Pharm - Sedatives and Hypnotics Flashcards
list the benzodiazepine antagonist
flumazenil
-pam suffix indicates what type of drug
benzodiazepines
-barbital indicate what type of drug
bartbiturates
compare sedatives to hypnotic drugs
sedatives: decrease CNS activity, moderates excitement, calms pt
hypnotic drug: produces drowsiness, facilitates onset and maintenance of sleep
- more pronounced depression of the CNS
MOA benzodiazepines
binds to GABA-A receptor and enhances GABA’s effects
–> chloride influx –> hyperpolarization –> fewer number of action potentials –> CNS depression
describe the advantages of benzos
1) high therapeutic index
2) antagonist available for OD
3) low risk of drug-drug interactions
4) minimal effect on CV or autonomic system
describe the disadvantages of benzos
1) risk of dependence
2) depression of CNS function
3) amnestic effects
4) bad when combined with alcohol
describe the half life, active metabolite status, and rate of onset for Diazepam
half life: >100 hours
active metabolites: yes
rate of onset: very fast
describe the half life, active metabolite status, and rate of onset for Alprazolam
half life: 12-15 hrs
active metabolites: insignificant
rate of onset: fast
list the short to intermediate acting benzos
1) alprazolam
2) oxazepam
3) temazepam
4) midazolam
5) traizolam
list the intermediate to long acting benzos
1) diazepam
2) lorazepam
3) clonazepam
indications for Alprazolam
- anxiety disorder
- panic disorder
contraindications for Alprazolam
- pts w/ acute narrow angle glaucoma
- w/ ketoconazole and itraconazole
indications for midazolam
preoperative sedation/anxiolysis/amnesia
black box warning for midazolam
respiratory depression
indications for diazepam
- management of anxiety disorders and for short term relief of sx of anxiety
- also used in acute alcohol withdrawal
how does milk to moderate cirrhosis affect use of diazepam
the average half-life is increased from 2-5 fold
contraindications for diazepam
1) peds pts under 6 months
2) myasthenia gravis
3) respiratory insufficiency
4) severe hepatic 3 insufficiency
5) sleep apnea
6) acute narrow angle glaucoma
warnings for diazepam
not recommended in tx of psychotic pts and don’t use w/ alcohol
indications oxazapam
anxiety, anxiety w/ depression, and acute alcohol withdrawal
indications triazolam
short term tx of insomnia (7-10 days)
indications chlordiazepoxide
1) management of anxiety disorders or for short term relief of anxiety
2) alcohol withdrawal
4) preoperative apprehension and anxiety
indications flurazepam
long acting hypnotic agent useful for tx of insomnia
indications lorazepam
seizure disorders like epilepsy
- can also be used before surgery to relieve anxiety
indications buspirone
tx of generalized anxiety disorder
***takes more than a week to become establihsed
indications flumazenil
complete or partial reversal of sedative effects of benzos
- management of ODs
MOA flumazenil
competitively inhibits activity at benzo recognition site on GABA receptor
black box warning flumazenil
seizures most frequently in pts who have been on benzos for long time
MOA barbituates
binds to GABA-A receptor and increases duration of GABA gated channel openings
–> chloride influx –> hyperpolarization –> decreased number of action potentials –> CNS depression
compare the typical indications for ultra short acting, short acting, and long acting barbiturates
ultra short: anesthesia
short: insomnia
long: seizures
indications thiopental
1) sole anesthetic agent for brief procedures
2) induction of anesthesia prior to other anesthetic agents
3) supplements regional anesthesia
4) hypnosis during balanced anesthesia w/ other agents
5) control convulsive states during or following anesthesia
6) increase intracranial pressure in neurosurgical pts
indications secobarbital
hypnotic for the short term tx of insomnia (loses effectiveness after 2 weeks)
contraindications secobarbital
marked impairment of liver, respiratory dz
indications phenobarbital
sedative or hypnotic
contraindications phenobarbital
pts with history of manifest or latent porphyria
MOA ramelteon
full agonist at MT1 and MT2 melatonin receptors
metabolism of ramelteon
metabolized by CYP1A2
adverse effects ramelteon
dizziness, somnolence, fatigue, endocrine changes
indications ramelteon
insomnia characterized by difficulty with sleep onset
MOA zaleplon
interacts with GABA-benzodiazapine receptor complex (but is not a benzo)
indications zaleplon
short term tx of insomnia
indications zolpidem
short term tx of insomnia characterized by difficulties with sleep initiation
indications eszopiclone
insomnia
indications meprobamate
anxiety disorders or for short term relief of sx of anxiety
MOA meprobamate
slowing activity in brain to allow for relaxation
indications chloral hydrate
short term use as sedative or sleep med