Stimulants

Question 1

Ephedrine and psuedoephedrine

Answer 1

From epehdra plant

used for cough, flu, allergies and asthma

synthesised in 1885 in japan and mass produced in 1920 in china.

Vicks made a nose drop of ephedrine in 1948 - now withdrawn

both compounds cause peripheral sympathomimetic effects and CNS stimulation through their adrenergic agonism

can be used for meth synthesis

due to these effects, pseudo is limited to 720mg and ephedrine for 180mg per sale in the UK

Question 2

Khat

Answer 2

a plant found in east africa and southwest arabia.

contains cathinone - B-keto-amphetamine

some structural overlap with bupropion.

similar pharmacology to amphetamine but more mild

Question 3

Amphetamine and meth

Answer 3

amphetamine synthesised in 1887 and then marketed as benzedrine in 1933. in 1936 used for narcolepsy, and fro 1937 identified to help attention in school children with behavioural problems

meth synthesised in 1938 in germany.

both meth and amphetamine were used extensively in ww2 - meth axis, amphetamine - allies

meth also likely used in the 1954 world cup by west germany. pretended it was vit c injections

Inhibit DAT and VMAT - increased dopamine

Question 4

methylphenidate

Answer 4

first synthesised in 1944 and used in 1854 for psychiatric disorders: ADHD narcolepsy.

dose dependent effects.

DAT and NET blockade

Question 5

modafinil

Answer 5

developed in the 1970s and approved by FDA in 1998. used for narcolepsy.

wakefulness-promoting instead of stimulant.

acts via a1B-AR agonism

used as nootropic and by military in 1st gulf war

Question 6

PMA/PMMA effects and reason for production

Answer 6

Following 50 ton seizure of sassafras oil (safrole for MDMA production, production was swapped with anethole (from anise and fennel). this produced PMA and PMMA precursors instead of MDMA.

less potent then MDMA but more toxic

Question 7

Mephedrone

Answer 7

4-MMC, produced as a legal high in china from 2008. bought on the internet as “plant fertiliser”.

a cathinone-based drug

oral or nasal administration to cause increased locomotor activity and similar effects to other stimulants

5HT and dopaminergic effects. more dopaminergic than MDMA. middle ground between amphetamine and MDMA - neurotoxic

Question 8

a-PVP

Answer 8

flaka - synthesised in 1963 and identified in drug seizures in 2011 from france. stimulant effects with psychotic episodes, anxiety, and hallucinations reported from hospitals

NDRI mechanism

Question 9

statistics of stimulant use

Answer 9

amphetamines quite prevalent, with usage highest in early 2000s. continuous decrease in amphetamines use since early 2000s.

meth use very low in the UK, same with mephedrone (especially after making it illegal in 2010)

amphetamines remain the stimulant causing most deaths over cathinones, however use is also much higher than cathinones. approx 100 deaths from amphetamine last year and about 10 from cathinones