Psycho-Babble Medication Thread 542666

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What makes a drug good for sublingual absorption?

Posted by Ame Sans Vie on August 16, 2005, at 19:42:01

Hi everyone! So happy to be posting back on here... I went through some rough times and sort of posted on and off here for the past two years, though prior to that I was quite the regular PB'er. :-)

But anyway, down to business. I've been considering trying Niravam (sublingual alprazolam [Xanax]), and my interest, coupled with a relative lack of biochemical knowledge, has left me wondering -- of the drugs that I take, which can be taken sublingually? Which will be better absorbed sublingually? What is it that make a drug a good candidate for under-the-tongue absorption? Water-solubility... ?

I'm not concerned with the drugs I take such as fluoxetine, dextromethorphan, and Xyrem; I know from extensive experience that Xanax is far more effective sublingually. But what about clonazepam [Klonopin], secobarbital [Seconal], methamphetamine [Desoxyn], and zaleplon [Sonata]?

For example, I read the following on http://www.rxlist.com about zaleplon:

"Zaleplon is rapidly and almost completely absorbed following oral administration. Peak plasma concentrations are attained within approximately 1 hour after oral administration. Although zaleplon is well absorbed, its absolute bioavailability is approximately 30% because it undergoes significant presystemic metabolism."

Could bioavailability, for example, be increased by taking the drug sublingually? Or even rectally? (being into herbal medicines, I'm well-versed in making effective suppositories.)

Thanks so much in advance, everyone! :-)

~Michael

 

Re: What makes a drug good for sublingual absorption?

Posted by Paulbwell on August 16, 2005, at 19:49:04

In reply to What makes a drug good for sublingual absorption?, posted by Ame Sans Vie on August 16, 2005, at 19:42:01

> Hi everyone! So happy to be posting back on here... I went through some rough times and sort of posted on and off here for the past two years, though prior to that I was quite the regular PB'er. :-)
>
> But anyway, down to business. I've been considering trying Niravam (sublingual alprazolam [Xanax]), and my interest, coupled with a relative lack of biochemical knowledge, has left me wondering -- of the drugs that I take, which can be taken sublingually? Which will be better absorbed sublingually? What is it that make a drug a good candidate for under-the-tongue absorption? Water-solubility... ?
>
> I'm not concerned with the drugs I take such as fluoxetine, dextromethorphan, and Xyrem; I know from extensive experience that Xanax is far more effective sublingually. But what about clonazepam [Klonopin], secobarbital [Seconal], methamphetamine [Desoxyn], and zaleplon [Sonata]?
>
> For example, I read the following on http://www.rxlist.com about zaleplon:
>
> "Zaleplon is rapidly and almost completely absorbed following oral administration. Peak plasma concentrations are attained within approximately 1 hour after oral administration. Although zaleplon is well absorbed, its absolute bioavailability is approximately 30% because it undergoes significant presystemic metabolism."
>
> Could bioavailability, for example, be increased by taking the drug sublingually? Or even rectally? (being into herbal medicines, I'm well-versed in making effective suppositories.)
>
> Thanks so much in advance, everyone! :-)
>
> ~Michael

Hi AME,

I'v had trouble sleeping, you mentioned having having trouble sleeping, and only Tuinal (seconal+amytal) helping, do you still find success in these?

Thanks

 

Re: What makes a drug good for sublingual absorption? » Ame Sans Vie

Posted by ed_uk on August 17, 2005, at 6:11:48

In reply to What makes a drug good for sublingual absorption?, posted by Ame Sans Vie on August 16, 2005, at 19:42:01

Dear M,

Secobarbital is absorbed rectally.......

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=7110754&query_hl=7

..........be careful 'K? I wonder whether it will irritate your rectum?

~ed

 

Re: What makes a drug good for sublingual absorption?

Posted by Empathy on August 17, 2005, at 23:16:20

In reply to What makes a drug good for sublingual absorption?, posted by Ame Sans Vie on August 16, 2005, at 19:42:01

Wow... good question.

You just taught me something! I didn't know that they made Xanax in liquid form... All these years I have been chewing my Xanax up when I take them... my DR. thinks that is so bizarre, but I have always sworn that Xanax - although gross tasting - works better if I break it up and dissolve it in my mouth. Evidently this is the case for some other people too? Cool.

I hope someone will answer this - I want to know too.

 

Re: What makes a drug good for sublingual absorption?

Posted by Declan on August 18, 2005, at 17:22:14

In reply to What makes a drug good for sublingual absorption?, posted by Ame Sans Vie on August 16, 2005, at 19:42:01

Michael, most drugs I take sublingually. Just not the ones that tast too awful. Benzos and desoxyn, certainly. Especially ones that are not absorbed so well from the stomach.
Declan

 

Re: What makes a drug good for sublingual absorption? » Declan

Posted by ed_uk on August 18, 2005, at 18:09:10

In reply to Re: What makes a drug good for sublingual absorption?, posted by Declan on August 18, 2005, at 17:22:14

>Just not the ones that tast too awful.

Like Parnate!

~ed

 

Re: What makes a drug good for sublingual absorption?

Posted by Declan on August 18, 2005, at 18:16:37

In reply to Re: What makes a drug good for sublingual absorption? » Declan, posted by ed_uk on August 18, 2005, at 18:09:10

Nah Ed, Parnate's a piece of cake. It has to be pretty bad. There is one herb that I found challenging...Coleus Forskoli.

It has (theoretically) very interesting properties. You might find them interesting. Much much worse than paregoric, I can't tell you how awful it tastes.

Declan

 

Re: What makes a drug good for sublingual absorption? » Declan

Posted by ed_uk on August 18, 2005, at 18:34:05

In reply to Re: What makes a drug good for sublingual absorption?, posted by Declan on August 18, 2005, at 18:16:37

Hi Dec,

>Much much worse than paregoric....

Hehe, it's not often you here of paregoric. I don't think I'd like it. I don't like codeine so.......

What does the Coleus do?

~ed

 

Re: What makes a drug good for sublingual absorption? » Declan

Posted by Iansf on August 19, 2005, at 0:10:44

In reply to Re: What makes a drug good for sublingual absorption?, posted by Declan on August 18, 2005, at 17:22:14

> Michael, most drugs I take sublingually. Just not the ones that tast too awful. Benzos and desoxyn, certainly. Especially ones that are not absorbed so well from the stomach.
> Declan

Declan, which of the commonly prescribed psych drugs are absorbed poorly by the stomach? And does that mean you could get equal benefit from a smaller dose of those drugs if taken sublingually - and consequently have fewer or less intrusive side effects?
Ian

 

Re: What makes a drug good for sublingual absorption? » Iansf

Posted by Declan on August 19, 2005, at 3:59:44

In reply to Re: What makes a drug good for sublingual absorption? » Declan, posted by Iansf on August 19, 2005, at 0:10:44

Hi Ian

Benzos I always take that way. I have wondered about MAOIs. If the most MAO-A is found in the gut.....

Some drugs are simply too toxic to put under the tongue and no point either, methadone for example....makes your mouth shrivel up, and is well absorbed anyway. (Morphine would be an example of one that is better sublingually).

I'd be cautious about a lot of psychdrugs sublingual because they are synthetic/whatevertherightwordis.

But Nardil is supposed to smell nice. That's a good start.

A lot of the new psychdrugs I know nothing about, and the old APs I'd never take again.

Declan


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