Pharmacology - Grapefruit Juice and Benzodiazepines

[hoodabudda]

does vitamin c play a role in this because all of these jucies sound like hi vitamin c juices.

[rod]

Swim has been trying a 1000mg of vitamin c w/other minerals its called emergeyc from/Wall----. Swim`s said it would cover benzo`s, along w/4 325mg of aspirn 2 hrs b4 urine test would work. It was as worthless as something called The Stuff which had a money back guarentee, which swim mailed back 3 months ago and is still waiting 4 refund, howerver with the emergencyC swim hasnt had a cold or sniffles once. thats about all it is good 4 it comes in a box of 36 pcks. it mixes w/4 ozs of water.

[testodan]

Does orange juice has an effect too?

[Jatelka]

^^^ No

Please read the rest of the posts in this thread!

[hoodabudda]

the antacid/antiulcer drug ranitidine (zantac if swim remebers correctly)has been proven to be a moderatly powerful inhibitor of the enzyme that removes both benzos and alcohol from the body which increases the effects noticably.http://www.ncbi.nlm.nih.gov/entrez/q...&dopt=Abstract http://www.blackwell-synergy.com/doi...1993.tb06944.x cimitadine(tagment) was used in these tests but ranitadine is listed as more effective than its cousin cimitadine at http://www.medscape.com/viewarticle/464898_4 many other drugs are in this family all with varying potencies.swim wonder if any of the variations would work better than ranitadine.

[rod]

Originally Posted by hoodabudda

the antacid/antiulcer drug ranitidine (zantac if swim remebers correctly)has been proven to be a moderatly powerful inhibitor of the enzyme that removes both benzos and alcohol from the body which increases the effects noticably.http://www.ncbi.nlm.nih.gov/entrez/q...&dopt=Abstract http://www.blackwell-synergy.com/doi...1993.tb06944.x cimitadine(tagment) was used in these tests but ranitadine is listed as more effective than its cousin cimitadine at http://www.medscape.com/viewarticle/464898_4 many other drugs are in this family all with varying potencies.swim wonder if any of the variations would work better than ranitadine.

Swim recently had to give a urine and swim had been on zantac for 1 year. The zantac didnt help a bit. Swim had been takin it easy on valium cause swim knew it was bout time for the urine. Swim had took zelnorm which is 4 irritable bowel syndrome, when swim took this 1 x a day swim had no trouble passing a urine, no matter how much valium swim used that month. The bad thing they took it off the market in the us. It was causin unsual bleeding and heart attacks. Last week swim was given somin in its place. In 3 weeks or so swim will let you knoif this covers it

Reputation Comments on this post:

Learning to swim

[hoodabudda]

^^^swim tried this with 1.25 mg lorazapam(ativan) and noticed a longer lasting high than usuall. he had absained from benzos(but not zolpidem/ambien IDK if there is cross tolerance.) for a week before so tolerance was minimal.swim wonders what a combo of this plus grape fruit juice would be like....mabey next week

[Laudaphun]

Temazepam (Restoril) definitely is potentiated by ruby red pink grapefruit juice in me... I really believe this to be true, but I am not so proud to admit there is a small chance that it could be placebo effect... I really am 95% sure that it potentiates temazepem.... speeking of which its time for bed.

[hoodabudda]

anyone else tried the acid reducer (zantac or pepsid or tagment)it really works quite well, the peak seems to last a lot longer probably by a good 20-30 min at least,swim reccomends it,it is now a must for swim he always has a few ranitadine incase he scores some benzos

[allyourbase]

SWIM has never found grapefruit juice to help benzodiazapines....it should in theory....but it hasnt in SWIM's practice.

[Jatelka]

SWIJ would like some more qualitative reports here:

How much benzo would it normally take to feel effect? How much grapefruit juice did the flamingo imbibe? How much benzo did it actually take to feel effect?

Experiences with the other juices mentioned are also most welcome

[Nargyle]

the little leprechaun that lives in swim's garden first drank 2 glasses of graperuit juice and 30 minutes later ingested 20mg valium, he says the feeling he got was similar to doing 40mg valium, he's really joyeus that now he can make his benzos last longer
, and the doctor won't get suspicious of him renewing his prescription too often

Reputation Comments on this post:

good data, thanks for the report

[pankreeas]

What about a tolerance re: needing more and more grapefruit juice? ask the leprechaun if he's ready to stock up on grapefruits! they aren't always in season you know. And in the offseason the juice can be more expensive effects wise than benzos.

[allyourbase]

SWIM has tried: 300 ml grapefruit juice 30 minutes prior to oral dosing with 4 mg alprazolam - no noticeable impact

600 ml grapefruit juice 1 hour after ingestion of 2 mg alprazolam - no noticable impact

6 ~ 27 oz glasses of (30% actual juice) ruby red grapefruit juice starting 45 minutes before and not finishing the juice until about half an hour after oral dosing with 2 mg clonazepam - no impact

swim has tried similar experiments with diazepam as well, to no avail. it would be nice if it worked as well as with opiates. so much money could be saved.

SWIM needs 2 mg of alprazolam to even feel it slightly. the clonazepam bit mentioned above occured during a "dry spell" and swim was left heavily dissappointed.

