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Cardiac Pharmacology: Professor slides > ANS Pharmacology > Flashcards

ANS Pharmacology Flashcards

1
Q

What is the major neurotransmitter in all pre-ganglionic sites?

A

A.Ch

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2
Q

To what organ is A.Ch sympathetic to?

A

Sweat glands and some blood vessels

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3
Q

A.Ch is also a major transmitter to what sites?

A

All Post-ganglionic para-sympathetic sites, skeletal muscle, and CNS

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4
Q

What is the MOA of botulinum toxin?

A

It enters cholinergic nerve terminals and prevents the release of A.Ch by cleaving SNAP and VAMP

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5
Q

Uses of Botulinum toxin?

A

Management of dystonia and spasticity, chronic pain and local spasms, and, cosmetic use

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6
Q

Why is the half-life of A.ChE small?

A

Because A.ChE RAPIDLY splits A.Ch into CHOLINE and ACETATE in the cholinergic synapses

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7
Q

Which other cholinesterase has LOW specificity for A.Ch?

A

Butyrylcholinesterase a.k.a PSEUDO CHOLINESTERASE

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8
Q

Where is True A.ChE found?

A

All cholinergic sites, RBCs, and GRAY matter

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9
Q

Where is Pseudo A.ChE found?

A

Plasma, liver, Intestines, and WHITE matter

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10
Q

How do True A.ChE and Pseudo A.ChE differ based on their action on Methacholine?

A

True A.ChE’s action: Slow
Pseudo A.ChE’s action: Not hydrolysed

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11
Q

How do True A.ChE and Pseudo A.ChE differ based on their action on A.Ch?

A

True A.ChE’s action: Very Fast
Pseudo A.ChE’s action: Slow

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12
Q

Which cholinesterase plays a significant role in the hydrolysis of ingested esters?

A

Pseudo A.ChE

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13
Q

Which Cholinesterase is more sensitive to OP?

A

Pseudo A.ChE

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14
Q

Which Cholinesterase is more sensitive to Physostigmine?

A

True A.ChE

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15
Q

Types of cholinergic receptors?

A

M (muscarinic): M1. M2, M3, M4, M5 (Gq, Gi, Gq, Gi, Gq)
N (nicotinic): Nm and Nn (ligand-gated)

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16
Q

Where is Nm found?

A

Muscle

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17
Q

What drugs are antagonists for Nm?

A

Tubocuraine and Atracurium

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18
Q

Where is Nn found?

A

Autonomic ganglia (Symp. Parasymp., and adrenal medula)

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19
Q

What drugs are potent Agonists for Nm and Nn apart form A.Ch?

A

Nm: Carbochol (CCh), Suxamethonium

Nn: CCh, NICOTINE
(Remember Nicotine acts only on ANS, all cigarette smokers would twitch every time they smoke if it acted on Nm receptors LOL)

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20
Q

What drug is used as an antagonist for Nn receptor?

A

Trimethaphan and Hexamethonium

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21
Q

What compound found in mushrooms cause one to SLUDGE MoBBB?

A

Muscarine

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22
Q

What drug is administered to counteract the effects of Muscarine?

A

Atropine

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23
Q

Locations of M 1,2,3,4,5 receptors:

A

M1, M4, M5: CNS and ANS ganglia
M2: Heart»>CNS
M3: Smooth muscle of Viscera, eye, exocrine glands (why? bc endocrine glands are supplied by their respective receptors) and endothelium

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24
Q

Effect of A.Ch on M2?

