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Injecting VERY small dose of Codeine

^ I wouldn't inject Opium gum/latex if I were you, there are many, many alkaloids, not to mention some plant matter that would not be very welcoming to your veins. The overall consensus on injecting even small amounts of plant matter, is that it shouldn't be done.
 
thus the micron filter (0.2um...)
This is purely academic anyway, but if I were to do this I would:

boil down opium, filter (down to 0.2um,) add activated charcoal & stir for a while (anybody got any suggestions on this step? would activated charcoal absorb the morphine or just the tar crap? how long would it take?) then centrifuge to get the charcoal into a pellet.
Now adjust pH to 11, using NaOH. A brown precipitate should form and then redissolve again. Add chloroform & invert repeatedly, gently. Use a syringe to take off chloroform layer & discard, repeat twice or thrice. Adjust pH to 8.5 (and this is the step I'm unsure of - its ripped from homebaking methods) - rub glass rod vigorously on side of beaker to induce precipitation of morphine base. Filter. Wash. Dissolve in HCl, add bicarb until it stops fizzing. Inject.

Ok here's an edit:
a.) "The resulting residue, which contains the alkaloids, is mixed or extracted with an basic aqueous solution having a pH of at least 11, preferably an aqueous solution of an alkali hydroxide. This converts the morphine free base present into its anionic (morphinate) form which is soluble in basic solutions of pH values of 11 or above. Other opium alkaloids are relatively insoluble and, in general, at least partially precipitate out of the basic aqueous solution. After removing any precipitate, preferably by filtration, the remaining alkaloids are separated from the morphine containing basic aqueous solution by extraction with a substantially water-immiscible solvent, such as toluene or benzene [or chloroform]. Finally, the morphine free base is precipitated out of the resulting aqueous solution by adjusting the pH of the aqueous filtrate to pH 8.5 to 9.5. Preferably, the pH to precipitate the morphine ranges from about 9 to 9.3, and most preferably is about 9.1" from http://designer-drugs.com/pte/12.162.180.114/dcd/chemistry/morphextr.html
 
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IM use and histaminergics

The old pictures of codeine injection were not labled for IV use because the rush of histamine can cause serious problems, the codeine itself causes histamine release. If you could prevent the histamine effects you still have other problems, none of which can be prevented by antihistamines. I included some other info that may help in other situations as well. I wouldnt try IV codeine, its been shown to cause seizures in some cases.

You would have to get the right antihistamine as well, there are more than one histamine receptor subtype, theres H1, H2, H3 that i know of. There are both H1 and H2 receptor ligands on the market over the counter.

Diphenhydramine is an H1 antagonist, as is promethazine, chlorpromazine and some others you wouldnt find anywhere. as an aside, cetirizine and loratadine happen to be non CNS active, so that may be of use.

Cimetidine is an H2 antagonist, as is ranitidine, there are tons of those piperidine H2 drugs available.

As for H3 you wont find any that i know of, they are usually modifications of histamine itself and used in research.

TheTripDoctor,
Recreational Pharmacist

AIM: Mrsteveman1
 
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mattwestm said:
I injected a small, very small dose of codeine before and had no problems. It actually didn't do that much except make me very tired.

How much did you inject?

That's very interesting, I would love to hear other reports of people injecting very small doses of Codeine.
 
mrsteveman1 said:
The old pictures of codeine injection were not labled for IV use because the rush of histamine can cause serious problems, the codeine itself causes histamine release. If you could prevent the histamine effects you still have other problems, none of which can be prevented by antihistamines. I included some other info that may help in other situations as well. I wouldnt try IV codeine, its been shown to cause seizures in some cases.

You would have to get the right antihistamine as well, there are more than one histamine receptor subtype, theres H1, H2, H3 that i know of. There are both H1 and H2 receptor ligands on the market over the counter.

Diphenhydramine is an H1 antagonist, as is promethazine, chlorpromazine and some others you wouldnt find anywhere. as an aside, cetirizine and loratadine happen to be non CNS active, so that may be of use.

Cimetidine is an H2 antagonist, as is ranitidine, there are tons of those piperidine H2 drugs available.

As for H3 you wont find any that i know of, they are usually modifications of histamine itself and used in research.

