Flashcards in Anxiolytics & Hypnotics Deck (49)
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1
Benzodiazepines
Potentiate the effect of GABA at Cl- ion channels
2
Diazepam
-A BZD that is a pos allosteric modulator of GABA A Rs
3
Propranolol
Helps with performance anxiety
4
GABA shunt
Refers to alpha ketoglutarate from the Krebs Cycle, converted to glutamic acid by GABA-transaminase; then subsequently to GABA by glutamic acid decarboxylase (GAD). GABA is then metabolized to form succinic semialdehyde to succinic acid and returns to the Krebs Cycle.
5
Glutamine loop
Glutamine is formed as GABA is transaminated and converted to glutamine. The glutamine is reconverted to glutamate; then decarboxylated by neuronal GAD to GABA
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What do BZD not do themselves?
open the GABA Cl- channel
7
The GABA site of the GABA R is distinct from
the BDZ site and encompasses alpha-1 and beta-2 subunits
8
Flumazenil
BZD antag
9
Barbiturates
-Bind to a distinct subunit combination on the GABA receptor
-At high concentrations can open the channel on their own (without GABA).
10
BZD and hepatic induction
Benzodiazepines do not induce hepatic microsomal enzymes
11
Diazepam uses
anxiety, insomnia, pre-op, muscle relaxant
12
Chlordiazepoxide uses
alcohol detox
13
Flurazepam, Temazepam and Triazolam use
insomnia
14
Clonazepam
-Panic
-Anxiety
-Seizure
15
Alprazolam
-Short acting BZD
-Panic
-Anxiety
-First line treatment for panic disorder withSSRI
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Lorazepam
-Short acting BZD
-Anxiety
-Alcohol related seizure
17
Adverse effects of BDZ
-Sedation
-Tolerance
-Physical dependence
-Self-admin
18
Toxicity of BZD
-Impaired judgment
-Slurred speech
-Incoordination
-Stupor
-Respiratory depression
-Death
19
Non-BDZ
-Anxiolytic
-Buspirone (5-HT1A R partial agonist)
20
First line treatment for all anxiety disorders
SSRI + BZD
--provides early coverage
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Cognitive behavioral therapy (CBT)
Often used in conjunctive with SSRIs for anxiety
22
When do we see severe respiratory depression
When BZD are combined with other sedatives/CNS depressants (like alcohol)
23
GAD first line treatment
SSRI, usually venlafaxine, paroxetine or escitalopram
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Panic disorder first line treatment
SSRI + benzodiazepine for immediate action (alprazolam)
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PTSF (post traumatic stress disorder) first line treatment
SSRI, usually paroxetine or sertraline
26
Which BZD are used for sleep?
Estazolam, flurazepam, quazepam, temazepam, triazolam
27
Which drugs are typically used for sleep?
Eszoiclone, hydroxyzine, zolpidem, zaleplon, ramelteon
28
Describe the adult sleep cycle
Duration of about 90 min; includes NREM and REM sleep
29
Melatonin
produced in the pineal gland at night
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Hypnotics
Produce drowsiness and promote the onset and maintenance of sleep
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What are the symptoms of insomnia?
Difficulty falling asleep, frequent wakenings, poor quality of sleep
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What is sleep deprivation?
Inadequate opportunity for sleep; sleep itself is relatively normal
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What is insomnia disorder?
Insomnia complaint and significant daytime impairment
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Short acting BZDs
Alprazolam, triazolam, lorazepam, oxazepam
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Long acting BZDs
Flurazepam, clorazepate, prazepam
36
Doxepin
-TCA
-low dose mechanism for insomnia is histamine H1
37
Non-BZD GABA A agonists
Eszopiclone, zolpidem, zaleplon
38
Ramelteon
Melatonin agonist for sleep
39
Which drugs are sedating antidepressants
Trazodone, mirtazapine, amyitriptyline
40
Zolpidem advantges
Shorten sleep latency, improve duration, can be used as needed, no negative effect on sleep architecture
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Zolpidem disadvantages
4-6 hr effect, therefore not for middle of the night awakenings, associated with parasomnias
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Traditional BZD disadvantages
Rebound insomnia, memory impairments, loss of coordination, abuse potential, not good for those with respiratory conditions
43
Barbiturates and GABA
Increase duration of channel opening, powerful CNS depression; low margin of safety
44
Diphenhydramine
Benadryl; sedating antihistamine
45
Anxiety, insomnia, pre-op, muscle
-Long acting BZD
-insomnia
46
Temazepam
-BDZ
-insomnia
47
Triazolam
-Short acting BZD
-Insomnia
48
Oxazepam
-Short acting BZD
-Alcohol detox
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