Boil the liquid in the microwave, watch *very* carefully. When it starts boiling/bubbling a lot, stop the microwave and take it out. Remove any congealed crap floating on top with a spoon.
(6) Boil off about 3/4 of the remaining water to concentrate the solution bupropion-wise. If you see more congealed particulate matter floating on top, remove it with a spoon. If it's on the bottom of the cup, just leave it.
(7) Get some kind of small container... this person used contact lens vials, which are very small and made of glass with a black plastic cap. Bigger ones will work as well. It's important to be able to shake well though. Fill each vial halfway with the liquid from step (6) above, and the other half with Naptha (Zippo lighter fluid). This is "step 5" from the above website, except without the alcohol. Shake the vial(s) well for 5 minutes, let sit. Siphon off the naptha top layer (or most of it) with an eyedropper. Optional -- add more naptha and repeat this step once or twice more.
(8) You should be left with a light pink or purple fluid (coloration is from remaining dye from original bupropion tabs). Spread this fluid on a piece of glass (old flatbed scanner) or flat kitchen dinner plate. Dry with a blow dryer (if there's any remaining naptha, it will evaporate). Repeat this step a couple times, covering over the dried stuff on the glass with new liquid and re-drying. Allow to air dry for a good while as well.
(9) Scrape off the dried-out crystals on the glass with a sharp razor blade. This is reasonably pure Bupropion HCL (pure enough to snort anyway... never inject anything without lab tests for purity). The crystals are slightly hydrophilic, but nothing like in previous botched extractions when there was a lot of cellulose crap never removed properly. In those previous instances, the crystals would either clump during the scraping phase or clump once stored after a short time. This stuff does not.
Two steps this person sees as critical to this procedure:
(1) Microwave "defatting" (congealing of cellulose) working thoroughly and successfully. This really removes a large proportion of crap from the tablets somehow. (2) Using a *lot* of Bupropion tablets to a relatively small amount of boiling water in the beginning step. Once the other crap is mostly removed, the concentration of Bupropion dissolved in H2O should be *really, really* strong so the final step results in largest possible actives to (remaining cellulose) ratio. Also, this allows for a LOT of wastage in the coffee filtering steps etc. without it being a big deal. Probably the best to use is Wellbutrin XL 300mg (best ratio of crap to actives).
G'Luck people. This is all pretty oversimplified, but there's a lot of room for inventiveness herein. And probably many better ways to extract bupropion, but not without at least some chemistry set parts .
Closing notes: bupropion HCL is not intended to be nasally insufflated (snorted), and can cause seizures at higher doses. Extreme caution is advised. Naptha is reasonably safe to work with, but avoid contact with skin and use proper ventilation. Microwave ovens can cause burns. And attempting to extract a month's worth of one's antidepressant medication means that (particularly in case of failure) one gets depressed.
P.S.: The bupropion described herein was legally prescribed to this person, and he did nothing wrong in extracting it. Special thanks to him for sending me the instructions for posting here.
From: DEHughes
Date: Thurs, Nov 19 1998 12:00 am
Groups: sci.med.pharmacy
Here is the text with references of a report I wrote on Benzedrex inhalers for
a project during a rotation assignment....
The Benzedrex Inhaler is indicated for the temporary relief of nasal
congestion due to the common cold, hay fever, or associated with
sinusitis1. The active ingredient is propylhexedrine 250 mg which
is soaked into a fibrous medium, and the vapors are inhaled
nasally. This dosage form delivers in each 800 ml of inhaled
air 0.40 - 0.50 mg of propylhexedrine1.
