Drugs of Abuse Flashcards
ethanol
CNS depressant & sedative
RR addiction=3
MOA: Potentiate GABAa
Increased Cl- influx–>neuronal hyperpolarization
Inhibit glutamate excitatory actions at NMDA receptros–> black outs
Metabolism: in liver, excreted by kidneys and lungs
EtOH–>acetaldehyde by ADH–>acetate by ALDH
fomepizole
CNS depressant & sedative
MOA: inhibits ADH–>blocks conversion of methanol and ethylene glycol to toxic formaldehyde/ formate
Use: antifreeze toxicity
disfulfram (Antabuse)
CNS depressant & sedative
MOA: inhibits ALDH–>accumulation of acetalaldehyde with EtOH consumption–> “hangover”
Use: chronic alcoholism
diazpeam
alprazolam
flunitrazepam
Sedatives-benzodiazepines
RR addiction=3
MOA: potentiate GABAa
Increase opening of Cl- channels–>hyperpolarization
Activate mesolimbic reward pathway
Effects: anterograde amnesia, alcohol potentiates effects
flumazenil
Benzodiazepine receptor antagonist
Use: treatment of overdose
pentobarbital
Sedative-barbiturates
RR addiction=3
lower margin of safety–>decease in use
gamma-hydroxybutyric acid (GHB)
Sedative
RR addiction=3
MOA: activation of GABAb receptors–>disinhibition of dopamine neurons in VTA
Use: primarily general anesthetic
“liquid ecstasy”, “easy lay”, “date rape drug”
cocaine
Psychostimulant
RR addiction=5
MOA: inhibits DAT–>increased DA conc. extracellularly
Increase DA within nucleus accubens
Inhibits voltage gated Na+ channels in periphery–> local anesthetic
Effects: loss of appetite, hyperactivity, hyperthermia, coma, death
Addiction only after few exposures, withdrawal is mild
amphetamine
methamphetamine
methylphenidate (Ritalin)
Psychostimulants
RR addiction=5
MOA: substrates for DAT–>inhibit DA uptake–> increase extracellular DA
Increases release of DA
Withdrawal: dysphoria, drowsiness, irritability
ecstasy (MDMA)
Psychostimulant
RR addiction=5
“designer drug”–>no medical implications
MOA: inhibits SERT–> increased release of serotonin
Effects: feeling of intimacy, dehydration, permanent serotonin depletion–> irreversible brain damage
Withdrawal: offset in mood, depression, aggression
LSD
psilocybin
Psychedelics (hallucinogens)
RR addiction=1
MOA: activate 5-HT2–>increase glutamate
Do NOT stimulate mesolimbic DA release–> NOT adictive
Psilocybin= mushrooms
Bad trip= severe anxiety and/or pain, depression, suicidal thoughts
Hallucinogen persisting perception disorder (HPPD) or “flashback”= episodic disturbances resembling experience of prior trip even years after use
ketamine
phencyclidine (PCP)
Psychedelics (hallucinogens)
RR addiction=1
MOA: block NMDA-type glutamate receptors inc cortex and limbic system–> decrease overall excitability
Use: dissociative anesthetics
“special K” and “angel dust”
Effects: impaired memory, visual alterations, increaed BP, unplesant out-of body experiences
codeine
heroin
morphine
oxycodone
Opioids
RR addiction=4
MOA: couple to inhibitory G protein
Activate VTA mu-opioid receptors–>disinhibition of VTA DA neurons–>euphoria
Activate VTA kappa-opioid receptors–> disinhibition–> dysphoria
Withdrawal: dysphoria, nausea, vomiting, body aches, chills, diarrhea, sweating, rhinorrhea
Treatment: naloxone (emergency overdose), naltrexone (opioid addiction), methadone (addiction)
THC
dronabinol (Marinol)
Cannabinoids
RR addiction=2
MOA: THC binds inhibitory presynaptic CB1 receptor–> disinhibition of DA neuron in VTA
Onset within minutes, reaches max 102 hrs
Dronabinol and nabilone= synthetic cannabinoid
Use: increase appetite, attenuation of nausea, intraocular pressure, chronic pain
nicotine
RR addiction=4
MOA: nAChR agonist
Activation of nAChR in DA neurons in VTA–>release DA
Withdrawal symptoms mild, common relapse
Treatment: transdermal nicotine patch, buproion, cytisine, varenicline (Chantix)
