Sedatives

Benzodiazepine

• PAM-cakes: "-pam" suffix of benzodiazepines (e.g. diazepam, lorazepam, oxazepam)

• Fast ox: oxazepam (a short-acting benzodiazepine)

• "All A.M.": "-olam" suffix of short-acting benzodiazepines (triazolam, alprazolam, midazolam)

• "Addictive flavor": benzodiazepines have the potential to cause addiction (more common with short-acting agents)

• Liver spot: short acting benzodiazepines are metabolized by the liver (long acting agents form active metabolites) (cirrhosis may lead to over sedation )

• Cab-A: benzodiazepines bind to an allosteric site on the GABA-A receptor (inhibitory)

• CNS light: benzodiazepines potentiate/enhance GABA-A transmission in the CNS

• "Chlo-Rider": the GABA-A receptor is a chloride channel, increased Cl conductance hyperpolarizes and inhibits depolarization

• "Take it easy": GABA (with glycine) is a major inhibitory neurotransmitter in the CNS

• "Open more frequently": benzodiazepines increase the frequency of ion channel opening

• Alcoholic on Cab-A: alcohol binds the GABA-A receptor at a separate allosteric site

• Hangover special: benzodiazepines treat alcohol withdrawal

• Long tapering flag: long-acting benzodiazepines (e.g. diazepam, chlordiazepoxide, flurazepam) are useful in the treatment of alcohol withdrawal

• Ivy: IV administration of benzos is useful for the management of alcohol withdrawal, seizures, and anesthesia

• Alcohol withdrawal symptoms (8-12 hours) - insomnia, tremulousness, anxiety, autonomic instability

• Alcohol withdrawal symptoms (12-48 hours) - seizures

• Alcohol withdrawal symptoms (48-96 hours) - delirium tremens (fever, disorientation, severe agitation)

• Status epilepticus (SE) is an epileptic seizure of greater than five minutes or more than one seizure within a five-minute period

• Unplugging jackhammer: benzodiazepines treat status epilepticus

• Intubated customer: IV benzos can be used in general anesthesia (muscle relaxation, amnesia)

• "Lite": IV benzos can induce conscious sedation for minor procedures and surgeries

• Question mark hat: benzodiazepines can cause anterograde amnesia (useful during conscious sedation)

• Sleeping customer: benzodiazepines treat insomnia (not first line due to side effect of physical dependence)

• Crying kid in pajamas: benzodiazepines treat parasomnias in children (e.g. sleepwalking, night terrors)

• Relaxing chair: benzodiazepines treat spasticity caused by upper motor neuron disorders (e.g. MS, stroke, spinal cord trauma, tetanus)

• Anxious customer: benzodiazepines treat generalized anxiety disorder (GAD) (SSRIs and SNRIs are first line)

• The Scream: benzodiazepines treat panic disorder (SSRIs and SNRIs are first line)

• All are welcome: benzodiazepines can cause tolerance (downregulation of GABA-A)

• Disoriented old man: elderly patients are more sensitive to the side effects of benzodiazepines (including somnolence, confusion, disorientation)

• Unbalanced stack: benzodiazepines can cause central ataxia (causing falls in the elderly)

• Bee swatter smacking head: benzos should be avoided with 1st gen. antihistamines and other CNS depressants (e.g. alcohol, barbs, neuroleptics).

• Decreased CNS with normal vitals

• Barbershop next to Cab-A: barbiturates bind the GABA-A receptor at a separate allosteric site

• Antagonizing fluffy muzzled dog: flumazenil (competitive antagonist at the BZD receptor) reverses benzo induced sedation (but precipitates seizures)

Nonbenzodiazepine hypnotics, melatonin, ramelteon

• 3 Zs: Zolpidem, Zaleplon, esZopiclone (nonbenzodiazepine hypnotics)

• Cab-A: nonbenzodiazepine hypnotics (e.g. zolpidem) bind to an allosteric site on the GABAA receptor

• "Chlo-Rider": the GABAA receptor is a chloride channel

• CNS light: benzodiazepines potentiate GABAA transmission in the CNS

• "Take it easy": GABA (with glycine) is a major inhibitory neurotransmitter in the CNS

