CNS Stimulants and Marijuana Flashcards
Name 3 methylxanthines
caffeine
theophylline - tea
theobromine - cocoa
avg. intake: 200 mg / person / day
What are methylxanthine’s effects on:
CNS?
Cardio?
SM?
Kidney?
Striated muscle?
MOA?
CNS: stimulant - increase mood / work capacity, decrease fatigue
Cardio: increase HR
SM: relaxation, especially bronchial SM
Kidney: weak diuretic
Striated muscle: Increase contraction strength
MOA: Increase cAMP by inhibiting cAMP phosphodiesterase
Toxic effects of methylxanthines?
CNS: nervousness, insomnia, hand tremors, seizures at very high doses
Other: cardiac arrhythmias
LD50: 7.5 g
ED50: 75 mg
TI: 100
What are the effects of tolerance and withdrawal from methylxanthines?
“chronic poisoning” - insomnia, tacchycardia, GI upset
Abstention: headache, lethargy, irritability
Pharmacokinetics of Cocaine?
T1/2: 1 hr
cocaine is a weak base, if treated with base, it is more readily absorbed
“crack” is thus “free-based” and is mostly the neutral form
Mechanism and sites of action for cocaine?
SEs?
CNS: increase mood, increase energy, decrease appetite, decreased need for sleep
MOA: prevents reuptake of NE, 5HT, DA in CNS
SEs: increase BP, increased body temp and local vasoconstriction
Do not administer with NE
Name a clinical use of cocaine
local anesthetic in eye
What are the toxic effects of cocaine?
- anxiety
- paranoia
- insomnia
- nervousness
- psychosis: hallucinations - similar to schizo
- seizures
- vasoconstriction at local tissues - tissue anoxia and cell death
- urticaria: itching sensation
- tolerance develops to euphoria = down-regulations of CNS NT —> exhaustion
- cardiac arrhythmias
- decreased blood flow to uterus —> low birth weight
In what way amphetamine, methamphetamine ad methylphenidate work?
what are the effects?
Increase release of DA, NE in CNS (recall indirect-acting amines)
Effects: increase body temp, BP and HR
in comparison to cocaine, slow onset
T1/2 10 hrs
“meth-mouth”
What are the clinical uses for amphetamine, methamphetamine, methylphenidate?
Tx for narcolepsy
ADD - methylphenidate
name 2 additional CNS stimulants that work as reuptake inhibitors.
armodafinil
modafinil
what is the MOA for cannabinoids?
name for endogenous THC?
effects of cannabinoids?
SM effects?
anticholinergic effects?
MOA: binds to cannabinoid receptors in CNS
anandamide
- euphoric effect
- antiemetic effect
- decreased intraocular pressure
- anticonvulsant
- stimulate appetite
- some analgesic / antinociceptive
SM: bronchodilation, dilate conjunctival vessel (red eye)
anticholinergic: dry mouth
TI of cannabinoids?
can they pass placenta?
Should you operate heavy machinery?
TI approx 1000
CAN pass placenta
Probs NOTS!!!!!!!!!!!!!
Name 2 drugs that administer THC
For what effects are they used?
dronabinol
nabilone
used for antiemetic effects, appetite stimulation - typically given to cancer px
cigarettes release how many micrograms nicotine per inhalation?
100 micograms
nicotine works on what receptors?
presynaptic nicotinic cholinergic receptors
you can have withdrawal from quitting! it makes you sad, mad, not glad, etc.
name and nicotine partial agonist and its use!
varenicline
used to quit smoking
