Codeine FAQ
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From: [email protected] (Jakub Buzdygan)
Newsgroups: alt.drugs,alt.drugs.hard
Subject: codeine FAQ (updated)
Date: Sun, 28 Apr 1996 01:37:45 GMT
Title : Codeine FAQ
Author : [email protected]
Update: Aurelius (Stuff in [] is mine.)
Newsgroup : alt.drugs
Last Revision : April 27, 1996
Introduction:
Codeine is a member of the drug class opiates. Opiates include all
naturally occurring drugs with morphine-like effects such as
codeine and all semi and fully synthetic drugs with morphine-like
effects such as heroin and meperidine (Demerol).
Codeine was first discovered as a natural constituent of opium in
very small concentrations, in the range of 0.7% - 2.5% by weight.
Most codeine found in pharmaceutical products today is
synthetically produced via the methylation of morphine.
Codeine is available by prescription only in most areas of the US.
Exceptions are seen in some states where codeine can be purchased
over-the-counter (OTC) in products containing a small dose of
codeine. Also in Canada, some codeine containing products are
available OTC in most if not all provinces. With the codeine
available in the US OTC, release forms may have to be signed,
including your name and address, in order to keep track of how
much codeine you are buying.
[In Canada you will have no difficulty buying codeine. Not only
are there no forms to sign, but no questions are usually asked. In
the US some paternalistic pharmacists will not sell if they don't
like your looks.]
The amount of codeine allowable by law in OTC products is 8mg per
unit dose of a drug. A example is 325mg of acetaminophen (a unit
dose of acetaminophen) and 8mg codeine per tablet. This law is
used to prevent the excessive use of codeine as one would have to
take doses reaching toxicity of acetaminophen before any real
problems with the codeine administration would occur. It's the
same situation with aspirin. With OTC cough medications, the
highest amount of codeine allowed is 3.3mg/ml. This concentration
is _so_ low that this FAQ will not be discussing cough syrups as a
source of recreational codeine. The tablet form of OTC codeine
products usually also includes 15mg of caffeine in each standard
dose.
[In Canada the law dictates that all codeine OTC products must
contain at least two other active ingredients. This usually
translates into caffeine and acetominophen/APAP.]
Prescription codeine containing products are usually not available
without another drug included such as acetaminophen. Rx
(prescription) products include the Tylenol w/ codeine series
(#1,2,3,4) containing respectively 8mg, 15mg, 30mg, 60mg of
codeine. Each tablet also contains caffeine in doses of 15mg,
30mg, 30mg and 0mg respectively. Thus Tylenol #4 w/ codeine (the
most desired one) contains 325mg of acetaminophen, 60mg of codeine
and no caffeine. Another Rx product is the 222, 292, 293, 294
series. They are identical to the Tylenol w/ codeine series,
except aspirin replaces the acetaminophen. The Rx products are
good sources of codeine for recreational use except most of us
don't have sources that can obtain these drugs, therefore this FAQ
contains a procedure so that one can easily obtain large amount of
codeine from OTC products.
Effects And Uses
Codeine is mainly used as a pain reliever, but is also used for
the relief of a non-productive cough, and as a anti-diarrheal
agent. 120mg of codeine administered SC (subcutaneously, injected
under the skin) provides pain relief equal to 10mg of morphine
administered by the same route. Doses used to relieve cough or
diarrhea range from 5mg to 30mg.
Codeine is absorbed quickly from the GI tract and it's first pass
through the liver results in very little loss of the drug. This
contrasts with morphine in which over 90% of the drug is
metabolized in the first pass through the liver resulting in a
considerable loss of potency when administered orally. This is why
codeine is a common opiate in the relief of pain, the ease of oral
administration.
Codeine can be administered by many routes, this includes, SC, IM
(intramuscularly), as an enema, and orally. Note, codeine can't be
administered safely by IV (intravenously) injection as it can
result in pulmonary edema (fluid in lungs), facial swelling and
other life threatening complications.
Codeine is converted to morphine in the brain. This of course will
result in a positive result in a drug test for the opiates. It is
not known whether or not the drugs heroin, morphine or codeine can
be separately determined on a drug test. In other words it isn't
likely that the drug tester can determine which of the three above
drugs you have taken, he just knows you've taken one or more of
them.
Note! Addiction to codeine can occur. Tolerance is also seen with
chronic use. Although the withdrawal is minimal with codeine, it
is not a fun time. Please be cautious in your use of the drug.
Some common side effects from codeine include drowsiness,
light-headedness, dry mouth, urinary retention (difficulty in
urination), constipation and of course, euphoria. Adverse effects
can include itchiness (common), confusion, nausea and vomiting.
