M1 L4 Flashcards by CHESKA CIANNELLE FRANCISCO

Q

estimate drug dosing and predict the time course of drug efficacy for a given dose

A

MODEL

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Q

it is a mathematic description of a biologic system and is used to express quantitative relations concisely

A

MODEL

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Q

It refers to a GROUP OF TISSUES with similar blood flow and drug affinity, but is NOT a real physiologic or anatomic region

A

COMPARTMENT

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Q

CENTRAL compartment

A

BLOODSTREAM

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Q

PERIPHERAL compartment

A

TISSUES

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Q

SIGNIFICANCE OF COMPARTMENT

used to ____ a set of data obtained by experimentation

A

describe and interpret

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Q

SIGNIFICANCE OF COMPARTMENT

used to characterize with reproducibility the ____ and the ____ in biologic system when given by a ertain route of administration and in a particular dosage form

A

behavior and the fate of a drug

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Q

it is a HYPOTHESIS using mathematical terms to desccribe QUANTITATIVE relationships
uses the observed time course for drug concentrations in the body and, from these data, obtains various pharmacokinetic parameeters to predict drug dosing OUTCOMES, pharmacodynamics, and toxicity

A

PHARMACOKINETIC MODEL

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Q

it is CONSTANT parameter of property of drug that is estimated from the experimental data

A

PHARMACOKINETIC PARAMETER

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Q

MATHEMATICAL EQUATION that relates an independent variable (time) to a dependent variable (drug concentration), often through the use of parameters

A

PHARMACOKINETIC FUNCTION

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Q

PHARMACOKINETIC MODELS ARE USED TO:

predict ____, ____, and ____ levels with any dosage regimen

A

plasma, tissue, urine drug levels

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Q

PHARMACOKINETIC MODELS ARE USED TO:

calculate the ____ for each patient individually

A

optimum dosage regimen

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Q

PHARMACOKINETIC MODELS ARE USED TO:

estimate the ____ of drugs and/or metabolites

A

possible accumulation

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Q

PHARMACOKINETIC MODELS ARE USED TO:

correlate drug concentrations with ____ or ____ activity

A

pharmacologic or toxicologic

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Q

PHARMACOKINETIC MODELS ARE USED TO:

evaluate differences in the ____ of availability between formulations (bioavailability)

A

rate & extent

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Q

PHARMACOKINETIC MODELS ARE USED TO:

describe how changes in ____ affect the absorption, distribution, or elimination of the drug

A

physiology or disease

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Q

PHARMACOKINETIC MODELS ARE USED TO:

explain ____

A

drug interactions

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Q

CLASSES OF PHARMACOKINETIC MODEL

are focused on DESCRIBING THE DATA with the specification of very few assumptions about the data being analyzed
are PRACTICAL but NOT VERY USEFUL in explaining the mechanism of the actual process by which the drug is absorbed, distributed, and eliminated in the body

A

EMPERICAL MODELS

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Q

CLASSES OF PHARMACOKINETIC MODEL

EXAMPLE:
* A model used for allometric scaling, a type of prediciton of PK parameters across diverse species

description is PER species

A

EMPERICAL MODELS

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Q

CLASSES OF PHARMACOKINETIC MODEL

SPECIFY ASSUMPTIONS and attempt to incorporate known factors about the systems surrounding the data into the model, while describing the available data

A

MECHANISTIC MODELS

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Q

CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS

there is a necessity to sample tissue and monitor blood flow to the liver IN VIVO
also requires understadinf of the clinical implication of liver drug concentration, type of cell representing the liver in case of biopsy, spatial location of the liver tissue to hepatic blood vessels, liver blood perfusion, etc.

A

PHYSIOLOGICALLY BASED MODELS

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Q

CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS

PHYSIOLOGICALLY BASED MODELS:
* also known as BLOOD FLOW or PERFUSION MODELS
* are pharmacokinetic models based on known ANATOMIC and PHYSIOLOGIC DATA
* describes the data kinetically, with the consideration that blood flow is responsible for distributing drug to various parts of the body

A

PHYSIOLOGIC PHARMACOKINETIC MODEL (FLOW MODEL)

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Q

CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS

PHYSILOGICALLY BASED MODELS:
* Physiologic Pharmacokinetic Model other names

A

Blood flow
Perfusion models
Flow Model

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Q

CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS

PHYSIOLOGIC PHARMACOKINETIC MODEL:
* rate of BLOOD PERFUSION to the tissue

A

Q

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# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** PHYSIOLOGIC PHARMACOKINETIC MODEL: * the **first order rate constant** for **URINARY DRUG EXCRETION**

ke

# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** PHYSIOLOGIC PHARMACOKINETIC MODEL: * the **rate constant** for **HEPATIC elmination**

km ## Footnote Q

# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** PHYSIOLOGIC PHARMACOKINETIC MODEL: * **RAPIDLY** equilibrating tissue

RET

# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** PHYSIOLOGIC PHARMACOKINETIC MODEL: * **SLOWLY** equilibrating tissue

SET

# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** * **Catenary model** * **Mamillary** model

