Cocane

methy (1R,2R,3S,5S)-3- (benzoyoxy)-8-methy-8-azabcyco|3.2.1| octane-2-

carboxyate
Cnca data
AHFS/Drugs.com Mcromedex Detaed Consumer Informaton
Pregnancy cat. C
Lega status Controed (S8) (AU) Schedue I (CA) A (UK) Schedue II (US)
Narcotc Schedues I and III (UN)
Dependence abty Hgh
Routes Topca, Ora, Insuffaton, IV, PO
Pharmacoknetc data
Boavaabty Ora: 33%|1|
Insuffated: 60|2|-80%|3|
Nasa Spray: 25|4|-43%|1|
Metabosm Hepatc CYP3A4
Haf-fe 1 hour
Excreton Rena (benzoyecgonne and ecgonne methy ester)
Synonyms methybenzoyecgonne, benzoymethyecgonne, ecgonne
methy ester benzoate, 2b-Carbomethoxy -3b-benzoyoxy tropane
Chemca data
Formua C17H21NO4
Mo. mass 303.353 g/mo
Cocane (INN) (benzoymethyecgonne, an ecgonne dervatve) s a
crystane tropane akaod that s obtaned from the eaves of the coca pant.
|5| The name comes from "coca" and the akaod suffx "-ne", formng
"cocane". It s a stmuant, an appette suppressant, and a nonspecfc
votage gated sodum channe bocker, whch n turn causes t to produce
anaesthesa at ow doses. Boogcay, cocane acts as a serotonn-
norepnephrne-dopamne reuptake nhbtor, aso known as a trpe reuptake
nhbtor (TRI). It s addctve because of ts effect on the mesombc reward
pathway.|6| It s markedy more dangerous than other CNS stmuants,
ncudng the amphetamne cass, at hgh doses due to ts effect on sodum
channes, as bockade of Nav1.5 can cause sudden cardac death.|7|
Unke most moecues, cocane has pockets|carfcaton needed| wth both
hgh hydrophc and pophc effcency, voatng the rue of hydrophc-
pophc baance. Ths causes t to cross the bood-bran barrer far better
than other psychoactve chemcas|ctaton needed| and may even nduce
bood-bran barrer breakdown.|8||9|
It s controed nternatonay by Snge Conventon on Narcotc Drugs
(Schedue I, preparaton n Schedue III).
Medca effects
Data from The Lancet suggests cocane s ranked both the 2nd most addctve
and the 2nd most harmfu of 20 popuar recreatona drugs.|10|
Cocane s a powerfu nervous system stmuant.|11| Its effects can ast from
15-30 mnutes to an hour, dependng on dosage and the route of
admnstraton.|12|
Cocane ncreases aertness, feengs of we-beng and euphora, energy and
motor actvty, feengs of competence and sexuaty. Anxety, paranoa and
restessness can aso occur, especay durng the comedown. Wth excessve
dosage, tremors, convusons and ncreased body temperature are observed.
|11| Severe cardac adverse events, partcuary sudden cardac death,
become a serous rsk at hgh doses due to cocane's bockng effect on
cardac sodum channes.|7|
Occasona cocane use does not typcay ead to severe or even mnor
physca or soca probems.|13||14|
Acute
Man artce: Cocane ntoxcaton
Wth excessve or proonged use, the drug can cause tchng, tachycarda,
haucnatons, and paranod deusons.|15| Overdoses cause hypertherma
and a marked eevaton of bood pressure, whch can be fe-threatenng,|15|
arrhythmas,|7| and death.|7|
Chronc
Sde effects of chronc cocane use
Cocane hydrochorde
Chronc cocane ntake causes bran ces to adapt functonay to strong
mbaances of transmtter eves n order to compensate extremes. Thus,
receptors dsappear from the ce surface or reappear on t, resutng more or
ess n an "off" or "workng mode" respectvey, or they change ther
susceptbty for bndng partners (gands) - mechansms caed
down-/upreguaton. However, studes suggest cocane abusers do not show
norma age-reated oss of strata dopamne transporter (DAT) stes,
suggestng cocane has neuroprotectve propertes for dopamne neurons.|16|
Possbe sde effects ncude nsatabe hunger, aches, nsomna/overseepng,
ethargy, and persstent runny nose. Depresson wth sucda deaton may
deveop n very heavy users. Fnay, a oss of vescuar monoamne
transporters, neurofament protens, and other morphoogca changes
appear to ndcate a ong term damage of dopamne neurons. A these
effects contrbute a rse n toerance thus requrng a arger dosage to acheve
the same effect.|17|
The ack of norma amounts of serotonn and dopamne n the bran s the
cause of the dysphora and depresson fet after the nta hgh. Physca
wthdrawa s not dangerous. Physoogca changes caused by cocane
wthdrawa ncude vvd and unpeasant dreams, nsomna or hypersomna,
ncreased appette and psychomotor retardaton or agtaton.|18|
Physca sde effects from chronc smokng of cocane ncude hemoptyss,
bronchospasm, prurtus, fever, dffuse aveoar nftrates wthout effusons,
pumonary and systemc eosnopha, chest pan, ung trauma, sore throat,
asthma, hoarse voce, dyspnea (shortness of breath), and an achng, fu-ke
syndrome. Cocane constrcts bood vesses, dates pups, and ncreases
body temperature, heart rate, and bood pressure. It can aso cause
headaches and gastrontestna compcatons such as abdomna pan and
nausea. A common but untrue beef s that the smokng of cocane
chemcay breaks down tooth ename and causes tooth decay. However,
cocane does often cause nvountary tooth grndng, known as bruxsm,
whch can deterorate tooth ename and ead to gngvts.|19| Addtonay,
stmuants ke cocane, methamphetamne, and even caffene cause
dehydraton and dry mouth. Snce sava s an mportant mechansm n
mantanng one's ora pH eve, chronc stmuant abusers who do not
hydrate suffcenty may experence demnerazaton of ther teeth due to the
pH of the tooth surface droppng too ow (beow 5.5).
Chronc ntranasa usage can degrade the cartage separatng the nostrs
(the septum nas), eadng eventuay to ts compete dsappearance. Due to
the absorpton of the cocane from cocane hydrochorde, the remanng
hydrochorde forms a dute hydrochorc acd.|20|
Cocane may aso greaty ncrease ths rsk of deveopng rare autommune or
connectve tssue dseases such as upus, Goodpasture's dsease, vascuts,
gomeruonephrts, Stevens-|ohnson syndrome and other dseases.|21||22|
|23||24| It can aso cause a wde array of kdney dseases and rena faure.
|25||26|
Cocane msuse doubes both the rsks of hemorrhagc and schemc strokes,
|27| as we as ncreases the rsk of other nfarctons, such as myocarda
nfarcton.|28|
Addcton
Man artce: Cocane dependence
Cocane dependence (or addcton) s psychoogca dependency on the
reguar use of cocane. Cocane dependency may resut n physoogca
damage, ethargy, psychoss, depresson, akathsa, and fata overdose.
Bosynthess
Man artce: Bosynthess of cocane
The frst synthess and eucdaton of the cocane moecue was by Rchard
Wsttter n 1898.|29| Wsttter's synthess derved cocane from tropnone.
Snce then, Robert Robnson and Edward Leete have made sgnfcant
contrbutons to the mechansm of the synthess. (-NO3)
The addtona carbon atoms requred for the synthess of cocane are derved
from acety-CoA, by addton of two acety-CoA unts to the N-methy-A1-
pyrronum caton.|30| The frst addton s a Mannch-ke reacton wth the
enoate anon from acety-CoA actng as a nuceophe towards the
pyrronum caton. The second addton occurs through a Casen
condensaton. Ths produces a racemc mxture of the 2-substtuted
pyrrodne, wth the retenton of the thoester from the Casen condensaton.