The nausea experienced with codeine is less common and less
intense than that experienced with the stronger opiates such as
morphine. A tip to all those using opiates, lying down does
wonders to the nausea. If you ever experience nausea on opiates it
is different than the commonly experienced nausea as it is more of
a light-headed nausea. Lying down will almost always relieve the
nausea in a couple minutes, which after you can attempt to stand
up again.
Codeine is a _excellent_ opiate to start experimenting with.
Although the euphoria is not as intense as that experienced with
the stronger opiates, the euphoria can still be quite intense. It
also must be noted that like most other drugs, some experience is
required before the full effects can be noticed and enjoyed. The
best dose to start at is the 30mg - 60mg dosage. That way you
won't experience many adverse effects and you can continue to take
this small amount until you feel the desired effects, after that
you can increase the dosage as you please. Most people settle
around the 250mg mark for the best euphoria, with the least side
effects. The best idea is to take in a situation where you won't
become distracted. You can get yourself into a comfortable
position and relax because you will become _quite_ relaxed. It may
take 5 to 20 times before you can appreciate the effects. The
effects are subtle like marijuana and it takes some time before
you come to recognize them all.
The LD50 (lethal dose for %50) is 800mg in the average person.
Death from codeine, unlike most opiates, includes restlessness,
seizures and eventually death from respiratory arrest.
[Some sources indicate that the lower-end LD50 may be around
500mg, so doses above 450mg are in the red zone.]
Using Codeine
Again a good dose to start using codeine at is in the 30mg to 60mg
range. At this dosage range the adverse effects tend to be
minimal, and the pleasurable effects quite noticeable.
[I have never noticed any euphoria below 100mg, so don't give up
just because two 3s don't give you a high. *However, some
unfortunate individuals are allergic to codeine, and, if you have
never used it before, first try a dose of around 30-60mg and see
what will happen. It is dangerous to start off in the high dose
range.*]
It is usually a good idea to take the drug on an empty stomach,
and if nausea is experienced or you get hungry (not likely) you
can have something to eat. On an empty stomach the effects will
become noticeable within 15 min depending on the dose. With higher
doses the effects can begin in as little as 7 min. The effects
peak at around 1 hr with the experience nearing it's end at around
the 3 - 4 hr point. Again with higher doses effects may last 4 - 6
hours.
The effects will usually begin with a slight sedation, and a
feeling of warmth coming over you body. Muscular relaxation is
also quite noticeable. The subjective effects are quite hard to
describe beyond the word euphoria. The sedation associated with
codeine is quite a lot less than that experienced with morphine or
other stronger opiates. A strong feeling of contentment is usually
also experienced. Most people enter a phase where you become quite
content and tend to lose interest in their surroundings. A heavy
feeling in the limbs also becomes quite noticeable. This will peak
at 1hr with the effects slowly tapering off after 2hr.
Codeine Extraction Technique
Due to the difficulty in obtaining Rx drugs containing enough
codeine to be used recreationally, I have included a procedure
that allows one to extract the codeine from OTC products to obtain
enough of the drug to use recreationally.
This extraction can *only* be used on OTC products containing
either acetaminophen or aspirin in addition to the codeine. There
is one exception to this rule. Products containing caffeine can be
used with the knowledge that the most of the caffeine contained in
the OTC product, *will* be found in the finished product. This
should not matter to most people, but to those with problems in
taking caffeine, *you have been warned*!
[I have found that it is better to use products containing asprin,
as opposed to tylenol, because the filtering process goes more
smoothly and, if one is not allergic to salicilates, aspirin is
safer (easier on the liver, etc). Given its solubility, you will
also end up with far less aspirin than acetominophen per volume of
the product.]
The idea behind the following extraction is that acetaminophen and
aspirin (I'll use A/A from now on) are very _insoluble_ in cold
water. Codeine phosphate (the most common salt of codeine) is very
_soluble_ in water including cold water. The following table
explains:
|Codeine Type| Solubility (31C water)|Solubility (21C water)|
Aspirin 1g / 100 ml 1g / 300ml
Acetaminophen 1g / 70 ml 1g / 150 ml
Codeine 1g / 2.3 ml 1g / 0.7 ml
Phosphate ?g / ? ml ?g / ? ml
So as you can see, both A/A aren't very soluble in 21C water, so
if you cool the water to around 10C, the solubility will drop even
further. That way you can dissolve 20 tablets in 50ml of hot
water, cool the water down to 10C, filter the solution and end up
with the same amount of codeine as the tablets contained but only
a fraction of the original amount of A/A.
