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allelipraise's version from 2017-11-09 05:18

Section 1

Question Answer
ZERO ORDERConcentration- independent
ZERO ORDERTime- dependent
ZERO ORDERFixed amount of drug is removed per unit time
ZERO ORDERIn graph: conc (y) and time (x) produces straight line
ZERO ORDERFollows Non-Linear pharmacokinetics
ZERO ORDERType of process that ends
FIRST ORDERConcentration- dependent
FIRST ORDERTime- independent
FIRST ORDERFixed percentage of drug is removed per unit time
FIRST ORDERIn graph: natural logarith (ln) conc(y) and time (x) produces straight line
FIRST ORDERFollows linear pharmacokinetics
FIRST ORDERType of process that never ends
FIRST ORDERDescribes the rate or drug movement between compartment
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Section 2

Question Answer
PharmacokineticsStudy and characterization of the time course of drug liberation, absorption, distribution, metabolism and excretion.
Chemical KineticsStudy of chemical processes and rates of reactions or processes.
Pharmacokinetic ModelsHypothesis that utilize mathematical terms to quantitatively describe relationships in biological processes in the body.
Compartment Model Empirical Model
Compartment ModelDescribes the fate of a drug in the body, depicted as an entity divided into compartments.
Compartment ModelMost widely used approach to pharmacokinetic characterization of drug.
Compartment ModelType of model that interpolate the experimental data and allow on empirical formula to estimate drug concentration with time.
CompartmentGroup of tissues with similar blood flow and drug affinity.
Rate ConstantUsed to represent rate of entry into and exit from compartment.
Mammillary ModelConsists of 1 or more peripheral compartments connected to the central compartment.
Mammillary ModelMost commonly used compartment model.
One Compartment Open ModelAka Instantaneous Distribution Model
One Compartment Open ModelSimplest model
One Compartment Open ModelGenerally used to describe plasma levels following the administration of a single dose.
One Compartment Open ModelIn this model, the rate of absorption is neglected in calculations.
EliminationMetabolism and excretion
EliminationIt is a first -order process with first-order rate constant.
Elimination Rate ConstantIt represents the sum of each rate constant of metabolism and excretion.
Drug in the Body (DB)Computed via first-order process.
Apparent Volume of DistributionRepresents a volume that must be considered in estimating the amount of drug in the body from the concentration of drug found in the sampling compartment blood samples are collected at periodic intervals and the plasma portion of blood is analyzed for their drug concentrations.
Volume of DistributionDetermined by extrapolating the value of initial concentration (đ¶đ‘‚) in 𝑃 a given set of data.
Two Compartment ModelDrug appears to distribute instantaneously throughout a central compartment but more slowly and a at a single finite rate to a peripheral compartment.
Three Compartment ModelDrug is distributed most rapidly to a highly perfused central compartment, less rapidly to the second or tissue compartment, and very slowly to the third or deep tissue compartment, containing such poorly perfused tissue as bone and fat.
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Section 3

Question Answer
DistributionTransfer of the drug from the plasma to the interstitium.
DistributionMechanism of drug removal from the blood.
MetabolismIrreversible transformation of parent compounds into daughter metabolites.
MetabolismMajor organ: LIVER
MetabolismMajor substructure: hepatic microsomes in the smooth endoplasmic reticulum
Hepatic MicrosomesMajor substructure of Smooth ER for metabolism
First Pass Effect“Presystemic Metabolism”
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Section 4

Question Answer
Phase I Reaction“Functionalization”
Phase I ReactionConvert lipophilic molecules into more polar molecules
Phase I ReactionIntroducing or unmasking polar functional groups (-OH or -NH2)
Phase I ReactionCan be excreted by the kidneys
Phase I ReactionFrequently catalyzed by cytochrome P450
Oxidation Addition of oxygen and/or removal of hydrogen
OxidationMostly occurs in endoplasmic reticulum
ReductionAddition of hydrogen and/or removal of oxygen
HydrolysisAddition of water with the breakdown of the molecule
Phase II Reactions“Conjugation”
Phase II ReactionsConjugation reactions with endogenous substrates that result to polar, more water-soluble compounds.
Phase II ReactionsOccur when the metabolites from phase I are too lipophilic to be retained in the kidney tubules.
GlucuronidationMain phase II (conjugation) reaction
GlucuronidationOccurs in the liver with bilirubin and thyroxine.
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Section 5

Question Answer
PharmacogeneticsStudy of the effects in that genetic differences have on the metabolism of certain drugs.
ExcretionIrreversible transfer of drug from the blood to the urine or other excretory compartments.
KidneyMajor organ site of excretion.
NephronFunctional unit in excretion
Filtration- “Glomerulus” - Low MW molecules
FiltrationIt is measured by the renal clearance of inulin
Normal Glomerular Filtration Rate (GFR)100-130 mL/min
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Section 6

