Term
| An experimental science dealing with the properties of drugs and their side effects on living systems |
|
Definition
|
|
Term
| The difference btw a drug & a poison is a matter of _____. |
|
Definition
|
|
Term
| The mechanism of drug rxn is _____ across species. |
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Definition
|
|
Term
| all articles recognized in the USP & NF |
|
Definition
|
|
Term
| Articles intended to be used in the diagnosis, mitigation, Tx, or prevention of diseases in humans & animals |
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Definition
|
|
Term
| articles other than food intended to affect the structure or function of the body |
|
Definition
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|
Term
| 7-chloro-1,3-dihydro-1-methyl 5-prenyl-2H-1,4benzodiazepin 2-one is an example of the _________ of a drug. |
|
Definition
|
|
Term
| The name to identify a particular drug entity (incorrectly called generic name) |
|
Definition
|
|
Term
| Give an example of a nonproprietary name |
|
Definition
|
|
Term
| Brand names assigned & possibly trade marked by a manufacturer. |
|
Definition
|
|
Term
| Give an example of a proprietary name. |
|
Definition
|
|
Term
| To study the response of an organism or tissue to the actions of drugs in the absence of disease |
|
Definition
|
|
Term
|
Definition
| The use of drugs in the Tx of Dz |
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|
Term
| Treatments of diseases in general incl. the use of drugs, Sx, radiation, behavior modification, &/or other modalities |
|
Definition
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|
Term
| The study & characterization of the time course of drug ADME. Basis for drug dosage regimens in various species. |
|
Definition
|
|
Term
|
Definition
| Absorption, Distribution, Metabolism, Excretion |
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|
Term
| a branch of pharmacotherapy dealing w/ drugs that selectively inhibit or destroy specific agents such as bacteria, fungi, viruses or other parasites. Use of this term has been extended for Tx of neoplasms/neoplastic diseases |
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Definition
|
|
Term
| How does the body see drugs, and what does it therefore want to do? |
|
Definition
| Foreign materials; Get rid of them |
|
|
Term
| "Opposite of pharmacology" |
|
Definition
|
|
Term
|
Definition
|
|
Term
| The science that defines limits of safety of chemical agents to humans & animals |
|
Definition
|
|
Term
|
Definition
| The study of sources of drugs/The study of naturally occurring drug sources |
|
|
Term
| Study of medicine dosage, which varies w/ the species of animals as well as individual animals |
|
Definition
|
|
Term
|
Definition
| Quantity of medication to be administered at one time |
|
|
Term
|
Definition
| Determination & regulation of doses |
|
|
Term
| a separate & complementary health care profession concerned w/ collection, preparation, standardization, & dispensing of drugs |
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Definition
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|
Term
| pertaining to or founded on actual observation & tx of patients |
|
Definition
|
|
Term
| An understanding of pharmacology is requisite for the comprehension of _____, _____ & other clinical disciplines. |
|
Definition
|
|
Term
|
Definition
| Minimal Essential Drug Information Checklist |
|
|
Term
| What are the 8 steps of MEDIC |
|
Definition
| Therapeutic Goal, Routes of Administration & Dose Forms, Dose Regimen, Legal/Withdrawal Times, Cost, Special Precautions & Contraindications, Adverse Rxns, Evaluations |
|
|
Term
|
Definition
| A problem-solving approach |
|
|
Term
| With pharmacotherapy, what steps of MEDIC should be used? |
|
Definition
|
|
Term
| Why is the subject of pharmacology so difficult to master? |
|
Definition
| Multiplicity of species concerned |
|
|
Term
| Drug binds to _____ & produces a _____ _____. |
|
Definition
| Receptor; Detectable Response |
|
|
Term
| The component of the organism w/ which a chemical agent acts in some specific fashion to cause an action which leads to an observable effect. |
|
Definition
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|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| Give an example of an intracellular, structural protein receptor. |
|
Definition
|
|
Term
| What are the receptors for anti-cancer drugs? |
|
Definition
|
|
Term
| Give 2 examples of endogenous ligands. |
|
Definition
|
|
Term
| Drugs can aim to _____ or _____ endogenous ligands. |
