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Dr. Bob is Robert Hsiung, MD,
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Posted by ed_uk on July 24, 2005, at 4:58:30
In reply to Re: FDA okays sleep drug Rozerem(TM) (ramelteon) » djmmm, posted by linkadge on July 24, 2005, at 3:09:18
>Whenever a nutritional supplement proves to be an effective alternative to a prescription it poses a significant risk to sales.
Melatonin isn't even available here! Also, I've read that its illegal to import it into the UK.
~Ed
Posted by ed_uk on July 24, 2005, at 6:38:48
In reply to Re: FDA okays sleep drug Rozerem(TM) (ramelteon) » linkadge, posted by ed_uk on July 24, 2005, at 4:58:30
So, Rozerem will be available in the US in about a month?? I hope it won't be delayed as much as Lunesta was!
From the Rozerem website..........
>The body's own melatonin binds to MT1 and MT2 receptors in the SCN, suppressing the circadian alerting signal. This is believed to facilitate sleep.
>ROZEREM (ramelteon) is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor.
The activity of ramelteon at the MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties, as these receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle.
My question........
How does the hypnotic efficacy of ramelteon differ from that of melatonin?
What does the MT3 receptor do?
>M-II (the major active metabolite of ramelteon) has weak affinity for the serotonin 5-HT2B receptor..........
What is the significance of this??
>DOSAGE AND ADMINISTRATION
>The recommended dose of ROZEREM is 8 mg taken within 30 minutes of going to bed. It is recommended that ROZEREM not be taken with or immediately after a high fat meal.
>HOW SUPPLIED?
>ROZEREM is available as round, pale orange-yellow, film-coated, 8 mg tablets.
>Controlled Trials Supporting Efficacy
Although ramelteon can help people fall asleep, it doesn't appear to increase total sleep time. Mild residual effects were observed the following day.
>Rebound Insomnia/Withdrawal
No w/d symptoms were detected. Let's see whether ramelteon lives up to its promise.
>Abnormalities were, however, noted within the reproductive axis. Overall, the mean serum prolactin level change from baseline was 4.9 µg/L (34 % increase) for women in the ROZEREM group compared with -0.6 µg/L (4% decrease) for women in the placebo group (p=0.003). No differences between active- and placebo-treated groups occurred among men. Thirty-two percent of all patients who were treated with ramelteon in this study (women and men) had prolactin levels that increased from normal baseline levels compared to nineteen percent of patients who were treated with placebo.
Oh dear.
>In a 12-month, open-label study in adult and elderly patients, there were two patients who were noted to have abnormal morning cortisol levels, and subsequent abnormal ACTH stimulation tests.
A 29-year-old female patient was also diagnosed with a prolactinoma.
Hmmm.......
>ROZEREM is indicated for the treatment of insomnia characterized by difficulty with sleep onset.
Makes sense.
>The failure of insomnia to remit after a reasonable period of treatment may indicate the
presence of a primary psychiatric and/or medical illness that should be evaluated. Worsening of insomnia, or the emergence of new cognitive or behavioral abnormalities, may be the result of an unrecognized underlying psychiatric or physical disorder and requires further evaluation of the patient.Is this a euphemistic way of saying that ramelteon can cause psychiatric adverse effects LOL?! A bit like 'Halcion may uncover depressive tendencies'.
>As with other hypnotics, exacerbation of insomnia and emergence of cognitive and behavioral abnormalities were seen with ROZEREM during the clinical development program.
:-(
>Patients should be advised to take ROZEREM within 30 minutes prior to going to bed.....
Useful to know :-)
>Patients should be advised that they should not take ROZEREM with or immediately after a high fat meal.
Delays the onset of action.
>Patients should consult their health care provider if they experience one of the following: cessation of menses or galactorrhea in females, decreased libido, or problems with fertility.
Signs of hyperprolactinemia.
>For patients presenting with unexplained amenorrhea, galactorrhea, decreased libido, or problems with fertility, assessment of prolactin levels and testosterone levels should be considered as appropriate.
Ramelteon can apparantly lower testosterone levels, as well as increasing prolactin.
