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Benzodiazepines All about benzodiazepines (downers)

 
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  #76  
Old 12-11-2009, 21:36
hypernovax hypernovax is offline
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Re: Grapefruit Juice and Benzodiazepines

I heard info about this before, I tried white grapfruit juice hours after popping some valiums and it kinda seemed like I just popped 10mg after a bit... although it may have been a placebo... but nevertheless i just drank about 300ml of grapefruit juice and popped 10mg

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  #77  
Old 13-12-2009, 02:10
VirtuallyEmotionless VirtuallyEmotionless is offline
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by hoodabudda View Post
does vitamin c play a role in this because all of these jucies sound like hi vitamin c juices.
No, it's the Bergamottin in the grapefruit juice.
  #78  
Old 15-12-2009, 00:57
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Re: Grapefruit Juice and Benzodiazepines

grapefruit juice just potentiates. swim used to drink a couple litres of GFJ pop a few benadryls nd then do w.e OC i had....makes the high a lot better
  #79  
Old 30-01-2010, 22:18
SyntheticSatori SyntheticSatori is offline
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Re: Grapefruit Juice and Benzodiazepines

Two abstracts taken from a PsycInfo, a journal database I have access to because I am a student at a large university. It took me about 30 seconds to dig these from the literature.

This shows that cimetidine WILL have an affect on alprazolam peak plasma (probably AUC).

The cytochrome P450 IIIA subfamily appears to mediate alprazolam metabolism in humans. Ketoconazole, cimetidine, macrolide antibiotics, and serotonin-reuptake-inhibitor antidepressants impair alprazolam biotransformation in vitro. Reduced clearance of alprazolam in vivo has been demonstrated for drugs in this group that have been studied in humans; for those not yet studied, impaired alprazolam clearance should be anticipated during coadministration. Studies of plasma alprazolam concentration vs clinical response during short-term treatment of panic disorder indicate that therapeutic response at steady-state plasma levels of 20 to 40 ng/mL is significantly greater than at levels less than 20 ng/mL. However, side effects attributable to benzodiazepine agonist activity (e.g., drowsiness, sedation) increase in frequency with increasing steady-state plasma levels. The article is followed by a discussion of its subject matter. (PsycINFO Database Record (c) 2009 APA, all rights reserved)


THis shows grapefuit juice WILL NOT:


The effects of repeated ingestion of grapefruit juice, an inhibitor of cytochrome P₄₅₀ 3A4 (CYP3A4), on the pharmacokinetics and pharmacodynamics of both single and multiple oral doses of alprazolam, a substrate of CYP3A4, were examined. In study 1, 8 healthy volunteers (mean age 31.1 yrs) ingesting 600 ml/day water or grapefruit juice for 10 days took a single oral 0.8-mg dose of alprazolam on the eighth day. Plasma drug concentrations were monitored up to 48 h after alprazolam dosing together with evaluation of psychomotor function. Grapefruit juice altered neither the plasma concentrations of alprazolam at any time points, any pharmacokinetic parameters, nor the majority of psychomotor function parameters in Ss. In study 2, 11 patients (mean age 47.2 yrs) with anxiety disorders receiving alprazolam (0.8–2.4 mg/day) ingested grapefruit juice (600 ml/day) for 7 days. Blood samples were collected before and during grapefruit juice ingestion and 1 week after its discontinuation together with an assessment of clinical status. Grapefruit juice altered neither the steady-state plasma concentration of alprazolam nor the clinical status in patients. Thus, grapefruit juice is unlikely to affect pharmacokinetics or pharmacodynamics of alprazolam due to its high bioavailability. (PsycINFO Database Record (c) 2009 APA, all rights reserved)



It's always good to have hard science on your side.

If anyone needs any more info about those studies or about potentiating other benzos, search the literature. Best way to find out.

SyntheticSatori added 235 Minutes and 16 Seconds later...

