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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


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poster:Ame Sans Vie thread:542666
URL: http://www.dr-bob.org/babble/20050816/msgs/542666.html