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155 Cards in this Set
- Front
- Back
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Where is acetylcholine found?
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-In the Brain (Pons, Hippocampus, medial septum, basal forebrain)
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What is the function of Acetycholine in the autonomic nervous system?
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Causes relaxation and mslows down heart beat
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What is the function if acetylcholine at the neuromuscular junction?
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Activation of muscle movement
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What is the function of acetylcholine in the brain?
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REM sleep and learning and meomry
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What drugs block or increase ACh release?
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Botox = blocks
spider venom = increaes |
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What would be some of the behavioral effects of Botox and Spider Venom?
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botox = stop contractions of neuromuscular joints
Spider venom = lots of movement |
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How is Actylcholine removed from the synapse?
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Acetylcholinesterase
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How does Acetycholinterase inhibition affect acetycholine levels?
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It increases the amount of time it stays in the body.
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What are the two types of Acetycholinergic receptors?
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Muscarinic and nicotine
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What are examples of agonists and antagonists for these receptors?
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Agonist - muscarinic and nicotine
Antagonist - atropine, scopo, curare |
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What are some of the likely effects of these agonists and antagonists?
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Antagonists will overstimulate the heart because they will [[block the calmer]]
agonist - slow down the heart too much |
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Where is dopamine found in the brain?
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Neocortext, mesolimbic, and nigrostratial system
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What functions is dopamine involved in?
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Pleasure, movement
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What are some of the consequences of too little or too much dopamine?
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Too much or too little deliberate movement
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What happens in parkinson's disease (PD)?
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One can't move if he/she tries
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What drug is used to treat Parkinson's?
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El-Dopa
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How does this drug affect dopamine?
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Makes more dopamine
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What are pscyhoactive effects of drugs that increase brain dopamine levels
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pleasure
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Why do dopamine antagonists reduce the symptoms of schizophrenia
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Schizophrenia can be caused by having too much dopamine
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What is the first dopamine antagonist ever used to treat schizophrenia?
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CHLORPROMAZINE!
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How is dopamine removed from the synapse?
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Enzymes or reuptake
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What drugs block dopamine re-uptake?
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Ritalin, Cocaine, amphetamines, methylphenidate
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Why do people use these drugs recreationally or medically?
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Increases them
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What is MAO?
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Monoamine Oxidase
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What are the consequences of MAO inhibition?
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Dopamine stays longer
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What are the psychoactive effects of MAO inhibitors?
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Anit-depressant, happy longer
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What happens to dopamine levels in the synapse following MAO inhibition?
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Increase!
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What are the cell bodies of serotonin (5-Hydroxitryptamine) neurons?
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98% cut, 2% brain
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Where do the axons of serotonin go?
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To the cortex
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What are some of the functions influenced by 5-HT
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Regulates mood, food intake, sleep, arousal and pain
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How is 5-HT removed from the synapse?
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Termination
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What happens if 5-HT reuptake is inhibited
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It increases the amount of time in the system
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What are the psychoactive effects of 5-HT reputake inhibitors
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No depression or anxiety
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What is glutamate?
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Main excitatory agonist
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What types of receptors does Glutamate bind to?
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NDMA glutmate
AMPA Metabotrophic ones |
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What ion channels are attached to NMDA receptors?
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calcium channels
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What do you think are the effects of opening these channels on potential?
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Causes it to be more excitatory
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Which glutamate receptor is implicated in a variety of disorders?
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NMDA receptor
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What is GABA?
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Inhibtory agonist
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What is a major function of GABA?
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Controls brain stability
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What are the types of receptors that GABA binds to?
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Gaba A + Gaba B
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What is the effect of opening these channels on the membrane potential?
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GABA A - chlorine opens so more inhibitory
GABA B - potassium opens, so more excitatory |
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What kinds of psychoactive drugs bind to the GABA-A receptor?
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Barbiturates, Alcohol, and Benzodiazepine (Valium)
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Which peptide is involved in analgesia and in the psychoactive effects of heorin and morphine?
