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Pharmacology > L4: Cholinergics > Flashcards

L4: Cholinergics Flashcards

(64 cards)

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1
Q

What drug class is Acetylcholine?

A

direct acting cholinomimetics

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2
Q

What drug class is Bethanechol?

A

Direct Acting cholinomimetics

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3
Q

What drug class is Nicotine?

A

Direct-acting cholinomimetics

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4
Q

what drug class is pilocarpine?

A

Direct-acting cholinomimetics

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5
Q

What drug class is Edrophonium?

A

Indirect acting cholinomimetics

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6
Q

What drug class is physostigmine?

A

Indirect acting cholinomimetics

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7
Q

What drug class is Echothiophate?

A

Indirect-acting cholinomimetics

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8
Q

What drug class is atropine?

A

Muscarininc inhibitor

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9
Q

what drug class is ipratropium?

A

Muscarinic inhibitor

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10
Q

What drug class is tiotropium?

A

Muscarinic inhibitor

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11
Q

What is the acetlycholine signal terminated by?

A

AchE

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12
Q

Which direct acting Ach agonists are choline esters?

A
  • Ach
  • Methacholine
  • Bethanechol
  • Carbachol
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13
Q

Which direct acting Ach agonists are alkaloids?

A
  • muscarine
  • Pilocarpine
  • Nicotine
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14
Q

What is the difference between choline esters and alkaloids?

A

Alkaloids aren’t charged so they can cross the BBB

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15
Q

Which cholinergic receptor can each drug bind:
* Ach
* Methacholine
* Bethanechol
* Carbachol
* Muscarine
* Pilocarpine
* Nicotine

A
  • Both
  • Muscarininc
  • Muscarininc
  • both
  • Muscarininc
  • Miscarinic
  • Nicotinic
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16
Q

What g-protein are odd numbered muscarinic receptors coupled with?

A

Gq

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17
Q

What is the effect of Gq stimulation?

A

Phospholipase C activation, increased DAG and IP3 leading to increased Ca2+

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18
Q

What g-protein are even numbered muscarinic receptors coupled with?

A

Gi

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19
Q

What is the effect of Gi (GPCR) stimulation

A

Inhibits adenylyl cyclase and decreases cAMP and protein kinase A

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20
Q

What muscarininc receptor is responsible for most excitatory responses?

A

M3

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21
Q

What muscarininc receptor is able to decrease interocular pressure?

A

M3

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22
Q

What effect does muscarininc activation have on the heart?

A

Decreased funny channel activity which leads to decreased HR

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23
Q

What is the effect of muscarinic activation on the vascular endothelium?

A

Increased Ca from endothelial cells produces NO which leads to VSM dilation and decreased blood pressure

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24
Q

What kind of selectivity do muscarinic agonists have?

