Pharm Stimulants Flashcards
1. List the prototype methylxanthines, describe their mechanism of action and pharmacological effects, and list their major side effects. 2. List the prototype psychomotor stimulants, cocaine, and nicotine, describe their mechanism of action and pharmacological effects, and list their major side effects. 3. Describe the pattern and nature of abuse observed with psychomotor stimulants, cocaine and nicotine, the degree of tolerance and dependence, and the treatment of the abuse. 4. Describe the
strychnine class
convulsant
picrotoxin class
convulsant
pentylenetetrazol class
convulsant
MOA of strycninie
blocks gly receptos in spinal cord resulting in disinhibition
MOA of picrotoxin and pentylenetetrazol
non-competitively blocks Cl-channels of GABA, resulting in disinhibition
sx of strychnine poisoning
( opisthotintus (tenatny) and risus sardonicus
treatment for strychninie poisoning
IV diazepam, reduced envoronmental stress and activated charchol
caffeiene class
methylxanthine
theophylline class
methylxanthine
theobromine class
methylxanthine
cognitive effetcs of methylxanthines
increases capacity for intellectual effort and decreases reaction time, decreases fine motor coordination, timing skills ans possibly math
CNS actions of methylxanthine
increase sensitivity of medullary respiratory centers to CO2 - increases ventilation
CV actions of methylxanthine
increase HR (slight), dialates peripherial vasculatire, constricts cerebral vasculature
muscle effects of methylxanthine
smooth - dilates brochioles
skeletal - increased capacity for work, some performance enhancing effects
GI effects of methylxanthine
stimulates peristalsis
MOA of methylxanthine at high levels
mobilization of intracellular Ca++/inhibits phostphodiasterase
clinical MOA of methylxanthine
antagonism of Adenosine receptors
presence of food in GI will do what with methylxanthine
reduce rate of absorption but decrease gut irritation
increases t 1/2 of methylxanthine
hepatic disease, pregnancy and OCPs
decreases t 1/2
smoking , phenytoin, barbos
methylxanthine t 1/2 is longest in
pre-term infants
sx of methylxanthine toxicity
nervousness, insomnia, delirium, convulsions, olfactory.gustatory hallucinations
caffiene can cause headaches in people who
are non-tolerent
varenicline MOA
partial agonistat nicotinic receptor
use of varenicline
smoking cessation
effect of varenicline
blunting of rewarding effects of nicotine
rimobabant MOA
atagonist/inverse agonistat CB1 cabbabinoid receptors
SE of rimonabant
depression and suicidal idealation
methylphenidate class
psychomotor stimulant
stereochemical form of psychomotor stiumulants most active
L version
most potent psychomotor stiumulants
meth
least potent psychomotor stiumulants
cocaine/methylphenate
CNS effects of psychomotor stiumulants
stimulate medullary respiratory centers, increase motor activity, elevate mood, reduce fatigue, insomnia
MOA of anphetamines
release catecholamines and 5-HT, inhibit reuptake of same
MOA of methylphidate and cocaine
inhibit reuptake of MOA via blockade of transporters
psychomotor stiumulant that the “high” tracks alongside plasma levels
cocaine
perception of “high” dependant upon
uptake into brain
thereputic uses of amphetamines
weight loss (not legit)
ADHD
narcoplepsy
non-stimulant treatment of narcolepsy
modafinil
toxicity of ampetamines sx
psycotic reacton (visual hallucinations, paranoia, change in affect) sympathomimetic increase
primary NT receptor MDMA effects
5-HT
active ingrediant in “bath salts”
cathinone
