In article <37bcb72f.1823...@news.newsfeeds.com>, drago...@nwu.edu
(dragon) wrote:
> Benzos are usually divided into two categories designated as long
> half-life benzos and short to intermediate half-life benzos (you
> probably already knew that)
Benzos are usually grouped in four categories, based on
chemical structure and pharmacokinetics:
1. "2-keto": diazepam, chlordiazepoxide (Librium), flurazepam,
chlorazepate (Tranxene), prazepam, halezepam, quazepam.
2. "3-hydroxy": oxazepam, temazepam, lorazepam
3. "7-nitro": clonazepam, nitrazepam, flunitrazepam
4. "triazolo": alprazolam, triazolam, midazolam (any -zolam)
2-keto's: -- have long half-life active metabolites
-- tend to have short latencies of onset and
varying (parent drug) elimination half-lives
-- undergo oxidative metabolism (N-dealkylation,
and C3-hydroxylation)
3-hydroxy's: -- no active metabolites.
-- usually have long latencies of onset and
short/intermediate elimination half-lives
7-nitro's: -- "little" or no active metabolite
-- intermediate onset latency and intermediate
to long elimination half-life
-- undergo oxidative metabolism (N-dealkylation and
C3-hydroxylation and nitro-reduction)
Triazolo's: -- have very short half-life active metabolites
-- short latencies of onset and short to intermediate
(parent drug) half-lives
-- undergo oxidative metabolism (N-hydroxylation)
There are some notable incongruencies. Neither chlordiazepoxide
nor quazepam actually has a 2-keto constituent, and midazolam
is really an "imidazolo-benzodiazepine". Also, the 7-nitro benzos
do, technically, have active metabolites, but normally are weak
and reduction of the nitro group to an amine is the major pathway
and renders the molecule inactive.
>...it's a deceptive designation 'cause it
> doesn't correspond at all to the half life of the benzo itself...best
> i can tell it really refers to metabolite half-life plus the original
> drug half-life
That's why the categorizations I've listed above are better.
They also tell you which drugs can be "potentiated" by drugs
like cimetidine. The 3-hydroxy's can't. The rest can. (The
7-nitro's are subject to oxidative metabolism.)
>...all the long half-life benzos (of which valium is
> one) have metabolite half-lifes lasting up to 100 hrs, of course, i've
> no idea if any of these metabolites are active...
Yup, nordiazepam is active. Temazepam and oxazepam are also
metabolites of diazepam, though shorter-lived (and temazepam
only in small amounts.)
> the short to
> intermediate benzos on the other hand have no major metabolites and so
> their effective half-lives are only 50 hrs in the longest cases....i
> guess i should have said klonopin was an intermediate half-life
> benzo....irregardless, half-life isn't any direct measure of strength
> or duration of action so it doesn't really matter
That's right. In fact some of the longer-half life drugs actually
tend to be _shorter_ acting in single doses. They tend to have very
fast distribution half-lives (especially diazepam), meaning that
the drug gets "diluted" (high volume of distribution) quickly.
Shorter half-life drugs (esp. lorazepam) usually "dilute" more
slowly, and have longer durations of action with single doses.
With repeated dosing, the case is the opposite. Long half-life
drugs accumulate and stay at a steady-state concentration, and
shorter half-life drugs don't (unless you take them every two
hours...)
Clonazepam sort of presents the best of both worlds. Reasonably
fast distribution -- but not *too* fast. And eliminated slowly
enough to keep a steady state.
My personal favorite, it is. Diazepam follows closely. (Can't
beat that instant gratification...)
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From: isis13 - view profile
Date: Mon, Aug 23 1999 12:00 am
Email: "isis13" <isi...@adelphia.net>
Groups: alt.drugs.hard, alt.drugs
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xanax and klonopin are far more addictive than valium.....2weeks off the vals and on xanax I had a habit
worse than any valium habit much much more addictive.Severe seizures,can't talk,hair hurts worse than any H
withdrawel isis13
gore od dopa.....1000 puta......
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From: Murry Boyton - view profile
Date: Mon, Aug 23 1999 12:00 am
Email: murry...@hotmail.com (Murry Boyton)
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> xanax and klonopin are far more addictive than valium..
Yeah my experience was I took the .5 for about four days and when I
stopped I felt like SHIT! This stuff is terribly addicting and yet they
hand it out like candy....go figure
MB
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From: Eaton T. Fores - view profile
Date: Mon, Aug 23 1999 12:00 am
Email: "Eaton T. Fores" <fug...@yeah.right.sure>
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You forgot the 1,5-benzodiazepines (clobazam).
Samson wrote in message ...
<a bunch of stuff about benzos>
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From: Samson - view profile
Date: Tues, Aug 24 1999 12:00 am
Email: smi.za....@ti.za.ac.ne.za.t (Samson)
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In article <7pt17p$uc...@nntp1.atl.mindspring.net>, "Eaton T. Fores"
<fug...@yeah.right.sure> wrote:
> You forgot the 1,5-benzodiazepines (clobazam).
Yeah, it's got that screwey diazepine ring, but it should
count as a '7-nitro' for all intents and purposes of that
list.
