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Flashcards in Sleep Deck (20):
1

Properties of Ideal Hypnotic Agent

Rapidly induce sleep – influenced by rate of absorption

Sufficient duration to maintain sleep – influenced by t1/2

No tolerance development with repeated use

No rebound insomnia with abrupt d/c - influenced by t1/2

High therapeutic index

Normalize disturbed sleep without disturbing normal sleep

“Z”-drugs (zolpidem) closest to ideal

2

Night terrors are

Stage 3

3

“Z”-Drugs

Eszoplicone
Zaleplon
Zolpidem

4

Benzodiazepines

Triazolam
Temazepam
Flurazepam

5

Non-GABA Actions

Ramelteon - Melatonin
Trazodone
Diphenhydramine
Chloral hydrate

6

Hypotnitic vs anx benzo=

(↑ dose= sleep, lower dose = ↓ anx)
dose

7

BDZs enhance channel opening in presence of _____only

GABA

8

BARBs prolong channel opening in presence of GABA and at higher doses _____________

open channel directly

9

Less hangover effect w/

short half life

10

Rebound insomnia has?

short half life

11

Triazolam (Halcion)

Benzodiazepine Pharmacokinetics

Rapid oral absorption

Short t1/2: 1.5-5 hrs - eliminated in 1 dosing cycle

Less daytime sedation (hangover)

Rebound insomnia next day due to rapid elimination

12

Temazepam (Restoril)

Benzodiazepine Pharmacokinetics

Slow absorption - minimal effect on sleep latency

Intermediate t1/2 (9-13 hrs)

13

Flurazepam (Dalmane)

Benzodiazepine Pharmacokinetics

Long t1/2 + active metabolite (75-90 hrs) - low tolerance

Can accumulate in elderly - impaired hepatic clearance  daytime sedation (“hangover”) / overdosage

14

Zolpidem (Ambien) and Zaleplon (Sonata)

Rapid oral absorption

Shortest durations of action (6-8 hours) and half-lives of available agents (zolpidem: 2-2.5 hrs - zaleplon: 1 hr)

Zolpidem eliminated more slowly in females - dose recommendation halved to prevent daytime hangover

Z drug

15

Eszopiclone (Lunesta)

Structurally different from zolpidem or zaleplon with longer t1/2 ( 6 hrs)

z drug

16

Recommendations for Treatment of Insomnia

Nondrug measures emerging as preferred treatment

Cognitive behavioral therapy – alone or with drug

Drug treatment also first-line option

Nonbenzodiazepines (Z-drugs, ramelteon)

Shorter-acting BDZs (temazepam)

Lowest effective dose – taper when possible

Address underlying causes: sleep apnea, pain, restless leg syndrome, anxiety or depression

Check that stimulating (caffeine, decongestants, stimulants, SSRIs) or sleep-interrupting meds (diuretics) not taken hs

17

Serotonin receptor antagonist and reuptake blocker
Decrease in REM sleep – no change or increase in SWS
ADRs: Oversedation, orthostasis (α-1 block), priapism (rare but serious)
Role: An antidepressant – very sedating and improves sleep continuity
No concerns with tolerance or dependence if abuse concerns with patient
Often used empirically for insomnia, but efficacy in non-depressed patients uncertain

Trazodone

18

Agonist at melatonin receptors
MT1 (induce sleepiness) and MT2 (regulate circadian rhythms)
ADRs (

Ramelteon

19

• Antagonist at CNS histamine-H1 and muscarinic receptors
• ADRs: Generally minimal, BUT antimuscarinic actions can be troublesome, especially in elderly
• Role
Minimally effective, generally NOT recommended long-term
Can see tolerance after > 10 days use – consider “off” night after 3 days of use to reduce tolerance

Diphenhydramine - Doxylamine

20

Both benzodiazepines (e.g., temazepam [Restoril]) and non-benzodiazepines (e.g., zolpidem [Ambien]) are used in the treatment of insomnia. All of the pharmacologic properties listed below are shared by both classes of drugs, except that only zolpidem:


Produces additive CNS depression if taken with ethanol- yes
Can produce tolerance and dependence (controlled substance)- z less but can sched 4
Has a high therapeutic index relative to barbiturates- both
Can cause anterograde amnesia- both
Binds selectively to GABA receptors containing the α1 subunit- only z drug ***