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