Quote:
Originally Posted by hypernovax View Post
I heard info about this before, I tried white grapfruit juice hours after popping some valiums and it kinda seemed like I just popped 10mg after a bit... although it may have been a placebo... but nevertheless i just drank about 300ml of grapefruit juice and popped 10mg
That's not the right way to do it anyways. SWIY needs to drink 2-3 glasses of white grapefruit juice because it takes 30-40 minutes for it to inhibit the necessary enzymes. Drink the juice on an empty stomach, 30-40 minutes later (maybe even an hour later), then take the valium and you will not notice much of a difference in intensity but you will notice an increase in duration.

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Well researched post

Last edited by SyntheticSatori; 30-01-2010 at 22:18. Reason: Automerged Doublepost
  #80  
Old 31-05-2010, 02:35
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Re: Grapefruit Juice and Benzodiazepines

SWIM has a question he could not decipher amongst other material. Grapefruit juice is obviously a promoter of benzo's but does the quantity of grapefruit juice matter (i.e. if he just keeps drinking grapefruit juice instead of say, water for the afternoon)?

Does grapefruit juice intensify the effects exponentially does X amount of juice produce the max effect and it goes no farther than that point?
  #81  
Old 22-06-2010, 04:06
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by dadrone View Post
SWIM has a question he could not decipher amongst other material. Grapefruit juice is obviously a promoter of benzo's but does the quantity of grapefruit juice matter (i.e. if he just keeps drinking grapefruit juice instead of say, water for the afternoon)?

Does grapefruit juice intensify the effects exponentially does X amount of juice produce the max effect and it goes no farther than that point?
The more Grapefruit juice sitting in your small bowel, the less CYP 3A4 will be there, so when your valium or klonopin or whatever passes through that area much less of it will be metabolized, leading to increased serum concentrations, and slowing of the benzo's excretion from your system.

SWIM supposes the benzo intensification via White Grapefruit Juice probably reaches a limit at some point, because not ALL 3A4 is going to be inhibited no matter how much you drink, your genetic code probably has an upper and lower limit to things like that. SWIM might theorize that massive doses of WGFJ on a daily basis for a long period of time (several months at least) could reduce 3A4 to a point so low that respective benzos effects could be exponentially enhanced for a drastically longer amount of time - especially with long acting benzos with extensive half lives.

EDIT: In further dispelling the idea that grapefruit cyp 3a4 inhibition does not have an effect on clonazepam (klonopin), SWIM drank over 70 ounces of 100% white grape fruit juice over the course of the day and has just dosed with 1.5mg of Clonazepam. SWIM feels absolutely drunk and can barely stand up without falling over.

Can some more Clonazepam SWIMMER stry the white grapefruit juice deal, report your effects and see if we can put a rest to the back and forth contradicting theories? A few people in this thread have already said they felt it potentiated their k-pins.

Last edited by Roads; 23-06-2010 at 03:47.
  #82  
Old 31-07-2010, 20:35
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Re: Grapefruit Juice and Benzodiazepines

Swim keeps his fridge stocked with ruby red grapefruit juice. Swim always drinks a couple glasses before every alprazolam and tramadol dose, he notices a huge difference when doses are taken without the gfj.
  #83  
Old 04-01-2012, 21:43
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Re: Grapefruit Juice and Benzodiazepines

Hi all

From what I have researched inhibiting the cytochrome P₄₅₀ 3A4 (CYP3A4) with grapefruit juice leads to a build of toxins that are normally metabolised out CYP3A4.

Just my 2 cents worth


cheers
  #84  
Old 04-01-2012, 22:07
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Re: Grapefruit Juice and Benzodiazepines

Sources?

Because to me it sounds like you are saying that eating grapefruit is dangerous, and that sounds like crazy talk to me.

Journal articles concerning this should be uploaded to the file archives and linked to your post. Since you are new here, you can't really do that, so head up to the "medline access thread", post the citations, and someone will help put them in our database, once there they can be added to this thread.

Just to clarify, it isn't like people are using some sort of irreversible MAO-I on their liver here, just eating some well known fruits and vegetables.