A

Reduces HR by slowing down depolarization

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25
Effect of A.Ch on Blood Vessels (M3)?
Limited cholinergic innervation: Skin of face and neck Vasodilation: by NO --> fall in BP Penile erection
26
Effect A.Ch on M3 receptors of glands?
Increase in secretions (less effect on pancreas and GI)
27
Why does parasympathetic stimulation of M3 receptors in the eye cause Miosis (Shrinkage of the pupil), spasm in accommodation, and reduction in IOP?
Miosis: Contraction of circular fibers of Iris Spasm of accommodation: contraction of ciliary muscles Reduction of IOP: Increased outflow
28
Will IV infusion of A.Ch have any effect on the CNS
No, it does NOT cross the BBB
29
Effect of CNS on Nn?
Stimulates both sympathetic and parasympathetic ganglia
30
Effect of IV injection of A.Ch on muscles?
No effect
31
Effect of A.Ch on muscles
Contraction
32
Types of cholinometrics?
Direct acting: Stimulates A.Ch receptors Indirect acting: Inhibits A.ChE ---> Increase availability of A.Ch
33
Examples of DIRECT muscarinic agonists?
A.Ch Bethanechol Carbachol Pilocarpine
34
Example of DIRECT nicotinic agonists?
Nicotine Varenicline
35
Which direct-acting muscarinic drug is used as an ileus in postop, urinary retention?
Bethanechol: Bladder, Bowel (B, B, B)
36
Which direct-acting muscarinic drug is used as a diagnostic test for bronchial hyperreactivity?
Methacholine
37
Which direct-acting muscarinic drug is given for open-angle glaucoma?
Pilocarpine
38
Which direct-acting muscarinic drug is given for xerostomia?
Cevelamine >>>> Pilocarpine
39
How are Indirect-acting cholinergics classified?
Reversible and Irreversible
40
Examples of reversible A.ChE-I:
Physostigmine Neostigmine Pyridostigmine Donezepil Rivastigmine Edrophonium
41
Examples of irreversible A.ChE-I:
OPC Echothiophate Parathion Nerve gas Carbamate esters
42
What happens to an indirect-acting cholinergic if it binds to the Anionic site?
REVERSIBLE: Physostigmine and Neostigmine
43
What happens to an indirect-acting cholinergic if it binds to the Esteric site?
IRREVERSIBLE: Carbamate esters and OPCs
44
What is aging?
Process by which phosphrylated enzyme loses alkyl group and becomes resistant to hydrolysis
45
What type of amine can NOT cross the BBB?
Quarternary amine: Neostigmine
46
What type of amine can show effects on the CNS?
Tertiary amine: Physostigmine
47
Why is it vital to bring the patient OP poisoning to the emergency room ASAP?
To avoid aging
48
What Indirect-cholinergic are given to a patient with Myasthenia gravis?
Edrophonium Neostigmine Pyridostigmine
49
What Indirect-cholinergics are given to a patient as an ileus or for urinary retention or for the reversal of NM blocade?
Neostigmine Pyridostigmine
50
What Indirect-cholinergic are given to a patient with Alzheimers?
Donezepil Rivastigmine
51
SLUDGe/ MoBBB?
S- Salivation L- Lacrimation U- Urination D- Defecation G- Gastric; e- emesis M- Miosis B- Bronchorrhea B- Bronchospasm B- Bradycardia
52
Treatment for OP poisoning?
Atropine + Cholinesterase reactivator: Oximes
53
Examples of Cholinesterase reactivators?
Pralidoxime Obidoxime
54
What are Nn antagonists also known as?
Ganglion blockers
55
What are Nm blockers also known as?
NM blockers
56
What is the prototype anti-cholinergic drug?
ATROPINE
57
Which drug that causes sedation is also used for motion sickness?
Scopalamine
58
Which Anti-cholinergic drug is used as an anti-spasmodic, anti-secretory, and in mushroom poisoning?
Atropine
59
Effects of atropine:
Opposite effects of SLUDGE/ MoBBB: CNS Stimulant (except scopolamine: drowsiness) Tachycardia Mydriasis (dilation of the pupil) Cycoloplegia (loss of accommodation) Abolition of light reflex Increase in IOP Dry eye Bronchodilation: useful in COPD and Asthma Relaxation of UB and ureter: helps in urinary retention Constipation (M3 blockade) Decreases sweating Increase in temperature: because of a decrease in sweating
60
