““Bath Salts”Bath Salts”The synthetic cathinoneThe synthetic cathinone

Drugs of abuseDrugs of abuse

Ryan Gregg

Doctoral Candidate, CSAR, TUSMtud51613@temple.edu

Thursday, April 24th 2014

Give me your thoughts:Give me your thoughts:

For the first 5 minutes of class, give me your thoughts on the following question:

What do you typically think of when you hear the term “designer drugs”? What about the term “research chemical”? Are they more or less dangerous? What type of people abuse them? Can you become addicted to designer drugs?

OutlineOutline

• Chemical classification• History of synthetic cathinones• Neurological and pharmacological effects of “Big 3”• Prevalence/Legality• Clinical observations• Trends in new and emerging cathinones• Discussion

Synthetic CathinonesSynthetic Cathinones

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Synthetic Cathinones: Novel PsychostimulantsSynthetic Cathinones: Novel Psychostimulants

• New class of designer psychostimulants known on the streets as “plant food” or “bath salts”

• Beta-ketone amphetamines

• Popularized as “legal high” alternatives in head shops and Internet sites

Mephedrone

MDPV

Methylone

Cathinone

Methcathinone

Amphetamine

History: CathinoneHistory: Cathinone

• Cathinone is the primary psychoactive component of the plant Catha edulis aka khat

• Native to North Africa and the Arabian peninsula

• Leaves are chewed for their stimulant properties

Catha edulis

Yemenese man chewing khat leaves

History: Cathinone and MethcathinoneHistory: Cathinone and Methcathinone

• Cathinone produces stimulant-like profile similar to ephedrine

• Methcathinone, the alpha methylated version of cathinone, was synthesized in the US in 1928 and patented in the US in 1957 80 million yuan ($12.6 million US)

seized in China in 2011 from organized crime selling methcathinone

Revival: Mephedrone, MDPV, MethyloneRevival: Mephedrone, MDPV, Methylone

• Mephedrone, MDPV, and methylone were synthesized in the 1960s, but re-emerged in 2003

• Online designer drug communities linked to rapid rise in use worldwide

• Commonly substituted for older abused drugs by dealers

• Online drug markets offered mephedrone, MDPV, and methylone alone or in brand-name formulations for cheap prices

Revival: Mephedrone, MDPV, MethyloneRevival: Mephedrone, MDPV, Methylone

MephedroneMephedrone

• Classified as a substrate-type releaser

• Produces release of dopamine (DA), serotonin (5-HT) and norepinephrine (NE)

• Order of potency: – DA>NE>>5-HT

MDPVMDPV

• Potent monoamine reuptake inhibitor at monoamine transporters

• Order of potency: – DA=NE>>>5-HT

• More potent than cocaine

MethyloneMethylone

• Classified as a monoamine substrate-type releaser

• Order of potency– 5-HT>>>DA>NE

• More potent 5-HT release than MDMA

Big 3 ComparisonBig 3 Comparison

Drug Mechanism Monoamine Preference

Mephedrone Substrate releaser DA>NE>>5-HT

MDPV Reuptake inhibitor DA=NE>>>5-HT

Methylone Substrate releaser 5-HT>>>DA>NE

Synthetic Cathinones: Legality and PrevalenceSynthetic Cathinones: Legality and Prevalence

• Gradually made illegal in UK and Europe from 2009-2010

• Mephedrone, MDPV and methylone given emergency Schedule I distinction in September 2011– Permanent Schedule I status in

July 2012 • Federal Analog Act, an amendment

to the CSA, allows for any compound “substantially similar” to a Schedule I compound to be labeled Schedule I

President Richard Nixon with AG John Mitchell and first DEA president Jack Ingersoll signing the Controlled Substance Act into law

Synthetic Cathinones: Legality and PrevalenceSynthetic Cathinones: Legality and Prevalence

• Mephedrone was reported as the 6th most commonly abused drug in the UK in 2012

• Mephedrone is more popular in UK, MDPV and methylone more popular in the US

• Poison control centers report over 9,800 exposures from 2011-2013 in US

• ~23,000 emergency room visits in US in 2011

Reported Effects in Human AbusersReported Effects in Human Abusers

Positive effects•Euphoria•Pro-social/Empathogen

– Mephedrone/Methylone

•Increased alertness, arousal, and concentration

– Mephedrone/MDPV

•Some reports of hallucinations and sexual stimulation

Negative effects•Tachycardia and heart palpatations•Excited delirium and severe psychosis•Serotonin syndrome•Severe hyperthermia•Tissue necrosis (intranasal)•Addiction/dependence•Intense craving to redose•Rhabdoymyolysis

Reported Effects in Human AbusersReported Effects in Human Abusers

• Users commonly go through “binge” periods of bath salt use• High potential for overdose with heavy use

– Overdose- cardiac arrest following tachycardia or overheating

• OD’s treated symptomatically with benzodiazepines, activated charcoal, ice baths

• Several clinicians have reported abusers of synthetic cathinones have met DSM-V criteria for dependence

Synthetic cathinone abuse liabilitySynthetic cathinone abuse liability

Synthetic Cathinone: At-risk populationsSynthetic Cathinone: At-risk populations

• Mephedrone and methylone are especially popular in rave/nightclub cultures in the UK– Especially prevalent 18-25 year white old males

• The novelty of designer cathinones prevents many forensic labs and drug testing companies from screening for it with blood/urinalysis

• Higher than normal population of abusers in following groups: – Active and retired military members– Amateur and professional athletes

Bath Salts Zombie Theory: ExplainedBath Salts Zombie Theory: ExplainedSymptomatology:•Psychosis- Derived from severe hyperthermia in brain areas controlling cognition•Tissue necrosis- Often found with unpure products via intranasal or intravenous administration causing cell death

Discussion: Drug Policy in the United StatesDiscussion: Drug Policy in the United States

Taken from NIDA presentation in 2004

Stats taken from Drug Policy Alliance: -Number of people arrested in 2012 in US for non-violent drug charges: 1.55 million-Number of people who died from OD in 2010: 38,329