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101 Cards in this Set
- Front
- Back
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Pharmacology |
the scientific study of the actions of drugs and their effects on a living organism |
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Neuropharmacology |
specialization concerned with drug-induced changes in the functioning cells of the nervous system |
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Psychopharmacology |
specialization emphasizing changes in mood, thinking, and behavior |
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neuropsychopharmacology |
~goal to identify chemical substances that act on the nervous system to alter behavior that is disturbed because of injury, disease, or environmental factors ~using chemical agents as probes to gain an understanding of the neurobiology of behavior |
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Drug action |
the specific molecular changes produced by a drug when it binds to a specific target site or receptor ~mimicking brain functions in excess ~stimulates or inhibits release of a neurotransmitter ~facilitate or inhibit entrance of neurotransmitter into vesicles ~inhibit or facilitate reuptake |
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Drug effects |
alterations in physiological or psychological functions caused by molecular changes from drug action ~site of action may be different from site of effects |
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Therapeutic effects |
the desired physical or behavioral changes produced by the drug/receptor interaction |
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Side effects |
all other effects produced by drug/receptor interaction ~negative or undesired effects ~range from mildly annoying to distressing and dangerous |
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specific drug effects |
effects based on the physical and biochemical interactions of a drug with a target site in living tissue |
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nonspecific drug effects |
effects based on unique characteristics of the individual ~mood, expectations, attitude towards drug or administrator, etc. all influence outcome |
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Placebo |
substance that is pharmacologically inactive, but in many instances still causes both therapeutic and side effects |
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Bioavailability |
concentration/amount of drug in the blood that is free to bind at specific target sites |
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Pharmacokinetic |
factors that contribute to bioavailability: 1. routes of administration 2. absorption and distribution 3. binding 4. inactivation 5. excretion |
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biotransformation |
drug inactivation; occurs as a result of metabolic processes in the liver |
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depot binding |
type of drug interaction involving binding to an inactive site, such as to proteins in the plasma, to bone, or to fat |
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Enteral vs. Parenteral methods of administration |
E: utilizes gastrointestinal (GI) tract ~ slow onset, highly variable blood levels of drug ~oral or suppository P: everything else; injection, pulmonary, topical |
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Oral Administration (PO) |
~most popular route of ingestion ~safe, self administered, economical, comfortable ~dissolve in stomach, pass through wall to reach blood capillaries ~resistant to destruction by stomach acid and enzymes important to normal digestion |
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Absorption |
movement of the drug from the cite of administration to the blood circulation ~most drugs not fully absorbed until they reach small intestines |
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first-pass metabolism |
liver metabolizes some of a drug before it can circulate through the body, particularly when taken orally |
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Intravenous (IV) |
injection is the most rapid and accurate method ~precise quantity placed directly into blood stream ~quick onset, can't be removed in case of allergy or overdose ~reaches brain almost instantly |
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Intramuscular (IM) |
~slower, more even absorption (10-30 min) ~rate of drug absorption is dependent on rate of blood flow to muscle ~solution can be irritating and cause muscle discomfort |
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Intraperitoneal (IP) |
common for small lab animals injected through abdominal wall into peritoneal cavity |
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Subcutaneous (SC) |
~injected just below the skin ~absorption rate dependent on blood flow to the site ~slow and steady absorption ~often used to administer hormones |
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Inhalation |
~absorbed into the blood by passing through lungs ~rapid absorption b/c area of pulmonary absorption is large and rich with capillaries ~rapid effect on the brain |
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Topical |
application to mucous membranes ~some topically administered drugs can be readily absorbed into circulation ~Intranasal application allows blood-brain barrier to be bypassed |
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Transdermal |
drug administration with skin patches controlled and sustained delivery of drug at pre-programmed rate painless, avoids first-pass effect |
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epidural injection |
spinal anesthetics are administered directly into cerebrospinal fluid surrounding spinal cord, by passing blood-brain barrier |
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Psychoactive Drugs |
drugs that have an effect on thinking, mood, and behavior target the brain |
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phospholipids |
~complex lipid (fat) molecules that make up cell membranes ~negatively charged region at one end, 2 uncharged lipid tails ~arranged in a bilayer, phosphate ends form 2 sheets filled with fatty material ~polar heads are attracted to polar water molecules |
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passive diffusion |
~ how drugs with high lipid solubility move through cell membranes ~movement across membranes is always higher to lower concentration |
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concentration gradient |
~concentration difference on each side of the membrane ~the larger the difference, the more rapid is diffusion ~lipid solubility increases the absorption of drug into the blood and determines how readily a drug will pass the lipid barriers to enter the brain |
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Cerebrospinal fluid |
~liquid that fills the subarachnoid space that surrounds the bulk of the brain and spinal cord ~fills hollow spaces (ventricles) and their interconnecting channels (aqueducts), and central canal |
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blood-brain barrier |
~separation between brain capillaries and the brain/cerebrospinal fluid ~selectively permeable ~capillaries in brain are different than the rest of the body - no intercellular cleft glial cells and astrocites regulate |