In formaton of tropnone from racemc ethy |2,3-13C2|4(Nmethy-2-
pyrrodny)-3-oxobutanoate there s no preference for ether stereosomer.
|31| In the bosynthess of cocane, however, ony the (S)-enantomer can
cycze to form the tropane rng system of cocane. The stereoseectvty of
ths reacton was further nvestgated through study of prochra methyene
hydrogen dscrmnaton.|32| Ths s due to the extra chra center at C-2.|33|
Ths process occurs through an oxdaton, whch regenerates the pyrronum
caton and formaton of an enoate anon, and an ntramoecuar Mannch
reacton. The tropane rng system undergoes hydroyss, SAM-dependent
methyaton, and reducton va NADPH for the formaton of methyecgonne.
The benzoy moety requred for the formaton of the cocane dester s
syntheszed from phenyaanne va cnnamc acd.|34| Benzoy-CoA then
combnes the two unts to form cocane.
N-methy-pyrronum caton
Bosynthess of N-methy-pyrronum caton
Bosynthess of cocane
Robnson bosynthess of tropane
Reducton of tropnone
The bosynthess begns wth L-Gutamne, whch s derved to L-ornthne n
pants. The ma|or contrbuton of L-ornthne and L-argnne as a precursor to
the tropane rng was confrmed by Edward Leete.|35| Ornthne then
undergoes a Pyrdoxa phosphate-dependent decarboxyaton to form
putrescne. In anmas, however, the urea cyce derves putrescne from
ornthne. L-ornthne s converted to L-argnne,|36| whch s then
decarboxyated va PLP to form agmatne. Hydroyss of the mne derves N-
carbamoyputrescne foowed wth hydroyss of the urea to form putrescne.
The separate pathways of convertng ornthne to putrescne n pants and
anmas have converged. A SAM-dependent N-methyaton of putrescne gves
the N-methyputrescne product, whch then undergoes oxdatve deamnaton
by the acton of damne oxdase to yed the amnoadehyde. Schff base
formaton confrms the bosynthess of the N-methy-A1-pyrronum caton.
Robert Robnson's acetonedcarboxyate
The bosynthess of the tropane akaod, however, s st uncertan.
Hemschedt proposes that Robnson's acetonedcarboxyate emerges as a
potenta ntermedate for ths reacton.|37| Condensaton of N-
methypyrronum and acetonedcarboxyate woud generate the
oxobutyrate. Decarboxyaton eads to tropane akaod formaton.
Reducton of tropnone
The reducton of tropnone s medated by NADPH-dependent reductase
enzymes, whch have been characterzed n mutpe pant speces.|38| These
pant speces a contan two types of the reductase enzymes, tropnone
reductase I and tropnone reductase II. TRI produces tropne and TRII
produces pseudotropne. Due to dfferng knetc and pH/actvty
characterstcs of the enzymes and by the 25-fod hgher actvty of TRI over
TRII, the ma|orty of the tropnone reducton s from TRI to form tropne.|39|
Pharmacoogy
Appearance
A pe of cocane hydrochorde
A pece of compressed cocane powder
Cocane n ts purest form s a whte, peary product. Cocane appearng n
powder form s a sat, typcay cocane hydrochorde (CAS 53-21-4). Street
market cocane s frequenty aduterated or "cut" wth varous powdery fers
to ncrease ts weght; the substances most commony used n ths process
are bakng soda; sugars, such as actose, dextrose, nosto, and mannto;
and oca anesthetcs, such as docane or benzocane, whch mmc or add to
cocane's numbng effect on mucous membranes. Cocane may aso be "cut"
wth other stmuants such as methamphetamne.|40| Aduterated cocane s
often a whte, off-whte or pnksh powder.
The coor of "crack" cocane depends upon severa factors ncudng the
orgn of the cocane used, the method of preparaton - wth ammona or
bakng soda - and the presence of mpurtes, but w generay range from
whte to a yeowsh cream to a ght brown. Its texture w aso depend on
the aduterants, orgn and processng of the powdered cocane, and the
method of convertng the base. It ranges from a crumby texture, sometmes
extremey oy, to a hard, amost crystane nature.
Forms
Sats
Cocane s a weaky akane compound (an "akaod"), and can therefore
combne wth acdc compounds to form varous sats. The hydrochorde (HC)
sat of cocane s by far the most commony encountered, athough the
sufate (-SO4) and the ntrate (-NO3) are occasonay seen. Dfferent sats
dssove to a greater or esser extent n varous sovents - the hydrochorde
sat s poar n character and s qute soube n water.
Basc
Man artce: Freebase (chemstry)
As the name mpes, "freebase" s the base form of cocane, as opposed to
the sat form. It s practcay nsoube n water whereas hydrochorde sat s
water soube.
Smokng freebase cocane has the addtona effect of reeasng
methyecgondne nto the user's system due to the pyroyss of the
substance (a sde effect whch nsuffatng or n|ectng powder cocane does
not create). Some research suggests that smokng freebase cocane can be
even more cardotoxc than other routes of admnstraton|41| because of
methyecgondne's effects on ung tssue|42| and ver tssue.|43|
Pure cocane s prepared by neutrazng ts compoundng sat wth an akane
souton whch w precptate to non-poar basc cocane. It s further refned
through aqueous-sovent Lqud-qud extracton.
Crack cocane
Man artce: Crack cocane
A woman smokng crack cocane
Crack s a ower purty form of free-base cocane that s usuay produced by
neutrazaton of cocane hydrochorde wth a souton of bakng soda (sodum
bcarbonate, NaHCO3) and water, producng a very hard/brtte, off-whte-to-
brown coored, amorphous matera that contans sodum carbonate,
entrapped water, and other by-products as the man mpurtes.
The "freebase" and "crack" forms of cocane are usuay admnstered by
vaporzaton of the powdered substance nto smoke, whch s then nhaed.
|44| The orgn of the name "crack" comes from the "crackng" sound (and
hence the onomatopoec monker "crack") that s produced when the cocane
and ts mpurtes (.e. water, sodum bcarbonate) are heated past the pont
of vaporzaton.|45| Pure cocane base/crack can be smoked because t
vaporzes smoothy, wth tte or no decomposton at 98 C (208 F),|46|
whch s beow the bong pont of water. The smoke produced from cocane
base s usuay descrbed as havng a very dstnctve, peasant taste.
In contrast, cocane hydrochorde does not vaporze unt heated to a much
hgher temperature (about 197C), and consderabe decomposton/burnng
occurs at these hgh temperatures. Ths effectvey destroys some of the
cocane, and yeds a sharp, acrd, and fou-tastng smoke.
Smokng or vaporzng cocane and nhang t nto the ungs produces an
amost mmedate "hgh" that can be very powerfu (and addctng) qute
rapdy - ths nta crescendo of stmuaton s known as a "rush". Whe the
stmuatng effects may ast for hours, the euphorc sensaton s very bref,
promptng the user to smoke more mmedatey.
Coca eaf nfusons
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Coca herba nfuson (aso referred to as coca tea) s used n coca-eaf
producng countres much as any herba medcna nfuson woud esewhere
n the word. The free and ega commercazaton of dred coca eaves under
the form of ftraton bags to be used as "coca tea" has been actvey
promoted by the governments of Peru and Bova for many years as a drnk
havng medcna powers. Vstors to the cty of Cuzco n Peru, and La Paz n
Bova are greeted wth the offerng of coca eaf nfusons (prepared n tea
pots wth whoe coca eaves) purportedy to hep the newy arrved traveer
overcome the maase of hgh attude sckness. The effects of drnkng coca
tea are a md stmuaton and mood ft. It does not produce any sgnfcant
numbng of the mouth nor does t gve a rush ke snortng cocane. In order
to prevent the demonzaton of ths product, ts promoters pubcze the
unproven concept that much of the effect of the ngeston of coca eaf
nfuson woud come from the secondary akaods, as beng not ony
quanttatvey dfferent from pure cocane but aso quatatvey dfferent.