Propylhexedrine is an a-agonist with main clinical usefulness
as a nasal decongestant. Structurally it is related to the
stimulant methamphetamine. The only difference between them
is the phenyl ring of methamphetamine is replaced with a hexyl
ring in propylhexedrine. It is this similarity that has led
to the abuse of propylhexedrine. Propylhexedrine has been
extracted from inhalers and injected IV as an amphetamine
substitute, and has also been ingested by soaking the fibrous
interior in hot water. It is not without risks, and reported
cases of psychosis, myocardial infarction, pulmonary vascular
disease and pulmonary hypertension are well reported in the
medical literature. From 1973 to 1979, 12 cases of sudden death
were reported in Dallas County related to the IV use of Benzedrex,
with right ventricular hypertrophy present in 9 of the 12. The
potent vasoconstricting a-agonist property can lead to damage
of the tissues where it was injected. In one case, the artery
where it was injected constricted and lead to ischemic damage
of the hand, resulting in amputation of part of the hand. In
Portland, Oregon a male subject died after attempting to inject
into his right jugular vein. His neck contained extensive
necrotic tissue with swelling and displacement of the
trachea.
Benzedrex inhalers are frequently stolen from pharmacies. We
currently keep them behind the counter and supply them only
when requested. Teenagers will attempt to purchase them, but
are denied by the staff. It is of interest to note that the
manufacturer Menley & James maintains an Internet site where,
amongst other items, the Benzedrex inhaler can be purchased
via mail order for $4.49 ea. or $51.00/dozen.8
For its indicated use as a nasal decongestant, one study only
showed 2 hours of decreased congestion after inhalation. The
therapeutic blood levels to reach nasal decongestion are
1/30th that of the levels achieved when abused by injection.
This is an OTC product that can have serious health
implications, and all pharmacist need to be aware of
who are purchasing them, and in what quantity the stock
is being moved.
References
1. Benzedrex Inhaler package labeling. Manley & James
Laboratories, Inc. Horsham, PA 19044
2. Hoffman BB, Lefkowitz RJ. Sympathomimetic drugs.
In: Goodman & Gilman’s Pharmacological Basis of
Therapeutics 9th ed. New York. McGraw Hill, 1996:
202-21
3. Riley MR et al. Nasal Decongestants. Facts &
Comparisons. St Louis. 1998: 186
4. Fornazzari L, Carlen PL, Kapur BM. Intravenous
abuse of propylhexedrine (Benzedrex) and the risk
of brainstem dysfunction in young adults. Can J
Neurol Sci 1986 Nov 13:4 337-9
5. Anderson RJ, Garza HR, Garriott JC, Dimaio V.
Intravenous propylhexedrine abuse and sudden death.
Am J Med 1979 Jul 67:1 15-20
6. Covey DC, Nossaman BD, Albright JA. Ischemic injury
of the hand from intra-arterial propylhexedrine injection.
The Journal Of Hand Surgery 1988;13A:58-61
7. Perez J, Burton BT, McGirr JG. Airway compromise and
delayed death following attempted central vein injection
of propylhexedrine. J Emerg Med 1994 Nov-Dec 12:6 795-7
8. http://www.menleyjames.com/order.html
9. Hamilton LH. Nasal decongestant effect of propylhexedrine.
Ann Otol Rhinol Laryngol 1982 Jan-Feb 91:1 Pt 1 106-11
10. DiMaio VJ, Garriott JC. Intravenous abuse of
propylhexedrine. J Forensic Sci 1977 Jan 22:1 152-8
===============================================================
From: CLYDE ALDRIDGE - view profile
Date: Mon, Oct 9 1995 12:00 am
Groups: sci.med.pharmacy
The Benzedrex inhaler contains a stimulant compound,
prophylhexadrine, which alone would probably be a C-II
narcotic. Drug addicts are taking the cotton wad that
is soaked with camphor, menthol and prophylhexadrine
and ingesting it for the intense stimulant effect. How
can such drugs sit on counters where people can buy them
w/o Rx? What are the long term effects of ingesting this
product? I remember getting out of my car at a local
pharmacy and seeing about twenty empty Benzedrex packages
in tne parking lot. I am not a pharmicist rather an Electrical
Engineer
===============================================================
From: BrianFromID - view profile
Date: Thurs, Jan 27 2000 12:00 am
Groups: alt.drugs.chemistry
Yes, I feel too that the Propylhexedrine in Benzedrex, better
known as Hexahydrodesoxyephedrine is ok, I too remember when
they pulled Dristans of the market around 1984, 250mg :thats
a whole quarter gram,rather than in Vicks,which is only 50mg
and garbage anyway because of its polarization,"Levo"
state......
