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Designer Drugs (Synthetics): drugs, which are created (or reformulated, if the drug already existed) to get around existing drug laws CSA (controlled substance act), usually by modifying the molecular structures of existing drugs to varying degrees Sources of Incense Products: internet/on-line sources head shops/alternative medicine stores / convenience stores/flea markets 1-(800) phone ordering services individual distributors Preparation of the incense: Botanical plants/herbs are sprayed with liquid preparations of: HU-210 HU-211 CP 47,497 JWH-018 JWH-073 JWH-250 JWH-081 JWH-210 XLR-11, UR-144 And many more Origins of Synthetic Cannabinoids CP 47,497 - developed by Pfizer in 1980 as an analgesic (pain reliever) HU-210 & HU-211 - synthesized at Hebrew University , Israel in 1988. HU-210 is an anti- inflammatory; HU-211 as an anesthetic JWH-018 & JWH-073 - synthesized by a researcher at Clemson (1995) for use in THC receptor research - John W. Huffman more than 200 different synthetic cannabinoids have been created How K2/Spice works: 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 the naturally occurring substance. Receptor Drug (agonist) Why Change the Key? • prolong the effect of the drug • increase the potency of the drug select the desired effect • avoid patent infringement • make the drug more difficult to detect • make an illegal drug legal
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Page 1: Designer Drugs (Synthetics): Sources of Incense Productsojacc.org/wp-content/uploads/2013/10/Happ-Handouts.pdf · Jeffery Moran and colleagues note that synthetic marijuana, often

Designer Drugs (Synthetics):

drugs, which are created (or reformulated, if the drug already existed) to get around existing drug laws CSA (controlled substance act), usually by modifying the molecular structures of existing drugs to varying degrees

Sources of Incense Products:

  internet/on-line sources   �head� shops/alternative medicine stores /

convenience stores/flea markets   1-(800) phone ordering services   individual distributors

Preparation of the �incense�:

 Botanical plants/herbs are sprayed with liquid preparations of:  HU-210  HU-211  CP 47,497  JWH-018  JWH-073

 JWH-250  JWH-081  JWH-210  XLR-11, UR-144  And many

more

Origins of Synthetic Cannabinoids   CP 47,497 - developed by Pfizer in 1980 as an

analgesic (pain reliever)   HU-210 & HU-211 - synthesized at Hebrew

University, Israel in 1988. HU-210 is an anti-inflammatory; HU-211 as an anesthetic

  JWH-018 & JWH-073 - synthesized by a researcher at Clemson (1995) for use in THC receptor research - John W. Huffman

  more than 200 different synthetic cannabinoids have been created

How K2/Spice works: 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

the naturally occurring substance. Receptor

Drug (agonist)

Why Change the Key? • prolong the effect of the drug •  increase the potency of the drug • �select� the desired effect • avoid patent infringement • make the drug more difficult to detect • make an illegal drug �legal�

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Pharmacological Effects of Synthetic Cannabinoids are Similar to THC   increase heart rate & blood pressure   altered state of consciousness, mild euphoria   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   kidney damage

Synthetic Marijuana Use Linked to Kidney Damage Such designer drugs, called Spice or K2, may have toxic additives, researchers say By Mary Elizabeth Dallas - Tuesday, February 12, 2013

(HealthDay News) -- Case studies analyzed by doctors from the University of Alabama at Birmingham found that this designer drug, which mimics the effects of marijuana, has been directly linked to serious kidney damage. The researchers suggested that doctors should suspect the use of synthetic marijuana when patients, particularly young adults, have unexplained acute kidney damage "Cases of acute coronary syndrome associated with synthetic marijuana use have been reported, but our publication is the first to associate use with acute kidney injury," study co-author Dr. Gaurav Jain, an assistant professor in the nephrology division, said in a university news release. Abnormally rapid heart rate and seizures have also been reported with synthetic marijuana use, he noted.

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?

Cannabis (THC) vs. Cannabinoids (k2): Effects Seen in Clinical Cases Most symptoms are

similar to cannabis intoxication:

-Abnormally rapid heart rate – Reddened eyes – Anxiousness – Mild sedation – Hallucinations – Acute psychosis – Memory deficits

Symptoms not typically seen after cannabis intoxication:

– Seizures – Potassium deficiency – Hypertension – Nausea/vomiting – Agitation – Violent behavior – Coma

SOURCES: Hermanns-Clausen et al . (In Press), Addiction; Rosenbaum et al . (2012). Journal of Medical Toxicology; Forrester et al. (2011). Journal of

Addictive Disease; Schneir et al . (2011). Journal of Emergency Medicine.

