Sedatives And Hypnotic Drugs Dr. Wolff Flashcards
(52 cards)
1
Q
Benzodiazepines that I need to know
A
- Alprazolam
- Clonazepam
- Diazepam
- Lorazepam
- Midazolam
- Temazepam
2
Q
Barbituates that I need to know
A
Pentobarbital
Phenobarbital
Thiopental
3
Q
Non-Benzodiazepine BZ1 Agonist that I need to know
A
Eszopiclone
Zolpidem
4
Q
Benzodiazepine Antagonist
A
Flumazenil
5
Q
Maybe 5-HT Agoinst ? MOA drug used for sedation/hypnosis that I need to know
A
Buspirone
6
Q
Melatonin Agonsit that I need to know
A
Ramelteon
7
Q
Dual Orexin R Antagonist that I need to know
A
Suvorexant
8
Q
Antihistamine that I need to know
A
Doxepin
9
Q
These CNS depressants do what 4 things
A
- Anxiolysis
- Sedation : relax, decrease motor activity with no LOC
- Hypnosis : drowsiness, depressed state of consciousness like sleep, impaired sensory responsiveness easily aroused from
- Anesthesia : unconscious state
10
Q
Transition from sleep to awake, what chemical
A
Melatonin
11
Q
Cl- channel for GABA has bnding sites for what
A
- Bezoodiazepines
- Barbiturates
- Non-selective benzodiazepines
= GABA presses on breaks, these other drugs are break pads helping stop faster
12
Q
Benzodiazodiazepines vs barbiturates
A
- 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) - Also not as addictive (scedule 4 vs scheduele 2)
- Barbiturates increase duration of GABAa
13
Q
Xanax
A
Alprazolam (Benzodiazodiazepines)
14
Q
Low Potency Benzodiazepines with long halflife
A
Diazepam (20-80 hours)
15
Q
Low Potency Benzodiazepines with short halflife
A
Temazepam (10-40hrs)
= amneisa is common side effect, confusion, delusions, abused recreationally
16
Q
High Potency Benzodiazepines with long half life
A
Clonazepam (18-50hrs)
17
Q
High Potency Benzodiazepines short halflife
A
Alprazolam (Xanax)
Lorazepam
Triazolam
18
Q
Flunitrazepam (rohypnol)
A
Not sold legally in US = date rape drug
19
Q
Benzodiazepines
- MOA
- Best for what
- Little effect on what
A
- Increase Cl- channel opening by GABAa stimulation (Indirect)
- Antianxiety , skeletal muscle relaxants, sedative, anti-convulsive , alcohol withdrawal
- Cardiac and lung problems (midazolam is exception ususally when added with opioids)
20
Q
Benzodiazepines that can casues accumulation effect and with multiple doses can cause excessive drowsiness
A
- Diazepam and chlorodiazepoxemide
21
Q
Benzodiazepines side effects are hyper and lower in who, what can happen to rapid stop of usage
A
- Hyper effects in elderly, lower effect in barbiturate and alcohol dependent pts
- Effects REM , so fast stop = rebound insomnia
22
Q
Benzodiazepines Use Disorder SX
A
- Act as drunk
2. Addicted = push family and friends away
23
Q
Diazepam
- MOA and halflife
- Used for
- Side effects
A
- GABAa, 60-72hr
- Anxiety, sedation(usually midazolam), seizures, tremor, alcohol withdrawal, muscel spasms, and for serotonin/hydroxychloroquine/cocaine,meth OD, opiod withdrawal (oral)
- Harmful when used with other benzodiazepines or opiates
24
Q
Alprazolam (Xanax)
- MOA and halflife
- used for
- Side effects
A
- GABAa, 6-27hrs (11hrs)
- Anxiety and panic, general, with depression, short-term (oral)
- Used with other benzodiazepine or opiate can cause death/harm, dependence
25
Other drug then Alprazolam hat has longer halflife and used for anxiety also
Clonazepam and Lorezempam
26
Temazepam
1. MOA and halflife
2. used for
3. Side effects
1. GABAa, 5-18hrs
2. Insomnia (oral)
3. Anterorade amnesia
27
What is also used for insomnia with more anterograde amnesia
Triazolam
28
Midazolam
1. MOA and halflife
2. used for
3. Side effects
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
Non-Benzopiazapine BZ Agonist that has no dependence or tolorance effect
Eszopiclone
30
Zolpidem :
1. MOA and halflife
2. used for
3. Side effects
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
Flumazenil
1. MOA and halflife
2. used for
3. Side effects
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
Phenobarbital use and halflife
Control tonic clonic sezuires
| 1hrs
33
Butablbital use and halflife
Headaches and 35hrs
34
Pentobarbital Use and halflife
Sedative and hypnitic (repleaced by benzodiazepines), 3-8hrs
35
Thiopental use and halflife
15-30min, IV sedation only repleaced by propofol
36
Barbituates onset time and marketed as what and induces what
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
Buspirone
1. MOA and halflife
2. used for
3. Side effects
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
Ramelteon
1. MOA and halflife
2. used for
3. Side effects
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
Suvorexant
1. MOA and halflife
2. used for
3. Side effects
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
Other orexin antagonist not suvorexant
Lemborexant
41
Doxepin
1. MOA and halflife
2. used for
3. Side effects
1. H1 antagonist, inhibits NE and 5-HT reuptake (15hrs)
2. Insomnia maintenance ,major unipolar depression(2weeks)
3. Increase suicide, cns depression
42
Anti-histamines do what
Sedation , DO NOT relieve anxiety
43
H1 receptor
1. Location
2. Drug inhibiting it
1. SM, CNS, endothelial cells (Gq/11)
| 2. Chlorpheniramine (Benadryl)
44
H2 receptor
1. Location
2. Drug inhibiting it
1. GI parietal cells, cardiac muscle, mast cells, CNS (Gs)
| 2. Ranitidine
45
H3 receptor
1. Location
2. Drug inhibiting it
1. CNS, presynaptic (Gi/o)
| 2. Pitolisant
46
Generalized Anxiety Disorder TX
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
Panic Disorder + Agoraphobia TX
1. CBT
2. SSRIs, SNRIs then 2nd SSRI try
3. Benzodiazepines if no substance use past problem (otherwise gabapentin, pregabalin Phenylzine)
48
Phobias TX
1. Exposure therapy
2. CBT
3. Benzodiazepines
49
Social Phobias TX
1. CBT
2. SSRIs, SNRIs (then try 2nd one also)
3. . Benzodiazapines (no Obuse)
4. Busperone
50
Separation Anxiety TX
1. CBT with or without SSRIs****
51
Insomnia TX ONSET vs Maintanence
1. CBT
2. ONSET no benzos= Rameltion, herbal melatonin, amitryptoline, diphenylhydramine)
2. ONSET benzos = Rameltion, eszopiclone / Zalepion / Zolpidem(non-benzos BZ agonist)
3. MANINTAIN or mixed no benzos= DORA (Daridoraxant, Lemborexant, suvorexant), low dose doxepin, amitryptin, gapapentin
3. MAINTAIN or mixed benzos = DORA, non-benzoz BZ agonist
52
How to get someone off benzodiazepman or Z drug(non-benzo BZ)
Tapering off, 6-10 weeks, (pt can go from short-term to long-term benzo)
