Pharmacology Kruse Flashcards

1
Q

what is the enzyme that catalyzes choline transport? also what reaction does it catalyze?

what kind of patients have reduced production of this enzyme?

A
Choline acetyltransferase (ChAT)
AcCoA + choline --> ACh

Alzheimer’s patients

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2
Q

what is the molecule involved in ACh storage?

A

ACh vesicular transporter

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3
Q

What kind of channels open during ACh release?

what facilitates vesicle-plasma membrane fusion?

A

Voltage-gated Ca2+

VAMP(synaptobrevin) and SNAP

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4
Q

what enzyme destroys ACh—> choline and acetate?

A

AChE

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5
Q

what are the 4 steps in junctional transmission?

A

ACh synthesis
storage
release
destruction

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6
Q

where are nAChR receptors located?

what are the agonists?

what kind of receptor?

A

skeletal m.

ACh and nicotine

ligand-gated

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7
Q

where are mAChR receptors located?

what type?

Agonists?

function?

A

smooth and cardiac m.

GPCR

ACh and Muscarine

for cardiac m. - DEC HR, conduction velocity, contraction

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8
Q

what do the fastest synaptic events in the nervous system use?

A

nAChRs (miliseconds)

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9
Q

what amino acids line the nAChR pores?

what charge do they have?

A

glutamic and aspartic acid

negative

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10
Q

what are the nAChR antagonists?

A

VAPiD

Vecuronium
Atracurium
Pancuronium
d-turbocurarine

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11
Q

what are the Nm subunits?

where are they found?

A

a,b,d,e,g

skeletal m. motor end plates

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12
Q

what are the Nn subunits?

where are they found?

A

a and b OR all a

CNS, autonomic ganglia, adrenal medulla

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13
Q

what is tetrodotoxin?

MOA?

symptoms?

A

puffer fish poison

inhibits VG-Na+ channels and blocks axonal conductance

weakness, dizziness, paralysis

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14
Q

what is the MOA for local anesthetics?

examples of some?

A

inhibition of VG-Na+ channels, inhibits axonal conductance

lidocaine, bupivacaine, procaine

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15
Q

what is Batrachotoxin?

what does it cause?

A

poison dart frog

INC in permeability of Na+ channels, persistent depolarization

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16
Q

what causes Botulism?

where is it found?

MOA?

A

Clostridium botulinum

veggies, fruit, seafood, soil

cleaves SNARE complex involved in exocytosis, prevents ACh release

17
Q

what toxin targets synaptobrevin (VAMP)?

A

Tetanus

Botulinum B, D, F, G

18
Q

what toxin targets Syntaxin?

A

Botulinum C1

19
Q

what toxin targets SNAP-25

A

Botulinum A/E

20
Q

how is botulism classically described?

what are the symptoms of foodborne botulism?

A

acute onset of bilateral cranial neuropathies, symmetric weakness, blurred vision

nausea, ab pain, diarrhea

21
Q

what are the clinical uses for botulinum?

A

face wrinkles, prevention of migraine headaches

22
Q

what causes tetanus?

MOA?

symptoms?

A

Clostridium tetani found in soil

blocks SNARE by targeting synaptobrevin

spastic paralysis, lock jaw, stiff neck, tachycardia, sweating, restlessness

23
Q

what is the protypical curare alkaloid?

MOA?

clinical use?

destruction of drug?

A

d-tubocurarine (antagonist)
competes with ACh for nAChR on motor end plate, dec. EPP size (it is a NONdepolarizing nAChR comp)

anesthesia to relax skeletal m.

increase ACh in the NMJ

24
Q

what is succinylcholine?

MOA?

how is it reversed?

A

agonist that causes muscle fasciculations

depol neurom. blocker that binds to nAChRs and initially causes depol and continued depol which leads to receptor blockade and paralysis

TIME

25
Q

what is succinylcholine used for?

A

induction agent for anesthesia

26
Q

what do cholinesterase inhibitors do?

clinical uses?

A

bind AChE and block its enzymatic activity thus INC [ACh] at NMJ

dementia, Alzheimer’s, MYASTHENIA GRAVIS, reverse neurom. blockade during anesthesia

27
Q

what does tetrodotoxin do?

A

blocks outer mouth of Na+ channels and inhibits APs

28
Q

what does Dantrolene do?

clinical uses?

A

inhibits ryanodine receptors in SR, blocks Ca2+ release

malignant hyperthermia and spasticity

29
Q

what is synaptotagmin?

A

Ca2+ sensor that detects a rise in intracellular Ca2+ and triggers membrane fusion and exocytosis