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Pharmacology - Winter > Lecture 2 > Flashcards

Lecture 2 Flashcards

0
Q

Vesamicol:

A

Vesamicol can block the transport of acetylcholine into the storage vesicle

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1
Q

List the direct acting cholinergic agonists:

A 
Acetylcholine
Pilocarpine
Cevilimine
Bethanochol
Nicotine
Vemilicline
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2
Q

Botulinum toxin:

A

Botulinum toxin blocks the release of acetylcholine into the synaptic cleft

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3
Q

Location of cholinergic receptors within the synaptic cleft:

A
  1. Post synaptic neurons

2. Presynaptic nerve terminals

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4
Q

Cholinergic agonists and choline stress inhibitors are together known as….

A

Cholinergic stimulants

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5
Q

Direct vs indirect cholinesterase stimulants:

A

Direct: discriminate between muscarinic and nicotinic receptors. They bind directly to them to evoke a response

Indirect: do not discriminate. They alter the ability of ACh to bind to receptors therefore muscarinic and nicotinic effects occur

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6
Q

Acetylcholine:

A

Direct acting cholinergic stimulus: able to bind to both nicotinic and muscarinic receptors. However half life is so short that there is no clinical use

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7
Q

Bethebachol:

A

Specific for M receptors
Quaternary structure prevents CNS penetration
Most often used in GI/GU tracts

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8
Q

Pilocarpine:

A

Specific for M receptors
Tertiary structure. Small enough to enter the CNS
Especially active on sweat and salivary glands

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9
Q

Cevimiline:

A

Specific for M3 receptors

Fewer side effects than pilocarpine bc not active on M1 (sweat glands)

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10
Q

Nicotine and varenicline:

A

Selective for N receptors. Used to help people quit smoking

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11
Q

Methacholine:

A

Cholinergic agonist used to test for asthma.

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12
Q

Which muscarinic agonist is most commonly used to treat glaucoma?

A

Pilocarpine

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13
Q

Which muscarinic agonist is most commonly used to increase GI peristalsis and urinary voiding n patients with urinary retention?

A

Bethanechol

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14
Q

Which direct acting cholinergic agonists can be used to treat dry mouth caused by Sjorgens syndrome and which one is the preferred drug?

A

Pilocarpine and cevimeline

Cevimeline is preferred bc unlike pilocarpine it does not activate M1 receptors therefore it dies not cause perfuse sweating

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15
Q

Side effects of muscarinic agonists:

A

Diarrhea, abdominal cramps, sweating and salivation

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16
Q

Contraindications to muscarinic agonists:

A

Peptic ulcer
Coronary insufficiency
Asthma

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17
Q

Low dose effects of nicotinic agonists:

A

Alertness and attention

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18
Q

High dose effects of nicotinic agonists:

A

Tremor

Vomiting

19
Q

Peripheral effects of nicotinic agonists:

A

Depends on tone of organ system. For example it will cause tachycardia and increased BP

20
Q

3 parts of nicotine poisoning treatment:

A

Atropine
Mechanical respiration
Anticonvulsants to decrease seizures

21
Q

Varenicline:

A

Partial agonist of alpha4beta2 receptor in the brain. Used to help ppl quit smoking. Causes nausea, vomiting, nightmares, psych problems,

22
Q

List the cholinesterase inhibitors:

A 
Neostigmine
Edrophonium
Physostigmine
Echothiophate
Donepezil
Organophosphate pesticides
2-Pam
23
Q

Which cholinesterase inhibitors are carbamates?

A

Neostigmine

Physostigmine

24
Q

Neostigmine

A 
Cholinesterase inhibitor
Quaternary structure
Cannot enter CNS
carbamate
Lasts 30 minutes to 6 hours
25
Q

Physostigmine

A 
Cholinesterase inhibitor
Carbamate
Tertiary structure
Can enter CNS
Lasts 30 minutes to 6 hours
26
Q

Edrophonium

A

Cholinesterase inhibitor
Quaternary
Cannot enter CNS
Short acting (5-10 minutes)

27
Q

Organophosphate

A 
Used as pesticides and nerve gases
Cholinesterase inhibitors
Very long lasting, aging -> irreversible
Fatal if aging is not prevented (prevent with early administration of 2-Pam
Generally very lipid soluble
28
Q

2-Pam

A

Cholinesterase inhibitor
Use to counter organophosphate poisoning and prevent bond aging is controversial bc it can also inhibit Acetylcholinesterase

29
Q

Determining the effects of cholinesterase inhibitors:

A

Mimic effects of both PNS and SNS. So the dominant effect will be determined by the dominant tone of each specific organ/system

30
Q

Which cholinesterase inhibitor is used in the treatment of myasthenia gravis?

A

Neostigmine. Increases half life of ACh. May also have a direct stimulatory effect on the NMJ

31
Q

Which cholinesterase inhibitor is used in the treatment of glaucoma?

A

Physostigmine

32
Q

Which cholinesterase inhibitors are used to treat Alzheimer’s?

A

Donepezil and rivastigmine. These are similar to physostigmine. They easily enter the CNS and are well absorbed orally

33
Q

How is neostigmine administered?

A

Orally

34
Q

Physostigmine administration?

A

Rarely given orally bc of side effects. More often administered directly into the eyes

35
Q

Which cholinesterase inhibitor is used in the diagnosis of myasthenia gravis?

A

Edrophonium

36
Q

Echothiophate

A

Lipid insoluble organophosphate than can be used for long term control of intra ocular pressure. Often used in glaucoma emergency situations

37
Q

Dfp

A

Prototype organophosphate that was developed as a pesticide

38
Q

Soman and sarin

A

Both are organophosphate s that act as nerve gases

39
Q

Parathion and malathion

A

Organophosphates. Thiophosphate insecticides

40
Q

Which cholinesterase inhibitors can be used to treat glaucoma?

A

Physostigmine and echothiophate

41
Q

Of the three drugs (pilocarpine, physostigmine, and echothiophate which is most commonly used in glaucoma treatment?

A

Pilocarpine

42
Q

Treatment of open angle vs closed angle glaucoma:

A

Open angle glaucoma can be treated with cholinesterase inhibitors or direct acting muscarinic agonists. Most often pilocarpine is used. Closed angle is treated with pilocarpine and a combination of cholinesterase inhibitors to keep pressure under control until it can be fixed with surgery.

43
Q

Which cholinesterase inhibitors can reverse NMJ blockades from surgery?

A

Neostigmine and edrophonium

44
Q

Edrophonium and myasthenia gravis:

A

Edrophinium can be used to diagnose myasthenia gravis. It can also be used to determine if current medication doses are too high or too low and causing decreased effectiveness of treatment. If administration makes things better it means the dise was too low. If edrophonium makes it worse that means the dose was too high and receptors have been down regulated

Pharmacology - Winter (2 decks)

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