Anxiolytic: Barbiturates Flashcards

(44 cards)

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
high abuse potential is due to rapid______ and _______
tolerance and dependence
26
when are amphetamines and barbiturates used
- amph-> during the day - barb-> during the night
27
what do barbiturates have a high potential to interact with
ethanol
28
what does decreasing safety margin with tolerance lead to
high potential for overdose
29
what receptor do barbiturates act at and what does result in
GABA(A) receptor - positive allosteric modulation increases GABA affinity and prolongs open time
30
where does an important effect of barbiturates happen
in the reticular formation - pontine-> normally activates cortical centres - medullary-> normally suppresses cortical centres
31
what are the balances of barbiturate effect in the reticular formation
-medullary fist- euphoria resulting from cortical activation - pontine first- relaxation, drowsiness, sleep from cortical depression
32
true or false: barbiturates decrease mesolimbic DA release
Paradoically decrease mesolimbic DA release Activates GABA inhibitory interneuron on VTA --> x Nucleus accumbens
33
can pentobarbital administration inhibit NAc dopamine release and inhibit ketamine-induced dopamine release
yes it can
34
in metabolic tolerance what do barbiturates induce in
induces microsomal enzyme leading to greater liver metabolism and leads to cross-tolerance
35
in pharmacodynamic tolerance what changes are made
cellular changes in GABA(A) receptor function and expression
36
fill in the blank: tolerance leads to decreased _______ ______
safety margin
37
look at slides 21,22 and 23 about dependence and withdrawal
38
what does pharmacological tolerance result in
rebound hyperactivity for more information please look at slide 24 (thanks)
39
when did psychosis develop
- 3-5 days after withdrawal lasting as long as 9 days - delirium, agitation, insomnia, confusion, etc. - high BP, temperature and pulse
40
Why does effects of ultra-short acting barbiturates end?
They are highly **lipophillic**, thus **redistribute into fatty tissue**
41
Short/intermediate acting bariturates are _____
sedative
42
What is an example of a short/intermediate acting barbirturate that acts as a sedative?
Amobarbital
43
What does the termination of amobarbital depend on? Does this drug have a high abse potential
Liver metabolsim ; yes!
44
Two ways tolerance develops w/ barbiturates?
**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.**