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Codeine FAQ
by MDH and Jbuzdyga
v 2.0 - Apr 27, 1996
minor update Nov 2008, by Erowid
Erowid Note: This FAQ was not authored by Erowid. It may include out-of-date and/or incorrect information. Please check the version date to see when it was most recently revised. It appears on Erowid as part of our historical archives. For current information, see Erowid's summary pages in the substance's main vault.
INDEX
INTRODUCTION
EFFECTS AND USES
USING CODEINE
EXTRACTION TECHNIQUE
PHARMACOLOGY & DRUG INTERACTIONS
CREDITS & REVISION HISTORY



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 8 mg per unit dose of a drug. A example is 325 mg of acetaminophen/paracetamol (a unit dose of acetaminophen) and 8 mg 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 3.3 mg/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 15 mg 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 8 mg, 15 mg, 30 mg, 60 mg of codeine. Each tablet also contains caffeine in doses of 15 mg, 30 mg, 30 mg and 0 mg respectively. Thus Tylenol #4 w/ codeine (the most desired one) contains 325 mg of acetaminophen, 60 mg 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. 120 mg of codeine administered SC (subcutaneously, injected under the skin) provides pain relief equal to 10 mg of morphine administered by the same route. Doses used to relieve cough or diarrhea range from 5 mg to 30 mg.

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 during hapatic metabolism (see Pharmacology & Drug Interactions below). 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 30 mg - 60 mg 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 250 mg 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 800 mg 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 500 mg, so doses above 450 mg are in the red zone.

[Erowid Note: We believe the LD50 data listed above is based on a single paper which reported a human death at 12 mg/kg. Unfortunately the route of administration for this death was not listed. Without this information, the report is basically meaningless. Estimating an LD50 in humans is nearly impossible as LD50 data cannot be directly interpreted between humans and other species. Known oral LD50s for codeine sulphate are: 430 mg/kg in rats and 395 mg/kg in mice. Oral LD50s for codeine phosphate include: 266 mg/kg in rats, 237 mg/kg in mice, and 100 mg/kg in rabbits. It should be remembered that a dose which can be easily tolerated by someone with a significate opiate tolerance could kill an individual with no tolerance.]


Using Codeine

Again a good dose to start using codeine at is in the 30 mg to 60 mg 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 100 mg, 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 30-60 mg 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 TypeSolubility (31C water) Solubility (21C water)
Aspirin 1g / 100 ml 1g / 300 ml
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 50 ml 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 300 mg of caffeine in the finished product (15 mg/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 * 8 mg/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. 40 ml / 20 tablets or more if needed. I would suggest you don't go over 50 ml 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.)

[Erowid Note -- The described method may not form crystals large enough to be filtered by non-lab grade filters (i.e. coffee filters). A reader suggests no agitation during cooling, slow stirring until a temperature of 15 degrees C is reached, and a period of 5-10 minutes with slow chilling on ice prior to moving the mixture into the refrigerator. Note that crystals may not be visible, and cloudiness may not indicate crystallization.]

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.]


Credits & Revision History

June 28, 1994 - Original FAQ by mdh@debug.cuc.ab.ca
April 27, 1996 - Version 2.0 by jbuzdyga@mustang.uwo.ca (Jakub Buzdygan)
Feb 5, 2007 - Version 2.1 - Erowid takes over stewardship, as author now unreachable. Holds unmodified for archival purposes, except for minor corrections.

Nov 11, 2008 - Version 2.2 - Erowid adds note to extraction section.