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PSYCH 478 > Anxiolytic: Barbiturates > Flashcards

Anxiolytic: Barbiturates Flashcards

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1
Q

fill in the blank: anxiety is the_______ of potential danger

physiological responses including _________ _______

A
  • anticipation
  • sympathetic activation
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2
Q

what is an anxiolytic, sedative, hypnotic

A
  • anxiolytic-> reducing anxiety or tranquillizing
  • sedative-> calming, relaxing, or sleep inducing
  • hypnotic-> sleep inducing or sopoforic
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3
Q

what are sympathetic effects

A
  • increased muscle tension, digestive problems and sleep disturbance
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4
Q

fill in the blank:________ _______ cycle is due to performance decrease and fear of failure

A

escalating anxiety

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5
Q

what disorders does anxiety have high comorbidity with

A
  • depressive disorders and substance abuse
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6
Q

what are rates of alcohol abuse highest with

A

social anxiety disorders

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7
Q

how is generalized anxiety disorder different from panic attacks

A

generalized anxiety-> symptoms on anxiety without identifiable cause
panic attacks-> experiencing physiological effects of fear reaction without threatening stimulus

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8
Q

what can panic attack in response to a cue lead to

A

phobia

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9
Q

what are panic attacks accompanied by

A
  • strong sympathetic NS activation
  • increased heart rate, sweating, shortness of breath, choking, fear of losing control or dying
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10
Q

what was the first drug that was widespread to reduce anxiety

A

alcohol

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11
Q

what are the two contemporary anxiolytics and sedative-hypnotics

A

barbiturates; benzodiazepine

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12
Q

what are bromides

A

are sedatives possible through effects on cl- balance in the CNS and were the first effective anticonvulsants

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13
Q

what does bromism result from

A
  • bromide toxicity
    -impaired thought and memory, drowsiness, irritability, skin eruption (rash)
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14
Q

what was the first psychoactive barbiturate synthesized and what was it marketed as

A
  • barbital ( relaxing and sopoforic effects)
    -> long half-life meant drowsiness extended for days
  • veronal
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15
Q

true or false: phenobarbital was noted to be faster acting,, shorter duration and have excellent anticonvulsant properties

A

true

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16
Q

how can barbiturates be classed

A

according to the relative lipophilicity of the compound

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17
Q

true or false: decreasing the lipophilicity of barbiturates results in slower uptake into the brain and slower sedation

A

true

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18
Q

how are phenobarbital, amobarbital and thiopental different

A
  • pheno-> low lipho and slow uptake
  • amo-> medium lipho and intermediate uptake
  • thio-> high lipho and fast uptake
19
Q

what do low, moderate and high doses result in

A
  • low-> anxiolytic and tranquillizing
  • moderate -> sedation and sopoforic
  • high-> anesthetic
20
Q

Ultrashort acting bariturates are ____

A

anaesthetic ; example: thiopental

21
Q

true or false: long-acting barbiturates have high lipophilicity and are effective for treating seizure disorders and anxiety

A

false; low
such as phenobarbital

22
Q

what kind of side effects are accompanied by anxiolytic effects and what are they

A
  • cognitive side effects
  • mental clouding, loss of judgement, slowed reflexes
23
Q

what is coma and death result of

A

respiratory depression

24
Q

true or false: barbiturates induce restful sleep

A

false; they do not
- short term use does result in rapid sleep but decreased stages 3 and 4
- chronic decreases REM sleep and stages 3 and 4, it also increases spontaneous awakening

25
Q

high abuse potential is due to rapid______ and _______

A

tolerance and dependence

26
Q

when are amphetamines and barbiturates used

A
  • amph-> during the day
  • barb-> during the night
27
Q

what do barbiturates have a high potential to interact with

A

ethanol

28
Q

what does decreasing safety margin with tolerance lead to

A

high potential for overdose

29
Q

what receptor do barbiturates act at and what does result in

A

GABA(A) receptor
- positive allosteric modulation increases GABA affinity and prolongs open time

30
Q

where does an important effect of barbiturates happen

A

in the reticular formation
- pontine-> normally activates cortical centres
- medullary-> normally suppresses cortical centres

31
Q

what are the balances of barbiturate effect in the reticular formation

A

-medullary fist- euphoria resulting from cortical activation
- pontine first- relaxation, drowsiness, sleep from cortical depression

32
Q

true or false: barbiturates decrease mesolimbic DA release

A

Paradoically decrease mesolimbic DA release

Activates GABA inhibitory interneuron on VTA –> x Nucleus accumbens

33
Q

can pentobarbital administration inhibit NAc dopamine release and inhibit ketamine-induced dopamine release

A

yes it can

34
Q

in metabolic tolerance what do barbiturates induce in

A

induces microsomal enzyme leading to greater liver metabolism and leads to cross-tolerance

35
Q

in pharmacodynamic tolerance what changes are made

A

cellular changes in GABA(A) receptor function and expression

36
Q

fill in the blank: tolerance leads to decreased _______ ______

A

safety margin

37
Q

look at slides 21,22 and 23 about dependence and withdrawal

A
38
Q

what does pharmacological tolerance result in

A

rebound hyperactivity

for more information please look at slide 24 (thanks)

39
Q

when did psychosis develop

A
  • 3-5 days after withdrawal lasting as long as 9 days
  • delirium, agitation, insomnia, confusion, etc.
  • high BP, temperature and pulse
40
Q

Why does effects of ultra-short acting barbiturates end?

A

They are highly lipophillic, thus redistribute into fatty tissue

41
Q

Short/intermediate acting bariturates are _____

A

sedative

42
Q

What is an example of a short/intermediate acting barbirturate that acts as a sedative?

A

Amobarbital

43
Q

What does the termination of amobarbital depend on? Does this drug have a high abse potential

A

Liver metabolsim ; yes!

44
Q

Two ways tolerance develops w/ barbiturates?

A

Pharmacodynamic: changes in GABA A receptor function and expression

Metabolic: Greater liver enzymes (p450)

Tolerance to sedative/hypnotic (desired efffects) are greater than toelrance to resp. depression —> decrease in safety margin.

PSYCH 478 (28 decks)

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