History

15 downloads 2860 Views 3MB Size Report
•1991 - Alexander Shulgin published PiHKAL (and in 1997 – TiHKAL). •2000 - BZP sold by legally Stargate until controlled in 2008. •2004 – K2 and Spice ...
Analogue Drugs In Australia 2012

Andrew Camilleri

Analogues History •1925 – International Opium Convention banned use of morphine and heroin.

Analogues History •1925 – International Opium Convention banned use of morphine and heroin. Alternate esters of morphine, such as dibenzoylmorphine , were manufactured to circumvent the Convention.

Analogues History •1925 – International Opium Convention banned use of morphine and heroin. Alternate esters of morphine, such as dibenzoylmorphine , were manufactured to circumvent the Convention. •1930 - The League of Nations passed analogue resolutions controlling all esters of morphine.

Analogues History •1972 – MDMA

MDA

PMA

Analogues History •1991 –Alexander Shulgin published PiHKAL

Analogues History •1991 –Alexander Shulgin published PiHKAL (in 1997, TiHKAL)

Analogues Structural Relationship to Dopamine Phenethylamine

Dopamine

Amphetamine

Cathinone

Analogues History •2000 – BZP sold legally by Stargate until controlled in 2008

BZP

Analogues History •2004 – K2 and Spice products emerge Originally developed in the 1960’s by Hebrew Uni (HU), 1970’s by Pfizer (CP) & 1980’s by Huffman (JWH) for analgesic effects.

RCS8

AM-2201

O

O

N

HU-210 HO

OH H

H

O

XLR11

THC

Analogues History •2007 - Cathinone products emerge in Australia Seizures in Europe of several methcathinone analogues but emergence, in Australia, from 2007 in Neorganics products.

4-methylmethcathinone

2-fluoromethamphetamine

Ethylcathinone

Main Drug Found In Illicit Tablets Ketamine 5%

Other 8% Ketamine 10%

2003

MA 20%

MA 10%

2007

MA 18%

2005

MDMA 72%

MDMA 62%

Ketamine 1%

Ketamine 1%

Other 5%

Other 3%

MA 3%

Other 7%

MDMA 82%

2008

MDMA 93%

Analogues History •2009 - MDMA Shortage 100 90

Percentage of Total Seizures

80 70 60 50 40 30 20 10 0

MDMA 2008/1 2008/2 2008/3 2008/4 2009/1 2009/2 2009/3 2009/4 2010/1 2010/2 2010/3 2010/4

Year/Quarter

MDMA Dosage in Tablets 120

100

87.4 80.6

80.0

mg

80

64.8

54.8

60

54.1 55.0

40

24.4 20

0 2003

2004

2005

2006

2007

Year

2008

2009

2010

Analogues History •2009-10 – MDMA detected in Wastewater

Chen C. et al 2011

Analogues History •2009-10 – Tablet composition changes dramatically 100 90

Percentage of Total Seizures

80

non-illicit drugs (caffeine, paracetamol etc)

70 60 50 40 30 20

MDMA

10 0 Year/Quarter

Analogues History •2009-10 – Tablet composition changes dramatically 100 90

non-illicit drugs (caffeine, paracetamol etc)

Percentage of Total Seizures

80 70 60 50

MDMA

40 30 20 10

MA

0 Year/Quarter

Analogues History •2009-10 – Tablet composition changes dramatically 100 designer drugs (total piperazines, cathinones, 2CI etc)

90

Percentage of Total Seizures

80 70

non-illicit drugs (caffeine, paracetamol etc)

60 50 40

MDMA

30 20 10

MA

0 Year/Quarter

Analogues History •2010 - Other ‘Legal Highs’ products begin rapidly emerging - Cathinones O CH3

4-methylmethcathinone (mephedrone, meow meow)

H3C

N CH3

H

O CH3

Other cathinone based drugs (eg flephedrone)

F

N CH3

H O

Naphyrone

N

O O

3,4-methylenedioxypyrovalerone (MDPV)

O

N

Analogues History •2010 - Other ‘Legal Highs’ products begin rapidly emerging - Cannabinoids Used in mining industry as not screened for in urine testing.

