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Lunesta

Aka: Lunesta, Eszopiclone
  1. Indication
    1. Insomnia
  2. Mechanism
    1. Nonbenzodiazepine hypnotic agent
    2. Acts at gamma-aminobutyric acid receptors
    3. Isomer of Zopiclone (Imovane)
    4. Schedule IV controlled substance
  3. Dosing
    1. Standard: 2 mg po at bedtime
    2. Reduced Indications (1 mg po at bedtime)
      1. Severe liver disease
      2. Age >65 years
      3. Concurrent use of CYP 3A4 inhibitor
    3. Maximum: 3 mg po at bedtime
  4. Pharmacokinetics
    1. Onset of action: 10-18 minutes
    2. Half-Life: 4-6 hours
    3. Duration of action: 6-8 hours
    4. Metabolism: CYP450 3A4
    5. Delayed activity if taken after a fatty meal
  5. Adverse effects
    1. Nonbenzodiazepine hypnotic agent for common effects
    2. Metallic Taste
      1. Reported in up to 34% of patients on 3 mg
      2. Very bothersome - discontinuation is common
    3. Amnesia
    4. Hallucinations
    5. Worsening depression
  6. Advantages
    1. See Nonbenzodiazepine hypnotic agent
    2. Effective
  7. Disadvantages
    1. Expensive: Over $100 for 1 month supply
  8. References
    1. (2005) Med Lett Drugs Ther 47:17-9
    2. Wessel (2005) Am Fam Physician 71(12):2359-60

Lunesta (C1579761)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C515051
English Lunesta
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Eszopiclone (C1436328)

Definition (NCI) A nonbenzodiazepine, cyclopyrrolone and active stereoisomer of zopiclone with hypnotic and sedative activity and without significant anxiolytic activity. Although the exact mechanism of action remains to be fully elucidated, eszopiclone is able to bind to and activate the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization, inhibition of neuronal firing, and enhancement of the inhibitory effect of GABA. This eventually leads to a hypnotic effect and allows for an induction of sleep.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C515051
SnomedCT 409421001, 409420000
English eszopiclone, (+)-(5S)-6(chloropyridine-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo(3,4-b)-pyrazin-5-yl-4-methyl-piperazine-1-carboxylate, eszopiclone (medication), (S)-Zopiclone, (+)-(5S)-6-(5-Chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo(3,4-b)pyrazin-5-yl 4-methylpiperazine-1-carboxylate, ESZOPICLONE, eszopiclone [Chemical/Ingredient], Eszopiclone (product), Eszopiclone (substance), Eszopiclone
Spanish eszopiclona (producto), eszopiclona (sustancia), eszopiclona
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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