It has been promoted as an ad|uvant for the treatment of cocane
dependence. In one controversa study, coca eaf nfuson was used -n
addton to counseng- to treat 23 addcted coca-paste smokers n Lma, Peru.
Reapses fe from an average of four tmes per month before treatment wth
coca tea to one durng the treatment. The duraton of abstnence ncreased
from an average of 32 days pror to treatment to 217 days durng treatment.
These resuts suggest that the admnstraton of coca eaf nfuson pus
counseng woud be an effectve method for preventng reapse durng
treatment for cocane addcton. Importanty, these resuts aso suggest
strongy that the prmary pharmacoogcay actve metabote n coca eaf
nfusons s actuay cocane and not the secondary akaods.
The cocane metabote benzoyecgonne can be detected n the urne of
peope a few hours after drnkng one cup of coca eaf nfuson.
Routes of admnstraton
Ora
A spoon contanng bakng soda, cocane, and a sma amount of water. Used
n a "poor-man's" crack-cocane producton
Many users rub the powder aong the gum ne, or onto a cgarette fter
whch s then smoked, whch numbs the gums and teeth - hence the
cooqua names of "numbes", "gummers" or "cocoa puffs" for ths type of
admnstraton. Ths s mosty done wth the sma amounts of cocane
remanng on a surface after nsuffaton. Another ora method s to wrap up
some cocane n rong paper and swaow (parachute) t. Ths s sometmes
caed a "snow bomb."
Coca eaf
Coca eaves are typcay mxed wth an akane substance (such as me) and
chewed nto a wad that s retaned n the mouth between gum and cheek
(much n the same as chewng tobacco s chewed) and sucked of ts |uces.
The |uces are absorbed sowy by the mucous membrane of the nner cheek
and by the gastrontestna tract when swaowed. Aternatvey, coca eaves
can be nfused n qud and consumed ke tea. Ingestng coca eaves
generay s an neffcent means of admnsterng cocane. Advocates of the
consumpton of the coca eaf state that coca eaf consumpton shoud not be
crmnazed as t s not actua cocane, and consequenty t s not propery the
ct drug. Because cocane s hydroyzed and rendered nactve n the acdc
stomach, t s not ready absorbed when ngested aone. Ony when mxed
wth a hghy akane substance (such as me) can t be absorbed nto the
boodstream through the stomach. The effcency of absorpton of oray
admnstered cocane s mted by two addtona factors. Frst, the drug s
party catabozed by the ver. Second, capares n the mouth and
esophagus constrct after contact wth the drug, reducng the surface area
over whch the drug can be absorbed. Nevertheess, cocane metabotes can
be detected n the urne of sub|ects that have spped even one cup of coca
eaf nfuson. Therefore, ths s an actua addtona form of admnstraton of
cocane, abet an neffcent one.
Oray admnstered cocane takes approxmatey 30 mnutes to enter the
boodstream. Typcay, ony a thrd of an ora dose s absorbed, athough
absorpton has been shown to reach 60% n controed settngs. Gven the
sow rate of absorpton, maxmum physoogca and psychotropc effects are
attaned approxmatey 60 mnutes after cocane s admnstered by
ngeston. Whe the onset of these effects s sow, the effects are sustaned
for approxmatey 60 mnutes after ther peak s attaned.
Contrary to popuar beef, both ngeston and nsuffaton resut n
approxmatey the same proporton of the drug beng absorbed: 30 to 60%.
Compared to ngeston, the faster absorpton of nsuffated cocane resuts n
qucker attanment of maxmum drug effects. Snortng cocane produces
maxmum physoogca effects wthn 40 mnutes and maxmum psychotropc
effects wthn 20 mnutes, however, a more reastc actvaton perod s coser
to 5 to 10 mnutes, whch s smar to ngeston of cocane. Physoogca and
psychotropc effects from nasay nsuffated cocane are sustaned for
approxmatey 40-60 mnutes after the peak effects are attaned.|47|
Coca tea, an nfuson of coca eaves, s aso a tradtona method of
consumpton. The tea has often been recommended for traveers n the
Andes to prevent attude sckness.|48| However, ts actua effectveness has
never been systematcay studed.|48| Ths method of consumpton has been
practced for many centures by the natve trbes of South Amerca. One
specfc purpose of ancent coca eaf consumpton was to ncrease energy and
reduce fatgue n messengers who made mut-day quests to other
settements.
In 1986 an artce n the |ourna of the Amercan Medca Assocaton reveaed
that U.S. heath food stores were seng dred coca eaves to be prepared as
an nfuson as "Heath Inca Tea."|49| Whe the packagng camed t had been
"decocanzed," no such process had actuay taken pace. The artce stated
that drnkng two cups of the tea per day gave a md stmuaton, ncreased
heart rate, and mood eevaton, and the tea was essentay harmess.
Despte ths, the DEA sezed severa shpments n Hawa, Chcago, Inos,
Georga, and severa ocatons on the East Coast of the Unted States, and the
product was removed from the sheves.
Insuffaton
A man snffng cocane
Nasa nsuffaton (known cooquay as "snortng," "snffng," or "bowng") s
the most common method of ngeston of recreatona powdered cocane n
the Western word. The drug coats and s absorbed through the mucous
membranes nng the snuses. When nsuffatng cocane, absorpton through
the nasa membranes s approxmatey 30-60%, wth hgher doses eadng to
ncreased absorpton effcency. Any matera not drecty absorbed through
the mucous membranes s coected n mucus and swaowed (ths "drp" s
consdered peasant by some and unpeasant by others). In a study|50| of
cocane users, the average tme taken to reach peak sub|ectve effects was
14.6 mnutes. Any damage to the nsde of the nose s because cocane hghy
constrcts bood vesses - and therefore bood and oxygen/nutrent fow - to
that area. Nosebeeds after cocane nsuffaton are due to rrtaton and
damage of mucus membranes by foregn partces and aduterants and not
the cocane tsef; as a vasoconstrctor, cocane acts to reduce beedng.
Pror to nsuffaton, cocane powder must be dvded nto very fne partces.
Cocane of hgh purty breaks nto fne dust very easy, except when t s
most (not we stored) and forms "chunks," whch reduces the effcency of
nasa absorpton.
Roed up banknotes, hoowed-out pens, cut straws, ponted ends of keys,
specazed spoons, ong fngernas, and (cean) tampon appcators are often
used to nsuffate cocane. Such devces are often caed "tooters" by users.
The cocane typcay s poured onto a fat, hard surface (such as a mrror, CD
case or book) and dvded nto "bumps", "nes" or "ras", and then
nsuffated.|51| The amount of cocane n a ne vares wdey from person to
person and occason to occason (the purty of the cocane s aso a factor),
but one ne s generay consdered to be a snge dose and s typcay 35 mg
(a "bump") to 100 mg (a "ra")|dubous - dscuss|. As toerance buds rapdy
n the short-term (hours), many nes are often snorted to produce greater
effects.
A study by Bonkovsky and Mehta|52| reported that, |ust ke shared needes,
the sharng of straws used to "snort" cocane can spread bood dseases such
as Hepatts C.
