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Suboxone + St. Johns Wort

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#1 JahRed24



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Posted March 17 2008 - 01:28 PM

OK so the word on the net ('street') is that taking St. Johns Wort with your daily Suboxone dose will actually increase the "good" opiate effects and make it last longer... I have yet to try it but im gonna start my experiment tomorrow and use the SJW for a week and see if i can notice a difference and let you guys know..

!~(By the way, this is a theory and its only useful to people who are addicted to opiates and are on Suboxone to get off opiates, basically it will only work on people that take suboxone/subutex daily)~!

Heres a post from another person on another site on the subject:

Potentiation of Suboxone using St. Johns Wort (SJW)

I already leaked the secret I was shown to a friend; I might as well share it with the world. Most likely someone has already mentioned this concept, but I haven't seen anyone talk about it, so hopefully this is a new theory for you all:

Buprenorphine has one major dealkylated metabolite: Norbuprenorphine. Here is some information on its agonist properties, and binding affinities:

[3]NorBUP exhibited high affinities for µ-, delta -, and kappa -opioid receptors with Ki values in the nanomolar or subnanomolar range, comparable to those of BUP. NorBUP and BUP had low affinities for the ORL1 receptor with Ki values in the micromolar range. In the [35S]GTPgamma S binding assay, norBUP displayed characteristics distinct from BUP. At the delta -receptor, norBUP was a potent full agonist, yet BUP had no agonist activity and antagonized actions of norBUP and DPDPE. At µ- and kappa -receptors, both norBUP and BUP were potent partial agonists, with norBUP having moderate efficacy and BUP having low efficacy. At the ORL1 receptor, norBUP was a full agonist with low potency, while BUP was a potent partial agonist. In the writhing test, BUP and norBUP both suppressed writhing in an efficacious and dose-dependent manner, giving A50 values of 0.067 and 0.21 mg/kg, s.c., respectively. These results highlight the similarities and differences between BUP and norBUP, each of which may influence the unique pharmacological profile of BUP.

Norbuprenophine is a more potent agonist in most areas, and has a higher affinity in most areas. Though it is allegedly not good at crossing the BBB [I lost this citation]. I find though that this may not be entirely true from my own experiences...

Buprenorphine is metabolized into Norbuprenorphine almost entirely by the P450 cytochrome[1]. This being the case, a P450 Inducer should increase the ratio of Nor-buprenorphine to Buprenorphine. Unfortunately there are not many easily obtained P450 inducers on the market...except for one: St. Johns Wort[2].

SJW is actually a fairly potent P450 inducer, and it specifically involves the enzymes most important of the P450's in the creation of NOR-BUP.

[2]The ratios of the treatment to baseline values for CYP3A4 using cortisol as the probe were 1.5 [95% confidence interval (CI) 1.3, 1.9] for males, and 1.9 (1.1, 3.0) for females. The corresponding ratios using dextromethorphan as the probe for CYP2D6 were 0.9 (95% CI 0.5, 2.1) for males and 1.9 (1.3, 3.2) for females. For CYP1A2, a significant increase in the metabolic ratios was found only for females (ratio of values 1.2; 95% CI 1.1, 1.4). No influence of SJW on CYP2D6, NAT2, and XO activities was observed.

CYP3A4 is the primary enzyme involved in the creation of NOR-BUP[3]. The others it induces are also involved in its metabolism; furthering its effect on Nor-bup "synthesis".

This being the case, our theory was such: Taking SJW with Buprenorphine may induce or more opiate like effect than with buprenorphine alone.

Both I and the theories creator found this to be true, inspite of the information stating that Norbuprenorphine has difficulty crossing the Blood Brain Barrier.

Bottom line, tonight was our last human trial: We both have been taking Suboxone for 3 months and it does nothing to me anymore as far as a High goes. When I took St. John's Wort 1.5 hours after taking Suboxone. 45 minutes later I began to enter a manic state. I myself always become manic on opiates. My friend on the other hand becomes quite sedated, and became this way when combining the same two drugs as I. I checked pupil size at this point and found them to be PINPOINT small. About a 45 mintues after this we both began to experience the typical opiate itches. We also ebgan to experience more euphoria then we have had from suboxone since the first days of taking Suboxone, or maybe ever.

For us Saint John's Wort caused Buprenorphine, in Buprenorphine tolerant individuals, to induce a true opiate high. We name this potentiation theory after our muse: We call it the Vickers Method

I do not feel in any way that this was placebo, but no one is immune to the placebo effect. I don't encourage anyone to try this I am simply stating our theory. I would hate to be the person to destroy a "miracle drug".

Dosages Buprenorphine: 12mg Suboxone each (out standard)
Dosages SJW: 600 mg SJW extract ( 0.3 % Hypercin (1.8 mg) )

Again, please we ask no one try this out. We are simply ameteur scholars that had no human subjects other than ourselves.

Be safe everyone, and Props to our Muse.

Some of the sources we used (there were many more):

[1]Characterization of the pharmacokinetics of buprenorphine and
norbuprenorphine in rats after intravenous bolus administration of
Sumithra Gopala ,*, Tsang-Bin Tzenga, Alan Cowanb
aSchool of Pharmacy, Temple University, Philadelphia, PA 19140, USA
bSchool of Medicine, Temple University, Philadelphia, PA 19140, USA
Received 23 July 2001; received in revised form 21 January 2002; accepted 24 January 2002

[2]Effect of St John's wort on the activities of CYP1A2, CYP3A4, CYP2D6, N-acetyltransferase 2, and xanthine oxidase in healthy males and females

* Markus Wenk,
* Liliane Todesco &
* Stephan Krähenbühl

Division of Clinical Pharmacology & Toxicology, Department of Internal Medicine, University Hospital, Basel, Switzerland

[3]Comparison of Pharmacological Activities of Buprenorphine and Norbuprenorphine: Norbuprenorphine Is a Potent Opioid Agonist
Peng Huang, George B. Kehner, Alan Cowan and Lee-Yuan Liu-Chen

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