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Opoid receptors
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What is tolerance?
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Decreased sensitivity due to previous exposure
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What is cross-tolerance?
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Tolerance to one drug results in decreased sensitivity to another drug
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What is drug addiction and what is the primary brain structure involved in drug abuse/dependence and what neurotransmitter is involved?
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Body needing more of a drug to survive,
Limbic system Dopamine |
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What example of cross-tolerance was discussed in class?
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Alcohol and Barbiturates
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What is the problem with tolerance?
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May not occur to all effects of a drug
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How does tolerance affect the therapeutic index?
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Shrinks it
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What is pharmacokinetic tolerance?
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The body making enzymes
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What is context-specifc tolerance?
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Affected by the environmental association
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How do pharmacokinetic, pharmcodynamic, and context-specific tolerance differ?
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Pharmacokinetic has to do with enzymes. Pharmacodynamic has to do with neurotransmitters. Context-specific has to do with environment.
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Describe the mechanism of pharmacokinetic tolerance?
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More enzyme --> Better metabolism --> shorter half life --> less drug getting to brain
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How can it account for cross-tolerance?
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Increases release, prevents reuptake
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Describing the two mechanisms of pharmacodynamic tolerance
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1 - Drug depletes the neurotransmittter that is critical to the drug's effects (Need more of a drug to work)
2 - Drug-induced alteration in receptor sensitivity with repeated exposure |
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How can the mechanisms of tolerance account for cross-toleance?
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If exposure to a drug decreases the receptor, other drug that targets the receptor won't work
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How does pharmacodynamic tolerance develop to receptor agonists and receptor antagonists?
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Agonist - 1) down-regulate receptors, 2) desensitize 3)decrease receptor lifetime
Antagonist - up-regulation |
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What do the terms up-regulation, down-regulation, desensitization and sensitization mean
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up-regulation: make more sensitive,
down-regulation/desnsitize - make less sensitive |
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How do they contribute to tolerance?
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Need more of the drug to get the same effect
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What does homoestasis have to do with tolerance?
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The body is always trying keep a balanced system
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What is the mechanism of context-specific tolerance?
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Targets learning and memory and associates environment with taking drugs
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How can Pavlovian Conditioning create tolerance?
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Sign of syringe -- primary effect of drug on brain -- compensatory reactions
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What is drug dependence?
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pattern of drug use that leads to uncontrollable and unpleasant mood state that then leads to compulsive drug use
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What is an abstinence syndrom?
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Symptoms of withdrawal are oppostie to the effect produced by the drug
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What is secondary psychological dependence?
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Fear of experiencing abstinence syndrome
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What drugs have moderate to strong potential for pscyhological and physiological dependence?
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Alcohol, Barbiturates, Anesthetic gases, anti-anxiety opoids
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Which drugs tend to produce only psychological dependence?
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Amphetamines, cocaine, LSD, mescaline, and marijuana
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What are the different ways that drugs can be categorized?
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1. chemical
2. stimulant 3. drug use |
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What are the strengths and weaknesses of the three drug categorizations?
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Chemical - good for development
stimulant-inhibit = bad because tehy don't have much information |
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What is an optical isomer (enantiomer)
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identical except they are mirror images and have different effects
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What is stereospecificity?
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Isomers with different receptor binding properties
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Why are optical isomers and stereospecificity a problem for categorizing drugs according to their structure and function?
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Because some are actives, but others are not and some drugs do both at different levels
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WHat are different biological levels that can be stimulated or depressed?
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at the:
1 - receptors 2 - action potentials 3 - behavior or emotion |
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What are the dfiferent ways a drug can be named?
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Chemical name, trade name, generic name, street name
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What is the function of sedative-hypnotics?
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To sedate, calm, and induce sleep
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What are some examples of sedative-hypnotics?
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Alcohol and Barbiturates
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What is the function of anxiolytics?
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To break anxiety. They have a higher therapeutic index and no anesthetic properties.
