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PSYC 2220 EXAM #2
Terms in this set (121)
What is 1st pass metabolism?
when a drug goes to the GI tract --> body --> blood --> passes through the liver
What is a lesion?
damage to brain area for research
What is ablation?
removal of brain area
drug induced amnesia studies
temporarily induce anterograde amnesia
What is tDCS?
direct current applied; synaptic channels; depression
what is cocaine?
dopamine agonist w/ some norepine action
what is the problem with double blind tests and the placebo effect?
the placebo effect can be eliminated because those who respond positively are dropped
what the drug does to the body
what does the liver do in excretion?
protects the body with enzymes to detoxify substances; changes high lipid soluble to low; and can produce active metabolite
what are the disadvantages of oral administration?
vomiting, stomach distress, genetics can affect how much is absorbed
what the body does to the drug
what is the bioavailability of metabolism?
how fast is it eliminated? is there an active metabolite?
what is involved in the PARENTERAL route of administration?
NOT GI tract
What are the parenteral forms?
injection; inhalation; transdermal (skin); intranasal (nose/mucous membrane)
where and how are drugs absorbed when orally administered?
upper intestine by passive diffusion
what must the drug be for oral administration?
lipid soluble and stable in stomach fluid?
what are the entral route forms?
oral (pills/liquids); rectal (suppositories)
what is involved in the ENTRAL route of administration?
what is the bioavailability of distribution?
how much and what form does the drug cross the blood-brain barrier?
what is the bioavailability of absorption?
how much makes it to the bloodstream
What does ADME determine?
the bioavailibilty of a drug
What is elimination?
how the drug leaves the body
What is metabolism?
how a drug is broken down into waste products
What is distribution?
how a drug is spread throughout the body and where
What is absorption?
how drug gets into the body (blood)
what are the four core processes (ADME)
absorption, distribution, metabolism, elimination
what must a drug be if it is absorbed in the mucous membrane?
in the mouth or nose and water soluble
what are examples of drugs absorbed transdermally (skin)?
skin patches (nicotine/estrogen) or gels (testosterone)
what is intravenous injection?
the drug goes directly to bloodstream very fast in precise dosages but is most dangerous
what is intramuscular injection?
drug goes directly to skeletal muscle and is faster than pills but slower than intravenous
what is subcutaneous injection?
injection under the skin
when will a drug have effect after traveling via bloodstream?
when it reaches site of action (aka receptors)
What causes side effects?
the drug being elsewhere in the body
what is alcohol dehydrogenase?
an enzyme that breaks down alcohol
What is biotransformation/metabolism?
chemical changes that reduce a drugs effect and increases excretion over a span of time
what are the routes of elimination (KLBS)?
kidneys as urine, lungs, bile/intestines, skin as sweat
what does grapefruit juice do to drugs?
blocks c4p-3a4 and increases absorption
what routes are not affected by 1st pass metabolism?
injection and inhalation
What happens in the liver?
the drugs re broken down and some amount is inactivated/metabolized
what is type 1 and 2 intramuscular injection?
1 = fast in water solution
2= is slow in oily solution
what are examples of drugs that are absorbed in the mucous membrane?
cocaine or nicotine gum
where does the drug travel when inhaled?
the pulmonary capillaries to the left aorta heart and arteries and to the brain
what form is inhalation used and why?
recreational drugs because it is quickly absorbed to the blood (faster than injection)
why is rectal administration not preferred?
absorption is irregular, unpredictable, and incomplete
when is rectal administration typically used?
when pt is vomiting, unconscious, or unable to swallow
what is in phase 1 of drug metabolism?
cytochrome p450-cyp, cyp1,2,3, cyp2d6
what is an example of an enzyme inducer?
st johns wort
what are examples of enzyme inhibitors?
SSRI or grapefruit juice
what do they kidneys do in excretion?
salt/water balance; filter blood; manipulate urine ph; eliminate drug overdose
what is the 1st order system?
a drugs metabolized amount is proportional to the amount of drug present; independent of initial administration
what is an example of physical dependence?
what are the mechanisms of tolerance development?
metabolic tolerance, cellular adaptive tolerance, behavioral conditioning process
What is drug tolerance?
progressive decrease in response to the same dose of a drug
what is the therapeutic window?
blood concentration is equal because the right amount of drug is maintained in blood
What is steady state?
bring as much in as you put out; drug administration=drug excretion
What is a half-life?
metabolic clearance time; time it takes for the body to eliminate 1/2 of a drug or rate of excretion
What are examples of drugs that may not be metabolized and excreted intact?
lithium, mushroom amanita muscaria, methamphetamine
how do genetics affect metabolism?
