Sedatives And Hypnotic Drugs Dr. Wolff Flashcards

1
Q

Benzodiazepines that I need to know

A
  1. Alprazolam
  2. Clonazepam
  3. Diazepam
  4. Lorazepam
  5. Midazolam
  6. Temazepam
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2
Q

Barbituates that I need to know

A

Pentobarbital
Phenobarbital
Thiopental

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3
Q

Non-Benzodiazepine BZ1 Agonist that I need to know

A

Eszopiclone

Zolpidem

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4
Q

Benzodiazepine Antagonist

A

Flumazenil

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5
Q

Maybe 5-HT Agoinst ? MOA drug used for sedation/hypnosis that I need to know

A

Buspirone

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6
Q

Melatonin Agonsit that I need to know

A

Ramelteon

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7
Q

Dual Orexin R Antagonist that I need to know

A

Suvorexant

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8
Q

Antihistamine that I need to know

A

Doxepin

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9
Q

These CNS depressants do what 4 things

A
  1. Anxiolysis
  2. Sedation : relax, decrease motor activity with no LOC
  3. Hypnosis : drowsiness, depressed state of consciousness like sleep, impaired sensory responsiveness easily aroused from
  4. Anesthesia : unconscious state
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10
Q

Transition from sleep to awake, what chemical

A

Melatonin

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11
Q

Cl- channel for GABA has bnding sites for what

A
  1. Bezoodiazepines
  2. Barbiturates
  3. Non-selective benzodiazepines
    = GABA presses on breaks, these other drugs are break pads helping stop faster
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12
Q

Benzodiazodiazepines vs barbiturates

A
  1. Benzodiazodiazepines platau at a certain level not leading to coma, like the barbiturates
    = stop at anesthesia (anxiolysis, anti-convulsion, sedation——> Hypnosis ——> Anesthesia ——> Meduallary depression ——> coma)
  2. Also not as addictive (scedule 4 vs scheduele 2)
  3. Barbiturates increase duration of GABAa
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13
Q

Xanax

A

Alprazolam (Benzodiazodiazepines)

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14
Q

Low Potency Benzodiazepines with long halflife

A

Diazepam (20-80 hours)

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15
Q

Low Potency Benzodiazepines with short halflife

A

Temazepam (10-40hrs)

= amneisa is common side effect, confusion, delusions, abused recreationally

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16
Q

High Potency Benzodiazepines with long half life

A

Clonazepam (18-50hrs)

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17
Q

High Potency Benzodiazepines short halflife

A

Alprazolam (Xanax)
Lorazepam
Triazolam

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18
Q

Flunitrazepam (rohypnol)

A

Not sold legally in US = date rape drug

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19
Q

Benzodiazepines

  1. MOA
  2. Best for what
  3. Little effect on what
A
  1. Increase Cl- channel opening by GABAa stimulation (Indirect)
  2. Antianxiety , skeletal muscle relaxants, sedative, anti-convulsive , alcohol withdrawal
  3. Cardiac and lung problems (midazolam is exception ususally when added with opioids)
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20
Q

Benzodiazepines that can casues accumulation effect and with multiple doses can cause excessive drowsiness

A
  1. Diazepam and chlorodiazepoxemide
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21
Q

Benzodiazepines side effects are hyper and lower in who, what can happen to rapid stop of usage

A
  1. Hyper effects in elderly, lower effect in barbiturate and alcohol dependent pts
  2. Effects REM , so fast stop = rebound insomnia
22
Q

Benzodiazepines Use Disorder SX

A
  1. Act as drunk

2. Addicted = push family and friends away

23
Q

Diazepam

  1. MOA and halflife
  2. Used for
  3. Side effects
A
  1. GABAa, 60-72hr
  2. Anxiety, sedation(usually midazolam), seizures, tremor, alcohol withdrawal, muscel spasms, and for serotonin/hydroxychloroquine/cocaine,meth OD, opiod withdrawal (oral)
  3. Harmful when used with other benzodiazepines or opiates
24
Q

Alprazolam (Xanax)

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. GABAa, 6-27hrs (11hrs)
  2. Anxiety and panic, general, with depression, short-term (oral)
  3. Used with other benzodiazepine or opiate can cause death/harm, dependence
25
Q

Other drug then Alprazolam hat has longer halflife and used for anxiety also

A

Clonazepam and Lorezempam

26
Q

Temazepam

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. GABAa, 5-18hrs
  2. Insomnia (oral)
  3. Anterorade amnesia
27
Q

What is also used for insomnia with more anterograde amnesia

A

Triazolam

28
Q

Midazolam

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. GABAa, 1-4hr
  2. Preoperative sedation (scoping or prcedures), general anesthesia, anxiolysis (IV or IM watere then lipid soluable)
  3. IV use needs to be monitored for depression in resp
29
Q