ADDED:

I see some old s asking about the quality of the juice and I have to say yes, there is a significant difference between good quality grapefruit juice and some of the lower quality juices. I've always found fresh squeezed to be superior, not just because I find low grade GFJ terrible, but I suspect too much pasteurization and the reconstituting process probably wreck havoc with GFJ much in the same manner as Raw Milk is ruined during processing. I can't offer any studies, but after you run a few trials, you'll agree
  #85  
Old 04-01-2012, 22:46
frost458 frost458 is offline
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Re: Grapefruit Juice and Benzodiazepines

Cytochrome P450 is a group of enzyme, does grapefruit juice as an impact on all of them?

CYP1, CYP2 and CYP3
and their sub-familly :
CYP1A, CYP2D, etc,
CYP3A4, CYP2D6, etc.
  #86  
Old 22-06-2012, 15:28
Duke of Aquasparta Duke of Aquasparta is offline
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Re: Grapefruit Juice and Benzodiazepines

I have a friend who has tried white grapefruit juice and tagamet as noted in these forum posts to potentiate benzodiazepines with good results. His doctor agrees with his assessment. However, he has reported to me that baclofen (a muscle relaxant and not a controlled substance) potentiates benzodiazepines to an even greater degree and works with both xanax and klonopin so much so that w/o baclofen he feels little results from benzos w/o using baclofen. Methinks that your body must build up some kind of dependency on baclofen after using it with benzos for some time. He reports that the specific manufacturer of generic baclofen may also play role as he claims the Northstar brand is the best manufacturer as he has used other manufacturers w/o the same success. He has sourced this manufacturer from both Cub Foods and Costco (Costco has by far the cheapest price on meds and you do not even have to be a member to use their pharmacy).

He takes six 20mg of baclofen every night with his benzos. Timing is not an issue as he takes his benzos right along with the baclofen.

Please keep in mind that since baclofen more strongly potentiates benzos (as he claims) to go about using it carefully so as not to OD.

Duke of Aquasparta added 9 Minutes and 29 Seconds later...

When I wrote in my previous post the line, "His doctor agrees with his assessment." this was not properly placed. His doctor agrees that baclofen will potentiate benzos so his experience with baclofen and benzos is backed by his doctor.

Last edited by Duke of Aquasparta; 22-06-2012 at 15:28. Reason: Automerged Doublepost
  #87  
Old 23-06-2012, 16:17
dkane180 dkane180 is offline
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Re: Grapefruit Juice and Benzodiazepines

I can promise for a fact that taking 600mg Cimetidine 1 hour before a dose of Alprazolam will greatly increase it effectiveness significantly. Adding a little grapefruit juce doesn't hurt either but sn't as effective as the cimetidine.
  #88  
Old 23-06-2012, 21:52
kailey_elise Gold member kailey_elise is offline
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Re: Grapefruit Juice and Benzodiazepines

I just want to mention, most of those "Ruby Red" grapefruit juices have very little actual GFJ in them. Even the "100%Juice!" ones - read the label; most of the juice is of apple and/or white GRAPE variety & these are basically sugar.

Most of the "good stuff" is in the peel of white grapefruits. Therefore, the best way to get the most out of your GFJ experience is to obtain 100% white grapefruit juice CONCENTRATE. The way they squish up the grapefruits to get the most juice out of them ends up putting the juices & oils from the peels too.

I've found that if one wants the health benefits you can obtain from white grapefruit juice, the easiest way is to get the concentrate, put a tablespoon or so in a glass and then pour some other juice over it to melt the concentrate. I like pineapple, as it almost seems to cover the taste of GFJ. Now, this is less of a worry if you actually like the taste of GFJ! *grin* Anyway, I put in just enough juice to get it melted, then belt it back, followed by a glass of water. (I *really* dislike the taste of GFJ!)

Be careful when doing this! Remember you can always take more, but you can't undo what you've already taken!

~Kailey
  #89  
Old 27-07-2012, 22:20
mPRH mPRH is offline
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Re: Grapefruit Juice and Benzodiazepines

...............................

Last edited by mPRH; 28-08-2012 at 08:25. Reason: unintentional derailment. my bad.
  #90  
Old 19-08-2012, 05:58
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Re: The Combined Grapefruit Juice and Benzodiazepines Thread

Yes it will have the same effect because it's a benzodiazepine. Klonopin has a longer half life than xanax though, so SWIM might feel buzzed longer.