TheTripDoctor,
Recreational Pharmacist

AIM: Mrsteveman1

Most commonly available OTC "antihistamines" will be H1 inhibitors, and therefore will inhibit histamine mediated inflammatory reactions (to some extent.) H2 antagonists (omeprazole?) are used to counter gastric reflux as H2 is involved in stomach acid secretion. I doubt you'd find that in the anti-allergenics section of the pharmacy - its probably prescription only. If it were OTC the pharmacist would definitely check with you that you were going to be using it for acid reflux / stomach problems.
 
what might be interesting is to do a standard allergy test with a solution of codeine. Make a prick (that draws a little bit of blood) on the underside of your forearm just above your wrist and place a little codeine solution (preferably made my dissolving a codeine tab in water, but I suppose a cold water extraction would work: you'd have to do another one with paracetamol/acetaminophen as a control.) Leave it there for 15 minutes (try not to move it) and see if a welt forms. The size of the welt would be proportional to the extent of the allergic response.

Alternatively, injecting a few miligrams of codeine wouldn't be likely to set off a large reaction - anaphylatic shock or seizures or what have you. So inject maybe 5mg, then try 15mg, then 30mg, then 100mg, with an hour or so between injections. I suppose everyone's bodies have different reactions. I've talked to someone who almost had to have his leg amputated due to repeated intramuscular injections of codeine, and I've also talked to people who have intravenously injected hundreds of miligrams regularly and found it quite enjoyable. Alt.drugs.hard might have something to say about this...

here's what I found:
"I have witnessed an aquaintance hit up codeine twice now. Not a pretty
sight, he went from caucasian to bright red all over in 10 seconds, his face
all puffed up. It went away after 20 minutes or so (the histamine reaction)
and he said it's not so bad if you can ride out those 20 minutes without
ripping your face off. Fuck that, you can die from that shit. He did it at
my house once without telling me what he was hitting up. I gave him the
biggest bollocksing afterwards and told him if he does that at my place
again *I'll* kill him. I don't want to have to be explaining corpses in my
lounge. " -misfit
 
Allergy

I listed the drugs i did because they were obtainable, H2 antagonists are common, even the prescription ones. Cimetidine, Famotidine, Ranitidine. Cimetdine is an over the counter drug all over the US. Its common.

They are all antihistamines, regardless of their use in a pharmacy, or what counter theyre behind or what section their in.

Definition: Cimetidine is a Histamine H2 antagonist, Antihistamine


My post was a furtherance of the idea of blocking the histamine response. Weather that histamine response is because of activity at H1, H2, or H3, i didnt say and dont know off hand. Probably H1 but you never know.


Much of the allergic reaction effect caused by histamine is peripheral, as in anything with antihistamine action that can enter the body would have a chance at affecting those symptoms. If its a CNS effect then the drug has to be able to get past the BBB first.


BY THE WAY, other than for PURE curiosity like jasoncrest intended in his post, this use of codeine has more risks than trying to beat a train to the station by running in front of it.
 
^ Man I don't understand what that post is trying to say.

No doctor, or pharmacist, when you ask for an antihistamine, is going to give you cimetidine.

If you're having histaminergic side effects from opioids, you need H1 antagonsits, not H2 (or H3 or H4) antagonists.
 
BilZ0r said:
If you're having histaminergic side effects from opioids, you need H1 antagonsits, not H2 (or H3 or H4) antagonists.

So an H1 antihistamine like Promethazine can stop the histamine release caused by a Codeine injection (a very small dose)?
 
Very simple

That post was very simple, first i never said to ask a pharmacist. I wouldnt, and i doubt anyone here would either, hence they are here.

I also responded to someone saying H2s were not OTC, cimetidine is OTC, i dont care what its used for or if it works in this case. Its an H2 and its OTC, period. Just listing them for others.......

I defined antihistamines, despite what they are USED for.

"They are all antihistamines, regardless of their use in a pharmacy, or what counter theyre behind or what section their in.

Definition: Cimetidine is a Histamine H2 antagonist, Antihistamine"

Second i furthered the idea of blocking the histamine response in the body, and theorized that it might not be CNS effects that cause the reactions, rather peripheral histamine action on any of the Histamine receptor types.

