Pharmacology - Autonomics I Flashcards

(118 cards)

1
Q

Postganglionic PS fibers release:

A

Aceytlcholine

“cholinergic”

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2
Q

Postganglionic symptathetic fibers generally release:

A

Norepinephrine

“adrenergic”

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3
Q

T/F: Not all postganglionic sympathetic fibers are adrenergic - other NTs can be used.

A

True

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4
Q

All preganglionic neurons, both sympathetic and parasympathetic, release:

A

ACh and stimulate nicotinic receptors on postganglionic neurons

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5
Q

All preganglionic neurons, both sympathetic and parasympathetic, release ACh and stimulate ______ receptors on postganglionic neurons.

A

Nicotinic

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6
Q

All postganglionic PS neurons release ACh and stimulate _____ ACh receptors on target tissues.

A

Muscarinic

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7
Q

Postganglionic symptathetic fibers to sweat glands release:

A

ACh

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8
Q

Postganglionic sympathetic fibers to renal vessels release:

A

Dopamine

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9
Q

____ blocks ACh and, when, injected, can locally inhibit muscle contraction.

A

Botulinim Toxin A

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10
Q

Drugs that block NE synthesis, storage or release, for example, guanethidine, are useful in several diseases like hyptertension, because they block _____ function

A

sympathetic, but NOT parasympathetic

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11
Q

What is the physiologic effect of cocaine?

A

To block NE uptake –> increase adrenergic transmission

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12
Q

Cholinoceptors include:

A

Muscarinic

Nicotinic

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13
Q

Where are M1 receptors found?

A

Location:
CNS
sympathetic PG neurons

Effects:
formation of IP3 and DAG
increased intracellular Ca
**same as M3 receptors (exocrine glands, CNS, vessels)
**same as M5 receptors (vascular endothelium esp cerebral vessels, CNS)

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14
Q

Where are M2 receptors found?

A

Location:
Myocardium
Smooth muscle
CNS

Effects:
open K channels
inhibit Adenyl cyclase
**same as M4 receptors (CNS)

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15
Q

Nicotinic receptors, both Nn (N2) and Nm (N1) have what effect?

A

Opening of Na and K channels, depolarization

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16
Q

Where are Nm (N1) receptors found?

A

Skeletal muscle neuromuscular end plates

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17
Q

What is the effect of Alpha 1 adrenergic receptors?

A

Effects:
Formation os IP3 and DAG
increased intracellular Ca

Location:
Postsynaptic effector cells esp smooth muscle

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18
Q

What is the effect of Alpha 2 (adrenoreceptors) receptors?

A

Effects:
Inhibition of adenyl cyclase
decreased cAMP

Location:
Presynaptic adrenergic nerve terminals, 
platelets
lipocytes
smooth muscle
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19
Q

All beta (adrenoreceptors) receptors have what function?

A

stimulate AC
increase cAMP

all found in heart, beta-1 found most widespread in the body

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20
Q

All muscarinic receptors (M1-M5) are

A

GPCRs
M2, M4 –> Gi (decrease cAMP, hyperpolarize) –> inhibition of neurotransmitter release

M1, M3, M5 –> Gq (increase IP3 and DAG)

**enables ACh to have specific effects, depending on the receptor

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21
Q

Class: Bethanechol

A

Direct acting carbamic acid ester

cholinomimetic

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22
Q

MOA: Bethanechol

A

Direct-acting muscarinic cholinomimetic

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23
Q

Uses: Bethanechol

A
Post-operative and neurogenic ileus; 
urinary retention (bowel and bladder smooth muscle ACh-innervated)
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24
Q

Side Effects: Bethanechol

A

SLUDGE
Salivation: stimulation of the salivary glands
Lacrimation: stimulation of the lacrimal glands
Urination: relaxation of the internal sphincter muscle of urethra, and contraction of the detrusor muscles
Diaphoresis
Gastrointestinal upset: Smooth muscle tone changes causing gastrointestinal problems, including diarrhea
Emesis: Vomiting

