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  • BDD Moderators: Keif’ Richards

true opiate potentiatators?

A

Anon54

Ex-Bluelighter
Joined
Jun 11, 2010
Messages
861
Cytochrome P450 Drug Interactions
http://www.ildcare.eu/Downloads/arts...teractions.pdf
It lists Diphenhydramine as a potentiator to Oxy, Codeine, Morphine & also Meth which is interesting. So

What about the other antihistamines?

It has no mention of Promethazine or Doxylamine or maybe they're just not included in this chart because I think DPH has to many side effects. I actually like Promethazine. Would be good if that was a potentiator

Can anyone find any links like the one I've provided here that list other antihistamines that are potentiators for opiates?

GFJ appears to only potentiate Hydrocodone, Methadone & Tramadol but not the other opiates.
Off topic, but for anyone interested it listed Valium, K-pins, Xanax & Temaz to be potentiators by GFJ

maybe it's only listing the most common drugs & that's why it only has DPH listed & only 4 benzos because im mostly curious as to whether DPH is the only true opiate potentiator.

Please dont write. Yes I've tried Promethazine & Oxy & it worked great. I want actual sources please.

It would also be interesting to know if Antipsychotics ca potentiate opiates. Seroquel for example if listed on wikipedia as an Antihistamine & most APs are AHs. On this chart they only have those APs as substrates and not inhibitors.
 
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Classic antihistamines, namely diphenhydramine, chlorpheniramine, clemastine, perphenazine, hydroxyzine, and tripelennamine, share structural features with substrates and inhibitors of the polymorphic cytochrome P450 (CYP) isozyme CYP2D6. Therefore, the current study was undertaken to characterize the in vitro inhibition of CYP2D6 by these commonly used, histamine H1 receptor antagonists. Microsomal incubations were performed using bufuralol as a specific CYP2D6 substrate and microsomes derived from human cells transfected with CYP2D6 cDNA. Reaction velocities were assessed in the absence and presence of antihistamines (20 microM) at 11 substrate concentrations (1, 2.5, 5, 7.5, 10, 15, 20, 25, 50, 75, and 100 microM), as well as at three nonsaturating substrate concentrations (2.5, 5, and 20 microM) and three inhibitor concentrations (5, 20, and 50 microM). In the presence of all antihistamines, the Vmax and KM of bufuralol 1'-hydroxylation were significantly altered, compared with the uninhibited reaction (p < 0.05). Lineweaver-Burke plots suggested competitive inhibition of the reaction by diphenhydramine and mixed inhibition by all other antihistamines tested. Diphenhydramine and chlorpheniramine, with estimated Ki values of approximately 11 microM, were the weakest inhibitors of CYP2D6 in vitro. Whereas tripelennamine, promethazine, and hydroxyzine were similar in their inhibitory capacities (Ki approximately 4-6 microM), clemastine appeared to be significantly more potent, with a Ki of approximately 2 microM. These data demonstrate that classic histamine H1 receptor antagonists, available in over-the-counter preparations, inhibit CYP2D6 in vitro. Furthermore, the CYP2D6-inhibitory concentrations of these antihistamines are in the range of their expected hepatic blood concentrations, suggesting that, under specific circumstances, clinically relevant interactions between classic antihistamines and CYP2D6 substrates might occur.
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http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=Retrieve&db=PubMed&list_uids=9616188&do pt=Citation
 
OnCloud9 said:
As far I know, GFJ also potentiates morphine as well.
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Well it didnt say so in the link I provided in the chart. Do u have any sources?
(Im currently trying to find sources that other AHs potentiate opiates.)
 
