Grapefruit Juice and Drug Bioavailability

I was flipping through my collection of drug-related books and articles and I found that quite a few were related to grapefruit juice. Grapefruit juice? That sounds like my experience with mangoes amplifying a trip, which I wrote about here if you're curious. I thought maybe there was some correlation, so I investigated furthur.

Drug bioavailability is the percentage of a drug that you ingest that actually makes it to its biological target. When you take a drug orally, whether it's LSD or aspirin, some of it is metabolized (digested & taken apart) before it can reach your bloodstream. If you inject a drug, its bioavailability is 100%. Grapefruit juice will increase the bioavailability of certain drugs by interfering with the metabolizing process, and therefore increase their effectiveness and potency.

Scientists first discovered this when they were experimenting with the effects of mixing alcohol and another drug, felodipine. With their test subjects, they used grapefruit juice to mask the flavor of the alcohol mix as they drank it, and it ended up increasing the bioavailability of the felodipine. Even a single glass of grapefruit juice, taken within 24 hours of the administered dose, will create these effects.

Other scientists found that cytochrome, which occurs naturally in the small intestine and is responsible for the metabolizing of certain molecules, is what the grapefruit juice inhibits. Though it's not known exactly what chemical in the juice causes it, they have narrowed it down to a few theories: naringin (which doesn't occur in other fruit juices and is known to limit metabolism), quercetin, kaempferol, furanocoumarians, and bergamottin. In case you were curious.

What does this mean for recreational drug use? Well, unfortunately, not much. Though it increases bioavailability in a variety of substances, it doesn't do so for all of them. One chemical it does affect is setraline, also known as Zoloft. It is a Selective Serotonin Reuptake Inhibitor, or SSRI, meaning that it prevents your body from reabsorbing and metabolizing serotonin, a neurological chemical that plays a part in keeping you happy. By keeping more serotonin active in your body, your mood stabilizes. By increasing the bioavailability of SSRIs, grapefruit juice makes them more potent. LSD also functions by serotonin-- it blocks serotonin's receptors because of its similar shape. Therefore, grapefruit juice shouldn't have an effect on LSD and related hallucinogens, unless you're taking an SSRI already, and then it will make the LSD even less effective.

Of course, I am not a biologist or a chemist; just a careful reader and researcher. If I drew an incorrect conclusion or you know something more on the matter, please tell me in the comments and I will edit the post.

tl;dr: To the best of my knowledge, grapefruit juice will not make hallucinogens any more potent, and will actually decrease potency furthur if one is already taking an SSRI.

Source:

Food-drug interaction: grapefruit juice augments drug bioavailability-- mechanism, extent and relevance

by A. Dahan and H. Altman

Psychedelic Artist Alex Grey

You don't need to be tripping to appreciate Alex Grey's intricate artwork, because he will take you there himself. He combines his passion for artwork with his medical knowledge of anatomy and with the insights from his drug experiences.

His most acclaimed series, Sacred Mirrors, invites introspection through depictions of various ways of looking at the self. It took him ten years to complete. Much of his artwork continues in the same style.

I love the way that he states complex concepts in a manner that is both beautiful and non-lecturing. His paintings go past the literal, and they say to me a lot about the miracle of life and the beauty of science. The fact that we understand the tiny tickings of our bodies doesn't diminish how transcendent our bodily experiences can be.

To hear about his life, artwork, and philosophy from the man himself, here's an interview that will also show you a lot of his best works. Listening to him speak is great, because even though his artwork is pretty far-out, he doesn't conform to the stereotype of a spacey, strung-out artist. He is eloquent and cohesive, and a pleasure to listen to.

Here's another one about his Ayahuasca experience:

Alex Grey makes me wish I was an artist, because words can't describe the things that he shows so eloquently. All I can hope for is to someday be as intelligent and thoughtful as he is. Wish me luck, I'll need it!

Time Flies... or Jumps, or Skips, or....

