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All 15 posts Subject: loperamide question? Please login to post Down

kreo
(Stranger)
07-18-02 03:10
No 333910
      loperamide question?

recently swim had a dream. the dream proceeds as follow: swim aquired 6mg loperamide hcl. swim decided to poor 20ml dilute acetic acid ~5% making it a ~1:1 mole ratio. nothing was happening so swim decided to chunk in an acid (ascorbic acid ~125mg), didnt have any sulfuric acid, just for shits and gigles the solution turned a deep orange color. prior knowledge tells swim that the orange is from the precense of dehydroascorbate, the oxidized form of ascorbic acid. the resulting product had strong opiate like effects in the microgram dose. swim would like to know what the hell happened since swim wasnt expecting much. swim thinks it just formed an acetic ester but swims confused on what the ascorbic acid did. would any bee mind helping swim out with his problem?
im an artist. i look at things from a creative perspective.
peace out

Dr_Heckyll
(Stranger)
07-18-02 03:52
No 333927
      Question

the resulting product had strong opiate like effects in the microgram dose.

How did swim determine that?

Dr. Heckyll & Mr. Jive by Men at Work
...tells my tale.

kreo
(Stranger)
07-18-02 17:45
No 334193
      swim has EXTREMELY limited improvised resources ...

swim has EXTREMELY limited improvised resources and equiptment due to a nosy three lettered freind. as for the bioassay swim just railed a tiny tiny line of the crude product ~.025-.05mg its hard for swim to tell by eye especially seeing that an unknown percentage is crude byproducts. the previous dose had effects similer to ~7.5mg hydrocodone not to mention crazy ass itching. swim is cautious of experimenting further without further knowledge on what sort of "frankendrug" was producted, even swims got limits on how far swim pushes swims body.
im an artist. i look at things from a creative perspective.
peace out

foxy2
(Distinctive Doe)
07-18-02 18:34
No 334205
User Picture       well probably nothing

I have read an article that stated snorting drugs can directly bypass the blood-brain barrier, to a limited extent.

I forget the details.
Those who give up essential liberties for temporary safety deserve neither liberty nor safety

kreo
(Stranger)
07-18-02 20:38
No 334240
      swim says insufflated loperamide is extremely ...

swim says insufflated loperamide is extremely unpleasant, it takes ~6mg to feel threshold effects, it makes swims nose itch like hell and swell up, and its got a lot of toxic side effects, eg. facial swelling, profuse sweating, itching. swims face and hands were breaking out for about a week while swim only felt threshold effects for the first few hours. maybe it was a placebo but the toxic effects were very real. swims freinds thought swim was being attacked by a flesh eating bacteria.
im an artist. i look at things from a creative perspective.
peace out

foxy2
(Distinctive Doe)
07-18-02 21:16
No 334248
User Picture       opiate

Those sound like opiate side effects. Which is typically all you get from loperamide, and thus its otc.

Maybee whatever you insuffelated with it caused the permiability of your membranes to increase.

Or your full of shit.
I'll flip a coin.

Tails, I think your full of shit.

The scientific method at its finest tongue smile
Those who give up essential liberties for temporary safety deserve neither liberty nor safety

carboxyl
(Hive Bee)
07-18-02 21:49
No 334269
User Picture       am i getting this right?

so you took some otc loperamide, tossed it in some vinegar, threw in some vitamin c, and got a compound active at
.025-.05 mg??? Doesn't it sound a little bit far fetched? I think I'm with foxy on this one, but please correct me if i'm wrong
The above post is purely fictional. Any resemblance to "real-life" is purely coincidental.

kreo
(Stranger)
07-18-02 23:01
No 334312
      yeah dude swim thought it was pretty far fetched ...

yeah dude swim thought it was pretty far fetched too. swim cant really rule out that there might have been impurities in the reaction vessel or that swim has abnormal sensitivity to certain chemicals. so swim was hoping someone on the forum might be able to duplicate the result seeing that niether chemistry nor psychoactive substances are swims area of expertise. swim let it react in room temperature for two days.
im an artist. i look at things from a creative perspective.
peace out

kreo
(Stranger)
07-18-02 23:17
No 334320
      swim doesnt think swim made 'swimself' clear but ...

swim doesnt think swim made 'swimself' clear but on the post where swim was describing effects, swim was refering to insufflated loperamide NOT 'frankendrug'. swim wants some feedback on this. maybe a response of a more chemical or biological nature would be a little more helpful.
im an artist. i look at things from a creative perspective.
peace out

Dr_Heckyll
(Stranger)
07-19-02 02:45
No 334395
      Shit or not shit?

foxy2: Tails, I think your full of shit.