Public release date: 2-Oct-2013 American Chemical Society 

Toward understanding the dangers of the fake marijuana called 'Spice' or 'K2’ The study, published in the ACS journal Analytical Chemistry, describes development of a method that could someday help physicians diagnose and treat the thousands of young adults and teens who end up in emergency rooms after taking the drugs. Jeffery Moran and colleagues note that synthetic marijuana, often marketed as "natural incense," "potpourri," Spice or K2, is a significant public health concern, and 1 in 9 high school seniors admit recent use. The substances produce a "high," but also can cause a wide range of dangerous side effects including seizures, hallucinations, severe kidney damage, psychotic behavior and heart attacks. To gain insight into the effects of designer marijuana products, Moran's team developed a new method and used it to study how the body processes two popular forms in Spice and K2, known as JWH-018 and AM2201. Urine samples from 15 people who tested positive for use showed significant differences in how the individuals' bodies processed the drugs. This finding could help explain why some people experience more severe effects from the drugs than others.

Drug Testing: Synthetic THC / K2   Rapid, onsite instant test (as of 3/1/12)

  Laboratory-based screening test (limited)   Most Laboratories are employing LC/MS/MS

technology   Primarily via urine, however some labs can test via

oral fluid and blood   $$$ varies greatly   Onsite vs Lab is very different testing methodology

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On-site vs Laboratory testing for K2

On-site K2

  JWH-018 & JWH-073 primarily

  Cut-off at 25 or 50ngs/ml   Testing limited metabolites   Much higher threshold to

trigger positive   Screening technology

Laboratory K2

  JWH-018, 073, plus *17 other synthetic cannabinoid structures

JWH-019, 081, 122, 200, 203, 210, 250, 398, AM2201, MAM2201, RCS4, RCS8, AM-694, AM-1248, AKB-48,UR-144, XLR-11   Cut-off 1ng/ml or less   Testing for hydroxy acid & other

components/metabolites   Detecting presence

  Confirmatory technology

*Redwood Toxicology Laboratory

CESAR FAX U n i v e r s i t y o f M a r y l a n d , C o l l e g e P a r k

A Weekly FAX from the Center for Substance Abuse Research

•  The majority of synthetic cannabinoid users reported that they used the drug to avoid positive drug tests, either because they were under community correctional supervisions, seeking employment, residing in a sober living facility, or joining the military. According to one user, �Spice would give you a weed like effect without the positive test�

•  �Most of the users of Spice-type products in this study consumed these products as a substitute for marijuana during drug-testing periods, and returned to marijuana use once that period ended�. According to one user, �I was trying to get a job where they were going to drug test . . . so I got that stuff [Spice], and I liked it enough. I enjoyed it. I did it for a while . . . Then, my job search ended �cause I wasn’t going to do any of them. So I went back to the regular stuff�

•  Nearly all the SC users learned of the drug from someone who was using SC to avoid detection on drug tests. For example, one user reported that he �was talking to some kids that went to a Christian school, and they get drug tested. So, all the kids there would smoke Spice instead of weed�

•  All the SC users also used marijuana, and half had a history of drug problems, such as sobriety attempts, drug-related offending, and negative drug experiences.

July 8, 2013 Vol. 22, Issue 27

Synthetic Cannabinoid Users Report Using the Drug to Avoid Positive Drug Tests; Return to Marijuana Use When Not Being Tested

!! 301-405-9770 (voice) !! 301-403-8342 (fax) !! [email protected] !! www.cesar.umd.edu !!

NOTE: Findings are from in-depth, semi-structured interviews with 25 Southern California adults who had used K2, mephedrone, bath salts, or Salvia divinorum at least once. Participants were recruited using flyers distributed to head shops, cafes and other businesses; advertisements posted in free weekly newspapers; and snowball sampling.

.

