Sedatives/Hypnotics Flashcards
chlordiazepoxide
chlordiazepoxide: Librium
Anxiety, alcohol withdrawal, pre-anaesthetic
long acting benzo
(active metabolites)
alprazolam
alazopram: Xanax
anxiety
intermediate acting benzo
(active metabolites)
clonazepam
clonazepam: Klonopin
SEIZURES, mania, movement disorders
intermediate acting benzo & centrally acting spasmolytic
diazepam
diazepam: Valium
anxiety, STATUS EPILEPTICUS,muscle relaxant, pre-anaesthetic
long acting benzo & centrally acting spasmolytic
(active metabolites)
estazolam
estazolam: Prosom
insomnia
intermediate acting benzo
flurazepam
flurazepam: Dalmane
insomnia
intermediate acting benzo
(active metabolites)
lorazepam
lorazepam: Ativan
anxiety, STATUS EPILEPTICUS, pre-anaesthetic
intermediate acting benzo
midazolam
midazolam: Versed
pre-anaesthetic, intraoperative medication
short acting benzo
quazepam
quazepam: Doral
insomnia
long acting benzo
(active metabolites)
temazepam
temazepam: Restoril
insomnia
intermediate acting benzo
triazolam
triazolam: Halcion
insomnia
short acting benzo
(active metabolites)
flunitrazepam
flunitrazepam: Rohypnol
date rape drug
long acting benzo
How do benzodiazepines work?
increase GABA(a) receptor-mediated inhibition (increase Cl- conduction -> hyperpolarize neuron -> CNS depression)
Adverse effects of benzodiazepines
- altered sleep
- CNS depression: impaired mental/motor function, ataxia…
- withdrawal sx: anxiety, nausea, seizures
- tolerance
- abuse
How are benzodiazepines metabolized?
hepatic: CYP3A4 glucuronidation –> urinary excretion
some are active metabolites
zolpidem
zolpidem: Ambien
increase sleep duration
- withdrawal: anxiety, tremor, agitation, rebound insomnia, seizures
short term (8-10d) non-benzo
zaleplon
zaleplon: Sonata
help fall asleep
- risk of addiction in long term use
short term (<10d) non-benzo
eszopiclone
eszopiclone: Lunesta
increase sleep duration
- potential for tolerance, dependence, abuse
long term (up to 6mo) non-benzo
Advantages of non-benzodiazepines over benzodiazepines
- less rebound insomnia/withdrawal symptoms
- lower potential for tolerance, dependence, abuse
How do non-benzodiazepines (z-drugs) work?
bind BZ1 receptors of GABA receptor-Cl channel complex
flumazenil
flumazenil: Romazicon
reverse action of benzodiazepines (competitive antagonist)
also cause:
- agitation, confusion, dizziness, nausea
- withdrawal sx, seizures in benzo overdose/dependence
ramelteon
ramelteon: Rozeram
melatonin agonist (MT1/MT2)
no CNS depression
CYP1A2
Advantages of Melatonin agonist
- no CNS depression
- no motor/cognitive impairment
- little withdrawal sx/rebound insomnia
- can be used long term
- not controlled, no abuse potential
Adverse effects of Melatonin agonist
- increased serum prolactin
- decreased testosterone
buspirone
partial agonist at serotonin receptor
: anxiolytic
less abuse potential than benzos
no CNS depression
doxylamine
doxylamine: Unisom (and others)
OTC sleep aid
diphendydramine
diphenhydramine: Benadryl (and others)
OTC sleep aid
How does alcohol affect sleep?
hypnotic:
- initial CNS depression
- later rebound excitation (disrupts sleep)
GHB
gamma-hydroxybutyrate/sodium oxybate:
metabolite and precursor for GABA
: cataplexy, narcolepsy
- addictive, abuse risk: hallucinogenic, euphoric
What do spasmolytics do and what conditions can they treat?
muslce relaxants: tx for spasms
- MS
- ALS
- spinal cord transection
- cerebral palsy
- stroke
- local muscle trauma
Centrally acting spasmolytics
- diazepam/clonazepam
- baclofen
- tizanidine
baclofen
baclofen: Lioresal
centrally acting spasmolytic, less sedation than benzos
GABA(b) receptor agonist
tizanidine
tizanidine: Zanaflex
centrally acting spasmolytic
alpha-2 adrenergic agonist (pre-/post-synaptic inhibition of motor neurons)
dantrolene
dantrolene: Dantrium
direct acting spasmolytic
causes muscle weakness (not for ALS)
can treat malignant hyperthermia