DNA testing detects slow, normal, or fast metabolizers
what is enzyme inhibition?
cyp enzymes are inhibited to increase a drugs level
St. John's Wort
a plant that grows in the wild, has been used for centuries for mental health conditions
*widely prescribed for depression
What is enzyme induction?
a past experience with a drug can increase levels of enzymes so you metabolize it faster
what factors influence cytochrome p450 enzyme activity? (DSAGE)
liver disease, species, age, genetics, environment
how does the liver handle drugs?
liver cells (hepatocytes) have microsomal enzymes (cytochrome p450) to transform drugs
What is a receptor?
large molecule sites where naturally occurring compounds produce biological effect
how are drugs and receptors related?
drugs are more specific than neurotransmitters and drugs form reversible ionic bonds w/ specific receptors
what is an antagonistic action?
binding to a receptor site and blocking transmitter access to site
what are the characteristics of antagonists?
produces no response, reduces effect of agonist, blocks receptors, competitive, irreversible
what are the characteristics of agonists?
bind to receptors for functional response, full, partial, inverse
what is an example of a monoamine oxidase inhibitor?
what does the inhibition by drugs do?
increase transmitter availability
what are acute chronic receptor effects?
psychoactive drugs bind to receptor and has immediate response
what are chronic receptor effects?
drugs over long time changes receptor properties
what is a relationship between receptors and affinities?
different drugs can bind to the same receptor but have different affinities (strength)
how is slope on the DRC interpreted?
steep slopes have a small dose change but large effect and shallow slopes have a large dose change and small effect
What is ED50?
effective dose; drug dose that produces desired effect in 50% of test subjects
what is the LD50?
lethal dose for 50% of the population; animal testing
what should you keep in mind about the LD50?
desirable or undesirable side effects that can be lethal
what is the relationship between TI and drugs?
greater TI=safer drug;
what is the difference between low ED50 and low TI?
low ED50=greater potency; low TI=less safe
how do you calculate therapeutic index
LD50/ED50 OR LD1/ED99
what is efficacy and its relationship to drugs?
the maximum effect obtainable; drugs can be potent but not peak;
more efficacious = greater peak/max
what is another name for binding and its relationship to its effect?
affinity; tighter binding=stronger effect
What is potency?
how well drug molecules attach to their sites of action; more potent=better binding
What is a dose-response curve?
the relationship of dose and response
what is up vs down regulation?
up is supersensitive and down is less response
what are examples of irreversible acetylcholine esterase inhibitors?
pesticides or nerve gases
what is the relationship of drugs and carrier proteins?
drugs block carrier proteins (SSRIs)
what are carrier proteins?
bind to neurotransmitters to transport them to presynaptic neuron
what is an allosteric action?
binding to a nearby site to facilitate transmitter binding
what is an agonistic action?
binding to site of normal endogenous neutrotrans to initiate similar cellular response
who is affected by placebo effects?
What are benzodiazepines?
drugs to treat anxiety and insomnia; GABA agonists; pure agonist
why are grapefruit juice and alcohol bad for benzodiazepines?
boost effects and increases metabolic clearance time
What does suboxone do?
most effective treatment; controls withdrawal and blocks effects
what makes up suboxone?
buprenorphine and naloxine
what is Narcan/naloxone?
pure opioid antagonist that binds but doesn't induce activity so it throws you into immediate withdrawal
What is happening when a person overdoses?
they no longer experience enzyme induction and slower metabolism so they lose their tolerance
what is repeated use?
needs lots of doses to prevent withdrawal discomfort or pain relief
what is intermittent use?
little tolerance develops and retains initial efficacy
what is receptor desensitization?
progressive failure to receptors to respond
what do opioids metabolize into?
morphine, hydromorphone, oxymorphone
what are the major effects of opiates?
analgesia, euphoria, depression, gastrointestinal, edocrine, suppression of cough, sedation, nausea, pupil constriction
how to opiates interact with the limbic system, brain stem, and spinal cord?
acts on them to control emotion, coughing, breathing, and pain messages
What are nocebo effects?
experience side effects when warned of them
what is amphetamines?
potent norephine actin less dopamine action
What are CT scans used for?
detect tumors and abnormalities in the brain
What's a problem with CT scans?
can't detect fine grain details of brain
What is an MRI?
magnetic resonance imaging
What is Eros?
using infrared light to image neural brain activity on the cortex surface
What is TMS?
currents applied to manipulate brain to excite or inhibit cortex
what is the subtractive method?
ignore unnecessary brain activity; averaged results
What is a PET scan?
pt injected with radioligand to bind to spec. molecules 9hemoglobin, glucose, neurotrans); subtractive method; one scan a year
What is an fMRI?
measures ratio of oxygenated and unoxygenated hemoglobin; subtractive method; fast
what is in vivo single unit recording?
records action potentials in single cells using the firing rate principle
what is a MEG?
measures electrical activity by detection of magnetic field to see neural firing patterns; very expensive
What is an ERP system?
time locked recording of electrical activity; linked to one events and averaged in many trials
What is an EEG?
electrodes attached to scalp measure ongoing electrical activity in brain for real time info; cheap
what is diffusion tensor imaging?
advanced mri technique to measure white and grey matter volume and brain connections
What does a MRI do?
looks at hydrogen atoms in water and fat; better diagnostic abilities; and the clarity of the image is related to magnetic field strength
What does a CT scan do?
used x-ray technology to create a 3D image of the brain but has HIGH RADIATION
how are cocaine and amphetamine the same and different?
cant reverse or treat either; same pharmacodynamic properties; different pharmacokinetic properties
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