Synthetic cannabinoids, also known as K2 or Spice, are not included in most routine drug test panels because they require specialized, more expensive testing. Furthermore, studies have shown that the types and amounts of synthetic cannabinoid (SC) metabolites can vary greatly between products, lots, and even within the same package1, making it difficult to decide which specific SC metabolite should be included in drug testing programs. Some SC users use the drug as a substitute for marijuana to avoid positive drug tests, according a qualitative study of SC users in Southern California. The study found that:

CESAR Pilots New Community Drug Early Warning System in Criminal Justice System; Finds Synthetic Cannabinoids in All Populations Studied

UR-144 and XLR-11

31%

XLR-11Only4%

UR-144 Only60%

UR-144 and JWH-018

3%3+ Metabolites

2%

•  SCs were detected in the specimens from all participating sites in the District of Columbia, Maryland, and Virginia. Furthermore, all of the SC positive specimens contained one or two of the metabolites (UR-144 and XLR-11)

•  SCs were most likely to be detected in younger men. What was not expected was the level of use that was found. For example, one-quarter to one-third of young men in the three populations studied in DC tested positive for SC.

•  Unlike other prescription and illicit drugs, SCs were as likely to be found in persons who had failed the limited CJS screen as in persons who had passed. In other words, current drug testing screens which do not test for SCs are likely missing significant drug use (and users) in the populations they monitor. One possibility is that persons who know they will be tested use SC products because they know that the drug is not included in most test panels.

Metabolites Found in All Synthetic Cannabinoid Positive Specimens from

Five CJS Populations, 2013 (N=118)

Detection Window ???

  testing for metabolites   educated guess - same as real marijuana?  many labs advertise �up to 72 hours�   limited studies  passive inhalation?   fact is - we don�t know all the answers

Wet Marijuana   Embalming Fluid-Soaked Marijuana: smoking marijuana soaked in embalming fluid is gaining popularity throughout the United States. The syndrome of intoxication looks nearly identical to that seen following phencyclidine (PCP) use, with agitation, disorganized speech, and thoughts, and diminished attention. This new trend in drug use involving marijuana also presents a resurgence in PCP use.   Soaked in water – uneven burn   Mixed with PCP: wet, fry, crystal joint, supergrass   Mixed with codeine containing cough syrup   Mixed with methamphetamines

What’s in Bath Salts:

  MDPV (Methylenedioxypyrovalerone) - a psychoactive drug with powerful stimulant properties which acts as both a norepinephrine & dopamine reuptake inhibitor (NDRI). “A two for”

  usually snorted like cocaine   duration of effect 2-3 hours /adverse effect 6-8 hrs   MDPV - no history of FDA approved medical use   Sold as a “research chemical”   adverse medical or psychiatric ramifications

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  amphetamine-like properties, powerful stimulant   �rediscovered� by synthetic chemists in 2003   reformulation of cathinone, a chemical found in the

khat plant of Eastern Africa   khat existence traced to 15th C. Ethiopia   khat is banned in the U.S.

Mephedrone (Methylmethcathinone)

Methylone (3,4-methylenedioxy-N-methylcathinone)

 very similar to MDMA   stimulant  phenethylamine, amphetamine, and

cathinone properties   euphoria and increased sociability   insomnia and restlessness  hallucinations and psychosis

    

   Bath Salts and beyond!!! Expanded Synthetic Stimulant Panel �-PVP BZP     Butylon Buphedrone   Cathinone     Ethylone     Flephedrone MBDB      mCPP MDA

MDEA  MDMA MDPV Mephedrone  Methcathinone 4-Methylethcathinone  Methylone Pentedrone Pentylone Pyrrolidinopentiophenone TFMPP

MDMA – Molly/Ecstasy - Molly is not new, exactly. - MDMA, or 3,4-methylenedioxy-N-methylamphetamine, was patented by Merck pharmaceuticals in 1914 - did not make much news until the 1970s, when psychotherapists began giving it to patients to get them to open up.

-arrived at New York nightclubs in the late 1980s, and by the early ’90s it became the preferred drug at raves, inducing feelings of euphoria, closeness and diminished anxiety,

- Ecstasy was quickly embraced by Wall Street traders and Chelsea gallerinas. as demand increased, so did the adulterants in each pill (caffeine, speed, ephedrine, ketamine, LSD, talcum powder and aspirin, to name a few), and by the new millennium, the drug’s reputation had soured. - in the last decade, it returned to clubs as Molly, a powder or crystalline form of MDMA that implied greater purity and safety: Ecstasy re-branded as a gentler, more approachable drug.