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Just because is a benzo it doesn't mean its true, they are metabolised by more than one enzyme
  #91  
Old 22-10-2012, 00:42
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Re: Grapefruit Juice and Benzodiazepines

For the person asking about Nitrazepam, on the insert it mentions cimetidine and grapefruit juice (among others) should not be used while taking this product. That spells potentiators to me.

For the person asking about baclofen adding to the effects, I would say it's the complete opposite.
I take 230mg daily baclofen. To me I get little effects except the hypnotic portion (sleep) which is why I primarily ever use them now anyways, too bad.

Baclofen is a gaba b agonist and I am guessing at higher doses that effect outweighs the gaba a effects of the benzo. Just a guess. Perhaps at a low dose of baclofen but I would be surprised.

I have not had luck with grapefruit juice but my chemistry is whacky thanks to the baclofen.

I may try it with the nitrazepam but not sure how I would measure that since it's really just a sleep agent.
  #92  
Old 15-11-2012, 15:51
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Re: Grapefruit Juice and Benzodiazepines

Hello, does anyone know if adding Valium to morphine sulfate is an appropriate way to increase the effectiveness od the analgesics which I hve been using. The Dr told me to add my valium to my MSIR dose, but nothing, and I really do not want to take 16 tabs of MSIR per dose to stop the pain. I als do not want to die, and he has me on a cocktail of Baclofen, Valium and MSIR. Anybody ever heard of this. Oh, I also have Gabapentin, which appears to work better than anything else.

Would Grapfruit juice increase the strength of any of these ??
  #93  
Old 18-12-2012, 03:56
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by zerox38 View Post
Hi all

From what I have researched inhibiting the cytochrome P₄₅₀ 3A4 (CYP3A4) with grapefruit juice leads to a build of toxins that are normally metabolised out CYP3A4.

Just my 2 cents worth


cheers
1) I don't know if the above is true or not. Is it?

More importantly:

2) Are there ANY health risks associated with potentiating benzos with grapefruit juice (besides the obvious increased OD risk) ?
  #94  
Old 23-12-2012, 21:14
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by Roads View Post
The more Grapefruit juice sitting in your small bowel, the less CYP 3A4 will be there, so when your valium or klonopin or whatever passes through that area much less of it will be metabolized, leading to increased serum concentrations, and slowing of the benzo's excretion from your system.

SWIM supposes the benzo intensification via White Grapefruit Juice probably reaches a limit at some point, because not ALL 3A4 is going to be inhibited no matter how much you drink, your genetic code probably has an upper and lower limit to things like that. SWIM might theorize that massive doses of WGFJ on a daily basis for a long period of time (several months at least) could reduce 3A4 to a point so low that respective benzos effects could be exponentially enhanced for a drastically longer amount of time - especially with long acting benzos with extensive half lives.

EDIT: In further dispelling the idea that grapefruit cyp 3a4 inhibition does not have an effect on clonazepam (klonopin), SWIM drank over 70 ounces of 100% white grape fruit juice over the course of the day and has just dosed with 1.5mg of Clonazepam. SWIM feels absolutely drunk and can barely stand up without falling over.

Can some more Clonazepam SWIMMER stry the white grapefruit juice deal, report your effects and see if we can put a rest to the back and forth contradicting theories? A few people in this thread have already said they felt it potentiated their k-pins.
Me myself tonight is probably going to try it, as I have not found anything else that's cheap you can retrieve at a grocery store that would help. I will message you.
  #95  
Old 25-12-2012, 09:38
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by dreamz View Post
1) I don't know if the above is true or not. Is it?

More importantly:

2) Are there ANY health risks associated with potentiating benzos with grapefruit juice (besides the obvious increased OD risk) ?
Anyone?

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  #96  
Old 25-12-2012, 15:16
methylman251 methylman251 is offline
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by dreamz View Post
1) I don't know if the above is true or not. Is it?

More importantly:

2) Are there ANY health risks associated with potentiating benzos with grapefruit juice (besides the obvious increased OD risk) ?
1. The original post quoted 'inhibition of 3A4 leads to the build up of toxins normally metabolised out'. Given that there are probably tens of thousands of toxins I am sure he isn't completely wrong. Is the statement relevant to the discussion and people looking at potentiating benzo with grapefruit juice? Unless you spend your days eating mouldy foods and poking snakes and spiders with sticks - No.