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25
Class: Pilocarpine
Direct acting non-ester alkaloid | cholinomimetic
26
MOA: Pilocarpine
Direct-acting muscarinic cholinomimetic
27
Uses: Pilocarpine
Glaucoma (ACh activates sphincter and ciliary muscles of eye)
28
Side Effects: Pilocarpine
SLUDGE Salivation: stimulation of the salivary glands Lacrimation: stimulation of the lacrimal glands Urination: relaxation of the internal sphincter muscle of urethra, and contraction of the detrusor muscles Diaphoresis Gastrointestinal upset: Smooth muscle tone changes causing gastrointestinal problems, including diarrhea Emesis: Vomiting
29
Class: Cevimeline
Direct acting non-ester alkaloid | cholinomimetic
30
MOA: Cevimeline
Direct-acting muscarinic cholinomimetic
31
Uses: Cevimeline
Dry mouth/xerostomia (in, e.g., Sjogren's, post-radiation therapy; via increased salivation)
32
Side Effects: Cevimeline
SLUDGE Salivation: stimulation of the salivary glands Lacrimation: stimulation of the lacrimal glands Urination: relaxation of the internal sphincter muscle of urethra, and contraction of the detrusor muscles Diaphoresis Gastrointestinal upset: Smooth muscle tone changes causing gastrointestinal problems, including diarrhea Emesis: Vomiting
33
Class: Nicotine
Direct acting non-ester alkaloid | cholinomimetic
34
MOA: Nicotine
Direct-acting muscarinic cholinomimetic
35
Uses: Nicotine
Smoking cessation/reduces craving
36
Class: Physiostigmine
Indirect acting carbamate | cholinomimetic
37
MOA: Physostigmine Echothiophate
AChE inhibitor (short acting)
38
Uses: Physostigmine Echothiophate
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
39
Side Effects: Physostigmine
SLUDGE general increase in cholinergic neurotransmission; paralysis
40
``` Class: Muscarine Pilocarpine Cevimeline Nicotine ```
Direct acting non-ester alkaloid | cholinomimetic
41
Uses: Pilocarpine Physostigmine Echothiophate
Glaucoma
42
Class: Edrophonium
Indirect acting non-ester | cholinomimetic
43
MOA: Edrophonium
AChE inhibitor (v. short acting)
44
Uses: Edrophonium Pyridostigmine Neostigmine
Myasthenia Gravis
45
Side Effects: Edrophonium
SLUDGE general increase in cholinergic neurotransmission; paralysis
46
Class: Neostignmine
Indirect acting carbamate | cholinomimetic
47
Class: Neostigmine Physostigmine
Indirect acting carbamate
48
MOA: Neostigmine
AChE inhibitor (short acting)
49
Uses: Neostigmine
Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade
50
Side Effects: Neostigmine
SLUDGE general increase in cholinergic neurotransmission; paralysis
51
Class: Muscarine
Direct acting non-ester alkaloid | cholinomimetic
52
MOA: Muscarine
Direct-acting muscarinic cholinomimetic
53
Side Effects: Muscarine
SLUDGE
54
Class: Donepezil
Indirect acting non-ester | cholinomimetic
55
MOA: Donepezil
AChE inhibitor
56
Uses: Donepezil
Alzheimer's (amplifies endogenous ACh in brain)
57
Side Effects: Donepezil
SLUDGE general increase in cholinergic neurotransmission; paralysis
58
Class: Donepezil Edrophonium
Indirect acting non-ester | cholinomimetic
59
``` Side Effects: Neostigmine Physostigmine Donepezil Sarin Edrophonium Echothiophate Pralidoxime ```
SLUDGE general increase in cholinergic neurotransmission; paralysis
60
``` Side Effects: Bethanechol Muscarine Pilocarpine Cevimeline ```
SLUDGE
61
Class: Echothiophate
Indirect acting organophosphate | cholinomimetic
62
MOA: Echothiophate
AChE inhibitor (long acting)
63
Uses: Echothiophate
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
64
Side Effects: Echothiophate
SLUDGE general increase in cholinergic neurotransmission; paralysis
65
Class: Sarin
Very potent indirect acting organophosphate | cholinomimetic
66
MOA: Sarin
AChE inhibitor
67
Uses: Sarin
volatile nerve gas
68
Side Effects: Sarin
SLUDGE general increase in cholinergic neurotransmission; paralysis DEATH
69
Class: Pralidoxime
Strong nucleophile | cholinomimetic
70
MOA: Pralidoxime
AChE inhibitor
71
Uses: Pralidoxime
Poisoning by nerve gas, insecticide
72
Class: Atropine
Tertiary amine antimuscarinic | cholinergic receptor inhibitor
73
``` Class: Atropine Scopolamine Dicyclomine Tropicamide Tolterodine Benztropine ```
Tertiary amine antimuscarinic | cholinergic receptor inhibitor
74
MOA: Atropine
Blocks muscarinic receptors
75
``` MOA: Atropine Scopolamine Dicyclomine Tropicamide Tolterodine Benztropine Ipratroprium Tiotropium ```
Blocks muscarinic receptors
76
``` Side Effects: Atropine Scopolamine Dicyclomine Tropicamide Tolterodine Benztropine Ipratroprium Tiotropium ```
General block of muscarinic functions
77
Uses: Atropine Tropicamide
To cause: Mydriasis Cycloplegia is paralysis of the ciliary muscle of the eye, resulting in a loss of accommodation *Tropicamide has a short half life
