SEDATIVES / HYPNOTICS

MOA of benzodiazepines

enhances the inhibitory effects of GABA on GABA receptors causing chloride channels to open, hyper polarizing the cell

→ increases the duration of chloride ion channel opening

→ makes neurons less likely to fire

Benzodiazepines

Alprazolam (Xanax), diazepam, lorazepam, and midazolam

Benzodiazepine antagonist

Flumazenil

Clinical application of benzodiazepines

pre-operative sedation and amnesia, alcohol withdrawal syndrome, and skeletal muscle relaxation

Flumazenil clinical use

management of benzodiazepines overdose

Zolpidem MOA

Enhances effects of GABA

Eszopiclone MOA

Enhances the effects of GABA

Clinical use of Zolpidem and Eszopiclone

Sedative-hypnotic and insomnia

Melatonin MOA

Agonist at melatonin receptor

Suvorexant MOA

Inhibitor of orexin 1 and 2 receptors

Suvorexant clinical use

Decreases sleep latency and enhances sleep maintenance

Effects of benzodiazepines on sleep

Decreases sleep latency, increases duration of sleep, decreases number of awakenings

Characterization of barbiturates

Schedule II-IV controlled substances

List of barbituates

Phenobarbital and methohexital

MOA of barbiturates

Binds to HABA receptor sites to facilitate chloride channel opening

Clinical applications of barbiturates

Anesthesia, insomnia, and sedation

Toxicity of barbituates

respiratory depression, CNS depressions, dependance

Hydroxyzine and promethazine MOA

Histamine H1 receptor inverse agonist

Clinical use of Hydroxyzine and promethazine

alternate anxiolytic

Propranolol clinical use

situational anxiety

Side effects of propanolol

sleep problems and GI problems

Diazepam MOA

facilitates GABA

Clinical use of diazepam

spasticity

Side effects of diazepam

sedation, dizziness, ataxia, cognitive slowing, antergrade amnesia

Cyclobenaprine MOA

structurally related to tricyclic antidepressant → inhibits both gamma and alpha motor systems

Clinical application of cyclobenzaprine

muscle spasm of local origin

Baclofen MOA

GABA receptor agonist

Baclofen clinical use

spasticity associated with multiple sclerosis and spinal cord injury

Tizanidine MOA

alpha 2 adrenergic receptor agonist

→ reduces spasticity by increases presynaptic inhibition of motor neurons

Tizanidine clinical application

spasticity (muscle spasms)

Tizanidine adverse effects

Hypotension, sedation, dry mouth, fatigue