- thanks in part to that new friendly moniker, MDMA has found a new following in a generation of conscientious professionals who have never been to a rave and who are known for making careful choices in regard to their food, coffee and clothing. - -

Molly - continued   common side effects, include teeth grinding, dehydration, anxiety, insomnia,

fever and loss of appetite.   more dangerous ones include hyperthermia, uncontrollable seizures, high blood

pressure and depression caused by a sudden drop in serotonin levels in the days after use, nicknamed Suicide Tuesdays.

  capsules sell for $8 to $40.   the most common Molly additives are bath salts, including methylone and

mephedrone. Bath salts are chemically similar to MDMA.   A report recently released by the DEA's New York division highlighted the

results of 143 lab tests over the past four years of substances suspected of being Molly. Only 13% of the drugs were MDMA, while 41% were 4-MEC, a type of bath salt, and 20% were methylone.

  Veteran MDMA users say they ask that drugs be tested before they buy them, using kits that can be bought online. "If I'm getting more than a gram, they'll test it right in front of you," said a 27-year-old ad salesman from Oakland, Calif. DanceSafe, an organization that promotes safety at raves, sets up testing tables at some events.

Pharmacological Effects of �Bath Salts�:

  increase heart rate & blood pressure   pupil dilation, rapid speech   hyperactivity, arousal, & over stimulation   increased energy & motivation   euphoria - agitation   dizziness, nausea   hallucinations, seizures, convulsions   breathing difficulties!!!   diminished perception of the requirement for food and sleep   death

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Testing for Bath Salts?? Yes! However:

  No on-site, rapid, instant tests   No laboratory-based screening tests   Laboratories employing GC/MS and

LC/MS/MS technologies   Detection times remain unknown   Best procedure for detecting

metabolites vs parent drug unknown

Legal Status of Synthetics with the (DEA) Fed - Update

  June, 2012 DEA added 26 compound to the CSA   “9 different 2C chemicals and 15 synthetic cannabinoids   cannabamimetic agents”or similar compounds

  July 9, 2012 bill signed into Law -   Synthetic Drug Abuse Prevention Act of 2012

  45 States have some type of legislative ban   Synthetic cannabinoids and stimulants treated as Schedule 1

drugs   a high potential for abuse

  no currently accepted medical use

  lack of accepted safety for use of the drug under medical supervision

Status of Synthetics in OH HB 64 (Signed July 2011)

- Effective October 20111 JWH-018; JWH-073; JWH-200; CP 47,497 and C8 homologue.

 Bans Synthetic Stimulants  Bath Salts

-MDPV / Mephedrone and others

2C-I Nicknamed “Smiles”   popular among teens, responsible for dozens of overdoses

and deaths especially in Midwest.   white crystalline powder, typically snorted or ingested.   High & Effects can last a few hours to a few days,

described as being a “roller coaster through hell”   a combination of MDMA and LSD, only more intense.   2C-I is being made by dealers and “hobbyists,”   chemicals can be obtained over the internet   2C-I overdoses can cause seizures, kidney failure, and fatally

high blood pressure.

Pharmacological Effects

 Dilated pupils   Sweating  Dry mouth  Rapid speech  Rapid/frequent mood swings  Hyperactivity/ Elevated BP  Hair standing on end  Nasal passage irritation

Erowid.com “Documenting the complex relationships between humans and psychoactives”

 Great resource for information  Take with a grain of salt  Your clients are probably aware of this site as

well

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An additional challenge beyond the Synthetics:

Opiates &

Suboxone/Buprenorphine

The Opiate Family

Opiates: Heroin Morphine Codeine Hydrocodone - (Vicodin, Loratab) Hyrdomorphone -(Dilaudid) Oxycodone – (Oxycontin, Percocet, Roxicodone) Oxymorphone - (Opana)

