Chapter 8 - Depressants Flashcards
What is a depressant?
drug that diminishes physiological activity
Therapeutic uses of depressants
anxiety, sleep management, seizures, anesthesia
-most produce positive subjective effects (activate reward pathways); high abuse liability
What are some common depressants?
alcohol, barbiturates, benzodiazepines, opioids
Most depressants act through increased activity of ____
GABA
Depressants and GABAA receptor
Ionotropic receptor that allows entry of Cl- ions; hyperpolarizes neurons which decreases their firing rate; five subunits; two binding sites for GABA
There are ____ sites on the GABAA receptor that enhance GABA transmission
allosteric
What are barbiturates?
became available after development of barbital from barbituric acid; became widely used for insomnia, nervousness, sedation, anesthesia; first effective anti-seizure medication
Barbiturates are ____ depressants and are sometimes referred to as ____
CNS; sedatives
barbiturates are classified by their…
speed of onset and duration of action
speeds and durations of barbiturates
ultra-shortacting: effects in 20-30s, lasts ~30min ex. thiopental
short-acting/intermediate: ex. pentobarbital
long-acting: effects in ~1hr, last ~12hr ex. phenobarbital
Barbiturate as a drug of abuse
positive reinforcing effects; reduce feelings of stress and anxiety; produce feelings of well-being and lower inhibitions
depressants enhance GABA inhibition at sites of action such as…
cerebral cortex, amygdala, thalamus, and medulla
HOWEVER as doses increase the effects reach deeper into brain cortex>amygdala>medulla
cortex: disinhibition
amygdala: red. anxiety
medulla: resp. depression
Inhibition of ____ accounts for
the effects on seizures, memory, attention, and other cognitive functions
cortical activity
the ____ effects of barbiturates are due to the inhibition of the amygdala
anti anxiety
The effects on ____ result from inhibition of the medulla
respiratory function
overdose potential of barbiturates
main concern is respiratory depression; memory blocking effects (forgetting if they took a dose); long term use can lead to shrinking therapeutic index
chronic use of barbiturates causes tolerance to the ____ but not to the ____
therapeutic effects: respiratory depressant effects