Analogues History •1972 - MDMA •1991 - Alexander Shulgin published PiHKAL (and in 1997 – TiHKAL) •2000 - BZP sold by legally Stargate until controlled in 2008 •2004 – K2 and Spice products emerge •2007 - Neorganics products emerge •2009 - MDMA Shortage •2010 - Other ‘Legal Highs’ products begin rapidly emerging

Analogues History •1972 - MDMA •1991 - Alexander Shulgin published PiHKAL (and in 1997 – TiHKAL) •2000 - BZP sold by legally Stargate until controlled in 2008 •2004 – K2 and Spice products emerge •2007 - Neorganics products emerge •2009 - MDMA Shortage •2010 - Other ‘Legal Highs’ products begin rapidly emerging 1997-2010 – 150 new substances identified in EU through their early warning system

Analogues History •1972 - MDMA •1991 - Alexander Shulgin published PiHKAL (and in 1997 – TiHKAL) •2000 - BZP sold by legally Stargate until controlled in 2008 •2004 – K2 and Spice products emerge •2007 - Neorganics products emerge •2009 - MDMA Shortage •2010 - Other ‘Legal Highs’ products begin rapidly emerging 1997-2010 – 150 new substances identified in EU through their early warning system 2010 - 41 new substances identified in EU (15 cathinones, 11 cannabinoids) 2011 - 49 new substances identified in EU, SA saw 20 new analogue drugs

Analogues Why are analogues a problem?

Analogues Why are analogues a problem?

Analogues Why are analogues a problem? Doses and contents unknown and vary

Combined with other chemicals (both active and inactive)

Listed contents inaccurate

Easy access

Easy access for all ages

No drug “dealer”

Analogues Where to next? •Will a return of MDMA, make the problem disappear? Tryptamines

Cathinones

BZP

Phenethylamines

Synthetic Cannabinoids

•Over 450 Synthetic cannabinoids, steroids, human growth hormones, ketamine, cocaine, pharmaceuticals, weight loss products etc…………

Analogues Where to next?

Analogues What are we doing to control analogues in Australia? •Listing all new substances as they arise can be time consuming and substance popularity can be short-lived.

Analogues What are we doing to control analogues in Australia? •Listing all new substances as they arise can be time consuming and substance popularity can be short-lived. •Using Analogue Provisions (differs in each state jurisdiction and Federally). A chemical which has “a substantially similar chemical structure to the substance, but differing in elemental composition due to the addition, deletion or replacement of any substituent element or group”

Analogues Issues meeting Legal Definitions • Chemical structure must be unambiguously determined This cannot always be determined by GCMS. Access to Standards to confirm this is not always possible. How far can a chemist go in saying something is substantially similar. O Me N

O

O

PAPP

O Me

Cathinone NH2

Analogues What are we doing to control analogues in Australia?

Analogues What are we doing to control analogues in Australia? •Listing all new substances as they arise can be time consuming and substance popularity can be short-lived. •Using Analogue Provisions (differs in each state jurisdiction and Federally). A chemical which has “a substantially similar chemical structure to the substance, but differing in elemental composition due to the addition, deletion or replacement of any substituent element or group” and/or having “substantially similar pharmacological effects” to a listed controlled substance

Analogues What are we doing to control analogues in Australia? •Listing all new substances as they arise can be time consuming and substance popularity can be short-lived. •Using Analogue Provisions (differs in each state jurisdiction and Federally). A chemical which has “a substantially similar chemical structure to the substance, but differing in elemental composition due to the addition, deletion or replacement of any substituent element or group” and/or having “substantially similar pharmacological effects” to a listed controlled substance

Structural similarity to a controlled drug does not guarantee activity eg phenethylamine

Analogues How do we keep pace? •DrugSAG committed to exchanging information about new substances as they are detected locally.