===============================================================
From: The Skipper - view profile
Date: Mon, Jun 1 1998 12:00 am
Groups: alt.drugs.chemistry
On 1 Jun 1998 22:04:08 +0200, nob...@REPLAY.COM (Anonymous) wrote:
>Or you could just put the racemic mixture in your nose. But obviously
>this won't work, because if it did, everyone would be taking Vicks
>Inhalers and alkali and making crank this way. There wouldn't be any
>Vicks Inhalers on the shelves.
A few years ago, there was a brand of inhaler called Benzedrex.
I knew a lot of people that used them to make "crank". The
stuff wasn't too bad, but it did take a lot more of it to do
the same thing that the other isomer would. Vicks supposedly
didn't have as much in them so people didn't bother with them.
===============================================================
From: John Doe - view profile
Date: Fri, Oct 24 1997 12:00 am
Groups: alt.drugs.chemistry
According to the Merck index, 12th ed, #8045 " prep by
catalytic hydrogenation of the phenyl analogue using adams
platinum catalysts and glacial acetic acid as the solvent "
They're just changing the flat old benzene ring into a more
flexible cyclohexyl....ya know, just saturating the aromatic
part of the meth molecule..
Anthony Ankrom wrote:
> In article <199710192227.TAA22...@privacynb.ml.org>,
> Anonymous wrote:
> >Does anyone have any info on propylhexedrine. Does its activity vs.
> >chirality resemble that of of meth? Do inhalers contain the
> >l-propylhexedrine as opposed to a more CNS active d compound? ( I would
> >assume so, but can't find any info with search engines or Deja News)
> >
> >(note, propylhexedrine is the cyclohexane isomer of meth)
> >thanks, John
> >
> Propylhexedrine is not CNS active. No appreciably anyway.
> I once read in a forensic journal about a guy who died from
> eating some 20 "Benzedrex" inhaler innards. (Benzedrex is
> propylhexedrine.)
>
> So why didn't you ask if methedrine could be made from propylhexedrine?
> I bet you could re-aromatize it by heating it in tetradecalin with
> sulfur or selenium or maybe even 10% Pd/C. Would have to get it
> really hot. Sulfur would be the easiest to monitor since H2S
> is evolved. Although this gas is toxic it's not as toxic as
> H2Se. The Pd/C would just suck up the H2. I don't know what
> would happen to the aliphatic chain during the reaction though...
>
> Anthony
> (Mr. Peabody)
(information herein is believed to be included appropriately under copyright laws
governing fair Use in the USA. Email the webmaster if the information belongs to you and you'd like it removed from this page. Emails to the webmaster unrelated to copyright will not be read or answered).
1: J Forensic Sci. 1977 Jan;22(1):152-8. Related Articles, Links
Intravenous abuse of propylhexedrine.
DiMaio VJ, Garriott JC.
Propylhexedrine, a local vasoconstrictor, is the active ingredient in the
Benzedrex nasal inhaler. In a six-month period, the Office of the Medical
Examiner of Dallas County has encountered three deaths resulting from
intravenous injection of propylhexedrine. Two of these individuals showed
vascular changes in the lungs, apparently from chronic intravenous
injections of this drug. Body distribution of the drug was determined
in all of the cases by gas chromatographic analysis. An experiment was
conducted to determine "therapeutic blood concentrations" in which a
normal subject inhaled propylhexedrine from the Benzedrex inhaler.
The maximum blood concentration was only 1/30 of the minimum
concentration encountered in the reported cases.
===================================================
1: J Toxicol Clin Toxicol. 1983-1984;21(3):359-72. Related Articles, Links
Tissue injuries associated with parenteral propylhexedrine abuse.
