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PCM Exam 2 > Cholinergic Agonist And Antagonists 1 > Flashcards

Cholinergic Agonist And Antagonists 1 Flashcards

1
Q

Stimulation of adrenergic receptors in the pancrease will most likely cause an overall ________

A

↓ in insulin secretion

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2
Q

Where in the heart can you find high concentrations of muscarinic receptors?

A

Atria

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3
Q

_______ doses of acetylcholine will cause vasodilation, a fall in blood pressure (M3) and bradycardia (M2)

A

LARGE;

Small doses will not have bradycardia because the baroreceptor reflex will be more powerful than the drugs

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4
Q

Atropine is a _______________ and allows large doses of acetylcholine to produce only _______ effects such as _________ and ________

A

Muscarinic antagonist;
Nicotinic effects ;
↑ in BP and vasoconstriction

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5
Q

The effects of atropine as due to stimulation of ________ and release _________

A

SYMPATHETIC ganglia; epinephrine from adrenal medulla

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6
Q

What are the two families of direct acting cholinergic agonists

A
  • esters of choline

- alkaloids

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7
Q

Drugs that are choline esters (4)

A
  • acetylcholine
  • methacholine
  • carbachol
  • bethanechol
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8
Q

choline esters differ in their susceptibility to hydrolysis by cholinesterase.
_____________ is very rapidly hydrolyzed

A

Acetylcholine;

Methacholine, carbachol, and bethanechol are more resistant to hydrolysis by cholinesterase

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9
Q

What is the clinical use of bethanechol?

A
  • post operative and post partum urinary retention
  • atonic bladders

It is a muscarinic agonist

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10
Q

What drugs would you give to someone to ↓ intraocular pressure after cataract surgery and for miosis during surgery?

A

Carbachol;

It is both a muscarinic and nicotinic agonist

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11
Q

What is the use of the methacholine challenge test?

A

Used to diagnose subclincal asthma;

Diagnosis of bronchial airway hyperactivity

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12
Q

What are the two natural alkaloids

A
  • pilocarpine

- nicotine

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13
Q

What are the major uses for pilocarpine

A
  • second line agent for open angle glaucoma
  • management of acute angle closure glaucoma
  • treatment of dry mouth
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14
Q

What is the effect of LOW doses of nicotine?

A

Ganglionic stimulation by depolarization → simultaneous discharge of both parasympathetic and sympathetic nervous systems

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15
Q

Low doses nicotinic actions on the CV system, GI and urinary tracts, and secretions

A

CV: mainly sympathomimetic effects such as ↑ HR and BP

GI and urinary: mainly parasympathetic such as nausea, vomiting, diarrhea, etc

Secretion: stimulation of salivary and bronchial secretions

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16
Q

What family of drugs that are indirect acting cholinergic agents (anti cholinesterases)

A
  • edrophonium
  • carbamates: physostigmine, neostigmine, pryridostigmine
  • organophosphate: echothiophate, parathion and malathion, sarin
17
Q

Mechanism of action of edrophonium

A

It is an acetylcholinesterase that binds reversible tot he activate site and DOES not involve a covalent bond and is short lived

18
Q

Edrophonium‘s effect is short/long lived

A

Short

19
Q

Which of the anti acetylcholinesterases forms a covalent bond?

A

Carbamates and organophosphate (organophosphate phosphorylates the enzyme and is stable and long lived)

20
Q

Oraganophopshates undergoes a process called ageing which ________

A

Strengthens the phosphorous bond

21
Q

What is the difference between LOW and HIGH concentrations of choilnesterase inhibitors on the CNS

A

Low: CNS activation

High: convulsions → coma and respiratory arrest

22
Q

What are the systems that are well innervated by parasympathetic? And what is the effect of cholinesterase inhibitors on them?

A

eye, respiratory tract, GI, and urinary trac t

Similar to direct acting cholinomimetics

23
Q

In the ________ cholinesterase inhibitors activate both sympathetic and parasympathetic but the ____________ predominates

A

Heart;

Parasympathetic → ↓ cardiac output

24
Q

What is the effect of choliesterase inhibitors on the vascular smooth muscle?

A

MINIMAL EFFECTS because they dont have much cholinergic innervation

Moderate doses will cause ↑ in resistance and BP but due to the actuation of sympathies ganglia and central sympathetic centers

25
Q

What are the net CV effects of cholinesterase inhibitors?

A
  • modest bradycardia (M2 receptors in heart)
  • ↓ CO
  • ↑ vascular resistance
  • ↑ BP
26
Q

What is the effect of toxic doses of cholinesterase inhibitors on the CVS?

A
  • marked bradycardia
  • significant ↓ in CO
  • HYPOtension
27
Q

Cholinesterase inhibitors _______ the strength of contractions and it is useful for treating ________

A

Strength;
Myasthenia gravis;

Useful to reverse action of nondepolarizing neuromuscular blockers

28
Q

___________ is used to treat myasthenia gravis

A

Edrophonium

29
Q

________ is used tot real overdoses of anticholinergic drugs (atropine)

A

Physostigmine

30
Q

What are two drugs used for postoperative urinary retention?

A

Bethanechol and neostigmine

31
Q

What are some uses for neostigmine

A
  • post op urinary retention
  • reversing effect of non depolarizing NM blockers after surgery
  • treating myasthenia gravis
32
Q

Which of the cholinesterase inhibitors do NOT enter CNS?

A

Edrophonium, neostigmine, pyridostigmine

33
Q

What are malathion and parathion used for?

A

Insecticides

34
Q

What kind of people would be at risk for toxic symptoms of anti-cholinesterase and by which drugs?

A

Farmers exposed to heavy insecticides;

Malathion and parathion

35
Q

What is the most potent acetylcholine esterase inhibitors?

A

Sarin

36
Q

Another use of centrally acting acetylochilinesterase inhibitors in in slowing the progression of __________

A

Alzheimer’s Disease

37
Q

What are the central acting acetylcholine esterase inhibitor drugs (3)

A
  • donepezil
  • rivastigmine
  • galantamine
38
Q

_________ is a reactivator of acetylcholinesterase and thus is used to treat anti acetylcholinesterase poisoning

A

Pralidoxime

39
Q

A farmer using insecticides comes in with toxic symptoms, what would you give to reverse the effects?

A

Pralidoxime (give it before ageing has occurred) to regenerate the cholinesterase
Also give atropine to block the acetylcholine receptors so acetylcholine doesnt bind to them

PCM Exam 2 (32 decks)

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