Sedative-hypnotics Flashcards
what is a short acting benzo
triazolam
what is a intermediate acting benzo
alprazolam
what is a long acting benzo
flurazepam
what is a ultra-short acting barbiturates
thiopental
–used for anesthesia
what is a short acting barbiturates
secobarbital
–used for insomnia
what is a long acting barbiturates
phenobarbital
–used seizures
list of misc agents
buspirone
eszopiclone
zaleplon
zolpidem
list of benzos
alprazolam chlordiazepoxide clonazepam clorazepam diazepam flurazepam lorazepam midazolam oxazepam triazolam
list of barbiturates
-barbital
thiopental
what is flumazenil
benzo antagonist
definition of a sedative
drugs that decreases CNS activity, moderates excitement, and calms the recipient
definition of hypnotic
drugs that produce drowsiness and facilitates the onset & maintenance of sleep & from which the recipient can be aroused easily
MOA of benzos
act on GABAa receptors
- -increase Cl influx, cause hyperpolarization, decreased # of action potentials
- -cause sedation, hypnotic effects, muscle relaxation, anxiolytic & anticonvulsant effects
MOA of barbiturates
act on GABAa receptors
- -cause wide spectrum of effects: mild sedation to anesthesia
- -increase chloride influx, causes hyperpolarization, decreased # of action potentials
MOA of misc sedative-hypnotics
act on multiple receptors: GABAa, melatonin
–used as sleep aids, tx of delirium, anxiety, seizures
advantages & disadvantages of using benzos for anxiety
advantages: high therapeutic index, antagonist available (flumazenil), low risk drug interactions, minimal CV effect
disadvantages: risk of dependence, CNS depression, amnestic effects
dIazepam
1/2 life: >100 hrs
active metabolites: yes
pathway of metabolism: oxidation
rate of onset via oral: very fast
alprazolam
1/2 life: 12-15 hrs
active metabolites: not important
pathway of metabolism: oxidation
rate of onset via oral: fast
cumulative toxicity
benzos with long 1/2 lives are more likely to cause cumulative effects (excessive drowsiness) with multiple doses
indications for alprazolam
management of anxiety disorder, or short-term relief of symptoms
also tx of panic disorder
warnings: dependence & withdrawal rxs including seizures
midazolam drug profile
- -given IM or IV
- -IV for sedation/anxiolysis/amnesia prior to procedures
- -warnings: assoc with resp depression & arrest
diazepam drug profile
- -exerts anxiolytic, sedative, muscle relaxant, anticonvulsant
- -has distribution phase (1/2 life 48 hours) followed by terminal elimination phase (1/2 life up to 100 hrs)
- -1/2 life increased in mild-mod cirrhosis
- -management of anxiety disorders
- -can be used for acute alcohol withdrawal to relieve agitation & tremor
- -contraindicated in myasthenia gravis, sleep apnea,
- -WARNING: not recommended for tx of psychotic pts
When is oxazapam used
tx of anxiety, anxiety with depression, and acute alcohol withdrawal
when is triazolam used
short term tx of insomnia (7-10 days)
BB warning: if used with opioids may result in sedation, resp depression, coma, and death
when is chlordiazepoxide used
management of anxiety disorders or for short term relief of symptoms. acute alcohol withdrawal, preoperative apprehension
BB warning:if used with opioids may result in sedation, resp depression, coma, and death
when is flurazepam used
long acting hypnotic used for tx of insomnia
when is lorazepam used
tx of seizure disorders
can be used before surgery for anxiety
flumazenil
- -benzo receptor antagonist
- -complete or partial reversal of sedative effects of benzos when general anesthesia has been induced or in management of benzo overdose
- -warning: has been assoc with occurence of seizures
what are barbiturates
tx of anxiety, epilepsy, to induce sleep, and as anesthetics
- -extreme cases of insomnia
- -seizures that are unresponsive to other, less toxic, agents
- -induction of anesthesia
- -in combo with acetaminophen & caffeine for tension HA
- -counteract the stimulant effects from drugs such as cocaine & meth
thiopental drug profile
administered by IV
as the sole anesthetic agent for brief 15 min procedures
for control of convulsive states during or following inhalation anesthesia, local anesthesia, or other causes
AE:
–resp depression, myocardial depression, cardiac arrhythmias, prolonged somnolence
secobarbital drug profile
Indications:
- -hypnotic, short-term tx of insomnia- loses effectiveness after 2 wks
- -preanesthestic
phenobarbital drug profile
Indications:
- -used as a sedative or hypnotic
- -contraindicated in those with history of porphyria
- -administered with caution in those who are mentally depressed, have suicidal tendencies, or a hx of drug abuse
benzos can be used for insomnia but cause what?
daytime sedation & pts may develop anterograde amnesia & tolerance
What drugs are used for insomnia?
zolpidem, zaleplon, and eszopiclone
MOA of newer hypnotics
binds to GABAa receptors that contain a1 subunit
- -increase chloride influx, increase hyperpolarization, decrease # of action potentials
- -only approved for sleep disorders
- -no anxiolytic, anesthetic, anticonvulsant, muscle relaxing, resp or cv effects
DRUGS: eszopiclone, zolpidem, zaleplon
Buspirone drug profile
- -approved for tx of generalized anxiety disorder
- -anxiolytic effects may take more than 1 wk to become established
zaleplon drug profile
- -short term tx of insomnia
- -contraindicated in pt with hypersensitivity to drug
zolpidem drug profile
- -indicated for short term tx of insomnia characterized by difficulties initiating sleep
- -warnings: severe anaphylactic reactions, worsening of depression
- -drug interactions: CNS depressants
ramelteon drug profile
- -indicated for tx of insomnia characterized by difficulty with sleep onset
- -melatonin receptor agonist
eszopiclone drug profile
- -indicated for tx of insomnia– decrease sleep latency & improve sleep maintenance
- -warnings: CNS depressant effects
- -SE: unpleasant taste, somnolence, resp infection, HA
meprobamate drug profile
- -indicated for tx of anxiety disorders or for short-term relief of symptoms of anxiety
- -works by slowing activity in the brain to allow for relaxation
chloral hydrate drug profile
–short term use as a sedative or sleep medicine
The failure of insomnia to remit after how many days of tx may indicate the presence of a primary psychiatric &/or medical illness that should be evaluated?
7-10 days