Trouble and confusion regarding the passage of time is a really common characteristic of hallucinogenic experiences. Some people find it pleasant when time slows down or seems to behave strangely, and others will become baffled and anxious. This is sometimes exacerbated by the need to keep track of time for worldly engagements, or by paying too much attention to where you are in relation to your peak. Time perception is a really intricate brain process, involving many different pieces working together, and is by no means regular or infalliable.

There are many things that can affect your time perception even while sober. For example, the efforts of your eyes to maintain a clear picture can affect time perception. The eye actually makes many more jerky motions than we notice, and therefore has processes in place to give us the movie that we're used to. If you move your eyes very quickly to a clock with a second hand, you'll see that that one second seems to last longer than it should. The visual parts of the brain extend that image backwards in time so you perceive a smoother transition between your last focus and this new one.

I am by no means an expert on this matter, but from what I do know of perception and hallucinogens, these drugs affect the way your brain integrates the information that comes to it. I assume that that is why you sometimes see multiples-- your brain loses the ability to mesh the images from each of your eyes together. The kaleidoscope or fractal effect seems to me to be a result of the doubling of the edges of complex or irregular shapes, like clouds. Therefore, it's not a stretch that maybe the parts of your brain involved in time misfire similarly. LSD (I'm not so sure about other hallucinogens) results in sleeplessness and a loss of appetite, which may affect the Circadian Rhythm, which is the body process that tells you when it's time to eat and sleep. And experiencing novel things makes time seem to slow, and with hallucinogens novel is the name of the game.

My first trip was really interesting in this regard, and I didn't take it very well. I was reminded of this by both my friend's trip the other day and because I found my graphical representation of my time perception during that trip while I was cleaning out my drawer. :)

My ex-boyfriend took me out to the nearby park for my first peak. I figured I would feel very comfortable there because we hung out there a lot, but it was an unseasonably nice day so it was very crowded. It began to remind me strongly of a day that I had spent there with him a year earlier, and as that idea began to grow in my mind I became very confused. It seemed that the year had formed a loop, and that it was up to me to figure out the secret of breaking the loop so we didn't endlessly relive that year. Obviously, I had no idea how to go about this. I asked him if we could go back to his house, and he agreed. I sat down on his bed and asked for a piece of paper so I could try to explain my problem in a drawing. "I'm confused," I repeatedly whined. I felt that something important had happened on the journey home (probably just my peak) but I couldn't remember it.

TRANSCRIPTION:

I was trying to explain to you how time kept getting reset every 20 seconds. Minutes feel like hours. I feel like... who knows. I should just let it do its thing. I can't wrap my head around time. Like, the leaves could have been spring or autumn and then it was the day we met, it was a funeral was a wedding everything kept getting reset. What the hell was up with the pinecones? It seems tragic that I could have made that much of a fool of myself. I should stop fighting.

Time just got too much for me to handle. I should let myself float. I shouldn't be this confused.

All I can see are the leaves on the ground-- registers as orange. Orange? Could that be right? What? What day is it? Suddenly this matter o time is of utmost importance

I am glad that I saved this because I find it hilarious. :)

SOURCES

First Science

Wikipedia

Microbes & LSD: Disappointing Hype

Scientists are making LSD from microbes? Hardly. I was really excited when I first saw this article, but its title is woefully inflated, although the actual facts are still pretty cool.

There's a guy named Jake Wintermute whose job is to make synthetic biofuels. He was kidding around one day and said that he'd like to make LSD, since it's so expensive. LSA, a related compound, is currently synthesized from the Ergot fungus and then purified and used to make a dementia medicine called nicergoline. Right now he's working on genetically modifying yeast to make this compound (just add water!) but he's only one third of the way there.

This is not a "living LSD factory." He's doing perfectly legal and legitimate things with that yeast. However, it would be great to be able to make LSA that easily, since it's also hallucinogenic: it's what you get from eating morning glory seeds. I'd love to be able to buy that at the supermarket, but unfortunately, that's not what's happening. At all.