Chapter 7 Flashcards
what are tranquillizers
anxiolytics. they are used to treat anxiety disorders and agitation
what are sedative-hypnotics
drugs that are used to sedate and aid sleep
what type of tranquilizer or sedative hypnotic accounts for roughly two thirds of all psychotropic drug prescriptions?
benzodiazepines
what is the principal mechanism of action of anxiolytics and sedative hypnotic drugs
they are modulators of GABA(a) activity
What is the primary pharmocokinetic difference between sedative hypnotics and tranquilizers
sedative hypnotics have a fast kinetic profile. they are fast acting, and have only a short effect.
tranquillizers are slower acting and thus have a longer effect
what is the primary situation that barbiturates are still used today
for severe seizures (like phenobarbital) or severe headaches (butalbital)
Are barbiturates acids or bases
acids
are benzodiazepines acids or bases
acids
are Z-drugs acids or bases
acids
What is the pKa of barbiturates
8, with a therapeutic index of 3-4
what is the pKa of benzodiazepines
3.5-5, with a very high therapeutic index
what is the pKa of Z-drugs
5.6 or so
absorption from the ____ is more rapid than through a(n) ______
- digestive system
- intramuscular site
why is absorption faster through the digestive system than intramuscularly
the drugs bind to protein, which occurs more readily at an intramuscular injection site than it does in the digestive tract
how long does it take for Z-drugs to reach peak concentration
as little as about an hour
“the redistribution of benzodiazepines following absorption into the bloodstream creates a:”
two phase excretion curve
what is a two phase excretion curve
the first phase of excretion occurs when there is a rapid drop in levels as it is distributed throughout the bloodstream. in the second phase, levels begin to drop slower as when the original drug is broken down, it is replaced by other molecules that are slowly released from body fat (active metabolites !!!!!!)
nordiazapam is an active metabolite released from which drug
diazepam. its right there in the name brother
Barbiturates, Benzos, and Z-drugs are all positive _____ (nt) modulators
GABA(a)
what do barbiturates, benzos, and Z-drugs do for GABA
they increase the ability for GABA to open the Cl- ion channel
what can barbiturates do at high doses in terms of inhibitory effects
at high doses it is able to open ion channels themselves, without GABA present
why can Z-drugs work as sedatives, without having any anti-anxiety effects
because Z-drugs only target GABA alpha 1, 2, and 3, but not 5
which type of GABA receptor is responsible for sedation, as well as the amnesic and anticonvulsant effects
GABA alpha 1
which type of GABA receptor is involved in muscle relaxation, but also largely in learning and memory
GABA alpha 5
