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CYP3A4 inhibitor & ketamine experiment

madpilot

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Joined
Nov 22, 2010
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3
http://dmd.aspetjournals.org/content/30/7/853.full.pdf

I do believe CYP3A4 plays the biggest role in the metabolization of ketamine to nor-ketamine.

According to the linked report, i conclude that i can lower the dose of ketamine to half or less by using an inhibitor to the liver enzyme CYP3A4.

I have wondered why nobody has suggested ketoconazole
http://en.wikipedia.org/wiki/Ketoconazole

anyways see en.wikipedia.org/wiki/CYP3A4 for more inhibitors

looking forward to replies as i am thinking of doing an experiment with 2-400 mg ketoconazole before doing ketamine.

would you advice me to not do this?
Anyone with experience in using an enzyme inhibitor in order to get altered drug effect?
 
http://dmd.aspetjournals.org/content/30/7/853.full.pdf

I do believe CYP3A4 plays the biggest role in the metabolization of ketamine to nor-ketamine.

According to the linked report, i conclude that i can lower the dose of ketamine to half or less by using an inhibitor to the liver enzyme CYP3A4.

I have wondered why nobody has suggested ketoconazole
http://en.wikipedia.org/wiki/Ketoconazole

anyways see en.wikipedia.org/wiki/CYP3A4 for more inhibitors

looking forward to replies as i am thinking of doing an experiment with 2-400 mg ketoconazole before doing ketamine.

would you advice me to not do this?
Anyone with experience in using an enzyme inhibitor in order to get altered drug effect?

Anti-fungal drugs are really toxic, and the toxicity is very difficult to predict (ie doesn't correlate at all with dose). If you do this, be careful.

"Neither concentration in serum, toxicity, nor outcome correlated with dose, calculated in milligrams per kilogram at the fixed doses (400-mg increments) under study."

"Toxicity was reversible, and principal side effects were nausea and vomiting (50% ), gynecomastia (21% ), decreased libido (13% ), alopecia (8% ), elevated liver function tests (5% ), pruritus (5% ), and rash (4% )" (ref)

The drug also carries a 1:10,000 risk of acute irreversible liver failure and a higher than normal risk of anaphylaxis
 
That's fantastic, thanks for sharing :)

I suppose it wouldn't hurt to try it with a mix of Grapefruit Juice, Cimetidine, Echinacea, Milk Thistle, and Black Pepper? If anything, all this stuff is good for your health.

I will definitely be trying this soon.

And btw, anyone who knows me personally is going to laugh once they read the article's heading ;).
 
Please report back after your experiment :) i plan doing it on christmas eve night
 
Cyp3a4

What will happens if a person takes Erythromycin after 8 days of Pepper contain food or piperine as both are CYP3A4 inhibitors.
What happens to pharmacokinetic of erythromycin. Is it enhances or decreses the activity of erythromycin.
 
Piperine inhibits CYP3a4 - so there would be increased blood levels of erythromycin and decreased metabolism in the liver.
(I'm not sure how effective eating cracked pepper is to inhibit CYP though!)
 
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