exam 1: lecture 2 Flashcards

1
Q

what does cholinergic mean?

A

cholinergic receptors respond to aCH

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2
Q

what are the two preganglionic nerves that contributes to PARAsympathics?

A

cranial (from midbrain and medulla) and splanchic nerves (from sacral region)

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3
Q

for parasympathetics, is the terminal ganglion close or far from target organ?

A

CLOSE to target organ

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4
Q

where are the pre-ganglionic fibers from in sympathetic?

A

thoracic region (white rami communication) and lumbar region

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5
Q

are the ganglions far or close to the target organ in sympathetics?

A

FAR AWAY from target organs

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6
Q

what are the 4 cranial nerves part of parasymapethics? and where do they come from?

A

CN 3 7 9 10
3 oculomotor nerve - mid brain
7 facial nerve - medula
9 glossopharyngeal nerve - medula
10 vagus nerve

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7
Q

where does the oculomotor nerve take off from? WEIRD NAME

A

takes off from the etenger wessfold nucleolus

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8
Q

for CN3, what are the presynaptic fibers, post synaptic fibers and what does it do?

A

presynaptic fibers synapses at the ciliary ganglion* and it goes to the post synaptic fibers to the eye and does:
constriction = myosis, cilliary body constriction, pupillary muscle constriction, accomdation

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9
Q

for CN7, what are the presynaptic fibers and post ganglion fibers?

A

the presynaptic fibers are sphenopalatine ganglion* and goes to the post gang fibers to stimulate salvation (via submandibular gang*) and lacrimation

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10
Q

For CN9, what are the presynaptic fibers and post synaptic fibers?

A

presynaptic fibers synapses at the otic ganglion and the post synaptic fibers synapses at the parotid glands and stimulates salvation too

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11
Q

for CN10, what effects does it have on the heart, lungs, gut?

A

heart: slows it down as its a negative inoctropic
lungs: bronchoconstriction, increases secretion
gut: peristalsis

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12
Q

where do splanchnic n come from and what effect does it have on the bladder and gut?

A

comes from sacral region S2-S4

constriction of bladder and peristalsis of the gut

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13
Q

what do cholinergic neurons release? what are examples of cholinergic?

A

they release aCH. EX are:
- ALL of parasympathetics (pre gang and post gang fibers)
- pre ganglionic fibers in sympathetic
- post ganglionic fibers in sympathetic to sweat glands
- motor and skeletal nerves

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14
Q

what do adrenergic release? are they majority sympathetic or parasympathetic?

A

NE. Mostly sympathetic fibers and they innervate heart / blood vessels –> vasoconstrictions

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15
Q

explain how cholinergic neurons release aCH. 6 steps

A

choline acetyltransferase enzyme (in the cytosol) combines acetyl coA and choline to make aCH.

aCH goes to the vesicle.

AP travels down the cell and Ca voltage gated channel opens and Ca rushes into the cell and binds to the vesicle

causes exocytosis of the vesicle

aCh will bind and act on the two receptors: muscarinic or nicotinic receptors

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16
Q

what are two ways to stop aCH signals?

A

acetylcholinesterase and BOTOX

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17
Q

how does acetylcholinesterase work?

A

this enzyme breaks down aCH into choline and acetate

acetate will be metabolized and choline will go back to the axon with sodium

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18
Q

diff between acetylcholinesterase and choline acetyltransferase?

A

acetylcholinesterase is an enzyme that breaks down aCH

choline acetyltransferase is an enzyme that combines choline and acetyl coA to make aCH

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19
Q

how does botox work?

A

it blocks the release of acH!!

botox goes into the axon and binds to the vesicle to prevent it from binding to the membrane for exocytosis

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21
Q

whats a danger effect of botox?

A

dangerous to the diaphragm

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21
Q

what kind of receptor is nicotinic and muscarinic receptor?

A

nicotinic receptor is a ligand gated ion channel

muscarinic receptor is a GCPR receptor

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22
Q

where are nicotinic receptors found on? two places!

A

nicotinic receptors are found on ALL POST ganglionic cell in BOTH sympathetic and parasympathetic and on skeletal muscles at the neuromuscular junctions

23
Q

what type of structure is the nicotinic receptor? what are the subunits for each?

A

Pentameric structure
it has two subtypes: muscle and neuronal

muscle: 2 alpha, 1 beta, 1 gamma, 1 delta
neuronal: 2 alpha, 3 beta or ALL alpha

COMMON: alpha subunits for binding of aCH

24
Q

what happens when ach binds to the alpha subunit on the nicotinic receptor?

A

ach binds to the alpha subunit and causes conformational change, causes Ca/Na to rush into the cell and AP is reached

25
Q

which is more faster: nicotinic or muscarnic receptors?

A

nicotinic!

26
Q

where are muscarinic receptors found?

A

the target organs are in the parasympathetic systems:
sacral splanchnic nerves: bladder and gut, parotid glands, submandibular glands, lungs, heart

AND sweat glands in the sympathetic nervous system

27
Q

what are the subtypes for muscarinic receptors?

A

stimulatory: M1 M3 M5
inhibitory: M2

28
Q

where are the stimulatory/inhibitory muscarinic subtypes found?

A

stimulatory: target organs and sweat glands, ass w Gq proteins which activates phospholipase C –> IP3-DAG –> releases Ca –> muscle contractions

inhibitory: heart organ, ass w Gi proteins, inhibits adenylyl cyclase –> turns off cAMP production –> K+ release, hyperpolarizattion –> decreases HR

29
Q

what is the MOA of acetylcholine?

A

muscarinic agonist!

30
Q

how does aCH affect CV, lungs, urinary, GI, and eye?

