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155 Cards in this Set

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Where is acetylcholine found?
-In the Brain (Pons, Hippocampus, medial septum, basal forebrain)
What is the function of Acetycholine in the autonomic nervous system?
Causes relaxation and mslows down heart beat
What is the function if acetylcholine at the neuromuscular junction?
Activation of muscle movement
What is the function of acetylcholine in the brain?
REM sleep and learning and meomry
What drugs block or increase ACh release?
Botox = blocks
spider venom = increaes
What would be some of the behavioral effects of Botox and Spider Venom?
botox = stop contractions of neuromuscular joints
Spider venom = lots of movement
How is Actylcholine removed from the synapse?
Acetylcholinesterase
How does Acetycholinterase inhibition affect acetycholine levels?
It increases the amount of time it stays in the body.
What are the two types of Acetycholinergic receptors?
Muscarinic and nicotine
What are examples of agonists and antagonists for these receptors?
Agonist - muscarinic and nicotine
Antagonist - atropine, scopo, curare
What are some of the likely effects of these agonists and antagonists?
Antagonists will overstimulate the heart because they will [[block the calmer]]

agonist - slow down the heart too much
Where is dopamine found in the brain?
Neocortext, mesolimbic, and nigrostratial system
What functions is dopamine involved in?
Pleasure, movement
What are some of the consequences of too little or too much dopamine?
Too much or too little deliberate movement
What happens in parkinson's disease (PD)?
One can't move if he/she tries
What drug is used to treat Parkinson's?
El-Dopa
How does this drug affect dopamine?
Makes more dopamine
What are pscyhoactive effects of drugs that increase brain dopamine levels
pleasure
Why do dopamine antagonists reduce the symptoms of schizophrenia
Schizophrenia can be caused by having too much dopamine
What is the first dopamine antagonist ever used to treat schizophrenia?
CHLORPROMAZINE!
How is dopamine removed from the synapse?
Enzymes or reuptake
What drugs block dopamine re-uptake?
Ritalin, Cocaine, amphetamines, methylphenidate
Why do people use these drugs recreationally or medically?
Increases them
What is MAO?
Monoamine Oxidase
What are the consequences of MAO inhibition?
Dopamine stays longer
What are the psychoactive effects of MAO inhibitors?
Anit-depressant, happy longer
What happens to dopamine levels in the synapse following MAO inhibition?
Increase!
What are the cell bodies of serotonin (5-Hydroxitryptamine) neurons?
98% cut, 2% brain
Where do the axons of serotonin go?
To the cortex
What are some of the functions influenced by 5-HT
Regulates mood, food intake, sleep, arousal and pain
How is 5-HT removed from the synapse?
Termination
What happens if 5-HT reuptake is inhibited
It increases the amount of time in the system
What are the psychoactive effects of 5-HT reputake inhibitors
No depression or anxiety
What is glutamate?
Main excitatory agonist
What types of receptors does Glutamate bind to?
NDMA glutmate
AMPA
Metabotrophic ones
What ion channels are attached to NMDA receptors?
calcium channels
What do you think are the effects of opening these channels on potential?
Causes it to be more excitatory
Which glutamate receptor is implicated in a variety of disorders?
NMDA receptor
What is GABA?
Inhibtory agonist
What is a major function of GABA?
Controls brain stability
What are the types of receptors that GABA binds to?
Gaba A + Gaba B
What is the effect of opening these channels on the membrane potential?
GABA A - chlorine opens so more inhibitory
GABA B - potassium opens, so more excitatory
What kinds of psychoactive drugs bind to the GABA-A receptor?
Barbiturates, Alcohol, and Benzodiazepine (Valium)
Which peptide is involved in analgesia and in the psychoactive effects of heorin and morphine?
Opoid receptors
What is tolerance?
Decreased sensitivity due to previous exposure
What is cross-tolerance?
Tolerance to one drug results in decreased sensitivity to another drug
What is drug addiction and what is the primary brain structure involved in drug abuse/dependence and what neurotransmitter is involved?
Body needing more of a drug to survive,
Limbic system
Dopamine
What example of cross-tolerance was discussed in class?
Alcohol and Barbiturates
What is the problem with tolerance?
May not occur to all effects of a drug
How does tolerance affect the therapeutic index?
Shrinks it
What is pharmacokinetic tolerance?
The body making enzymes
What is context-specifc tolerance?
Affected by the environmental association
How do pharmacokinetic, pharmcodynamic, and context-specific tolerance differ?
Pharmacokinetic has to do with enzymes. Pharmacodynamic has to do with neurotransmitters. Context-specific has to do with environment.
Describe the mechanism of pharmacokinetic tolerance?
More enzyme --> Better metabolism --> shorter half life --> less drug getting to brain
How can it account for cross-tolerance?
Increases release, prevents reuptake
Describing the two mechanisms of pharmacodynamic tolerance
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
How can the mechanisms of tolerance account for cross-toleance?
If exposure to a drug decreases the receptor, other drug that targets the receptor won't work
How does pharmacodynamic tolerance develop to receptor agonists and receptor antagonists?
Agonist - 1) down-regulate receptors, 2) desensitize 3)decrease receptor lifetime