In|ecton
Drug n|ecton provdes the hghest bood eves of drug n the shortest
amount of tme. Sub|ectve effects not commony shared wth other methods
of admnstraton ncude a rngng n the ears moments after n|ecton
(usuay when n excess of 120 mgrams) astng 2 to 5 mnutes ncudng
tnntus & audo dstorton. Ths s cooquay referred to as a "be rnger".
|53| In a study|50| of cocane users, the average tme taken to reach peak
sub|ectve effects was 3.1 mnutes. The euphora passes qucky. Asde from
the toxc effects of cocane, there s aso danger of crcuatory embo from
the nsoube substances that may be used to cut the drug. As wth a
n|ected ct substances, there s a rsk of the user contractng bood-borne
nfectons f stere n|ectng equpment s not avaabe or used. Addtonay,
because cocane s a vasoconstrctor, and usage often entas mutpe
n|ectons wthn severa hours or ess, subsequent n|ectons are
progressvey more dffcut to admnster, whch n turn may ead to more
n|ecton attempts and more sequeae from mpropery performed n|ecton.
An n|ected mxture of cocane and heron, known as "speedba" s a
partcuary dangerous combnaton, as the converse effects of the drugs
actuay compement each other, but may aso mask the symptoms of an
overdose. It has been responsbe for numerous deaths, ncudng ceebrtes
such as |ohn Beush, Chrs Farey, Mtch Hedberg, Rver Phoenx and Layne
Staey.
Expermentay, cocane n|ectons can be devered to anmas such as frut
fes to study the mechansms of cocane addcton.|54|
Inhaaton
See aso: Crack cocane
Inhaaton or smokng s one of the severa means cocane s admnstered.
Cocane s smoked by nhang the vapor by submatng sod cocane by
heatng.|55| In a 2000 Brookhaven Natona Laboratory medca department
study, based on sef reports of 32 abusers who partcpated n the
study,"peak hgh" was found at mean of 1.4mn +/- 0.5 mnutes.|50|
Smokng freebase or crack cocane s most often accompshed usng a ppe
made from a sma gass tube, often taken from "Love roses," sma gass
tubes wth a paper rose that are promoted as romantc gfts.|56| These are
sometmes caed "stems", "horns", "basters" and "straght shooters". A sma
pece of cean heavy copper or occasonay staness stee scourng pad -
often caed a "bro" (actua Bro pads contan soap, and are not used), or
"chore", named for Chore Boy brand copper scourng pads, - serves as a
reducton base and fow moduator n whch the "rock" can be meted and
boed to vapor. Crack smokers aso sometmes smoke through a soda can
wth sma hoes n the bottom.
Crack s smoked by pacng t at the end of the ppe; a fame hed cose to t
produces vapor, whch s then nhaed by the smoker. The effects, fet amost
mmedatey after smokng, are very ntense and do not ast ong - usuay 5
to 15 mnutes.
When smoked, cocane s sometmes combned wth other drugs, such as
cannabs, often roed nto a |ont or bunt. Powdered cocane s aso
sometmes smoked, though heat destroys much of the chemca; smokers
often sprnke t on cannabs.
The anguage referrng to paraphernaa and practces of smokng cocane
vary, as do the packagng methods n the street eve sae.
Suppostory
Ltte research has been focused on the suppostory (ana or vagna nserton)
method of admnstraton, aso known as "puggng". Ths method of
admnstraton s commony admnstered usng an ora syrnge. Cocane can
be dssoved n water and wthdrawn nto an ora syrnge whch may then be
ubrcated and nserted nto the anus or vagna before the punger s pushed.
Anecdota evdence of ts effects are nfrequenty dscussed, possby due to
soca taboos n many cutures. The rectum and the vagna cana s where the
ma|orty of the drug woud key be taken up, through the membranes nng
ts was.|ctaton needed|
Mechansm of acton
Cocane bnds drecty to the DAT1 transporter, nhbtng reuptake wth more
effcacy than amphetamnes whch phosphoryate t causng nternazaton;
nstead prmary reeasng DAT (whch cocane does not do) and ony
nhbtng ts reuptake as a secondary, and much more mnor, mode of acton
than cocane and n another manner: from the opposte
conformaton/orentaton to DAT.
The pharmacodynamcs of cocane nvove the compex reatonshps of
neurotransmtters (nhbtng monoamne uptake n rats wth ratos of about:
serotonn:dopamne = 2:3, serotonn:norepnephrne = 2:5|57|) The most
extensvey studed effect of cocane on the centra nervous system s the
bockade of the dopamne transporter proten. Dopamne transmtter reeased
durng neura sgnang s normay recyced va the transporter; .e., the
transporter bnds the transmtter and pumps t out of the synaptc ceft back
nto the presynaptc neuron, where t s taken up nto storage vesces.
Cocane bnds tghty at the dopamne transporter formng a compex that
bocks the transporter's functon. The dopamne transporter can no onger
perform ts reuptake functon, and thus dopamne accumuates n the
synaptc ceft. Ths resuts n an enhanced and proonged postsynaptc effect
of dopamnergc sgnang at dopamne receptors on the recevng neuron.
Proonged exposure to cocane, as occurs wth habtua use, eads to
homeostatc dysreguaton of norma (.e. wthout cocane) dopamnergc
sgnang va down-reguaton of dopamne receptors and enhanced sgna
transducton. The decreased dopamnergc sgnang after chronc cocane use
may contrbute to depressve mood dsorders and senstze ths mportant
bran reward crcut to the renforcng effects of cocane (for exampe,
enhanced dopamnergc sgnang ony when cocane s sef-admnstered).
Ths senstzaton contrbutes to the ntractabe nature of addcton and
reapse.
Dopamne-rch bran regons such as the ventra tegmenta area, nuceus
accumbens, and prefronta cortex are frequent targets of cocane addcton
research. Of partcuar nterest s the pathway consstng of dopamnergc
neurons orgnatng n the ventra tegmenta area that termnate n the
nuceus accumbens. Ths pro|ecton may functon as a "reward center", n
that t seems to show actvaton n response to drugs of abuse ke cocane n
addton to natura rewards ke food or sex.|58| Whe the precse roe of
dopamne n the sub|ectve experence of reward s hghy controversa
among neuroscentsts, the reease of dopamne n the nuceus accumbens s
wdey consdered to be at east partay responsbe for cocane's rewardng
effects. Ths hypothess s argey based on aboratory data nvovng rats that
are traned to sef-admnster cocane. If dopamne antagonsts are nfused
drecty nto the nuceus accumbens, we-traned rats sef-admnsterng
cocane w undergo extncton (.e. ntay ncrease respondng ony to stop
competey) thereby ndcatng that cocane s no onger renforcng (.e.
rewardng) the drug-seekng behavor.
Cocane's effects on serotonn (5-hydroxytryptamne, 5-HT) show across
mutpe serotonn receptors, and s shown to nhbt the re-uptake of 5-HT3
specfcay as an mportant contrbutor to the effects of cocane. The
overabundance of 5-HT3 receptors n cocane condtoned rats dspay ths
trat, however the exact effect of 5-HT3 n ths process s uncear.|59| The 5-
HT2 receptor (partcuary the subtypes 5-HT2AR, 5-HT2BR and 5-HT2CR)
show nfuence n the evocaton of hyperactvty dspayed n cocane use.|60|
In addton to the mechansm shown on the above chart, cocane has been
demonstrated to bnd as to drecty stabze the DAT transporter on the open
outward-facng conformaton whereas other stmuants (namey
phenethyamnes) stabze the cosed conformaton. Further, cocane bnds n
such a way as to nhbt a hydrogen bond nnate to DAT that otherwse st
forms when amphetamne and smar moecues are bound. Cocane's
bndng propertes are such that t attaches so ths hydrogen bond w not
form and s bocked from formaton due to the tghty ocked orentaton of the
cocane moecue. Research studes have suggested that the affnty for the
transporter s not what s nvoved n habtuaton of the substance so much as
the conformaton and bndng propertes to where & how on the transporter
the moecue bnds.|61|
Sgma receptors are affected by cocane, as cocane functons as a sgma
gand agonst.|62| Further specfc receptors t has been demonstrated to
functon on are NMDA and the D1 dopamne receptor.|63|
Cocane aso bocks sodum channes, thereby nterferng wth the
propagaton of acton potentas;|7| thus, ke gnocane and novocane, t
acts as a oca anesthetc. It aso functons on the bndng stes to the
dopamne and serotonn sodum dependent transport area as targets as
separate mechansms from ts reuptake of those transporters; unque to ts
oca anesthetc vaue whch makes t n a cass of functonaty dfferent from
both ts own derved phenytropanes anaogues whch have that removed and
the amphetamne cass of stmuants whch as we atogether ack that. In
addton to ths cocane has some target bndng to the ste of the Kappa-
opod receptor as we.|64| Cocane aso causes vasoconstrcton, thus
reducng beedng durng mnor surgca procedures. The ocomotor
enhancng propertes of cocane may be attrbutabe to ts enhancement of
dopamnergc transmsson from the substanta ngra. Recent research ponts
to an mportant roe of crcadan mechansms|65| and cock genes|66| n
behavora actons of cocane.