Question Answer
Secretion“Proximal Tubule”
SecretionActive secretion of some weak electrolyte especially weak acids and reabsorption of water.
Secretion- Requires a carrier and energy supply - Reabsorption (Distal Tubule)
SecretionPassive excretion and reabsorption of lipid soluble drugs.
BioavailabilityMeasurement of both the rate of drug absorption and total amount of drug that reaches the general circulation from an administered dose.
Bioavailability Factor (F)Fraction of administered dose that was absorbed.
Bioavailability Factor (F)- Unitless - For IV route: F = 1-For First Pass Effect: F<1
Equivalent Dose- It is used when different dosage forms and/or strengths are used. - Used for pharmaceutical alternatives.
Amount of Drug Absorbed from a Salt or Ester FormWhen a salt or ester of a drug is administered, F is multiplied by the fraction of the total molecular weight which the active drug represents (S).
Amount of Drug Absorbed from a Salt or Ester FormFor parent drug: S = 1
Cumulative Urinary Drug Excretion CurveMeasurement of the concentration of the intact drug and its metabolite in the urine.
Area Under the Curve (AUC)Amount of drug absorbed systemically.
Area Under the Curve (AUC)Simple numeric estimation of the extent of absorption of a drug from a product.
Area Under the Curve (AUC)For calculating the relative efficiency of different drug products.
Area Under the Curve (AUC)K = zero or first order constant
Absolute Bioavailability (Fabs)Comparison of the test drug to 100% absorption (IV)
Relative Bioavailability (Frel)Comparison of the test drug to reference standard.
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Section 7

Question Answer
GENERIC DRUG- Same active ingredients and the same labelled strength - Same dosage form, same administration, same packaging - Bioequivalent with the innovator drug
GENERIC DRUG- Essentially the same labelling as the innovator drug - Full documentation of the drug's chemistry, manufacturing steps, and quality control measures
GENERIC DRUG- Raw materials and finished product meet standard specifications - Remain potent and unchanged until the expiration date - Comply with GMP regulations
PHARMACEUTICAL EQUIVALENTS- Same active ingredient(s) - Same dosage form and route of administration - They are identical in strength or concentration
PHARMACEUTICAL ALTERNATIVESSame therapeutic moiety, but are different salts, esters, or complexes of that moiety, or are different dosage forms or strengths.
THERAPEUTIC EQUIVALENTSPharmaceutical equivalents that have the same clinical effect and safety profile when administered to patients.
THERAPEUTIC ALTERNATIVESDifferent drug but safe clinical effect.
BIOAVAILABILITY AND BIOEQUIVALENCEEvaluate the clinical efficacy of different dosage forms or products made by different manufacturers.
BIOPHARMACEUTICS CLASSIFICATION SYSTEM (BCS)Provides a of oral immediate release (IR) drug products by classifying drug compounds based on their SOLUBILITY related to dose and INTESTINAL PERMEABILITY in combination with the dissolution properties of the dosage form.
BIOPHARMACEUTICS DRUG DISPOSITION CLASSIFICATION SYSTEM (BDDCS)Modified version of bcs
BIOPHARMACEUTICS DRUG DISPOSITION CLASSIFICATION SYSTEM (BDDCS) Useful in predicting overall drug disposition, including routes of drug elimination and the effects of efflux and absorptive transporters on oral drug absorption; when transporter-enzyme interplay will yield clinically significant effects (e.g., low bioavailability and drug-drug interactions); the direction, mechanism, and importance of food effects; and transporter effects on post absorption systemic drug concentrations following oral and intravenous dosing.
BIOPHARMACEUTICS DRUG DISPOSITION CLASSIFICATION SYSTEM (BDDCS)Well supported by experimental data on the effect of transporter inhibition and induction on drug metabolism
BIOPHARMACEUTICS DRUG DISPOSITION CLASSIFICATION SYSTEM (BDDCS)Uses elimination criteria, may expand the number of class 1 drugs eligible for a waiver of in vivo bioequivalence studies and provide predictability of drug disposition profiles for classes 2, 3, and 4 compounds.
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Section 8

Question Answer
HIGHLY SOLUBLEHighest strength is soluble < 250 ml water over a pH range of 1 to 7.5.
HIGHLY PERMEABLEExtent of absorption > 90% of an administered dose in humans, based on mass balance or in comparison to an intravenous reference dose.
RAPIDLY DISSOLVING> 85% of the labelled amount of drug substance dissolves within 30 minutes using USP apparatus I or II in a volume of < 900 ml buffer solutions.
CLASS I DRUGSExhibit a HIGH absorption number and a HIGH dissolution number.
RATE-LIMITING STEP is drug dissolution.
CLASS II DRUGSHave a HIGH absorption number but a LOW dissolution number.
IN VIVO DRUG DISSOLUTION:is the rate limiting step for absorption except at a very high dose number.
Absorption for class II drugsusually SLOWER than class I and occurs over a LONGER PERIOD of time systems developed for class II drugs
Permeability rate limiting step for drug absorption.
CLASS III DRUGSPermeability
CLASS III DRUGSExhibit a HIGH variation in the RATE and extent of DRUG ABSORPTION.
CLASS III DRUGSRequire technologies that address fundamental limitations of absolute or regional permeability.
CLASS IV DRUGSExhibit a lot of PROBLEMS for effective oral administration.
CLASS IV DRUGSRoute Of Choice: Parenteral with the aid of solubility enhancers.
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Section 9

Question Answer
CLASS IV DRUGSTaxol
CLASS III DRUGSProteins
CLASS III DRUGSPeptides
CLASS III DRUGSCaptopril
CLASS III DRUGSNeomycinB
CLASS III DRUGSAcyclovir
CLASS III DRUGSCimetidine
CLASS I DRUGSPropranolol
CLASS I DRUGSVerapamil
CLASS I DRUGSDiltiazem
CLASS I DRUGSMetoprolol
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Section 10

Question Answer
Vascular systemplasma substitutes and drugs bound to plasma protein
Body watersome low MW water soluble compounds
One or more tissues that may or may not be the site of actionhighly lipid soluble compounds that distribute into fat tissue
Combinationdetermined by membrane permeability and lipid/water solubility highest concentrations in the kidney, liver, and intestine
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