Antagonist - up-regulation
What do the terms up-regulation, down-regulation, desensitization and sensitization mean
up-regulation: make more sensitive,
down-regulation/desnsitize - make less sensitive
How do they contribute to tolerance?
Need more of the drug to get the same effect
What does homoestasis have to do with tolerance?
The body is always trying keep a balanced system
What is the mechanism of context-specific tolerance?
Targets learning and memory and associates environment with taking drugs
How can Pavlovian Conditioning create tolerance?
Sign of syringe -- primary effect of drug on brain -- compensatory reactions
What is drug dependence?
pattern of drug use that leads to uncontrollable and unpleasant mood state that then leads to compulsive drug use
What is an abstinence syndrom?
Symptoms of withdrawal are oppostie to the effect produced by the drug
What is secondary psychological dependence?
Fear of experiencing abstinence syndrome
What drugs have moderate to strong potential for pscyhological and physiological dependence?
Alcohol, Barbiturates, Anesthetic gases, anti-anxiety opoids
Which drugs tend to produce only psychological dependence?
Amphetamines, cocaine, LSD, mescaline, and marijuana
What are the different ways that drugs can be categorized?
1. chemical
2. stimulant
3. drug use
What are the strengths and weaknesses of the three drug categorizations?
Chemical - good for development
stimulant-inhibit = bad because tehy don't have much information
What is an optical isomer (enantiomer)
identical except they are mirror images and have different effects
What is stereospecificity?
Isomers with different receptor binding properties
Why are optical isomers and stereospecificity a problem for categorizing drugs according to their structure and function?
Because some are actives, but others are not and some drugs do both at different levels
WHat are different biological levels that can be stimulated or depressed?
at the:
1 - receptors
2 - action potentials
3 - behavior or emotion
What are the dfiferent ways a drug can be named?
Chemical name, trade name, generic name, street name
What is the function of sedative-hypnotics?
To sedate, calm, and induce sleep
What are some examples of sedative-hypnotics?
Alcohol and Barbiturates
What is the function of anxiolytics?
To break anxiety. They have a higher therapeutic index and no anesthetic properties.
What are some examples of anxiolytics?
Benzodiazepines (Valium)
What is the function of psychostimulants?
To increase alertness, reduce fatigue, and elevate mood at low doses
What are some examples of pscyhostimulants?
Amphetamines, cocaine, caffeine, nicotine
What is the function of antipsychotics?
To treat major mental and emotional disturbances
What are some examples of antipsychotics?
Chlorpromazine and haloperidol
What is the function of antidepressants?
To treat severe depression and decrease rapid mood swings
What are some examples of antidepressants?
Fluoxine, lithium salt, and phenelzine
What is the function of anesthetics?
To treat pain so one can not feel it
What are examples of anesthetics?
Morphine, heroine, codeine, meperidine
What is the function of analgesics?
To treat pain
What are examples of analgesics?
Narcotics, inhalants, ketamine, cocaine
How does the schedule-controlled drug classification scheme group drugs?
By medical use and potential for abuse
What kinds of drugs are in each scheudle?
I - no medicinal use
II - some medicinal use
III - less abuse
What is the Analog Act?
"Designer Drug" law so the government is not fooled by new drugs that don't fit the classification scheme
What are the three parts of the Analog Act?
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
What other two names are used to label sedative-hypnotics?
Anxiolytics and ___?
Name three types of sedative-hypnotes
Baribiturates, alcohol, benzodiazepine
What are the dose-response characteristics of sedative-hypnotics?
Psychological calming at low doses and sleep-inducing at high doses
What is fermentation?
Yeast + glucose + water + warmth
What is distillation?
Remove water to increase percent ethanol
What is fortification?
Adding ethanol (to wines, etc.)
How is proof calculated?
2x absolute percent ethanol

15% EtOH = 30 proof
What is a dose of alcohol?
# EtOH molecules
(1 oz distilled = 1 glass beer = 1 cup wine)
What are the behavioral consequences of low does of alcohol?
Decreased anxiety and disinhibition
What are the behavioral consequences of high does of alcohol?
Inhibit brain areas and impaired functions with higher processing
What are the behavioral consequences of alchol at the highest doses?
Sedation, coma, death
What brain areas are likely involved int he different effects of alcohol?
speech, planning, complex motor behavior