Because ncotne ncreases the eves of dopamne n the bran, many cocane
users fnd that consumpton of tobacco products durng cocane use enhances
the euphora. Ths, however, may have undesrabe consequences, such as
uncontroabe chan smokng durng cocane use (even users who do not
normay smoke cgarettes have been known to chan smoke when usng
cocane), n addton to the detrmenta heath effects and the addtona
stran on the cardovascuar system caused by tobacco.
Cocane can often cause reduced food ntake, many chronc users ose ther
appette and can experence severe manutrton and sgnfcant weght oss.
Cocane effects, further, are shown to be potentated for the user when used
n con|uncton wth new surroundngs and stmu, and otherwse nove
envrons.|67|
Metabosm and excreton
Cocane s extensvey metabozed, prmary n the ver, wth ony about 1%
excreted unchanged n the urne. The metabosm s domnated by hydroytc
ester ceavage, so the emnated metabotes consst mosty of
benzoyecgonne (BE), the ma|or metabote, and other sgnfcant
metabotes n esser amounts such as ecgonne methy ester (EME) and
ecgonne. Further mnor metabotes of cocane ncude norcocane, p-
hydroxycocane, m-hydroxycocane, p-hydroxybenzoyecgonne (pOHBE), and
m-hydroxybenzoyecgonne.|68|
Dependng on ver and kdney functon, cocane metabotes are detectabe
n urne. Benzoyecgonne can be detected n urne wthn four hours after
cocane ntake and remans detectabe n concentratons greater than 150
ng/mL typcay for up to eght days after cocane s used. Detecton of
accumuaton of cocane metabotes n har s possbe n reguar users unt
the sectons of har grown durng use are cut or fa out.
If consumed wth acoho, cocane combnes wth acoho n the ver to form
cocaethyene. Studes have suggested cocaethyene s both more
euphorgenc, and has a hgher cardovascuar toxcty than cocane by tsef.
|69||70||71|
A study n mce has suggested that capsacn found n pepper spray may
nteract wth cocane wth potentay fata consequences. The method
through whch they woud nteract however, s not known.|72||73|
Detecton n boogca fuds
Cocane and ts ma|or metabotes may be quanttated n bood, pasma or
urne to montor for abuse, confrm a dagnoss of posonng or assst n the
forensc nvestgaton of a traffc or other crmna voaton or a sudden
death. Most commerca cocane mmunoassay screenng tests cross-react
apprecaby wth the ma|or cocane metabotes, but chromatographc
technques can easy dstngush and separatey measure each of these
substances. When nterpretng the resuts of a test, t s mportant to consder
the cocane usage hstory of the ndvdua, snce a chronc user can deveop
toerance to doses that woud ncapactate a cocane-nave ndvdua, and the
chronc user often has hgh basene vaues of the metabotes n hs system.
Cautous nterpretaton of testng resuts may aow a dstncton between
passve or actve usage, and between smokng versus other routes of
admnstraton.|74| In 2011, researchers at |ohn |ay Coege of Crmna
|ustce reported that detary znc suppements can mask the presence of
cocane and other drugs n urne. Smar cams have been made n web
forums on that topc.|75|
Loca anesthetc
Cocane was hstorcay usefu as a topca anesthetc n eye and nasa
surgery, athough t s now predomnanty used for nasa and acrma duct
surgery. The ma|or dsadvantages of ths use are cocane's ntense
vasoconstrctor actvty and potenta for cardovascuar toxcty. Cocane has
snce been argey repaced n Western medcne by synthetc oca
anesthetcs such as benzocane, proparacane, gnocane/xyocane/docane,
and tetracane though t remans avaabe for use f specfed. If
vasoconstrcton s desred for a procedure (as t reduces beedng), the
anesthetc s combned wth a vasoconstrctor such as phenyephrne or
epnephrne. In Austraa t s currenty prescrbed for use as a oca anesthetc
for condtons such as mouth and ung ucers. Some ENT specasts
occasonay use cocane wthn the practce when performng procedures
such as nasa cauterzaton. In ths scenaro dssoved cocane s soaked nto a
ba of cotton woo, whch s paced n the nostr for the 10-15 mnutes
mmedatey before the procedure, thus performng the dua roe of both
numbng the area to be cauterzed, and vasoconstrcton. Even when used
ths way, some of the used cocane may be absorbed through ora or nasa
mucosa and gve systemc effects.
In 2005, researchers from Kyoto Unversty Hospta proposed the use of
cocane n con|uncton wth phenyephrne admnstered n the form of an eye
drop as a dagnostc test for Parknson's dsease.|76|
Hstory
Dscovery
Coca eaf n Bova
For over a thousand years South Amercan ndgenous peopes have chewed
the eaves of Erythroxyon coca, a pant that contans vta nutrents as we
as numerous akaods, ncudng cocane. The coca eaf was, and st s,
chewed amost unversay by some ndgenous communtes. The remans of
coca eaves have been found wth ancent Peruvan mummes, and pottery
from the tme perod depcts humans wth buged cheeks, ndcatng the
presence of somethng on whch they are chewng.|77| There s aso evdence
that these cutures used a mxture of coca eaves and sava as an anesthetc
for the performance of trepanaton.|78|
When the Spansh arrved n South Amerca, most at frst gnored aborgna
cams that the eaf gave them strength and energy, and decared the
practce of chewng t the work of the Dev.|ctaton needed| But after
dscoverng that these cams were true, they egazed and taxed the eaf,
takng 10% off the vaue of each crop.|79| In 1569, Ncos Monardes
descrbed the practce of the natves of chewng a mxture of tobacco and
coca eaves to nduce "great contentment":
When they wshed to make themseves drunk and out of |udgment they
chewed a mxture of tobacco and coca eaves whch make them go as they
were out of ther wttes.