|
Definition
|
|
Term
| What are the 5 types of molecular binding? |
|
Definition
| Covalent, Electrostatic, Hydrogen, Van Der Waals, Hydrophobic |
|
|
Term
| What are the primary ways that drugs interact with receptors? |
|
Definition
| Electrostatic binding & Hydrogen binding |
|
|
Term
| Binding: Strong, electron pair from both atoms, frequently irreversible |
|
Definition
|
|
Term
| Binding: Common w/ drugs, simple interaction btw opposite charged groups on the receptor & drug, important in attracting drug to receptor |
|
Definition
|
|
Term
| Binding: Sharing of H bonds btw an acidic & basic group, also observed w/ drugs, may help position & stabilize drug on R |
|
Definition
|
|
Term
| Binding: weak attraction btw either a polar or nonpolar molecule, as a group may play a role in receptor shape (agonist v. antagonist) |
|
Definition
|
|
Term
| Binding: interaction of 2 nonpolar substances |
|
Definition
|
|
Term
| What are the 3 types of receptors, and which is the most common? |
|
Definition
| Cell Membrane, Cytoplasm, Nucleus; Cell Membrane |
|
|
Term
| What types of R's does ACh have? |
|
Definition
|
|
Term
| Give 3 examples of membrane bound/NT/Hormone protein R's |
|
Definition
|
|
Term
| What type of R's are NT/Hormone R's? |
|
Definition
|
|
Term
| Give 2 examples of ion channel R's |
|
Definition
| Voltage-sensitive Sodium & Calcium channels |
|
|
Term
| What are 2 types of soluble protein R's? |
|
Definition
| Steroid Hormones, GTP Binding Proteins |
|
|
Term
| Give 2 examples of soluble protein R's. |
|
Definition
| Estrogen, GTPase Activating Proteins |
|
|
Term
| What is 1 example of a steroid hormone R? |
|
Definition
|
|
Term
| What is 1 example of a GTP binding protein? |
|
Definition
| GTPase Activating Proteins |
|
|
Term
| What is 1 example of an allosteric site on an enzyme? |
|
Definition
| Dihydrofoliate reductase inhibitors |
|
|
Term
| What is 1 example of a DNA R? |
|
Definition
| Binding sites for chemotherapeutic agents |
|
|
Term
| Give 2 examples of adrenergic protein R's. |
|
Definition
| Epinephrine, Norepinephrine |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Maximum effect w/ only a portion of the R's occupied |
|
|
Term
|
Definition
| All R's occupied - never reach maximum effect |
|
|
Term
|
Definition
| R's unoccupied at maximum effect |
|
|
Term
| When a full agonist elicits its maximum response, what are the unoccupied R's referred to as? |
|
Definition
|
|
Term
|
Definition
| Block agonists from binding, and therefore diminish the desired effect |
|
|
Term
| What are 3 examples of transduction mechanisms that an agonist can elicit? |
|
Definition
| Enzyme activation/inhibition, Ion channel modulation, DNA Transcription |
|
|
Term
| What is the result of blockers binding to ion channels? |
|
Definition
|
|
Term
| What is the result of modulators binding to ion channels? |
|
Definition
| Increased or Decreased Opening Probability |
|
|
Term
| What is a NT, in terms of its binding to a R? |
|
Definition
|
|
Term
| Of the following, which give a pharmacological response when bound to a R? NT, Agonist, Antagonist. |
|
Definition
|
|
Term
| Of the following, which do not give a pharmacological response when bound to a R? NT, Agonist, Antagonist. |
|
Definition
|
|
Term
| A finite number of R's per cell creates _____. |
|
Definition
|
|
Term
| Drugs have a complementary structure w/ specific R's - This is referred to as _____. |
|
Definition
|
|
Term
| Slightly modify the chemical structure of a drug, and you will modify its _____, therefore its _____. |
|
Definition
|
|
Term
| Drug binds to R & then dissociates in its non-metabolized form. This is referred to as _____. |
|
Definition
|
|
Term
| For Reversibility to be possible, the binding must not be _____ |
|
Definition
|
|
Term
| What is an atypical, more permanent type of binding that is used more by toxins & organophosphates? |
|
Definition
|
|
Term
| As the number of R's occupied increases, the effect _____. |
|
Definition
|
|
Term
| _____ prevents drugs from binding to the wrong R's. |
|
Definition
|
|
Term
| Is a linear or a logarithmic dose response curve a better representation? |
|
Definition
|
|
Term
| What is the plateau on the high end of a DRC? |
|
Definition
| R's saturated, no more increase in response |
|
|
Term
| The same drug & dose can be given orally to 10 dogs, but each DRC will be different. This is due to _____ |
|
Definition
|
|
Term
| What are the types of variability, which change the DRCs? |
|
Definition
| Patient, Environmental Factors, Disease. Drug |
