Term
| factors that regulate sleep |
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Definition
age
sleep history
drug ingestion
circadian rhythms |
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Term
| factors that regulate sleep-neurotransmitters |
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Definition
catecholamines
serotonin
histamine
acetylcholine
adenosine
GABA |
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Term
| factors that regulate sleep-neuromodulators |
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Definition
growth hormone
prolactin
melatonin
endogenous peptides |
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Term
| ligands acting at the BZD binding site |
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Definition
benzodiazepines
non-benzodiazepines
BZD antagonists
Inverse BZD agonists |
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Term
| ligands acting at other sites |
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Definition
barbiturates
alcohol
GABA blockers
GABA agonist
etomidate and propofol |
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Term
| chlordiazepoxide (Librium) |
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Definition
benzodiazepine
slow elimination rate
1st benzodiazepine
used as an anxiolytic and for alcohol withdrawal
accumulation of metabolites |
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Term
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Definition
benzodiazepines
slow elimination rate
prototypical benzodiazepine
used as an anxiolytic, for alcohol withdrawal, and for treatment of convulsive disorders, accumulation of metabolites |
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Term
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Definition
benzodiazepines
slow elimination rate
used as a hypnotic, accumulation of metabolites |
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Term
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Definition
benzodiazepines
slow elimination rate
used as an anxiolytic, for alcohol withdrawal, and for treatment of convulsive disorders
accumulation of metabolites |
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Term
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Definition
benzodiazepines
slow elimination rate
used as a hypnotic
accumulation of metabolites |
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Term
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Definition
benzodiazepines
slow elimination rate
currently unavailable in the US
used as an anxiolytic |
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Term
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Definition
benzodiazepines
intermediate eliminate rate
withdrawal symptoms can present if abrupt discontinuation occurs, used as n anxiolytic and anesthetic |
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Term
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Definition
benzodiazepines
intermediate eliminate rate
used as an anxiolytic and as a hypnotic |
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Term
clonazepam (Klonopin)
C-IV |
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Definition
benzodiazepines
intermediate eliminate rate
tolerance may develop with prolonged use, used as an anticonvulsant |
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Term
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Definition
benzodiazepines
intermediate eliminate rate
used as an anxiolytic and for alcohol withdrawal |
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Term
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Definition
benzodiazepines
intermediate eliminate rate
used as a short-term hypnotic |
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Term
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Definition
benzodiazepines
intermediate eliminate rate
discontinued
used as a short-term hypnotic |
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Term
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Definition
benzodiazepines
rapid elimination rate
rapid anesthesia |
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Term
| triazolam (Halcion, discontinued) |
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Definition
| used as a short-term hypnotic |
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Term
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Definition
benzodiazepine antagonist
therapeutic use --> BZD overdose
initial dose- 0.2 mg IV over 30 sec, if desired consciousness not obtained increase to 0.3mg IV over 30 sec
max total cumulative dose- 3 mg (usual range 1-3mg)
side effects: induced convulsions, panic attacks, agitation, confusion, nausea and vomiting, headache |
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Term
zolpidem (Ambien, Ambien CR)
C-IV |
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Definition
non-benzodiazepine
short-term treatment of insomnia
with difficulty of sleep-onset
ambien CR for sleep maintenance
"A-minus" and "Zombie pills"
dangerous aid for sexual assault
teen party drug |
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Term
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Definition
non-benzodiazepine
short-term treatment of insomnia
MOA: facilitate GABA-mediated inhibition, act on GABAa receptor-BZ1
rapid acting
rapidly eliminated
little tolerance or dependence
short-term treatment- 7 to 10 days |
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Term
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Definition
non-benzodiazepine
MOA: facilitate GABA
active enantiomer of zopiclone- 50x greater affinity
treatment of insomnia- able to sleep all through the night with fewer interruptions, approved for long-term use (low tolerance over time, based on 6 mo study)
temporary side effect: unpleasant metallic taste |
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Term
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Definition
benzodiazepine
not available in the US
"roofies"
DEA recommends changing to C-I
anterograde amnesia- dangerous aid for sexual assault |
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Term
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Definition
anticonvulsants
phenobarbital (Luminal)
