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By: Paul L. Cary Toxicology Laboratory
University of Missouri
Presented by: Vinnie Happ Redwood Toxicology Laboratory,
An Alere group of companies.
Designer Drugs SPICE/K2, BATH SALTS, ETC.
PROBLEMS POSED BY
September 19, 2010 CCAPPOAP
The Story of Designer Drugs
Designer Drugs:
drugs, which are created (or reformulated, if the drug already existed) to get around existing drug laws (CSA), usually by modifying the molecular structures of existing drugs to varying degrees
Designer Drugs:
designer drug was first coined by law enforcement in the 1980s
second International Opium Convention in 1925 which specifically banned alternative esters of morphine
1960s - 1970s, new synthetic hallucinogens (modifications of LSD & PCP)
1980s - 1990s, design of MDMA (ecstasy) & methcathinone
2000 - 2005, derivatives of psilocybin & mescaline - anabolic steroid
What Drives the Production Designer Drugs ?
consumer preferences
law enforcement control
Spice/K2 and Synthetic Cannabinoids
What’s in these incense products?
Listed Ingredients in Spice Canavalia rosea: commonly known as beach bean or bay bean - vine
found in tropical and subtropical beach dunes
Nymphaea caerulea: also known as Blue Egyptian water lily
Scutellaria nana: perennial herb also known as Dwarf skullcap
Pedicularis densiflora: known commonly as Indian warrior - a perennial herb
Leonotis leonurus: also known as Lion's Tail and Wild Dagga - a perennial shrub native to southern Africa
Zornia latifolia: is a perennial herb
Nelumbo nucifera: known by a number of names including Indian Lotus, or simply Lotus - aquatic perennial commonly found in China
Leonurus sibiricus: commonly called Honeyweed or Siberian motherwort, herbaceous plant native to Asia
vanilla
honey
Preparation of the incense :
botanicals are sprayed with liquid preparations of:
HU-210
HU-211
CP 47,497
JWH-018
JWH-073
JWH-250
JWH-081
JWH-210
JWH-200
And many more
Synthetic cannabinoids are not Salvia divinorum.
Salvia divinorum is a
psychoactive plant which can induce dissociative effects.
Where can these incense products be
purchased?
Sources of Incense Products:
head shops/alternative medicine stores / convenience stores
internet/on-line sources (2004)
1-(800) phone ordering services
individual distributors
What s the story behind these synthetic THC
chemicals?
Origins of Synthetic Cannabinoids
HU-210 & HU-211 - synthesized at Hebrew University, Israel in 1988. HU-210 is an anti-inflammatory; HU-211 as an anesthetic
CP 47,497 - developed by Pfizer in 1980 as an analgesic (pain reliever)
JWH-018 & JWH-073 - synthesized by a researcher at Clemson (1995) for use in THC receptor research - John W. Huffman
more than 100 different synthetic cannabinoids have been created
Synthetic Cannabinoids Timeline:
first appearance on the Internet 2004
Europe was original target market
by 2008 widespread in Europe
University Hospital Freiburg, Germany first analysis of incense, late in 2008
2008 introduced into US
widespread in US by late 2008 - 2009
first email Spring 2009
first urine metabolite laboratory test available mid 2010 by Redwood Toxicology Lab
Synthetic Cannabinoids act as THC agonists
-An agonist is a chemical that binds to a receptor
and triggers a response – often mimicking the action of a naturally occurring substance.
Receptor
Drug (agonist)
Why Designer Drugs Work
Brain Receptors
Natural Neurotransmitters
noradrenaline
dopamine
Designer Chemists Trick Brain
Dopamine MDMA
Why Change the Key?
• prolong the effect of the drug • increase the potency of the drug • select the desired effect • make the drug more difficult to detect • avoid patent infringement • make an illegal drug legal
Drug
CB Receptors:
CB1 and CB2
CB1 receptor influence mainly the brain (central nervous system, CNS), but there are also effects expressed in the lungs, liver and kidneys
CB2 receptor effects mainly the immune system and in certain stem cells
CB Receptors:
Smoking Cannabinoids
BG: motor control, learning
Hippo: memory, spatial navigation
CB: cognitive functions - attention, language, emotions
What does CB1 receptor control?