|
|
Term
| Give an example of environmental variability. |
|
Definition
| Whether the animal has eaten recently |
|
|
Term
| In patients with hepatic disease, the effects of a drug are _____ _____ |
|
Definition
|
|
Term
| What are 2 factors that can affect drug clearance? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Inherent power or strength related to dose |
|
|
Term
| What is potency a function of? |
|
Definition
| Drug's affinity for R & ADME Factors |
|
|
Term
|
Definition
| Dose-Response relationships |
|
|
Term
| What are 4 measurements of Effect? |
|
Definition
| Molecular Response, Cellular Response, Organ Response, Whole Animal Response |
|
|
Term
| What measurement of effect looks at Modulation of enzyme activity/movement of ions across the plasma membrane? |
|
Definition
|
|
Term
| What measurement of effect looks at modulation of secretion of hormone or NT or the modulation of cell motility? |
|
Definition
|
|
Term
| What measurement of effect looks at smooth m. contraction? |
|
Definition
|
|
Term
| What measurement of effect looks at behavior changes/response can be lethal? |
|
Definition
|
|
Term
| If a drug has an ED50=30, and LD50=70, is the drug marketable? |
|
Definition
|
|
Term
| At LD50, what is happening? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| How do you calculate the therapeutic index? |
|
Definition
|
|
Term
| ED50 & LD50 should be _____. |
|
Definition
| As separated/far away from e/o as possible |
|
|
Term
| Is 2.3 considered a small or large TI? |
|
Definition
|
|
Term
| Is 10 considered a small or large TI? |
|
Definition
|
|
Term
| > ____ is considered a safer TI |
|
Definition
|
|
Term
| Does Warfarin have a small or large TI? |
|
Definition
|
|
Term
| Does Penicillin have a small or large TI? |
|
Definition
|
|
Term
| What are 3 types of antagonism? |
|
Definition
| Receptor, Physiological, Chemical |
|
|
Term
| Which type of antagonism refers to drugs binding to & possibly degrading other drugs? |
|
Definition
|
|
Term
| Which type of antagonism refers to opposing physiological effects of 2 drugs? |
|
Definition
|
|
Term
| Is it more desirable to have a small or large TW? |
|
Definition
|
|
Term
| What is the Therapeutic Window? |
|
Definition
| ~ED50 to 1st instances of LD & unwanted adverse effects |
|
|
Term
| What is the most common mechanism of receptor antagonism? |
|
Definition
|
|
Term
| What are the mechanisms of R Antagonism? |
|
Definition
| Competitive (Competitive Antagonism), Pseudo-Irreversible/Non-Competitive, Allosteric (Antagonism or Potentiation) |
|
|
Term
| Which type of antagonism is this? Agonist A & Antagonist B compete (both have specificity). As curve shifts R, more & more A is needed to produce desired response. |
|
Definition
|
|
Term
| Which type of antagonism is this? B binds and stays. No more effect, even w/ large quantities of A administered. |
|
Definition
| Noncompetitive Antagonism |
|
|
Term
|
Definition
| Different binding sites for A & B |
|
|
Term
| With Potentiation, B binding will _____ the affinity of A for its R. |
|
Definition
|
|
Term
| With allosteric antagonism, B binding will _____ the affinity of A for its R. |
|
Definition
|
|
Term
| Does allosteric antagonism entirely shut down A's efficacy? Why or why not? |
|
Definition
| No; Saturability component (B binding is a saturable response) |
|
|
Term
| What is pharmacokinetics? |
|
Definition
| Disposition & fate of drugs in the body |
|
|
Term
| Most effective use of drugs is based on an understanding of pharmacodynamic & pharmacokinetic principles w/ some understanding of product formulations |
|
Definition
|
|
Term
| To produce an effect, a drug must ______ at ______. |
|
Definition
| Reach effective concentrations; Site of action |
|
|
Term
| Species variability is usually explained by _____ or ________. |
|
Definition
| Biphasic availability; inherent tissue sensitivity at the R sites |
|
|
Term
| Most species differences are due to _____ |
|
Definition
|
|
Term
| True or False: Drugs have different therapeutic range across species. |
|
Definition
|
|
Term
| What may be a preferable method of determining dose, rather than per kg BW? |
|
Definition
|
|
Term
|
Definition
| Drug absorption & distribution |
|
|
Term
| What determines R site concentrations? |
|
Definition
|
|
Term
| What terminates drug action? |
|
Definition
| Biotransformation/Metabolism & Excretion |
|
|
Term
| _____ are very important to ADME. |
|
Definition
|
|
Term
| Membranes are a _____ to drug transport. |
|
Definition
|
|
Term
| What is the rate limiting step in pharmacokinetics? |
