Sedative-Hypnotics Flashcards

(44 cards)

0
Q

What does hypnotic drugs do?

A

They produce drowsiness and encourage onset/maintenance of sleep.

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1
Q

What does sedative drugs do?

A

They DECREASE anxiety and exert calming effects.

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2
Q

What are the main reasons for prescribing sedative-hypnotic drugs?

A

To decrease anxiety and onset/maintenance of sleep.

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3
Q

What is the main inhibitory transmitter of the CNS?

A

GABA

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4
Q

Which part of the brain is the most affected by sedatives?

A

Reticular formation:because it is highly connected part, so it is sensitive.

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5
Q

What are the classes of drugs?

A
  1. Benzodiazepines

2. Barbiturates

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6
Q

How long does it take to develop tolerance for benzodiazepines?

A

3-5 weeks

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7
Q

Can ORAL benzodiazepine produce anesthesia ?

A

No

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8
Q

What drug “acts” like benzodiazepine but is NOT benzodiazepine ?

A

ZOLPIDEM

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9
Q

What is the use of ZOLPIDEM ?

A

Use: when somebody has difficulty falling asleep (due to it being short acting).

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10
Q

What drugs are benzodiazepines?

A

They end in “PAM” with exception to triazoLAM.

  • LorazaPAM
  • QuazePAM
  • DiazePAM
  • FlurazePAM: long acting, use: staying asleep
  • TemazePAM: long acting, use: staying asleep
  • TriazoLAM: short acting, use: for falling asleep
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11
Q

Can barbiturates produce an anesthesia effect ORALLY?

A

Yes

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12
Q

How long does it take to build tolerance to barbiturates?

A

2 weeks

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13
Q

What drugs are barbiturates?

A

These drugs end in ‘BARBITAL’.

  • amoBARBITAL: long acting, for staying asleep
  • pentoBARBITAL:short acting, for falling asleep
  • secoBARBITAL:short acting, for falling asleep
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14
Q

What class does ALCOHOL act like but is NOT?

A

Barbiturates

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15
Q

What is another drug that does NOT fall under benzodiazepines and barbiturates but targets GABA/Cl channel?

A

ZolpidEM

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16
Q

What drugs are antihistaminics (same use as barbiturates and benzodiazepines) but does NOT target GABA/Cl channel?

A

They end in ‘AMINE’

  • DoxylAMINE
  • DiphenhydrAMINE
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17
Q

What receptor does benzodiazepines and barbiturates act on?

A

GABA receptor

18
Q

What happens when GABA binds?

A

It open Cl channels

19
Q

Do barbiturates and benzodiazepines bind to the same site?

A

No, they bind to different allosteric sites

20
Q

Does some drugs NOT work if GABA is not present?

A

True, SOME do not work

21
Q

What class of drugs requires GABA to be present to work?

A

Benzodiazepines require to be present in order to work (GABA dependent).ONLY DEPENDENT

22
Q

How does the channel work for benzodiazepines?

A

It INCREASES FREQUENCY of channel openings at ISPSs.

23
Q

Do barbiturates require GABA to be present in order to work?

A

No, barbiturates are both dependent AND independent (can open channel without GABA but would require higher doses than with GABA being present)

24
How does the channel work with barbiturates?
It INCREASES the DURATION that the channel is open
25
If benzodiazepines and barbiturates are present; does it cause GABA to bind better?
Yes
26
What is the order of action for CNS depression with iNCREASE dose of hypnotic/sedative drugs?
SHARD:Sedation (not exactly asleep)-->Hypnosis( asleep)--> anesthetic coma (can't wake up)--> respiratory depression--> death
27
What happens to benzodiazepines on a graph?
It plateaus because it GABA dependent, therefore it is limited by The amount of GABA present
28
What happens to barbiturates on a graph?
It continues to increase/grow because it is dependent AND independent of GABA.
29
What is REM sleep?
REM is Rapid Eye Movement, dreaming, muscle Antonia(lost of muscle strength)
30
What is NREM?
It is non-rapid eye movement
31
What are the stages of NREM ?
N1: twitching, still awake, loss of most awareness N2: COMPLETE loss of awareness, no eye movement, still easily awake N3: DEEP SLEEp, sleep inertia (30 mins to fully awake), some dreaming but not vivid, parasomnias such as bed wetting,sleep walking, sleep talking, night terrors
32
What stage of sleep does benzodiazepines and barbiturates block?
NREM:N3
33
Is insomnia a disease?
No, it is a symptom usually an underlying cause of depression, alcoholism or certain medications.
34
What type of drug would you use for falling asleep?
Short acting hypnotics (short 1/2 life) | * Do not affect sleep architecture due short life and use of falling asleep
35
What type of drug would you use to stay asleep?
Long lasting hypnotics (longer 1/2 life)
36
What are some General side effects?
- Morning sedation (long acting drugs) - Early morning awakening (short acting drugs) - anterograde Amnesia (such as rohypnol- date rape drug) - paradoxical reaction of excitation (increase anxiety, excitement, aggression) occurs in barbiturates, so it has an additive effect - lethal overdose can occur with barbiturates
37
Can anterograde amnesia result in lethal overdose of barbiturates?
Yes called drug automatism
38
Do sedatives mimic natural sleep?
No, it reduces REM and NREM- N3
39
Which class has stronger effects on sleep?
Barbiturates
40
Is NREM-N3 affected as tolerance increases?
No, NREM-N3 stays the same and is not affected with tolerance
41
What results in tolerance?
Withdrawal results in tolerance and therefore temporary rebound ( no tolerance effect in N3)
42
Do all sedative /hypnotic drugs produce tolerance ?
Yes ALL
43
How to counter effects of tolerance?
- By increasing does - by using a more potent drug *infrequent use does NOT induce (cause) tolerance