Today is Wednesday, July 28, 2010 and it is now 621AM here in Makati, Luzon, Philippines.
Recap: I had been discussing the Philippine Dope Scene, then meandered into a pedantic explanation of the Heroin Numbering System, another true blue American invention.
This Entry: "Mexican Tar Heroin" is usually considered as a class onto itself despite its technically meeting the threshold for #4 Heroin, heroin hcl.
Most people, including, amazingly, many forensic chemists, believe that Tar is manufactured by acetylysing opium. It is not, but before I explain THAT fallacy, I ought to explain acetylysation;
Heroin is merely a vehicle for the delivery of morphine. Most people do not realise this, but heroin, diacetylmorphine, is inactive in the human body! Once heroin is ingested, within 90 seconds your body has converted it to 6-MAM, a substance I will discuss, and then even more quickly to morphine, the substance you actually feel.
How does morphine become heroin? By adding water, a glacial acetic acid and heating, in reflux, the sugars in morphine actetylyse, creating diacetylmorphine, heroin. This change in structure increase lipid solubility so that the substance is able to cross the BBB (Blood to Brain Barrier) 3 times more efficiently than unacetylated morphine. In other words, making morphine into heroin allows morphine to do its job 3 times better than it would untouched.
When morphine crosses the BBB it almost immediately reverts to morphine, so, heroin simply serves as a more efficient way to get the morphine where it needs to go, this is why, most of the time, you are tested for morphine when tested for heroin in your system, etc. You can sometimes be tested for the afore mentioned 6-MAM which is ONLY found after the consumption of heroin, but 6-MAM is out of your body, entirely, within 20 hours of conversion from heroin.
So THAT is acetylysation, and that is why morphine goes through acetylysation.
The belief that Tar is acetylated opium seems like it makes good common sense. After all, heroin IS made from opium, and both have the same black latex appearance and consistency.
The problem though is that it does not make common sense at all. Opium averages a morphine content of 10%, and the highest recorded content in history was a sample with 23%, and that was only one time. So, if opium is used, and is converted directly into heroin, the highest purity Tar Heroin could ever have would be 23% with the vast majority being 10% pure. Tar IS an impure form but still clocks purities in the 80th percentile from time to time.
How can you make 80% pure heroin directly from opium? How does 10% morphine turn into 80% heroin? It can't, and it won't, ever.
The key to Tar is the acetylation process and agent, as well as the omission of 2 of the 4 manufacturing steps.
Step I) With the normal process you take opium and separate morphine from it, then crystallise it, all very crudely. When making Heroin #1 (which as we discussed earlier is not even heroin at all but rather morphine hcl) the extraction is done meticulously, but that is very rare.
Step II) You convert morphine freebase (or hcl in the case of Heroin #1) into heroin acetate, a crude salt.
Step III) Heroin acetate is converted to Heroin freebase, Heroin #2.
Step IV) Heroin freebase is converted to the hydrochloric salt.
Ideally the salt will be purified via 1 or 2 methods (decolourisation via activated charcoal and filtration and/or ether and alcohol treatments) but in today's world,sadly, it often isn't.
With Tar, morphine freebase is extracted from opium. THEN this freebase is acetylysed. Steps II and III are left by the wayside. The acetylysation process though is the real key.
Though any GAA (glacial acetic acid) will acetylyse morphine, using different acids will produce different characters in the finished product. Ideally AA (acetic anhydride is used), but Tar almost always utilises AC (acetyl chloride). While this produces a particular character, I will first look at 2 other aspects that result from this abbreviated process;
Acetylysation is done in reflux. "Reflux," in short, is a tightly controlled environment where mositure and oxegyn are not allowed in and out at will. Not being actual labs, and usually not actually chemists themselves, manufacturers utilise a crude reflux apparattus. Taking a large cooking pot, the powderised morphine freebase (or hcl.), water and GAA is combined. A rubber gasket is lain over the top, and then the lid. To firmly create a seal a c-clamp is used and tightened all the way.
With Tar, AC is used in place of AA, and no gasket or c-clamp are used so that reflux isn't achieved. Additionaly, time isn't optimised so that full acetylysation doesn't take place. While most morphine IS converted to heroin, the less than optimal acetylation produces marked metabolite characterisation. In short, the extra-crude process used in Mexico causes the heroin to have predictable amounts of 6-MAM and another metabolite, 3-MAM (both of which I will discuss shortly).
