26: Stimulants and Psychotomimetics Flashcards
central effects of amphetamines and related compounds
locomotor stimulation euphoria and excitement insomnia increased stamina anorexia anxiety, irritability, panic, paranoia
amphetamines and related compounds release
dopamine and noradrenaline from nerve terminals
how do amphetamines release DA and NE
- competitive inhibitors of monoamine uptake transporters DAT and NET
- are taken up into neuronal storage vesicles by VMAT2 and displace endogenous monoamines from vesicle into cytoplasm
- cytoplasmic monoamines transported out of nerve terminals by DAT and NET working in reverse
- can inhibit MAO at high conc
DA and NA release caused by amphetamines cause
locomotor and rewarding effects
peripheral effects of amphetamines are generally
mainly sympathomimetic
specific peripheral effects of amphetamines
increase BP and HR
reduce GI motility
what happens when you stop amphetamines
deep sleep
lethargy, depression, anxiousness, hunger on wakening
dependence develops as
dose is increased
uncontrolled binges cause
high risk for acute toxicity
- tachycardia
- hypertension
- hyperthermia
- rhabdomyolysis
what is used for ADHD
dextroamphetamine
mephedrone is a
cathinone derivative
cathinone and cathine are active ingredients in
khat shrub
mephedrone, methedrone, and methylone are
cathinone derivatives that produce amphetamine like effects
mechanism of action for cathinone derivatives
increase EC levels of DA and 5HT by inhibiting their reuptake and enhancing release
methylphenidate is also called
ritalin
methylphenidate mechanism
inhibits NET and DAT transporters
inhibits SERT. but not as potent as NET and DAT
modafinil is used for
narcolepsy
mechanism of modafinil
blocks DAT and DA reuptake
cocaine plant
south american coca shrub
mechanism of cocaine
inhibits NET, DAT, and SERT
cocaine resembles amphetamines but has less
stereotyped behaviour, delusions, paranoia, hallucinations
excessive dose of cocaine causes
tremors, convulsions, respiratory and vasomotor depression- generally sympathetic
2 main methylxantines
caffeine and theophylline
methylxantine side effects
diuresis
stimulation of cardiac muscle
relaxes smooth muscle- bronchioles