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PSYC-2920 > Chapter 7: Sedatives > Flashcards

Chapter 7: Sedatives Flashcards

1
Q

What 2 parts of the brain are affected by anxiety disorders?

A

1) hypersensitive amygdala

2) under-reactive ventromedial prefrontal cortex, which is supposed to suppress amygdala activity

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2
Q

Differences between tranquilizers and sedatives

A

tranquilizers treat anxiety and agitation

sedative-hypnotics are for sedation and sleep

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3
Q

3 categories of tranquilizers and sedative hypnotics

A

1) barbiturates
2) benzodiazepines
3) Z drugs

  • other non-benzo drugs include metaqualone and meprobamate
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4
Q

What is the principle mechanism of action for sedatives and hypnotics?

A

modulation of GABA A receptor activity.

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5
Q

What is Rohypnol?

A

a benzodiazepine also known as the “date rape” drug, often used in conjunction with alcohol to produce an exaggerated depressant effect.

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6
Q

what kind of modulation do benzos/barbituates/sedatives do to the GABA receptors?

A

benzos/barbituates/sedatives act as positive allosteric modulators. They have their own binding site that alters the effects of GABA binding to the orthosteric site.

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7
Q

T/F benzos/barbituates/sedatives actively alter levels of GABA and interact at the GABA binding site on the GABA receptors

A

False. benzos/barbituates/sedatives do not actively bind to the orthosteric site of GABA, or actively alter levels of GABA. They are positive allosteric modulators, which indirectly enhance GABA by acting at the allosteric site of the receptor protein

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8
Q

how are benzos/barbituates/sedatives potency effects dictated?

A

benzos/barbituates/sedatives potency effects are dictate by their AFFINITY to the allosteric site of the GABA receptor

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9
Q

how many types of alpha subunits are able to exist in a GABA receptor? What’re the differences?

A

there are 6 possible alpha subunits

alpha 1 receptors: cause more amnesic and anticonvulsant effects when activated.

Alpha 2 and 3 receptors: help regulate sleep-wakefulness and muscle relaxation
- found mostly in the limbic system, dorsal raphe nucleus and interrelated structures involving emotion regulation, and therefore are believed to play a role in anxiety reduction

Alpha 5: also play role in muscle relaxation and sedation, also in learning and memory.

  • largely found in the hippocampus
  • activation of alpha 5 gaba receptors related to the amnesic-properties of benzos/barbituates/sedatives.

Alpha 4 and 6: unknown specific function, but it is known that benzos/barbituates/sedatives do not readily bind to these receptors unless GABA is bound. Therefore the drugs do not bind as frequently to alpha 4 or 6 receptors.

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10
Q

Which type of alpha receptor is activated that may account for the amnesic side effects of benzos/barbituates/sedatives?

A

Alpha 5: also play role in muscle relaxation and sedation, also in learning and memory.

  • largely found in the hippocampus
  • activation of alpha 5 GABA receptors related to the amnesic-properties of benzos/barbituates/sedatives.
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11
Q

Which type of alpha receptor of the GABA receptor is activated that may play a role in anxiety reduction?

A

Alpha 2 and 3 receptors: help regulate sleep-wakefulness and muscle relaxation
- found mostly in the limbic system, dorsal raphe nucleus and interrelated structures involving emotion regulation, and therefore are believed to play a role in anxiety reduction

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12
Q

What makes barbituates more dangerous than benzodiazepines or Z drugs in terms of their upper limits

A

barbituates have NO upper limits to their effects, meaning they can cause death if you keep taking them. Unlike barbituates, benzos and Z drugs have upper limits. If you take a lot, the most you’ll get is Groggy and sleepy, but you will not die.

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13
Q

Why do barbituates not have an upper limit? (think of neurophysiology)

A

barbituates are able to open Cl- ion channels mediated by GABA receptors without GABA actually binding to the orthosteric site, unlike benzodiazepines and Z drugs.

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14
Q

How does death via barbituates occur?

A

by respiratory depression. barbituates are gaba agonists, causing a net inhibitory effect.

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15
Q

T/F: when stressed, an organism sees an enhancement in the receptivity of benzodiazepine receptors.