Mancusi-Ungaro HR Jr, Decker WJ, Forshan VR, Blackwell SJ, Lewis SR.
Propylhexedrine, the active ingredient in Benzedrex Inhalers, is extracted
from the wicks of the inhalers by drug abusers for intravenous injection to
provide a "desirable high." Six representative cases treated over a one-year
period are presented to exemplify the potential for soft tissue injury.
Because the actual constituents of the injected material prepared from
the inhalers were not established, solutions were prepared from Benzedrex
Inhalers according to the formula provided by one of the patients. The extract
was then subjected to vigorous qualitative and quantitative analyses; the
presence of essentially pure propylhexedrine hydrochloride was confirmed
in varying concentrations. To examine the progression of injury following
injection of the prepared extract, the ears of 12 New Zealand white rabbits
were injected either intra-arterially or subcutaneously. The opposite ear
of each rabbit served as a control. Both clinical and pathologic observations
demonstrated injury consistent with intense local vasoconstriction. Injury
did not appear to relate to impurities in the solution or other embolic
phenomena. Finally, the laboratory findings are discussed with regard to
the clinical examples. In sum, the insult to tissue from intravascular or
local injection with propylhexedrine appears to respond, although poorly,
to efforts to reverse the intense pharmacologic vasoconstriction.
===================================================
Can J Neurol Sci. 1986; 13(4):337-9 (ISSN: 0317-1671)
Fornazzari L; Carlen PL; Kapur BM
In 1949, amphetamine sulfate was replaced by propylhexedrine in the nasal
decongestant agent Benzedrex because of psychosis, sudden death, and
widespread abuse. Propylhexedrine is not without risks, and reported
cases of psychosis, myocardial infarction, pulmonary vascular disease
and pulmonary hypertension, and sudden death are well documented in the
medical literature. We are reporting 2 cases of definite brainstem dysfunction
and 5 cases of transient diplopia secondary to IV abuse of Benzedrex. This
widely abused drug is prepared by heating Benzedrex and hydrochloric acid,
and the resulting crystals are dissolved in water for injection. This agent
is called "stove-top speed". All 7 patients had transient diplopia, within
seconds after injection. One patient had evidence of a right-internuclear
ophthalmoplegia, and another had a depressed right gag reflex and paralysis
of the right half of the tongue. The deficits in these two patients, persisted
for many months. In young adults with history of drug abuse, the IV use of
Benzedrex should be considered in the differential diagnosis of transient
or permanent focal brainstem deficits.
===================================================
Intravenous Abuse of Propylhexedrine
DiMaio, VJM
Medical examiner, Dallas County, Southwestern Institute of Forensic
Sciences, Dallas; and assistant professor, Department of Pathology,
University of Texas, Southwestern Medical School at Dallas, Tex. 75235.
Garriott, JC
Chief toxicologist, Southwestern Institute of Forensic Sciences,
Dallas; and assistant professor in forensic sciences, Departments
of Pathology and Pharmacology, University of Texas, Southwestern
Medical School at Dallas, Tex.
Abstract
The Benzedrex® nasal inhaler is an over-the-counter device used for the
symptomatic treatment of nasal congestion resulting from head colds and
hay fever. The active ingredient is propylhexedrine, a local
vasoconstrictor. While only two deaths due to propylhexedrine are in
the medical literature [1], abuse of the drug occurs with greater frequency
than realized. Since 1974, the Dallas County Criminal Investigation Laboratory
has detected propylhexedrine in syringes in twelve cases submitted by
local police agencies. In a recent six-month period, the Office of the
Medical Examiner for Dallas County has encountered three deaths resulting
from intravenous injection of propylhexedrine as well as two deaths from
other causes in which the deceased had been injecting this drug. Two of
the individuals dying of propylhexedrine abuse showed vascular changes
in the lungs, apparently caused by chronic intravenous injection of
this drug.
===================================================
Pharmacos listing (appears to be an obsolete usage of propylhexedrine).