Thanks Tripman. I think hydroxyzine is otc but i havnt seen it before. Im more interested in the in the commonly used OTC AHs Doxylamine & Promethazine. It would be good to know if Promethazene worked because it has less side effects than DPH. Im also interested in APs like Seroquel & Zyprexa being anithistamines. I get precribed APs. I could take a small dose like 50mg of Seroquel before dosing Oxy in the future if it is a potentiator. Its the only AP on wikipedia listed as an Antihistamine but the most the other APs are also AHs but not as strong.
http://www.genemedrx.com/Cytochrome_P450_Metabolism_Table.php
there is another detailed chart but Im yet to find one that includes APs, Promethazine or Doxylamine. It atleast mentions chlorpheniramine hydroxyzine & Atara as well.
Maybe I'll just stick with DPH if I want something :|
 
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Both promethazine and doxylamine will infact work, if I have time i'll pull some sources for studies on that too.

For now you can have my anecdotal evidence: Coming from an ex-heroin addict - doxylamine is my favourite to potentiate with.
 
Tripman said:
Both promethazine and doxylamine will infact work, if I have time i'll pull some sources for studies on that too.

For now you can have my anecdotal evidence: Coming from an ex-heroin addict - doxylamine is my favourite to potentiate with.
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OK, thanks for the help. Im currently taking Zyprexa but Im going to change back to Seroquel which i will take 100-300mg a night.

Do u think that taking 50mg before taking any opiates could be a potentiator?
It is after all the only AP listed as an AH on wikipedia

Do u know which opiates besides Tramadol, Methadone & Hydrcodone are potentiated by GFJ?
Im just curious because I usually have GFJ with Valium & sometimes I take other opiates with the Valium.
 
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Anon54 said:
Well it didnt say so in the link I provided in the chart. Do u have any sources?
(Im currently trying to find sources that other AHs potentiate opiates.)
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I speak from personal experience on this one, but I'm sure the mods can back me up on this.
 
Here's Pill_head's handy dandy list of potentiators that I have personally tried with hydrocodone and would recommend and I would say is a safe amount when mixed with your regular dose of opiate. Don't exceed what I have listed below, especially your first time. And by the way, if your "regular dose" is an amount that totally knocks you on your ass, makes you puke, black out or whatever, you DON'T need to be adding a potentiator unless you want to end up in the ER.

350 mg Soma (try half a pill or 175 mg if you have no benzo tolerance)
70 mg DXM
25 mg benadryl
0.5 mg Xanax
10 mg Valium (5 mg if you have no benzo tolerance)
 
Potentiate can mean different things to different ppl. The CYP450 "potentiation" you referenced potentiates the same way GFJ does. It potentiates by prolonging the effects of the drug by preventing metabolism as the drug passes through the liver by occupying the enzymes that break down the drug with other things to break down leaving less enzymes available to work on the drug. Promethazine "potentiates" by having a synergistic effect with opiates in that it makes nodding out occur with less opiate than normal. Benzos, alcohol, etc all "potentiate" using the same theory as promethazine but in different ways as the potentiation in this case is simply the combination of 1 + 1 = 1.5 (or 2 or 7 depending).

Search for opiate potentiation mega thread. I printed out prolly 40 - 50 pages worth of info on all manner of ways to improve upon individual opiates and have found the info to be most useful. Dont assume what works for one wil work for another though. For instance, Codeine NEEDS to be broken down by the enzymes in order to work as its converted from codeine to morphine via demethylation. If you take your CYP450 enzyme inhibitors with it you'll get even less than what codeine normally delivers. OTOH, the following was my routine for years until I realized A) Im consuming way too much oxycontin and B) by concocting schemes to ensure it has as little a chance of naturally being eliminated from my body while simultaneously trying to increase its potency I was increasing my chances of a fatal OD exponentially. Be warned...the same thing that makes it feel better and last longer will work against you in a big way if you take too much. That said, heres how to get the most bang for your buck for oxycontin:

1 hour before dose take Tagament (cimitidine) 200mg. This is an enzyme inhibitor (for oxycodone...assume this entire scheme only works for oxyc until you research on your own how these things work on each opiate and to what extent. This is not how Id try to get the most of other opiates per se)

