Axinolytics Flashcards Preview

Pharmacology 2100 > Axinolytics > Flashcards

Flashcards in Axinolytics Deck (43):
1

benzodiazepams with long half lives

chlordiazepoxide
diazepam
prazepam
cloraepate
flurazepam

2

bzds with short half lives and no active metabolites

lorazepam
oxazepam

3

bzds with short half lives and active metabolites

alprazolam
triazolam

4

benzodiazepam antagonist

flumazenil

5

barbiturates

thiopental

6

anxiolytic

buspirone

7

other hypnotic

zoplicone

8

what is anxiolytic

calming
relief of anxiety

9

what is hypnotic

promotes drowsiness and onset and maintenance of sleep

10

what is the action site of bzds

GABA-A receptor

11

what is the gaba- a receptor and the structure

inhibitory transmitter in the brain
hetero-oligomeric glycoprotein with 2 alpha, beta subunits and 1 gamma subunit

12

how many isoforms of the alpha subunit

alpha 1- hypnotic
alpha 2-5- sedation and psychomotor effect

13

what does activation of gaba- a receptor do

chloride influx hyperpolarizes neurons and decreases neuronal activity

14

what do barbiturates do

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

15

how can you increased the onset of CNS drugs

increase lipophilicity so cross BBB

16

lipophilicity of bzds

traizolam>diaepam > lorazepam, oxazepam

17

what therapeutic used are preferred for short acting bzds?
long acting?

short acting- hypnotic
long acting - anxiolytic

18

how are bzds excreted

kidney

19

who should you consider when using bzds

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

20

how are barbiturates metabolized and the effects on the enzymes

metabolized in liver slowly
hepatic cyt-p450 inducers

21

therapeutic uses of bzds

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

22

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

acute- bzds
long term- SSRI

23

stages of sleep

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

24

how are bzds used as hypnotics

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

25

why are bzds used over barbituates for sedative or hypnotic

safer becuase less CNS depression, wont cause coma

26

what is thiopental used for

used to induce amnesia, rapid induction adn clearance

27

adverse effects of bzds

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

28

how does bzd tolerance occur

down-regulation of brain bzd receptors - pharmacodynamic

29

bzd withdrawal symtoms when are they more common

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

30

why are bzds abused

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

31

contraindications for bzd use

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

32

what is flumazenil used for

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

33

what is a caution with flumazenil use

if bzds used for seizures may have rebound seizure

34

adverse effects of barbiturates

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

35

difference between metabolic and pharmacodynamic tolerance

metabolic- induces enzymes
pharmacodynamic- down regulation of receptors

36

what is the action sire of buspirone

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

37

pharmacokinetics of buspirone

rapid oral absorption
extensive first pass metabolism to form active metabolites

38

what is buspirons therapeutic use

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

39

contraindication for busporin

monoamine oxidase inhibtors

40

action site of zoplicone

GABA-A alpha 1 subunit
enhances gaba mediated neuronal inhibition

41

pharmacokinetics of zoplicone

rapidly absorped and metabolizes

42

therapeutic uses of zpoplicone

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

43

adverse effects of zoplicone

drowsiness, memory impairment, dizziness, fatigue