Axinolytics

Question 1

benzodiazepams with long half lives

Answer 1

chlordiazepoxide 
diazepam 
prazepam 
cloraepate
flurazepam

Question 2

bzds with short half lives and no active metabolites

Answer 2

lorazepam

oxazepam

Question 3

bzds with short half lives and active metabolites

Answer 3

alprazolam

triazolam

Question 4

benzodiazepam antagonist

Answer 4

flumazenil

Question 5

barbiturates

Answer 5

thiopental

Question 6

anxiolytic

Answer 6

buspirone

Question 7

other hypnotic

Answer 7

zoplicone

Question 8

what is anxiolytic

Answer 8

calming

relief of anxiety

Question 9

what is hypnotic

Answer 9

promotes drowsiness and onset and maintenance of sleep

Question 10

what is the action site of bzds

Answer 10

GABA-A receptor

Question 11

what is the gaba- a receptor and the structure

Answer 11

inhibitory transmitter in the brain

hetero-oligomeric glycoprotein with 2 alpha, beta subunits and 1 gamma subunit

Question 12

how many isoforms of the alpha subunit

Answer 12

alpha 1- hypnotic

alpha 2-5- sedation and psychomotor effect

Question 13

what does activation of gaba- a receptor do

Answer 13

chloride influx hyperpolarizes neurons and decreases neuronal activity

Question 14

what do barbiturates do

Answer 14

bind to GABA-A receptor
increases the durationof channel opening events
GABA- mimetic at high concentrations
inhibit glutamate AMPA receptor

Question 15

how can you increased the onset of CNS drugs

Answer 15

increase lipophilicity so cross BBB

Question 16

lipophilicity of bzds

Answer 16

traizolam>diaepam > lorazepam, oxazepam

Question 17

what therapeutic used are preferred for short acting bzds?

long acting?

Answer 17

short acting- hypnotic

long acting - anxiolytic

Question 18

how are bzds excreted

Answer 18

kidney

Question 19

who should you consider when using bzds

Answer 19

pregnant and breast feeding, can cross placenta and in milk
older patient becuase decreased liver function and patients with liver tissue
obese patienys bc redistributed to adipose tissue

Question 20

how are barbiturates metabolized and the effects on the enzymes

Answer 20

metabolized in liver slowly

hepatic cyt-p450 inducers

Question 21

therapeutic uses of bzds

Answer 21

anxiety relief 
treatment of insomnia 
sedation and amnesia before surgery 
treat epilepsy and seizure states 
muscle relaxtion in neuromuscular disorders
control of ethanol withdrawal symptoms

Question 22

what is used for acute anxiety and what is used for long term anxiety treatment

Answer 22

acute- bzds

long term- SSRI

Question 23

stages of sleep

Answer 23

1: muscles relax
2: brain activity slows no eye movement
3/4: all eye and muscle movement seizes
rem: rapid eye movement

Question 24

how are bzds used as hypnotics

Answer 24

decrease the latency to sleep onset and increase stage 2 sleep
decrease rem and slow wave sleep

Question 25

why are bzds used over barbituates for sedative or hypnotic

Answer 25

safer becuase less CNS depression, wont cause coma

Question 26

what is thiopental used for

Answer 26

used to induce amnesia, rapid induction adn clearance

Question 27

adverse effects of bzds

Answer 27

``` drowsy confusion anterograde amnesia dizziness lethargy ataxia safe unless used with other CNS depressants ```

Question 28

how does bzd tolerance occur

Answer 28

down-regulation of brain bzd receptors - pharmacodynamic

Question 29

bzd withdrawal symtoms when are they more common

Answer 29

rebound anxiety insomnia restlessness more common and severs in short half lives

Question 30

why are bzds abused

Answer 30

effects similar to alcohol available tolerance and dependence associated with long term use

Question 31

contraindications for bzd use

Answer 31

``` myasthenia gravis narrow angle glaucoma alcoholism severe sleep apnea pregnant or nursing ```

Question 32

what is flumazenil used for

Answer 32

bzd competitive antagonist used to reverse CNS depressant effects of bzd overdose

Question 33

what is a caution with flumazenil use

Answer 33

if bzds used for seizures may have rebound seizure

Question 34

adverse effects of barbiturates

Answer 34

``` can cause cardiac and vascular depression low therapeutic index metabolic and pharmacodynamic tolerance severe withdrawal symptomes abuse no antidote ```

Question 35

difference between metabolic and pharmacodynamic tolerance

Answer 35

metabolic- induces enzymes | pharmacodynamic- down regulation of receptors

Question 36

what is the action sire of buspirone

Answer 36

partial agonist at serotonin receptor | presynaptic antagonist at presynaptic dopamine d2 receptor

Question 37

pharmacokinetics of buspirone

Answer 37

rapid oral absorption | extensive first pass metabolism to form active metabolites

Question 38

what is buspirons therapeutic use

Answer 38

relieve anxiety | takes over a week so not used in acute or panic disorder

Question 39

contraindication for busporin

Answer 39

monoamine oxidase inhibtors

Question 40

action site of zoplicone

Answer 40

GABA-A alpha 1 subunit | enhances gaba mediated neuronal inhibition

Question 41

pharmacokinetics of zoplicone

Answer 41

rapidly absorped and metabolizes

Question 42

therapeutic uses of zpoplicone

Answer 42

short term treatment of insomnia, increase stage 2 as well as stage 3/4

Question 43

adverse effects of zoplicone

Answer 43

drowsiness, memory impairment, dizziness, fatigue