|
Definition
| Dissolution of drug/Release from solid dosage form |
|
|
Term
| How is drug dissolution bypassed? |
|
Definition
|
|
Term
| What happens to a drug when it is biotransformed/metabolized? |
|
Definition
| More polar, more readily eliminated |
|
|
Term
| What is the most common way drugs move across membranes? |
|
Definition
|
|
Term
| Drugs move across membranes by _______ or by _______. |
|
Definition
| Passive transfer; Specialized Transport Processes |
|
|
Term
| What type of molecules move across membranes easily? |
|
Definition
|
|
Term
| AT is _____ & therefore _____. |
|
Definition
|
|
Term
| W/ passive transfer, how to molecules diffuse through the membrane? |
|
Definition
| Across concentration gradient |
|
|
Term
| What type of molecules can pass through passive diffusion? |
|
Definition
| Any w/ sufficient lipid solubility |
|
|
Term
| Rate of passive transfer is directly proportional to _____ across the membrane and the _____. |
|
Definition
| Concentration Gradient; Lipid-Water Coefficient |
|
|
Term
| What is the most important mechanism of drug transfer? |
|
Definition
|
|
Term
| What is an important characteristic of carrier mediated transport? |
|
Definition
|
|
Term
| Do AT & FD require energy? |
|
Definition
|
|
Term
| Is carrier mediated transport saturable? |
|
Definition
|
|
Term
| Give a location of AT for drug elimination. |
|
Definition
|
|
Term
| Where does passive reabsorption occur in the nephron? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| What are 2 critical physiochemical factors in drug absorption? |
|
Definition
|
|
Term
| What are some other important physiochemical factors? |
|
Definition
| Site, lipid solubility (unless placed w/i vicinity of capillary beds), |
|
|
Term
| Even drugs w/ MW as great as _____ may be absorbed though capillary walls by passive diffusion. |
|
Definition
|
|
Term
| In general, most drugs are weak acids or bases that are present in soln as both the ____ and _____ species. |
|
Definition
|
|
Term
| Do nonionized or ionized molecules have better lipid solubility? |
|
Definition
|
|
Term
| The degree of ionization of a drug d/o its ___ & the ___ of its environment. |
|
Definition
|
|
Term
| For a weak acid, the % ionized is... |
|
Definition
|
|
Term
| For a weak base, the % ionized is... |
|
Definition
|
|
Term
| When like is in like, the drug is mostly _____. |
|
Definition
|
|
Term
| When like is in unlike, the drug is mostly _____. |
|
Definition
|
|
Term
| Where will weak bases probably be absorbed? |
|
Definition
|
|
Term
| How do you calculate the concentration ratio for a weak acid? |
|
Definition
| pH-pka=log (conc ion/conc non) |
|
|
Term
| How do you calculate the concentration ratio for a weak base? |
|
Definition
| pH-pka=log(conc non/conc ion) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| At a steady state, an acidic drug will accumulate on the more _____ side of the membrane, and a basic drug on the more _____ side |
|
Definition
|
|
Term
| At a steady state, an acidic drug will accumulate on the more basic side of the membrane, and a basic drug on the more acidic side |
|
Definition
|
|
Term
| What is bypassed with parenteral administration? |
|
Definition
|
|
Term
| What are the major parenteral routes? |
|
Definition
|
|
Term
| What are some other parenteral routes? |
|
Definition
| intrarticular, subconjunctival, epidural |
|
|
Term
| What is necessary when using parenteral injection? |
|
Definition
|
|
Term
| What is meant when we say that IV inj is "unforgiving?" |
|
Definition
| Immediate placement into systemic sys, drug can't be stopped if an adverse rxn is encountered. |
|
|
Term
| What is the bioavailability of IV drugs? |
|
Definition
|
|
Term
| IV inj gives a _____ concentration in plasma and an _____ pharmacological response. |
|
Definition
|
|
Term
| Can the rate at which a drug is introduced systemically into an animal be controlled w/ IV inj? |
|
Definition
|
|
Term
| Certain _____ & _____ soln's must be given IV only to avoid tissue damage. |
|
Definition
|
|
Term
| Drugs in ______ or ______ should not be given IV. |
|
Definition
| oily vehicle; drug suspensions |
|
|
Term
| Continuous IV infusions are satisfactory for achieving and maintaining _____ |
|
Definition
| Steady state concentrations |
|
|
Term
| Can administer a _______ to more rapidly achieve steady state levels. |
|
Definition
|
|
Term
| IM/SQ inj have ______ absorption. |
|
Definition
|
|
Term
| What does epinephrine do to the injection site? |
|
Definition
| Decreases vascularity, keeping the drug local |
