessness, insomnia, tremors, confusion, ataxia, convulsions, respiratory depression, CVS collapse

Front 74

Used to regenerate Achase after it has been phosphorylated by irreversible anticholinesterase

Back 74

Pralidoxime

Front 75

Pralidoxime is Not used in intoxication by reversible anticholinesterase due to __________

Back 75

its own anticholinesterase activity

Front 76

Treatment of Organophosphorus Toxicity

Back 76

Treat symptomatically - support respiration and CVS

Front 77

___________ reverses neuromuscular effects of Organophosphorus Toxicity

Back 77

Pralidoxime

Front 78

_________used for muscarinic and CNS effects but scopolamine may be more effective for CNS effects of Organophosphorus Toxicity

Back 78

Atropine

Front 79

Prototype Cholinergic Antagonists are _______

Back 79

atropine and scopolamine

Front 80

Sensitivity of tissues to atropine:

Back 80

Salivary glands>sweat glands>eye and heart>GI and urinary tract

Front 81

________ is more effective in the eye and has more prominent CNS actions

Back 81

Scopolamine

Front 82

Cholinergic Antagonists Effects on CVS:
High therapeutic dosages produce _______

Back 82

tachycardia

Front 83

Cholinergic Antagonists Effects on CVS:
Small doses may decrease ____ due to central stimulation of vagus

Back 83

HR

Front 84

Cholinergic Antagonists effects on blood pressure

Back 84

Minimal

Front 85

Large doses of atropine may cause ________

Back 85

flushing (atropine flush)

Front 86

Cholinergic Antagonists Effects on GI and urinary tract

Back 86

Requires large doses
Reduces motility and tone more than secretion
Favors urinary retention by promoting contraction of sphincter

Front 87

Cholinergic Antagonists Effects on eye

Back 87

Produce prolonged (up to 2 weeks) mydriasis and cycloplegia

Front 88

Cholinergic Antagonists Contraindicated in

Back 88

narrow angle glaucoma patients

Front 89

Cholinergic Antagonists Effects on CNS

Back 89

High doses produce excitation, hallucinations, delirium
Scopolamine used for motion sickness, preanesthetic, sedation
Can produce amnesia

Front 90

Opthalmologic Uses of Cholinergic Antagonists

Back 90

Mydriatic
Break adhesions

Front 91

Perioperative uses of Cholinergic Antagonists

Back 91

Dry secretions
Prevent vagal bradycardia
Reduce dose of anesthetic
Scopolamine used for sedative and amnesic effects
Prevent muscarinic effects of neuromuscular blocking agent

Front 92

Cardiac uses of Cholinergic Antagonists

Back 92

Prevent bradycardia after MI

Front 93

GI disease uses of Cholinergic Antagonists

Back 93

Once used to treat peptic ulcer by decreasing vagal mediated secretion, relieve spasm, and slowing gastric emptying
Side effects limited use

Front 94

Uses of Cholinergic Antagonists

Back 94

Motion sickness
Antimuscarinic intoxication
Asthma

Front 95

Atropine Substitutes: Mydriatics (short acting)

Back 95

Homatropine Cyclopentolate
Tropicamide

Front 96

Atropine Substitutes: Anticholinergic smooth muscle relaxants

Back 96

Methscopolamine Propantheline
Dicyclomine
Use for GI problems has been replaced by antihistamines
Used for urinary incontinence

Front 97

Neuromuscular Blocking Agents Act on ________

Back 97

nicotinic receptors

Front 98

Nondepolarizing Agents compete with ____ for receptors

Back 98

Ach

Front 99

Depolarizing agents initially stimulate the neuromuscular junction and then _______

Back 99

block it.

Front 100

Nondepolarizing Agents

Back 100

Tubocurare Metocurine
Pancuronium Gallamine
Atracurium Vercuronium

Front 101

Botulinum Toxin Enters cholinergic nerve endings and inhibit ________

Back 101

exocytosis

Front 102

Botulinum Toxin Used for treatment of __________ of eye

Back 102

strabismus and blepharospasm

Front 103

Botulinum Toxin Used for smoothing _______

Back 103

wrinkles

Front 104

Side effects of Botulinum Toxin include excessive tearing and _________

Back 104

unilateral ptosis

Front 105

Ganglionic Blocking Drugs

Back 105

Hexamethonium
Trimethaphan

Front 106

Ganglionic Blocking Drugs In past, used as antihypertensives. Now, Rarely used due to _______

Back 106

toxicity

Front 107

The majority of therapeutic actions of cholinergic drugs are focused on an interaction at the __________ receptor

Back 107

muscarinic

Front 108

Side effects of cholinergic drugs are predictable, dose related
Excessive action on the muscarinic receptor
Interaction with ________ receptor

Back 108

nicotinic

Front 109

A

Back 109

B