Pharmacological Effects of Synthetic Cannabinoids are Similar to THC increase heart rate & blood pressure
altered state of consciousness
mild euphoria and relaxation
perceptual alterations (time distortion)
intensification of sensory experiences
pronounced cognitive effects
impaired short-term memory
reduction in motor skill acuity
increase in reaction times
Dependence Syndrome Similar to Marijuana
Reported Effects of Synthetic Cannabinoids are Different to THC
production inconsistencies
herbal incense blends are harsher to inhale
effect on appetite is non-existent
increased restlessness & aggressive behavior
herbal incense produces a shorter high (perceptual alterations & sensory effects are limited)
doesn t mix well with alcohol (hangovers)
incense costs more than marijuana
Prevalence of Synthetic THC? No national statistics
Louisiana: 9 clients pre-selected based upon suspicion
7 tested positive
Columbia MO: 17 clients pre-selected based upon suspicion
12 tested positive / 5 self-admissions
Pennsylvania:
Confirmed use in Bucks, Lehigh, Lancaster Counties
National Lab Drug Test Data (Redwood Toxicology Lab): 16.5% average positivity rate
(Treatment and/or via court order samples)
National Statistics for Synthetic THC
American Association of Poison Control Centers has reported:
All of 2009 13 cases
First half of 2010 567 cases in 41 states
4000% increase
As of July 31, 2011 4,137 reported exposures to bath salts
Can synthetic THC chemicals be detected by
drug testing?
Drug Testing:
NO on-site, rapid, instant tests
NO laboratory-based screening tests
Five laboratories employing LC/MS/MS technology
$25- $50 per sample
National Laboratory Statistics for “Synthetic Marijuana” Test Redwood Toxicology Laboratory began testing JWH-018, JWH-073
and their metabolites in July 2010.
Over 50,000 urine samples analyzed; primarily from treatment and drug court programs around the nation.
Alarming overall positivity rate of 18%.
Redwood also developed a Saliva based test that confirms presence of JWH-018, JWH-073 and JWH-250 in oral fluid.
Redwood analyzed over 600 samples with a positivity rate of 15%.
Information confirms popularity of these products.
Issues of Concern
What synthetic compounds (or metabolites) are being tested by these laboratories?
no standardized urine cutoff levels
no standardized methods (LC/MS/MS)
tests detect metabolites
no independent quality control materials
no proficiency testing
detection window unknown
Detection Window ???
testing for metabolites
educated guess - same as real marijuana
many labs advertising up to 72 hours
confounding issue - differing cutoff levels
fact is - we don t know!
A New Designer Drug – Bath Salts
Bath Salts: The term bath salts refers to a range of water-
soluble products designed to be added to a bath. They are said to improve cleaning, improve the experience of bathing, serve as a vehicle for cosmetic agents, and some even claim medical benefits. Bath salts have been developed which mimic the properties of natural mineral baths or hot springs.
Sold Under the Names:
Ivory Wave
Ivory Pure
Ivory Coast
Purple Wave
Vanilla Sky
Health Hazard?
What s in Bath Salts:
Methylenedioxypyrovalerone (MDPV) is a psychoactive drug with stimulant properties which acts as both a norepinephrine & dopamine reuptake inhibitor (NDRI).
MDPV has four times the potency of Ritalin
MDPV - no history of FDA approved medical use
sold since 2007 as a research chemical
MDPV:
currently popular in Europe, UK & Australia
is usually snorted - similar to cocaine
considered extremely addictive
adverse medical/psychiatric ramifications
no on-site or screening drug tests
designer drug chemically similar to cathinone
first synthesized in 1929
amphetamine-like properties
powerful synthetic stimulant
rediscovered by synthetic chemists in 2003
widespread in Europe, Australia, US
Methylmethcathinone (Mephedrone)
reformulation of cathinone, a chemical found in the
khat plant of Eastern Africa
khat existence traced to 15th C. Ethiopia
grown in Somalia, Yemen, Kenya, Ethiopia
khat is banned in the U.S.
Mephedrone
Pharmacological Effects of Bath Salts : increase heart rate & blood pressure
pupil dilation
hyperactivity, arousal & over stimulation
increased energy & motivation
euphoria - agitation
dizziness
nausea
breathing difficulties
diminished perception of the requirement for food and sleep
Can Bath Salts be Detected by Drug
Testing?