-|80|
In 1609, Padre Bas Vaera wrote:
Coca protects the body from many aments, and our doctors use t n
powdered form to reduce the sweng of wounds, to strengthen broken
bones, to expe cod from the body or prevent t from enterng, and to cure
rotten wounds or sores that are fu of maggots. And f t does so much for
outward aments, w not ts snguar vrtue have even greater effect n the
entras of those who eat t?|ctaton needed|
Isoaton and namng
Athough the stmuant and hunger-suppressant propertes of coca had been
known for many centures, the soaton of the cocane akaod was not
acheved unt 1855. Varous European scentsts had attempted to soate
cocane, but none had been successfu for two reasons: the knowedge of
chemstry requred was nsuffcent at the tme.|ctaton needed| Addtonay
contemporary condtons of sea-shppng from South Amerca coud degrade
the cocane n the pant sampes avaabe to Europeans.|ctaton needed|
The cocane akaod was frst soated by the German chemst Fredrch
Gaedcke n 1855. Gaedcke named the akaod "erythroxyne", and pubshed
a descrpton n the |ourna Archv der Pharmaze.|81|
In 1856, Fredrch Wher asked Dr. Car Scherzer, a scentst aboard the
Novara (an Austran frgate sent by Emperor Franz |oseph to crce the gobe),
to brng hm a arge amount of coca eaves from South Amerca. In 1859, the
shp fnshed ts traves and Wher receved a trunk fu of coca. Wher
passed on the eaves to Abert Nemann, a Ph.D. student at the Unversty of
Gttngen n Germany, who then deveoped an mproved purfcaton process.
|82|
Nemann descrbed every step he took to soate cocane n hs dssertaton
tted ber ene neue organsche Base n den Cocabttern (On a New Organc
Base n the Coca Leaves), whch was pubshed n 1860-t earned hm hs
Ph.D. and s now n the Brtsh Lbrary. He wrote of the akaod's "coouress
transparent prsms" and sad that, "Its soutons have an akane reacton, a
btter taste, promote the fow of sava and eave a pecuar numbness,
foowed by a sense of cod when apped to the tongue." Nemann named the
akaod "cocane" from "coca" (from Ouechua "cuca") + suffx "ne".|82||83|
Because of ts use as a oca anesthetc, a suffx "-cane" was ater extracted
and used to form names of synthetc oca anesthetcs.
The frst synthess and eucdaton of the structure of the cocane moecue
was by Rchard Wsttter n 1898.|29| The synthess started from tropnone,
a reated natura product and took fve steps.
Medcazaton
"Cocane toothache drops", 1885 advertsement of cocane for denta pan n
chdren
Advertsement n the |anuary 1896 ssue of McCure's Magazne for Burnett's
Cocane "for the har".
Wth the dscovery of ths new akaod, Western medcne was quck to
expot the possbe uses of ths pant.
In 1879, Vass von Anrep, of the Unversty of Wrzburg, devsed an
experment to demonstrate the anagesc propertes of the newy dscovered
akaod. He prepared two separate |ars, one contanng a cocane-sat
souton, wth the other contanng merey sat water. He then submerged a
frog's egs nto the two |ars, one eg n the treatment and one n the contro
souton, and proceeded to stmuate the egs n severa dfferent ways. The
eg that had been mmersed n the cocane souton reacted very dfferenty
from the eg that had been mmersed n sat water.|84|
Kar Koer (a cose assocate of Sgmund Freud, who woud wrte about
cocane ater) expermented wth cocane for ophthamc usage. In an
nfamous experment n 1884, he expermented upon hmsef by appyng a
cocane souton to hs own eye and then prckng t wth pns. Hs fndngs
were presented to the Hedeberg Ophthamoogca Socety. Aso n 1884,
|enek demonstrated the effects of cocane as a respratory system
anesthetc. In 1885, Wam Hasted demonstrated nerve-bock anesthesa,
|85| and |ames Leonard Cornng demonstrated perdura anesthesa.|86|
1898 saw Henrch Ouncke use cocane for spna anesthesa.
Today, cocane has very mted medca use. See the secton Cocane as a
oca anesthetc
Popuarzaton
Pope Leo XIII purportedy carred a hpfask of the coca-treated Vn Maran
wth hm, and awarded a Vatcan god meda to Angeo Maran.|87|
In 1859, an Itaan doctor, Paoo Mantegazza, returned from Peru, where he
had wtnessed frst-hand the use of coca by the natves. He proceeded to
experment on hmsef and upon hs return to Man he wrote a paper n whch
he descrbed the effects. In ths paper he decared coca and cocane (at the
tme they were assumed to be the same) as beng usefu medcnay, n the
treatment of "a furred tongue n the mornng, fatuence, and whtenng of the
teeth."
A chemst named Angeo Maran who read Mantegazza's paper became
mmedatey ntrgued wth coca and ts economc potenta. In 1863, Maran
started marketng a wne caed Vn Maran, whch had been treated wth
coca eaves, to become cocawne. The ethano n wne acted as a sovent and
extracted the cocane from the coca eaves, aterng the drnk's effect. It
contaned 6 mg cocane per ounce of wne, but Vn Maran whch was to be
exported contaned 7.2 mg per ounce, to compete wth the hgher cocane
content of smar drnks n the Unted States. A "pnch of coca eaves" was
ncuded n |ohn Styth Pemberton's orgna 1886 recpe for Coca-Coa, though
the company began usng decocanzed eaves n 1906 when the Pure Food
and Drug Act was passed. The actua amount of cocane that Coca-Coa
contaned durng the frst 20 years of ts producton s practcay mpossbe
to determne.|ctaton needed|
In 1879 cocane began to be used to treat morphne addcton. Cocane was
ntroduced nto cnca use as a oca anesthetc n Germany n 1884, about
the same tme as Sgmund Freud pubshed hs work ber Coca, n whch he
wrote that cocane causes:
Exharaton and astng euphora, whch n no way dffers from the norma
euphora of the heathy person. You perceve an ncrease of sef-contro and
possess more vtaty and capacty for work. In other words, you are smpy
norma, and t s soon hard to beeve you are under the nfuence of any
drug. Long ntensve physca work s performed wthout any fatgue. Ths
resut s en|oyed wthout any of the unpeasant after-effects that foow
exharaton brought about by acoho. Absoutey no cravng for the further
use of cocane appears after the frst, or even after repeated takng of the
drug.
In 1885 the U.S. manufacturer Parke-Davs sod cocane n varous forms,
ncudng cgarettes, powder, and even a cocane mxture that coud be
n|ected drecty nto the user's vens wth the ncuded neede. The company
promsed that ts cocane products woud "suppy the pace of food, make the
coward brave, the sent eoquent and render the sufferer nsenstve to pan."
By the ate Vctoran era cocane use had appeared as a vce n terature. For
exampe, t was n|ected by Arthur Conan Doye's fctona Sherock Homes,
generay to offset the boredom he fet when he was not workng on a case.
In eary 20th-century Memphs, Tennessee, cocane was sod n neghborhood
drugstores on Beae Street, costng fve or ten cents for a sma boxfu.
Stevedores aong the Msssspp Rver used the drug as a stmuant, and
whte empoyers encouraged ts use by back aborers.|88|
In 1909, Ernest Shacketon took "Forced March" brand cocane tabets to
Antarctca, as dd Captan Scott a year ater on hs -fated |ourney to the
South Poe.|89|
Durng the md-1940s, amdst WWII, cocane was consdered for ncuson as
an ngredent of a future generaton of 'pep ps' for the German mtary code
named D-IX.|90|
Prohbton
See aso: Lega status of cocane
Gobe con.
The exampes and perspectve n ths secton dea prmary wth the Unted
States and do not represent a wordwde vew of the sub|ect. Pease mprove
ths artce and dscuss the ssue on the tak page. (August 2012)
Prosttutes buy cocane capsues from a drug deaer n Bern, 1924
Prohbton of cocane n the Unted States
See aso: Cocane n the Unted States
Cas for prohbton began ong before the Harrson Act was passed by
Congress n 1914 - a aw requrng cocane and narcotcs to be dspensed
ony wth a doctor's order.|91| Before ths, varous factors and groups acted
on prmary a state eve nfuencng a move towards prohbton and away
from a assez-fare atttude.|92|
By 1903 cocane consumpton had grown to about fve tmes that of 1890.
