CHAPTER 9: Anxiolytic and Hypnotic Drugs- Barbiturates, etc. Flashcards
Flumazenil- GABA RECEPTOR ANTAGONIST
- 3 purposes
- IV only
3 purposes: - treat benzo overdose
- reverse sedation caused by benzo in adjunct w anesthesia
- reverse sedation after medical procedures
Barbiturates: purposes
-depress CNS
-inhib neuronal impulse
-conduction in RAS
-depress cerebral cortex
-depress motor output
CAUSE: sedation, hypnosis, anesthesia, coma (HIGH DOSE)
Barbiturates: pharmacokinetics
- well absorbed
-reach peak in 20-60 mins - metab in liver
duration of action:
thiopental: act in seconds, 30 mins DOA
pentobarbital, secobarbital, amobarbital: short acting
phenobarbital: DOA greater than a day
Barbiturates: adverse effects
CNS: drowsy, impair concentration, mental/physical sluggy
HANGOVER: tired after waking, impaired normal func, nausea and dizzy
WITHDRAWAL: tremor, anxiety, weak, restless, nausea/vomit, seizures, delirium, cardiac arrest, veritgo
OTHER Anxiolytic Drugs
- treat chronic anxiety
- first line for PT w addiction/dependance concerns
- use alone or w benzo during first week of treatment, after 4-6 week taper benzo
OTHER anxiolytics: Busprione
- for GAD
- no effective short term treatments
- no action of GABA receptors
- act on 5-HT2a receptors
- reduce anxiety w out many CNS side effect
-absorb in GI, PO drug, half life 2-3 hr
NO sedative, anticonvulsant, muscle relaxant properties–> NO hangover effect
OTHER hypnotic drugs
zaleplon and zolpidem, eszopiclone, antihistamines, amelteon and tasimelteon, suvorexant
OTHER hypnotics: Z drugs
- use
- metabolism
- properties
eszopiclone, zaleplon, zolpidem
- non benzo treatment for insomnia, bind to GABA-A, selective for a1
no anticonvul, muscle relax, few withdrawal effect, minimal rebound insomnia, little tolerance
METABOLISM
- hepatic oxidation by CYP450
OTHER hypnotics: Z drugs
- adv effects
- headache, dizzy, anterograde amnesia, next morning impairment
-sleep walk, sleep drive - doesn’t affect sleep stages a lot
all 3 are controlled substances
OTHER hypnotics: antihistamines
- diphendyramine, hydroxyzine, doxylamine
- sedating properties, less useful than benzo or nonbenzos
ex) benadryl
OTHER hypnotic drugs: ramelteon and tasimelteon
- selective agonists at MT1 and MT2 subtypes of melatonin receptors
- little dependence or withdrawal
other hypnotics: ramelteon and tasimelteon
-adv effects
ram: dizzy, fatigue, somnolence (too much sedation)
tasi: headache, abnormal dreams, inc liver function, upper resp infections
BOTH CYP450 isoforms