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What are some examples of anxiolytics?
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Benzodiazepines (Valium)
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What is the function of psychostimulants?
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To increase alertness, reduce fatigue, and elevate mood at low doses
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What are some examples of pscyhostimulants?
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Amphetamines, cocaine, caffeine, nicotine
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What is the function of antipsychotics?
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To treat major mental and emotional disturbances
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What are some examples of antipsychotics?
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Chlorpromazine and haloperidol
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What is the function of antidepressants?
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To treat severe depression and decrease rapid mood swings
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What are some examples of antidepressants?
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Fluoxine, lithium salt, and phenelzine
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What is the function of anesthetics?
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To treat pain so one can not feel it
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What are examples of anesthetics?
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Morphine, heroine, codeine, meperidine
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What is the function of analgesics?
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To treat pain
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What are examples of analgesics?
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Narcotics, inhalants, ketamine, cocaine
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How does the schedule-controlled drug classification scheme group drugs?
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By medical use and potential for abuse
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What kinds of drugs are in each scheudle?
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I - no medicinal use
II - some medicinal use III - less abuse |
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What is the Analog Act?
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"Designer Drug" law so the government is not fooled by new drugs that don't fit the classification scheme
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What are the three parts of the Analog Act?
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1 - chemical sustainability similar and either
2 - effects similar to substance in schedule I or II or 3. someone represents it as having the effect of a controlled substance |
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What other two names are used to label sedative-hypnotics?
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Anxiolytics and ___?
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Name three types of sedative-hypnotes
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Baribiturates, alcohol, benzodiazepine
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What are the dose-response characteristics of sedative-hypnotics?
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Psychological calming at low doses and sleep-inducing at high doses
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What is fermentation?
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Yeast + glucose + water + warmth
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What is distillation?
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Remove water to increase percent ethanol
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What is fortification?
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Adding ethanol (to wines, etc.)
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How is proof calculated?
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2x absolute percent ethanol
15% EtOH = 30 proof |
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What is a dose of alcohol?
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# EtOH molecules
(1 oz distilled = 1 glass beer = 1 cup wine) |
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What are the behavioral consequences of low does of alcohol?
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Decreased anxiety and disinhibition
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What are the behavioral consequences of high does of alcohol?
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Inhibit brain areas and impaired functions with higher processing
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What are the behavioral consequences of alchol at the highest doses?
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Sedation, coma, death
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What brain areas are likely involved int he different effects of alcohol?
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speech, planning, complex motor behavior
medulla = respiration |
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Why are coma and death following alcohol consumption rare?
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You pass out before death happens
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What is the balanced placebo design?
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Used to overcome subject expectations
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What is the balanced placebo design's goals
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To directly manipulate expectation
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How is the balanced placebo design executed?
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By having an equal amount of people on four levels (lie/lie, lie/truth, truth/lie, truth/truth)
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How are the balanced placebo designs interpreted?
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By looking at the numbers and accounting for expectation
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How would you describe the lipid and water-solubility of an ethanol molecule?
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Moderately lipid soluble, highly water soluble
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How does water-solubility affect ethanol's ability to distribute through the bodily compartments?
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Easily absorbed through the body
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Can alcohol enter the brain?
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Yes, easily enters the brain
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What organs are involved in ethanol absorption?
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The stomach and intestines
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How much of an ingested ethanol dose is absorbed in the stomach and intestines?
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20% by stomach, 80% by small intestine
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What are the factors that affect absorption in the stomach?
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Food in stomach, carbonation amount
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How does the activity of the pylorus sphinctor muscle affect ethanol absorption?
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It determines the rate of emptying of food from stomach to small intestine, so it controls how much is in the blood.
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Why is the pylorus sphinctor important for ethanol absorption?
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It can contribute to having too many ethanol molecules
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Where is ethanol metabolized?
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Alcohol dehydrogenase system (95%) (gastric + hepatic system)
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What is first pass metabolism?
