Anxiolytic-sedative-hypnotic Drugs (Slattery) Flashcards
Sedative-Hypnotic drug goals?
- Relief of anxiety
- Able to cause sedation
- Able to encourage sleep
anxiolytic?
Patient is related; unconcerned with surroundings but fully functional
sedative?
dec. activity; calms patient although awake
hypnotic?
make drowsy and facilitate the onset and maintenance of sleep; may be easily aroused
general anesthesia?
loss of consciousness and the patient can not be aroused
What is a linear slope drug?
inc. doses leads to greater effects with linear relationship; “Barbiturates”
What is a nonlinear slop drug?
inc. doses does not directly correlate with inc. in drug effects, requires more drug to get proportionate effects
“Benzodiazepines”
Common Barbiturates?
Phenobarbital
Pentobarbital
Thiopental
Barbiturate mech.
Binds to GABA-A receptor working as a chloride ion channel to hyper polarize cell; Barbiturates inc. the duration of the channel openings;
Barbiturate absorption
Absorbed rapidly after oral administration; Highly lipid soluble and reaches peak conc. in 30 seconds; oxidated by hepatic enzymes; long half-life (4-5 days)
Why is phenobarbital different?
often secreted unchanged and can be effected by pH (it is a weak acid), inc. pH can lead to more drug excretion
Barbiturate interactions?
activity of hepatic drug-metabolizing enzymes may be increased
Barbiturates can?
induce sleep with high enough doses
Thiopental?
very lipid soluble and favored for induction of anesthesia; short duration of action because of rapid tissue redistribution
Can barbiturates lead to drug dependence?
Yes
Barbiturates clinical uses?
Hypnosis
Seizure controle
anesthesia induction
Common Benzodiazepines?
Diazepam
Lorazepam
Triazolam
Alprazolam
benzodiazepine mech.?
Works on GABA-A receptor; binds allosterically to inc. frequency of chloride channels opening
Triazolam and Diazepam?
Very rapid effects cause of lipophilicity, Triazolam more so
Benzo. differences?
Unlike barbiturates they have little effect on hepatic drug metabolizing enzymes; Exert more anterograde amnesic effects
Lorazepam and Diazepam?
often used in anesthesia in combination with other agents
Flumazenil?
can reverse benzo. effects because it is a site antagonist; could be used in bento. caused respiratory depression
Non-Benzo. Receptor agonist?
Bind to certain GABA-A receptor subtypes; Giving rapid onset, short duration and slow tolerance development “Zolpidem (Ambien)”
Buspirone?
Relieves anxiety without sedative or hypnotic effects; Takes a week to kick in so not used for acute anxiety; less motor impairment
Ramelteon?
Used to help fall asleep; Agonist for melatonin rec. MT1 and MT2 in suprachiasmatic nuclei “master clock”; low abuse potential
