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PHARM Test 1 vocab

Test 1 vocab

QuestionAnswer
Absorption Process of drug transfer from site of administration out of GI tract
Affinity ability to bind to a receptor - a measure of "tightness" to a receptor - extent to which the ligand is capable of binding and remain bound - determines [drug] needed for a certain # of drug-receptor complexes
Agonist a different molecule that activates the signalling cascade upon binding - inhibition = concentration dependent - have affinity and efficacy
Antagonist does NOT activate signalling cascade upon binding - prevents agonist from activating response - have affinity but no efficacy
Autoinduction an inducer that increases the rate of its own metabolism - can be the a cause of tolerance
Bioavailablility term to describe availability - measures # or portion of oral dose makes it to systemic circulation - Foral = AUCpo/AUCiv (area under curve)
Bioequivalence Generic drugs must have bioequivalence - where rate and extent of absorption must not be different or any difference must not be medically significant
Biotransformation basically ADME (pharmokenetics)
Blood-Brain Barrier highly lipid soluble can pass - polar cannot. ABC transporteres rapidly transport drugs out - glial wrapping increases need for lipid solubility
Clearance quantitative measure of ELIMINATION
Competitive Reverse Antagonism Lowers Kd or POTENCY - binds to the anagonist receptor binding site
CSF Certain Safety Factor = LD1/ED99
Cytochrome P-450 not specific group of enzymes that metabolizes alot of drugs - CYP34A, CYP2D6, CYP2c19
DEA Drug Enforcement Agency - under the Justice Department - classifies controlled drugs into "5 Schedules"
Distribution drug must pass through circulatory, capillary wall, cell membrane to get to target tissue - lipid unionized molecules are the best
Excipients "Extra Junk" in a pill or capsule that is not the actual drug - could be inactive sunstances, bulk up formulations, drug stabilizers, color, solubility, binding, or lubrication
LD50 lethal dose for 50% of population
TD50 toxic dose for 50% of population
ED50 drug concetration that produces 50% of the max effect on a Dose- Response Curve - can be referred to as POTENCY as it can be compared to other ED50's
Emax max response that can be produced in a Dose-Response Curve - a measure of EFFICACY!!!
Dose how much drug is given
Dose Response Curve In a 'system', drug responses increase proportionally with dose in a hyperbolic curve
Dose-Dependent Kinetics rate if elimination depends on concentration of drug - elimination pathways are saturated
Drug chemical (except food) that affects living systems (NOT pills, tablets or capsules)
Drug Interaction influence of one drug on the effect of another
Drug Product pills, tablets, or capsules
Druge Selectivity ability to affect 1 tissue type, cell type, or organ, and spare others - depends on: dose, drug distribution, receptor distribution, or receptor selectivity.
Drug Substance active drug ingredient
Efficacy- Intrinsic Activity extent to which a bound ligand activates a receptor - antagonist have 0 intrinsic activity - High intrinsic activity = high effect
Enteral involves absorption through the GI tract
Excretion process of drug elimination - kindey = KEY
Extraction Ration ER = (Ci-Co)/Ci - High ER means lots were extracted thus LOW bioavailability
Food and Drug Administration (FDA) The administration where drugs companies get approval for their drug
First Pass Drug Have high extraction ratio - meaning not much make it pass liver and enter systemic circulation
First Pass Effect drugs absorbed through the gut must first pass bacterial enzymes in intestines, enzymes in intestinal cells, and liver enzymes - decreases the bioavailability of drugs by metabolization
Glomerular Filtration small molecules pass through here by flitration 100-120 ml/min
Graded Dose Response graph of increasing response to increasing dose
Half-life time it takes for half of a drug to be eliminated
Hypersensitivity undesirable effect produced by the immune system
Idiosyncracy genetically determined abnormal response to a drug - may be quantitative or qualitative
Induction increased enzyme level (ex= cyp p450 can be induced to increase metabolism)
Investigatoinal New Drug Application (IND) FDA has 30 to review a drug's application - need in order to test the drug on human subjects
