stimulants: cocaine and amphetamines

forms of cocaine

powder

freebase

crack

snorting powder

relatively slow way to get cocaine into the bloodstream

inhaling cacaine from heated crack

the cocaine is delivered to the bloodstream nearly as quickly as if injected

peak blood levels occur within several minutes and are much higher than similar dose of snorted powder

high only lasts ~30 mins

extremely rapid absorption occurs with…

iv injection and smoking

slow absorption occurs with…

snorting and oral use

cocaine inhibits the reuptake of … and …

NE and 5-HT

cocaine increases … levels by bidning to the plasma membrane … transporter and blocking reuptake of the neurotransmitter

DA

cocaine causes an

increase in the number of glutamate and increase in action potentials; more dopamine released

amphetamines

tyoically taken orally, IV, or injection

absorption from the GI tract is slow

IV injection provides a rapid and intense “high”

• greater addictive potential

methamphetamine

more potent

can be taken orally, snorted, injected intravenously, or smoked

amphetamines and methamphetamines are metabolized by the…

liver

methamphetamines and amphetamines have … half-lives than cocaine

longer

behavioral effects of amphetamines

alertness

increased confidence

exhileration

reduced fatigue

generalized sense of well-being

reduced sleep time, REM sleep

amphetamines are

indirect catecholamine agonists (stimulate DA and NE release)

chronic stimulant use effects

decreased DA synthesis

decreased DA release

less DAT binding

less DA receptor binding

decrease in postynaptic DA receptors

therapeutic uses for amphetamines and methamphetamines

narcolepsy

ADHD

appetite suppresant and anti-obesity treatment

ADHD

characterized by extreme inattentiveness, impulsivity, and hyperkinesis

Methlphenidate (ritalin)

activates catecholamnine transmission by blocking DAT and NET

increases extracellular levels of DA and NE

doesn’t increase DA release—solves potential for abuse