Hypnotics Flashcards Preview

Class: Neuro > Hypnotics > Flashcards

Flashcards in Hypnotics Deck (23):
1

What class of drugs is currently the MOST TYPICAL DRUG used to treat insomnia?

Newer GABAergic hypnotics - ZALEPLON, ZOLPIDEM, ESZOPICLONE

2

What does it mean to be a "controlled substance" by FDA rules?

The drug has a risk of dependence - both psychological and physiological

3

What do hypnotics promote? (2)

1) Encourage the ONSET of sleep - DECREASES sleep latency
2) Encourage sleep MAINTENANCE - INCREASES total sleep

4

CLASS 1 BZ) CLINICAL TOXICOLOGY: How are the withdrawal symptoms of BZ use for hypnosis compared to sedation?

WORSE Rebound hyperanxiety, insomnia/headaches, convulsions

5

CLASS 2 NEWER GABAergic HYPNOTICS) What is their mechanism of action?

Bind to the same site as BZ, but more specific in terms of the subunit isoform (only alpha1-containing subunits)

6

What are 2 classes of anxiolytics and 1 class of hypnotics that are NOT controlled substances?

1) Sed - BUSPIRONE
2) Sed - BETA-BLOCKERS
3) Hyp - RAMELTEON

7

CLASS 2 NEWER GABAergic HYPNOTICS) What are the two therapeutic effects of these drugs?

* All 3 DECREASE sleep latency - decreases the time it takes to fall asleep
ZALEPLON - Does NOT increase total sleep time
ZOLPIDEM + ESZOPICLONE - Do increase total sleep time

8

CLASS 2 NEWER GABAergic HYPNOTICS) PHARMACOKINETICS: Describe the onset of action and half-life.

Rapid onset of action
Short half-life (DESIRED effect) compared to BZ's that have long half-lives (except midazolam)

9

CLASS 2 NEWER GABAergic HYPNOTICS) Can ZALEPLON, ZOLPIDEM, and ESZOPICLONE be used to treat muscle spasms and manage seizures?

NO - Bec of receptor subunit specificity associated with these 3 newer GABAergic hypnotics

10

Can anxiolytics (sedatives) be used to produce hypnosis?

YES, at higher doses the anxiolytic, calming effects can promote sleep

11

What are the 3 classes of hypnotics?

CLASS 1) BZ
CLASS 2) NEWER GABAergic Hypnotics
CLASS 3) New non-GABAergic Hypnotics

11

CLASS 2 NEWER GABAergic HYPNOTICS) Name the 3 GABAergic hypnotics (*Hint: Z-drugs*)

ZALEPLON
ZOLPIDEM
ESZOPICLONE

12

What is 1 class of sedatives and 2 classes of hypnotics that are classified as "controlled substances" by FDA and thus have a high risk of dependence?

CONTROLLED SUBSTANCE = RISK OF DEPENDENCY
1) Sed - BZs
2) Hyp - Newer GABAergic Hypnotics - ZALEPLON, ZOLPIDEM, ESZOPICLONE
3) Hyp - SUVOREXANT

13

CLASS 2 NEWER GABAergic HYPNOTICS) Name the 4 advantages of these drugs: (1 PK, 1 PD, 2 side effects).

1) PHARMACOKINETICS - Act fast, go away fast
2) PHARMACODYNAMICS - Very specific effect of SLEEP
3) SIDE EFFECTS - Very modest psychomotor depression compared to BZs
4) SIDE EFFECTS - NO (few) amnesia

14

CLASS 2 NEWER GABAergic HYPNOTICS) What are the 2 disadvantages of these 3 drugs?

1) Controlled substance - aka risk of DEPENDENCY (ONLY use in times of crises)
2) Chance of REBOUND INSOMNIA when higher than hypnotic doses are administered

15

CLASS 3 NEW NON-GABAergic HYPNOTICS) Name the 2 drugs in this category

1) RAMELTEON
2) SUVOREXANT

16

CLASS 3 NEW NON-GABAergic HYPNOTICS) What is the mechanism of action of RAMELTEON?

Agonist of MELATONIN (M1 and M2) receptors in the BRAIN and has NO GABAergic effects on the CNS

17

CLASS 3 NEW NON-GABAergic HYPNOTICS) What are the 2 effects of RAMELTEON?

By activating melatonin receptors involved in the sleep-wake cycle, one's sleep state is promoted.
1) DECREASES Sleep latency
2) INCREASES sleep periods

18

CLASS 3 NEW NON-GABAergic HYPNOTICS) What are the 3 major advantages of RAMELTEON?
(*Hint: Controlled substance?, Side Effect, Mech of Action)

1) NO DEPENDENCE = Not a controlled substance
2) NO REBOUND INSOMNIA
3) NO PSYCHOMOTOR IMPAIRMENT - No GABAergic effects

19

CLASS 3 NEW NON-GABAergic HYPNOTICS) What are the 2 disadvantages of RAMELTEON?
(*Hint: drug interactions + effect on body systems)

1) Metabolized mainly by CYP1A2 - should NOT be taken with CYP1A2 inhibitors
2) Adverse effects are not as severe - dizziness + fatigue + endocrine changes [DECREASED testosterone + INCREASED prolactin]

20

CLASS 3 NEW NON-GABAergic HYPNOTICS) What is the mechanism of action of SUVOREXANT?

Orexin Receptor antagonist in the brain with NO GABAergic CNS effects
* Orexin - stimulating NT promoting "wake" in the sleep-wake cycle

21

CLASS 3 NEW NON-GABAergic HYPNOTICS) What are the two effects of SUVOREXANT?

1) DECREASES sleep latency
2) INCREASES sleep periods

22

CLASS 3 NEW NON-GABAergic HYPNOTICS) What are the SEVERE disadvantages of SUVOREXANT?
(*Hint: Controlled substance? Major side effect (1) Other adverse effects (1))

1) HIGH RISK OF ABUSE/DEPENDENCE = controlled substance
2) Can cause "sleep driving" + amnesic effects - no conscious recollection of driving
3) Body System Adverse Effects: Headache + Dizziness + Day-after somnolence