IRB Schools and Hospitals must have these- reviews a proposed clinical study for: scientific merit, ethical acceptability, protection of patient rights, informed conset in lay terms
Margin of Safety b/w ED99 and LD1 - the drug should be safe withing these concentations
Metabolic Activation a prodrug uses this - metabolism changes a drug from inactive to active
New Drug Application Sumbitted to FDA for approval - $1.54 Mil fee - contains manufacturing, formulation, preclinical, and clinal data - evaluates if drug is safe and effective, if the labelling is appropriate, and overal quality control of manufacturing
Non-Competitive Antagonism changes receptor to decrease efficac of agonist - is potency independent of dose and relative affinity of agonist cuz it binds to a dif site - eliminates a fraction of total receptors
OTC over-the-counter - deemed safe w/o medical supervision - can still be toxi - higher safety standards must be shown
Parenteral route of administration that ivolves piercing the skin - IV, subcutanous and intramuscular are examples
Partial Agonist drug that interacts with the same receptor but cannot produce same maximal effect of efficacy
Partition Coefficient High partion constant = high lipid solubility - and can pass through membranes [ drug ] in lipid phase/[ drug ] in aqueous phase
Pharmacodynamics actions of a drug on the body- involves receptor binding, post receptor effects and chemical interactions
Pharmacokinetics actions of the body on the drug - ADME (absorption, distribution, metabolism, excretion)
Pharmacological Antagonism Binds but does NOT activate receptor - effect is derived from preventing agonist binding and activation of receptor
Physiological or Functional Antagonism 2 drugs that produce opposite effects through different receptor systems - example = acetylcholine and norepinephrine
Placebo a positive control intented to decieve the recipient
Post-Marketting Surveillance may be mandated by FDA or undertaken but drug company - post approval safety monitoring - detect rare or long term side effects - afterwards may have to revise, include restrictions or remove from market
Potency related to the amount of drug needed to produce a given intensity of effect - determined by: affinity of receptor for drug and efficacy (lower Kd or ED50 = more potent)
Potentiation 0+2=10 drug A inhibits a process that blocks Drug B from having an effect which increases the effect
Quantal Dose Response Number of individuals w/in a group responding to a given dose - either a yes or no - used to find therapeutic index
Receptor what drugs bind to - determeines the relationship b/w drug dose and pharmacological effect - can be affected by receptor affinity or receptor number
Schedule Drug (Controlled) controlled drug by the DEA - scheduled according to: medical usage, abuse liability, or tendency to develop dependency - 1-5 with 1 being the worst
Side Effect synonymous with toxicity (produces an adverse effect)
Spare Receptors excess receptors at some sites- max biological response w/ only a fraction of the receptors occupied. This increased receptor number = increased sensitivity- lowers E50 - Kd50 stays the same
Synergism 2+3= 20 great for cancer drugs - 2 drugs together are greater than drugs by itself
Theraputic Index TI= LD50/ED50 - drug's safety margin - must be > 1 for a drug to be usable. Higher # = safer
Theraputic Window between MTC and MEC - range of plasma concentraion between minimal toxic and effective concentration
Tolerance a state of progessively decreasing responsiveness responsiveness to a drug - ie. larger drug dose requuired to achieve same effect
Topical applied with no intention of absorption and for local effects - should be lipid-insoluble
Toxicity leads to an adverse effect
Volume of Distribution =D/Cpo - a volume into which the total amount of drug would be UNIFORMLY distributed to give the observed plasma - does NOT tell you where drug is but rather that it is bound or in a compartment -higher Vd = longer in body
Fast absorption Methods Buccal, Intramuscula, Intravenous (IV), Inhalation, Intrathecal(drug into CSF)
Slow absorption methods Rectal, Percutaneous (transdermal ie on skin), Topical (no aborption), Subcutaneous
Created by: edwardccbb
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