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The metabolizing of alcohol the first time
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What is zero-order kinetics?
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Rate is constant for same individual
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Describe the metabolism of ethanol by the alcohol dehydrogenase system
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Rapid gastric emptying reduces first pass metabolism and increases blood alcohol levels
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What percent of ethnaol is metabolized by this system?
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95%
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How does high alcohol consumption affect the rate of metabolism in the system?
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Acetaldeyhyde = toxic and too much will cause headache, nausea, flushing, and throbbing because the methanol turns into formaldehyde
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How does disulfiram (Antibuse) work to treat alcoholism?
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Prevents aldehyde metabolism therefore increases aldehyde
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How do some ulcer medications affect metabolism in the alcohol dehydrogenase system?
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Zantac/Tagamet = less alcohol dehydrogenase --> increase half life --> stays longer
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What are the consequences of ulcer medications?
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Higher blood levels, more intoxification
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What are the sex differences in ethanol pharmacokinetics?
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Females have lass alcohol dehydrogenase therefore Ethanol stays longer in their blood
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What percentage of ethanol is not metabolized?
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2%
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What happens to the ethanol that is not metabolized?
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It is excreted through urine, sweat, and expired breath
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What is the relationship between the amount of alcohol excreted in your breath and the amount in your blood?
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Breath is ~0.05% of blood level
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How is alcohol excreted?
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via urine - kidney
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How does ethanol affect the cell membrane?
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Ethanol fluidizes the biological membranes
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Name three brain transmitter systems involved in the pharmacodynamic effects of ethanol on behavior
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1 - inhibit na+/k+ and reduces action potential
2 - GABA-A receptor agonist 3 - Glutamate NMDA receptor antagonist to block excitation |
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How does ethanol affect the GABAergic system?
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Increases Cl- flow and inhibits postsynaptic cell
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Would you call ethanol a GABA agonist?
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Yes, it is an agonist
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What does ethanol do at NMDA receptors
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Blocks excitation effect
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Would you call ethanol a glutamate agonist?
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No, it is a glutamate antagonis
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Which dopaminergic neurons are likely affected by alcohol?
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Increased ventral tegmental area (mesolimbic system) and increase dopamine by blocking glutamate
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Describe the pharmacokinetic and pharmacodynamic mechanisms of ethanol tolerance
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Kinetic - liver tolerance (up-regulation of enzymes)
Dynamic - brain - [Down-regulation of GABA receptors] |
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How does ethanol produce cross-tolernace?
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Cross-tolerance to other sedative-hypnotics
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What effects of ethanol show tolerance?
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Euphoric and anxiolytic effects
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Which effects of ethanol do not show tolerance?
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Lethal effects
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How is psychological dependence to ethanol produced?
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Through the nucleus accumbens
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What are the characteristics of abstinence syndrome produced by ethanol withdrawal?
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Seizures, increased blood pressure, and breathing rate, DT (Delerium Tremens)
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What are the neurological consequences of chronic ethanol consumption?
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Wernicke's encephalopathy and Korsakoff's syndrome
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What are the symptoms of Wernick'es encephalopahty syndrome
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It kills.
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what causes Wernicke's encephalopathy?
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Having a bulk of your calories from drinks and little vitamins
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How doe thiamine deficiencies produce brain damage?
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It kills brain cells and doesn't give access to the glucose.
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What is Korsakoff's syndrome?
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Profound amnesia, can't form new memories
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What is the main difference between Wernicke's encephalopahty and Korsakoff's syndrome?
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Korsakoff's forms from Wernicke's
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What is alcoholism?
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Continuous or periodic impaired control over drinking
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What is type I alcoholism?
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Abstain-binge patterns
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What is type II alcoholism?
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Continuous use; thrill-seeking personality, low need for social reward, little guilt or fear about alcohol use
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What are some treatments for alcoholism?
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Coercion, chemical treatment, treatment of underlying disorder, serotonergic drugs...
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