Drink white gfj pretty much constantly from the one hour pre dose mark until about an hour or so after. Some do continually but I dont like the taste enogh. Note that red ruby gfj doesnt have the same effect

take 3 luvox (fluvoximine...not exactly an antipsychotic but an SSRI for OCD thats one of the most potent enzyme inhibitors) 30 mins before dose

take 2x normal dose of sodium bicarbonate 15 mins prior to dose to help max absorption

take another 200mg cimitidine 5 min prior to dose

take dose (reduced to accomodate whatever other synergistic drugs you plan) with any of the following synergistic acting substances: promethazine, benadryl, benzos, nyquil (has three useful ingredients for potentiating...doxylamine succonate, apap and dxm which helps reduce tolerance), etc.

take another 2 luvox with dose.

The above concoction of enzyme inhibitors will extend an oxy buzz by at least 1.5x normal duration. The synergistic agents will determine to what extent the oxy buzz increases in strength. Of course, the best opiate potentiator strength wise imo is more opiates. But search the mega thread for much much much more info. GFJ is an enzyme inhibitor just like cimitidine and works on way more than hydrocodone, methadone and tramadol. And while diphenhydro does potentiate its hardly the best in terms of enzyme inhibition potentiation. There's a shit ton of info out there. First realize "potentiate", while having only one true definition, means different things to different people and your going to get some confusing info if you dont separate potentiation into two groups: makes it last longer and makes it feel stronger.

DPH is most definitely not the only opiate potentiator no matter which definition you go with.
 
NOLA wrote:
It potentiates by prolonging the effects of the drug by preventing metabolism as the drug passes through the liver by occupying the enzymes that break down the drug with other things to break down leaving less enzymes available to work on the drug.
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that's what im looking for. not just drug combos
dr wanted to give me luvox says its an AD but it makes ya tired. i might do a bit of research on why it makes ya tired im assuming its because its an antihistamine like mirtazepine. Whats luvox like, any good?
Pilll_head said:
Here's Pill_head's handy dandy list of potentiators that I have personally tried with hydrocodone and would recommend and I would say is a safe amount when mixed with your regular dose of opiate. Don't exceed what I have listed below, especially your first time. And by the way, if your "regular dose" is an amount that totally knocks you on your ass, makes you puke, black out or whatever, you DON'T need to be adding a potentiator unless you want to end up in the ER.

350 mg Soma (try half a pill or 175 mg if you have no benzo tolerance)
70 mg DXM
25 mg benadryl
0.5 mg Xanax
10 mg Valium (5 mg if you have no benzo tolerance)
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The drugs listed there are actually ones im really interested in whether they're true potentiators
we know benadryl (DPH Is a potentiator but what about the others listed there.
I love mixing opiates with benzos but isnt it simply a good combo? )valium doesnt actually make ya opiate stronger or last longer does it?)
DXM is otc here so i could give that one a try. But is it a combo or a potentiator it would be tempting to drink the whole bottle & go robotripping though :)
be good if someone could right a list like

Valium = combo
DPH = Potentitor
Soma = Combo
GFJ = Potentitor

or something like that.....
 
Luvox is listed as an anti depressant, however, unlike all the other SSRIs that are specified for depression, anxiety, etc. its ONLY specified for control of obsessive compulsive disorder. Can it help with depression? Maybe but I dont know. I actually have OCD and tried various SSRIs before landing on Luvox which is a wonder drug in that regard. Does it make you tired? Not in my experience. In fact I feel zero physical effects from it at all. I suppose the first few days on it maybe but its not a sedative type drug at all. For me it works becuase I take it for OCD but cant comment on depression. Does it work as an enzyme inhibitor? Absolutely. Look at the charts (I didnt look at the one you posted but theres several out there that list them as mild, moderate and strong inhibitors and Luvox is one of the strongest). Hope that helps.
 
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