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Clinician’s Corner: GABA(A)-(gamma-aminobutyric acid type A) receptors

Mechanism: The GABA(A)-(gamma-aminobutyric acid type A) receptors are the major inhibitors of brain activity. When these receptors are activated, brain activity declines.

Selected benzodiazepine hypnotics:

Temazepam (Restoril®) capsules Most commonly used BZ hypnotic

  • Half-life is 3.5-18 hours
  • NOTE: one of the safer benzos for elderly, as it is less like to accumulate. Metabolized by conjugation. Less dependent on global liver function.

Estazolam (Prosom®)  tablets 1mg and 2mg

  • Half-life is 8-28 hours

Triazolam (Halcion®) tablets .125mg and .25mg

  • Very short acting. Peak 1-2 hours, with a half-life is 1.5 to 5.5 hours
  • Side effects: anterograde amnesia, sleep rebound

THE “Z” Hypnotics= Ambien, Sonata, Lunesta

[04-30-2019] The Food and Drug Administration (FDA) is advising that rare but serious injuries have happened with certain common prescription insomnia medicines because of sleep behaviors, including sleepwalking, sleep driving, and engaging in other activities while not fully awake (making phone calls, having “sleep sex”, or preparing and eating food). These complex sleep behaviors have also resulted in deaths. These behaviors appear to be more common with eszopiclone (Lunesta), zaleplon (Sonata), and zolpidem (Ambien) than other prescription medicines used for sleep. All received a black box warning.

  • Mechanism: They also bind to the GABA receptor and decrease brain activity causing sleep.

Zolpidem (Ambien®)  Schedule-IV       All formulations are generically available.

  • Usual adult dose: 10mg.  If elderly or debilitated or female start with 5mg.
  • Very little rebound insomnia upon discontinuation. Very little withdrawal syndrome.
  • Very little effect on sleep stages.  Preserves deep sleep stages (3 & 4)
  • Avoid alcohol when taking this medication.

Feb2018: FDA release: FDA has informed the manufacturers that the recommended dose of zolpidem for women should be lowered from 10 mg to 5 mg for immediate-release products. FDA recommends that the bedtime dose be lowered because new data show that blood levels in some patients may be high enough the morning after use to impair activities that require alertness, including driving.

Zaleplon (Sonata®)       Schedule IV     generic formulations are available

  • Usual adult dose: 10mg at bedtime. If elderly or low weight start with 5mg. Take right at bedtime OR may take if having trouble falling asleep.
  • Maximum dose: 20mg if patient does not benefit from a trial of lower dose.
  • High fat meal does decrease absorption, and therefore reduce effect of Sonata on sleep latency.
  • Little rebound insomnia. Has been reported in patients taking the 20mg dose.   Was resolved by the second night.
  • Amnesia: may be caused by Sonata, which can be avoided if patient is able to get over 4 hours of sleep.
  • Avoid alcohol
  • Most common use: Zaleplon is the drug of choice for sleep lab studies.

Eszopiclone (Lunesta®)  Schedule IV      Generic formulations are available.

  • Usual adult dose: starting- 2mg immediately before bedtime. May increase to 3mg if indicated, which is more effective for sleep maintenance.
  • Elderly: starting: 1mg immediately before bedtime. May increase to 2mg.   If can’t stay asleep, recommended dose is 2mg.
  • High fat meals decrease absorption & reduce effect upon sleep latency
  • Precautions: avoid alcohol when taking this drug
  • Eszopiclone works quickly and should be taken right before bed because of risk of falling.
  • Avoid alcohol. Will increase side effects.
  • Do not take unless you are able to get 8 or more hours of sleep, before you must be active again.
  • Eszopiclone does not lose effectiveness over 6 month and was the first prescription sleep aid approved for long term use.

Commentary

Your Thompson Pharmacist is concerned about all aspects of your health even while you are asleep.  These drugs should be only used for short term use.  They should never be taken with alcohol. If you need a good night sleep Go Ahead and ASK… at Thompson Pharmacy it’s All for YOU!!!