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Neurology > Sedative/Hypnotic/Anxiolytic Drugs > Flashcards

Sedative/Hypnotic/Anxiolytic Drugs Flashcards

1
Q

Benzos, Barbiturates, and alcohols are all CNS _______

A

depressants

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2
Q

In general, physical dependence presents as the _________ of the effects of the drug

A

opposite

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3
Q

Physical dependence of Benzos/Barbs/alcohol presents how?

A

CNS stimulation (then delirium tremens, seizures/status epilepticus)

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4
Q

What is the DOC for withdrawal symptoms from CNS depressants?

A

Lorazepam is best

only option is to re-depress the CNS

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5
Q

Benzos tend to __________ in CNS effects as dose increases, compared to Barbs and alcohol

A

plateau

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6
Q

What is the reason that Benzos are not linear in the dose-dependence curve?

A

they DO NOT exhibit GABAmimetic effects on their own

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7
Q

A patient theoretically has no GABA in their brain. Which drug groups can still cause GABA stimulation?

A

Barbiturates and Alcohols

NOT Benzodiazepines

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8
Q

Compare the ions involved in GABAa vs GABAb receptors

A

a: Cl influx
b: K efflux

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9
Q

Stimulation of which GABA Receptor types involve hyperpolarization of the neuron?

A

BOTH a and b!

only difference is what ion is moving

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10
Q

Hyperpolarization of a neuron will do what to its activity?

A

make it LESS active (harder to hit threshold)

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11
Q

Which GABA receptor is G protein coupled?

A

GABAb

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12
Q

What receptor found in SA and AV nodes is essentially the same thing as GABAb of the CNS?

A

M2 receptor

both G protein coupled, both will cause K efflux

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13
Q

What is the only drug that acts at the GABAb receptor?

A

Baclofen

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14
Q

Describe the structure of the GABAa receptor.

A 
5 subunits (alpha, etc.)
Cl channel in center
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15
Q

GABA binds to the _______ subunit of the GABAa receptor

A

alpha

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16
Q

Benzodiazepines bind to the _________ subunit of the GABAa receptor

A

gamma (has BZ1 and BZ2 varieties)

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17
Q

Barbiturates bind to the _______ subunit of the GABAa receptor

A

beta

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18
Q

What is the term for the way in which Benzos, Barbs, and alcohols interact with the GABAa receptor?

A

Alllosteric modulation

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19
Q

Typically how many GABA molecules are needed to activate a GABAa receptor?

A

2

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20
Q

What is the key phrase to remember for the action of Benzodiazepines?

A

They POTENTIATE GABA

make GABA more potent; less drug for same effect

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21
Q

Benzos will _________ GABA which will increase the _________ of Cl channel opening

A

potentiate

frequency

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22
Q

Benzos will _________ GABA activity, while Barbiturates will _________ GABA activity

A

potentiate

prolong

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23
Q

Benzodiazepine is to increased frequency as Barbiturates is to increased __________

A

duration

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24
Q

The ______ subunit of Benzo binding is associated with Sedative effects, while the ________ subunit of Benzo binding is associated with Antianxiety+Anterograde amnesia

A

BZ 1

BZ 2

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25
Q

Where does the DOC for Benzo toxicity bind?

A

to both the BZ1 and BZ2 sites

Flumazenil

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26
Q

Flumazenil is the DOC for toxicity of the Benzodiazepines and?

A

the Z hypnotics (Zolpidem, Zaleplon, eszopiclone)

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27
Q

Imagine a graph with log dose of GABA on the x and % CNS depression on the y. What will Benzodiazepines do to the GABA/control curve?

A

shift it LEFT

potentiation = need less drug for same effect

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28
Q

While Barbiturates increase duration of Cl channel opening, they also exhibit _________ effects on GABAa

A

GABAmimetic

can open the channel themselves

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29
Q

What specific enzyme in metabolism will be affected by Barbiturates?

A

Complex 1 of the ETC

thus will decrease ATP, stop pumps, cause neuron swelling/death

30
Q

What is the biggest thing to remember for Barbiturate pharmacokinetics?

A

they INDUCE cyp450

31
Q

What are other drugs that exhibit similar effects on p450 as Barbiturates?

A

Phenytoin+Carbamazepine, Rifampin, chronic EtOH, chronic CXS

32
Q

When you induce an enzyme (ex: p450), you increase the ____ of the enzyme. Does this increase the Km or Vmax?

A

increase # of enzyme

higher Vmax

33
Q

Inducers of enzymes will do what to a line on a Lineweaver Burke plot?

A

same x inercept

lower y intercept (due to higher v max)

34
Q

Inducers of cyp450 are all contraindicated in what group of conditions?

