Kruse- Intro to Drugs of Abuse Sedative-Hypnotics Alcohol Flashcards

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1
Q

Sedatives do what?

A

-decrease CNS activity, moderate excitement, and calms the recipient

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2
Q

Hypnotics do what?

A

-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

Where/How do Benzodiazpines work?

A
  • Act on ligand gated ion channels aka GABAa receptors
  • cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects
  • makes receptor more active in lower concentrations of GABA
  • so you need BOTH a BENZO and GABA receptor presents
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4
Q

Where/How do Barbiturates work?

A
  • Act on GABAa receptors
  • cause a wide spectrum of effects: mild sedation to anesthesia
  • Keep receptor open for longer period of time
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5
Q

Where do Benzodiazepines distribute?

A

-CNS, Placenta, and Breast-milk

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6
Q

How are Benzodiazepines processed?

A
  • CYP34A phase 1

- Glucuridation phase 2

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7
Q

Do Benzodiazepines have a risk of dependence and tolerance?

A

-yes

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8
Q

Benzodiazepines examples?

A
  • Diazepam (Valium)
  • alprazolam (Xanax)
  • lorazepam (Ativan)
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9
Q

Half life and onset of Chlordiazepoxide? active metabolites?

A
  • greater than 100 hours
  • intermediate onset
  • yes
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10
Q

Half life and onset of Diazepam? Active metabolites?

A
  • greater than 100 hours
  • very fast
  • yes
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11
Q

Half life and onset of Oxazepam? Active metabolites?

A
  • 5-14 hours
  • Slow
  • none
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12
Q

Half life and onset Lorazepam? Active metabolites?

A
  • 10-20 hours
  • intermediate
  • none
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13
Q

Use of Midazolam?

A
  • rapid on and rapid off

- dentists use this to induce anesthesia or in other quick surgery settings

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14
Q

Intermediate to lond acting Benzodiazepines are?

A
  • Diazepam
  • Lorazepam
  • Clonozepam
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15
Q

Short acting benzodiazepines are?

A
  • Midazolam
  • Oxazepam
  • Alprazolam
  • Temazepam
  • Triazolam
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16
Q

How do Barbiturates work?
What are examples?
risk of dependence and tolerance?

A
  • binding to GABA a receptor and increase duration of time the channel is actually open
  • —“arbitals”
  • yes, risk of both but not all people have risk or dependence. all people build tolerance
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17
Q

How do Benzodiazepines work?

A

-Causes GABA receptors to be activated at lower concentrations

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18
Q

Barbiturates are mostly used for what? examples?

A

-sleep aids
-Eszopiclone
-Zolpidem
-Zaleplon
“Sleep Ezzy with barbiurates”

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19
Q

Sedative-hypnotics are used to treat what?

A

-anxiety, insomnia, epilepsy, siezures, control withdrawals

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20
Q

Benzo Drugs to treat anxiety?
How high is the theraputic index? What is the antagonist (antidote) to overdose?

What are the disadvantages?

A
  • Clonazepam
  • Lorazepam
  • Alprazolam
  • Diazepam
  • high
  • Flumazenil treats OD

-disadvantages are dependence risk, CNS depression, SSRIs are preferred for these reasons

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21
Q

Benzo drugs used for insomnia? side effect?

A

-Eszopiclone (long half life)
-Zolpidem (2 sustain sleep)
-Zaleplon (both Zol and Zal act rapidly)
EZZy Sleep

-sleep shopping and sleep driving

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22
Q

Ramelteon is used to treat what?
MOA?
bioavailability?
Metabolized by?

A
  • insomnia
  • agonist at MT1 and MT 2 melatonin receptors
  • low bioavailability
  • CYP1A2
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23
Q
Buspirone is used to treat what?
how long to take affect?
Does it cause sedation, hypnotic, euphoric, etc?
MOA?
Metabolized for?
A
  • general anxiety
  • takes a full week
  • no it does not
  • unknown
  • CYP3A4
24
Q

What is responsible for breaking down alcohol?

How high is it’s first pass?

How much metabolized per hour?

A
  • alcohol dehydrogenase (ADH)
  • alcohol had zero order kinetics meaning as soon as you start drinking all the enzymes used in its biotransformation are maxed out
  • 7-10gs per hour should take 1 drink per hour
25
Q

What causes hangovers?
pathway?
why are fewer asains alcoholics?

A
  • acetaldehyde build up
  • alcohol–> acetaldehyde–>acetic acid
  • higher concentration of people with polymorphisms of alcohol dehydrogenase
26
Q

What is the primary excitatory NT in the CNS?
what does alcohol do to it?
whats the major inhibitor in the CNS?

A
  • NMDA glutamate receptors
  • alcohol inhibits this
  • GABA receptor
27
Q

what is acute alcohol intoxication? what should you do?