Non-medca users accounted for amost the entre ncrease as cocane-users
extended outsde the mdde-aged, whte, professona cass. Cocane became
assocated wth aborers, youths, backs and the urban underword.|93|
The popuarzaton of cocane frst began wth aborers who used cocane as a
stmuant to ncrease productvty.|93| Cocane was often supped by
empoyers.|94| Cocane was often supped to Afrcan Amercan workers, who
many empoyers beeved were better physca workers; cocane was thought
to provde added strength and consttuton and accordng to the Medca
News, made backs "mpervous to the extremes of heat and cod."|93|
However, users of cocane qucky acqured a reputaton as dangerous and n
1897, the frst state b of contro for cocane saes came from a mnng
county n Coorado.|95|
The popuarzaton of cocane use was not confned to Afrcan Amercans or
smpe aborers. In Northern ctes, cocane use ncreased amongst poorer
peope - n fact, cocane was often cheaper than acoho.|94| In the Northeast
n partcuar, cocane became popuar amongst workers n factores, texte
ms and on ra roads.|96| In some nstances, cocane use suppemented or
repaced caffene as the drug-of-choce to keep workers awake and workng
overtme.|96|
Ths perod of ncreasng cocane use foowed wth ncreasng fears that
young chdren were beng preyed upon and forced nto cocane addcton.
|97| Indeed, t was even thought that cocane was used to seduce young grs
away from ther homes and cause them to be addcted and dependent upon
the substance and therefore fa prey to an nescapabe cyce of prosttuton.
|98| Fears of the corrupton of the youth by cocane were popuar and
wdespread but there s tte evdence to support ther veracty.|97|
Manstream meda reported cocane epdemcs as eary as 1894 n Daas,
Texas. Reports of the cocane epdemc woud foreshadow a famar theme n
ater so-caed epdemcs, namey that cocane presented a soca threat more
dangerous than smpe heath effects and had nsdous resuts when used by
backs and members of the ower cass. Smar anxety-rdden reports
appeared throughout ctes n the South eadng some to decare that "the
cocane habt has assumed the proportons of an epdemc among the coored
peope." In 1900, state egsatures n Aabama, Georga and Tennessee
consdered ant-cocane bs for the frst tme.|99|
Hyperboc reports of the effect of cocane on Afrcan Amercans went hand-
n-hand wth ths hystera. In 1901, the Atanta Consttuton reported that
"Use of the drug |cocane| among negroes s growng to an aarmng
extent."|100| The New York Tmes reported that under the nfuence of
cocane, "sexua desres are ncreased and perverted . peacefu negroes
become quarresome, and tmd negroes deveop a degree of 'Dutch courage'
that s sometmes amost ncredbe."|101| A medca doctor even wrote
"cocane s often the drect ncentve to the crme of rape by the
negroes."|101| To compete the characterzaton, a |udge n Msssspp
decared that suppyng a "negro" wth cocane was more dangerous than
n|ectng a dog wth rabes.|102|
These atttudes not ony nfuenced drug aw and pocy but aso ed to
ncreased voence aganst Afrcan Amercans. In 1906, a ma|or race rot ed
by whtes erupted; t was sparked by reports of crmes commtted by back
cocane fends.|100| Indeed, whte-ed, race rots spawnng from reports of
backs under the nfuence of cocane were not uncommon.|103| Poce n the
South wdey adopted the use of a heaver caber handguns so as to better
stop a cocane-crazed back person - beeved to be empowered wth super-
human strength.|104| Another dangerous myth perpetuated amongst poce
was that cocane mbued Afrcan Amercans wth tremendous accuracy wth
frearms and therefore poce were better advsed to shoot frst n
questonabe crcumstances.|105|
Utmatey pubc opnon rested aganst the cocane user. Crmnaty was
commony beeved to be a natura resut of cocane use.|106| Much of the
nfuence for these knd of perceptons came from the wdespread pubcty
gven to notorous cases.|92| Whe the hstorca reaty of cocanes effect on
voence and crme s dffcut to dsentange from nfamed perceptons, t
does appear that pubc opnon was swayed by the mage of the voent,
cocane-crazed fend and pushed over the edge by a few voent epsodes.
|106| It was an mage of the cocane-user that carred acute raca overtones.
|92|
Before any substantve federa reguaton of cocane, state and oca
muncpates evoked ther own means to reguate cocane. Because of the
nta ack of targeted egsaton, on both federa and state eve, the most
typca strategy by aw enforcement was the appcaton of nusance aws
pertanng to vagrancy and dsturbng the peace.|107| Subsequent egsatve
actons amed at controng the dstrbuton of cocane rather than ts
manufacture.|108| Reformers took ths approach n part because of ega
precedents whch made t easer to contro dstrbutors such as pharmaces;
state and oca boards of hearth or boards of pharmacy often took the pace
of reguatory bodes for controng the dstrbuton of cocane.|108|
Some states took the poston of outrght bannng of a forms of cocane sae;
Georga was the frst to do ths n 1902.|109| A New Oreans ordnance
banned cocane saes as we but eft an -defned excepton for therapeutc
uses.|108| A more common requrement was to restrct the sae of cocane or
mpose abeng requrements. A 1907 Caforna aw mtng sae of cocane
to ony those wth a physcans prescrpton resuted n the arrest of over 50
store owners and cerks n the frst year.|108| A 1913 New York state aw
mted druggsts cocane stocks to under 5 ounces. Labeng requrements
ntay operated on a state eve wth some states even gong so far as to
requre that cocane and cocane-contanng products be abeed as poson.
|110|
Eventuay the federa government stepped n and nsttuted a natona
abeng requrement for cocane and cocane-contanng products through the
Food and Drug Act of 1906.|110| The next mpactfu federa reguaton was
the Harrson Narcotcs Tax Act of 1914. Whe ths act s often seen as the
start of prohbton, the act tsef was not actuay a prohbton on cocane,
but nstead setup a reguatory and censng regme.|91| The Harrson Act dd
not recognze addcton as a treatabe condton and therefore the therapeutc
use of cocane, heron or morphne to such ndvduas was outawed - eadng
the |ourna of Amercan Medcne to remark, "|the addct| s dened the
medca care he urgenty needs, open, above-board sources from whch he
formery obtaned hs drug suppy are cosed to hm, and he s drven to the
underword where he can get hs drug, but of course, surrepttousy and n
voaton of the aw."|111| The Harrson Act eft manufacturers of cocane
untouched so ong as they met certan purty and abeng standards.|112|
Despte that cocane was typcay ega to se and ega outets were more
rare, the quanttes of ega cocane produced decned very tte.|112| Lega
cocane quanttes dd not decrease unt the |ones-Mer Act of 1922 put
serous restrctons on cocane manufactures.|112|
Modern usage
D.C. Mayor Maron Barry captured on a surveance camera smokng crack
cocane durng a stng operaton by the FBI and D.C. Poce.
In many countres, cocane s a popuar recreatona drug. In the Unted
States, the deveopment of "crack" cocane ntroduced the substance to a
generay poorer nner-cty market. Use of the powder form has stayed
reatvey constant, experencng a new heght of use durng the ate 1990s
and eary 2000s n the U.S., and has become much more popuar n the ast
few years n the UK.|ctaton needed||when?|
Cocane use s prevaent across a socoeconomc strata, ncudng age,
demographcs, economc, soca, potca, regous, and vehood.|ctaton
needed|
The estmated U.S. cocane market exceeded $70 bon n street vaue for
the year 2005, exceedng revenues by corporatons such as Starbucks.|113|
|114| There s a tremendous demand for cocane n the U.S. market,
partcuary among those who are makng ncomes affordng uxury spendng,
such as snge aduts and professonas wth dscretonary ncome. Cocanes
status as a cub drug shows ts mmense popuarty among the "party crowd".
