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Neuro 2-Unit 2 > Cholinergic agonists and antagonists-Kruse > Flashcards

Cholinergic agonists and antagonists-Kruse Flashcards

1
Q

These direct-acting cholinergic agonists contain permanently charged quaternary NH4 groups that result in their poor absorption and distribution into the CNS

A

choline esters

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2
Q

List the ranking of direct-acting cholinergic agonists, choline esters, from most rapid to least rapid in terms of cholinesterase metabolism

A

ach > methacholine > carbachol = bethanechol

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3
Q

These direct-acting cholinergic agonists are uncharged tertiary amine that are well absorbed from most sites of administration

A

Alkaloids

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4
Q

Which choline ester has the greatest muscarinic action? Nicotinic action?

A

Muscarinic: Methacholine

Nicotinic: Ach and Carbachol

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5
Q

List the location, Structural features (2nd messenger), and mechanism of M1 receptors

A

location=nerves
Structural=Gq/11
Mechanism: IP3, DAG

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6
Q

List the location, Structural features (2nd messenger), and mechanism of M2 receptors

A

location=heart, nerves, smooth m
structural=Gi/0
Mechanism=inhibition of cAMP, activate K channels

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7
Q

List the location, Structural features (2nd messenger), and mechanism of M3 receptors

A

location=glands, smooth m., endothelium
structural=Gq/11
Mechanism=IP3, DAG

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8
Q

List the location, Structural features (2nd messenger), and mechanism of M4 receptors

A

location=CNS
structural=Gi/0
mechanism=inhibit cAMP

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9
Q

List the location, Structural features (2nd messenger), and mechanism of M5 receptors

A

location=CNS
structural=Gq/11
mechanism=IP3, DAG

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10
Q

List the location, Structural features (2nd messenger), and mechanism of Nn receptors

A

location=postganglionic cell body, dendrites, CNS
structural=alpha and beta only
mechanism=Na, K depolarizing ion channel

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11
Q

Nicotine has a greater affinity for __ nAChRs

A

Nicotine itself has a greater affinity for neuronal nAChRs than skeletal muscle nAChRs

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12
Q

list the parasympathetic effects of the following:

  • Sphincter muscle of iris: ___
  • Ciliary muscle of eye: ___
  • Heart: ___
  • Blood vessels: ___
  • Bronchial muscle: ___
  • Bronchial glands: ___
  • GI motility: ___
  • GI sphincters: ___
  • GI secretion: ___
  • Urinary detrusor muscle: ___
  • Urinary trigone and sphincter: ___
  • Sweat, salivary, lacrimal, nasopharyngeal glands: ___
A 
iris-contraction (miosis)
ciliary m.-contraction for near vision
heart-decrease rate/contractile strength/conduction velocity
blood vessels-dilation (via EDRF)
bronchial muscle-contraction (bronchoconstriction)
bronchial glands-stimulation
gi motility-increase
gi sphincters-relax
gi secretion-stimulation
detrusor-contract
trigone and sphincter-relax
glands-secretion
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13
Q

the major clinical uses of the direct-acting cholinomimetics are for ___

A

diseases of the eye (glaucoma, accommodative esotropia), and the GI/GU tracts (post-operative atony, neurogenic bladder)

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14
Q

describe the effects of muscarinic stimulants and glaucoma

A

cause contraction of ciliary body, which facilitates outflow of aq humor and reduces intraocular pressure

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15
Q

___ is the most widely used choline ester for GI/GU disorders, including postoperative ileus, congenital megacolon, urinary retention, esophageal reflux

A

bethanechol

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16
Q

___ are used to increase salivary secretion (eg dry mouth associated with Sjorgren syndrome

A

pilocarpine and cevimeline

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17
Q

overdoses of pilocarpine and the choline esters cause predictable muscarinic effects (nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, bronchial constriction) and are blocked by antimuscarinic compounds such as __-

A

atropine

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18
Q

what are some major contraindications to the use of mAChR agonists that are distributed systemically?

A

asthma
hyperthyroidism
coronary insufficiency
acid-peptic disease

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19
Q

what drug combination can be used in the case of acute nicotine toxicity?

A

atropine –> for excess muscarinic stimulation from parasympathetic ganglia
diazepam –> parenteral anticonvultant for CNS stimulation

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20
Q

__- is approved for intraocular use during surgery and causes miosis; rarely given systemically

A

acetylcholine

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21
Q

__- is rarely used but adminstered by inhalation for the diagnosis of bronchial airway hyperreactiviy in pts who do not have clinically apparent asthma

A

methacholine

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22
Q

___ can be used to treat pts with urinary retention and heartburn, is a selective mAChR agonist with little CV stimulation, and may produce UTI if sphincter fails to relax

A

bethanechol

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23
Q

___ is a nonspecific cholinergic agonist that is used for tx of glaucoma or to produce miosis during surgery or ophthalmic examination

A

carbachol

24
Q

___ is an oral table used to treat dry mouth (xerostomia) in pts with Sjorgren syndrome. It is metabolized via P450 pathways and eliminated in urine

A

cevimeline

25
Q

___ is a pure mAChR agonist that is approved for xerostomia tx in pts with Sjogrens syndrome or head and neck cancer tx related xerostomia (PO), miosis during opthalmic procedures (topical), and for glaucoma (topical)

A

pilocarpine

26
Q

Varenicline (Chantix) is a partial agonist that binds with high affinity and selectivity to what receptor? What is the most common adverse effect? The serious side effects?