A
  • drunk person
  • monitor breathing and inhaling of vomit
  • treat w/ glucose and thiamine to prevent korsakoff syndrome
28
Q

what is chronic alcohol abuse?

how to treat?

A
  • alcoholics

- avoid withdrawal symptoms w/ BENZOs

29
Q

what are withdrawal symptoms?

A

-seizures, delirium, and arrhythmias

30
Q

what treatment does alcohol dependence require?

A

-psycosocial therapy first and drugs second

31
Q

what drugs for alcoholism?

A

-Naltrexone

32
Q

What is Naltrexone?
what is it used for?
MOA?
what must patients be before starting therapy?

A
  • treatment of alcohol/opiate dependence and reduces craving
  • mu opioid receptor antagonist (long-acting)
  • patients must be alcohol and opioid free b/c if not you trigger alcohol withdrawal syndrome
33
Q

What is Acamprosate?

MOA?

A
  • treat alcohol/opiate
  • weak NMDA antagonist and GABA receptor agonist mimicking the effects of alcohol in the body
  • reduces relapse rates
34
Q

What is Disulfiram?

MOA?

what must the patient be?

A
  • for alcohol dependence
  • irreversibly inhibits aldehyde dehydrogenase causing build up of acetaldehyde
  • makes people feel shitty when they drink
  • the patient must be highly compliant because they could easily just not take the pill
35
Q

What are ethanol and Fomepizole used to treat?
What is the toxic build up?
MOA?

A
  • methanol OD seen with antifreeze, windshield washer fluid,
  • formaldehyde
  • ADH has higher affinity for ethanol than it does for methanol. allowing methanol to be cleared form the body unchanged
36
Q

Do schedule 1 drugs have medical use?
addictive?
examples?

A
  • no
  • strong opioids
  • highest addictive
  • rohypnol (date rape) Heroin, PCP, MDMA, LSD
37
Q

Schedule 4 drugs use?
addictive?
examples

A
  • medical use
  • least addictive
  • BENZOs and weak opioids
38
Q

Are phencyclidine and ketamine addictive?

A

-no that are rated a 1 on his chart meaning they are not addictive

39
Q

What receptors do addictive drugs commonly target?

A

-activate GPCRs

ie opiates, weed, GHB, LSD

40
Q

BENZOs, Nicotine, and alcohol bind to what receptors?

A

-ionotropic receptors and ion channels

41
Q

Are LSD, psilocybin, PCP., and mescaline addictive?

A

-no

42
Q

Long term effects of:
PCP?
LSD?

A

PCP= irreversible schizophrenia pshchosis

LSD= flashbacks and altered perception

43
Q

The Opioids— Naloxone, Naltrexone, and Methadone— inhibit what?

A

-inhibition of GABA inhibitory neurons

44
Q

Which of these acts longer?

Naloxone vs Naltrexone

A

-Naltrexone is the long acting antagonist

45
Q

Is Methadone a long acting antagonist or agonist?

A

-agonist

46
Q

Agitation, HTN, tachycardia, delusions, hallucinations, death, hyperthermia…….What did the patient OD on?

A

-Amphetamines and cocaine

47
Q

Slurred speech, drunk behavior, dilated pupils, clammy skin, coma, weak rapid pulse…..what did the patient OD on?

A

-Barbiturates, BENZOs, alcohol

48
Q

constricted pupils, clammy skin, nausea, drowsiness, respiratory depression, coma, death…..what did the patient OD on?

A

-Heroin or other opioids

49
Q

apathy, irritable, more sleep, disorientation, depression…..what are they withdrawaling from?

A

-Amphetamines and cocaine

50
Q

anxiety, insomnia, delirium, tremors, seizures……what are thy withdrawaling from?

A

-Barbiturates, BENZOs, alcohol

51
Q

Nausea, chills, cramps, lacrimation, rhinorrhea, yawning, hyperpnea, tremor….what are they withdrawaling from?

A

-Heroin and other opioids

52
Q

What are the only two conjugated BENZOs?

A
  • Oxazepam (slow and short acting)

- Lorazepam (intermediate and long acting)

53
Q

T/F: GABA neurons synapsing on dopamine neurons can shut off the dopamine neurons?

A

-True

54
Q

Cocaine blocks

A

-reuptake of dopamine

= more dopamine in the synapse

55
Q

Amphetamines works by

A

-fill up the vesicles keeping dopamine out of the vesicles causing cytoplasmic reverse of dopamine transporter leading to dopamine being pump against its gradient
=more dopamine in the synapse

56
Q

What’s a good BENZO to give an addict in order to avoid the dopamine reward pathway?

A

Oxazepam works because it has a slow onset