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Phys/Pharm Drugs Of Abuse > Novel Psychoactive Substances > Flashcards

Novel Psychoactive Substances Flashcards

1
Q

A timeline of drug control

A

1868: post isolation of morphine + coke Pharmacy Act: Opium sold only by pharm (kept records)

1908: Post heroin synthesis: pharm act: Morphine and Cocaine (and derivatives with more than 1%) sold only by pharmacist

1916: post MDMA synth + beg WW1: Defence of the Realm act- Offence for non-pharmacists or doctors to be in possession of cocaine – first time Home Office
becomes involved

1928: Dangerous Drugs act: Criminalising possession of cannabis –
responsibility moved to
Home from Health
ministry

1964: Post synth of Mephedrone + LSD - Drug Prevention of Misuse Act:
Amphetamines
criminalised – amended to include LSD in 1966

1977: MDMA illegal
2003: Meph. re-synth

2016: Psychoactive Substances Act

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2
Q

What was happening in history? (3)

A
  1. Chemists would synthesise a new drug – it would be unscheduled and therefore legal.
  2. Drug sold legally until the government managed to get it into the controlled drugs
    category - it would then
    become illegal
  3. A new drug would be
    synthesised and the cycle continues
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3
Q

The Psychoactive Substances Act 2016

A
  • Legislation varies internationally – in the
    UK it is now illegal to distribute or sell
    novel psychoactive substances, but
    possession is not a criminal offence
  • The Psychoactive Substances Act 2016
    criminalises any substance intended for
    human consumption that has a psychoactive effect…

It covers substances by virtue of their psychoactive properties, rather than the identity
of the drug or its chemical structure

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4
Q

Novel psychoactive substances =

A

compounds (former legal highs) designed to mimic existing established recreational drugs

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5
Q

Novel psychoactive substances can be grouped into four main categories… (4)

A

Stimulants (cathinone - methadone) -ST+LT

Depressants (opioids and benzo’s) - LT

Hallucinogens (psychedelics (2C family) + dissociative (-KET/PCP)

Cannabinoids (cannabis)

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6
Q

What is classified as a psychoactive substance?

A

A psychoactive substance is any substance which is: ‘capable of producing a
psychoactive effect in a person who consumes it’.

  • talks about property and not the specific drug name
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7
Q

What did the act try to do? (4)

A

make it an offence to: produce, supply, possess with intent to supply, import or export
psychoactive substances

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8
Q

How are psychoactive properties of a novel psychoactive substance assessed under The Psychoactive Substances Act 2016? (4)

A

Receptor binding assay
(to determine whether the drug binds to a receptor)

Functional assay
(to determine whether the drug activates a response following
interaction with the receptor)

OR

Published literature

Accounts from a witness of behaviour exhibited by an individual who has
taken the substance may also be relevant

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9
Q

Receptor binding and functional assays drug e.g.’s (7)

A

Immobilising cells that express specific receptors, exposing them to a drug and measuring the response:

  • CB1 (cannabis and synthetic cannabinoids)
  • GABAA (benzodiazepines)
  • 5-HT2A (e.g., psychedelics)
  • NMDA (dissociative/hallucinogenic drugs e.g., ketamine)
  • μ-opioid (opioid drugs e.g., heroin)
  • Monoamine transporters (psychostimulants e.g., MDMA, cocaine)
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10
Q

Published literature and witness accounts (3)

A

In vitro tests are not suited to all types of substance (e.g., nitrous oxide and solvents) – alternative sources of evidence are therefore required.