Heroin Makes a Comeback This Time, Small Towns are Increasingly Beset by Addiction, Drug-Related Crimes Thursday, August 8, 2013 As of 12:23 AM EDT - WSJ ELLENSBURG, Wash.—This small city east of the Cascade Mountains is known for its hay farms, rodeos and, increasingly, something more sinister: a growing heroin problem. The fatal overdose of a state trooper's son in May convulsed the town—especially when the two men arrested and charged with selling him heroin turned out to be a county official's sons. Heroin use in the U.S. is soaring, especially in rural areas, amid ample supply and a shift away from costlier prescription narcotics that are becoming tougher to acquire. Much of the heroin that reaches smaller towns such as Ellensburg comes from Mexico, where producers have ramped up production in recent years, drug officials say. Heroin seizures at the Southwest border, from Texas to California, ballooned to 1,989 kilograms in fiscal 2012 from 487 kilograms in 2008, according to figures from the Drug Enforcement Administration. The heroin scourge has been driven largely by a law-enforcement crackdown on illicit use of prescription painkillers such as oxycodone and drug-company reformulations that make the pills harder to crush and snort, drug officials say. That has pushed those who were addicted to the pills to turn to heroin, which is cheaper and more plentiful. A 21-year-old recovering addict said she made the switch from pain pills to heroin after her dealer one day held out both options in his hands and encouraged her to choose the cheaper one Drug experts say the heroin sold today is generally purer and thereby more potent than the varieties prevalent in past decades, increasing the risk of overdose. A baggie "may be 15% pure one day, and the next day it's 60%," said Skip Holbrook, the police chief in Huntington, W.Va., which sits in an area of Appalachia where heroin is spreading. "It's like playing Russian roulette."

Opiate epidemic spreading in Philly POSTED: October 10, 2013

ROLAND LAMB, director of the city's Office of Addiction Services, can rattle off drug stats all day long, but the button on his lapel - the word "stigma" with a slash through it - tells you where he stands on America's drug war. It's Lamb's way of protesting an "arrest first, treat later mentality" that he says is similar to "locking up type 2 diabetics for not following their medication and not staying on their diets.” Yesterday, Lamb presented his office's latest statistics, showing that Philadelphia continues to struggle with an opiate epidemic. Not just heroin, but also strong prescription painkillers that produce a similar high and can turn some patients - or  their friends and relatives - into addicts. "This is a serious issue that crosses all age groups and demographics," Lamb said.  Last year, for example, opiates accounted for five of the 10 most frequently detected drugs in bodies handled by the city Medical Examiner's Office.

Opiate vs Oxycodone Screen why you should consider splitting them out when testing

Opiate Screen @ 300ng

  Primarily targets morphine and codeine

  Oxycodone – 30,000ng   Needed to trigger a positive   Miss the chippers, O.O.U.

  Opana – Oxymorphone   100,000ng needed to trigger

positive on onsite Opiate test

Oxycodone Screen @ 100ng

  Oxycodone – 100ng   Needed to trigger a positive   Detect the chippers

  Will detect oxymorphone and hyrdocodone at 1562ngs

  Opana – Oxymorphone   Oxycodone lab EIA screen has

100% cross reactivity to Oxymorphone

  Opana (ER) – time release

Opana Information   Opana is more potent, per milligram, than Oxy   Users vulnerable to O.D, kidney failure, death   Street names: "stop signs," ”Obomb,”new blues”   crushed - either snorted or injected.   Endo Pharmaceuticals, announced in Dec 2011

that it would reformulate Opana. The new pill is being manufactured

  Opana ER (Extended Release)   Small blood clots under the skin/cause blood

disorders

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Take away comments

  If positive on an Opiate screening test – an Opiate family member most likely detected

  If confirmed for 6-AM (6-Acetylmorphine )at the Lab:  Heroin use

  If confirmed positive just for Morphine  Metabolized heroine to morphine and or  morphine use i.e. from a prescription,  poppy seed use

Suboxone-Buprenorphine   FDA approved in 2002   used to treat opiate addiction   alternative to methadone   partial agonist (ceiling)   in pill, film, patch   2mg & 8mg doses   will not test positive on an opiate test   significant diversion   contains naloxone- guard against misuse   Individuals will get high on this stuff

What’s the attraction to Bup?

  user’s experience a euphoria effect   if taken in conjunction with other sedative drugs like

alcohol, sleeping pills(ambien) or benzodiazepines (clonopin)- extreme sedation, drowsiness, unconscious, or even death may occur

  Method of ingestion – typically sublingual (under the tongue), pill format going away, reports of snorting

  injected?   only test positive if specifically testing for buprenorphine

Presented by: Vinnie Happ Redwood Toxicology Laboratory

An Alere Company

[email protected]

Thank you for your time.


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