|
|
Term
| Give an example of a gaseous anesthetic. |
|
Definition
|
|
Term
| How are gaseous anesthetics absorbed? |
|
Definition
| Diffusion across pulmonary epithelium |
|
|
Term
| Gaseous anesthetics vary in their degree in _______ which affects their rate of action, the ease at which the depth of anesthesia can be changed and the speed of recovery. |
|
Definition
|
|
Term
| What determines rate of absorption for IM/SQ inj's? |
|
Definition
| Vascularity of inj site, drug conc in soln, degree of ionization, lipid solubility, area of absorbing surface to which drug is exposed |
|
|
Term
| Give an example of a drug that is not completely available. |
|
Definition
|
|
Term
| Give an example of a drug that causes injection site pain. |
|
Definition
|
|
Term
| Give an example of a drug with sustained release. |
|
Definition
|
|
Term
| What is a disadvantage to IM/SQ inj? |
|
Definition
| drug can't be stopped if an adverse rxn is encountered |
|
|
Term
| What is another name for transdermal? |
|
Definition
|
|
Term
| What 3 events must an orally administered drug undergo before entering the systemic circ? |
|
Definition
1. Release of drug from solid dosage form (Dissolution)
2. Transport across GI Mucosal Barrier
3. Passage through Liver (First Pass Metabolism) |
|
|
Term
| What is the most common form of drug administration? |
|
Definition
|
|
Term
| What are 2 types of implantation administration? |
|
Definition
| Pellet, Osmotic mini-pump |
|
|
Term
| What does absorption of a percutaneous administration d/o? |
|
Definition
| Release from drug vehicle & penetration of keratin layer (stratum corneum) |
|
|
Term
| How does percutaneous absorption occur? |
|
Definition
|
|
Term
| What is the most important feature of a percutaneous drug? |
|
Definition
|
|
Term
| What type of skin promotes absorption of percutaneous admin? |
|
Definition
|
|
Term
| What are 2 vehicles form percutaneous admin? |
|
Definition
| Oil in water emulsions; Dimethyl sulfoxide |
|
|
Term
| What do oil in water emulsions do for transdermal inj? |
|
Definition
|
|
Term
| What does DMSO do for transdermal inj? |
|
Definition
| promotes absorption by rapidly carrying drugs through skin |
|
|
Term
| What polarizes drugs in the liver? |
|
Definition
|
|
Term
| Via what structure is a drug transported from the gut into the liver? |
|
Definition
|
|
Term
| How is dissolution of a drug enhanced? |
|
Definition
| Administering the drug as a salt |
|
|
Term
| What is one way of enhancing the absorption of a drug? Give an example. |
|
Definition
| Decreasing the particle size (Micronization); Griseofulvin |
|
|
Term
| What dissolves better than the micronized form of a drug? |
|
Definition
|
|
Term
| What are some factors affecting stability of a drug in GI fluids? |
|
Definition
| Enzymatic degradation, Acid instability, Complexed |
|
|
Term
| Give an example of enzymatic degradation. |
|
Definition
|
|
Term
| Give an example of acid instability. |
|
Definition
|
|
Term
| Give an example of a complexed drug. |
|
Definition
|
|
Term
| What is the principle site of absorption for orally administered drugs? |
|
Definition
|
|
Term
| What is an important determinant of drug absorption in the SI? |
|
Definition
|
|
Term
| Is gastric emptying the same across species? |
|
Definition
|
|
Term
| In what animals is gastric emptying the most important factor controlling drug absorption rate? |
|
Definition
|
|
Term
| What is the gastric pH in horses? How does this affect drug absorption? |
|
Definition
| Higher (5.5); some absorption occurs in LI |
|
|
Term
| What is the pH in the rumen? |
|
Definition
|
|
Term
| What maintains the rumen pH |
|
Definition
| Alkaline saliva (pH 8-8.4) |
|
|
Term
| Where are weak acids absorbed in ruminants? |
|
Definition
|
|
Term
| What happens to weak bases in ruminants? |
|
Definition
| Ionically trapped from systemic circulation |
|
|
Term
| What causes low starting concentrations in ruminants? |
|
Definition
| Rumen volume, Microflora metabolism |
|
|
Term
|
Definition
| The rate & extent to which a drug administered in a particular dosage form enters the systemic circulation |
|
|
Term
| What are 3 ways to calculate bioavailability? |
|
Definition
| Peak plasma concentration, Time to reach peak concentration, AUC |
|
|
Term
|
Definition
|
|
Term
| What would the Plasma Concentration over Time curve look like for an orally administered drug? |
|
Definition
| Starts at low plasma conc, gradually increases over time, then slowly decreases |
|
|
Term
| What does a lower AUC represent? |
