Chapter 6 - Psychostimulants Flashcards
What do sympathomimetics do?
increase sympathetic NS activity; inc motor activity; improve alertness; elevate mood
ex. amphetamine, methamphetamine; cocaine
medical vs non medical purposes of sympathomimetics
decongestant, ADHD, narcolepsy VS meth, crack, cocaine
First natural amphetamines were derived from ____ and was used as ____
Ephedra (ephedra sinica); cough suppressant (16th century China) and was a precursor for the illicit manufacture of methamphetamine
Amphetamine was developed by ____ and was used to ____
German chemists in 1887; inc BP (20s), treat adhd (30s) and in WWII
Two optical isomer forms of amphetamines
d-amphetamines and l-amphetamines; d is more potent
Racemic mixtures of amphetamines
contains both d- and l- isomers
ex. adderall contains 3:1 of d- to l-
-mostly used for narcolepsy and ADHD; less military use
Methamphetamine was developed by ____ and is mainly used ____
a JPN chemist in 1919; illicitly (notorious drug of abuse) but was recently approved by FDA as treatment for ADHD (Desoxyn)
Methylphenidate
relatively weaker psychostim; discovered in 1944 (Ritaline); prescribed to more than 2/3 US kids with ADHD
Cathinones
bath salts (new drugs, 90s); synthetic cathinone compounds
what is cocaine?
derived from Erythroxylon coca; salt/powder form is called cocaine hydrochloride
-crack cocaine is formed when hydrochloride is freed from base with baking soda
For therapeutic effects, psychostimulants are usually administered ____
orally (pills); however methylphenidate sometimes liquid and skin patch form
Why do users (for rewarding effects/illicit use) prefer intravenous injection/insufflation/inhalation?
these routes guarantee rapid absorption
inhalation: 1.4min
IV: 3.1min
Insufflation: 14.6min
The ____, the more likely is it for addiction to occur
quicker the route of administration
There are active metabolites for ___, ____, and ____
mathamphetamine, cathinone, and cocaine
-often have similar effects as original drug
____ use can also result in stronger active metabolites
polydrug
ex. cocaine and alcohol produces the metabolite cocaethylene which has greater rewarding properties than either drug alone
half lives of psychosimulants
methamphetamine = 11 hours
amphetamine = 10 hours
methylphenidate – 2.5 hours
cathinone = 1.5 hours
cocaine = 1 hour
amphetamine and methamphetamine increases DA levels in the synapse by 1. ____ and 2. ____
- reversing the direction of DA transporters found on the presynaptic cell
- displacing DA from synaptic vesicles which allows more DA to be released through the reversed transporters
pharmacodynamics of methylphenidate and cathinones
similar to amphetamine and methamphetamine; inc levels of monoamines DA, 5HT, NE; less efficacy than amphetamine