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Pharmacology 2100 > Axinolytics > Flashcards

Axinolytics Flashcards

1
Q

benzodiazepams with long half lives

A 
chlordiazepoxide 
diazepam 
prazepam 
cloraepate
flurazepam
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2
Q

bzds with short half lives and no active metabolites

A

lorazepam

oxazepam

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3
Q

bzds with short half lives and active metabolites

A

alprazolam

triazolam

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4
Q

benzodiazepam antagonist

A

flumazenil

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5
Q

barbiturates

A

thiopental

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6
Q

anxiolytic

A

buspirone

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7
Q

other hypnotic

A

zoplicone

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8
Q

what is anxiolytic

A

calming

relief of anxiety

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9
Q

what is hypnotic

A

promotes drowsiness and onset and maintenance of sleep

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10
Q

what is the action site of bzds

A

GABA-A receptor

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11
Q

what is the gaba- a receptor and the structure

A

inhibitory transmitter in the brain

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

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12
Q

how many isoforms of the alpha subunit

A

alpha 1- hypnotic

alpha 2-5- sedation and psychomotor effect

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13
Q

what does activation of gaba- a receptor do

A

chloride influx hyperpolarizes neurons and decreases neuronal activity

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14
Q

what do barbiturates do

A

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

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15
Q

how can you increased the onset of CNS drugs

A

increase lipophilicity so cross BBB

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16
Q

lipophilicity of bzds

A

traizolam>diaepam > lorazepam, oxazepam

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17
Q

what therapeutic used are preferred for short acting bzds?

long acting?

A

short acting- hypnotic

long acting - anxiolytic

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18
Q

how are bzds excreted

A

kidney

19
Q

who should you consider when using bzds

A

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
Q

how are barbiturates metabolized and the effects on the enzymes

A

metabolized in liver slowly

hepatic cyt-p450 inducers

21
Q

therapeutic uses of bzds

A 
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
Q

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

A

acute- bzds

long term- SSRI

23
Q

stages of sleep

A

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

24
Q

how are bzds used as hypnotics

A

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

25
Q

why are bzds used over barbituates for sedative or hypnotic

A

safer becuase less CNS depression, wont cause coma

26
Q

what is thiopental used for

A

used to induce amnesia, rapid induction adn clearance

27
Q

adverse effects of bzds

A 
drowsy 
confusion 
anterograde amnesia
dizziness
lethargy 
ataxia 
safe unless used with other CNS depressants
28
Q

how does bzd tolerance occur

A

down-regulation of brain bzd receptors - pharmacodynamic

29
Q

bzd withdrawal symtoms when are they more common

A

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

30
Q

why are bzds abused

A

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

31
Q

contraindications for bzd use

A 
myasthenia gravis 
narrow angle glaucoma
alcoholism 
severe sleep apnea
pregnant or nursing
32
Q

what is flumazenil used for

A

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

33
Q

what is a caution with flumazenil use

A

if bzds used for seizures may have rebound seizure

34
Q

adverse effects of barbiturates

A 
can cause cardiac and vascular depression 
low therapeutic index
metabolic and pharmacodynamic tolerance 
severe withdrawal symptomes 
abuse 
no antidote
35
Q

difference between metabolic and pharmacodynamic tolerance

A

metabolic- induces enzymes

pharmacodynamic- down regulation of receptors

36
Q

what is the action sire of buspirone

A

partial agonist at serotonin receptor

presynaptic antagonist at presynaptic dopamine d2 receptor

37
Q

pharmacokinetics of buspirone

A

rapid oral absorption

extensive first pass metabolism to form active metabolites

38
Q

what is buspirons therapeutic use

A

relieve anxiety

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

39
Q

contraindication for busporin

A

monoamine oxidase inhibtors

40
Q

action site of zoplicone

A

GABA-A alpha 1 subunit

enhances gaba mediated neuronal inhibition

41
Q

pharmacokinetics of zoplicone

A

rapidly absorped and metabolizes

42
Q

therapeutic uses of zpoplicone

A

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

43
Q

adverse effects of zoplicone

A

drowsiness, memory impairment, dizziness, fatigue

Pharmacology 2100 (13 decks)

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