Week 5: Cocaine & Psychomotor Stimulants Flashcards

1
Q

What’s one thing in common with stimulants

A
  • They all stimulate transmission of monoamines
    (eg. epinephrine, norepinephrine, dopamine, serotonin)
  • They are sympathomimimetic
    (aka mimic sympathetic arousal - and epinephrine is the primary transmitter in the sympathetic nevous system
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2
Q

sources and history of stimulants

A
  • some stimulants aren naturally-occuring, others are new synthetic drugs
  • naturally occurring stimulants have been used for centuries
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3
Q

Amphetamines

A
  • are synthetic stimulants
  • there’s two types
    1. Amphetamine
    2. Methamphetamine
  • These are used to treat ADHD, Narcolepsy and obesity
  • Methamphetamine can be synthesised from legally available materials (sold as meth, ice crystal)
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4
Q

Background of Amphetamines

A

-Ephedrine (found in the herb ma huang) has been used in china for over 5,000 years
- was isolated from the 1880s
- Propoerties investigated in 1924 by Ko Keui Chem and C.F Schmit. Found the structure and action is very similar to epinephrine

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5
Q

Ephedrine

A

-Ephedrine (found in the herb ma huang) has been used in china for over 5,000 years
- was isolated from the 1880s
- Properties investigated in 1924 by Ko Keui Chem and C.F Schmit. Found the structure and action is very similar to epinephrine

isolated Ephedrine
- Is more stable than epinephrine (then used to treat asthma). Could be administered in pill form and had a longer duration of action, less toxic
- use became so widespread it was feared that supplies would run out
- so there was a search for a synthetic substitute.
The first synthetic emphetamine was synthesised in 1887. But it remained untested until 1910 and was suggested as a substitute for ephedrine in 1927

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6
Q

Development of synthetic amphetamine history

A

-Ephedrine (found in the herb ma huang) has been used in china for over 5,000 years
- was isolated from the 1880s
- Properties investigated in 1924 by Ko Keui Chem and C.F Schmit. Found the structure and action is very similar to epinephrine

isolated Ephedrine
- Is more stable than epinephrine (then used to treat asthma). Could be administered in pill form and had a longer duration of action, less toxic
- use became so widespread it was feared that supplies would run out
- so there was a search for a synthetic substitute.
The first synthetic emphetamine was synthesised in 1887. But it remained untested until 1910 and was suggested as a substitute for ephedrine in 1927

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7
Q

History of Amphetamine in the 1900’s

A
  • In 1937 the American Medical Association authorised use of amphetamine for treatment of naroclepsy and as a stimulant for depression
  • By 1943, at least half the sales were prescribed for weight loss and diet control, antidepressent and stiulant effects and extended periods of alertness
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8
Q

Amphetamines today

A

Today many countries strictly regulate the manufacture and marketing of amphetamines
- generally prescribed for ADHD and narcolepsy

Not widely used for medicinal purposes today
- most amphetamine and methamphetamine are made in illicit labs

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8
Q

Cocaine

A
  • Extracted from the leaves of the coca bush (Erythroxylum Coca), native to south America.
  • For centuries these leaves have been chewed by various south American tribles
  • There’s even archeological evidence too show this (with face mask type models showing a lump for the coca leaf being chewed)
  • Incas began using the plant when they conquered the region in the 10th century in Peru. The coca was sacred and used by priests and nobility. Also used in ritual human sacrifice as it made people docile. This has been evidenced in mummified human remains
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8
Q

What effect does cocain have when it’s on your tongue

A

Cocaine numbs your tongue. This is why people test the quality of cocaine by putting it on their tongue

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8
Q

What happened with Cocaine when the Spanish Conquered the Incas?

A

When the spanish conquered the inacas, they banned coca use;
- picked up on it after they found it useful in commerce
- also found they could work slaves longer and harder and needed to feed them less if on coca. Potosi Silver Mine - Some 8 million incan and African slavees died during the Spanish colonial period

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8
Q

Cocaine after the 1700’s

A

Cocaine was classified as a stimulant in 1749
- Europeans had no interest in the drug until it was isolated (as they didn’t wan to chew it)

So, Albert Neimann isolated and named the substance cocaine in 1860

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8
Q

People who have used Cocaine

A

Cocaine has largely been used by professionals and intellectuals
eg. Freud - said it was a cure for many conditions like addiction and depression
eg. Robert Louis Stephenson
eg. Arther Conan Doyle’s Sherlock Holmes
eg. Karl Koller - found cocaine could be a useful as an anaesthetic and is still it’s only medical use

Cocaine has then become widely available in general purpose formulations
eg. toothache drops
eg. hair product for growth and shine
eg. soothing syrup for teething children
eg. as an anti-anxiety, nerve calming drug
eg. the pop used it in his fav wine tonic

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9
Q

Coca Cola and Cocaine

A

In 1886 John S. Pemberton made a drink of the Kola nut extract, adding soda water etc - he called it coca cola and to this day coca cola is made with coca leaves

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9
Q

Cocaine in the 20th century

A
  • In the early 20th century, there was a growing backlash against cocaine
  • included in the Harrison Narcotic Act of 1914, effectively banning its use
  • Began being used underground where it was used by artists, musicians, and wealthy upper class whites
  • After WW2 the ides of stimulants was common
    Cocaine use spread and increased
    Has gone down in recent years
    Appears to be creeping up in NZ
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9
Q

Neurophysiology of Stimulants

A
  • All stimulants have a common effect on synapses that use the monoamine transmitters
  • they achieve this effect in different ways
    Reuptake inhibition (eg. cocaine)
    Substrate-type release (eg. methamphetamines)
9
Q

Reuptake inhibition (eg. cocaine)

A

Cocaine blocks reuptake channels in the presynaptic membrane. This means that neurotransmitter is left in the cleft longer as it cannot be reuptaken in the presynaptic membrane

9
Q

Substrate-type release (eg. methamphetamines)

A

Meth will pump NT out of the presynaptic vesicles. This becomes toxic as the contents of vesicles shouldn’t be able to free-float in the presynaptic membrane

10
Q

Affinity for Cocaine and different Monoamine Transporters (MATS)

A

NETS > DATS >SERTs

(norepinephrine transporter, dopamine transporter, serotonin transporter)

11
Q

Amphetamine and affinity for MATS

A

NETS > DATS > SERTS
Norepinephrine transporters, dopamine transporters, serotonin transporters

12
Q

Cocaine and SERTS

A

Cocaine blocks serotonin transporters the same way as anti-depressents hence why Freud may’ve suggested it is a treatment for depression. However, it does not alleviate depression
The reason for this is unknown

13
Q

What determines the behavioural effect of stimulants

A

Behavioural effects of stimulants appear to be most related to their action on dopamine systems

14
Q

Effects of stimulants on the body

A

Increase heart rate and blood pressure and vasodilation
Increase bronchodilator (hence asthma application)
Reduce appetite and food consumption, mostly by stimulating other incompatible behaviours - missed food is made up for by excessive consumption later

15
Q

Effects of Stimulants on sleep

A
  • Produce insomnia - one reason for widespread use during WW2 and in the 1950s
  • Amphetamine, Methylphenidate, and modafinil are used to treat narcolepsy
16
Q
A