In what cases is Atropine contraindicated?
Narrow-angle glaucoma BPH
61
Treatment for atropine/belladonna poisoning?
Physostigmine
62
Examples of competitive ganglion blockers?
Hexamethonium Mecamylamine
63
What is the dominant tone in the heart and the effect of ganglion blockade on the heart?
Parasympathetic; Tachycardia (reduction in A.Ch)
64
What is the dominant tone in the arteriole and the effect of ganglion blockade?
Sympathetic; Vasodilation, and hypotension
65
What is the dominant tone in the veins and the effect of ganglion blockade?
Dilation, reduction in VR, and reduction in CO
66
Which drug is used to treat nicotine addiction?
Varenicline
67
What are the catecholamines of the sympathetic system?
Epi, NE, Dopa.
68
What enzyme metabolizes catecholamines?
MAO and COMT
69
How do Cocaine and TCA anti-depressants potentiate the effect of NE and E?
Neuronal reuptake inhibitors
70
What are the types of Adrenergic receptors and what types of receptors are they?
Alpha 1 - Gq Alpha 2 - Gi Beta 1 - Gs Beta 2 - Gs Beta 3 - Gs D1 - Gs [remember 'qissss']
71
Which is the only pre-synaptic adrenergic receptor?
Alpha 2: Gi; it inhibits the pre-synaptic release of NE
72
Primary function of Alpha 1 on blood vessels?
Vasoconstriction: increase in the VR (veins) and Increase in TPR and Increase in DBP (arterioles)
73
Primary function of B1?
Increases HR, Increases Contraction Increases renin release Increases O2 demand
74
Effect of B2?
Bronchodilation Vasodilation: Reduces TPR and DBP
75
Where does B3 work on?
Bladder and Fat cells
76
Which drug is used as a nasal decongestant?
Phenylephrine: A1 Selective, direct agonist
77
Which A2 Selective direct agonist is used to inhibit NE release?
Clonidine
78
Which drug acts centrally in the management of MS?
Tizanidine: Central A2 agonist
79
What are some important B2 agonists? And uses?
Albuterol Salmeterol Terbutaline ALL OF THEM ARE HELPFUL TO TREAT ASTHMA
80
Which drug other than Oxybutynin is used to treat urinary urgency and frequency
Mirabegron
81
Which selective B1 agonist increases HR and contractility?
Dobutamine
82
On what receptors does Epi work in low doses?
B2 > B1 = A1 = A2
83
On what receptors does Epi work in Medium doses?
B1 = B2 = A1 = A2
84
On what receptors does Epi work in high doses?
A1 > A2 = B1 = B2
85
What drug is given to the patient in anaphylactic shock?
Epi
86
NE action receptors?
A1 = A2 > B1 [Raises both SBP (B1) and DBP (A1)]
87
Uses of NE?
Cardiac arrest Hypotensive state in shock and MI
88
What is the effect of dopamine in low, med, and high doses?
In low doses: Acts on D1, Increases urine output and renal blood flow In med doses: Increases HR, CO and contractility via B1 action In high doses: Increases TPR and Increases DBP via A1 action
89
What is the drug of choice in Cardiogenic shock?
Dopamine: Because, D1 action maintains renal blood flow (prevents acute tubular necrosis), B1 action improves cardiac function, and A1 action maintains BP
90
On what receptor does Isoproterenol act?
B1 + B2 + B3 (Non-selective Beta agonist)
91
What is Dale's vasomotor reversal?
When Epi is given after a pre-treatment of Alpha-blockers: it causes hypotension due to the absence of the Alpha effect When Epi is given after a pre-treatment of Beta-blockers: A hypertensive effect (Apha effect)
92
Why are fermented products such as cheese, yogurt, wine, beer, and meats such as beef contraindicated when a patient is on MAO inhibitors?
Can cause a hypertensive crisis because Tyramine is metabolized by MAO and tyramine displaces NE from vesicles causing a marked increase in BP (alpha effect)
93
Non-selective Alpha antagonist example?
Phenoxybenzamine: Used in Pheochromocytoma, Raynaud's syndrome
94
What is an example of a competitive, reversible antagonist for A1 and A2?
Phentolamine
95
What is the suffix of drugs that selectively block A1?
-osin. Ex: Prazosin
96

Cardiac Pharmacology: Professor slides (8 decks)

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