A

CV: aCH will bind to M2 receptors on the heart (Gi inhibitory proteins) and will slow HR, negative chronotropic effect

Lung: aCH bind to M1 3 5 receptors on lungs (Gs) and increases mucus secretion and bronchospasm

Urinary: bind to M1 3 5 receptors on the bladder and increase bladder detrusors contractions

GI: bind to M1 3 5 on stomachs and increase peristalsis

Eye: bind to M1 3 5 on eye and increase myosis and contraction

31
Q

what are other effects of ACH muscarinic agonist?

A

lacrimal glands tear production, nasopharyngeal secretion, salivary glands secretion, sweat glands secretions

32
Q

what are two types of cholinergic receptors?

A

nicotinic and muscarinic receptors both of which can bind to ach

33
Q

easy way to think of m1-m5?

A

m1 m3 m5 - Gq - Ca+ - contraction of sweat glands and smooth muslces

M2 M4 - Gi - inhibitory of parasympathetic functions

34
Q

what are the four muscarinic agonist drugs?

A

PABC “pretty anika buys candy”
1. pilocarpine
2. ach
3. bethanechol
4. carbachol

35
Q

explain the pharmokinetics for muscarinic agonist? how are they given? what happens?

A

they are given topically for eye and PO in other cases.

Given PO, it can lead to poor absorption and peristalsis so increasing the dose is needed

36
Q

what are the untoward effects of muscarinic agonist drugs?

A

bradycarida, hyperhidrosis, asthma/COPD, or anything at leads to exaggerated organs

37
Q

what does aCH and carbachol treat?

A

ach is given topically for eyes and increases aqueous humor

carbachol tx glaucoma and increases AQ

38
Q

what does bethanechol and pilocarpine tx?

A

pilocarpine drugs increases salivary glands so it tx xerostomia (dry mouth) and Sjogren syndrome (autoimmune dx that attacks salivary glands). Can also be used for eyes

(b for bladder)
bethanechol drugs is used to tx post sx urinary retention. its used for bladder constriction so a small bladder

39
Q

what is inocybe mushroom and what three things does it contain?

A

pilocarpine!, muscarine, and areocline

40
Q

how will the present present if they consume inocybe mushroom and how to tx?

A

PT will have has EXCESS ACH!!! (since mushroom has pilocarpine)

Effects:
CV: bradycardia
GI: nausa, vomitting
Glands: high secretions
Lungs: bronchial constriction, increase secretion
Eyes: myosis pupils

TX: muscarinic antagonist drugs !!! to prevent more ach!!

41
Q

what are the 7 muscarinic antagonist drugs?

A
  1. Atropine
  2. Ipratropium
  3. Tiotroprium
  4. Tolterodine
  5. Oxybutynin
  6. Scopolamine
    7.Homatropin
42
Q

what is the MOA and indication for atropine?

A

MOA: muscarinic antagonist
indication: ach overdose!

if theres an ACH overdose, you would give a muscarinic antagonist to block the release of ach

43
Q

how does atropine affect CV, lungs, GI, eyes, CNS and others?

A

CV: blocks M2 receptor, tachycardia, + chronotropic effect
lungs: bronchodilation and decrease secretion
GI: constipation
eyes: pupillary dilation
CNS: mental status changes, seizure, coma, death

no lacrimal tears, no sweat glands secretion, dry mouth, dry skin

44
Q

what is the MOA + indication + effects + pharmacokinetics for ipotropium drug?

A

MOA: muscarinic antagoist! - it is used with B2 agonist (ex: albuterol)

Effects: it inhibits bronchial secretion and causes broncho dilation

pharmacokinetics: via inhilation

Indication: used for COPD

45
Q

what is the MOA + indication + effects + pharmacokinetics for tiotropium drug?

A

MOA: muscarinic antagoist! - it is used with B2 agonist (ex: albuterol)

Effects: it inhibits bronchial secretion and causes broncho dilation

pharmacokinetics: via inhilation

Indication: used for COPD

46
Q

what is the MOA, indication, effects for tolterodine drug?

A

MOA: muscarinic antagonist!

Effects: it inhibits bladder detrusors muscles from contracting

Indication: a child who cannot control their bladder –> reduce bladder contraction
- quadriplegics: reduce bladder contraction
(when u contract you have urge to pee)

47
Q

what is the metabolism for tolterodine drug?

A

CYP2D6 and CYP3A4

48
Q

what is the MOA, indication, effects for oxybutynin drug?

A

MOA: muscarinic antagonist!

Effects: it inhibits bladder detrusors muscles from contracting

Indication: a child who cannot control their bladder –> reduce bladder contraction
- quadriplegics: reduce bladder contraction
(when u contract you have urge to pee)

49
Q

what is the metabolism for oxybutynin drug?

A

CYP3A4 cytochrome enzyme PHASE 1!

so, oxybutynin will inhibit or activate CYP3X4

if we inhibit CYP, the drug will INCREASE the effective dose
if we activate CYP, the drug will DECREASE effective dose
(think about lecture 1 CYP450’s action)

50
Q

what is the MOA, indication, pharmacokinetics for scopolamine?

A

MOA: muscarinic antagonist. it prevents peristalsis and something in the middle ear is inhibited from triggering nausae too

indication: motion sickness :(

pharmacokinetics: transdermal patch!

51
Q

what is the drug for dx purpose when it comes to muscarinic agonist drugs?

A

methacholine - will bronchoconstrict and increase secretion

used for pulmonary test to airway hyperactivity

normal lungs will be okay but hyperactive lungs will be more reactivew

52
Q

what is the methacholine change test?

A

you take someones FEV1 and give dose of methacholine and measure FEV1 again. if theres 20% drop then that person is postive for maybe astha

53
Q
A