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BPS > Kruse: Intro to drugs of abuse sedative-hypnotics, alcohol > Flashcards

Kruse: Intro to drugs of abuse sedative-hypnotics, alcohol Flashcards

1
Q

What is a sedative

A

-a drug that decreases CNS activity, moderates excitement, and calms the recipient

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2
Q

What is a hypnotic

A

-a drug that produces drowsiness and facilitates the onset and maintenance of sleep and from which the recipient can be aroused easily

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3
Q

Why are benzodiazepines better than barbiturates?

A
  • barbiturates keep going up with the higher dose in CNS effects
  • Barbiturates will plateu
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4
Q

Benzodiazepenes

A
  • Act on GABA a receptors

- cause sedation, hynotic effects, muscle relaxation, anxiolytic and anticonvulsant effects

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5
Q

Barbiturates

A
  • Act on GABAa receptors

- cause a wide spectrum of effects: mild sedation to anesthesia

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6
Q

MOA for Benzos

A
  • bind to GABAa receptors and enhances GABA’s effects

- increased chloride influx, hyperpolarization, decreased number of action potentials

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7
Q

What enzyme will metabolize the benzos

A
  • liver
  • CYP3A4 and glucuronidation (phase 2)
  • cumulative toxicity
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8
Q

What excretes the benzos

A

Kidneys

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9
Q

Barbiturates metabolism

A
  • hepatic
  • excretion via kidney
  • Phenobarbital excreted unchanges
  • elimination half lives long and can lead to toxicity
  • can induce CYP450 enzymes
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10
Q

MOA for Barbiturates

A
  • binds to GABAa receptor

- increases the duration of GABA-gated channel openings

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11
Q

what are benzos used for?

A
  • anxiety sometimes
  • high therapeutic index, antagonist available for overdose
  • risk of dependence, depression of CNS function, amnestic effects, CNS depression when combined with other drugs
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12
Q

Which drugs are good for insomnia

A

-zolpidem, zaleplon, and eszopiclone

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13
Q

Ramelteon

A
  • MOA: agonist at MT1 and MT2 melatonin receptors
  • metabolized by CYP1A2 to active metabolite
  • dont give with fluvoxamine
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14
Q

adverse effects of Ramelteon

A

-dizziness, somnolence, fatigue, and endocrine changes

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15
Q

Buspirone

A

-good for generalized anxiety disorder
-anxiolytic effects may take more than a week to become established
-no sedation
-metabolized by CYP3A4 a lot
-

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16
Q

What do we have to know about alcohol?

A
  • high first pass metabolism by ADH
  • zero order inetics
  • 70kg adult can metabolize 7-10 g of alcohol per hour… one drink
17
Q

What enzyme will give us a hangover if it doesn’t work?

A
  • aldehyde dehydrogenase

- gets rid of acetaldehyde

18
Q

What do we do for acute alcohol intoxication

A
  • monitor respiratory depression and aspiration of vomitus
  • glc can treat metabolic alterations such as hypoglycemia and ketosis
  • thiamine to protect against wernicke-korsakoff syndrome
19
Q

Naltrexone

A
  • tx for alcohol and opiate dependence
  • MOA: mu opiod receptor antagonist
  • reduces craving for alcohol and the rate of relapse to either drinking or alcohol dependence for the short term
  • cant be on opioids before starting this therapy
20
Q

Acamprosate

A
  • MOA: weak NMDA-receptor antagonist and GABAa receptor agonist
  • reduces short-term and long term relapse rates (more than 6 months)
21
Q

Disulfiram

A
  • MOA: irreversibly inhibits aldehyde dehydrogenase and causes extreme discomfort in pts who drink alcoholic beverages
  • pts must be highly motivated
22
Q

What does cocaine and amphetamines do?

A

-keep dopamine concentration high in the synapse

23
Q

What does Alcohol dehydrogenase do?

A
  • metabolizes ethanol into things

- acetaldehyde is the bad one that gives us hangovers

24
Q

What CYP enzyme degrades alcohol?

A
  • CYP2E1

- turns it into Acetaldehyde

25
Q

What is an NMDA receptor

A
  • subtype of glutamate receptor
  • that is the primary excitatory NT in the CNS
  • learning and memory
  • glutamate binds and then a cation channel opends… good for CNS
26
Q

What does alcohol do to the NMDA?

A
  • inhibits the ability of glutamate to open the cation channel of the NMDA receptor
  • leads to and increased depression of the CNS
  • this is why memory loss occurs with alcohol consumption
27
Q

What do we give for acute withdrawal syndrome

A

-benzos

28
Q

What does aldehyde dehydrogenase do?

A

-turns acetaldehyde into other things like formic acid and whatnot

29
Q

With the schedule class thing, what does the numbers 1-4 mean?

A
  • 1 is the most addictive, no medical use

- 4 is the least addictive

30
Q

What is disinhibitio fo DA neurons in the VTA

A
  • inhibition of GABA inhibitory neurons
  • opioids do this
  • THC and other cannabinoids do this
  • and so does gamma hydroxybutyric acid (GHB)

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