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Pharmacology FINAL > Cholinergic Antagonists Part 1 > Flashcards

Cholinergic Antagonists Part 1 Flashcards

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1
Q

name 2 kinds of nicotinic antagonists

A

ganglionic blockers
neuromuscular blockers

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2
Q

cholinergic antagonists will cause what kind of responses?

A

FIGHT OR FLIGHT
will mimic sympathetic nervous systek

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3
Q

explain how neuromuscular blockers work

A

they bind to Nm receptors on the postsynaptic membrane of skeletal muscle, PREVENTING the binding of ACh

prevents motor endplate from depolarizing - muscle paralysis

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4
Q

explain how ganglionic blockers work

A

prevent ACh (released from preganglionic neuron) from binding Nn receptor on the ganglia, in both the PSNS and SNS

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5
Q

explain how muscarinic blockers work

A

prevent ACh from binding to the muscarinic receptors on smooth muscle, cardiac tissue, secretory glands, etc

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6
Q

explain the history of cholinergic antagonists

A

from Belladonna plants - Atropa Belladona (source of atropine) and Datura stramonium

preparations of belladonna were used in ancient india and the roman empire used it as poisoning

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7
Q

what are the 3 classes of cholinergic antagonists?

A

naturally occurring alkaloids

semisynthetic derivatives of these alkaloids

synthetic derivatives

*imp to know examples

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8
Q

name 2 naturally occuring alkaloids that are cholinergic antagonists

A

atropine
scopolamine

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9
Q

name 2 semisynthetic derivatives of atropine and scopolamine

A

homatropine

some quaternary ammonium derivatives

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10
Q

name a synthetic derivative that is a cholinergic antagonist

A

ipratropium — has selectivity for some subtypes of the muscarinic receptors

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11
Q

explain the action of muscarinic antagonists

A

prevent the effects of acetylcholine by blocking its binding to muscarinic receptors

these muscarinic receptors can be on effector cells at parasympathetic Neuroeffector junctions, in peripheral ganglia, and in the CNS

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12
Q

TRUE OR FALSE

muscarinic antagonists are not selective

A

FALSE

they are selective for certain subtypes

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13
Q

explain the metabolism and excretion of cholinergic antagonists

A

half of the drug is excreted UNCHANGED in the urine (bc so hydrophilic)

the other half is hydrolyzed and conjugated and ecreted

thus, the effects are gone very quickly in all organs EXCEPT THE EYE

the effect on iris + ciliary muscles may last over 72 hours

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14
Q

explain the mechanism of action of atropine

A

a competitive (reversible) blockade of ACh at muscarinic receptors

prevents the release of IP3 and prevents the inhibition of adenylyl cyclase (M1, M3, M5)

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15
Q

true or false

atropine is not selective for its receptors

A

FALSE

it’s highly selective for muscarinic receptors

binds M1, M2, and M3 - not selective for subgroups, but selective for muscarinic in general

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16
Q

explain the effect of scopolamine and atropine on the CNS

A

Scopolamine has CNS affects like drowsiness and amnesia

atropine has minimal effect on the CNS. slow, long lasting sedative effects

in toxic doses, esp scopolamine can cause hallucination and coma

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17
Q

true or false

atropine is used to treat parkinsons disease

A

FALSE – used to decrease the TREMORS that result from parkinsons

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18
Q

scopolamine is used to treat…..

A

vestibular disturbances - motion sickness
that involves cholinergic transmissionw

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19
Q

what is scopolamine

A

a muscarinic antagonist

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20
Q

name 2 cholinergic inverse agonists

A

atropine
ipratropium

brings original action down below the baseline

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21
Q

true or false

atropine is highly selective for muscarinic receptors

A

true
selective for muscarinic receptors in general but
not selective for M1,M2,M3 – binds all 3