Somehow I tend to second foxy2:

as for the bioassay swim just railed a tiny tiny line of the crude product ~.025-.05mg its hard for swim to tell by eye especially seeing that an unknown percentage is crude byproducts.

You cannot see 0.05 mg with your bare eye, much less rail a tiny tiny line from it. You don't have your facts straight.

But assuming that there is some truth to your story, not quantitatively, but qualitatively, what could have happened? The only moiety of loperamide with which the vitamin C could have possible reacted is the diphenylamido. Is there any precedence or possibility that ascorbic acid could reduce an amide to an alpha-hydroxy alkylamine?

Dr. Heckyll & Mr. Jive by Men at Work
...tells my tale.

vetya
(Stranger)
08-18-02 23:57
No 346529
      ascorbic acid and the blood brain barrier

While browsing swim found this article related to this recipe.
http://www.nmafaculty.org/news/ascorbic.htm
Claiming "According to Dr. Manfredini, 'Ascorbic acid works like a sort of shuttle. Theoretically it could transport onto the brain any compound.'"

Real question is how to cleave the ascorbic unto the loperamide.

Also, seem to recall that alcohols in general increase permeability of the BBB and perhaps it's worth trying the ascorbic/loperamide combo in other solvents. Unfortunately swim's background is focused on theoretical neurobio not the chem side.

Would appreciate comments (dried up opioids can be the mother of invention it seems).

Dr_Heckyll
(Hive Bee)
08-20-02 05:17
No 346969
      Looks like they are refering to 11806707 . Hmm.

Looks like they are refering to Medline (PMID=11806707). Hmm. Did kreo somehow attach the ascorbic acid, possibly as ester, to the available hydroxy of loperamide and thereby shuttled it into his CNS? So many questions and no answers...

http://lyricsdomain.com/lyrics/26021/

eugene
(Stranger)
08-26-02 07:52
No 349112
      Getting loperamide across the blood-brain barrier
(Rated as: excellent)

This looks interesting:

Pharm Res 1997 Mar;14(3):325-328 Delivery of loperamide across
the blood-brain barrier with polysorbate 80-coated
polybutylcyanoacrylate nanoparticles.

Alyautdin RN, Petrov VE, Langer K, Berthold A, Kharkevich DA,
Kreuter J

Department of Pharmacology, Sechenov Medical Academy, Moscow,
Russia.

PURPOSE: The possibility of using polysorbate 80-coated
nanoparticles for the delivery of the water insoluble opioid
agonist loperamide across the blood-brain barrier was
investigated. The analgesic effect after i.v. injection of the
preparations was used to indicate drug transport through this
barrier. METHODS: Loperamide was incorporated into PBCA
nanoparticles. Drug-containing nanoparticles were coated with
polysorbate 80 and injected intravenously into mice. Analgesia
was then measured by the tail-flick test. RESULTS: Intravenous
injection of the particulate formulation resulted in a long and
significant analgesic effect. A polysorbate 80 loperamide
solution induced a much less pronounced and very short analgesia.
Uncoated nanoparticles loaded with loperamide were unable to
produce analgesia. CONCLUSIONS: Polysorbate 80-coated PBCA
nanoparticles loaded with loperamide enabled the transport of
loperamide to the brain.

PMID: 9098875, UI: 97253432

----------

Life Sci 1983;33 Suppl 1:315-318 Loperamide: evidence of
interaction with mu and delta opioid receptors.

Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M,
Gori E

Loperamide was tested on electrically-evoked contractions using a
series of "in vitro" isolated preparations, in comparison with
morphine, met-enkephalin, beta-endorphin, ethylketocyclazocine
used as representative agonists of mu, delta, epsilon, kappa
receptors respectively. The IC50 of loperamide on myenteric
plexus longitudinal muscle of guinea pig ileum was found to be
1.90 X 10(-7)M and equal to that of morphine. The IC50 on mouse
vas deferens was found to be 13.02 X 10(-7)M. In this tissue,
loperamide resulted as active as morphine, but 54 times less
active than met-enkephalin (IC50 0.24 X 10(-7)M). On the rat vas
deferens where, as expected, beta-endorphin was strongly active
(IC50 1.38 X 10(-7)M), morphine exerted a stimulatory action
within the range 10(-5)M-10(-4)M and loperamide was only poorly
depressive. The Ke value of naloxone, a specific mu receptor
antagonist, against loperamide in the guinea pig ileum was 3.83
nM, and in the mouse vas deferens was 82.87 nM indicating that
loperamide in the guinea pig ileum acts on mu receptors while in
the mouse vas deferens on another opiate receptor.

PMID: 6319884, UI: 84116593

morpheus
(Hive Bee)
08-29-02 09:50
No 350368
      Not shit

Swim remembers reading somewhere(maybee PDR for otc drugs)
that loperamide given to opiate addicted rhesus monkeys
stopped or eased their withdrawl.Since monkeys can't
talk, don't ask me how they arrived at this conclusion.
Apparently besides helping your lower GI tract and constipating you,in large enough doses it has some opiate qualities.Unfortunatly in large doses you may end up with
an impacted bowel or colon.

ambientia
(Stranger)
09-24-02 13:17
No 359944
      p-glycoprotein and loperamide

What are P-glycoproteins?
http://www.mhc.com/PGP/PgpMain.HTML

Increased drug delivery to the brain by P-glycoprotein inhibition.
http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11014404&dopt=Abstract

Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein.
http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11964599&dopt=Abstract

Ritonavir increases loperamide plasma concentrations without evidence for P-glycoprotein involvement.
http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11719726&dopt=Abstract

Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4.
http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11741214&dopt=Abstract

Modulation of P450 CYP3A4-dependent metabolism by P-glycoprotein: implications for P450 phenotyping.
http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11160617&dopt=Abstract

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	All 15 posts		Subject: loperamide question?		Please login to post		Down


		kreo (Stranger) 07-18-02 03:10 No 333910				loperamide question?
						recently swim had a dream. the dream proceeds as follow: swim aquired 6mg loperamide hcl. swim decided to poor 20ml dilute acetic acid ~5% making it a ~1:1 mole ratio. nothing was happening so swim decided to chunk in an acid (ascorbic acid ~125mg), didnt have any sulfuric acid, just for shits and gigles the solution turned a deep orange color. prior knowledge tells swim that the orange is from the precense of dehydroascorbate, the oxidized form of ascorbic acid. the resulting product had strong opiate like effects in the microgram dose. swim would like to know what the hell happened since swim wasnt expecting much. swim thinks it just formed an acetic ester but swims confused on what the ascorbic acid did. would any bee mind helping swim out with his problem? im an artist. i look at things from a creative perspective. peace out



		Dr_Heckyll (Stranger) 07-18-02 03:52 No 333927				Question
						the resulting product had strong opiate like effects in the microgram dose. How did swim determine that? Dr. Heckyll & Mr. Jive by Men at Work ...tells my tale.



		kreo (Stranger) 07-18-02 17:45 No 334193				swim has EXTREMELY limited improvised resources ...
						swim has EXTREMELY limited improvised resources and equiptment due to a nosy three lettered freind. as for the bioassay swim just railed a tiny tiny line of the crude product ~.025-.05mg its hard for swim to tell by eye especially seeing that an unknown percentage is crude byproducts. the previous dose had effects similer to ~7.5mg hydrocodone not to mention crazy ass itching. swim is cautious of experimenting further without further knowledge on what sort of "frankendrug" was producted, even swims got limits on how far swim pushes swims body. im an artist. i look at things from a creative perspective. peace out