|
Definition
|
|
Term
| Can an orally administered drug be 100% BA? |
|
Definition
|
|
Term
| Oral availability is calculated against _____. |
|
Definition
|
|
Term
|
Definition
|
|
Term
| What are some factors influencing oral bioavailability? |
|
Definition
| Poor dissolution of drug product, instability of drug, poor passage of drug through mucosa, drug metabolism in the intestine or liver |
|
|
Term
| What orally administered drug has a bioavailability of 80% & Why? |
|
Definition
|
|
Term
| What is the BA of orally administered Propranolol? Why? |
|
Definition
|
|
Term
| Is BA the same across species? |
|
Definition
|
|
Term
| Why does the goat have such a low AUC? |
|
Definition
|
|
Term
| What accounts for a large majority of dosage differences across species? |
|
Definition
| Species differences in BA |
|
|
Term
| Why do cats have limited excretion of drugs? |
|
Definition
| Limited hepatic biotransformation |
|
|
Term
| Why do cows generally require higher doses of drugs, more frequently? |
|
Definition
| Diluting effect of the large GI tract |
|
|
Term
| What does the FDA expect for generic drugs? |
|
Definition
|
|
Term
| 2 drugs are bioequivalent when ______. |
|
Definition
| The rates & extents of absorption of the active ingredient in the 2 products are not significantly different under suitable test conditions. |
|
|
Term
| What is usually used to compare generic products with trademarked drugs? |
|
Definition
|
|
Term
| What are the 2 phases of a dissociation curve? |
|
Definition
| Distribution (alpha) phase & Elimination (beta) phase |
|
|
Term
| What graphically defines the decline in the plasma conc of a drug after IV admin? |
|
Definition
|
|
Term
| A disposition curve is used for _____ administration. |
|
Definition
|
|
Term
| What is the distribution phase of a distribution curve? |
|
Definition
| Attributed to rapid distribution into tissues & organs |
|
|
Term
| What is the elimination phase of a distribution curve? |
|
Definition
| Removal of drug by biotransformation & excretion |
|
|
Term
| Which phase of the disposition curve has a steeper slope? |
|
Definition
|
|
Term
| How can you tell that a graph is showing IV admin? |
|
Definition
| Drug conc. starts at peak and then goes down |
|
|
Term
| What order is drug elimination for IV drugs? |
|
Definition
|
|
Term
| What does first order elimination mean? |
|
Definition
| Constant fraction eliminated per unit time |
|
|
Term
| Which phase of the disposition curve is 1/2L calculated from? |
|
Definition
|
|
Term
|
Definition
| Add up all trapezoids + triangle |
|
|
Term
|
Definition
| The time req'd for the body to eliminate 1/2 of the drug |
|
|
Term
| What can knowledge of half life be used to predict? |
|
Definition
| Quantity of drug remaining in the body |
|
|
Term
| What is likely to cause change in the usual half-life of a drug? |
|
Definition
| Any state that alters either access of the drug to the organs of elimination or activity of the eliminating mechanism |
|
|
Term
| What are some factors influencing half-life? |
|
Definition
| Maturity, Drug interactions, Urinary pH, Species difference |
|
|
Term
| Do young animals eliminate drugs more quickly or more slowly than adult animals? Why? |
|
Definition
| More slowly; Lack mature drug metabolism enzymes |
|
|
Term
| Half lives are different/the same across species? |
|
Definition
|
|
Term
| Can half-life be used to determine the time to reach steady state? |
|
Definition
|
|
Term
| Factors that tend to keep the drug in the blood will usually _____ the VD. |
|
Definition
|
|
Term
| What is the volume of fluid that would be req'd to contain the amt of drug in the body if it were uniformly distributed at a conc = to that in plasma? |
|
Definition
|
|
Term
| Does a highly water-soluble drug have a small or large VD? |
|
Definition
|
|
Term
| Does a highly lipid-soluble drug have a small or large VD? |
|
Definition
|
|
Term
| What are 2 factors that tend to keep a drug in the blood? |
|
Definition
| High water solubility & High protein binding |
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|
Term
| What represents the total drug clearance based on the concept of the body as a whole acting as a drug eliminating system? |
|
Definition
|
|
Term
| What is body clearance defined as? How is it expressed? |
|
Definition
| V plasma cleared of drug by various elimination processes per unit time; ml/min/kg |
|
|
Term
| Give an example of 2 drugs with the same body clearance. |
|
Definition
|
|
Term
| If 2 drugs have the same body clearance, do they also have the same half life? |