>ROZEREM has a highly variable inter-subject pharmacokinetic profile (approximately 100% coefficient of variation in Cmax and AUC).
That's not what we like to hear! Presumably, more 'individualisation' of dosing will be required to optimise the effect. Doctors don't like this! Anyway, Rozerem only comes as an 8mg tablet.
>CYP1A2 is the major isozyme involved in the hepatic metabolism of ramelteon....
>Fluvoxamine (strong CYP1A2 inhibitor): When fluvoxamine 100 mg twice daily was administered for 3 days prior to single-dose co-administration of ROZEREM 16 mg and fluvoxamine, the AUC0-inf for ramelteon increased approximately 190-fold, and the Cmax increased approximately 70-fold, compared to ROZEREM administered alone.
Whoa! Take care if you're on Luvox.
>Adverse Reactions Resulting in Discontinuation of Treatment Five percent of the 3594 individual subjects exposed to ROZEREM in clinical studies discontinued treatment owing to an adverse event, compared with 2% of the 1370 subjects receiving placebo. The most frequent adverse events leading to discontinuation in subjects receiving ROZEREM were somnolence (0.8%), dizziness (0.5%), nausea (0.3%), fatigue (0.3%), headache (0.3%), and insomnia (0.3%).
Worsening of insomnia in 3% on ramelteon versus 2% on placebo. Depression in 2% on ramelteon versus 1% on placebo.
>DRUG ABUSE AND DEPENDENCE
>ROZEREM is not a controlled substance.
This will surely increase its popularity - especially since it can be used on a long-term basis.
~Ed
Posted by ed_uk on July 24, 2005, at 7:02:24
In reply to Rozerem Information, posted by ed_uk on July 24, 2005, at 6:38:48
.....it will be the official p-babble Rozerem thread - a bit like the massive Effexor thread that's been going for YEARS! People can use this thread to post their experiences and opinions RE ramelteon. It will be a fantastic source of info. When Rozerem hits the pharmacy shelves, please post your experiences here. Many people will be interested.
~ed
Posted by ed_uk on July 24, 2005, at 8:46:38
In reply to Let's keep this thread going........., posted by ed_uk on July 24, 2005, at 7:02:24
Who's gonna be queueing (sp) up outside the pharmacy?
Who's gonna be collecting Rozerem samples?
~Ed
Posted by linkadge on July 24, 2005, at 15:09:49
In reply to OK, so who wants to try Rozerem when it comes out?, posted by ed_uk on July 24, 2005, at 8:46:38
I think I'll stick to melatonin and spare the cancer risk or whatever it was.
Linkadge
Posted by ed_uk on July 24, 2005, at 16:21:46
In reply to Re: OK, so who wants to try Rozerem when it comes out?, posted by linkadge on July 24, 2005, at 15:09:49
Oh well, it probably won't be released in Canada for a few years yet!
~Ed
Posted by ed_uk on July 24, 2005, at 16:44:36
In reply to Re: OK, so who wants to try Rozerem when it comes out? » linkadge, posted by ed_uk on July 24, 2005, at 16:21:46
Surely someone is interested in Rozerem!!!
~Ed
Posted by linkadge on July 24, 2005, at 17:02:47
In reply to Where are all the INSOMNIA sufferers???, posted by ed_uk on July 24, 2005, at 16:44:36
They're just running out of the necessary letters to create euphonic medication names.
Linkadge
Posted by linkadge on July 24, 2005, at 17:04:18
In reply to Re: Where are all the INSOMNIA sufferers???, posted by linkadge on July 24, 2005, at 17:02:47
And when Rozerem came down from the mountain, God spakeith to him saying...
Linkadge
Posted by ed_uk on July 24, 2005, at 17:06:12
In reply to Re: Where are all the INSOMNIA sufferers???, posted by linkadge on July 24, 2005, at 17:02:47
Rozerem sounds kind of euphoric, not as much as Quaalude though!