A

alpha4beta2 (a4b2) nAChR’s

most common –> nausea

serious –> neuropsychiatric symptoms, changes in behavior, agitation, depressed mood, suicide ideation

27
Q

this drug is an indirect-acting cholinergic agonist that has an alcohol group

A

edrophonium

28
Q

these drugs are indirect-acting cholinergic agonists that are carbamic acid esters

A

neostigmine, pyridostigmine, physostigmine, and cabaryl

29
Q

echothiophate, parathion and malathion (insecticides), and sarin, soman, and tabun (nerve gases) are examples of what?

A

organophosphates–> indirect-acting cholinergic agonists

binding to AChE is covalent and irreversible

30
Q

Describe the effects on the CNS with low concentrations of AChE inhibitors:

A

diffuse activation on EEC and a subjective alerting response

31
Q

Describe the effects on the CNS with high concentrations of AChE inhibitors:

A

generalized convulsions d/t neuronal hyperstimulation (may be followed by coma or resp. arrest)

32
Q

Describe the effects on the eye, resp tract, gi tract, and urinary tract with AChE inhibitors:

A

similar to the direct acting cholinomimetics (bethanechol, carbachol, pilocarpine); these organs are innervated by mAChRs and stimulation results in parasympathetic responses

33
Q

describe the net cardiovascular effects with moderate doses of AChE inhibitors

A

modest bradycardia, a fall in CO (due to bradycardia, decreased atrial contractility, and some reduction in ventricular contractility), and a modest increase in BP

toxic doses of AChE inhibitors cause more marked bradycardia, occasionally tachycardia, and hypotension

34
Q

These AChE inhibitors can reverse the paralysis induced by neuromuscular blocking drugs during surgical anesthesia

A

Neostigmine and edrophonium are preferred

35
Q

Donepezil, rivastigmine, galantamine, and physostigmine are preferred for treatment of this neurological disorder

A

Progressive dementia of the alzheimer type

36
Q

List some effects of intoxication d/t anticholinergic agents and name a drug that can reverse these effects:

A 
Cutaneous vasodilation
Anhidrosis
Anhydrotic hyperthermia
Nonreactive mydriasis
Delirium
Hallucinations
Reduction or elimination of desire to urinate

-Physostigmine can reverse the above mentioned anticholinergic effects and is preferred because it crosses the BBB

37
Q

Nondepolarizing neuromuscular blocking agents in combination with AChE inhibitors will diminish neuromuscular blockade. One exception is the drug ___ (metabolized by AChE), where neuromuscular blockade is prolonged

A

Mivacurium

38
Q

This drug in combination with AChE inhibitors will enhance phase 1 block and antagonize phase 2 block

A

Succinylcholine

39
Q

Describe the interaction between direct-acting cholinergic agonists and AChE inhibitors:

A

Combination will enhance the effects of cholinergic agonists

40
Q

Describe the effects of beta-blockers in combination with AChE inhibitors:

A

Combination may enhance the bradycardic effects

41
Q

Describe the effects of the combination of AChE inhibitors and systemic corticosteroids:

A

Coadministration with AChE inhibitors may enhance muscle weakness seen in pts with myasthenia gravis

42
Q

This mAChR antagonist is the antidote recommended for cholinergic poisoning in combination with maintenance of vital signs (respiratory in particular)

A

Atropine

Atropine is ineffective against peripheral neuromuscular stimulation (nAChRs)

43
Q

List an example of a cholinesterase regenerator and describe the current antidotal therapy for organophosphate exposure resulting from warfare or terrorism:

A
  • Pralidoxime

- Atropine, an oxime (pralidoxime), and a benzodiazepine as an anticonvulsant

44
Q

Animal studies have shown that pretreatment with ___ reduces the incapacitation and mortality associated with nerve agent poisoning, especially with agents such as soman that show rapid aging. It has been approved for combat use in US military personnel

A

Pyridostigmine

-should be discontinued at 1st sign of nerve gas exposure

45
Q

___ drugs elicit their effects at the NMJ and on nAChRs in the ganglia

A

Antinicotinic

46
Q

The prototype antimuscarinic compound is ___

A

Atropine

47
Q

What are some mAChR antagonists that can be used to reduce the tremor associated with PD?

A

Benztropine and trihexyphenidyl

48
Q

This drug can be useful in treating motion sickness and is one of the oldest agents for seasickness and can be administered by injection, PO, and transdermal patch

A

Scopolamine

49
Q

This long-lasting mAChR antagonist is used to prevent synechia formation in uveitis and iritis

A

Homatropine

50
Q

Which antimuscarinic agents can be used to treat asthma and COPD?

A

Ipratropium and Tiotropium

51
Q

___ is used as an inhalational agent in the tx of asthma and COPD and is currently a first line therapy

A

Ipratropium

52
Q

THe recently approved agent ___ has a longer bronchodilator action than ipratropium and can be dosed once daily in pts with COPD

A

Tiotropium

53
Q

This mAChR antagonist is used in the tx of common travelers diarrhea. It is a combo of atropine and diphenoxylate.

A

Lomotil

54
Q

What is the prototypical antimuscarinic agent used in disorders of the GU tract?

A

Oxybutynin

55
Q

___ is a nonselective antagonist that is comparable in efficacy and side effects with oxybutynin

A

Trospium

56
Q

List some antimuscarinic agents for urinary disorders that are more selective and may produce less adverse effects

A

Darifenacin, solifenacin, and tolterodine

57
Q

What are some contraindications for antimuscarinic agents?

A

Pts with glaucoma (reduced secretions) and used with caution in elderly men with a history of prostatic hyperplasia

Neuro 2-Unit 2 (4 decks)

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