Chlordiazepoxide (Librium) – the first benzodiazepine

Chlordiazepoxide is the very first benzodiazepine that came out and
it’s the prototype for the benzodiazepine compounds. Leo Sternbach was
the man who discovered the psychoactive properties of chlordiazepoxide,
and it as a fluke too. He worked on synthesizing biotin when he first
went into Roche and when that was done, he was about to clear his lab
when he noticed a crystalline compound. He didn’t think it would be
worth sending for tests, but dropped it off anyway, and that decision
gave us the wonderful benzodiazepine family we have today. 😉

It’s all written down in “Good Chemistry: The Life and Legacy of Valium Inventor Leo Sternbach” and his personal memoir “The Benzodiazepine Story”
published in-house by Roche (rare book). The product trials started in
May 1957 and the excellent results from the clinical trials allowed
Roche to debut Librium (clordiazepoxide hcl) in 1960, which was well
received, considering the sedatives of that time didn’t exactly have
excellent safety profiles.

Valium (diazepam) was only marketed in 1963, and it was the
blockbuster hit that propelled Roche to fame and fortune. However,
Librium (chlordiazepoxide) is the first benzodiazepine and that gives
it a lot of historical value. The chemical structure of
chlordiazepoxide hydrochloride is 7-
chloro-2-(methylamino)-5-phenyl-3H-1, 4-benzodiazepine 4-oxide
hydrochloride. It has the 1,4 benzodiazepine structure that most other
benzodiazepines share. Librium is the Adam of the benzodiazepine world.

I’ve taken chlordiazepoxide before and I wasn’t very impressed,
considering the heavyweights like clonazepam and alprazolam had been
released since the first benzodiazepine. However, I wanted to get more
before I write about it and that was difficult coz most GPs don’t stock
this considerably weak and old benzodiazepine anymore. I got my
pharmacy in Sibu to get one in through “unofficial channels” (it’s
faster) and received it when I was back home the week before. I
purchased it for RM 250 (!) which was a pleasant surprise, since
private channels usually doesn’t come cheap. I guess Thailand must have
really cheap generic benzodiazepines.

This is the bottle of generic chlordiazepoxide marketed under ATC
and named Benpine. I had asked him to get the 25 mg ones, but his
source could not get them. I don’t mind anyway, since it’s still a lot
of chlordiazepoxide. 🙂 It was obtained from Thailand and comes in a
1000 pill glass bottle containing 5 mg of sugar coated chlordiazepoxide
base (as Hcl). There is a red stamp with the words “FOR EXPORT ONLY – Psychotropic substance” on one side and “WARNING: MAY BE HABIT FORMING” on the other. Habit forming, eh? No shit… 😉

Anyway, these 5 mg sugar coated chlordiazepoxide tablets are nice to
suck on – I don’t measure how much I take, I just grab a handful and
suck on those since it’s a very low potency benzodiazepine. The sugar
coated feature is nice – there’s a burst of sweetness from the pills
you just popped in, and once that’s gone, a slightly bitter (not as
much as alprazolam) taste dominates. It comes on very fast; it’s one of
the rapid acting benzodiazepines. I felt the familiar benzodiazepine
effects within 30 minutes every time.

Chlordiazepoxide has the classic anxiolytic, sedative, hypnotic, and
anti-convulsant effects of benzodiazepines. It peaks at the 2 hour
point and starts to return to baseline after that. However, it doesn’t
leave you hanging just like that – chlordiazepoxide feels like diazepam
(Valium) in that sense…the peak plasma concentration slowly goes away
instead of just disappearing like Xanax. It’s interesting to read that
the monograph lists desmethylchlordiazepoxide, demoxepam,
desmethyldiazepam and oxazepam as the active metabolites which remains
in you for anywhere from 5-48 hours. It’s supposed to be notoriously
unpredictable in the time to peak plasma and half life calculations.

ATC 5 – The new Erimin 5. 😉

Chlordiazepoxide feels good – it’s nice to know that the very first
benzodiazepine can still perform. I went on a chlordiazepoxide-only
benzodiazepine intake for two days. It does the job (in large enough
doses) and I felt happy on it. 🙂 I didn’t notice much in the way of
what people call “hangover effects” since I don’t get them on other
benzos anyway. However, I noticed that my motor skills were slightly
impaired on the second day after a high dose on it. I’ve taken it for
quite a while now; I just grab a fistful of it like candy and pop them
in my mouth. I find that anything below 500 mg (approximate) didn’t do
much. It tastes like candy though, with its sugar coating. Heh!

Unfortunately, it goes all too quickly too…just like candy. I
won’t miss the effects (which was nice, btw, but the benzos I’m on now
suits me better), but the sugar coated 5 mg generic Chlordiazepoxide
Hcl pills will always bring a smile to my face. I found out that I did
like chlordiazepoxide, an not just for the historical value, but also
from the way the active metabolites slowly hangs around for the rest of
the day until you redose. I didn’t have to scramble for lorazepam or
more Xanax, unlike the newer benzodiazepine compounds coz of the sharp
blood plasma concentration reduction.

Chlordiazepoxide is worth exploring for historical value…getting
to sample the first benzodiazepine was fun. I remember the highest dose
taken was about 800 – 1000 mg over a 15 minute period one night to
finish of the rest of the bottle (it was still about 1/5 full), and I
was just watching a movie while repeatedly reaching for more until I
realized I finished it. I didn’t feel an urge to sleep, but I did get a
feeling as if I was stoned. It was fun.

However it should be noted that chlordiazepoxide has been associated
with seizures (?!?!) at high doses, so be careful. I didn’t get
seizures though, it could be an isolated incident like triazolam alone
causing an OD death in one patient. It would be wise to exercise
caution though – I was really irritable after the chlordiazepoxide
holiday and it took me a couple of days to normalize back to my usual
dose, and I had to up that to make it faster too. :p

Oh, and er…April Fool! Here at sixthseal.com, it’s still the 1st of April until I say it’s not. 😉