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All 4 posts Subject: Pharmacokinetics of hydrocodone... Please login to post Down

BlaseDeviant
(Hive Bee)
09-27-04 22:39
No 533458
      Pharmacokinetics of hydrocodone...

Hydrocodone metabolizes by CYP2D6-P450 to hydromorphone, correct? Are there any other active metabolites? Any that account for its effect more than hydrocodone itself does? Hydrocodone itself IS active before being metabolized, but is it also the main drug acting here?

Also, is the rate at which it metabolizes to hydromorphone significant enough for the hydromorphone to have an effect... or not? How is hydromorphone metabolized? Is there any way to inhibit hydromorphone's metabolization (I doubt it, but I can hold a glimmer of hope) then?

I read on pubmed that when enzyme deficient folks, and folks who had taken quinine (I think it was?) to inhibit metabolization to hydromorphone, it was still abusable, so obviously I guess hydrocodone is active, or else it has another major metabolite(s).

But my main concern is stopping/slowing the hydromorphone metabolization, which I'm feeling is probably a pipe dream?

Also, do benzos enhance or weaken it? I heard on another forum that gaba modulates dopamine-induced neuron firing, and that one of the proposed theories of opiate euphoria was that opiate receptors when activated, had an (one of many) effect of increasing dopamine, which accounts for PART of the effects.

But everyone who's done it says it's good, and I must say that .5 g Halcion + hydrocodone seemed stronger than the same amount the next day, sans Halcion, unless tolerance formed from one day of recent usage (highly unlikely, right?)? However, some say that it just increases sedation, which some people mistake for a better time. I dunno.

So differently divine...

jsorex
(Hive Addict)
09-28-04 00:05
No 533478
      British Journal of Clinical Pharmacology ...

This artcle here lists the metabolites and the mechanisms.

British Journal of Clinical Pharmacology
Volume 57 Issue 3 Page 287 - March 2004
DOI:10.1046/j.1365-2125.2003.02002.x

CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes

This one talks about the inhibition and quinine

Effect of Cytochrome P450 2D1 Inhibition on Hydrocodone
Metabolism and its Behavioral Consequences in Rats

D. M. TOMKINS, S. V. OTTON, N. JOHARCHI, N-Y. LI, R. F. BALSTER, R. F. TYNDALE and E. M. SELLERS
DOI:0022-3565/97/2803-1374$03.00/0

THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS Vol. 280, No. 3
Copyright © 1997 by The American Society for Pharmacology and Experimental Therapeutics Printed in U.S.A.
JPET 280:1374–1382, 1997

BlaseDeviant
(Hive Bee)
09-29-04 23:49
No 533805
      Thanks. An interesting note, if I'm reading...

Thanks. An interesting note, if I'm reading that correctly, is that only 4.6% of any hydrocodone dose is actually converted into hydromorphone.

So differently divine...

BlaseDeviant
(Hive Bee)
10-02-04 22:45
No 534212
      Speaking of pharmacokinetics, does anyone know

Speaking of pharmacokinetics, does anyone know WHY SSRIS blunt the effects of opiates? Similar to the DXM + morphine/opiates effect (and it's still argued whether it potentiates analegesia but attenuates euphoria, or potentiates both), it's documented, but unexplained, as far as I know.

So differently divine...

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	All 4 posts		Subject: Pharmacokinetics of hydrocodone...		Please login to post		Down


		BlaseDeviant (Hive Bee) 09-27-04 22:39 No 533458				Pharmacokinetics of hydrocodone...
						Hydrocodone metabolizes by CYP2D6-P450 to hydromorphone, correct? Are there any other active metabolites? Any that account for its effect more than hydrocodone itself does? Hydrocodone itself IS active before being metabolized, but is it also the main drug acting here? Also, is the rate at which it metabolizes to hydromorphone significant enough for the hydromorphone to have an effect... or not? How is hydromorphone metabolized? Is there any way to inhibit hydromorphone's metabolization (I doubt it, but I can hold a glimmer of hope) then? I read on pubmed that when enzyme deficient folks, and folks who had taken quinine (I think it was?) to inhibit metabolization to hydromorphone, it was still abusable, so obviously I guess hydrocodone is active, or else it has another major metabolite(s). But my main concern is stopping/slowing the hydromorphone metabolization, which I'm feeling is probably a pipe dream? Also, do benzos enhance or weaken it? I heard on another forum that gaba modulates dopamine-induced neuron firing, and that one of the proposed theories of opiate euphoria was that opiate receptors when activated, had an (one of many) effect of increasing dopamine, which accounts for PART of the effects. But everyone who's done it says it's good, and I must say that .5 g Halcion + hydrocodone seemed stronger than the same amount the next day, sans Halcion, unless tolerance formed from one day of recent usage (highly unlikely, right?)? However, some say that it just increases sedation, which some people mistake for a better time. I dunno. So differently divine...



		jsorex (Hive Addict) 09-28-04 00:05 No 533478				British Journal of Clinical Pharmacology ...
						This artcle here lists the metabolites and the mechanisms. British Journal of Clinical Pharmacology Volume 57 Issue 3 Page 287 - March 2004 DOI:10.1046/j.1365-2125.2003.02002.x CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes This one talks about the inhibition and quinine Effect of Cytochrome P450 2D1 Inhibition on Hydrocodone Metabolism and its Behavioral Consequences in Rats D. M. TOMKINS, S. V. OTTON, N. JOHARCHI, N-Y. LI, R. F. BALSTER, R. F. TYNDALE and E. M. SELLERS DOI:0022-3565/97/2803-1374$03.00/0 THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS Vol. 280, No. 3 Copyright © 1997 by The American Society for Pharmacology and Experimental Therapeutics Printed in U.S.A. JPET 280:1374–1382, 1997



		BlaseDeviant (Hive Bee) 09-29-04 23:49 No 533805				Thanks. An interesting note, if I'm reading...
						Thanks. An interesting note, if I'm reading that correctly, is that only 4.6% of any hydrocodone dose is actually converted into hydromorphone. So differently divine...



		BlaseDeviant (Hive Bee) 10-02-04 22:45 No 534212				Speaking of pharmacokinetics, does anyone know
						Speaking of pharmacokinetics, does anyone know WHY SSRIS blunt the effects of opiates? Similar to the DXM + morphine/opiates effect (and it's still argued whether it potentiates analegesia but attenuates euphoria, or potentiates both), it's documented, but unexplained, as far as I know. So differently divine...

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