Analogues How do we keep pace? •DrugSAG committed to exchanging information about new substances as they are detected locally. •Use international databases and discussion forums to help identify unknowns.

Analogues How do we keep pace? •DrugSAG committed to exchanging information about new substances as they are detected locally. •Use international databases and discussion forums to help identify unknowns. •Share information with other agencies (in SA created SADEWS).

Unusual Seizure Alert Pills containing 2C-C and 2C-E

Contents of Seizure Seven whole light blue/purple speckled pills, which were poorly formed, each impressed with a “2-stripe” design.

Comments about the Seizure The tablets were irregular in shape and crumbly, however all seven pills visually appeared the same. Analysis of two individual pills revealed two distinct results. Pill one contained caffeine, dextromethorphan and 2C-C (2,5-dimethoxy-4-chloro-phenethylamine). 2C-C is a short-acting (4-8 hours) psychedelic chemical with a dosage of generally between 20-40mg. It is structurally similar to the more commonly encountered phenethylamines 2C-B and 2C-I. However it appears to be more powerful and longer acting than these two chemicals. The onset of effects can be delayed by 1-2 hours after consumption. Pill two contained dextromethorphan and 2C-E (2,5-dimethoxy-4-ethyl-phenethylamine). 2C-E has an effective duration of between 8-10 hours and a dosage of between 10-25mg. It is a strong acting psychedelic with effects becoming too intense and adverse at doses higher than 25mg, which can also increase the duration of effects.

Conclusions This seizure represents the first time that 2C-C and 2C-E have been detected in South Australia however, at this stage, this is an isolated seizure. Detections of 2C-C and 2C-E have been rare internationally and little is known about either chemical. This seizure follows a trend in the detection of “analogue” type chemicals in pills and capsules since a global Ecstasy (MDMA) shortage became apparent locally in the latter part of last year. Some of the “analogue” type chemicals recently detected locally include mephedrone (4-methylmethcathinone), 2C-I (2,5dimethoxy-4-iodo-phenethylamine) and 3,4-methylenedioxymethcathinone (methylone). Psychedelic chemicals are best described as enhancing visual and auditory perceptions/experiences and can create distortions but would not be considered truly hallucinogenic. While 2C-C is explicitly listed in the Controlled Substances (General) Regulations 2000, 2C-E is not. 2C-E however could conceivably be considered as an analogue of the listed chemical 2,5-dimethoxy-4-methyl-phenethylamine.

Analogues How do we keep pace? •DrugSAG committed to exchanging information about new substances as they are detected locally. •Use international databases and discussion forums to help identify unknowns. •Share information with other agencies (in SA created SADEWS). •Gather intelligence information from other sources.

Excretion (mg/d/1000 people)

Designer drugs in 2009-2011 wastewater

1. Population drug use in Australia: a wastewater analysis. Irvine RJ, Kostakis C, Felgate PD, Jaehne EJ, Chen C, White JM. Forensic Sci Int. 2011 Jul 15;210(1-3):69-73. Epub 2011 Mar 9 2. Marked Decline in 3,4-Methylenedioxymethamphetamine (MDMA) Based on Wastewater Analysis. Chen C, Kostakis C, Harpas P, Felgate PD, Irvine RJ, White JM. J Stud Alcohol Drugs. 2011 Sep;72(5):737-40

Analogues How do we keep pace? •DrugSAG committed to exchanging information about new substances as they are detected locally. •Use international databases and discussion forums to help identify unknowns. •Share information with other agencies (in SA created SADEWS). •Gather intelligence information from other sources. •Advise, inform and influence relevant authorities.

Analogues How do we keep pace? •Initial Toxicological screen did not pick up 25B-NBOMe

2C-B

Analogues Questions?

www.anzfss2014.com.au