In 1995 the Word Heath Organzaton (WHO) and the Unted Natons
Interregona Crme and |ustce Research Insttute (UNICRI) announced n a
press reease the pubcaton of the resuts of the argest goba study on
cocane use ever undertaken. However, a decson by an Amercan
representatve n the Word Heath Assemby banned the pubcaton of the
study, because t seemed to make a case for the postve uses of cocane. An
excerpt of the report strongy confcted wth accepted paradgms, for
exampe "that occasona cocane use does not typcay ead to severe or
even mnor physca or soca probems."|115| In the sxth meetng of the B
commttee the US representatve threatened that "If WHO actvtes reatng
to drugs faed to renforce proven drug contro approaches, funds for the
reevant programs shoud be curtaed". Ths ed to the decson to
dscontnue pubcaton. A part of the study has been recuperated. Avaabe
are profes of cocane use n 20 countres.
It was reported n October 2010 that the use of cocane n Austraa has
doubed snce montorng began n 2003.|116|
A probem wth ega cocane use, especay n the hgher voumes used to
combat fatgue (rather than ncrease euphora) by ong-term users, s the rsk
of effects or damage caused by the compounds used n aduteraton.
Cuttng or "steppng on" the drug s commonpace, usng compounds whch
smuate ngeston effects, such as Novocan (procane) producng temporary
anesthaesa as many users beeve a strong numbng effect s the resut of
strong and/or pure cocane, ephedrne or smar stmuants that are to
produce an ncreased heart rate. The norma aduterants for proft are
nactve sugars, usuay mannto, creatne or gucose, so ntroducng actve
aduterants gves the uson of purty and to 'stretch' or make t so a deaer
can se more product than wthout the aduterants.|ctaton needed| The
aduterant of sugars therefore aows the deaer to se the product for a
hgher prce because of the uson of purty and aows to se more of the
product at that hgher prce, enabng deaers to make a ot of revenue wth
tte cost of the aduterants. Cocane tradng carres arge penates n most
|ursdctons, so user decepton about purty and consequent hgh profts for
deaers are the norm.|orgna research?| A study by the European Montorng
Centre for Drugs and Drug Addcton n 2007 showed that the purty eves for
street purchased cocane was often under 5% and on average under 50%
pure.|117|
Socety and cuture
Lega status
Man artce: Lega status of cocane
The producton, dstrbuton and sae of cocane products s restrcted (and
ega n most contexts) n most countres as reguated by the Snge
Conventon on Narcotc Drugs, and the Unted Natons Conventon Aganst
Ict Traffc n Narcotc Drugs and Psychotropc Substances. In the Unted
States the manufacture, mportaton, possesson, and dstrbuton of cocane
s addtonay reguated by the 1970 Controed Substances Act.
Some countres, such as Peru and Bova permt the cutvaton of coca eaf
for tradtona consumpton by the oca ndgenous popuaton, but
nevertheess prohbt the producton, sae and consumpton of cocane. In
addton, some parts of Europe and Austraa aow processed cocane for
medcna uses ony.
Interdcton
In 2004, accordng to the Unted Natons, 589 tonnes of cocane were sezed
gobay by aw enforcement authortes. Coomba sezed 188 t, the Unted
States 166 t, Europe 79 t, Peru 14 t, Bova 9 t, and the rest of the word 133
t.|118|
Ict trade
Because of the extensve processng t undergoes durng preparaton, cocane
s generay treated as a 'hard drug', wth severe penates for possesson and
traffckng. Demand remans hgh, and consequenty back market cocane s
qute expensve. Unprocessed cocane, such as coca eaves, are occasonay
purchased and sod, but ths s exceedngy rare as t s much easer and more
proftabe to concea and smugge t n powdered form. The scae of the
market s mmense: 770 tonnes tmes $100 per gram reta = up to $77
bon.|ctaton needed|
Producton
Unt 2012, Coomba was the word's eadng producer of cocane.|119||120|
Three-quarters of the word's annua yed of cocane has been produced n
Coomba, both from cocane base mported from Peru (prmary the Huaaga
Vaey) and Bova, and from ocay grown coca. There was a 28% ncrease
from the amount of potentay harvestabe coca pants whch were grown n
Coomba n 1998. Ths, combned wth crop reductons n Bova and Peru,
made Coomba the naton wth the argest area of coca under cutvaton
after the md-1990s. Coca grown for tradtona purposes by ndgenous
communtes, a use whch s st present and s permtted by Coomban aws,
ony makes up a sma fragment of tota coca producton, most of whch s
used for the ega drug trade.
An ntervew wth a coca farmer pubshed n 2003 descrbed a mode of
producton by acd-base extracton that has changed tte snce 1905.
Roughy 625 pounds of eaves were harvested per hectare, sx tmes per year.
The eaves were dred for haf a day, then chopped nto sma peces wth a
strmmer and sprnked wth a sma amount of powdered cement (repacng
sodum carbonate from former tmes). Severa hundred pounds of ths
mxture was soaked n 50 US gaons (190 L) of gasone for a day, then the
gasone was removed and the eaves were pressed for remanng qud, after
whch they coud be dscarded. Then battery acd (weak sufurc acd) was
used, one bucket per 25 kg (55 b) of eaves, to create a phase separaton n
whch the cocane free base n the gasone was acdfed and extracted nto a
few buckets of "murky-ookng smey qud". Once powdered caustc soda
was added to ths, the cocane precptated and coud be removed by
ftraton through a coth. The resutng matera, when dred, was termed
pasta and sod by the farmer. The 3750 pound yeary harvest of eaves from a
hectare produced 2.5 kg (6 b) of pasta, approxmatey 40-60% cocane.
Repeated recrystazaton from sovents, producng pasta avada and
eventuay crystane cocane, were performed at specazed aboratores
after the sae.|121|
Attempts to eradcate coca feds through the use of defoants have
devastated part of the farmng economy n some coca growng regons of
Coomba, and strans appear to have been deveoped that are more resstant
or mmune to ther use. Whether these strans are natura mutatons or the
product of human tamperng s uncear. These strans have aso shown to be
more potent than those prevousy grown, ncreasng profts for the drug
cartes responsbe for the exportng of cocane. Athough producton fe
temporary, coca crops rebounded n numerous smaer feds n Coomba,
rather than the arger pantatons.
The cutvaton of coca has become an attractve, and n some cases even
necessary, economc decson on the part of many growers due to the
combnaton of severa factors, ncudng the persstence of wordwde
demand, the ack of other empoyment aternatves, the ower proftabty of
aternatve crops n offca crop substtuton programs, the eradcaton-
reated damages to non-drug farms, and the spread of new strans of the
coca pant.
Estmated Andean regon coca cutvaton and potenta pure cocane
producton|122|
2000 2001 2002 2003 2004
Net cutvaton (km2) 1875 2218 2007.5 1663 1662
Potenta pure cocane producton (tonnes) 770 925 830 680 645
The atest estmate provded by the U.S. authortes on the annua producton
of cocane n Coomba refers to 290 metrc tons. As of the end of 2011, the
sezure operatons of Coomban cocane carred out n dfferent countres
have totaed 351.8 metrc tons of cocane, .e. 121.3% of Coombas annua
producton accordng to the U.S. Department of States estmates. |123||124|
Synthess
Synthetc cocane woud be hghy desrabe to the ega drug ndustry, as t
woud emnate the hgh vsbty and ow reabty of offshore sources and
nternatona smuggng, repacng them wth candestne domestc
aboratores, as are common for ct methamphetamne. However, natura
cocane remans the owest cost and hghest quaty suppy of cocane. Actua
fu synthess of cocane s rarey done. Formaton of nactve enantomers
(cocane has 4 chra centres - 1R,2R,3S,5S - hence a tota potenta of 16
possbe enantomers and dastereosomers) pus synthetc by-products mts
the yed and purty. Names ke "synthetc cocane" and "new cocane" have
been msapped to phencycdne (PCP) and varous desgner drugs.