midterm 2: 5, 6, 10 Flashcards
common characteristics of psychomotor stimulants
stimulate transmission at synapses that use E, NE, DA, or 5-HT as transmitters
monoamines/ biogenic amines (4)
E, NE, DA, (catecholamines) and 5-HT (indolamine)
are amphetamines synthetic or naturally occuring?
synthetic
Adderall is what psychomotor stimulant?
dl-amphetamine
use of dl and d-amphetamine (Adderall) (2)
(1) ADHD treatment and (2) narcolepsy treatment
Dexedrine
d-amphetamine
Methedrine or Desoxyn
methamphetamine
use of methamphetamine
(1) ADHD treatment and (2) obesity treatment
recrystallized methamphetamine powder is known as
crystal ice or crystal meth
synthetic drugs similar to cocaine (2)
methylphenidate (Ritalin) and pipradrol Meratran)
Ritalin used to treat ____
ADHD
Meratran used to treat symptoms of ____
senile dementia
bupropion (syntehtic derivative of cathinone)
a drug used as both an antidepressant and a smoking cessation aid
amphetamines are weak ___ with a pKa of between
bases; 9 and 10
what happens when amphetamines are taken orally?
tend to be ionized in the digestive system, which slows the rate of absorption
amphetamines are more potent when administered by (3)
injection, inhalation, or snorting
When given for medicinal purposes or to prevent sleep and fatigue, am- phetamines are always administered _____ and the decrease in potency can be compensated for by ______.
orally; increasing the dose
advantage of oral admin of amphetamines
blood levels may be kept fairly constant without too much variation over time
When amphetamines are taken for the rush they produce, they are administered _____, which causes the _____ required for this effect.
by injection; sudden high blood levels
pKa of cocaine
8.7
crack
cocaine HCl mixed with a solution of baking soda (sodium bicarbonate)
what does the baking soda base of crack do
removes the ionic charge from the molecules of cocaine and increases its lipid solubility
factors affected the absorption rate of amphetamines taken orally (2)
(1) food in the stomach and (2) degree of physical activity
when is peak blood level of amph reached when taken orally?
30 min - 4 hours
when is peak blood level of cocaine reached when taken intranasally (sniffing)?
10-20min
distribution: amphetamines, cocaine, and other drugs in this class cross the blood–brain barrier and are concentrated in the (3)
spleen, kidneys, and brain
excretion of the amphetamines depends to a very great extent on ___
the pH of the urine
when it is acidic, it gets ionized and excreted in the urine
when it is more basic, excretion falls to metabolism in the liver which extends its halflife from 7-14 hours to 16-34 hours
excretion of amphetamine
urine, metabolized in liver, sweat, saliva
Cocaine is excreted much ____ (faster/slower) than the amphetamines.
faster
half-life of cocaine
45-75 min
also depends on urine pH
general psychostimulant mechanism (maybe?)
cause higher dopamine concentrations int eh synaptic cleft
either block reuptake (cocaine) or reverse the function of transporters on the presynaptic cell that usually reuptake but not expel more DA (amphetamine)
how does cocaine also function as a local anesthetic?
blocks Na+ ion channels, blocking APs along nerve axons
psychomotor stimulants activate the ____ NS
sympathetic (increase HR, BP, vasodilation and bronchodilation)
what is the psychomotor stimulant effect useful for treating asthma
bronchodilation
what is a possible mechanism for reduced food consumption as an effect of psychomotor stimulants?
stimulates engagement in behaviours other than eating; miss food consumption
maybe serotonin (5-HT)??
why were amphetamines used during WWII?
sleep prevention, block fatigue, increase concentration
most noticeable effect of iv amph and cocaine
improved mood (well-being and exhilaration)
factor affecting subjective effects of amph
expectation
coke-out
acute tolerance to cocaine (lasts 24 hrs)
tolerance to subjective effects but not to the effects on BP and HR
dangerous
pre-exposure to amphetamine decreased ______, but not ______
potency, effectiveness
which effect of amphetamine does not show chronic tolerance
blocking of sleep
reverse tolerance or sensitization: which amph effects
stereotyped behaviour and psychotic behaviour
reverse tolerance or sensitization: which cocaine effects
convulsions, electrical activity within the brain, stereotyped behaviour, spontaneous motor activity
what causes sensitization to cocaine and amph?
increased sensitivity of the mesolimbic DA system
withdrawal from amph and cocaine
not associated with severe or medically serious withdrawal
can experience depression
crash or comedown
period of depression and lethargy after a single dose of amph or cocaine (severity determined by dose and duration of intake period)
this is immediatly relieved by another admin of the drug
when is withdrawal from a single dose of cocaine?
within 30 min
when is withdrawal from a single dose of amph?
number of hours
After chronic heavy use, abrupt discontinuation of amphetamine or cocaine use will cause withdrawal symptoms within ____ of the last dose
24 hours
The DSM-IV-TR criteria for diagnosing amphetamine withdrawal include:
depression, fatigue, vivid or unpleasant dreams, insomnia or hypersomnia, increased appetite, and psychomotor agitation or retardation
speed ball
a combination of cocaine (or amphetamine) and heroin.
heroin reduces the jitteriness that cocaine arouses by stimulating the sympathetic nervous system, and the cocaine diminishes the sleepiness or nod caused by heroin.
