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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
Q

Effect of A.Ch on Blood Vessels (M3)?

A

Limited cholinergic innervation: Skin of face and neck

Vasodilation: by NO –> fall in BP

Penile erection

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26
Q

Effect A.Ch on M3 receptors of glands?

A

Increase in secretions (less effect on pancreas and GI)

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27
Q

Why does parasympathetic stimulation of M3 receptors in the eye cause Miosis (Shrinkage of the pupil), spasm in accommodation, and reduction in IOP?

A

Miosis: Contraction of circular fibers of Iris

Spasm of accommodation: contraction of ciliary muscles

Reduction of IOP: Increased outflow

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28
Q

Will IV infusion of A.Ch have any effect on the CNS

A

No, it does NOT cross the BBB

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29
Q

Effect of CNS on Nn?

A

Stimulates both sympathetic and parasympathetic ganglia

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30
Q

Effect of IV injection of A.Ch on muscles?

A

No effect

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31
Q

Effect of A.Ch on muscles

A

Contraction

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32
Q

Types of cholinometrics?

A

Direct acting: Stimulates A.Ch receptors
Indirect acting: Inhibits A.ChE —> Increase availability of A.Ch

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33
Q

Examples of DIRECT muscarinic agonists?

A

A.Ch
Bethanechol
Carbachol
Pilocarpine

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34
Q

Example of DIRECT nicotinic agonists?

A

Nicotine
Varenicline

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35
Q

Which direct-acting muscarinic drug is used as an ileus in postop, urinary retention?

A

Bethanechol: Bladder, Bowel (B, B, B)

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36
Q

Which direct-acting muscarinic drug is used as a diagnostic test for bronchial hyperreactivity?

A

Methacholine

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37
Q

Which direct-acting muscarinic drug is given for open-angle glaucoma?

A

Pilocarpine

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38
Q

Which direct-acting muscarinic drug is given for xerostomia?

A

Cevelamine&raquo_space;» Pilocarpine

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39
Q

How are Indirect-acting cholinergics classified?

A

Reversible and Irreversible

40
Q

Examples of reversible A.ChE-I:

A

Physostigmine
Neostigmine
Pyridostigmine
Donezepil
Rivastigmine
Edrophonium

41
Q

Examples of irreversible A.ChE-I:

A

OPC
Echothiophate
Parathion
Nerve gas
Carbamate esters

42
Q

What happens to an indirect-acting cholinergic if it binds to the Anionic site?

A

REVERSIBLE: Physostigmine and Neostigmine

43
Q

What happens to an indirect-acting cholinergic if it binds to the Esteric site?

A

IRREVERSIBLE: Carbamate esters and OPCs

44
Q

What is aging?

A

Process by which phosphrylated enzyme loses alkyl group and becomes resistant to hydrolysis

45
Q

What type of amine can NOT cross the BBB?

A

Quarternary amine: Neostigmine

46
Q

What type of amine can show effects on the CNS?

A

Tertiary amine: Physostigmine

47
Q

Why is it vital to bring the patient OP poisoning to the emergency room ASAP?

A

To avoid aging

48
Q

What Indirect-cholinergic are given to a patient with Myasthenia gravis?

A

Edrophonium
Neostigmine
Pyridostigmine

49
Q

What Indirect-cholinergics are given to a patient as an ileus or for urinary retention or for the reversal of NM blocade?

A

Neostigmine
Pyridostigmine

50
Q

What Indirect-cholinergic are given to a patient with Alzheimers?

A

Donezepil
Rivastigmine

51
Q

SLUDGe/ MoBBB?

A

S- Salivation
L- Lacrimation
U- Urination
D- Defecation
G- Gastric; e- emesis
M- Miosis
B- Bronchorrhea
B- Bronchospasm
B- Bradycardia

52
Q

Treatment for OP poisoning?

A

Atropine + Cholinesterase reactivator: Oximes

53
Q

Examples of Cholinesterase reactivators?

A

Pralidoxime
Obidoxime

54
Q

What are Nn antagonists also known as?

A

Ganglion blockers

55
Q

What are Nm blockers also known as?

A

NM blockers

56
Q

What is the prototype anti-cholinergic drug?

A

ATROPINE

57
Q

Which drug that causes sedation is also used for motion sickness?

A

Scopalamine

58
Q

Which Anti-cholinergic drug is used as an anti-spasmodic, anti-secretory, and in mushroom poisoning?

