Sedatives And Hypnotics Block III Flashcards
What is a sedative
reduces anxiety and exerts a calming effect with little or no effect on motor or mental function
Hypnotic
produces drowsiness and encourages the onset and maintenance of a state of sleep resembling natural sleep
What are the two major classes of Sedatives
BZD and barbiturates
How are most anxiety DO tx acutely
BZD, Barbiturates, SSRIs
What happens when GABA binds to the GABA receptor
When GABA binds to the GABA receptor it results in relaxation and sedation
Major inhibitor receptor
Cl- channel
Barbiturates are no longer indicated for what sleep DO
Insomina
What are the disadvantages of barbiturates
ability to cause coma in toxic doses, physical dependence, and severe withdrawal symptoms
What is methohexital
A barbituate that is shirt acting and used for anesthesia
C-IV
What is Pentobarbital
Short acting barbiturate that is C-II used for anesthesia
What is secobarbital
A short acting barbituate that is PO only and used for anesthesia
What is amobarbital
A short acting barbituate that is used for anesthesia, C-II
What are the ADE of Barbituates
CNS depression, hangover effect, WTHDRAWL
What are the clinical uses of barbituates
Induction of anesthesia, Status epilepticus, Insomina
What are the severe ADE of barbituates
SJS, bone marrow suppression, hepatotoxicity, osteopenia
What medication can be used for generally every SZR type
Phenobarbital
What are the ADE of phenobarbital
Bradycardia, Sex dysfunction, Drowsiness, cognitive impairment
What are the short acting BZD
T.O.M.
Triazolam
Oxazepam
Midazolam
What are the Intermediate acting BZD
T.E.A.L
Temezepam
Estazolam
Alprazolam
Lorazepam
BZD with long half life’s have more or less hangover and break through S/s
Withdrawal symptoms may be less pronounced
Less breakthrough symptoms
More “hangover” symptoms
BZDs with short half lives have more or less break through s/s
Tolerance of the hypnotic effect develops rapidly
Withdrawal is common (breakthrough symptoms)
What are the clinical uses of BZDs
Anxiolytic (Sedative)
Hypnotic: all benzodiazpines induce sleep if high enough doses are given
Muscle Relaxation
Anticonvulsant
Anesthesia/Amnesic actions
Do BZDs effect pain >?
NO !
Which two BZDs are indicated for alcohol withdrawal
Lorazepam and Diazepam
Which BZD is perferred in liver dz
Lorazepam
What should the BZD treatment period be restricted to
3-4 months
If you must use BZD in the elderly which should be used
LOT
Lorazepam
Oxazepam
Temazepam
What is the reversal agent for BZD
Flumazenil
What is the clinical use of busprione
Management of anxiety disorders or short-term relief of the symptoms of anxiety
Slower onset then BZD, but no abuse potential
Appropriate use is to start patient on BZD then switch while tapering BZD
Often used as a second line agent or when BZD should avoided
What is the MOA and clincal use of Zolpidem
acts on the benzodiazepine receptor by enhancing GABA activity (not chemically related to BZD)
Clinical Use:
Only use is for insomnia
IR for difficulty going to sleep
CR for sleep maintenance issues
What are the advantages of zolpidem to BZD
Less dependence and cravings
Lower risk of tolerance and withdrawal
Lacks respiratory depressant properties
What is the clinical use of Eszopiclone
Sleep initiation and maintenance
What are the ADE of the sleep drug eszopiclone
Metallic taste, SI, abnormal thinking (hallucinations)
Causes functional dependence
What is the MOA and clin use of Zaleplon
acts on BZD receptor, but is chemically not related to BZD
Clinical Use:
Short-term treatment of insomnia
Which of the hypnotics is least likes to causes daytime somnolence
Zaleplon
What is the MOA and Clincal use of Surorexant
Mechanism of Action: orexin-receptor antagonist
Clinical Use: treatment of insomnia