A

Porphyrias

35
Q

Describe the relationship of Barbiturates with porphyrias

A

cyp450 enzymes have heme groups

therefore, Barbs will induce cyp450 AND heme enzymes/pathway

this causes MORE buildup of precursors in porphyria pt

36
Q

What is the rate limiting enzyme of the heme synthesis pathway?

A

D-ALA synthase (the 1st one)

37
Q

Benzos all end in ________, while all Barbiturates end in __________

A
  • azolam or -azopam

- barbital or -pental

38
Q

What is the most key aspect of Benzodiazepine pharmacokinetics?

A

they are often broken down to ACTIVE metabolites

39
Q

What benzodiazepines are not broken down to active metabolites?

A

Oxazepam, Temazepam (short lives)

Lorazepam (long life)

40
Q

What Benzos are good for insomnia and why?

A

Oxazepam and Temazepam

no active metabolites + short acting

41
Q

The shortest Benzo is ______ and the shortest Barb is _________

A

Midazolam

Thoipental

42
Q

What are the 3 Benzos best suited for Anxiety and why?

A

Lorazepam, Alprazolam, Diazepam

long half lives + last two have active metabolites

43
Q

What is the MOA of the Z hypnotics?

A

BZ1 agonists

44
Q

What are the Z hypnotics?

A

Zolpidem, Zalepon, Eszopiclone

45
Q

How do alcohols exert their CNS depressing effects?

A

GABAmimetic

46
Q

What are the 2 common side effects for all alcohol toxicities?

A

CNS depression

metabolic acidosis

47
Q

What is the alcohol to think of with suicides and/or children?

A

Ethylene glycol

48
Q

What is the alcohol to think of with moonshine or wood?

A

Methanol

49
Q

What is the metabolic progression of the alcohol in antifreeze?

A

ethylene glycol - glycoaldehyde - Oxalic acid

50
Q

What is the alcohol that directly causes ATN?

A

ethylene glycol

51
Q

What is the alcohol that directly causes Ocular damage?

A

Methanol

52
Q

What is the cause of ATN/acute renal failure in pts who drink ethylene glycol?

A

sharp oxalic acid crystals

53
Q

What are the big 3 toxicities of ethylene glycol?

A

CNS depression
metabolic acidosis
Nephrotoxicity

54
Q

What are the big 3 toxicities of methanol?

A

CNS depression
metabolic acidosis (wide anion gap)
Ocular damage/blindness

55
Q

What drug is used to inhibit the enzyme responsible for both steps of methanol+ethylene glycol metabolism?

A

Fomepizole

56
Q

What is the alcohol metabolite responsible for ocular damage?

A

Formic acid

methanol

57
Q

What are the 2 metabolic products of Ethanol?

A

Acetaldehyde

Acetic Acid

58
Q

Describe how ethanol can be used as calories.

A

acetic acid is a metabolite
it comobines with CoA to make acetyl CoA
7 kcal/g

59
Q

Methanol uses the enzyme _________ for metabolism, while ethanol uses __________?

A

alcohol dehydrogenase (both steps)

alcohol dehydrogenase, then acetaldehyde dehydrogenase

60
Q

What drug inhibits the second step in ethanol metabolism?

A

Disulfiram

61
Q

What are the specific toxicities that come with acetaldehyde?

A

hangover (N/V, Mallory Weiss, Booerhaave)
vasodilation+hypotension
inactivates Folate
decreases Thiamine availability

62
Q

What two organs show the most pathology after an acute ethanol intoxication?

A

Liver steatosis, Mallory bodies

Pancreatitis

63
Q

Pt presents after binge drinking with stabbing epigastric pain that radiates to the back. He’s in shock and has DIC. Dx?

A

acute pancreatitis

64
Q

What metabolic pathway is essentially reversed in chronic alcoholics?

A

gluconeogenesis

65
Q

What are the manifestations of thiamine deficiency in alcoholics?

A

beriberi, Wernicke Korsakoff
also risk for dilated cardiomyopathy
metabolic pathways need thiamine too!

66
Q

What type of liver necrosis is seen in chronic alcoholics?

A

centrilobular

67
Q

What 2 malignancies are associated with chronic alcoholism?

A

squamous cell CA of the esophagus

signet ring/diffuse stomach cancer

68
Q

A drug that exhibits disulfiram-like effects does what?

A

makes ya get drunk/sick faster

69
Q

What drugs exhibit disulfiram like effects?

A

any azole drug

METRONIDAZOLE is #1

70
Q

What is the antidote for Barbiturate toxicity?

A

nothing

Neurology (4 decks)

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