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intercellular clefts |
small gaps between adjacent cells in walls of capillaries made up of endothelial cells |
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fenestrations |
large openings in walls of capillaries through which molecules can pass |
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astrocytes |
~provide structural support for neurons ~maintain ionic balance in the extracellular environment ~store nutrients to provide energy for neurons ~perform phagocytosis ~extensions of the glial cells ~help maintain endothelial tight junctions |
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depot binding |
binding of a drug to inactive sites ~reduces concentration of a drug at action sites |
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first - order kinetics |
exponential drug clearance from the body |
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half-life |
the amount of time required for removal of 50% of the drug from the blood (t1/2) ~determines the time interval between doses ~shorter half-life, more doses table 1.5 |
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zero-order kinetics |
drugs are eliminated at a constant, linear rate, not in percentages |
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biotransformation |
inactivation of a drug through a chemical change, usually by metabolic processes in the liver ~liver produces enzymes to change molecules ~drugs are eliminated via metabolism and metabolites are excreted |
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microsomal enzymes |
liver enzymes lack strict specificity, can metabolize a variety of foreign chemicals |
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cytochrome P450 |
microsomal enzymes oxidize psychoactive drugs found in liver, kidney, lungs, intestine, nasal passages |
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enzyme induction |
increase in particular liver enzyme caused by repeated use of psychoactive drugs ~increases the rate of biotransformation ~speeds transformation of other drugs that the enzyme acts on and reduces their effects opposite: enzyme inhibition; increased potential for toxicity, more intense or prolonged drug effect |
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pharmacodynamics |
the study of the physiological and biochemical interaction of drug molecules with target tissue that is responsible for the ultimate effects of a drug |
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receptors |
large protein molecules located on the surface of or within cells ~protein found on surface of cell, receives chemical signals from outside the cell ~extracellular: outside of cells to relay information through the membrane to affect intracellular processes ~intracellular: within the target cell, in cytoplasm or nucleus, hormones to influence neural events ~"door" ~number and sensitivity of receptors can change |
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ligand |
any molecule that binds to a receptor with some selectivity ~"key" ~binding causes change in receptor shape that initiates a series of events in the cell |
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receptor agonists |
neurochemicals or drugs that have the best chemical "fit" to bind to a particular receptor protein to initiate a cellular response ~attaches readily, produces significant biochemical effect best fit = high affinity |
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receptor antagonists |
ligands that produce fit but have no cellular effect after binding (low efficacy) and prevent an active ligand from binding; blocks the receptor |
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inverse agonists |
produces an effect opposite one by an agonist |
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up-regulation |
receptor numbers increase |
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down-regulation |
receptor numbers decrease in response to absense of ligands |
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receptor subtypes |
~receptors with different characteristics in different tissues ~respond to the same neurotransmitter but vary in design |
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dose-response curve |
describes the extent of biological or behavioral effect (response) produced by a given drug concentration (dose) ~used to evaluate receptor activity ~classic S shape curve |
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therapeutic index |
TD50/ED50 toxic dose (for 50% population) /effective dose (dose that produces half of the maximal effect for 50% population) ~the wider the difference, the better common drugs: weed = 1000:1; cocaine = 15:1; alcohol = 10:1; morphine = 70:1 |
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potentiation |
combination of two drugs produces effects that are greater than the sum of their individual effects |
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tollerance |
diminished response to drug administration after repeated exposure to that drug ~increasingly larger doses necessary to recieve same reaction ~metabolic, pharmacodynamic, and behavioral tollerance |
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Sensitization |
enhancement of particular drug effects after repeated administration of the same dose of that drug |
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pharmacogenetics |
the study of the genetic basis for variability in drug response among individuals |
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neurons |
nerve cells, transmit info in the form of electrical signaling soma: cell body, contains nucleus dendrites: branches from soma that receive info from other cells; signals originate here axon: single tubular extension that conducts the electrical signal to the cell body to the terminal buttons on the axon terminals |
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glial cells |
provide metabolic support, insulation, and protection for neurons ~four types: schwann cells, oligodendroglia, astrocytes, microglia |
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sensory neurons |
convert physical stimuli into electrical signals sensitive to environmental stimuli, convert physical stimuli in the world around us and in our internal environment into an electrical signal and transmit info |
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interneurons |
nerve cells (neurons) within the brain and spinal cord that receive electrical signals ~form interacting neural circuits responsible for making conscious decisions, recognition, memory, decision making, cognition |
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motor neurons |
control biobehavioral responses appropriate for a given situation "the essence of life" |
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extracellular fluid |
surrounds neurons, provides nutrients |
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mitochondria |
generate energy from glucose in the form of adenosine triphosphate (ATP) |
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synapse |
gap between cells' dendrites ~dendrites and soma receive info from other cells across the synapse |
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dendritic spines |
branch off dendrites, increase receiving surface area ~dendrites and their spines are constantly modified and can change shape rapidly in response to changes in synaptic transmission "use it or lose it" changes throughout life permit us to learn new associations |