Drug Testing:
NO on-site, rapid, instant tests
NO laboratory-based screening tests
laboratories employing LC/MS/MS technology
unknowns regarding this testing
cutoff levels
detection times
standardized testing procedures
National Laboratory Statistics for “Bath Salt” Test Redwood Toxicology Laboratory began testing designer stimulants
in January 2011.
As of May, over 2,000 urine specimens received from treatment and drug court programs nationwide have been analyzed.
So far, 8% of the specimens analyzed were found to be positive for one or more designer stimulant substance.
88% of the positive specimens detected MDPV
33% of the positive specimens detected Methylone
Mephedrone was found in 5 specimens, Butylone in 2, TFMPP and BZP in one specimen each.
Clearly MDPV and Methylone are the cause of greatest immediate concern.
The Next Wave?
2C-E Nicknamed "Europa"
synthesized in 1970 s -1980 s
psychedelic phenethylamine
taken orally
powerful hallucinogenic effects
high can last 6- 12 hours
sold through European sources
one death reported in MN on March 11, 2011
2C-E Nicknamed "Europa" synthesized by Alexander Shulgin
popularized MDMA (Ecstasy)
PIHKAL book (1991)
2C-I another phenethylamine available
2C-E is chemically related to other 2C phenethylamines
exact legal status is unclear - 2C-B banned under CSA
What s the legal status of synthetic
cannabinoids and stimulants?
Legal Status of Synthetics with the (DEA)
March 1, 2011, the DEA, issued final notice to temporarily place five (5) synthetic cannabinoids into the Controlled Substances Act (CSA) for at least one year
synthetic cannabinoids treated as Schedule 1 drugs
a drug that has a high potential for abuse
a drug that has no currently accepted medical use in treatment in the United States
there is a lack of accepted safety for use of the drug under medical supervision
September 7, 2011 — DEA Moves to Emergency Control Synthetic Stimulants. Ban to cover: Mephedrone , MDPV and Methylone
Legal Status of Synthetic Cannabinoids /Stimulants (DEA)
DEA took action - imminent hazard to the public safety
imposes criminal sanctions and regulatory controls of Schedule I substances under the CSA
covers the manufacture, distribution, possession, importation, and exportation
Ramifications of DEA Action:
eliminate the commercial distribution of synthetic cannabinoids
drive synthetic cannabinoids underground
limit their availability
impact on criminal justice - wait and see?
States Banning Bath Salts : Control status typically features MDPV and/or Mephedrone
Louisiana
North Dakota
Florida
New Jersey
Pennsylvania
Washington
Kansas
Arkansas
New Mexico
Idaho
Oregon
Tennessee
West Virginia
Wisconsin
Virginia
Wyoming
Missouri
Kentucky
Hawaii
Mississippi
Alabama
Michigan
Georgia
Oklahoma
Utah
Legal Status of Synthetics in (PA)
Senate Bill 1006
Signed into law June 23, took effect on August 22, 2011
Bans eight (8) synthetic cannabinoids and their analogues along with salvia divinorum
Bans six (6) synthetic stimulants including MDPV, Mephedrone and Methylone
Amendment 7 was added that includes language barring all chemicals that are similar to the substances found in bath salts, synthetic cannabinoids and 2C
PA’s Act 7 of 2011 The following substances are added to PA Department of Health’s Schedule I effective August
22, 2011, under Act 7 of 2011 (Senate Bill 1006), and are thus illegal under the Controlled Substance, Drug, Device and Cosmetic Act (35 P.S. 780-101 et seq.):
“Salvia” Salvia Divinorum Salvinorin A Divinorin A “Synthetic Cannabinoids” CP 47,497 and Homologues, 2-[(1R, 3S)-3-Hydroxycyclohexyl]-5-(2-