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22
Q

true or false

atropine is competitive with Ach at muscarinic receptors

A

TRUE

reversible and competitive
both bind to same site

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23
Q

true or false

scopolamine is a muscarinic antagonist

A

TRUE

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24
Q

what is mydriasis

A

dilation of the eye

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25
what is cycloplegia
weakened contraction of the ciliary muscle
26
what drug can be used to cause mydriasis and cycloplegia?
ATROPINE ******8
27
true or false atropine increase lacrimation
FALSE - decreases that's why used for treatment of mydriasis and cycloplegia
28
what is the result of atropine on the heart
causes TACHYCARDIA (fast heartbeat) SA and AV node are very sensitive to antimuscarinics
29
HOW does atropine cause tachycardia
by blocking vagal slowing
30
true or false atropine causes vasodilation
FALSE vasoconstriction
31
true or false atropine can cause increased blood pressure
TRUE due to vasoconstriction + tachycardia
32
what is the effect of an anticholinergic on salivary secretion
decreases salivary secretion and causes dry mouth
33
true or false anticholinergics cause bronchoconstriction
FALSE - bronchodilation
34
selective ________ agents are best for treatment of asthma and COPD
selective to M3 bronchodilation M3 is glands, smooth muscle, and endothelium
35
TRUE OR FALSE anticholinergics have no effect on the uterus
TRUE
36
what is the effect of anticholinergics on the genitourinary tract
the smooth muscle of the ureters and bladder wall relaxes and SLOWS VOIDING
37
true or false anticholinergics contract the smooth muscle of the ureters and bladder wall and thus slow voiding
FALSE relax this smooth muscle which slows voiding
38
what is the effect of atropine on sweating?
suppresses THERMOREGULATORY sweating
39
as mentioned, atropine suppresses thermoregulatory sweating explain a negative effect of this
in infants and children, even normal doses can cause "atropine fever" bc the body isn't sweating enough to cool itself down
40
true or false anticholinergics increase tremors
FALSE - decrease ex: atropine used to treat parkinson's tremors
41
besides atropine, name 3 other anticholinergics used to treat the tremors from parkinsons
benztropine (cogentin) benzhexol (Artane) procyclidine
42
name 2 adverse effects of scopolamine
sedation, dry mouth
43
true or false homoatropine is synthetic
false - semisynthetic
44
how are anticholinergics used in ophthalmic examination?
to cause mydriasis and cycloplegia (ciliary paralysis)
45
for adults and for older children, _____ acting drugs are preferred for ophthalmic examination
shorter
46
true or false cholinomimetics are used for ophthalmic examination
false anticholinergics
47
what kind of preparations are useful to prevent synechia (adhesion) formation in uveitis and iritis?
longer lasting anticholinergics like homoatropine
48
name 5 anticholinergics used as eye drops
atropine scopolamine homatropine cyclopentolate tropicamide
49
rank the 5 anticholinergic eye drops in order of duration of action
longest: atropine scopolamine homatropine cyclopentolate shortest = tropicamide
50
name 2 drugs used pre-surgery to prevent laryngospasm and decrease secretions
atropine and scopolamine
51
name 3 drugs used in COPD
ipratropium tiotropium aclidinium iprat and tio also used in asthma
52
true or false to treat asthma and COPD, an anticholinergic can be used
true
53
graves disease
hyperthyroidism
54
how can atropine be used in people with graves disease?
hyperthyroidism can cause atrial fibrillation atropine can treat
55
_______ can be used in myocardial infarction
atropine bc myocardial infarction leads to bradycardia and decreased cardiac output, potentially leading to fainting
56
atropine can be used in patients with circulating......
cardiac M2 antibodies
57
what can treat traveler's diarrhea
atropine + diphenoxylate (low dose opioid) = lomotil
58
how can anticholinergics be used in urinary disorders
in bladder spasm and urinary urgency, urinary incontinence
59
what is urinary incontinence and how can it be treated
involuntary leakage of urine bc of loss of bladder control treated with anticholinergics
60
name 3 sources of cholinergic poisoning
insecticides (cholinesterase inhibitors) wild mushrooms chemical warfare
61
name 2 remedies to cholinergic poisioning
-use antimuscarinic therapy (atropine - a tertiary amine) -use cholinesterase regenerators (pralidoxime)
62
true or false there is NO way to directly block the nicotinic effects that occur bc of cholinesterase inhibition
true only the muscarinic part - give atropine
63
how is it possible for pralidoxime to be used in cholinergic poisoning
pralidoxime can remove the phosphate from the enzyme-organophosphate complex bc it has a higher affinity for the phosphate enzyme has been regenerated
64
what is mushroom poisoning and what is used to treat it
due to too much cholinergic activity - nausea, vomiting, diarrhea, urinary urgency, sweating, salivaiton, bronchoconstrivtion PARENTERAL ATROPINE IS GIVEN **
65
when an antimuscarinic agent is used to reduce GI motility/secretion, name 2 adverse effects
mydriasis cycloplegia
66
what are the results of atropine poisoning
dry mouth mydriasis tachycardia hot and flushed skin agitation delirium for as long as 1 week children and infants = atropine fever. very subject to hyperthermic effects
67
what are ganglionic blockers/ganglion blocking agents?
COMPETITIVELY block the action of ACH and similar agonists at Nn receptors of parasymp and symp autonomic ganglia some also BLOCK THE ION CHANNEL that's gated by the nicotinic cholinoceptor
68
explain the clinical use of ganglionic blockers
they can block all autonomic outflow, and have a LACK of selectivity this, there are a lot of undesirable effects when used, and thus they have limited clinical use
69
true or false ganglionic blockers noncompetitively block the action of ACh at Nm receptors of both parasympathetic and sympathetic autonomic ganglia
FALSE competitively block at Nn RECEPTORS (neuronal nicotinic)
70
name 4 ganglionic blockers******* what are they blocking?
blocking action of ACh at Nn receptors of both sympathetic and parasympathetic ganglia hexamethonium mecamylamine tetraethylammonium decamethonium
71
explain the structure of the ganglionic blockers
they are synthetic amines and structurally similar to acetylcholine (remember - competes with same site ! makes sense that they're similar)
72
which of the ganglionic blockers was first identified? what is its duration of action?
tetraethylammonium short duration
73
which of the ganglionic blockers was first used clinically to treat hypertension
hexamethonium
74
why was mecamylamine developed originally
to improve absorption from GI trat]ct
75
analog of hexamethonium and a depolarizing neuromuscualr blocking agent
decamethonium
76

Pharmacology FINAL (11 decks)

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