Substances ingested metabolise, they change in a reaction with the human body. With drugs, sometimes these new substances, or "metabolites," are "active," meaning that they have a marked reaction on body and/or mind...or else they are "inactive," having no discernible effect.
One active metabolite specific to heroin, 6-Monoacetylmorphine (6-MAM), is actually more powerful than heroin. Heroin, as I stated, is merely a delivery vehicle for morphine itself. Heroin is worthless as a drug itself because the acetylation which allows much greater pentration of the Blood to Brain Barrier also prevents the diacetylmorphine (heroin) from getting hold of the relevant binder. This is why everything you, or someone else feels when using heroin is related to the morphine carried with THAT heroin.
This failure to bind cannot be mitigated but let us imagine there was a way. We would still have a 2nd insurmountable hurdle to deal with in that heroin's half life is a mere 90 seconds. "Half Life" is the avg.time it takes a substance to leave a human body.
Ergo, if heroin's half life is 90 seconds, heroin is gone within 3 minutes of consuming it.
6-MAM, as I said specific to heroin (not found in morphine, duh), is created naturally in degradation, and itself degrades very quickly as well. Other than that natural degradation creating it, it is also created via a process called "Hydrolysis." Hydrolysis takes place when a substance, susceptible to the dynamic, comes into contact with moisture...Conversely, if acetylysation takes place without benefit of reflux the requsite moisture is burned off/evaporates. This will give you less 6-MAM than heroin produced in reflux.
This leaves Tar with an anabnormally low percentage of 6-MAM, always.
On the other hand, Tar will always have abnormally high 3-MAM content. This is due from insufficient acetylysation. The use os acetyl chloride, insufficient time and temperature prevents a total conversion of morphine to diacetylmorphine (heroin).
Reflux also plays a part here but by adjusting time and temprature upwards the deficiencies caused by acetyl chloride can be overcome. Sadly, Mexican producers just do not get the point. By now the process is so well entrenched that I suspect Tar is here to stay, unfortunately.
"Homebake" is produced sans reflux, with different GAAs but the only REAL difference there is that O-demethylation is sometimes used to net morphine from a codeine precursor.
In addition, when Dicodin used to be used as a precursor the end product would be red or pink tar, but those rare times that Homebake still appears one sees only brown and black tar, since Dicodin is extinct.
I will continue...
(Edited for spelling)
Recap: I had been discussing the Philippine Dope Scene, then meandered into a pedantic explanation of the Heroin Numbering System, another true blue American invention.
This Entry: "Mexican Tar Heroin" is usually considered as a class onto itself despite its technically meeting the threshold for #4 Heroin, heroin hcl.
Most people, including, amazingly, many forensic chemists, believe that Tar is manufactured by acetylysing opium. It is not, but before I explain THAT fallacy, I ought to explain acetylysation;
Heroin is merely a vehicle for the delivery of morphine. Most people do not realise this, but heroin, diacetylmorphine, is inactive in the human body! Once heroin is ingested, within 90 seconds your body has converted it to 6-MAM, a substance I will discuss, and then even more quickly to morphine, the substance you actually feel.
How does morphine become heroin? By adding water, a glacial acetic acid and heating, in reflux, the sugars in morphine actetylyse, creating diacetylmorphine, heroin. This change in structure increase lipid solubility so that the substance is able to cross the BBB (Blood to Brain Barrier) 3 times more efficiently than unacetylated morphine. In other words, making morphine into heroin allows morphine to do its job 3 times better than it would untouched.
When morphine crosses the BBB it almost immediately reverts to morphine, so, heroin simply serves as a more efficient way to get the morphine where it needs to go, this is why, most of the time, you are tested for morphine when tested for heroin in your system, etc. You can sometimes be tested for the afore mentioned 6-MAM which is ONLY found after the consumption of heroin, but 6-MAM is out of your body, entirely, within 20 hours of conversion from heroin.
So THAT is acetylysation, and that is why morphine goes through acetylysation.
The belief that Tar is acetylated opium seems like it makes good common sense. After all, heroin IS made from opium, and both have the same black latex appearance and consistency.
The problem though is that it does not make common sense at all. Opium averages a morphine content of 10%, and the highest recorded content in history was a sample with 23%, and that was only one time. So, if opium is used, and is converted directly into heroin, the highest purity Tar Heroin could ever have would be 23% with the vast majority being 10% pure. Tar IS an impure form but still clocks purities in the 80th percentile from time to time.
How can you make 80% pure heroin directly from opium? How does 10% morphine turn into 80% heroin? It can't, and it won't, ever.
