White grapefruit potentiates ketamine

[Hal_1ncandenza]

According to this study:

S-ketamine concentrations are greatly increased by grapefruit juice - PubMed

Grapefruit juice significantly increased the plasma concentrations of oral ketamine in healthy volunteers.Dose reductions of ketamine should be considered when using oral ketamine concomitantly with grapefruit juice.

www.ncbi.nlm.nih.gov

From what I can tell, this would only affect oral use, but still, interesting information.

 

[Delsyd]

I wonder if this is true for other dissociatives?

 

[Chris Timothy]

Works wonders for DXM at least.

 

[Blowmonkey]

Oh no it definitely still affects the way ketamine is broken down into norketamine and other metabolites, irregardless of the administration method really. As long as it inhibits those isoenzyme pathways, so simultaneous administration of iv or im ketamine/grapefruit juice will start working and be broken down before the grapfruit juice will have an effect, as opposed to oral/insufflated, blood always has to go through the liver eventually.

 

[Hal_1ncandenza]

So, to clarify, IV/IM/Oral admin will be affected but not insufflated?

 

[Blowmonkey]

I think every administration method will be affected, as long as the grapefruit juice is already in your system before you im or iv, or insufflated for that matter, because I have no idea if the gf juice will be that quick if you do them at exactly the same time.

 

[perpetualdawn]

Thats so surprising. There must be so many other strange interactions between drugs and food that have not yet been pinpointed.

I didn't bother reading the full paper, anyone care to give a quick rundown on why this happens?

 

[Hal_1ncandenza]

Grapefruit affects hundreds of other substances, not sure why...

 

[Chris Timothy]

Thats so surprising. There must be so many other strange interactions between drugs and food that have not yet been pinpointed.

I didn't bother reading the full paper, anyone care to give a quick rundown on why this happens?

Grapefruit inhibits a liver enzyme called CYP3A4, which is one of the enzymes that turns ketamine into norketamine.

 

[Blowmonkey]

It's not only grapefruit btw, lot's of drugs are metabolized by it and inhibit them, cannabis for example does, or alcohol, or acetaminophen for that matter.

The "active ingredients" in gf juice are 2 coumarins, dihydroxybergamottin and bergamottin apparently.

Two Major Grapefruit Juice Components Differ in Time to Onset of Intestinal CYP3A4 Inhibition

Grapefruit juice elevates blood levels of some drugs taken orally, primarily by inhibiting intestinal CYP3A4-mediated first-pass metabolism. Two prominent furanocoumarins in the juice, 6′,7′-dihydroxybergamottin (DHB) and bergamottin (BG), have been demonstrated as important contributors to...

jpet.aspetjournals.org

So about 30 mins before you take your regular dose of k, drink a liter of grapefruit juice, lol, and report back, for science. Maybe go to the bathroom beforehand.

 

[Hal_1ncandenza]

Some anecdotal evidence:
Drank roughly 500ml of white gf juice last night. Did ~240mg K. I really think that the gf potentiated it. I have a pretty high tolerance right now, but I was in another dimension for 1 hour+

 

[Chris Timothy]

Oh, grapefruit. Not a girlfriend with medical abnormalities..