A

NONE

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25
What is the nervous system response to muscarinic agonists?
Parasympatho**mimetic**
26
Do muscarninc agonists desensitze the muscarinic receptors?
NO
27
How is ocular hypertension relieved?
by increasing Aq humor flow out of the canal of Schlemm which is opened by m3 activation via the ciliary muscle and trabeculae network
28
What disease is associated with IOP?
Open angle glaucoma | Causes loss of optic nerve and perm blindness
29
What drug is best for tx of glaucoma?
Pilocarpine
30
What are the adverse effect sof direct-acting cholinomimetics?
Super strong parasympathetic rxn
31
When is it contraindicatated to use direct-acting cholinomimetics?
* asthma * COPD * peptic ulcers * hypotension * hyperthyroidsim * if pt is on beta-blockers
32
Is nicotine an alkaloid or a choline esterase?
Alkaloid | Can cross BBB
33
Where are nicotinic receptors located?
* all preganglionic nerves in ANS * NMJ * Adrenal medulla
34
Do nicotinic Ach receptors have selectivity?
Yes | There are different types of receptors with different pentameric arrange
35
Can nictotinic receptors be desensitized?
Yes, with extremely prolonged activation
36
What ions flow through nicotinic receptors and in whch direction?
Na and Ca inside
37
What do nicotinic receptor agonists stimulate?
* all nicotinic receptor subtypes * CNS and all peripheral ganglia * skeletal muscle
38
Which organs are preferentially parasympathetic?
* Eyes * Secretory organs * Digestive system * GI
39
Which organs are preferentially sympathetic?
* heart (contractile force) * Sweat glands * Vascular system
40
What type of selectivity do muscarinic antagonists have?
Limited selectivity | mostly activate everything
41
What type of nervous system response happens with muscarinic antagonsist?
Parasympatholytic effects | Lytic-> to lyse meaning no more parasympathetic
42
What is required for antagonists to have an effect?
Agonists- antagonists can only block agonists, they can not produce their own effect.
43
What is the effect of a muscarinic antagonist on the: 1. Eye 2. GI 3. Gut 4. Mucosal glands 5. Lung 6. Heart 7. Vasculature 8. Sweat glands 9. CNS
1. Increase IOP 2. Decreased peeing 3. Constipiation 4. No secretion 5. Bronchodilation 6. Increase HR 7. Nothing 8. decrease secretion 9. Sedation
44
Under what circumstances can a muscarinic antagonist increase blood pressure?
If there was already a lot of muscarinic agonist in circulation.
45
What is the name of naturally occuring muscarinic antagonsist?
Belladona Alkaloids / Atropine
46
What are the two parts of atropine and what are their functions?
Tropic acid to bind the receptor and a base to increase bioavailibilty.
47
Are the follwing tertiary amines or quatenary amines: 1. Tropicamide? 2. Benztropine? 3. Ipratropium? 4. Propantheline?
1. Tertiary 2. benztropine 3. Ipratropium 4. Propantheline
48
What is the difference between tertiary amines and quaternary amines?
Tertiary amines are uncharged and easily absorbed and quatenary amines are changed and poorly absorbed
49
What is each drug used for: 1. Tropicamide? 2. Benztropine? 3. Ipratropium? 4. Propantheline?
1. Eye exams 2. Parkinsons 3. Asthma 4. Gut
50
How can muscarinic antagonists help with asthma and COPD?
There is a reflex arc that senses inhaled irritants and sends a signal to the CNS which makes the lungs secrete more mucous so if we inhibit the M3 receptor, we can decrease mucosal secretions.
51
What is the clinical use of: 1. Atropine? 2. Benztropine? 3. Scopolamine? 4. Ipratroprium? 5. Tiotropium?
1. Bradycardia 2. Parkinsons 3. Motion sickness 4. Lung disorders 5. Lung disorders
52
What are the toxic effects of muscarinic agonists?
* Blurred vision * Drymouth * hyperthermia * Urine retention * Delerium * Tachycardia and angina * Costipation | Dry as bone, blind as a bat, red as a beet, mad as a hatter and hot as a
53
What disease is contracindicated for muscarinic antagonist use?
Glaucoma
54
What is the MOA of AchE inhibitors?
Block AchE to increase 1/2 life of Ach
55
What is the purpose of the key sites on AchE: 1. Choline subsite 2. Acyl pocket
1. Has a negative charge which attracts the positive choline 2. Acetate binds to serine and then breaks of and leaves Ach as acetate and choline | Acetate quicky leaves serine after choline leaves
56
What is the MOA of: 1. Edrophonium? 2. Neostigmine? 3. Organo-phosphates?
1. Binds the choline subsite and acyl pocket to block Ach 2. Binds to the serine and takes hours to release (slow decarbamoylation) 3. Binds to the serine and takes days to release (slow dephosphorylation)
57
What are the physiological effects of AchE inhibitors?
* increased alertness * Increased strength * Increased HR * pupil constriction * Increased peeing and digestion * Low dose-> decreased BP * High dose-> increased BP
58
What class of drug is used for myasthenia gravis
AchE inhibitors
59
What drug is used to: 1. Diagnose myasthenia gravis 2. Treat myasthenia gravis
1. Edrophonium 2. Physostigmine, neostigmine and pyridostigmine
60
What is the effect of AchE inhibitors on glaucoma?
decreased IOP
61
What are the toxic effects of AchE inhitors?
* convulsions * Death via paralyzed diaphargm * depression * extreme bradycardia * extreme hypotension * peeing, pooping and sweating
62
What is the difference between myasthenia gravis and AchE inhibitor OD?
With OD youll be peeing yourself
63
What is used to treat muscarinic inhibitor poisoning?
AchE inhibitors | Physostigmine
64
What is used to treat AchE inhibitor poisoning?
Muscarininc inhibitors | Atropine

Pharmacology (8 decks)

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