Sedative Hypnotic Drugs Flashcards
Benzodiazepenes
- binding site b/w alpha and gamma subunit on the GABAa receptor (BZ site)
- increases affinity of GABA for the GABA binding site
INDICATIONS
acute anxiety
panic attacks
generalized anxiety disorder
insomnia - decreased REM sleep
muscle relaxants
INTERMEDIATE ACTING BENZODIAZEPINES
LATE CLN
Lorazepam
Alprazolam
Temazepam
Estazolam
Clonazepam
Lormetazepam
Nitrazepam
Benzodiazepine SE
drowsiness
dec conc
dec reaction time
fast speech
ANTEROGRADE AMNESIA
ataxia
respi depression — COMA
Used for benzodiazepine overdose
FLUMAZENIL
Barbiturate
-binds to GABAa receptor of the alpha or beta subunit
-increases Chloride action DURATION
-deceases activity of excitatory NT - Ach, glutamate
-HIGHER DOSES - can mimic GABA - profound CNS depression
-lower therapeutic index than benzodiazepenes - toxic dose is not much higher than the therapeutic dose
INDICATIONS
acute anxiety attacks
preop sedation
dec cerebral blood flow and induce coma
Barbiturates SE
drowsiness
sleepiness
memory and attention impairment
respiratory depression
CI - porphyria
Antidote for Barbiturate overdose
NaHCO3
Non-Benzodiazepine Hypnotics
-alpha 1
for INSOMNIA
IMIDAZOPYRIDINE
Zolpidem
Zaleplon
Eszopiclone
Causes anterograde amnesia
Midazolam
Benzodiazepines used for anxiety
Alprazolam (Xanax)
Clonazepam, Lorazepam, Diazepam
Benzodiazepine used for muscle spasticity
Diazepam
Benzodiazepines used for ethanol withdrawal
Diazepam
Chlordiazepoxide
Melatonin Receptor Agonist
Activates MT1 and MT2 receptors in SUPRACHIASMATIC NUCLEUS
Ramelteon
5-HT agonist
partial agonist at 5-HT receptors and D2 receptors
Buspirone
for generalized anxiety states
SE
*GI distress
*tachycardia
*paresthesia
5 Principle Pharmacologic Effects of Benzodiazepines
Anxiolysis
Sedation and Hypnosis
Anticonvulsant Actions
Spinal Cord Mediated Skeletal Muscle Relaxation
Anterograde Amnesia