[Laudaphun]

to be a little more specific to a previous post, SWIM is prescribed 30mg restoril at bedtime. SWIM finds that if he takes his normal prescribed dose of 30mg more than 2 days in a row, that, on the third day there will be very little effect. SWIM discovered that he was able to extend this an extra day or two with the use of 4-8oz of ruby red grapefruit juice... basically just a couple mouthfuls to get the pills down. SWIM will admit that it is entirely possible that it could have been a placebo effect, however he's been regularly prescribed restoril for 1 1/2 years and was convinced enough on several occasions that, now he never takes his restoril without ruby red grapefruit juice (and on an empty stomach.)

SWIM is also prescribed librium, which he doesn't take very often and has never noticed any increase in effect with the same amount of the same juice.

[all_time_high]

SWIM would like to know if grape juice can potentate nitrazepam. Any help would be appreciated

[Jatelka]

Wild grape juice is apparently a CY3PA inhibitor. Regular grape juice: No

SWIJ has to confess she has no idea what "Wild" grape juice is, she's certainly never come across it.

(Goes off to try and refind reference)

Reputation Comments on this post:

you've got some great leads on fruit based enzyme potentiators in this thread, thanks for a new line of experiments

[merc11292]

swim is a frequent user of diazapam for anxiety purposes and infrequently for recreation, swim doesnt completely understand how, but does know that grapefruit juice makes benzo's feel stronger, could anyone tell swim how grapefruit juice should be consumed with benzo's safely.

[psyche]

Wild grape juice is apparently a CY3PA inhibitor. Regular grape juice: No

I'd like to have this one clarified, becuse I find conflicting info on this one. Could these 'white' and 'regular' be synonyms to 'red' and 'white' when talking about GFJ? Paracelsus claimed that both of these have activity. And according to his own experience white is even more effective, but from what I've gathered both of these work.

[Jatelka]

Bear in mind people that "Grape" and "Grapefruit" are 2 different things!

Grapes = Grow on vines, come in red, white and (apparently) "wild". Only "wild" grape juice is reported to have CY3PA activity (only reference I have been able to find is linked to above). The others are used to make wine.

Grapefruit = Citrus fruit, commonly eaten for breakfast. Both Ruby and White grapefruit juice have CY3PA activity

"Grape" does NOT = "Grapefruit"

[psyche]

Benzos theoretically potentiated by grapefruit juice, but effects probably not clinically significant (because of high oral bioavailability):

Clonazepam (Klonopin), Lorazepam (Ativan), Chlordiazepoxide, Flurazepam (Dalmane), Temazepam (Restoril)

Wouldn't it still make the effects last longer if the only metabolic pathway is through the inhibited hepatic cytochrome enzyme? And in that case it would prolong the effects of snorted benzodiazepines too, which are metabolised by this enzyme, right?

[Paracelsus]

trptamene (?) uploaded a trial with different amounts of grapefruit juice and midazolam (search it in the archive if you wish). It concluded that small (~200 ml) amounts of grapefruit juice inhibit only intestinal CYP3A (and therefore just raise bioavailability due to elimination of first-pass metabolism), but large amounts (can't remember the exact amounts) were shown to also inhibit hepatic (liver) CYP3A.

The obvious conclusion is that large amounts of grapefruit juice can, besides potentiating CYP3A substrates by inhibiting first-pass metabolism, also prolong their duration. This most likely also applies to injected/snorted benzodiazepines. Although this is, to my knowledge, the only study about how large amounts of grapefruit juice work, the implications are certainly interesting.

[Jatelka]

I'm feeling magnanimous (and I love to get people looking at the archive!) so here are some links for those who can't be bothered to search...

http://www.drugs-forum.com/forum/loc...3438&catid=129
http://www.drugs-forum.com/forum/loc...1321&catid=129

be warned: I'm not always this generous

[Jatelka]

Talking of links, I've managed to find the full articles on the effects of other fruit juices on cytochrome.

Theoretically: pomegranate, star fruit, black mulberry and (the previously mentioned) "wild grape" are also effective inhibitors

have also found a fascinating article on the different effects of different compnonents of GFJ on different cytochrome enzymes

Acrobat seems to be screwed currently, so the archive links will have to wait: So watch this space....

[Laudaphun]

Potent CYP3A Inhibitors

Azole antifungal agents— Ketoconazole and itraconazole are potent CYP3A inhibitors and have been shown in vivo to increase plasma alprazolam concentrations 3.98 fold and 2.70 fold, respectively. The coadministration of alprazolam with these agents is not recommended.

Other azole-type antifungal agents should also be considered potent CYP3A inhibitors and the coadministration of alprazolam with them is not recommended (see
CONTRAINDICATIONS).

Drugs demonstrated to be CYP 3A inhibitors on the basis of clinical studies involving alprazolam (caution and consideration of appropriate alprazolam dose reduction are recommended during coadministration with the following drugs)
Nefazodone—Coadministration of nefazodone increased alprazolam concentration two-fold.

Fluvoxamine—Coadministration of fluvoxamine approximately doubled the maximum plasma concentration of alprazolam, decreased clearance by 49%, increased half-life by 71%, and decreased measured psychomotor performance.

Cimetidine—Coadministration of cimetidine increased the maximum plasma concentration of alprazolam by 86%, decreased clearance by 42%, and increased half-life by 16%.

The above was copy 'n pasted from a xanax package insert. While this isn't exactly grapefruit juice, it basically still working in a similar manner if I am correct. SWIM will have to do an experiment on his lab rat... 86% should be enough to definitely notice or not.