Propylhexedrine
Also marketed in the EU under the name(s): Eventin, Cafilon
INN: Propylhexedrine/ Fenbutrazate
Indication: Adjunctive therapy to diet, in patients with obesity and a
body mass index (BMI) of 30 kg/m2 or higher who have not responded to
an appropriate weight-reducing regimen alone
Marketing Authorisation Holder: Not available
===================================================
Original Sanction Against Dubin Upheld
Bonn, Germany - The International Paralympic Committee (IPC) announces that
the Internal Appeal requested by the National Paralympic Committee (NPC) of
Austria regarding the anti-doping rule violation of Wolfgang Dubin (Athletics,
F36), which occurred during the ATHENS 2004 Paralympic Games has been denied
after an Internal Appeal Hearing. The original decision imposed was upheld,
meaning that Dubin is retrospectively disqualified and loses his silver
medal from the men’s Shot Put final event and receives a minimum sanction.
The minimum sanction is a warning and reprimand and no period of
ineligibility considering that the substance used belongs to the list
of Specified Substances and that the use was not intended to enhance
sport performance (Article 12.3 of the IPC Anti-Doping Code).
Dubin, 36 years of age, from Austria, returned an adverse analytical finding
of a stimulant, propylhexedrine, a substance regarded as belonging to the list
of Specified Substances in a urine sample taken during the in-competition period
of the ATHENS 2004 Paralympics.
During the Internal Appeal Hearing, Dubin reiterated that he had no knowledge
of the substance being on the World Anti-Doping Code (WADC) 2004 Prohibited
List and as a result his NPC did not apply for a Therapeitic Use Exemption
(TUE) on his behalf.
The basis for the IPC's decision is the World Anti-Doping Agency's (WADA)
confirmation, prior to the initial notification, that propylhexedrine was
included on the 2004 Prohibited List through the clause SI (Stimulants).
===================================================
After i.v. application of barbexaclone the following pharmacokinetic
parameters for propylhexedrine were determined: t 0.5 0.31 h, t 0.5
2.5h, Vd 19.3l/kg; bioavailability (AUC oral/AUC i.v.) 0.37.
Propylhexedrine penetrated the blood-brain barrier rapidly. High
but unequal tissue accumulation was observed: lung=kidney>liver=brain
>spleen>heart>skeletal muscle.
===================================================
The chemical name for propylhexedrine is N,.alpha.-dimethylcyclo-
hexaneethylamine (IUPAC name). It is known as .beta.-cyclohexyl-
isopropylmethylamine in U.S. Pat. No. 2,454,746 to Ullyot, which
describes an earlier-used synthetic route for preparing
propylhexedrine. Propylhexedrine is represented by the
following chemical structure: ##STR1##
Propylhexedrine is a clear, colorless liquid having a characteristic
amine-like odor. It volatilizes slowly at room temperature and
solutions are alkaline when subjected to a litmus test. Propylhexedrine
therefore absorbs carbon dioxide from the air in an acid-base reaction.
The specific gravity is between 0.848 to 0.852. It boils at about 205.
degree. C. Propylhexedrine is only slightly soluble in water, with only
1 gram being dissolvable in 500 ml of water. On the other hand, 1 gram
of propylhexedrine is soluble in 0.4 ml alcohol, 0.2 ml of chloroform,
or 0.1 ml of ether. The hydrochloride form of propylhexedrine, formed
by reacting one molar equivalent of propylhexedrine with one molar
equivalent of hydrochloric acid, is soluble in water and is a
crystalline solid at room temperature.
Holy sh*t... this person performed his first really successful Bupropion HCL extraction. The stuff hits like a freight train when made into small lines and insufflated, in fact this person is not sure he likes the effects at all. There's a bit of an unpleasant rush combined with a headache, loud tinnitus + strange body load, and this person noticed almost total urinary retention (inability to piss)... unless that's from some other substance. Not likely though, it's a problem this person *very, very* rarely encounters. Even amphetamines or coke don't do that to this person.