medulla = respiration
Why are coma and death following alcohol consumption rare?
You pass out before death happens
What is the balanced placebo design?
Used to overcome subject expectations
What is the balanced placebo design's goals
To directly manipulate expectation
How is the balanced placebo design executed?
By having an equal amount of people on four levels (lie/lie, lie/truth, truth/lie, truth/truth)
How are the balanced placebo designs interpreted?
By looking at the numbers and accounting for expectation
How would you describe the lipid and water-solubility of an ethanol molecule?
Moderately lipid soluble, highly water soluble
How does water-solubility affect ethanol's ability to distribute through the bodily compartments?
Easily absorbed through the body
Can alcohol enter the brain?
Yes, easily enters the brain
What organs are involved in ethanol absorption?
The stomach and intestines
How much of an ingested ethanol dose is absorbed in the stomach and intestines?
20% by stomach, 80% by small intestine
What are the factors that affect absorption in the stomach?
Food in stomach, carbonation amount
How does the activity of the pylorus sphinctor muscle affect ethanol absorption?
It determines the rate of emptying of food from stomach to small intestine, so it controls how much is in the blood.
Why is the pylorus sphinctor important for ethanol absorption?
It can contribute to having too many ethanol molecules
Where is ethanol metabolized?
Alcohol dehydrogenase system (95%) (gastric + hepatic system)
What is first pass metabolism?
The metabolizing of alcohol the first time
What is zero-order kinetics?
Rate is constant for same individual
Describe the metabolism of ethanol by the alcohol dehydrogenase system
Rapid gastric emptying reduces first pass metabolism and increases blood alcohol levels
What percent of ethnaol is metabolized by this system?
95%
How does high alcohol consumption affect the rate of metabolism in the system?
Acetaldeyhyde = toxic and too much will cause headache, nausea, flushing, and throbbing because the methanol turns into formaldehyde
How does disulfiram (Antibuse) work to treat alcoholism?
Prevents aldehyde metabolism therefore increases aldehyde
How do some ulcer medications affect metabolism in the alcohol dehydrogenase system?
Zantac/Tagamet = less alcohol dehydrogenase --> increase half life --> stays longer
What are the consequences of ulcer medications?
Higher blood levels, more intoxification
What are the sex differences in ethanol pharmacokinetics?
Females have lass alcohol dehydrogenase therefore Ethanol stays longer in their blood
What percentage of ethanol is not metabolized?
2%
What happens to the ethanol that is not metabolized?
It is excreted through urine, sweat, and expired breath
What is the relationship between the amount of alcohol excreted in your breath and the amount in your blood?
Breath is ~0.05% of blood level
How is alcohol excreted?
via urine - kidney
How does ethanol affect the cell membrane?
Ethanol fluidizes the biological membranes
Name three brain transmitter systems involved in the pharmacodynamic effects of ethanol on behavior
1 - inhibit na+/k+ and reduces action potential
2 - GABA-A receptor agonist
3 - Glutamate NMDA receptor antagonist to block excitation
How does ethanol affect the GABAergic system?
Increases Cl- flow and inhibits postsynaptic cell
Would you call ethanol a GABA agonist?
Yes, it is an agonist
What does ethanol do at NMDA receptors
Blocks excitation effect
Would you call ethanol a glutamate agonist?
No, it is a glutamate antagonis
Which dopaminergic neurons are likely affected by alcohol?
Increased ventral tegmental area (mesolimbic system) and increase dopamine by blocking glutamate
Describe the pharmacokinetic and pharmacodynamic mechanisms of ethanol tolerance
Kinetic - liver tolerance (up-regulation of enzymes)
Dynamic - brain - [Down-regulation of GABA receptors]
How does ethanol produce cross-tolernace?
Cross-tolerance to other sedative-hypnotics
What effects of ethanol show tolerance?
Euphoric and anxiolytic effects
Which effects of ethanol do not show tolerance?
Lethal effects
How is psychological dependence to ethanol produced?
Through the nucleus accumbens
What are the characteristics of abstinence syndrome produced by ethanol withdrawal?
Seizures, increased blood pressure, and breathing rate, DT (Delerium Tremens)
What are the neurological consequences of chronic ethanol consumption?
Wernicke's encephalopathy and Korsakoff's syndrome
What are the symptoms of Wernick'es encephalopahty syndrome
It kills.
what causes Wernicke's encephalopathy?
Having a bulk of your calories from drinks and little vitamins
How doe thiamine deficiencies produce brain damage?
It kills brain cells and doesn't give access to the glucose.
What is Korsakoff's syndrome?
Profound amnesia, can't form new memories
What is the main difference between Wernicke's encephalopahty and Korsakoff's syndrome?
Korsakoff's forms from Wernicke's
What is alcoholism?
Continuous or periodic impaired control over drinking
What is type I alcoholism?
Abstain-binge patterns
What is type II alcoholism?
Continuous use; thrill-seeking personality, low need for social reward, little guilt or fear about alcohol use
What are some treatments for alcoholism?
Coercion, chemical treatment, treatment of underlying disorder, serotonergic drugs...