Sedative and Hypnotic Drugs - Iszard Flashcards
- alprazolam
- chlordiazepoxide
- clonazepam
- clorazepate
- diazepam
- flurazepam
- lorazepam
- midazolam
- oxazepam
- triazolam
benzodiazepines
flumazenil
benzodiazepine antagonist
amobarbital butaparbital pentobarbital phenobarbital secobarbital thiopental
barbiturates
buspirone chloral hydrate eszopiclone meprobamate ramelteon zaleplon zolpidem
misc/newer sedative-hypnotic drugs
triazolam
short action benzo
alprazolam
intermediate action benzo
flurazepam
long action benzo
thiopental
ultra-short action barbiturate
secobarbital
short action barbiturate
phenobarbital
long action barbiturate
drug that decreases CNS activity, moderates excitement, calms the recipient
sedative
drug that produces drowsiness and facilitates the onset and maintenance of sleep, from which the recipient can be aroused easily
hypnotic
NOTE: hypnotic effects involve more pronounced depression of the CNS, which can be achieved with many drugs in this class by increasing the dose
what is the relationship between benzodiazepines and barbiturates on CNS effects?
benzodiazepines level off around anesthesia (don’t cause medullary depression or come like barbiturates can)
- act on GABA-A receptors
- cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects
benzodiazepines
- act on GABA-A receptors
- cause a wide spectrum of effects: mild sedation to anesthesia
barbiturates
- act on multiple receptor systems: GABA-A and melatonin
- used as sleep aides, treatment of delirium, anxiety, seizures
miscellaneous sedative-hypnotics
hepatic metabolism and excretion via kidney
- CYP3A4 (phase I) ad glucuronidation (phase II)
- binds the GABA-A receptors and enhances GABA’s effects
benzodiazepines
NOTE: risk of dependence and tolerance
what are the disadvantages of benzodiazepines?
risk of dependence, depression of CNS function (especially bad if combined with alcohol!), amnesia
what is the half life of diazepam?
> 100 hours KNOW this
- has active metabolites
- half life is increased in mild/moderate cirrhosis, can be up to 500 hours!
what is the half life of alprazolam?
12-15 hours
- insignificant active metabolites
extensively metabolized in humans, primarily CYP3A4
- indicated in anxiety disorder and panic disorder
- may be used in pts with open angle glaucoma
alprazolam
which drug is contraindicated with ketoconazole and itraconazole?
alprazolam
- since these meds significantly impair CYP3A4
given IM or IV as sedation agent prior to procedures
- induction of general anesthesia
- black box warning associated with respiratory depression/arrest, especially when used in noncritical care settings
midazolam
this drug exerts anxiolytic, sedative, muscle relaxant, anticonvulsant and amnestic effects d/t GABA facilitation
- indicated for management of anxiety
- may be used in acute alcohol withdrawal
diazepam
when is diazepam contraindicated?
myasthenia gravis, severe respiratory insufficiency, severe hepatic insufficiency, and sleep apnea syndrome
what is the warning associated with dizepam?
- NOT recommended in tx of psychotic patients
- pts should NOT take with alcohol (d/t CNS depressant)
what drug is used in the treatment of anxiety, anxiety with depression and acute alcohol withdrawal?
oxazapam
what drug is indicated for the short-term treatment of insomnia (generally 7-10 days)
- black box warning concomitant use with opioids can result in profound sedation, respiratory depression, coma and death
triazolam
what drug is used from anxiety management, short term relief of sx of anxiety, withdrawal sx of acute alcoholism, and preoperative apprehension/anxiety
chlordiazepoxide
- also has black box warning against use with opioids
what drug is a long acting hypnotic agents, useful for the treatment of insomnia characterized by difficulty falling asleep, frequent nocturnal awakenings and/or early morning awakening
flurazepam
NOT used long-term! if insomnia doesn’t stop after 7-10 days, it may indicate a primary psychiatric illness is present
what drug is used in the treatment of seizure disorders (epilepsy)
- also used before surgery and medical procedures
lorazepam
- approved for the tx of generalized anxiety disorder
- effects may take more than a week
- does not cause sedation, hypnotic, euphoric, anticonvulsant or muscle relaxant effects
- extensive metabolism by CYP3A4
buspirone
what drug is indicated for the complete or partial reversal of the sedative effects of benzos, and the management of benzodiazepine overdose?
flumazenil (benzo antagonist)
- black box warning can cause seizures in patients showing signs of serious cyclic antidepressant overdose
what are the specific conditions that barbiturates are limited to treating?
- extreme insomnia
- seizures unresponsive to other meds
- induction of anesthesia
- in combination w/acetaminophen and caffeine to relieve tension headaches
- used to counteract the stimulant effects from coke and meth
these drugs bind the GABA-A receptor, increasing the duration of GABA-gated channel openings
- can induce CYP450 enzymes
barbiturates
- *risk of dependence and tolerance**
- *overdose can cause death**
given IV as sole anesthetic for brief (15 min) procedures or prior to administation of other anesthetic agents
thiopental (truth serum)
what are the adverse reactions of thiopental?
respiratory depression, myocardial depression, cardiac arrhythmias, prolonged somnolence and recovery
hypnotic, used for short-term treatment of insomnia or preanesthetic
- contraindicated in pts w/hypersensitivity to barbiturates, or a hx of manifest or latent porphyria, marked impairment of liver function, or respiratory disease
secobarbital
warning: failure of insomnia to remit after 7-10 days of treatment ay indicate psychiatric illness that should be evaluated
what drug is indicated for use as a sedative or hypnotic
- contraindicated in patients with hx of manifest or latent porphyria
phenobarbital
NOTE: should be administered with cause to pts who are mentally depressed, have suicidal tendencies, or hx of drug abuse
**has been shown to induce liver microsomal enzymes, thus increasing or altering the metabolism of barbiturates and other drugs
what drugs are used to treat insomnia?
benzodiazepines
NOTE: cause daytime sedation and patients may develop anterograde amnesia and tolerance
tx of insonmia
- highly effective, rapid onset, minimal hangover effects
zolpidem, zaleplon, eszopiclone
- zolpidem has biphasic release forumla for sustained sleep maintenance
- eszopiclone has longest half life
what drug is an agonist at melatonin receptors MT-1/2
- produces significant sedation
ramelteon
- metabolized by CYP1A2
hepatic metabolism and excretion via kidney (CYP3A4)
- relatively short half lives (<6hrs) so useful as hypnotics rather than sedatives
- binds GABA-A that contain a1 subunit
- ONLY approved for tx of sleep disorders
sleep aids
- eszopiclone, zolpidem, zaleplon
nonbenzo hypnotic agent that interacts with GABA-BZ receptor complex
- indicated for short-term treatment of insomnia
zaleplon
NOTE: if it doesn’t cure insomnia after 7-10 days, consider psychiatric illness
what drug is indicated for short-term treatment of insomnia characterized by difficulties with sleep initiation
zolpidem
NOTE: worsening depression or suicidal thoughts may occur. alcohol NOT recommended d/t CNS depressant effects
what drug is indicated for the treatment of insomnia characterized by difficult with sleep onset
- high affinity for MT-1/2 and selectivity over MT3
- CYP1A2 is major isozyme
ramelteon
what drug is indicated for treatment of insomnia, and has shown to decrease sleep latency and improve sleep maintenance
eszopiclone
- do NOT take with alcohol d/t CNS depressant effects**
- adverse rxns in pts with hepatic impairment, impaired respiratory function, impaired drug metabolism or hemodynamic response