mephobarbital (Mebaral) |
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Term
| short to intermediate acting barbiturates |
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Definition
sedative-hypnotics
amobarbital (Amytal)
butabarbital (Butisol Sodium)
pentobarbital (Nembutal)
secobarbital (Seconal)
aprobarbital (Alurate) |
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Term
| ultra-short acting barbiturates |
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Definition
IV anesthetics
thiopental (Pentothal)
methohexital (Brevital Sodium)
thiamylal (Surital) |
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Term
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Definition
GABAb receptor agonist
skeletal muscle relaxant (treatment of alcoholism) |
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Term
| Gamma-Hydroxybutyric Acid (GHB) |
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Definition
GABAb receptor agonist
central nervous system depressant |
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Term
| Phaclofen, Saclofen, and 2-Hydroxysaclofen |
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Definition
| GABAb receptor antagonist |
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Term
| Xyrem (Sodium Oxybate, GHB) |
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Definition
CI-->illicit use
CII-->medical use
available only to prescribers enrolled in the Xyrem Patient Success Program
-dispensed to the patient through a designated centralized pharmacy
-patients must be seen every 3 months
-rx can be written for a maximum of 3 mo supply
-1st Rx can only be written for a 1 mo supply
actions
-with concomitant stimulant use: decrease excessive daytime sleepiness, increase daytime wakefulness
-decrease cataplexy
pharmacology:
-GABAb, GABAa, and GHB(?) receptors
dosing: oral solution (500mg/mL), initial dose- 4.5g/night in 2 divided doses-1st dose given at bedtime, 2nd dose given 2.5 to 4 hours later, doses may be increased or adjusted in 2 week intervals, average dose: 6 to 9 g/night.
concerns: mechanism (?), other agents, red tape, abuse and misuse |
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Term
| Gamma-Hydroxybutyric Acid (GHB) |
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Definition
street names: "liquid ecstasy", "Liquid X", "Juice", "Grievous Bodily Harm", "Scoops", "Georgia Home Boy"
Background: 1960's to today: anesthetic, fat burner, GH promoter, "Raves", Date Rape, and body building
Pharmacology: CNS depression-->dose dependent, dizziness, drowsiness, coma
-patients often awaken spontaneously
-prodrugs: Gamma-Butryolactone(GBL), 1,4-Butanediol |
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Term
| Ramelteon (Rozerem): Melatonin Agonist |
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Definition
MOA: high affinity for MT1 and MT2 melatonin receptors, receptors located in the suprachiasmatic nucleus (SCN), servse as a "master clock" by regulating circadian rhythms-loss of melatonin in aging and alzheimer's
metabolism: CYP1A2, avoid with other CYP1A2 inhibitors-fluvoxamine and ciprofloxacin, use with caution in patients with moderate hepatic impairment and avoid use in patients with severe hepatic impairment
treatment of insomnia characterized by difficulty with sleep onset
non-controlled substance sleep aid
no abuse, withdrawal, or dependency
negligible risk for next-day "hangover" effects |
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Term
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Definition
antidepressant
unlabeled/investigational use |
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Term
| antihistamines (OTC drugs) |
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Definition
diphenhydramine
doxylamine
pyrilamine |
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Term
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Definition
dietary supplement
5HT precursor
withdrawn with market due to contamination-caused eosinophilia-myalgia syndrome |
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Term
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Definition
nutraceutical
traveler's jet lag
work shifts-insomnia
sleep disturbances
signs and symptoms of overdose
ataxia-drowsiness |
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Term
| lemon balm (Melissa officinalis) |
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Definition
herb
use with caution in patients with thyroid problems |
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Term
| valerian (Valerian officinlis) |
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Definition
herb
insomnia
hepatotoxicity has been noted |
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Term
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Definition
matricaria chamomilla
matricaria recutita
herb
mild sedative
avoid use in patients with a ragweed allergy
use with caution in patients using cytochrome P450 substrates |
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Term
| Kava Kava (Piper methysticum) |
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Definition
herb
insomnia
possibly hepatotoxic |
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Term
| structure activity relationships of benzodiazepines |
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Definition
1 position alkylation-->source of active metabolites
2 position NH2 or N(CH3)2 is active; oxo is active (i.e. valium)
3 position has decreased activity; 3-OH rapid excretion
4-Nonoxide is active
substitution on 5-phenyl has decreased activity
7 position with an electronegative group is good
anealating the 1-2 bond with an "electron rich" ring (triazole or imidazole) yields high affinity and decreased half life |
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Term
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Definition
| loss of consciousness and reflexes, nausea and vomiting, headache, seizures, death |
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Term
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Definition
| supportive treatment-no antagonist, other sedative-hypnotics-including alcohol, amnesia, date rape-examinations and counseling |
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