Drugs of abuse DSA (Kruse) Flashcards
__=compulsive drug-using behavior in which person uses the drug for personal satisfaction, often in face of known risks to health
addiction
addiction was formerly referred to as __
dependence was formerly referred to as __
psychological dependence
physical or physiologic dependence
__=a state characterized by signs and symptoms, frequently the opposite of those caused by a drug, when it is withdrawn from chronic use or when dose is abruptly lowered
Dependence
__=decreased response to a drug, necessitating larger doses to achieve the same effect. This can result from increased disposition of the drug, an ability to compensate for the effects of a drug, or changes in receptor or effector systems involved in drug actions
Tolerance
__=an increase in response with repetition of the same dose of the drug
Sensitization
Tolerance shifts the dose-response curve __
Sensitization shifts the dose-response curve __
right
left
__=adaptive changes that become fully apparent once drug exposure is terminated; generally d/t readaptation of CNS to absence of drug of dependence. This term is evidence of physical dependence
withdrawal
dependence-producing drugs activate the __ DA system, releasing DA
mesolimbic
which drugs activate GPCRs? Name their receptors and risk of addiction
Opioids –> mu opioid receptor, addictive (4/5)
Cannabinoids –> CB1R, slightly addictive (2/5)
Also has LSD, Mescaline, and psilocybin which are nonaddictive
which drugs bind ionotropic receptors and ion channels? Name their receptors and risk of addiction
Nicotine –> nAChR, addictive (4/5)
Alcohol –> GABA-A, 5-HT3, nAChR, NMDA, Kir, medium addictive (3/5)
also have benzos (3/5) and phencyclidine and ketamine (1/5)
which drugs bind to transporters of biogenic amines? Name their receptors and risk of addiction
Cocaine –> DAT, SERT, NET, Highly addictive (5/5)
Amphetamine –> DAT, SERT, NET, VMAT, Highly addictive (5/5)
nonaddictive drugs of abuse primarily target what?
cortical and thalamic circuits
rather than mesolimbic DA system
__ may lead to irreversible schizophrenia-like psychosis
__ can cause flashbacks of altered perception yrs after consumption
PCP
LSD
Naloxone MOA and clinical use?
pure opioid antagonist that reverses effects of a dose of opiates within mins; can provoke acute w/drawal syndrome if dependenet person has opiates in system
Tx opioid OD
Methadone and buprenorphine MOA and clinical use?
Long-acting opioids used for substitution tx (t1/2=25-52 hrs); given w/ supervised intake for opioid addiction
__ is an FDA-approved THC analog for anorexia and weight loss in AIDS pts and cancer-chemo induced n/v
Dronabinol
__ is a THC analog used for tx of refractory n/v assoc with cancer chemo and as an adjunct in chronic pain mgmt
Nabilone
__ is AKA the date rape drug. At higher dose it hyperpolarizes DA neurons and inhibits DA release. Targets GABA-B receptors on both GABA and DA neurons
GHB (gamma-hydroxybutyric acid)
Tx options for Nicotine addiction?
Nicotine: gum, lozenge, inhalers, transdermal patch
Bupropion: antidepressant w/unknown MOA
Varenicline: partial neuronal nAChR agonist
what is blocked by cocaine that produces rewarding effects? what is blocked by cocaine that activates the sympathetic NS?
DAT
NET
how to tx cocaine OD?
No antidote; Supportive, control rate/rhythm w/Propanolol and seizures w/Diazepam
MOA of amphetamines?
cause release of endogenous biogenic amines by reversing action of biogenic amine transporters at plasma membranes. Interferes with VMAT in the cell
DAT, SERT, and NET work in reverse and release amines into the synapse
MOA of ecstasy (MDMA)?
Similar to amphetamines but preferential affinity for SERT –> increased EC [5HT]
Schedule of heroid, LSD, mescaline, PCP, MDA, MDMA?
Schedule of Benzos, mild stimulants, most hypnotics and weak opioids?
I
IV
Schedule of Anabolic steroids, barbiturates, ketamine, moderate opioid agonists?
Schedule of Amphetamines, cocaine, methylphenidate, short acting barbiturates, strong opioids?
III
II