L17: Sedative-Hypnotics Flashcards
Alprazolam, Diazepam, Lorazepam, and Lidazolam all belong to which drug class?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines
E. Benzodiazepines
Zolpidem, Eszopiclone, and Suvorexant all belong to which drug class?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines
C. Sleep Aids
What drug class does Flumazenil belong to?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines
A. GABA Antagonists
Both Phenobarbital and Methohexital belong to which drug class?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines
D. Barbituates
Which drug class do Baclofen, Tizanadine, and Cyclobenzaprine belong to?
A. GABA Antagonists
B. Centrally Acting Muscle Relaxants
C. Sleep Aids
D. Barbituates
E. Benzodiazepines
B. Centrally Acting Muscle Relaxants
True or False: azolam’s have a SHORTER half life compared to azepams’s
True
True or False: Suvorexant is an orexant antagonist
True
All of these act on GABA-R, except which two?
Melantonin
Suvorexant
True or False: Promethazine and Hydroxazine act on histamine receptor
True
____: short acting benzo
____: intermediate acting benzo
____: long acting benzo
Triazolam
Alprazolam
Flurazepam
____: ultra-short acting barbituate
____: short acting barbituate
____: long acting barbituate
Thiopental
Secobarbital
Phenobarbital
Which is safer: Benzos or Barbituates?
Benzos
-Barbituates can lead to medullary depression, coma, etc
GABA binds to GABA-A receptors, which cause __ channels to __
A. Na; close
B. Cl; close
C. Cl; open
D. Na; open
C. Cl; open
- Influx of Cl- into the cell hyper-polarizes the cell , leading to decreased neuronal firing
True or False: Barbituates can act without GABA present
True
Which three drugs bind to the alpha subunit of GABA only?
- Flumazenil
- Zolpidem
- Benzodiazepines
True or False: Zolpidem is less effective at treating anxiety. However, less apt to cause tolerance or dependence!
True
True or False: Barbituates bind to alpha and beta subunits
True
What makes barbituates so dangerous?
- Do not require GABA binding
- Opens Cl- channel for longer, without GABA regulation
If a patient overdoses on a Benzodiazepine or Zolpidem, which drug can be given to reverse the effects?
Flumazenil
Shorter acting drugs, such as ____ and ___ have triazole ring
Triazolam and Alprazolam
- aka: azolams
What are four therapeutic effects of benzos?
- Sedative
- Hypnotic
- Anti-convulsant
- Muscle relaxant
How do the -azolams and -azepams work?
A. antagonist at benzodiazepine sites on GABA-A
B. binds to GABA-A receptor subunits, facilitates Cl- channel opening
B. binds to GABA-A receptor subunits, facilitates Cl- channel opening
- membrane hyperpolarization
What can the -azolams and
-azepams be used to treat?
- Acute anxiety states
- Panic attacks
- Insomnia
All of the -azolams and -azepams have hepatic metabolism, except which two (have OH group)?
Oxazepam and Lorazepam
- these drugs are better choice for someone with decreased liver function
True or False: Taking ETOH with benzos (-azolams and -azepams) results in an additive effect
True
True or False: Tolerance and dependence can result with use of benzodiazepines (-azolams and -azepams)
True
_____: antagonist at benzodiazepine sites on GABA-A receptor, used to manage benzodiazepine overdose
Flumazenil
Which drugs are most long acting?
Diazepam and Chlorazepate
Which receptor is associated with wakefulness, food intake, and energy/glucose metabolism?
Which is associated with circadian, energy balance, and insulin secretion?
1) Orexin
2) Melatonin
Benzodiazepines affect sleep by decreasing ___, duration of of stages _ and _, and number of ____
sleep latency; stages 3 and 4; number of awakenings
True or False: Benzos decrease duration in REM, but not as much as barbituates do
True
REM Rebound is commonly associated with abrupt cessation of which drug class?
A. Anti-histamines
B. Sedatives
C. Benzos
D. Barbituates
C. Benzos
- characterized by: increased frequency and intensity of dreams
How the sedative-hypnotics, Zolpidem and Eszopiclone, act? What do they treat?
A. Agonist at melatonin receptor
B. Enhance GABA effects
C. Inhibit orexin 1 and 2
B. Enhance GABA effects
Treats: insomnia
True or False: Hypotension is associated with use of Zolpidem and Eszopiclone
True
____: A schedule IV controlled substance that inhibits orexin 1 and 2 receptors
A. Diazepam
B. Chlorazepate
C. Suvorexant
C. Suvorexant
True or False: Suvorexant is associated with daytime somnolence, worsening depression, and SI
True
How does Suvorexant work?
Decreases sleep latency
Enhances sleep maintenance
True or False: The barbituates thiopental and thiamylal have longer half lives
False - shorter
- Presence of sulfur decreases their solubility and duration of action
What is the barbituate methohexital used for? phenobarbital?
Anesthesia
Seizure
True or False: Barbituates have extension CNS effects, may lead to tolerance and dependence
True
True or False: Lipid solubility allows benzodiazepines to readily cross BBB
False - this is the case with barbituates
True or False: Redistribution is important for termination of action of US acting barbituates (e.g thiopental)
True
What are three unique side effects of barbituates?
- Allergic reactions
- Aggravation of acute intermittent porphyria
- Respiratory depression - no cure
- Withdrawal syndrome
Barbituates and DDI?
- Additive effect with CNS depressants
- MAO Inhibitors enhance CNS depression
- Induction of hepatic enzymes
____ and ____ are histamine H2 receptor inverse agonists
Hydroxyzine and Promethazine
True or False: Barbituate use can make warfarin less effective
True
____ is a competitive antagonist of beta-1 adrenergic receptor in the heart that is used for situational anxiety
Propranolol
- has extensive 1st pass met
___: facilitates GABA and is used to treat muscle spasms. Redistribution is important for its termination. However, is can lead to withdrawal syndrome.
A. Cyclobenzaprine
B. Tizanidine
C. Baclofen
D. Diazepam
D. Diazepam
____ is a GABA-B receptor agonist used to treat spasticity associated with MS – can cause CNS depression/dependency
A. Cyclobenzaprine
B. Tizanidine
C. Baclofen
D. Diazepam
C. Baclofen
____ is used to treat muscle spasms of local origin and inhibits both gamma and alpha motor systems
A. Cyclobenzaprine
B. Tizanidine
C. Baclofen
D. Diazepam
A. Cyclobenzaprine
____ is an alpha 2 adrenergic agonist used to relax skeletal muscles – can result in hypotension
A. Cyclobenzaprine
B. Tizanidine
C. Baclofen
D. Diazepam
B. Tizanidine
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