A

Atropine

59
Q

Effects of atropine:

A

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
Q

In what cases is Atropine contraindicated?

A

Narrow-angle glaucoma
BPH

61
Q

Treatment for atropine/belladonna poisoning?

A

Physostigmine

62
Q

Examples of competitive ganglion blockers?

A

Hexamethonium
Mecamylamine

63
Q

What is the dominant tone in the heart and the effect of ganglion blockade on the heart?

A

Parasympathetic; Tachycardia (reduction in A.Ch)

64
Q

What is the dominant tone in the arteriole and the effect of ganglion blockade?

A

Sympathetic; Vasodilation, and hypotension

65
Q

What is the dominant tone in the veins and the effect of ganglion blockade?

A

Dilation, reduction in VR, and reduction in CO

66
Q

Which drug is used to treat nicotine addiction?

A

Varenicline

67
Q

What are the catecholamines of the sympathetic system?

A

Epi, NE, Dopa.

68
Q

What enzyme metabolizes catecholamines?

A

MAO and COMT

69
Q

How do Cocaine and TCA anti-depressants potentiate the effect of NE and E?

A

Neuronal reuptake inhibitors

70
Q

What are the types of Adrenergic receptors and what types of receptors are they?

A

Alpha 1 - Gq
Alpha 2 - Gi
Beta 1 - Gs
Beta 2 - Gs
Beta 3 - Gs
D1 - Gs

[remember ‘qissss’]

71
Q

Which is the only pre-synaptic adrenergic receptor?

A

Alpha 2: Gi; it inhibits the pre-synaptic release of NE

72
Q

Primary function of Alpha 1 on blood vessels?

A

Vasoconstriction: increase in the VR (veins) and Increase in TPR and Increase in DBP (arterioles)

73
Q

Primary function of B1?

A

Increases HR, Increases Contraction
Increases renin release
Increases O2 demand

74
Q

Effect of B2?

A

Bronchodilation
Vasodilation: Reduces TPR and DBP

75
Q

Where does B3 work on?

A

Bladder and Fat cells

76
Q

Which drug is used as a nasal decongestant?

A

Phenylephrine: A1 Selective, direct agonist

77
Q

Which A2 Selective direct agonist is used to inhibit NE release?

A

Clonidine

78
Q

Which drug acts centrally in the management of MS?

A

Tizanidine: Central A2 agonist

79
Q

What are some important B2 agonists? And uses?

A

Albuterol
Salmeterol
Terbutaline

ALL OF THEM ARE HELPFUL TO TREAT ASTHMA

80
Q

Which drug other than Oxybutynin is used to treat urinary urgency and frequency

A

Mirabegron

81
Q

Which selective B1 agonist increases HR and contractility?

A

Dobutamine

82
Q

On what receptors does Epi work in low doses?

A

B2 > B1 = A1 = A2

83
Q

On what receptors does Epi work in Medium doses?

A

B1 = B2 = A1 = A2

84
Q

On what receptors does Epi work in high doses?

A

A1 > A2 = B1 = B2

85
Q

What drug is given to the patient in anaphylactic shock?

A

Epi

86
Q

NE action receptors?

A

A1 = A2 > B1 [Raises both SBP (B1) and DBP (A1)]

87
Q

Uses of NE?

A

Cardiac arrest
Hypotensive state in shock and MI

88
Q

What is the effect of dopamine in low, med, and high doses?

A

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
Q

What is the drug of choice in Cardiogenic shock?

A

Dopamine: Because, D1 action maintains renal blood flow (prevents acute tubular necrosis), B1 action improves cardiac function, and A1 action maintains BP

90
Q

On what receptor does Isoproterenol act?

A

B1 + B2 + B3 (Non-selective Beta agonist)

91
Q

What is Dale’s vasomotor reversal?

A

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
Q

Why are fermented products such as cheese, yogurt, wine, beer, and meats such as beef contraindicated when a patient is on MAO inhibitors?

A

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
Q

Non-selective Alpha antagonist example?

A

Phenoxybenzamine: Used in Pheochromocytoma, Raynaud’s syndrome

94
Q

What is an example of a competitive, reversible antagonist for A1 and A2?

A

Phentolamine

95
Q

What is the suffix of drugs that selectively block A1?

A

-osin.
Ex: Prazosin

96
Q
A

Cardiac Pharmacology: Professor slides (8 decks)

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