It must be noted that because most of the caffeine will also be in
the finished product, using large amount of tablets in the
following procedure will result in large amount of caffeine in the
finished product. For example the use of 20 tablets will result in
about 300mg of caffeine in the finished product (15mg/tablets * 20
tablets). I personally haven't experienced any adverse reactions
due to this amount of caffeine. Because of codeine's sedative
effects the "jitters" and other adverse effects of large amount of
caffeine are not experienced.
The Procedure
1. Obtain a quantity of tablets containing codeine, check to see
if they contain anything other than codeine, caffeine,
acetaminophen or aspirin. If they do, and you don't know whether
or not it will be a problem, your best bet is not to use them.
Measure out your desired amount of codeine (ex. 64 mg = 8 tablets
* 8mg/tablet). You may want to add 2 extra tablets as it is quite
likely you will lose some codeine in the procedure. As you get
more experience with the procedure you will be able to get approx.
95% of the codeine extracted.
2. Measure out some nice hot water, use approx. 40ml / 20 tablets
or more if needed. I would suggest you don't go over 50ml for 20
tablets. I don't know if the use of boiling water would destroy
any of the codeine but your best bet is not to use it. Use hot
water but not boiling. Make sure the tablets dissolve completely.
Some dissolve on contact with water while others need some help
dissolving by crushing them. Note : not all of the tablet will
dissolve, there are water-insoluble fillers in the tablet and not
all of the A/A will dissolve either(which is what we want).
[Most sources recommend that codeine not be stored at temperatures
in excess of 40C (104F), so its probably better to use warm, but
not hot, water. I find that it is best to crash the tablets
completely in a container, and then dissolve them in a glass with
water.]
3. Place the solution in a cold bath, I just use some ice cubes in
a container of water. Stir the mixture occasionally until the
solution drops to about 15C or lower. You won't need a thermometer
to measure the temperature, just make sure it's "cold". This will
take about 30 min. If you wish to speed this up, you can use less
water to dissolve the tablets, and add ice chips to cool the
mixture faster. Just make sure you don't add so much ice that you
drastically increase the volume of the mixture.
4. Filter the solution using whatever you have. Coffee filters
work well, but lab filters work the best. Just make sure you don't
end up with obvious solids in the filtered solution. This will
take about 1 hr. You may also want to rinse the solids left over
in the filter with some ice-water to extract any remaining
codeine.
[With aspirin this will take only about 20-30 minutes.]
5. Drink and enjoy! The solution will be _very_ bitter, so I mix a
little Kool-aid powder into the solution. The taste isn't really
bad but it's similar to sucking on a lemon.
[One gets used to the taste after a while.:)]
6. Sit back and wait for the effects. Because the codeine is
already in solution it only needs to be absorbed, while codeine in
the tablet form must dissolve before being absorbed. Because of
this, the effects will probably become noticeable within 15min.
Note : I don't suggest you evaporate the mixture unless you are
willing to wait a while. The Merck index warns that codeine is
sensitive to heat and light. For that reason if you wish to
evaporate the mixture, do it without heat, and shield the solution
from light.
Pharmacology and Drug Interactions
In order to take full advantage of codeine, it is helpful to be
familiar with some relevant pharmacology:
*CYP2D6
The body converts codeine into morphine (~10%) by using the so
called P450 cytochrome pathway, especially cytochrome 2d6
(cyp2d6). Unfortunately, cyp2d6 is missing in about 7% of the
white population, and its manifestation is quite variable in the
rest. Individuals who inherited a cyp2d6 deficiency will get many
of the adverse effects associated with codeine but little
euphoria. If codeine just doesn't work for you, this may be why.
Some drugs also interfere with cyp2d6. Prime among these are the
SSRIs, with the exception of Zoloft (if I remember correctly). The
most potent inhibitor is paroxetine (paxil), followed by
fluoxetine (prozac). If you are taking an SSRI, you will probably
experience a markedly decreased euphoria when using codeine.
(Paxil has a half life of only 24hrs, so not taking it for a few
days will do miracles; the half life of prozac is 7 days.)
Finally, codeine itself is a cyp2d6 inhibitor. This means that
taking the whole dose as quickly as possible will probably give
you the biggest high (ie. its a waste to redose in 30 mins).
*GLUTHETHIMIDE
A combination of codeine and gluthethimide (a sleeping agent) has
been used in some places as a heroin substitute. Gluthethimide is
an enzyme-inducer, and it allows the body to convert more than 10%
of codeine into morphine. Note that this combination increases the
addiction potential of codeine.]
---- End of FAQ
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