78
Uses: Scopolamine
Motion sickness
79
Uses: Dicyclomine
Reduce transient hypermotility of GI tract
80
Uses: Tolterodine
Treat transient cystitis; postoperative bladder spasms; incontinence
81
Uses: Benztropine
To prevent manifestations of Parkinson's disease
82
Class: Ipatroprium Tiotropium
Quarternary amine antimuscarinic | cholinergic receptor inhibitor
83
Uses: Ipatroprium Tiotropium
Bronchodilation in asthma or COPD
84
Class: Succinylcholine
Depolarizing blocker | cholinergic receptor inhibitor
85
MOA: Succinylcholine
Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation
86
Uses: Succinylcholine
Brief procedures (e.g., tracheal intubation, reset dislocated joints)
87
Side Effects: Succinylcholine Tubocurarine Mivacurium
Respiratory paralysis; | disturbance of autonomic function
88
MOA: Tubocurarine Mivacarium
Blocks nicotinic (Nm) receptor
89
Class: Tubocurarine Mivacarium
Nondepolarizing blocker | cholinergic receptor inhibitor
90
Uses: Tubocurarine Mivacarium
Muscle relaxant for surgery w/o deep anesthesia
91
Class: Botulinum Toxin A
local paralytic
92
MOA: Botulinum Toxin A
Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
93
Uses: Boltulinum Toxin A
Reduce frown lines and wrinkles; achalasia; strabismus; oromandibular dystonia
94
Class: Hexamethonium Mecamylamine
Ganglionic blocker | cholinergic receptor inhibitor
95
MOA: Hexamethonium Mecamylamine
Blocks ganglionic (Nn) receptor and sympathetic tone
96
Uses: Hexamethonium Mecamylamine
Hypertensive crisis; "Bloodless" field surgery
97
Clinical Uses: Ipratroprium Tiotroprium
to cause bronchodilation in asthma and COPD
98
What kind of amine is atropine?
Tertiary - can interact with CNS AND peripheral muscarinic receptors well - good for nerve gas exposure
99
Mnemonic for atropine overdose
Dry as a bone - no glandular secretions Blind as a bat - blockade of accomodation and excessive dilation Red as a beet - atropine flush - dilation of cutaneous blood vessels AND inhibition of sweat glands (inhibition alpha-1 mediated vasoconstriction) --also atropine fever from lack of sweating Mad as a hatter - delirium - CNS
100
Atropine fever can be lethal in:
infants and small children Sweat glands are sympathetic but utilize cholinergic post-ganglionic fibers **symptom managament** to treat, do not use a cholinesterase inhibitor ie physostigmine
101
Prazosin
alpha-blocker | alpha-1 selective antagonist
102
Phenoxybenzamine
alpha-blocker | Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor)
103
Therapeutic Use: Prazosin
Raynaud's BPH Primary HTN
104
Therapeutic Use: Phenoxybenzamine
Pheochromocytoma, Raynaud's, frostbite
105
MOA Tyramine
Increases NE release | gets uptaken into cleft like NE
106
Best way to adrenergically increase HR:
Epinephrine | Beta-1 effects greater than NE
107
MOA Terbutaline
beta-2 selective agonist Uses: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD; early labor
108
Glaucoma is treated with muscarinic agonists or antagonists?
muscarinic agonists, which facilitate the outflow of aqueous humor
109
An alpha agonist vasodilates or vasocontricts?
Vasoconstricts
110
Parasympathetic control of salivation is mediated by:
M3 receptors found in salivary glands; these receptors elevate calcium concentration and activate the secretory process.
111
T/F: Although MAO may contribute to the ultimate metabolism of NE, it does not assist in the termination of NE neurotransmission.
True Termination of NE neurotransmission: Uptake by non-neuronal cells. Diffusion out of the synaptic cleft. Uptake by neuron plasma membrane.
112
Phenylephrine MOA
alpha-1 agonist decongestant vasoconstriction → increase in total peripheral resistance → increase in blood pressure → activation of a baroreceptor response to decrease sympathetic outflow and increase parasympathetic outflow, resulting in a decrease in heart rate.
113
For prevention of migraines, consider:
Propranolol, methysergide, and calcium channel blockers have all been shown to be prophylactic in migraine therapy.
114
For treatment of an acute migraine, consider:
Ergotamine and the several “triptans” (e.g. sumatriptan [Imitrex]) are effective in the acute treatment of a migraine headache.
115
T/F: Activation of α2 receptors which are presynaptic can reduce subsequent release of norepinephrine from post-ganglionic fibers.
True
116
MOA Succinylcholine
Succinylcholine (diacetylcholine) activates Nm persistently because it is poorly hydrolyzed at the NMJ. This hyperactivation causes persistent depolarization at the endplate, blocking Nm function and leading to flaccid paralysis.
117
Side effects: Prazosin
Orthostatic HTN; | Tachycardia
118
How would metoprolol decrease renin release?
blocking beta receptors on juxtaglomerular apparatus cells