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57 Cards in this Set

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what Drugs used to treat dependence and addiction are
a) Opioid receptor antagonist
i
) Naloxone (Narcan)
ii) Naltrexone
what drug used to treat dependence is a Synthetic opioid
i) Methadone
what drug that is used to treat dependence is a Partial µ-opioid receptor agonist
Buprenorphine
what drug used to treat dependence is a Nicotinic receptor partial agonist
Varenicline (Chantix)
what drug used to treat dependence are benzodiazepines
i) Oxazepam
ii) Lorazepam
what drug used to treat dependence is a NMDA receptor antagonist
i) Acamprosate
what is dependence
i) Defined, in part, as the compulsive use of a substance despite significant problems resulting from such use
what are some of the characteristics of being dependent
(1) Preoccupation with use of the chemical between periods of use
(2) Using more of the chemical than had been anticipated
(3) The development of tolerance to the chemical in question
(4) A characteristic withdrawal syndrome from the chemical
(5) Use of the chemical to avoid or control withdrawal symptoms
(6) Repeated efforts to cut back or stop the drug use
(7) Intoxication at inappropriate times (such as at work), or when withdrawal interferes with daily functioning (such as when hangover makes person too sick to go to work)
(8) A reduction in social, occupational or recreational activities in favor of further substance use
(9) Continued substance use in spite of the individual having suffered social, emotional, or physical problems related to drug use
how many sx do you need and for how long until the dx of dependent
need 3 of the and for 12 months
what is abuse
abuse is defined as a pattern of substance use leading to significant impairment in functioning
what needs to be present and for how long until the dx of abuse
1 dependent criteria for 12 months
what direction do dose response curves shift in tolerance
to the right
what happens to GABA a and NMDA receptors in chronic ethanol exposure
decreased expression of GABAA receptors and increased expression of NMDA receptors due to chronic ethanol exposure causes hyperarousal of the CNS during ethanol withdrawal
what system is the prime target of addictive drugs
mesolimbic DA system
where does mesolimbic dopamine system originate and where does it project to?
ii) Originates in the ventral tegmental area (VTA), a tiny structure at the tip of the brainstem, which projects to the nucleus accumbens, the amygdala, the hippocampus, and the prefrontal cortex
what causes pleasure
activation of the dopamine reward pathway which is the mesolimbic
da- is assoc with positive reward and not negative reward
three classes of molecular targets have been identified:
(1) Gio-coupled receptors
(2) Ionotropic receptors (ion channels)
(3) Monoamine transporters
what do nonadditive agents target
cortical and thalamic circuits. alter perception without causing sensations of reward and euphoria
what does Lysergic acid diethylamine (LSD), mescaline, psilocybin
Repetitive exposure leads to
rapid tolerance (tachyphylaxis)
what effect do Phencyclidine (PCP) and ketamine have
Psychedelic effects last for about 1 hour and also include increased blood pressure, impaired memory function, and visual alterations
Developed as general anesthetics (ketamine is still used for this purpose)
what long lasting effects do PCP and LSD cause
PCP may lead to irreversible schizophrenia-like psychosis
LSD can cause flashbacks of altered perception years after consumption
a) Drugs that activate Gio-coupled receptors: cause
disinhibition of DA neurons
µ receptors cause ____ when activated and are implicated in the reward effects of opiates
euphoria
(commonly abused µ opioids are
morphine, heroin, codeine, oxycodone, and meperidine)
Withdrawal symptoms from opioids include :
intense dysphoria, nausea or vomiting, muscle aches, lacrimation, rhinorrhea, mydriasis, piloerection, sweating, diarrhea, yawning, fever
what are the drugs that can be used for the treatment of opioid overdose
(a) Methadone, buprenorphine
(b) Naloxone
what is the MOA of nalaxone
pure opioid antagonist that reverses effects of a dose of opiates within minutes..Provokes an acute withdrawal syndrome in situations where a dependent person has opiates in their system
what are ethadone, buprenorphine and what makes them more beneficial than some other drugs
Long-acting opioids used for substitution therapy (half-life 25-52 hrs), Tolerance and physical dependence develop more slowly in comparison to other opioids (e.g., morphine)
(4) Effects of THC include
