Bupe Prednisone and buprenorphine, CYP3A4 inducer

[hatrix]

I just want to confirm that what I've read up on the interaction between these two drugs is correct.... Prednisone is an inducer of cytochrome P450 3A4, so if I took prednisone along with a 2-4mg dose of buprenorphine, it would cause more norbuprenorphine to be metabolized, resulting in more norbuprenorphine at my mμ receptors.

I may totally have this backwards though, and it may just cause the drugs half life to shorten and the duration of the high, and not actually increase intensity/potentiate the effects at all.

Anyone have any insight on what taking prednisone with buprenorphine would do metabolite wise? I looked at the charts, but I'm not sure I'm fully understanding inhibitors vs inducers.

I don't want to take the prednisone solely to increase the high I get from bupe, I'm taking it for allergy related reasons, but when I read up on it being an inducer of CYP3A4, it got me thinking it would increase the high I'm already receiving from the bupe I took a little bit ago.

This may be more suited for ADD, but that's a mods call. Hopefully someone knows the correct answer to my question.

And for reference, I was looking at this list. Ignore the highlighted in red comment, the formatting isn't going to copy over and it doesn't matter anyways for this purpose.

Here is a list of CYP3A4-modulators as well as substrates. The list is taken from http://www.uspharmacist.com/oldforma...article_id=704, and there you can also find a similar listing for CYP2D6-interactions.

Highlighted substances in red are considered as of higher interest for Bluelighteners (my own selection).

3A4 inhibitors: Cimetidine, Clarithromycin, Clotrimazole, Delavirdine, Diltiazem, Erythromycin, Fluconazole, Fluoxetine, Fluvoxamine, Grapefruit juice (6,7-dihydroxybergamottin), Indinavir, Intraconazole, Ketoconazole, Metronidazole, Mibefradil, Miconazole , Nefazodone, Nelfinavir, Nifedipine, Norfloxacin, Omeprazole, Paroxetine, Propoxyphene, Quinine, Ritonavir, Saquinavir, Sertraline, Troleandomycin, Verapamil, Zafirlukast

3A4 substrates: Alfentanil, Alprazolam, Amiodarone, Amlodipine, Astemizole, Benzphetamine, Carbamazepine, Cilostazol, Cisapride, Chlorpromazine, Clarithromycin, Clonazepam, Cocaine, Cortisol, Cyclophosphamide, Cyclosporine, Dantrolene, Dapsone, Delavirdine, Dextromethorphan, Diazepam, Digitoxin, Diltiazem, Disopyramide, Enalapril, Erythromycin, Estradiol, Estrogen, Ethosuximide, Ethylmorphine, Etoposide, Felodipine, Flutamide, Fluconazole, Indinavir, Itraconazole, Ketoconazole, Lidocaine, Loratadine, Lovastatin, Mephenytoin, Miconazole, Midazolam, Nefazodone, Melfinavir, Nevirapine, Nicardipine, Nifedipine, Omeprazole, Paclitaxel, Paracetamol, Prednisone, Propafenone, Progosterone, Quetiapine, Quindine, Ritonavir, Saquinavir, Sertraline, Simvastatin, Tacrolimus, Tamoxifen, Testosterone, Triazolam, Venlafaxine, Verapamil, Vinblastine, Warfarin (R isomer), Zolpidem

3A4 inducers: Carbamazepine, Dexamethasone, Ethosuximide, Isoniazid, Nevirapine, Phenobarbital, Phenytoin, Prednisone, Prednisone, Rifabutin/Rifampicin

 

[David Wooderson]

prednisone is can be some real nasty shit...

It's the onl substance that had me trying to climb walls, you couldn't get me to take that shit if it guaranteed the best opiate high available period.

 

[Kittycat5]

You have the basics down. Induction of CYP enzymes causes an overexpression of them leading to increased formation of the metabolite. This often leads to subtherapeutic results as more of an inactive substance is forming. But if the metabolite is also an active compound, and a more potent one than the parent, you will have an increase in effects.

But bupe is a funny drug. Although buprenorphine is a partial and norbuprenophine possibly a full agonist at MOR, buprenorphine seems to be the compound that results in more significant analgesia. This is because norbuprenorphine is also a substrate for P-glycoprotein (Pgp) and buprenorphine is not. Pgp is a protein that helps mediate access through the blood brain barrier by pumping substates of it out of the CNS and back into the blood. Since buprenorphine isnt affected by Pgp, more can enter the brain and cause the things that make you feel high (pain relief, euphoria, sedation) while the full agonist norbupe gets pumped (effluxed is the correct term) out not being to do anything centrally.

 

[hatrix]

You have the basics down. Induction of CYP enzymes causes an overexpression of them leading to increased formation of the metabolite. This often leads to subtherapeutic results as more of an inactive substance is forming. But if the metabolite is also an active compound, and a more potent one than the parent, you will have an increase in effects.

But bupe is a funny drug. Although buprenorphine is a partial and norbuprenophine possibly a full agonist at MOR, buprenorphine seems to be the compound that results in more significant analgesia. This is because norbuprenorphine is also a substrate for P-glycoprotein (Pgp) and buprenorphine is not. Pgp is a protein that helps mediate access through the blood brain barrier by pumping substates of it out of the CNS and back into the blood. Since buprenorphine isnt affected by Pgp, more can enter the brain and cause the things that make you feel high (pain relief, euphoria, sedation) while the full agonist norbupe gets pumped (effluxed is the correct term) out not being to do anything centrally.

Thank you for the explanation, I didn't think I was too far off! I appreciate it. Figured this might be above some people's heads on OD.

I took 10mg of prednisone along with my bupe last night (prednisone was dosed after) and it was my second day in a row taking bupe in recreational doses. I had much more opiate itch and even a slight nod going. It may have been the prednisone a bit, but it may also just have been a better dose that I plugged.

 

[CfZrx]

I am sitting here on both and can tell you the synerjism is negligible.

 

[mmchase8680]

Wish I could understand that

 

[mmchase8680]

No I mean I wish it was a chemist and head that incredible understanding of how the brain a different chemicals work that’s fascinating