2. No, unless you are taking a prescribed medication which you haven't heard of before and don't know much about as some are not to be fucked with. If you are a quick search on google scholar, medline or anything else reputable (not wikipedia - with something pharmacology related it is an incomplete and sometimes completely inaccurate source of information) with "[prescribed drug you are taking - drug name not brand name] metabolism" or if that fails "[prescribed drug you are taking]" and "CYP3A4" read the abstracts of the first few papers. If CYP3A4 is mentioned do a more in depth search or post on DF.
  #97  
Old 27-12-2012, 03:19
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by methylman251 View Post
1. The original post quoted 'inhibition of 3A4 leads to the build up of toxins normally metabolised out'. Given that there are probably tens of thousands of toxins I am sure he isn't completely wrong. Is the statement relevant to the discussion and people looking at potentiating benzo with grapefruit juice? Unless you spend your days eating mouldy foods and poking snakes and spiders with sticks - No.

2. No, unless you are taking a prescribed medication which you haven't heard of before and don't know much about as some are not to be fucked with. If you are a quick search on google scholar, medline or anything else reputable (not wikipedia - with something pharmacology related it is an incomplete and sometimes completely inaccurate source of information) with "[prescribed drug you are taking - drug name not brand name] metabolism" or if that fails "[prescribed drug you are taking]" and "CYP3A4" read the abstracts of the first few papers. If CYP3A4 is mentioned do a more in depth search or post on DF.
Thank you, I'm finding that "Adderall (amphetamine) metabolism is not clearly defined, but CYP2D6 is definitely involved, it has minor inhibition of 1A2, 2D6, and 3A4." Does that mean that grapefruit juice could somehow had adverse effect on a person taking Adderall? No, right?
  #98  
Old 27-12-2012, 05:36
methylman251 methylman251 is offline
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Re: Grapefruit Juice and Benzodiazepines

God I just wasted so much time.... Tried to search for what enzymes metabolise amphetamines and was wondering why I couldn't get anywhere and why it was so damn hard then I remembered that amphetamines don't really get metabolised well so they are just excreted renally (urine via the kidneys). Only a proportion of amphetamines gets metabolised but the amount that does is via 2D6. Grapefruit juice only really inhibits 3A4 so grapefruit wouldn't have a large impact. However 2D6 is inhibited by some SSRI's strongly, some SNRI's moderately and is inhibited but no one has checked by how much by a fair few anti-psychotics, antihistamines and a miscellaneous selection of other drugs.

Because the majority of it is cleared anyway by the kidneys it wouldn't just sit and float around forever but it would mean that it lasts longer so it is something you'd definitely want to take into consideration.
  #99  
Old 27-12-2012, 07:52
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Re: Grapefruit Juice and Benzodiazepines

I have a question that maybe somebody here can help with. I was told at hospital that my liver enzymes are slightly elevated and stop drinking. So I've been using xanax because I ran out of blood pressure medicine last week. I know self medicating is stupid, but I'm awaiting approval to get the county hospital insurance. I don't want to have another stroke. Will the grapefruit juice affect my liver capacity along with xanax? I know it's gotta be better than alcohol but could it mess me up? Thanks for any advice!
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Old 31-12-2012, 02:57
RoK Krawler RoK Krawler is offline
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Re: Grapefruit Juice and Benzodiazepines

Quote:
Originally Posted by methylman251 View Post
Because the majority of it is cleared anyway by the kidneys it wouldn't just sit and float around forever but it would mean that it lasts longer so it is something you'd definitely want to take into consideration.

LMFAO
You never herd of the spun out meth heads drinking truckers piss they find in bottles at rest areas?

They got it in their head, After two weeks up, That all truckers were usuing amphetamines so they were stalking rest areas and would drink trucker piss lol. We knew about it so we did it just so they drank piss for no reason.

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benzodiazepine potency, cyp2d6, cyp3a4, cyp450 inhibitor, grapefruit juice, potentiating benzodiazepines

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