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Would injected, sublingual, et. al., administration of an MAOI work for ayahuasca

red22

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DMT is not orally active but is metabolized by the stomach enzyme monoamine oxidase (MAO). Certain chemicals in the vine inhibit the action of MAO and are therefore referred to as MAO-inhibitors: their presence in the brew makes the psychoactive principle available and allows it to circulate through the bloodstream into the brain, where it triggers the visionary access to otherworldly realms and beings.

Ayahausca: Sacred Vine of the Spirits. Ralph Metzner (editor), 2005, Introduction


The following statement incited this question:

Another advantage is that the drug does not go through the digestive system. This means the drug is not metabolized through the liver, and thus a lower dose can be used.

http://www.healthline.com/health/sublingual-and-buccal-medication-administration
It notes that the article was "Medically Reviewed on June 14, 2013 by George Krucik, MD, MBA"


Another question I have is do you think that high doses of selegiline are sufficient to use for ayahuasca, which requires an MAO-A inhibitor?


All of the studies below can be downloaded here.

High doses, e.g., 10 mg/kg, of selegiline are reported to inhibit partially MAO-A activity as assessed by an inhibition of the deamination of the preferred MAO-A substrate, 5-HT (Green et al., 1977; Demarest et al., 1980)

Green AR, Mitchell BD, Tordoff AF, Youdim MB. 1977. Evidence for dopamine deamination by both type A and type B monoamine oxidase in rat brain in vivo and for the degree of inhibition of enzyme necessary for increased functional activity of dopamine and 5-hydroxytryptamine. Br J Pharmacol. Jul 1977; 60(3): 343–349

Demarest KT, Smith DJ, Azzaro AJ. 1980. The presence of the type A form of monoamine oxidase within nigrostriatal dopamine-containing neurons. J Pharmacol Exp Ther. 1980 Nov;215(2):461-8.



Butcher SP, Fairbrother IS, Kelly JS, Arbuthnott GW, 1990, Effects of selective monoamine oxidase inhibitors on the in vivo release and metabolism of dopamine in the rat striatum. Journal of Neurochemistry, Vol. 55, No. 3, 981-988


MAOI research for the harmine found in traditional ayahuasca brews:

Udenfriend S, Witkop B, Redfield B, Weissbach H. 1958. Studies with reversible inhibitors of monoamine oxidase: Harmaline and related compounds. Biochemical Pharmacology, 1(2):160-165. DOI:10.1016/0006-2952(58)90025-X

Buckholtz NS, Boggan WO. 1977. Monoamine oxidase inhibition in brain and liver produced by beta-carbolines: structure-activity relationships and substrate specificity. Biochemical Pharmacology, 26(21):1991-6. DOI:10.1016/0006-2952(77)90007-7
 
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Also, I'm on selegiline. Could I immediately switch to a different MAOI, or ingest a harmine-based ayahuasca preparation, or would I have to wait the 40 days...


After the administration of a therapeutic dose (5–10 mg), the peak plasma concentration is reached within 30–120 min; 90% is bound to plasma proteins [60,62,63]. Within 30–90 min, platelet MAO-B activity is inhibited by 90% in PD patients, indicative of rapid cellular uptake; recovery of activity requires as long as 40 days [14,64].

14. Fowler JS, Volkow ND, Logan J, Wang GJ, MacGregor RR, Schyler D, Wolf AP, Pappas N, Alexoff D, Shea C. Slow recovery of human brain MAO-B after l-deprenyl (selegiline) withdrawal. Synapse 1994;18:86–93.

64. Riederer P, Youdim MBH, Rausch WD, Birkmayer W, Jellinger K, Seemann D. On the mode of action of l-deprenyl in the human central nervous system. Journal of Neural Transmission 1978;43:217–26.



Foley P, Gerlach M, Youdim MB, Riederer P. MAO-B inhibitors: multiple roles in the therapy of neurodegenerative disorders? Parkinsonism Related Disorders, 6(1):25-47
 
Also, I'm on selegiline. Could I immediately switch to a different MAOI, or ingest a harmine-based ayahuasca preparation, or would I have to wait the 40 days...

We can't advise you on what you can do safely on your medication. Do you really want to risk hurting yourself based on our best guess?

Other than that I don't really see a question in this thread, so I'll just comment on this:

Another advantage is that the drug does not go through the digestive system. This means the drug is not metabolized through the liver, and thus a lower dose can be used.

All blood passes through the liver. If the drug enters the blood, it will eventually go through the liver. Drugs delivered orally pass through the liver before they enter general circulation. This means that some of the drug will be eliminated on this first pass before it can travel throughout the rest of the body. This does not mean that drugs administered through other routes don't go through the liver, just that they don't go through the liver before entering general circulation.
 
Thanks. The question is does ayahuasca only work if the MAOI is administered orally?
 
So only self-experimentation will reveal if non-oral administration accumulates in the body in a way sufficient to make the DMT absorbable...
 
No, MAOIs should be effective via alternate routes of administration. However, there's a high concentration of MAO in the GI tract, so concentrated administration there is useful.

Also, selegiline is not a good choice for Ayahuasca. It is irreversible and inhibits MAOA (that's the subform that breaks down tryptamines selectively) only at high doses. And then you're stuck with the MAOI effect for up to 2 weeks, while your body synthesizes more MAO.
 
Also, selegiline is not a good choice for Ayahuasca. It is irreversible and inhibits MAOA (that's the subform that breaks down tryptamines selectively) only at high doses. And then you're stuck with the MAOI effect for up to 2 weeks, while your body synthesizes more MAO.

But some people follow the diet anyway, which apparently isn't even that strict (see below). Also, I find this to be intriguing:

Taking 5mg of selegiline and 4-5+ grams (dried) of shrooms, often lead to overwhelming experiences, more profound and more beautiful, longer, and more of a too long DMTish feel; with the "into the void and piercing the veil" type trips. And if I could get brave enough to "let go" I would experience constant Ego Loss over and over again while being overwhelmed with epiphanies of myself, surroundings, and my little social web and life.

http://www.shroomery.org/forums/showflat.php/Number/19914585#19914585 (04/29/14)


Thanks for the response, ebola.


Can I still get drunk on it and eat pepperoni pizza?

Yes.


http://www.socialanxietysupport.com/forum/1072244025-post515.html (05-02-2014)

[They're speaking about Nardil.]


I drink beer on Nardil all the time. 4 is the most I've ever had and I've never once had a sneaking suspicion that I was putting myself in danger.

http://www.socialanxietysupport.com/forum/651105-post7.html (08-09-2008)
 
No, MAOIs should be effective via alternate routes of administration. However, there's a high concentration of MAO in the GI tract, so concentrated administration there is useful.

So what's the final word on parenteral MAOIs and ayahuasca?
 
Here's a question. Is there any reason to believe that taking psychedelics with large doses of irreversible MAOIs is dangerous?

(One at a time, of course.)
 
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