euphoria, relaxation, feelings of well-being, grandiosity, and altered perception of passage of increased appetite, attenuation of nausea, decreased intraocular pressure, and relief of chronic pain have led to the use of cannabinoids in medical therapy
what is Dronabinol
FDA-approved THC analog used for anorexia and weight loss in AIDS patients and cancer-chemotherapy induced nausea and vomiting
what is Nabilone
THC analog used for the treatment of refractory nausea and vomiting associated with cancer chemotherapy and as an adjunct in chronic pain management
what is the moa of GHB
Activates the GABAB receptor with low affinity and produces euphoria, enhanced sensory perceptions, feelings of social closeness, and amnesia before causing sedation and coma (originally introduced as a general anesthetic)
(
what is another name for GHB
Also known as liquid ecstasy or the date rape drug (has been used in date rapes because it is odorless, readily dissolved in beverages, reaches maximal plasma concentration 20-30 minutes after ingestion, and has an elimination half-life of 30 mintes)
(5) GHB targets GABAB receptors on both GABA and DA neurons, but those on GABA neurons are more
sensitive to GHB and lead to disinhibition of DA neurons when activated
Recreational use of GHB only inhibits GABA neurons but at higher doses GHB hyperpolarizes
DA neurons and inhibits DA release
(1) Endogenous cannabinoids that act as neurotransmitters include
2-arachidonyl glycerol and anandamide, both of which bind to CB1 receptors
(2) Endocannabinoids are called retrograde messengers because they bind to presynaptic CB1 receptors and
inhibit the release of either glutamate or GABA
(3) The exogenous cannabinoid Δ9-tetrahydrocannabinol (THC) causes
disinhibition of DA neurons by presynaptic inhibition of GABA neurons in the VTA (similar to opioids)
what is the MOA of nicotine
selective agonist of the nicotinic acetylcholine receptor (nAChR)
where are NACHRs located
(b) Neuronal nAChRs are expressed on DA neurons in the VTA; activation fulfills the DA requirement of addictive drugs
what antidepressant can be Used alone or in combination with nicotine-replacement therapy and/or behavioral therapy
bupropion
what is Varenicline
Derivative of the plant-extract cytisine
Partial neuronal nAChR agonist
Only approved for treating smoking cessation,Prevents nicotine stimulation of mesolimbic dopamine system associated with nicotine addiction
what is moa of cocaine
Blocks the DAT and inc the DA conc in the nucleus accumbens (rewarding effects) and Blocks the NET and activ the symp ns which leads to inc in arterial pressure, tachy,arrhythmias, and pupil dilation
what are sx of cocaine use and what are signs of OD
loss of appetite, hyperactivity, and lack of sleep while overdose may lead to hyperthermia, coma, and death
Exposure to cocaine increases risk for
intracranial hemorrhage, ischemic stroke, myocardial infarction, and seizures
what can be done to treat cocaine OD r
supportive with agents to control heart rate/rhythm (β-adrenergic receptor antagonist propranolol) and seizures (sedative-hypnotic diazepam)
what is the moa of amphetamines
cause the release of endogenous biogenic amines by reversing the action of biogenic amine transporters (dat, sert, net) at the plasma membrane(c) Increasing levels of amines in the cytoplasm
what are the effects of withdrawal from amphetamines
dysphoria, drowsiness (insomnia in some cases), and general irritability
what is the MOA of esctasy aka MDMA;methylenedioxymethamphetamine)
similar to amphetamines (reverses the action of biogenic amine transporters)
with a preferential affinity for SERT and an increase in serotonin
what are long term effects of ecstasy
cognitive impairment due to long term decrease in serotonin
what are the acute toxic effects of ecstasy
hyperthermia, dehydration, serotonin syndrome (mental status change, autonomic hyperactivity, neuromuscular abnormalities), and seizures
what are the withdrawal syndrome of ecstasy
mood “offset” characterized by depression lasting up to several weeks, possible increased aggression
what are example of sched one drugs
heroin, lysergic acid diethylamide (LSD), marijuana, and methaqualone.
what are examples of sched II drugs
morphine, phencyclidine (PCP), cocaine, methadone, and methamphetamine.
what are examples of sched III drugs
Anabolic steroids, codeine and hydrocodone with aspirin or acetaminophen, and some barbiturates are examples of Schedule III substances.
what are examples of sched IV
propoxyphene plus aspirin (Darvon), pentazocine, meprobamate, diazepam, and alprazolam.
What are the classic clue that someone is on LSD?
slow, lazy, hallucinate (vivid colors/patterns)