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61 Cards in this Set
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Pharmacology
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the study of the interaction of chemicals with living systems
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Pharmacokinetics
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the branch of pharmacology that focuses on the effects of absorption, distribution, metabolism, and excretion on the time course of drug concentration on an organism
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ADME
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Pharmacodynamics
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drug receptor interactions and other mechanisms by which drugs affect living organisms
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Pharmacotherapeutics
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The use of medications in the prevention, diagnosis and treatment of diseases and modification of physiology such as reproductive functions
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Adverse drug reaction
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any undesirable and unintended events associated with drug use
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Pharmacological management
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includes the entire realm of assessment, diagnosis, treatment and evaluation of the patients condition
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Toxicology
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deals with undesirable effects of chemicals of living systems
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Drug
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substance that brings about change in biological function through its chemical actions
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What is a component of a cell of organism which interacts with a drug to show observable effects on the body?
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A receptor, which fits like a lock and key
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What does it mean when there are alpha receptors, beta receptors and opoid receptors?
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That they are membrane bound receptors bound to self membrane
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What are the 4 physical nature of drugs?
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solid, liquid, gas, and a weak acid or weak base
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Out of the 4 physical nature of drugs, which one is what most drugs are?
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weak acid or base
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What is the range of Molecular Weight for drug size?
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MW 7-59,500
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What is the MW of most drugs
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100-1,000
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What does the MW need to be in order for the drug to get through the membrane?
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less than 1000
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How do drugs interact with receptors?
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by bonds or chemical forces
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What are the 3 types of bonds that help a drug interact with a receptor
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covalent, electrostatic, hydrophobic
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What is a covalent bond
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strong and not reversible under biological conditions
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The bond formed between the acetyl group of aspirin and it's enzyme target in platelets( cyclooxygenase) is not readily broken down This effect lasts long after free ASA has disappeared from the blood stream, is reversed only by synthesis of new platelets
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What is a electrostatic bond
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Common bond, vary from strong linkages to weaker bonds, these bonds are weaker than covalent bonds
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What is a hydrophobic bond?
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they are quite weak, important in interactions of highly lipid soluble drugs
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What is the drug and receptor represent
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a lock and key
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What are the 3 types of drug receptor interactions
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agonist, antagonist, and partial agonist
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What is an agonist
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binds to receptor good key, opens the lock, It activates the receptor which brings about an indirect or direct affect
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What is an antagonist
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Binds to receptor bad key, it does not open the lock , it prevents binding of other molecules
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acetylcholine receptor blockers such as atropine are antagonists because they prevent access of acetylcholine and similar agonist drugs to the acetylcholine receptor and they stabalize receptor in its inactive state
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What is a partial agonist
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When drugs bind to receptors but do not activate a full response.
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pindolol a beta adrenoceptor
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How long does the duration of a drug last
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it lasts until the drug receptor site is destroyed and new receptors or enzymes are synthesized
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What are 2 drugs that are an example of duration
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ASA and phenoxybenzamine alpha blocker
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Inert binding sites act as what such as plasma proteins an albumin
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they act as storage depot sites which are not available to other areas that are gradually released
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What are the main concepts of Pharmacokinetic Principles?
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Prodrug, Permeation, Fick's Law of Diffusion, and Henderson-Hasselbalch equation
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What does it mean for a chemical to be a pro drug
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The chemical which is readily absorbed, distributed and administered is then converted to the active drug by a metabolism
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What are does permeation of a drug mean?
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How the drug gets into the cell
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What are the main 4 factors of permeation
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aqeous diffusion, lipid diffusion, special carriers, and endocytosis, and exocytosis
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What is aqeous diffusion
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occurs within the interstitial space, cytosol across the epithelial membrane and tight junctions into the cell membrane
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What is lipid diffusion
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THe most important factor to permeation because of the large numbers of lipid barriers that seperate the compartments of the body
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What do special carriers do in permeability
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actve transport which requires energy and facilitated diffusion
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What is Fick's Law of DIffusion
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The passive flux of molecules down a concentration gradient
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What is flux in Fick's Law of Diffusion?
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The amount of chemical that passes through the skin (Molecules per unit in time)
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What is the formula of Fick's law of diffusion
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(C1-C2) X area X permeability coefficient over thickness
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What does C1 and C2 stand for in Fick's law of diffusion
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C1= higher concentration
C2= lower concentration This is the difference in the permeability of the for example the skin |
example of having 1% cream vs. 2% cream, obviuosly the 2 % cream is going to absorb greater than the 1 % cream into the skin
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What is the area in Fick's law of diffusion
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this is the area where diffusion is occuring, Larger the area, more chemicals from a topical drug will get into the body
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all over body compared to finger
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What is the permeability coefficient for Flick's law of diffusion
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Fxn of chemical, some chemicals just get through the skin faster than others
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What does thickness mean in the equation for Fick's law of diffusion?
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larger the thickness, smaller the number flux will be
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skin of arm compared to skin of feet, obviously the drug will not absorb as well on the feet as it will on the arm
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What does protonated and unprotonated mean?
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Protonated means having a hydrogen ion and unprotonated is not having a hydrogen
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For an acid what form is neutral, meaning it is lipid soluble?
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Protonated which haves a hydrogen ion, when the hydrogen ion leaves it is less lipid soluble
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For a base what form is neutral, meaning it is lipid soluble?
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Unprotonated
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Where does the ph need to be for a acid and base to be more lipid soluble?
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For acid it needs to be a low ph and for a base it needs to be a high ph, these become less ionized so more lipid soluble
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Where are most drugs filtered
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glomerulus
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are drugs lipid soluble?
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yes
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When they are lipid soluble are they excreted or are they reabsorbed?
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reabsorbed
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What is ion trapping
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when you have an acidic drug which will accumulate more on the basic side of the membrane compared to a basic drug which accumulates more on the acidic side
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So in theory would a weak acid be excreted faster in alkaline urine or acidic urine?
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alkaline urine
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Would a weak base be excreted better in a more alkalotic or acidotic state?
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Acidic urine
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What is the ph of urine
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5-8
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What is the ph of breast milk
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6.4-7.6
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What is the ph of intestine
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7.5-8.0
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what is the ph in the stomach?
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1.9-2.6
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What in the ph of human blood?
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7.4
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What is the ph for human blood?
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7.4
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Is the urine acidic or alkalotic
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acidic
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Is the intestine alkalotic or acidic
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alkalotic
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Is the stomach more acidic or alkalotic
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very acidic
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