A

True. this makes organisms less sensitive to cognitive effects of distress.

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16
Q

Describe the relationship between benzos/barbituates/sedatives and adenosine

A

benzos/barbituates/sedatives enhance the effects of adenosine, another inhibitory transmitter. They do this by BLOCKING REUPTAKE, permitting adenosine accumulation in the synapse.

  • opposite to caffeine
  • increases appetite and relaxes muscles
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17
Q

difference between barbituates and benzos in terms of seizure prevention

A

benzos can treat petit mal seizures and infantile spasms, whereas barbiturates protect against grand mal and long term epilepsy

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18
Q

Which drug is more acidic? benzo or barbituates?

A

both are acidic and will readily be absorbed by the digestive tract, however, benzos have a pka of 3 and barbituates have a pka of 8.

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19
Q

does alcohol speed up or slow down the absorption of benzos/barbituates/sedatives?

A

absorption from the digestive system speeds up when paired with EtOH. Blood levels of diazepam can be doubled with the ingestion of small amounts of alcohol.

20
Q

Lipid solubility of a benzos/barbituates/sedatives ____ speed of action, but also means ____duration

A

Lipid solubility of a benzos/barbituates/sedatives INCREASES THE speed of action, but also means SHORTER duration

21
Q

A benzos/barbituates/sedative that passes the blood brain barrier quickly and leads to fast effects has a ____ lipid solubility

A

has a high lipid solubility

22
Q

redistribution of BDZ follow a __-phase excretion curve with ___ half lives as a result of active metabolites extending and producing different effects

A

redistribution of BDZ follow a 2-phase excretion curve with 2 DIFFERENT half lives as a result of active metabolites extending and producing different effects

23
Q

Why does increased lipid solubility result in effects falling quickly?

A

because the drug quickly enters other fat-containing parts of the body

24
Q

T/F Benzodiazepines cause respiratory depression

A

false, barbiturates cause respiratory depression

25
Q

Discuss sleep effects of BDZ’s and Z drugs, what happens to your sleep if these drugs are discontinued?

A

BDZ and Z drugs increase sleeping time and decrease wakefulness, however, they also decrease REM sleep– but this effect goes away with continued use.

if these drugs are discontinued, REM REBOUND may occur, with more time being spent in the REM stage, causing bizarre dreams and insomnia. Z drugs cause less REM REBOUND

26
Q

How do BDZ’s affect memory?

A

cause anterograde AMNESIA: loss of memories for events that occurred while under the influence of the drugs.

found to effect EXPLICIT memory rather than implicit; indicating people can USE information but no recall to working memory– like alcoholic grey out

27
Q

BDZ and barbiturates ____ the critical frequency of fusion threshold

A

BDZ and barbiturates INCREASE the critical frequency of fusion threshold

28
Q

What are residual effects? Why is this important to consider when giving an individual drugs?

A

impairment from drug effects that are seen long after the drug was taken. BDZ’s taken for insomnia may work, but the effects might still be present during the day time, which is bad for a person who needs attention like a crane operator or a surgeon. Z drugs have less residual effects, which might be a better option.

29
Q

How is a person’s ability to drive affected by benzos/barbituates/sedatives?

A

benzos/barbituates/sedatives increase collisions in simulated driving. Residual effects may influence driving.

30
Q

What is the taming effect and how is it displayed in experiments with non-humans when the animals are injected with benzos/barbituates/sedatives?

A

Taming effect: reduction in defensive aggression, no change seen in unprovoked aggression– often seen as a result in the ability of the benzos diminishing anxiety.

diminished anxiety seen because there are increased levels of open arm exploration of the elevated plus maze in individuals injected with BDZs, and decreased time spent defensive burying.

31
Q

How do benzos/barbituates/sedatives affect conditioned behaviour in non-humans?

A
  • avoidance behaviour is blocked at lower doses than those that block escape–> seems to affect motivation.
  • increase in punishment-suppressed behaviour–> animals injected with barbiturates continue to make responses that are punishable by electric shock.