		foxy2 (Distinctive Doe) 07-18-02 18:34 No 334205				well probably nothing
						I have read an article that stated snorting drugs can directly bypass the blood-brain barrier, to a limited extent. I forget the details. Those who give up essential liberties for temporary safety deserve neither liberty nor safety



		kreo (Stranger) 07-18-02 20:38 No 334240				swim says insufflated loperamide is extremely ...
						swim says insufflated loperamide is extremely unpleasant, it takes ~6mg to feel threshold effects, it makes swims nose itch like hell and swell up, and its got a lot of toxic side effects, eg. facial swelling, profuse sweating, itching. swims face and hands were breaking out for about a week while swim only felt threshold effects for the first few hours. maybe it was a placebo but the toxic effects were very real. swims freinds thought swim was being attacked by a flesh eating bacteria. im an artist. i look at things from a creative perspective. peace out



		foxy2 (Distinctive Doe) 07-18-02 21:16 No 334248				opiate
						Those sound like opiate side effects. Which is typically all you get from loperamide, and thus its otc. Maybee whatever you insuffelated with it caused the permiability of your membranes to increase. Or your full of shit. I'll flip a coin. Tails, I think your full of shit. The scientific method at its finest Those who give up essential liberties for temporary safety deserve neither liberty nor safety



		carboxyl (Hive Bee) 07-18-02 21:49 No 334269				am i getting this right?
						so you took some otc loperamide, tossed it in some vinegar, threw in some vitamin c, and got a compound active at .025-.05 mg??? Doesn't it sound a little bit far fetched? I think I'm with foxy on this one, but please correct me if i'm wrong The above post is purely fictional. Any resemblance to "real-life" is purely coincidental.



		kreo (Stranger) 07-18-02 23:01 No 334312				yeah dude swim thought it was pretty far fetched ...
						yeah dude swim thought it was pretty far fetched too. swim cant really rule out that there might have been impurities in the reaction vessel or that swim has abnormal sensitivity to certain chemicals. so swim was hoping someone on the forum might be able to duplicate the result seeing that niether chemistry nor psychoactive substances are swims area of expertise. swim let it react in room temperature for two days. im an artist. i look at things from a creative perspective. peace out



		kreo (Stranger) 07-18-02 23:17 No 334320				swim doesnt think swim made 'swimself' clear but ...
						swim doesnt think swim made 'swimself' clear but on the post where swim was describing effects, swim was refering to insufflated loperamide NOT 'frankendrug'. swim wants some feedback on this. maybe a response of a more chemical or biological nature would be a little more helpful. im an artist. i look at things from a creative perspective. peace out



		Dr_Heckyll (Stranger) 07-19-02 02:45 No 334395				Shit or not shit?
						foxy2: Tails, I think your full of shit. Somehow I tend to second foxy2: as for the bioassay swim just railed a tiny tiny line of the crude product ~.025-.05mg its hard for swim to tell by eye especially seeing that an unknown percentage is crude byproducts. You cannot see 0.05 mg with your bare eye, much less rail a tiny tiny line from it. You don't have your facts straight. But assuming that there is some truth to your story, not quantitatively, but qualitatively, what could have happened? The only moiety of loperamide with which the vitamin C could have possible reacted is the diphenylamido. Is there any precedence or possibility that ascorbic acid could reduce an amide to an alpha-hydroxy alkylamine? Dr. Heckyll & Mr. Jive by Men at Work ...tells my tale.



		vetya (Stranger) 08-18-02 23:57 No 346529				ascorbic acid and the blood brain barrier
						While browsing swim found this article related to this recipe. http://www.nmafaculty.org/news/ascorbic.htm Claiming "According to Dr. Manfredini, 'Ascorbic acid works like a sort of shuttle. Theoretically it could transport onto the brain any compound.'" Real question is how to cleave the ascorbic unto the loperamide. Also, seem to recall that alcohols in general increase permeability of the BBB and perhaps it's worth trying the ascorbic/loperamide combo in other solvents. Unfortunately swim's background is focused on theoretical neurobio not the chem side. Would appreciate comments (dried up opioids can be the mother of invention it seems).