Non-Benzopiazapine BZ Agonist that has no dependence or tolorance effect

A

Eszopiclone

30
Q

Zolpidem :

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. Binds to BZ1 a group of GABAa, 2hrs (LONGEST HALFLIFE), a non-benzodiazepine BZ agonist
  2. insomnia, safe in preg, NOT anxiolytic, (IR, sublingual, spray)
  3. Sleep behaviors (walking, driving, eating, talking)
31
Q

Flumazenil

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. Benzodiazepine Antagoinist on GABA**, and zolpidem antaggonist (1-2min)
  2. Benzodiazepine OD or reversal (1-2min), (IV)
  3. Seizures, esp if treated with TCAs or long term sedation pts = WATCHFUL waiting if pt is stabilized
32
Q

Phenobarbital use and halflife

A

Control tonic clonic sezuires

1hrs

33
Q

Butablbital use and halflife

A

Headaches and 35hrs

34
Q

Pentobarbital Use and halflife

A

Sedative and hypnitic (repleaced by benzodiazepines), 3-8hrs

35
Q

Thiopental use and halflife

A

15-30min, IV sedation only repleaced by propofol

36
Q

Barbituates onset time and marketed as what and induces what

A
  1. More lipid soluable the faster it goes to brain and starts effects
  2. Sodium Salts
  3. CYP3A4, dont use with some drugs and definetly not alcohol, schedule 2 drug like opioids, HIGH withdrawal
37
Q

Buspirone

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. Nonbenzodiazepine Anxiolytic, partion 5-HT AGONIST, short halflife
  2. Anxiety, help antidepressant (oral), however takes 1-2 weeks to give response
  3. NO tolotance or withdrawal , tachy, NO sedation, little psychomotor impariment, no augmentation with alcohol or other depressant use**
38
Q

Ramelteon

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. MT1 and MT2 receptor agonist (stimulate melatonin)
  2. Fast sleep for insomina falling aleep (no withdrawal) (oral), not very efficient (less then 50% feel effect)
  3. Fluvoxamine interations
39
Q

Suvorexant

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. Blocks orexant (Neuropeptide promoting wakeness), 12hrs
  2. Insomina,
  3. day driving impairment, complex sleep behaviors can happen (not used or prefered by many(
40
Q

Other orexin antagonist not suvorexant

A

Lemborexant

41
Q

Doxepin

  1. MOA and halflife
  2. used for
  3. Side effects
A
  1. H1 antagonist, inhibits NE and 5-HT reuptake (15hrs)
  2. Insomnia maintenance ,major unipolar depression(2weeks)
  3. Increase suicide, cns depression
42
Q

Anti-histamines do what

A

Sedation , DO NOT relieve anxiety

43
Q

H1 receptor

  1. Location
  2. Drug inhibiting it
A
  1. SM, CNS, endothelial cells (Gq/11)

2. Chlorpheniramine (Benadryl)

44
Q

H2 receptor

  1. Location
  2. Drug inhibiting it
A
  1. GI parietal cells, cardiac muscle, mast cells, CNS (Gs)

2. Ranitidine

45
Q

H3 receptor

  1. Location
  2. Drug inhibiting it
A
  1. CNS, presynaptic (Gi/o)

2. Pitolisant

46
Q

Generalized Anxiety Disorder TX

A
  1. CBT
  2. SSRIs, SNRIs
  3. Buspirone
  4. Pregabalin
  5. Benzodiazepine (if pt has no drug misuse PMH), or ACUTE before SSRI/SNRI effect comes which takes 2 weeks
47
Q

Panic Disorder + Agoraphobia TX

A
  1. CBT
  2. SSRIs, SNRIs then 2nd SSRI try
  3. Benzodiazepines if no substance use past problem (otherwise gabapentin, pregabalin Phenylzine)
48
Q

Phobias TX

A
  1. Exposure therapy
  2. CBT
  3. Benzodiazepines
49
Q

Social Phobias TX

A
  1. CBT
  2. SSRIs, SNRIs (then try 2nd one also)
  3. . Benzodiazapines (no Obuse)
  4. Busperone
50
Q

Separation Anxiety TX

A
  1. CBT with or without SSRIs**
51
Q

Insomnia TX ONSET vs Maintanence

A
  1. CBT
  2. ONSET no benzos= Rameltion, herbal melatonin, amitryptoline, diphenylhydramine)
  3. ONSET benzos = Rameltion, eszopiclone / Zalepion / Zolpidem(non-benzos BZ agonist)
  4. MANINTAIN or mixed no benzos= DORA (Daridoraxant, Lemborexant, suvorexant), low dose doxepin, amitryptin, gapapentin
  5. MAINTAIN or mixed benzos = DORA, non-benzoz BZ agonist
52
Q

How to get someone off benzodiazepman or Z drug(non-benzo BZ)

A

Tapering off, 6-10 weeks, (pt can go from short-term to long-term benzo)