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Dr. C. Rollins
Dr. C. Rollins, Pharm. D.
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Do you know if etizolam and its metabolite eliminates at the

Customer Question

Do you know if etizolam and its metabolite eliminates at the same rate (half-life) regardless of how many consecutive days you take the drug or does it accumulate materially over time? In other words, is half-life elimination consistent regardless of the
amount or duration consumed? Thanks in advance for your response.
Submitted: 2 years ago.
Category: Pharmacy
Expert:  adamousacom replied 2 years ago.
The half-life elimination is consistent regardless of the amount or duration consumed.
Expert:  adamousacom replied 2 years ago.
I believe this answers your question.
If you do not require further assistance PLEASE rate this answer so I can be freed to help another person.
Even after you rate my response we can continue to chat here at no extra cost to you.
As I strive for quality vs. quantity, I find I can only handle a limited number of questions at a single time.
Customer: replied 2 years ago.
Was the questioned answered by someone with medical expertise?
Expert:  adamousacom replied 2 years ago.
I researched this, found the correct answer, because I thought it was a homework question as it was asked in homework.
The half-life is the same regardless of dosage or if you have taken it a day or for a month.
Expert:  adamousacom replied 2 years ago.
It has a mean elimination half life of about 3.5 hours.
That is a VERY short half-life...
Expert:  adamousacom replied 2 years ago.
Has your question been answered?
Customer: replied 2 years ago.
thank you.
Expert:  adamousacom replied 2 years ago.
Awesome. Hopefully I get a great rating!
Have a great day.
Expert:  Dr. C. Rollins replied 2 years ago.

Here is the full correct answer on the half life of the medication you were asking about. I do think you spelled it incorrectly. Hopefully this fully answers your question as metabolites half lives and the active drugs are often not the same.

Metabolism / Excretion:

The range of estimates for the mean elimination half-life of estazolam varied from 10 to 24 hours. The clearance of benzodiazepines is accelerated in smokers compared to nonsmokers, and there is evidence that this occurs with estazolam. This decrease in half-life, presumably due to enzyme induction by smoking, is consistent with other drugs with similar hepatic clearance characteristics. In all subjects and at all doses, the mean elimination half-life appeared to be independent of the dose. If satisfied please rate my answer. Thanks.

Estazolam is extensively metabolized, and the metabolites are excreted primarily in the urine. Less than 5% of a 2 mg dose of estazolam is excreted unchanged in the urine, with only 4% of the dose appearing in the feces. 4′-hydroxy estazolam is the major metabolite in plasma, with concentrations approaching 12% of those of the parent eight hours after administration. While it and the lesser metabolite, 1-oxo-estazolam, have some pharmacologic activity, their low potencies and low concentrations preclude any significant contribution to the hypnotic effect of estazolam.

Postulated relationship between elimination rate of benzodiazepine hypnotics and their profile of common untoward effects: The type and duration of hypnotic effects and the profile of unwanted effects during administration of benzodiazepine drugs may be influenced by the biologic half-life of administered drug and any active metabolites formed. If half-lives are long, drug or metabolites may accumulate during periods of nightly administration and may be associated with impairments of cognitive and/or motor performance during waking hours; the possibility of interaction with other psychoactive drugs or alcohol will be increased. In contrast, if half-lives are short, drug and metabolites will be cleared before the next dose is ingested, and carry-over effects related to excessive sedation or CNS depression should be minimal or absent. However, during nightly use for an extended period, pharmacodynamic tolerance or adaptation to some effects of benzodiazepine hypnotics may develop. If the drug has a short elimination half-life, it is possible that a relative deficiency of the drug or its active metabolites (ie, in relationship to the receptor site) may occur at some point in the interval between each night's use. This sequence of events may account for two clinical findings reported to occur after several weeks of nightly use of rapidly eliminated benzodiazepine hypnotics, namely, increased wakefulness during the last third of the night and increased daytime anxiety in selected patients.