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ALL THE PHARM > CNS drugs > Flashcards

CNS drugs Flashcards

1
Q

What are 3 main classes of sedative drugs?

A

Ethanol, benzodiazepines, barbiturates

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2
Q

What is different about the dose-dependent sedation caused by benzodiazepines vs. ethanol and barbiturates?

A

Benzodiazepines - reaches a plateau vs. ethanol and barbiturates - keeps going to coma

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3
Q

What happens as you increase the dose of a sedative drug?

A
  1. Sedation
  2. Anxiolytic
  3. Possible anticonvulsant and muscle-relaxing activity
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4
Q

Where does GABA bind on the GABA-A receptor?

A

Alpha subunit

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5
Q

Where does benzodiazepine bind on the GABA-A receptor?

A

Gamma subunit

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6
Q

Where does barbiturate bind on the GABA-A receptor?

A

Beta subunit

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7
Q

What does stimulation of GABA-A affect?

A

Increased Cl influx - result in membrane hyperpolarization (inhibitory)

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8
Q

How do benzodiazepines work?

A

Increase frequency of Cl channel opening

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9
Q

Does benzodiazepine have a side effect of anterograde or retrograde amnesia?

A

Anterograde

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10
Q

What does flumazenil do?

A

Inhibits BZ1 and BZ2 receptors - reverse the effect of benzodiazepines

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11
Q

Can benzo’s or barbiturates open the GABA channel on their own?

A

Benzo’s - no, barbiturates - yes

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12
Q

How do barbiturates work?

A

Prolong duration of Cl channel opening

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13
Q

What does the liver do to benzodiazepines?

A

Metabolizes them to active forms

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14
Q

What are 3 benzodiazepines that are not metabolized to active forms?

A

Oxazepam, temazepam, lorazepam

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15
Q

Why do we like to use temazepam and oxazepam for sleep disorders?

A

Short half life

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16
Q

What do we like to use benzo’s with long half life (e.g. alprazolam, diazepam, lorazepam) for?

A

Anxiety

17
Q

What is the ultra short acting benzo?

A

Midazolam - used for preop sedation

18
Q

What do we use phenobarbital for?

A

Seizures (especially good for pregnant women)

19
Q

What do we use thiopental for?

A

Induction of anesthesia

20
Q

Are barbiturates P450 inducers or inhibitors?

A

Inducers

21
Q

Why are barbiturates contraindicated in porphyrias?

A

All cytochrome p450 inducers are contraindicated in porphyrias because they induce activity of ALAS - they would lead to further build up of porphyrins

22
Q

Which has the least potential for abuse - benzos, barbs, or ETOH?

A

Benzos < Barbs, EtOH (remember the plateau effect of sedation caused by benzodiazepines)

23
Q

What drug-drug interaction do we worry about with our sedative drugs?

A

Other CNS depressants - anesthetics, antihistamines, opiates, beta blockers

24
Q

What are zolpidem and zalepon?

A

Nonbenzo’s that act on benzo receptors (BZ1) - used in sleep disorders, less effect on cognitive function

25
Q

What acid-base disturbance are alcohols associated with?

A

Metabolic acidosis

26
Q

Why does ethylene glycol cause nephrotoxicity?

A

Eventually metabolized to oxalic acid which makes crystals that damage renal tubules

27
Q

What is the general metabolism of an alcohol?

A

Alcohol –> aldehyde –> acid (all via action of dehydrogenases)

28
Q

What is fomepizole?

A

Long acting inhibitor of alcohol dehydrogenase that is used to treat alcohol overdose

29
Q

Why do alcoholics get thiamine deficiency?

A

The first metabolic product of alcohol is acetaldehyde which combines with both folate and thiamine

30
Q

How does chronic alcoholism affect glucose states?

A

Hypoglycemia from decreased gluconeogenesis (acetic acid - the eventual metabolic product of alcohol makes lots of acetyl coA which can be used for energy)

31
Q

Why do we get lactic acidosis with alcohol?

A

When we make pyruvate from lactate we need to also turn NAD into NADH. With lots of alcohol however, the body also makes lots of NADH to carry that energy. This reverses the reaction so instead we make lactate from pyruvate.

32
Q

Why do chronic alcoholics get gout?

A

Lactate competes with urate for excretion

33
Q

What does disulfiram inhibit?

A

Acetaldehyde dehydrogenase

34
Q

What drugs cause disulfiram like effects?

A

Any drugs with “zole” at the end (e.g. metronidazole, azoles), some cephalosporins, chlorpropamide, griseofulvin

ALL THE PHARM (10 decks)

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