drugs of abuse Flashcards
amphetamine-related designer drug
MOA: reverses action of SERT, increasing release of 5-HT, and to a lesser extent DA and NE
Adverse: hyperthermia spurs excessive water drinking: hyponatremia, seizures and death
MDMA (Ecstasy)
mu receptor agonist used to treat opioid and alcohol addiction
blocks the reinforcing properties of alcohol
naltrexone
Class: opioid antitussive dissociative drug that distorts perception of sight and sound
MOA: blocks NMDA receptors, leading to disinhibition of excitatory pathways
-receptors involved in the efficacy are not the receptors for analgesia
-dose is lower than required to achieve analgesia
-death in children taking over the counter formulations has caused revision to only above age 6 use, but FDA considering use in children at all, due to variations in metabolism of codeine
dextromethorphan
benzodiazepine that binds to GABAa receptors producing sedative effects
produces anterograde amnesia
“date rape drug”
lethal when combined with alcohol or other CNS depressants
Royhypnol
MOA: noncompetitive antagonism of NMDA receptor, causing dissociation
can be injected, snorted, smoked or ingested
not addictive but can lead to psychosis
Ketamine & PCP
selective agonist of nAChR
highly addictive
excitation of VTA dopamine neurons causes release of dopamine in the nucleus accumbens and the prefrontal cortex
nicotine
“liquid ecstasy” that dissolves in beverages
produced during the metabolism of GABA and receptor is GABAb, causing disinhibition of DA neurons
can be prescribed in low doses for narcolepsy
was synthesized as an anesthetic but it has a narrow safety margin & is addictive
Before causing sedation and coma it causes euphoria, enhanced sensory perceptions, amnesia, feeling of social closeness
Gamma-Hydroxybutyric Acid (GHB)
Main target is 5-HT2a receptor
increases glutamate release at the cortex
causes shape and color distortion, depersonalization, hallucinations, distorted time perception, dizziness, nausea, paresthesia, blurred vision
Does not cause dependence or addiction
LSD, mescaline & psilocybin
blocks aldehyde dehydrogenase, resulting in an accumulation of acetaldehyde which produces unpleasant flushing when alcohol is present
disulfiram (antabuse)
psychological dependence
addiction
endogenous neurotransmitters that inhibit glutamate or GABA at presynaptic CB1 receptor
exogenous: contains powerful psychoactive substance which causes disinhibition of GABA (DA) neurons at the VTA, producing euphoria and relaxation
cannabinoids
positive modulators (meaning it binds to allosteric site) of GABAa receptors with alpha1 subunit in VTA interneurons, causing disinhibition of DA neurons "opens the door over and over"
benzodiazepines
GABA analog that normalizes dysregulated neurotransmission in treatment for alcoholism
acamprosate
MOA: partial agonist of mu receptor
less psychoactive & binds with high affinity, as well as slowly dissociates
treatment of opioid addiction with less risk of overdose or resp depression
Oral formula: Subutex
if combined with naloxone: Suboxone (if this is crushed and injected, naloxone blocks the high)
buprenorphine
full agonist of mu receptors with long duration of action binds with high affinity less psychoactive shows cross tolerance with heroin has potential for abuse & OD
methadone
mixed agonist of opioid receptors
high binding affinity for mu receptor but low activity
antagonist of delta & kappa receptors
Use: alternative to methadone for management of opioid withdrawal
Adverse: psychotomimetic effects, hallucinations, nightmares, anxiety
combination formulas with naloxone have potential for abuse and can cause serious resp depression and death if extracted or injected
buprenorphine (Buprenex)
pentazocine (Talwin)
nalbuphine (Nubain)