AFFECTS ON CONDITIONED BEHAVIOUR SIMILAR TO THOSE SEEN WITH ALCOHOL

32
Q

T/F the effects of benzos/barbituates/sedatives can be diminished by simulants like coffee and speed

A

FALSE. the effects of benzos/barbituates/sedatives can only be blocked by drugs than block the GABA receptor.

33
Q

Can Z drugs be generalized to alcohol and other depressants?

A

No. Z drugs cannot generalize to alcohol, and only slightly generalize to other benzos/barbituates/sedatives.

34
Q

Can Benzodiazepines generalize to alcohol and other depressants?

A

No, benzos can partially generalize to other benzos, but not to anti-psychotics or ketamine. it CAN BE POTENTIATED WITH ALCOHOL

35
Q

What kind of behaviors are seen to have acute tolerance to benzos/barbituates/sedatives?

A

digit symbol substitution and tracking is seen to have acute tolerance. Phenobarbital has more pronounced effects at a given concentration as the blood level is rising, than when it is descending.

36
Q

is chronic tolerance a problem for benzos/barbituates/sedatives? which type of benzo has a tendency to develop tolerance faster?

A

benzos/barbituates/sedatives become less and less effective in their ability to modulate their effects of GABA.
SHORT ACTING benzos meant for insomnia (they are short acting to prevent residual effects in the morning) show the fastest acting tolerances.

37
Q

T/F: people who abuse alcohol are likely to be more tolerant to benzos/barbituates/sedatives

A

true

38
Q

are BDZ-tolerant individuals more tolerant to barbiturates?

A

No. Barbiturate-tolerant people are more tolerant to alcohol and BDZs, but BDZ-tolerant people are barely tolerant to barbiturates. Indicates that barbiturates are stronger and operate on slight different mechanisms compared to BDZ’s

39
Q

How can withdrawal symptoms from phenobarbital and heavy barbiturates be blocked? what is this called?

A

withdrawal symptoms from phenobarbital and heavy barbiturates be blocked by BENZODIAZEPINES. this indicates CROSS-DEPENDENCE

40
Q

Two types of Benzodiazepine withdrawal

A

1) Sedative-Hypnotic Type: typically seen in short-half life benzodiazepines, involves tremors, cramps, possible convulsions. can be expected in individuals who have been taking higher than reccommended doses for over a month, symptoms gone within 10 days of abstinence
2) LOWDOSE withdrawal: seen in individuals who have taken the prescribed amount of drug for over 6 months. Emerges slower than sedative-hypnotic type withdrawal. Results in anxiety, panic, increased BP, concentration and memory impairment. Can last longer- 2 weeks to a year.

41
Q

How can you reverse the effects of LOW DOSE withdrawal?

A

low dose with drawal effects can be quickly reversed by a small amount of BDZ.

42
Q

T/F individuals who have been taking the prescribed dose of drug for 4 years will have worse LOW-DOSE withdrawal symptons than a person who has been taking the prescribed dose of drug for 2 years

A

FALSE. Low dose withdrawal symptoms are correlated with AMOUNT/DOSE of benzodiazepine, not duration of use. If the individuals were taking the same amount, it is most likely their withdrawal symptoms will be of the same magnitude.

43
Q

Define Reemergent symptoms

A

Reemergent symptoms may be present or more intense than original symptoms. The Expression of symptoms that were present before the drug was started and suppressed while the drug was being used are beginning to show again.

44
Q

Compare diazepam and phenobarbital in terms of their reinforcing effects?

A

diazepam was not chosen more than the placebo, even in highly anxious patients —> low reinforcing effects, but will be chosen if individuals know there is a relaxation task needing to be completed.

phenobarbital has high reinforcing effects–> people will work harder to get a dose of phenobarbital.

45
Q

Are short acting or longer acting barbituates better reinforcers?

A

shorter acting barbituates are better reinforcers because of instant gratification.

46
Q

Often times, barbiturates are able to kill an individual, but benzos are a lot more safe. When can benzos kill someone?

A

if benzos are coupled with alcohol; causes respiratory depression

47
Q

Benzodiazepine metabolism is ____ (quickened, slowed) by alcohol

A

slowed. half lives increase therefore longer effects

PSYC-2920 (15 decks)

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