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Flashcards in Other Sedatives Deck (15):
1

Describe H1 histamine antagonists

Diphenhydramine, doxylamine, hydroxyzine
Anticholinergic actions
Mild insomnia
Tolerance but no dependence or abuse

2

Describe melatonin

Hormone synthesized in the pineal gland
Controls circadian, seasonal, and reproductive rhythms
Normally released prior to induction of sleep
Decreases sleep latency, increases sedation
Resets clock in jet-lag, late-shift workers, elderly
Very few side effects, available OTC

3

Describe Ramelteon

MT1 and MT2 receptor agonist (melatonin receptors)
Similar efficacy as melatonin but product quality better regulated

4

Describe suvorexant

Hypocretin/orexin antagonist
Approved for insomnia in August 2014

5

Describe GHB

Naturally occurring fatty acid
Synthesized, stored, released like a NT
Metabolized from GABA
high affinity, NA dependent transporter specific for GHB
Highest in hippocampus, basal ganglia, and hypothalamus
Activates GHB receptor
---G-protein coupled to IP3 and DAG production
---Selective antagonists
High doses activate GABA-B receptor

6

What are GHB CNS effects

Sedation
Catalepsy - decrease nigrostriatal dopamine release
Euphoria - increase mesolimbic dopamine at higher doses
Increase growth hormone release

7

What is the therapeutic use of GHB

Approved to treat narcolepsy
Decreases sleep latency, increases sleep time
Does not disrupt sleep cycles
Alleviates daytime drowsiness
Some tolerance after repeated high dose use
No evidence of dependence

8

What are side effects of GHB?

Dizziness, mental clouding
Abuse liability increased by ethanol and other sedatives
Overdose usually in association with other drug use

9

Describe Pre-Gabalin and Gabapentin

Structural analogs of GABA
No activity at any GABA receptors or transporters
Anticonvulsants, relieves neuropic pain/fibromyalgia
Blocks VGCC - decreases pain neurotransmission
Some sedative side effect
Off label use for depression, mania, anxiety, insomnia

10

Describe cyclobenzaprine

Used for skeletal spasms, fibromyalgia

11

Describe metaxalone

Used as a muscle relaxant, MOA unknown

12

Describe carisprodol

Prodrug of meprobamate

13

Describe ketamine

Inhibits NMDA receptor, binds phencyclidine site

Dissociative anesthetic - no complete loss of conciousness
Clinically used as general anesthetic IV
Increases BP
No respiratory effect
Less sensory distortion/euphoria than phencyclidine
Some dysphoria during recovery, less in children

Low doses abused with ethanol as a sedative

14

What are treatment options for nicotine?

Nicotine itself
Nicotine antagonists/partial agonists - mecamylamine, varenicline
Clinidine - offsets adrenergic stimulation during w/d
Bupropion - DA and NE uptake inhibitor
Gamma-vinyl GABA - irreversible inhibitor of GABA-T

15

What are treatment options for stimulant addiction?

Cold turkey
Substitution detoxification - bupropion
Gamma-vinyl GABA, baclofen, other GABA B agonists