|
Definition
|
|
Term
| For drugs w/ similar body clearance values, the smaller the VD, the _____ the half-life. |
|
Definition
|
|
Term
| Binding of drug to PP limits drug ______ & _____. |
|
Definition
| Distribution & Elimination |
|
|
Term
| True or false? Protein binding is an irreversible process. |
|
Definition
|
|
Term
| The drug-protein complex serves as a circulating reservoir of _________. |
|
Definition
|
|
Term
| What PP does binding occur to? |
|
Definition
|
|
Term
| How is PP Binding expressed? |
|
Definition
|
|
Term
| PP Binding keeps drug trapped in _______. |
|
Definition
|
|
Term
| What % of PP Binding is considered extensively protein bound? |
|
Definition
|
|
Term
| What % of PP Binding is considered moderately protein bound? |
|
Definition
|
|
Term
| What % of PP Binding is considered low protein binding? |
|
Definition
|
|
Term
|
Definition
| Dose less than available binding sites |
|
|
Term
|
Definition
| Dose greater than available binding sites |
|
|
Term
| Give some examples of drugs that are extensively bound to PP. |
|
Definition
| Warfarin, Digoxin, Diazepam, Propranolol |
|
|
Term
| True or False? With class I drugs, all binding sites are occupied. |
|
Definition
|
|
Term
| True or False? With class II drugs, all binding sites are occupied. |
|
Definition
|
|
Term
| Do class I or II drugs have a higher concentration of free drug? |
|
Definition
|
|
Term
| Do Class I or II drugs occupy all binding sites? |
|
Definition
|
|
Term
| When 2 highly protein bound drugs are used concurrently, displacement from binding sites can result in ________. |
|
Definition
| Increased free (active) drug |
|
|
Term
| What happens when a Class I & a Class II drug are administered concurrently? |
|
Definition
| Displacement of Class I drug occurs. |
|
|
Term
| What is enzymatic alteration of a drug? |
|
Definition
|
|
Term
| Drugs undergo metabolic changes that favor their _____ & _____. |
|
Definition
|
|
Term
| Drugs generally become less/more lipid-soluble, & less/more polar. |
|
Definition
|
|
Term
| What type of compounds are more suitable for carrier-mediated excretion processes? |
|
Definition
|
|
Term
| The general pattern of drug elimination is usually _____. |
|
Definition
|
|
Term
| What are the main organs of drug elimination? |
|
Definition
| Liver, kidneys, lungs, plasma, intestinal mucosa |
|
|
Term
| What are the types of Phase I rxn's? |
|
Definition
| Oxidation, Reduction, Hydrolysis |
|
|
Term
| What are the types of Phase II rxn's? |
|
Definition
|
|
Term
| After a Phase I rxn, the drug may be _____, _____, or _____. |
|
Definition
| Activated, Unchanged, Inactivated |
|
|
Term
| After a Phase II rxn, the drug is usually _____. |
|
Definition
|
|
Term
| True or False? A drug must pass through a Phase I rxn before passing through a Phase II rxn. |
|
Definition
|
|
Term
| Phase I rxn's unmask or introduce _____ groups, such as _____ or _____. |
|
Definition
|
|
Term
| Phase II rxn's conjugate the drug to _____ compounds. |
|
Definition
|
|
Term
| Conjugates are usually _____ & _____. |
|
Definition
| Water-soluble, Pharmacologically inactive |
|
|
Term
| _____ structure predicts metabolic transformation. |
|
Definition
|
|
Term
| Give 4 examples of drug conjugates. |
|
Definition
| Glucaronic acid, Acetate, Sulfate, aa's |
|
|
Term
| What are the 3 options for drug metabolism? |
|
Definition
1. Active to Inactive
2. Active to Active Metabolite
3. Inactive to Active |
|
|
Term
| What is the term for an inactive drug that is metabolized to an active drug? |
|
Definition
|
|
Term
| Give an example of a drug that is converted from active to inactive. |
|
Definition
|
|
Term
| Give an example of a drug that is converted from active to active metabolite. |
|
Definition
|
|
Term
| Give an example of a drug that is converted from inactive to active. |
|
Definition
|
|
Term
| True or False? Drug elimination is first order for all methods of administration. |
|
Definition
|
|
Term
| What are some examples of oxidative rxn's? |
|
Definition
| O-dealkylation, N-dealkylation, Oxidative deamination |
|
|
Term
| Is aromatic hydroxylation phase I or II? |
|
Definition
|
|
Term
| Is oxidative deamination phase I or II? |
|
Definition
|
|
Term
| Is glycine conjugation phase I or II? |
|
Definition
|
|
Term
| What toxic metabolite is made by cats treated with acetaminophen? |
|
Definition
|
|
Term
| What normally absorbs NAPQI in the body? |
|
Definition
|
|
Term
| What cells are affected by NAPQI? |
|
Definition
|
|
Term
|
Definition
| A glutathione donor that absorbs NAPQI |