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axon hillock |
portion of axon adjacent to cell body generates action potential |
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terminal buttons |
located near the dendrites or somas of other cells, at the ends of the axons contain neurotransmitters |
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myelin |
fatty insulated coating wrapped around axons created by concentric layer of glial cells ~schwann cells and oligodendroglia ~myelin sheath increases speed of conduction along the axon - the thicker the myelin, the faster the conduction |
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nodes of Ranvier |
breaks in myelin sheath on axon where action potential is regenerated during conduction of the electrical signal along the length of the axon |
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NMDA |
protein/molecule, receptor activated when you're presented with new stimuli |
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Watson and Krick 1953 |
discovered the shape/structure of DNA and that it effects behavior with its changes/differences ~behavioral patterns coded in DNA ~depending on the environment and what's happening around you, they'll react and express DNA differently |
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DNA |
macromolecule encoding the instructions for the development and functioning of all living things |
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RNA |
memory encoding/changing DNA |
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Cell |
closed structural, functional, and biological unit of all living organisms ~building blocks of life ~can replicate independently |
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Membrane |
separates and protects a cell from its surrounding environment ~made mostly from a double layer of phospholipids bilayer structure: ~negatively charged hydrophilic heads ~uncharged hydrophobic tails ~provides ways for the cell to decide what gets inside ~receptors decide whats getting in and process info |
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Chemical reaction |
leads to transformation of one substance to another |
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biochemical reaction |
process that leads to transformation of a set of substances to another, usually with the help of a third molecule (enzyme) ~enzyme will fit receptor exactly |
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Drugs |
~drugs are molecules that travel through the blood to the head to bind with fitting receptors ~mimic regular brain functions, but in excess ex. cocaine mimics dopamine ~act at several target sites, have multiple effects ~most drugs don't pass into neurons, but act on surface receptors |
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partition coefficient |
measure of a drug's lipid solubility ~used to predict its relative rate of movement across cell membranes ~extend of ionization determines the oil/water solubility of the drug ~higher solubility = more efficient |
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ionization |
dissociation of an electrically neutral molecule into charged particles (ions) ~most drugs are not readily lipid soluble because they are weak acids or weak bases that become ionized when dissolved in water ~extent of ionization depends on the relative acidity/alkalinity of the solution (pH) and the intrinsic property of the molecule (pKa) |
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pH |
~1-14 scale, 7 is neutral ~acidic solutions lower pH, alkaline/basic solutions higher pH |
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pKa |
~represents the pH of the aqueous solution in which that drug would be 50% ionized and 50% not ionized ~weak acids become ionized quicker in an alkaline environment and less ionized in an acidic environment ~weak bases ionize quicker in acidic environment and less ionized in alkaline environment |
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drugs as agonists |
~ enhance synaptic function by increasing or decreasing neurotransmitter synthesis or release ~prolonging action of the neurotransmitter within the synapse |
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drug competition |
for an enzyme: elevated levels of one drug reduces metabolism of the second, causing potential toxic levels ~ex. alcohol and sedatives (like valium) compete for cytocrome P450 |
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potency |
absolute amount of drug necessary to produce a specific effect ~the less you need for the desired effect, the higher the potency |
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threshold dose |
smallest dose that produces a measurable effect |
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microglia |
~perform phagocytosis (removing dying cells at sites of nerve damage) ~provide immune system function responsible for immune response in cells |
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Schwann cells |
~form myelin sheath in a single axon in the PNS ~release growth factors following neuron damage ~provide a channel to guide axons to targets |
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Oligodendroglia |
~form myelin sheath on multiple axons in the CNS ~ inhibit regrowth of axons following neuron damage |
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Ion channels |
relatively specific for a particular ion (some allow more than one type to pass through) ~most are gated channels: closed and can be opened momentarily by specific stimuli |
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ligand-gated channels |
opens when a ligand binds to a receptor on the channel and changes the shape and opens the gate |
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voltage-gated channels |
opened when electrical potential across the membrane near the channel os altered |
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Resting membrane potential |
difference in electrical charge between inside and outside of cell ~at rest, the inside of the cell is more negative ~selective permeability of the membrane and uneven distribution of ions inside and outside of the cell are responsible for the membrane potential ~uneven distribution is due to specific ion channels |
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action potential |
rapid change in the electrical signal that is sent down the axon ~membrane potential must be changed from resting (-70mV) to the threshold for firing (-50mV) "all or nothing" rapid changes in the membrane potential of neurons allow them to conduct information and influence other cells |
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threshold |
membrane potential (typically -50mV) at which voltage-gated Na+ channels will open, generating an action potential |
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steroids |
soluble in lipids can bypass blood-brain barrier and membrane influences gene expression fig. 1.2 |
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peptides |
interact with gene proteins used as chemical messengers |
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common drugs |
cocaine: mimics dopamine atropine: dilates pupils, effect and site = same morphine: inject anywhere, effects everywhere xanax: activates GABA, calms you down |