~Ed
Posted by ed_uk on July 24, 2005, at 17:20:10
In reply to Re: Where are all the INSOMNIA sufferers???, posted by linkadge on July 24, 2005, at 17:04:18
>And when Rozerem came down from the mountain, God spakeith to him saying...
LOL, that gave me a good laugh!
~Ed
Posted by Phillipa on July 24, 2005, at 19:28:15
In reply to Re: Where are all the INSOMNIA sufferers??? » linkadge, posted by ed_uk on July 24, 2005, at 17:20:10
So, if I continue on luvox it's another drug that luvox potentiates the action of like xanax. See Ed I do know a little. Fondly, PJ O
Posted by Cecilia on July 25, 2005, at 4:17:56
In reply to OK, so who wants to try Rozerem when it comes out?, posted by ed_uk on July 24, 2005, at 8:46:38
> Who's gonna be queueing (sp) up outside the pharmacy?
>
> Who's gonna be collecting Rozerem samples?
>
> ~EdNot me, Melatonin didn`t help me sleep and gave me nightmares when I finally did. One thing I`ve never understood, though, is how Melatonin got classified as a non prescription "nutritional supplement." It`s a hormone, and other hormones like estrogen and thyroid require prescriptions. Cecilia
Posted by Cecilia on July 25, 2005, at 4:58:07
In reply to OK, so who wants to try Rozerem when it comes out?, posted by ed_uk on July 24, 2005, at 8:46:38
> Who's gonna be queueing (sp) up outside the pharmacy?
>
> Who's gonna be collecting Rozerem samples?
>
> ~EdNot me, Melatonin didn`t help me sleep and gave me nightmares when I finally did. One thing I`ve never understood, though, is how Melatonin got classified as a non prescription "nutritional supplement." It`s a hormone, and other hormones like estrogen and thyroid require prescriptions. Cecilia
Posted by Jakeman on July 26, 2005, at 20:08:24
In reply to Where are all the INSOMNIA sufferers???, posted by ed_uk on July 24, 2005, at 16:44:36
> Surely someone is interested in Rozerem!!!
>
> ~EdHi Ed,
This drug leaves me scratching my head. I was very hopeful that the makers had come up with a break-thru in sleep medication, but I don't see it from the reports I've read (of course a lot of the research is not on the web). Looking at the phase 1 and 2 trials...it didn't do much other than making you fall asleep earlier...so it may help in resetting circadian rhythm which is good for people with "delayed sleep phase". I've read nothing about it making you sleep longer, deeper, or more efficiently.
Apparently it is more potent than melatonin, but why no head to head studies with melatonin? As some have speculated, maybe they are positioning themselves as the "doctor prescribed" alternative to self-medication with melatonin. Can you get melatonin by prescription in the UK? As you know, it's an over-the-counter supplement here.
warm regards ~Jake
Yes Phillipa I think drug company reps and other observers read this board. One reason being to gauge whether or not to buy stock in a pharma co. about to release another drug :-)
Posted by jerrympls on July 26, 2005, at 20:46:32
In reply to Where are all the INSOMNIA sufferers???, posted by ed_uk on July 24, 2005, at 16:44:36
> Surely someone is interested in Rozerem!!!
>
> ~EdCount me in.
Posted by Phillipa on July 26, 2005, at 21:12:30
In reply to Re: Where are all the INSOMNIA sufferers??? » ed_uk, posted by Jakeman on July 26, 2005, at 20:08:24
Jake, I never thought of that. But wouldn't the stock of MAOI's go up if that were the case? Fondly, Phillipa
Posted by Jakeman on July 26, 2005, at 22:00:12
In reply to Re: Where are all the INSOMNIA sufferers??? » Jakeman, posted by Phillipa on July 26, 2005, at 21:12:30
> Jake, I never thought of that. But wouldn't the stock of MAOI's go up if that were the case? Fondly, Phillipa
Phillipa,
These companies all are racing to get in first place in the insomnia market. Whoever produces the perfect sleep drug will make billions. But it hasn't happened. Takeda has got a lot of interest but I don't think they will pass snuff. (non-southerners will wonder about that expression).
