Re: New drug FDA approved for insomnia works on melatonin receptors
jamie dolan
Provigilant
Creature from the Black Lagoon wrote:
> There is a new sleep drug which was recently FDA approved for insomnia
> that works totally differently than previous hypnotics. This new drug
> works on melatonin receptors, rather than GABA. Sounds
> interesting...probably would have little addiction properties if it is
> a non benzo hypnotic.
>
> Read about it here:
>
> http://www.currentpsychiatry.com/article_pages.asp?AID=2833
>
> Eric
I was given samples of Rozerem (at risk of being confused with Remeron
by pharmacists, btw) several weeks ago. I took an 8 mg tab and it
produces sounder sleep and a quicker onset than Ambien or Lunesta,
however it definitely has a greater next-day effect than any of the
recently-approved sleep hypnotics.
Before you try any sleep medicine ---->>>
http://www.sacbee.com/content/news/projects/drugs/story/13132395p-13976434c.html
"There are no consistent advantages of one drug over another in
effectiveness, next day impairment, or risk of withdrawal and
dependence."
Subtle differences, yes. My experience with sleeping pills is that
they're good as a stop-gap measure, but contributory to depression,
long-term - just as with benzodiazepines. Also, they're necessary
while adjusting to certain antidepressants (SSRIs) or at high doses.
http://www.nice.org.uk/pdf/TA077fullguidance.pdf
*****************************************************
A Comparison of the Newer Hypnotics
Medication Company Year approved Mechanism Dose Range Half-life
Comments
Ambien (zolpidem) Sanofi-Aventis 1992 GABA 1 receptor agonist 5
mg-10 mg 2.5 hrs Old standby; goes generic 2006; Ambien CR about to
be approved
Sonata (zaleplon) King 1999 GABA 1 receptor agonist 5 mg-10 mg 1
hr No hangover, but doesn't increase total sleep time
Lunesta (eszopiclone) Sepracor 2004 GABA 1 receptor agonist 1 mg-3
mg 6 hrs Approved for long-term use; tastes bad; precursor
(zopiclone) associated with car accidents
Rozerem (ramelteon) Takeda 2005 Melatonin receptor agonist 8 mg
1-6 hrs Unpredictable metabolism; increases prolactin in women; no
abuse potential
indiplon
Neurocrine Early 2006? GABA 1 receptor agonist 10 mg-20 mg 1.5 hrs
Will come in both IR and MR forms
Effectiveness.
All the hypnotics get patients to sleep better than placebo, a quality
known in the research studies as "reducing sleep latency." Only
Ambien, Lunesta, and indiplon can also claim that they increase total
sleep time. Ultra-short half-life Sonata is typically put forth as a
drug for middle-of-the-night insomnia, but experienced clinicians know
that many patients find it perfectly helpful for initial insomnia, and
appreciate its absolute absence of next morning grogginess. Indiplon
will be offered in two versions: an IR version that will be essentially
identical to Sonata and an MR (modified release) version that will be
similar to Ambien and Lunesta. A controlled release version of Ambien
will be released soon (Ambien CR) but there would appear to be little
clinical rationale for its use. Its usefulness for Sanofi-aventis is
clear-it's a patent extender, since Ambien IR goes generic in 2006.
Next-day impairment.
This is where Sonata really shines, since its one hour half-life
ensures that it's basically out of the system entirely within four
hours. One study showed that Ambien leads to more next-day impairment
than Sonata (J Clin Psychopharm 2002; 22:576-583). Lunesta, with its
particularly long half-life, will probably cause next day problems in
comparison with some of its cousins, but no comparative studies have
been conducted yet. Its racemic precursor, zopiclone, which shares its
pharmacokinetic profile, was associated with more traffic accidents
than short-acting BZs in one study (Lancet 1998; 352:1331-1336). We
expect that indiplon IR will be as clean as Sonata. Rozerem is a
troubling unknown, given the wide inter-individual variability in its
metabolism.
Long-term use.
Sepracor, when faced with the fact that Lunesta appeared, on paper, to
have no advantages over Ambien or Sonata, went about creating a market
niche by showing that Lunesta maintained its effectiveness over six
months (Sleep 2003; 26:793-799). With this single study, Sepracor
managed to gain two things: FDA approval for long-term use and a
remarkably effective ad campaign.
As it turns out, both Sonata and Ambien also have data indicating
long-term efficacy, but these are open label studies, with no placebo
controls. In one Sonata study, for example, 486 elderly patients who
had been enrolled in short-term double blind studies were continued in
a six to 12 month open-label extension. These patients maintained their
improved sleep on all measures (Sleep Med 2005; 6(2):107-113). Open
label studies of Ambien have shown similar long-term efficacy (J Int
Med Res 1992; 20:162-170). Word on the street is that indiplon will
probably be FDA-approved with a long-term indication. Rozerem
apparently has not yet been tested for long-term use.
The bottom-line is that probably all the hypnotics work over the long
term, but so far only Lunesta has FDA-sanctioned bragging rights.
Sepracor's lovin' it!
Abuse Potential.
One study asked 297 drug addicts questions about the likelihood that
they would abuse a variety of drugs. The most loved were the BZs, and
the least loved was Benadryl (diphenhydramine). The non-benzos
zopiclone (Lunesta's mother) and Ambien were considered only
"moderately" abusable, in the same category as tricyclic
antidepressants (Addiction 2004; 99:165-173).
However, in Lunesta's "General Summary Letter" (available from
Sepracor's medical affairs department), they report that when they
gave Lunesta 6 mg and 12 mg to known BZ abusers, the med produced the
same euphoriant effects as Valium 20 mg, and produced both amnesia and
hallucinations. In addition, clinicians have reported anecdotal
evidence of Ambien abuse, including one published series of eight cases
(J Psychopharmacol 2003; 17:131-5.)
The star in this niche appears to be Rozerem, which showed no abuse
potential in company-sponsored studies. Because of this, it is the only
FDA-approved hypnotic that is not a controlled substance.
Minor differences, but basically a sleeping pill is a sleeping pill!
culprit
"Creature from the Black Lagoon" <Deeps...@aol.com> wrote in message
news:1130827057.5...@g14g2000cwa.googlegroups.com...
> There is a new sleep drug which was recently FDA approved for insomnia
> that works totally differently than previous hypnotics. This new drug
> works on melatonin receptors, rather than GABA. Sounds
> interesting...probably would have little addiction properties if it is
> a non benzo hypnotic.
>
i thought messing with melatonin receptors was bad for people with clinical
depression.
-kelly
welshboy
increased prolactin levels. Sounds like a recipie for no sex drive what
so ever and I got enough problems with mine already with my lovely
cocktail of drugs.
I read about a drug for Parkinsons that lowers porlactin which is being
sold to increase libido.
Nom dePlume
news:7c3a4a532fd56f4c...@localhost.talkaboutsupport.com...
Dopamine agonists in general do this, although I suspect it's my
favorite DA (cabergoline, or Dostinex) that you've read about. I did a
Web search on it a few months ago, and was very surprised to see it
being promoted as a "sex drug!"
--
Nom dePlume, Ph.D.
Why, yes, in fact, I am a rocket scientist.
Guide to Medications for Mental Illness:
http://www.geocities.com/nomdeplume1000/
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