The key to Tar is the acetylation process and agent, as well as the omission of 2 of the 4 manufacturing steps.
Step I) With the normal process you take opium and separate morphine from it, then crystallise it, all very crudely. When making Heroin #1 (which as we discussed earlier is not even heroin at all but rather morphine hcl) the extraction is done meticulously, but that is very rare.
Step II) You convert morphine freebase (or hcl in the case of Heroin #1) into heroin acetate, a crude salt.
Step III) Heroin acetate is converted to Heroin freebase, Heroin #2.
Step IV) Heroin freebase is converted to the hydrochloric salt.
Ideally the salt will be purified via 1 or 2 methods (decolourisation via activated charcoal and filtration and/or ether and alcohol treatments) but in today's world,sadly, it often isn't.
With Tar, morphine freebase is extracted from opium. THEN this freebase is acetylysed. Steps II and III are left by the wayside. The acetylysation process though is the real key.
Though any GAA (glacial acetic acid) will acetylyse morphine, using different acids will produce different characters in the finished product. Ideally AA (acetic anhydride is used), but Tar almost always utilises AC (acetyl chloride). While this produces a particular character, I will first look at 2 other aspects that result from this abbreviated process;
Acetylysation is done in reflux. "Reflux," in short, is a tightly controlled environment where mositure and oxegyn are not allowed in and out at will. Not being actual labs, and usually not actually chemists themselves, manufacturers utilise a crude reflux apparattus. Taking a large cooking pot, the powderised morphine freebase (or hcl.), water and GAA is combined. A rubber gasket is lain over the top, and then the lid. To firmly create a seal a c-clamp is used and tightened all the way.
With Tar, AC is used in place of AA, and no gasket or c-clamp are used so that reflux isn't achieved. Additionaly, time isn't optimised so that full acetylysation doesn't take place. While most morphine IS converted to heroin, the less than optimal acetylation produces marked metabolite characterisation. In short, the extra-crude process used in Mexico causes the heroin to have predictable amounts of 6-MAM and another metabolite, 3-MAM (both of which I will discuss shortly).
Substances ingested metabolise, they change in a reaction with the human body. With drugs, sometimes these new substances, or "metabolites," are "active," meaning that they have a marked reaction on body and/or mind...or else they are "inactive," having no discernible effect.
One active metabolite specific to heroin, 6-Monoacetylmorphine (6-MAM), is actually more powerful than heroin. Heroin, as I stated, is merely a delivery vehicle for morphine itself. Heroin is worthless as a drug itself because the acetylation which allows much greater pentration of the Blood to Brain Barrier also prevents the diacetylmorphine (heroin) from getting hold of the relevant binder. This is why everything you, or someone else feels when using heroin is related to the morphine carried with THAT heroin.
This failure to bind cannot be mitigated but let us imagine there was a way. We would still have a 2nd insurmountable hurdle to deal with in that heroin's half life is a mere 90 seconds. "Half Life" is the avg.time it takes a substance to leave a human body.
Ergo, if heroin's half life is 90 seconds, heroin is gone within 3 minutes of consuming it.
6-MAM, as I said specific to heroin (not found in morphine, duh), is created naturally in degradation, and itself degrades very quickly as well. Other than that natural degradation creating it, it is also created via a process called "Hydrolysis." Hydrolysis takes place when a substance, susceptible to the dynamic, comes into contact with moisture...Conversely, if acetylysation takes place without benefit of reflux the requsite moisture is burned off/evaporates. This will give you less 6-MAM than heroin produced in reflux.
This leaves Tar with an anabnormally low percentage of 6-MAM, always.
On the other hand, Tar will always have abnormally high 3-MAM content. This is due from insufficient acetylysation. The use os acetyl chloride, insufficient time and temperature prevents a total conversion of morphine to diacetylmorphine (heroin).
Reflux also plays a part here but by adjusting time and temprature upwards the deficiencies caused by acetyl chloride can be overcome. Sadly, Mexican producers just do not get the point. By now the process is so well entrenched that I suspect Tar is here to stay, unfortunately.
"Homebake" is produced sans reflux, with different GAAs but the only REAL difference there is that O-demethylation is sometimes used to net morphine from a codeine precursor.
In addition, when Dicodin used to be used as a precursor the end product would be red or pink tar, but those rare times that Homebake still appears one sees only brown and black tar, since Dicodin is extinct.
I will continue...
(Edited for spelling)