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PHARM Test 1 vocab
Test 1 vocab
Question | Answer |
---|---|
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 |