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Pharmacology > Chapter 9 > Flashcards

Chapter 9 Flashcards

1
Q

What drug targets the Na+ choline transporter?

A

Inhibited by hemicholinium

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2
Q

What enzyme converts acetyl-CoA and Coline to acetylcholine?

A

Choline acetaltransferase (ChAT)

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3
Q

What action does vesimacol inhibit?

A

The ACh/H+ antiporter function. Therefore no ACh is sotred in the vessicles.

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4
Q

What kind of drugs will inhibit AChE?

A

AChE inhibitors. Allos ACh more time to interact with the receptors in the terminal bouton.

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5
Q

What does hexamethonium cause?

A

It causes a lack of positive feedback of ACh relase which decreases the autoincreaseing effect at high frequency stimulation.

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6
Q

What do cholinergic vessicles contain besides ACh?

A

ATP and Heparin sulfate proteoglycans which serve as counter ions for ACh

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7
Q

Increase of Ca2+ in the terminal bouton causes what?

A

Binding of synaptotagmin to the SNARE-complex which mediate attachment and fusion.

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8
Q

Location and Gprotein associated with Muscarinic M1

A

Gq/11

Located in the autonomic ganglia and the CNS

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9
Q

Location and Gprotein associated with muscarinic M2

A

beta gamma of G protein

Located in the Heart

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10
Q

Location and Gprotein associated with:

M3

M4

M5

A

M3: Smooth muscle, Gq/11

M4: CNS, Beta Gamma

M5: CNS, same as Gq/11

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11
Q

Which muscarinic receptors facilitate cellular excitability?

A

M1, M3, M5

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12
Q

Which muscarinic receptors surpress excitability?

A

M2, M4

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13
Q

How many molecules of ACh are required to open the nAChR?

A

Two, whcih bind between the alpha subunits

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14
Q

Which nicotinic receptors are located at the NMJ?

A

NM or N1

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15
Q

Which nicotinic receptors are located in the CNS or at autonomic ganglia?

A

NN or N2

-composed solely of alpha and beta subunits

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16
Q

What are the two types of cholinesterases?

A
  • AChE (acetylcholinesterase)
  • Butyrylcholinesterase
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17
Q

What is the net general response to clincal doses of atropine in a human adult with a normal hemodynamic state?

A

Mild tachycardia, with or without flushing of the skin, and no profound effect on blood pressure.

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18
Q

What are the four steps of the generalized response of the ANS to choinergic neurotransmission?

A
  • EPSP summation
  • Slow EPSP
  • IPSP

Late, Slow, EPSP

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19
Q

What is the primary event in the post-synaptic ganglionic response triggering a rapid depolariation of the post-ganglionic neuron?

A

EPSP (End plate synaptic potential)

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20
Q

What factors mediate the slow EPSP?

A

Mediated by M1 muscarinic receptors.

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21
Q

What causes the IPSP

A

largely a product of Catacholamine stimulation of dopaminergic and alpha-adrenergic receptors.

-some are mediated by M2 muscarinic receptors

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22
Q

What causes the late, slow EPSP

A

Mediated by a decrease in potassium conductance

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23
Q

How long does the Late, slow EPSP last and what is its purpose?

A
  • Several minutes
  • to regulate post synaptic neuronal sensitivity to repetitive depolarization
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24
Q