		Dr_Heckyll (Hive Bee) 08-20-02 05:17 No 346969				Looks like they are refering to 11806707 . Hmm.
						Looks like they are refering to Medline (PMID=11806707). Hmm. Did kreo somehow attach the ascorbic acid, possibly as ester, to the available hydroxy of loperamide and thereby shuttled it into his CNS? So many questions and no answers... http://lyricsdomain.com/lyrics/26021/



		eugene (Stranger) 08-26-02 07:52 No 349112				Getting loperamide across the blood-brain barrier (Rated as: excellent)
						This looks interesting: Pharm Res 1997 Mar;14(3):325-328 Delivery of loperamide across the blood-brain barrier with polysorbate 80-coated polybutylcyanoacrylate nanoparticles. Alyautdin RN, Petrov VE, Langer K, Berthold A, Kharkevich DA, Kreuter J Department of Pharmacology, Sechenov Medical Academy, Moscow, Russia. PURPOSE: The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid agonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used to indicate drug transport through this barrier. METHODS: Loperamide was incorporated into PBCA nanoparticles. Drug-containing nanoparticles were coated with polysorbate 80 and injected intravenously into mice. Analgesia was then measured by the tail-flick test. RESULTS: Intravenous injection of the particulate formulation resulted in a long and significant analgesic effect. A polysorbate 80 loperamide solution induced a much less pronounced and very short analgesia. Uncoated nanoparticles loaded with loperamide were unable to produce analgesia. CONCLUSIONS: Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain. PMID: 9098875, UI: 97253432 ---------- Life Sci 1983;33 Suppl 1:315-318 Loperamide: evidence of interaction with mu and delta opioid receptors. Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E Loperamide was tested on electrically-evoked contractions using a series of "in vitro" isolated preparations, in comparison with morphine, met-enkephalin, beta-endorphin, ethylketocyclazocine used as representative agonists of mu, delta, epsilon, kappa receptors respectively. The IC50 of loperamide on myenteric plexus longitudinal muscle of guinea pig ileum was found to be 1.90 X 10(-7)M and equal to that of morphine. The IC50 on mouse vas deferens was found to be 13.02 X 10(-7)M. In this tissue, loperamide resulted as active as morphine, but 54 times less active than met-enkephalin (IC50 0.24 X 10(-7)M). On the rat vas deferens where, as expected, beta-endorphin was strongly active (IC50 1.38 X 10(-7)M), morphine exerted a stimulatory action within the range 10(-5)M-10(-4)M and loperamide was only poorly depressive. The Ke value of naloxone, a specific mu receptor antagonist, against loperamide in the guinea pig ileum was 3.83 nM, and in the mouse vas deferens was 82.87 nM indicating that loperamide in the guinea pig ileum acts on mu receptors while in the mouse vas deferens on another opiate receptor. PMID: 6319884, UI: 84116593



		morpheus (Hive Bee) 08-29-02 09:50 No 350368				Not shit
						Swim remembers reading somewhere(maybee PDR for otc drugs) that loperamide given to opiate addicted rhesus monkeys stopped or eased their withdrawl.Since monkeys can't talk, don't ask me how they arrived at this conclusion. Apparently besides helping your lower GI tract and constipating you,in large enough doses it has some opiate qualities.Unfortunatly in large doses you may end up with an impacted bowel or colon.



		ambientia (Stranger) 09-24-02 13:17 No 359944				p-glycoprotein and loperamide
						What are P-glycoproteins? http://www.mhc.com/PGP/PgpMain.HTML Increased drug delivery to the brain by P-glycoprotein inhibition. http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11014404&dopt=Abstract Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11964599&dopt=Abstract Ritonavir increases loperamide plasma concentrations without evidence for P-glycoprotein involvement. http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11719726&dopt=Abstract Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4. http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11741214&dopt=Abstract Modulation of P450 CYP3A4-dependent metabolism by P-glycoprotein: implications for P450 phenotyping. http://www.ncbi.nlm.nih.gov%3A80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11160617&dopt=Abstract

All 15 posts	End of thread	Top