• Grabbing same cab handle: nonbenzodiazepine hypnotics and benzos bind to the same allosteric site on GABA-A

• Alcoholic on Cab-A: alcohol binds the GABAA receptor at a separate allosteric site

• Barbershop next to Cab-A: barbiturates bind the GABAA receptor at a separate allosteric site

• " fast": zaleplon and zolpidem have a rapid onset of action

• Quick jump and fall: nonbenzodiazepine hypnotics have a short duration of action

• Liver spot: zaleplon and zolpidem are rapidly metabolized by the liver, P450 system

• "Fall asleep": zaleplon and zolpidem treat sleep onset insomnia (eszopiclone has the longest half life and is effective for both sleep onset and sleep maintenance insomnia)

• Sleeping: nonbenzodiazepine hypnotics treat insomnia

• Disoriented old man: elderly patients are more sensitive to the side effects of nonbenzodiazepine hypnotics (e.g. cognitive impairment and delirium)

• Unbalanced stack: nonbenzodiazepine hypnotics can cause central ataxia (causing falls in the elderly)

• "Cannot combine with other CoupoNS": avoid use with other CNS depressants

• Bee swatter smacking head: avoid use with other CNS depressants (e.g. 1st generation antihistamines, alcohol, benzos, barbs)

• "not tolerated": nonbenzodiazepine hypnotics are less likely to cause tolerance

• "break bad habits": nonbenzodiazepine hypnotics are less likely to cause withdrawal symptoms and dependence

• Antagonizing fluffy muzzled dog: flumazenil (competitive antagonist at the BZD receptor) reverses the sedative actions of nonbenzodiazepine hypnotics (but precipitates seizures)

• "melt away": melatonin and ramelteon (a melatonin receptor agonist) treat insomnia

• Dark and light: melatonin receptors maintain circadian rhythm

• Nucleus above "X": MT1 and MT2 melatonin receptors are located in the suprachiasmatic nucleus of the hypothalamus (activated by ramelteon)

• Peacefully sleeping elderly: ramelteon has few side effects and are safe in geriatric patients

Barbiturates

• Cab-A: barbiturates bind to an allosteric site on the GABA-A receptor

• Ben's diner next to Cab-A: benzodiazepines bind the GABA-A receptor at a separate allosteric site

• Alcoholic on Cab-A: alcohol binds the GABA-A receptor at a separate allosteric site

• "Chlo-Rider": the GABA-A receptor is a chloride channel

• CNS light: barbiturates potentiate GABA-A transmission in the CNS

• "Take it easy": GABA (with glycine) is a major inhibitory neurotransmitter in the CNS

• "Open longer": barbiturates increase the duration of opening of the GABAA receptor

• Long tapering flag: barbiturates have long durations of action ("hangover" effects more common)

• "The ol' quick shave": thiopental has a rapid onset and short duration of action (highly lipid soluble) <30 s

• Intubated customer: IV thiopental can be used for induction of anesthesia

• Ivy: IV administration of barbiturates is useful for induction of anesthesia (thiopental) and management of seizures (phenobarbital)

• Hair "redistributed" onto arms and belly: plasma levels of thiopental decrease rapidly due to redistribution to skeletal muscle and adipose

• Decay line: rapid decay of plasma thiopental levels (due to redistribution)

• Brief peak: rapid accumulation of thiopental in brain tissue and rapid redistribution

• Growth line: rapid accumulation of thiopental in skeletal muscle and adipose (recovery from anesthesia)

• Unplugging jackhammer: IV phenobarbital can be used to treat seizures

• Perm is done!: primidone (a barbiturate used to treat seizures and essential tremor)

• Tremulous hand: primidone treats essential tremor (first line with propranolol)

• Collapsed heart and lungs: barbiturates can cause profound cardiac and respiratory depression

• Fainting: barbiturates can cause hypotension

• Brain hair dryer: barbiturates can cause severe CNS depression (e.g. coma) and should be avoided in the elderly

• "All are welcome": chronic barbiturate use leads to tolerance

• "Addicted": chronic barbiturate use leads to physical dependence

• Activated chrome bumper: barbiturates (e.g. phenobarbital) are potent inducers of the cytochrome P450 system