Different kinds of synaptic signal images

A
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25
What are the three predominantly sympathetic systems/organs?
- Arterioles (adrenergic) - Veins (adrenergic) - Sweat glands (cholinergic) \*the rest of the listed systems are Parasympathetic (cholinergic) systems.
26
What happens to ACh level durring wakefullness and REM sleep?
They increase
27
What happens to levels of ACh durring imes of inattentiveness and non-REM/Slow-wave sleep?
ACh decresses
28
How does a cholinergic dysfunction affect our cognitive function?
- Causes cognitive, behavioral and functional deficits. - E.g. AD, PDD, DLB
29
What are the major clinical uses of cholinergic and anticholinergic drugs?
- modulation of GI motility - Xerostomia (dry mouth) - Glaucoma - Motion sickness/antiemesis - Neuromuscular disease (myasthenia gravis/Eaton-lambert) - acute neuromuscular blockade and reversal - ganglionic blockade during aortic dissection - dystonias(torticollis), headaches and pain - reversal of vagal-mediated bradycardia - mydriasis - bronchodilators in COPD - Bladder spasms and urinary incontinence - cosmetic effect (skin lines etc.) - Tx of AD and cognitive dysfunction
30
What are the inhibitors of ACh synthesis, storage and release (3)
- Hemicholinium-3 (targets choline transporter) - Vesamicol (targets the ACh/H+ antiporter for vesicles) - Botulinum Toxin A (prevents vesical fusion)
31
What is botulinum toxin A used to treat?
- Toticollis, achalasia, strabismus, blepharospasm - Cosmetic treatment of facial lines and wrinkles (BoTOX) - Headache and pain syndromes
32
What is the action of acetylcholinesterase inhibitors?
Bind and inhibit AChE.
33
What is the clinical significance of Edrophonium?
- Rapid acting and short lived (2-10min) AChE inhibitor. - Allows for the determination of Disease affects caused by decreased ACh or by sustained depolarization. - If Disease is Myasthenia Gravis or Eaton-lambert then Edrophonium will help - Will not help muscle paralysis caused by sustain depolarization of the neuron.
34
What is the action of Neostigmine?
- blocks AChE and activates nAChR - potentiates parasympathetic action in the GI tract, increasing mobility and secretions.
35
What drug is used to counteract anticholinergic toxicity and how?
- Physostigmine - Able to enter the brain and spinal cord
36
How long is the half life of diisopropyl phluorophosphates?
100s of hours
37
What is "aging" in respect to diisopropyl fluorophosphates?
- A process in which the O-P bonds withen the enzyme-organophosphate complex are broken in favor of stronger bonds between the enzyme and the inhibitor. - makes the inhibition completely irreversible. - Pralidoxime before aging will recover AChE function.
38
What is a long lasting AChE used to treat Myasthenia gravis?
Pyridostigmine
39
What four (4) AChE inhibitors are commonly used to treat AD, and other conginitive diseases?
- Tacrine (AD but rarely used) - Donepezil (Severe AD) - Rivastigmine (PDD) - Gelantamine
40
What are 2 clinical uses of muscarinic receptor agonists?
- Diagnosis of asthma - Miotic agents
41
What are the clinical uses of nicotinic receptor agonists?
Clincally used for induction of paralysis.
42
What re the two divisions of muscarinic receptor agonists?
- Choline esthers - Alkaloids
43
What is the clinical use and selectivity of methacholine?
- Used in the diagnosis of Asthma. - Selective for cardiovascular muscarinic cholinergic receptors
44
Why is Carbecol not used systemically? Where and what is it used for?
- Cannot be used systemically becuase it is selective for nicotinic receptors and reacts unpredictably. - Used topically to induce miosis and reduce intraocular pressure
45
What is the drug of choice for promoting GI and urinary motility in postpartum, post-op, and other?
Bathanechol. -Selevtive for muscarinic receptors
46
What is the significant of muscarine?
Selective for muscarinic receptors and can easily cross GI mucosa.
47
What is the most clincally used alkaloid and what is it used for?
Pilocapine -Miotic agent and a sialagogue used to treat xerostomia
48
Cevimeline
Alkaloid -M1 and M3 agonist used to treat xerostomia in Sjogen's syndrome
49
What is succinylcholine typically used for and how does it work?
- Paralyzing agent used in surgery - Binds to nAChR and holds thme open causing depolarizing events in the neuron
50
What is the prototypic muscarine antagonist?
Atropine
51
What are the uses of Atropine?
- Pupil Dilation - Reversal of symptomatic sinus bradycardia - inhibit excessive salivation and mucus secretion as well as vagl reflexes from surgical trauma. - Reversal of **muscarine poisoning** (mushrooms)
52
What are the uses of Scopoloamine (hyoscine hydrobromide)?
Motion sickness, nausea, and antiemetic -Pallitive care (reduces orla secretions and is a mild sedative)
53
What are the uses of ipratropium and tiotropium?
Bronchodilator in the treatment of COPD
54
What are 5 antimuscarinic agents used in the treatment of urinary incontinence?
- oxybutinin - tolterodine (less dry mouth) - Fesoterodine - darifenacin (selectve M3) - salifenacin(Selective M3)
55
What are the uses of Biperiden, Benztropine, and Trihexylphenidyl and who is the exception?
- used to treat tremors and rigidity in PD pts - CANNOT USE IN ELDERLY, will exacerbate cognitive deficits.
56
What are other uses for Benztropine and trihexylphenidyl?
Used to treat EPS (extrapyramial symptoms of (akathisia restless leg syndrome))
57
What is the primary use of selective nicotinic receptor antagonists?
-produce nondepolarizing (competitive) neuromuscular blockade
58
What does Tubocurare do?
Blcocks nicotinic ACh receptors causing flaccid paralysis.
59
What is the difference between tubocurare and succinylcholine?
- Succinylcholine depolarizes the membrane before it causes paralysis (contraction followed by paralysis). - tubocurare blocks the receptor (flaccid paralysis)
60
What are anticholinergic symptoms?
Blind as a bat, mad as a hatter, red as a beet, hot as a hare, dry as a bone, bowel and bladder lose their tone, and the heart runs alone (tachycardia).
61
What is the use for mecamylamine and trimethaphan?
Major use is to reduce HTN in a pt with acute aortic dissection.
62
What is the common cause and treatment of Muscarinic cholinergic toxicity?
- Ingestion of toxic mushrooms - Competitive blockade using atropine is the treatment - Symptoms: Nausea, vommiting, diarrhea, sweating, hypersalivation, cutaneous flushing, brady, broncoconstriction
63
What are the common causes, symptoms are treatment of **nicotinic cholinergic toxicity**?
- Ingestion of cigarettes and pesticides - CNS overexcitation - Tx: Antiepileptic drugs, mechanical ventilation, **atropine**
64
What are the common causes, symptoms and Tx of cholinesterase inhibitor poisoning?
- Exposure to organophosphate pesticides - **Muscarinic toxicity signs followed by nicotinic signs** - Large atropine doses and administration of pralidoxime to regenerate the enzyme.

Pharmacology (17 decks)

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