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Ph 4 > Sedative-Hypnotics > Flashcards

Sedative-Hypnotics Flashcards

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
Q

How does the channel work with barbiturates?

A

It INCREASES the DURATION that the channel is open

25
Q

If benzodiazepines and barbiturates are present; does it cause GABA to bind better?

A

Yes

26
Q

What is the order of action for CNS depression with iNCREASE dose of hypnotic/sedative drugs?

A

SHARD:Sedation (not exactly asleep)–>Hypnosis( asleep)–> anesthetic coma (can’t wake up)–> respiratory depression–> death

27
Q

What happens to benzodiazepines on a graph?

A

It plateaus because it GABA dependent, therefore it is limited by The amount of GABA present

28
Q

What happens to barbiturates on a graph?

A

It continues to increase/grow because it is dependent AND independent of GABA.

29
Q

What is REM sleep?

A

REM is Rapid Eye Movement, dreaming, muscle Antonia(lost of muscle strength)

30
Q

What is NREM?

A

It is non-rapid eye movement

31
Q

What are the stages of NREM ?

A

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
Q

What stage of sleep does benzodiazepines and barbiturates block?

A

NREM:N3

33
Q

Is insomnia a disease?

A

No, it is a symptom usually an underlying cause of depression, alcoholism or certain medications.

34
Q

What type of drug would you use for falling asleep?

A

Short acting hypnotics (short 1/2 life)

* Do not affect sleep architecture due short life and use of falling asleep

35
Q

What type of drug would you use to stay asleep?

A

Long lasting hypnotics (longer 1/2 life)

36
Q

What are some General side effects?

A
  • 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
Q

Can anterograde amnesia result in lethal overdose of barbiturates?

A

Yes called drug automatism

38
Q

Do sedatives mimic natural sleep?

A

No, it reduces REM and NREM- N3

39
Q

Which class has stronger effects on sleep?

A

Barbiturates

40
Q

Is NREM-N3 affected as tolerance increases?

A

No, NREM-N3 stays the same and is not affected with tolerance

41
Q

What results in tolerance?

A

Withdrawal results in tolerance and therefore temporary rebound ( no tolerance effect in N3)

42
Q

Do all sedative /hypnotic drugs produce tolerance ?

A

Yes ALL

43
Q

How to counter effects of tolerance?

A
  • By increasing does
  • by using a more potent drug

*infrequent use does NOT induce (cause) tolerance

Ph 4 (7 decks)

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