Published literature: Wealth of evidence available on both in
vitro and in vivo studies by academic
researchers which can be referenced by
expert witnesses

FINAL:=
Accounts from a witness of behaviour exhibited by an individual who has taken the substance may also be relevant

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11
Q

What was legal? pre 2016 (3)

A

everything except:

Classes A-C
Schedules 1-5

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12
Q

What is legal? post 2016 (6)

A

everything is illegal except:

Alcohol
Caffeine
Food
Nicotine
Medicinal products
(controlled substances)

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13
Q

Is The Psychoactive Substances Act 2016 working? (4)

A

Before act: Total of 113 shops selling psycho. substance on internet in English + shipped to UK

After act: Only 52% remained open – those that remained were either based overseas
(65%), became a ‘headshop’ (19%) or were
inactive (16%)

Only 24% of UK-reg websters remained open after

unknown whether the UK retailers have ceased
selling or have been displaced to underground
markets (street level dealing or the hidden web

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14
Q

introduction to mephedrone (4)

A

Mephedrone is a synthetic cathinone – also known as ‘bath salts’, ‘plant food’ and ‘Meow-Meow’ (related to khat)

  • Abused due to their psychostimulant and
    hallucinogenic effects – similar to cocaine, MDMA, amphetamines and methamphetamines
  • Serious side effects including increased heart rate, chest pain, change in body temperature (sweating chills), insomnia, amnesia and seizures
  • Target of intense media interest – classified as a Class B substance under The Misuse of Drugs Act 1971 in April 2010
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15
Q

Mephedrone MoA: (3)

A
  • Mephedrone is a non-competitive blocker
    of the DAT + (NET) and (SERT)
  • This means less DA, NA and 5-HT are taken up into the pre-synaptic
    terminal
  • This leads to an increase in DA, NA
    and 5-HT in the synaptic cleft, leading to increased DA, NA and 5-
    HT post-synaptic receptor activation
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16
Q

Relative 5-HT/DA activity (determined by the DAT:SERT ratio) can be helpful in predicting
psychoactive effects, toxic effects and potential for addiction (4)

A

Low DAT/SERT inhibition ratio (<0.1) indicates tenfold greater relative 5-HT vs DA activity similar to MDMA

High DAT/SERT inhibition ratio (>10) indicates greater relative DA vs 5-HT activity similar to
methamphetamine

Mephedrone falls between MDMA
and methamphetamine ratios

This corresponds with the psychoactive effects of mephedrone

17
Q

Mephedrone Phys effects (3)

A

inc seizures
dec body temp - sweats
inc BP = tachycardia

18
Q

Mephedrone behavioural effects (3)

A

social : elated mood + impulsivity

cognitive: impairment of function (upon chronic use)

binging

19
Q

Alexander Shulgin

A
  • In 1991, Alexander Shulgin, along with his wife Ann, published PIHKAL, A Chemical Love Story (acronym representing ‘Phenethylamines I Have Known And
    Loved’)
  • Book detailed synthesis instructions for over 200
    psychedelic compounds including bioassays, dosages+ other commentaries
  • ‘Shulgin rating scale’ was used to report the
    subjective effect of psychoactive substances at a given dosage:
    -, +,++,+++,++++
  • Included the ‘2C’ series…
20
Q

2C series (3)

A
  • ‘2C’ is in reference to an acronym invented
    by Shulgin to describe the two carbons
    between the amino group and the
    benzene ring in the chemical structure
  • Designer substitution to the 2C structure
    can result in increased hallucinogenic
    activity

e.g. additions of methoxy groups at the 2 and 5 positions on the base structure ring or the substitution of iodine (6-10hrs) or bromine (4-8hrs) at the 4 position results in increased hallucinogenic effects

21
Q

2C-B and 2C-I (4)

A

two compounds have structures that are truly analogous.

strategically located iodine atom and an identically placed
bromine atom in other

directly above and below one-another in the periodic table. And what is particularly maddening to the synthetic diddler, is that they cannot be lengthened, or shortened, or squashed around in any way.

You can’t make a longer and narrower version of a bromine atom, as you can do with, say, a butyl group. You’ve got what you’ve got, like it or not

22
Q

‘2C’ series MoA (3)

A
  • A clear mechanism of action for the ‘2C’ series yet to be established
  • However, ‘2C’ compounds are partial
    agonists for different subtypes of 5-HT
    receptors – specifically 5-HT2A , 5-HT2B
    and 5-HT2C receptors
  • ‘2C’ compounds have also been shown to
    inhibit SERT, and to a lesser extent, NET and DAT – however, very low potency

Phys/Pharm Drugs Of Abuse (23 decks)

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