If anything goes up, it will be the the existing products. Best bets for a stock bet (in my opinion) is the long acting Ambien. I recently tried Restoril but switched back to Lunesta.warm regards, Jake
Posted by ed_uk on July 27, 2005, at 16:48:01
In reply to Re: Where are all the INSOMNIA sufferers??? » ed_uk, posted by Jakeman on July 26, 2005, at 20:08:24
Hi Jake,
>Apparently it is more potent than melatonin, but why no head to head studies with melatonin?
.......the manufacturer would never carry out such a study unless they have very good reason to suspect that it's more effective than melatonin.......which it probably isn't IMHO!
>Can you get melatonin by prescription in the UK?
It's not approved here so it's very rarely prescribed. Doctor's can prescribe meds which aren't approved but they rarely do.
Warm regards
~Ed
Posted by ed_uk on July 27, 2005, at 16:50:45
In reply to Re: Where are all the INSOMNIA sufferers???, posted by Jakeman on July 26, 2005, at 22:00:12
Hi Jake,
>I recently tried Restoril but switched back to Lunesta.
What do you prefer about Lunesta? What doses of Restoril and Lunesta did you take?
>Best bets for a stock bet (in my opinion) is the long acting Ambien.
I agree. It would be useful to have an Ambien CR tablet with an immediate release outer layer + a controlled release inner layer.
Kind regards
~Ed
Posted by jerrympls on July 27, 2005, at 16:56:10
In reply to Re: Where are all the INSOMNIA sufferers??? » Jakeman, posted by ed_uk on July 27, 2005, at 16:50:45
> Hi Jake,
>
> >I recently tried Restoril but switched back to Lunesta.
>
> What do you prefer about Lunesta? What doses of Restoril and Lunesta did you take?
>
> >Best bets for a stock bet (in my opinion) is the long acting Ambien.
>
> I agree. It would be useful to have an Ambien CR tablet with an immediate release outer layer + a controlled release inner layer.
>
> Kind regards
>
> ~Edis Ambien CR released yet???
Posted by ed_uk on July 27, 2005, at 17:58:45
In reply to Re: Where are all the INSOMNIA sufferers??? » ed_uk, posted by jerrympls on July 27, 2005, at 16:56:10
Hi J!
No :-(
~ed x
Posted by jakeman on July 28, 2005, at 17:03:48
In reply to Re: Where are all the INSOMNIA sufferers??? » Jakeman, posted by ed_uk on July 27, 2005, at 16:50:45
>
> What do you prefer about Lunesta? What doses of Restoril and Lunesta did you take?
>Hi Ed,
The first night I took 15 mg. of Restoril. Next night 30 mg. Is 30 considered a low dose? I'm taking 4.5 mg Lunesta.
I could not get into a deep sleep with Restoril,
and I seemed to wake up often during the night. I had about the same experience with Sonata. With the Lunesta I do tend to sleep deeper and longer, although it's no way close to perfect.Regarding Ramelteon...if melatonin is difficult obtain in the UK, then it would appear there's a market waiting for a prescription drug which mimics melatonin.
warm regards ~Jake
Posted by ed_uk on July 28, 2005, at 17:59:05
In reply to Re: Where are all the INSOMNIA sufferers??? » ed_uk, posted by jakeman on July 28, 2005, at 17:03:48
Hi Jake!
>Is 30 considered a low dose?
Not really. 10mg would be a low dose.
>Regarding Ramelteon...if melatonin is difficult obtain in the UK, then it would appear there's a market waiting for a prescription drug which mimics melatonin.
Absolutely, I agree. I wonder whether ramelteon will be approved here.
Kind regards
~Ed
Posted by ed_uk on August 6, 2005, at 13:44:10
In reply to Re: Where are all the INSOMNIA sufferers??? » jerrympls, posted by ed_uk on July 27, 2005, at 17:58:45
Hi!!!
I just got your babblemail - will reply tonight :-D
Are you interested in ramelteon? I wondered whether it might be useful in improving your sleep at night without causing a hangover. Perhaps this would reduce your daytime drowsiness...
Kind regards
~Ed
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