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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
Q

What are the three predominantly sympathetic systems/organs?

A
  • Arterioles (adrenergic)
  • Veins (adrenergic)
  • Sweat glands (cholinergic)

*the rest of the listed systems are Parasympathetic (cholinergic) systems.

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26
Q

What happens to ACh level durring wakefullness and REM sleep?

A

They increase

27
Q

What happens to levels of ACh durring imes of inattentiveness and non-REM/Slow-wave sleep?

A

ACh decresses

28
Q

How does a cholinergic dysfunction affect our cognitive function?

A
  • Causes cognitive, behavioral and functional deficits.
  • E.g. AD, PDD, DLB
29
Q

What are the major clinical uses of cholinergic and anticholinergic drugs?

A
  • 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
Q

What are the inhibitors of ACh synthesis, storage and release (3)

A
  • Hemicholinium-3 (targets choline transporter)
  • Vesamicol (targets the ACh/H+ antiporter for vesicles)
  • Botulinum Toxin A (prevents vesical fusion)
31
Q

What is botulinum toxin A used to treat?

A
  • Toticollis, achalasia, strabismus, blepharospasm
  • Cosmetic treatment of facial lines and wrinkles (BoTOX)
  • Headache and pain syndromes
32
Q

What is the action of acetylcholinesterase inhibitors?

A

Bind and inhibit AChE.

33
Q

What is the clinical significance of Edrophonium?

A
  • 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
Q

What is the action of Neostigmine?

A
  • blocks AChE and activates nAChR
  • potentiates parasympathetic action in the GI tract, increasing mobility and secretions.
35
Q

What drug is used to counteract anticholinergic toxicity and how?

A
  • Physostigmine
  • Able to enter the brain and spinal cord
36
Q

How long is the half life of diisopropyl phluorophosphates?

A

100s of hours

37
Q

What is “aging” in respect to diisopropyl fluorophosphates?

A
  • 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
Q

What is a long lasting AChE used to treat Myasthenia gravis?

A

Pyridostigmine

39
Q

What four (4) AChE inhibitors are commonly used to treat AD, and other conginitive diseases?

A
  • Tacrine (AD but rarely used)
  • Donepezil (Severe AD)
  • Rivastigmine (PDD)
  • Gelantamine
40
Q

What are 2 clinical uses of muscarinic receptor agonists?

A
  • Diagnosis of asthma
  • Miotic agents
41
Q

What are the clinical uses of nicotinic receptor agonists?

A

Clincally used for induction of paralysis.

42
Q

What re the two divisions of muscarinic receptor agonists?

A
  • Choline esthers
  • Alkaloids
43
Q

What is the clinical use and selectivity of methacholine?

A
  • Used in the diagnosis of Asthma.
  • Selective for cardiovascular muscarinic cholinergic receptors
44
Q

Why is Carbecol not used systemically?

Where and what is it used for?

A
  • Cannot be used systemically becuase it is selective for nicotinic receptors and reacts unpredictably.
  • Used topically to induce miosis and reduce intraocular pressure
45
Q

What is the drug of choice for promoting GI and urinary motility in postpartum, post-op, and other?

A

Bathanechol.

-Selevtive for muscarinic receptors

46
Q

What is the significant of muscarine?

A

Selective for muscarinic receptors and can easily cross GI mucosa.

47
Q

What is the most clincally used alkaloid and what is it used for?

A

Pilocapine

-Miotic agent and a sialagogue used to treat xerostomia

48
Q

Cevimeline

A

Alkaloid

-M1 and M3 agonist used to treat xerostomia in Sjogen’s syndrome

49
Q

What is succinylcholine typically used for and how does it work?

A
  • Paralyzing agent used in surgery
  • Binds to nAChR and holds thme open causing depolarizing events in the neuron
50
Q

What is the prototypic muscarine antagonist?

A

Atropine

51
Q

What are the uses of Atropine?

A
  • 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
Q

What are the uses of Scopoloamine (hyoscine hydrobromide)?

A

Motion sickness, nausea, and antiemetic

-Pallitive care (reduces orla secretions and is a mild sedative)

53
Q

What are the uses of ipratropium and tiotropium?

A

Bronchodilator in the treatment of COPD

54
Q

What are 5 antimuscarinic agents used in the treatment of urinary incontinence?

A
  • oxybutinin
  • tolterodine (less dry mouth)
  • Fesoterodine
  • darifenacin (selectve M3)
  • salifenacin(Selective M3)
55
Q

What are the uses of Biperiden, Benztropine, and Trihexylphenidyl and who is the exception?

A
  • used to treat tremors and rigidity in PD pts
  • CANNOT USE IN ELDERLY, will exacerbate cognitive deficits.
56
Q

What are other uses for Benztropine and trihexylphenidyl?

A

Used to treat EPS (extrapyramial symptoms of (akathisia restless leg syndrome))

57
Q

What is the primary use of selective nicotinic receptor antagonists?

A

-produce nondepolarizing (competitive) neuromuscular blockade

58
Q

What does Tubocurare do?

A

Blcocks nicotinic ACh receptors causing flaccid paralysis.

59
Q

What is the difference between tubocurare and succinylcholine?

A
  • Succinylcholine depolarizes the membrane before it causes paralysis (contraction followed by paralysis).
  • tubocurare blocks the receptor (flaccid paralysis)
60
Q

What are anticholinergic symptoms?

A

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
Q

What is the use for mecamylamine and trimethaphan?

A

Major use is to reduce HTN in a pt with acute aortic dissection.

62
Q

What is the common cause and treatment of Muscarinic cholinergic toxicity?

A
  • Ingestion of toxic mushrooms
  • Competitive blockade using atropine is the treatment
  • Symptoms: Nausea, vommiting, diarrhea, sweating, hypersalivation, cutaneous flushing, brady, broncoconstriction
63
Q

What are the common causes, symptoms are treatment of nicotinic cholinergic toxicity?

A
  • Ingestion of cigarettes and pesticides
  • CNS overexcitation
  • Tx: Antiepileptic drugs, mechanical ventilation, atropine
64
Q

What are the common causes, symptoms and Tx of cholinesterase inhibitor poisoning?

A
  • 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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