|
|
Term
|
Definition
| Microsomal Enzyme Inhibitor that decreases oxidation rxn |
|
|
Term
| What type of rxn takes place when a drug or Phase I metabolite contains a chemical group suitable for combining w/ a natural compound to form a readily excreted polar metabolite? |
|
Definition
|
|
Term
| Synthetic rxns take place when a _____ or _____ contains a chemical group suitable for combining w/ a natural compound to form a readily excreted polar metabolite. |
|
Definition
|
|
Term
| Name a few conjugating agents. |
|
Definition
| Glucaronic acid, Glycine, Cysteine, Methionine, Sulfate, Acetyl |
|
|
Term
| What conjugation rxn is absent in the dog? |
|
Definition
|
|
Term
| What conjugation rxn is present, but at a slow rate in the cat? |
|
Definition
|
|
Term
| If a drug's primary BT is ____, it must be adjusted for the dog. |
|
Definition
|
|
Term
| What is the primary organ of BT? |
|
Definition
|
|
Term
| Microbial metabolism may occur after _____ or _____ |
|
Definition
| Oral administration of a drug; Passive diffusion of non-ionized drug from systemic circ. into GI lumen |
|
|
Term
| ____ & _____ rxn's are the most common in microbial metabolism. |
|
Definition
|
|
Term
| _____ of glucaronide conjugates by bacterial beta-glucaronidase occurs in the _____. |
|
Definition
|
|
Term
| In ruminant microflora, chloramphenicol is inactivated by _____ of the nitro group. |
|
Definition
|
|
Term
| Alterations in the _____ of metabolism can affect _____ of drug action. |
|
Definition
|
|
Term
| Phenobarbital ____ enzyme synthesis. |
|
Definition
|
|
Term
| Chloramphenicol ____ microsomal enzyme activity. |
|
Definition
|
|
Term
| Decreased hepatic blood flow _____ the rate of metabolism. |
|
Definition
|
|
Term
| Decreased serum protein _____ drug availability for metabolism. |
|
Definition
|
|
Term
| What can be added to increase the half life of a drug? Give an example. |
|
Definition
| A microsomal enzyme inhibitor; ex: BNPP added to Propanidid |
|
|
Term
| What is the primary method of excretion for drugs with limited lipid solubility and are ionized at physiological pH? |
|
Definition
|
|
Term
| What are 3 mechanisms of renal excretion? |
|
Definition
| Glomerular filtration, Carrier-mediated excretion, Passive Reabsorption |
|
|
Term
| What type of drugs undergo glomerular filtration? |
|
Definition
|
|
Term
| What type of drugs undergo carrier-mediated excretion? |
|
Definition
|
|
Term
| What cells perform carrier-mediated excretion? |
|
Definition
|
|
Term
| Can carrier-mediated excretion be saturated? |
|
Definition
|
|
Term
| What does carrier-mediated excretion req? |
|
Definition
| Energy & nonspecific carriers of organic acids & bases |
|
|
Term
| Is carrier mediated excretion affected by protein binding? |
|
Definition
|
|
Term
| Where does passive renal absorption occur? |
|
Definition
|
|
Term
| Give a few examples of some acidic drugs excreted by carrier-mediated process. |
|
Definition
| Penicillin G, Ampicillin, Phenylbutazone |
|
|
Term
| Give a few examples of some basic drugs excreted by carrier-mediated process.. |
|
Definition
| Dopamine, Trimethoprim, Procainamide |
|
|
Term
| Give an example of an organic acid. |
|
Definition
|
|
Term
| What is the pka of salicylate? |
|
Definition
|
|
Term
| Salicylate toxicity can result in _____ filtrate w/ a urinary pH ____ |
|
Definition
|
|
Term
| More drug is I/U w/ an acidic filtrate. |
|
Definition
|
|
Term
| More drug is U w/ an acidic filtrate, thus it is _____. |
|
Definition
|
|
Term
| Urinary _____ with salicylate overdose promotes excretion. |
|
Definition
|
|
Term
| Quantitatively, biliary excretion is less/more important than renal excretion. |
|
Definition
|
|
Term
| What type of compounds are conjugated in hepatocytes w/ glucaronic acid & excreted in the bile? |
|
Definition
|
|
Term
| Enterohepatic circulation - Lipid reabsorption in the _____; prolongs/diminishes drug half-life. |
|
Definition
|
|
Term
| Loading dose; Constant infusion |
|
Definition
| Steady state concentration |
|
|
Term
| Plasma conc of the drug w/i therapeutic range for duration of Tx. |
|
Definition
|
|
Term
| _____ must be maintained during therapy to achieve the desired therapeutic response. |
|
Definition
|
|
Term
| single or multiple; rate; dosage interval; systemic availability |
|
Definition
|
|
Term
| conc of drug in plasma necessary to produce the desired pharmacological response |
|
Definition
|
|
Term
| What is the key route of elimination of Digoxin? |
|
Definition
|
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