Methyloctan-2-yl)phenol. HU-210, [(6AR, 10AR)-9-(Hydroxymethyl)-6,6-Dimethyl-3-(2-methyloctan-2-
yl)6A,7,10,10A-Tetrahydrobenzo[C]Chromen-1-ol)] HU-211, (Dexanabinol, (6AS,10AS)-9-(Hydroxymethyl)-6,6-Dimethyl-3-(2-
Methyloctan-2-yl)-6a,7,10,10A Tetrahydrobenzo[C]Chromen-1-ol) JWH-018, 1-Pentyl-3-(1-Naphthoyl)indole JWH-019, 1-Hexyl-3-(1-Naphthoyl)indole JWH-073, 1-Butyl-3-(1-Naphthoyl)indole JWH-200, (1-(2-Morpholin-4-ylethyl)indol-3-yl)-naphthalen-1-ylmethanone
Act 7 of 2011 “Bath Salts” 3,4-Methylenedioxymethcathinone (methylone) 3,4-Methylenedioxypyrovalerone (MDPV) 4-Methylmethcathinone (Mephedrone) 4-Methoxymethcathinone 4-Fluoromethcathinone 3-Fluoromethcathinone
Act 7 of 2011
“Phenethylamines” 2-(2,5-Dimethoxy-4-ethylphenyl) ethanamine (2C-E) 2-(2,5-Dimethoxy-4-methylphenyl) ethanamine (2C-D) 2-(4-Chloro-2,5-dimethoxyphenyl) ethanamine (2C-C) 2-(4-Iodo-2,5 dimethoxyphenyl) ethanamine (2C-I) 2-[4-(Ethylthio)-2,5-dimethoxyphenyl] ethanamine (2C-T-2) 2-[4-(Isopropylthio)-2,5-dimethoxyphenyl] ethanamine (2C-T-4) 2-(2,5-Dimethoxyphenyl) ethanamine (2C-H) 2-(2,5-Dimethoxy-4-nitro-phenyl) ethanamine (2C-N) 2-(2,5-Dimethoxy-4-(N)-propylphenyl) ethanamine (2C-P)
Is the Legislation having an impact??
Associated Press article
PepsiCo 3Q profit climbs on snack, beverage sales
By SARAH SKIDMORE , 10.12.11, 12:27 PM EDT
Are There Control Strategies Other Than
Testing?
Alternative Control Strategies:
community supervision
search & seizure -(probation/client contract)
car, home, possessions
Court s Response: place specific synthetic cannabinoid
prohibition in your client contract
establish a certain testing date - inform client population
establish sanction severity
select participants for testing where there are indications of herbal incense use
identify positive participants in court & sanction openly to enhance deterrent effect
provide opportunity for participants to self-report
Client Prohibition Guidance:
Any and all designer drugs that can be purchased legally, over the counter without a physician s prescription are strictly prohibited.
Any and all “smoking mixtures (other than products specifically designated to contain only tobacco) are strictly prohibited.
Any and all products sold or marketed under false pretenses with the warning “Not for Human Consumption are strictly prohibited.
Designer Drug Evolutionary Path
Plant to Designer Drug
Plant Natural Drug(s)
Synthetic Drug(s)
Designer Drug(s)
Ma Huang
Chinese herb
(ephedra sinica)
ephedrine & pseudo- ephedrine (natural stimulants)
amphetamine & meth-
amphetamine developed in
the early 1900 s
MDMA (Ecstasy)
Plant to Designer Drug
Plant Natural Drug(s)
Synthetic Drug(s)
Designer Drug(s)
Cannabis sativa
(marijuana)
delta - 9 tetrahydro-cannabinol
(THC)
Dronabinol & Marinol
HU, CP & JWH
synthetic cannabinoids
(JWH-018, HU-211,
CP-49,497)
Plant to Designer Drug
Plant Natural Drug(s)
Synthetic Drug(s)
Designer Drug(s)
Khat
(catha edulis)
cathinone (natural
stimulant)
phenyl-propanolamine
(PPA - weight loss drug)
methcathinone synthesized in 1928 in Soviet
Union (antidepressant)
mephedrone (methylmeth-cathinone)
one of the bath salt
constituents
Designer Drugs: designer drugs are here to stay
similar evolutionary patterns
testing will nearly always lag behind
legal controls will be challenging and delayed
BE PROACTIVE!
build community supervision/expand search & seizure efforts
design client contract specifically address designer drugs
Presented by: Vinnie Happ Redwood Toxicology Laboratory,
An Alere group of companies.
By: Paul L. Cary Toxicology Laboratory
University of Missouri
Thank you for your time.