"My post was a furtherance of the idea of blocking the histamine response. Weather that histamine response is because of activity at H1, H2, or H3, i didnt say and dont know off hand. Probably H1 but you never know."

If true, then who knows what will or wont help which symptoms. As before, I didnt say and i dont know off hand.
 
So an H1 antihistamine like Promethazine can stop the histamine release caused by a Codeine injection (a very small dose)?
Yeah, promethazine or diphenhydramine... they wont stop the histamine release, but they'll stop it's most dangerous effects.
 
By the way....

by the way, i didnt have a reference for this at the time, but since i was chewed out for suggesting H2 antagonists, perhaps i should post some references now.....



"Antihistamines may be helpful in relieving itch when associated with histamine release. Morphine causes non-immune mediated histamine release from mast cells. Although there is little data, many report advantages of combining H1 and H2 receptor subtype antihistamines. These may have central effects as well as peripheral antihistaminic effects."

http://www.eperc.mcw.edu/fastFact/ff_37.htm
 
Turns out you weren't as wrong as I though

Clin Pharm. 1984 Jan-Feb;3(1):60-4. Related Articles, Links

Effect of H1- and H2-receptor blockade on the inhibition of immediate cutaneous reactions.

Johnson CE, Weiner JS, Wagner DS, McLean JA.

The effects of cyproheptadine, cimetidine, and their combination on the wheal-and-flare skin-test response was evaluated using an intradermal skin-test technique in a double-blind, placebo-controlled study. Sixteen volunteers with known positive skin-test reactions to at least two antigens were divided into four treatment groups in a four-way crossover design. The patients received baseline intradermal skin tests on the back consisting of dilutions of mixed grasses and weeds, histamine diphosphate and codeine phosphate, and buffered-saline control. Following the baseline testing, the patients received cyproheptadine (4 mg q.i.d.), cimetidine (300 mg q.i.d.), the combination, and placebo in a double-blind trial. Of the 16 patients, 12 completed all treatment courses. Following pretreatment with cyproheptadine, cimetidine, and the combination, areas of wheal-and-flare response for each test substance were significantly suppressed. Although it appeared that the combination augmented wheal-and-flare suppression, the observed difference, compared with the cyproheptadine pretreatment sequence, was not statistically significant. The administration of H1 and H2 antagonists should be discontinued before the diagnostic use of immediate skin tests.

Anesthesiology. 1981 Sep;55(3):292-6. Related Articles, Links

The use of H1 and H2 histamine antagonists with morphine anesthesia: a double-blind study.

Philbin DM, Moss J, Akins CW, Rosow CE, Kono K, Schneider RC, VerLee TR, Savarese JJ.

High doses of morphine can produce significant cardiovascular effects generally attributed to histamine release. The authors examined the possibility that H1 and H2 histamine antagonists might prove beneficial in preventing these responses. In a randomized double-blind study, four groups of 10 patients each received 1 mg/kg morphine and either a placebo, diphenhydramine (H1), cimetidine (H2), or both of the histamine antagonists. The morphine-placebo group demonstrated a marked elevation in plasma histamine levels (880 +/- 163 to 7437 +/- 2684 pg/ml), a decrease in systemic vascular resistance (SVR) (15.5 to 9.0 l torr/(l . min-1) and diastolic BP (71 +/- 3 to 45 +/- 4 torr) and an increase in cardiac index (CI) (2.4 +/- 0.2 to 3.0 +/- 0.21 . min-1 . m-2). The administration of either cimetidine or diphenhydramine with morphine provided minimal protection. Those patients who received morphine and both antagonists demonstrated significant attenuation of these responses (CI 2.5 +/- 0.2 to 2.5 +/- 0.1 l . min-1 . m-2; SVR 17.4 to 14.6 torr/(l . min-1) although plasma histamine levels showed a comparable increase (1059 +/- 222 to 7653 +/- 4242 pg/ml). These data demonstrate directly that many of the hemodynamic effects of morphine can be attributed to histamine release. They further demonstrate that significant hemodynamic protection can be obtained by the use of histamine antagonists and the combination of H1 and H2 antagonists is superior to either given alone.
 
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