COMPARTMENTALLY MODELS

# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** COMPARTMENTALLY MODELS: * consists of **comparments joined to one another** like the compartments of a **TRAIN** * **continuous** compartment = continuous blood * blood **DOES NOT** flow back

CATENARY MODEL

# **CLASSES OF PHARMACOKINETIC MODEL | MECHANISTIC MODELS** COMPARTMENTALLY BASED MODELS: * **common** model * **estimate** the amount of drug in any compartment of the system **after drug is introduced into a given compartment** * it consists of **one or more compartments** around a central compartment like **SATELLITES** * blood can **GO BACK**

MAMILLARY MODEL

# **CLASSES OF PHARMACOKINETIC MODEL** * **SIMPLEST** model * assumes that the body can be described as a **single**, **uniform compartment**, and that drugs can **enter and leave** the body

ONE-COMPARTMENT OPEN MODEL

Ka

ABSORPTION rate constant

Ke

ELIMINATION rate constant

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** the drug **entering** the body (input) DISTRIBUTES (equiliberates) ____

**INSTANTLY**

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** Drug is **NOT** necessarily confined to the ____

circulatory system

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** DISTRIBUTION occurs ____

INSTANTLY

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** is ____ in a **specific area**

NOT POOLED

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** CHARACTERISTICS by INTRAVASCULAR ROUTES: * **absorption**

NO ABSORPTION

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** CHARACTERISTICS by INTRAVASCULAR ROUTES: * ____ distribution of drug between **blood stream** and **tissue**

RAPID

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** CHARACTERISTICS by INTRAVENOUS ROUTES: * **equilibrium** is ____ obtained

INSTANTLY

# **CLASSES OF PHARMACOKINETIC MODEL | ONE COMPARTMENT OPEN MODEL** CHARACTERISTICS by INTRAVENOUS ROUTE: * **Fall of drug concentration** depends on ____ and ____

excretion and metabolism

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** * governs the **rate** at which the drug concentration in the body **DECLINES OVER TIME** * **k = ke + km**

ELIMINATION RATE CONSTANT (k)

**RATE OF ELIMINATION** is a what order process

FIRST ORDER process

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** * this describes how a drub **DISTRIBUTES** in the body compared to the blood * it's a **theoretical volume** that relates the amount of drug in the body to the concentration measured in blood/plasma * can be expressed as simple volume or in terms of percent of body weight

VOLUME OF DISTRIBUTION

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** VOLUME OF DISTRIBUTION: * drug **LEAVES** blood and **SPREAD** into tissues

HIGH VD

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** VOLUME OF DISTRIBUTION: * drug mostly **STAYS** in the blood

LOW VD

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** TWO WAYS TO CALCULATE VD

Apparanet Volume of Distribution AUC (Model Independent Meethod)

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** VOLUME OF DISTRIBUTIONl: * most drugs have an **apparent VD** ____ the **body mass**

smaller than or equal to

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** VD: * drugs **moves INTO tissues** and **fat** (EV spaces)

LARGE VD

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** VD: * Drugs with **large apparent VD** are **MORE concentrated** in ____ and **LESS concentrated** ____

MORE - EV tissues LESS - intravascularly

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** * is a measure of **DRUG ELIMINATION** from the body * **Metabolism** and **Excretion**

CLEARANCE

# **OPEN ONE COMPARTMENT MODEL: IV BOLUS** * refers to the **VOLUME OF PLASMA FLUID** that is **CLEARED** of drug per unit time * **Fraction** of drug **REMOVED** per unit time

DRUG CLEARANCE

The plasma level-time curve for a drug that follows a ____ shows that the **plasma** drug concentration **declines BI-EXPONENTIALLY** as the **sum** of the **two first-order processes**

TWO COMPARTMENT OPEN MODEL

# **TWO COMPARTMENT OPEN MODEL** shows that plasma drug concentration **declines** ____ as **sum** of thw **two first-order processes**

BI-EXPONENTIALLY

# **TWO COMPARTMENT OPEN MODEL** TWO FIRST ORDER PROCESSES

Distribution Elimination

# **TWO COMPARTMENT OPEN MODEL** a drug that follows the pharmacokinetics of a **two-compartment model** ____ throughout the body but **distributes** into **two compartments** -- the **central** and **peripheral compartments**

DOES NOT EQUILIBRATE RAPIDLY

# **TWO COMPARTMENT OPEN MODEL** The drug **distributes** ____ in the **CENTRAL compartment**

RAPIDLY AND UNIFORMLY

# **TWO COMPARTMENT OPEN MODEL** the drug **equilibrates** ____ in the **tissue** or **PERIPHERAL compartment**

MORE SLOWLY

# **TWO COMPARTMENT OPEN MODEL** the **rate of drug TRANSFER** between the two compartments is assumed to ____

FIRST ORDER PROCESS

# **TWO COMPARTMENT OPEN MODEL** * **STANDARD** model * ELIMINATION is from the **CENTRAL** comparment

MODEL A

# **TWO COMPARTMENT OPEN MODEL** * ELIMINATION is from **TISSUE** compartment

MODEL B

# **TWO COMPARTMENT OPEN MODEL** * ELIMINATION is from BOTH **CENTRAL** and **TISSUE** compartments

MODEL C

# **TWO COMPARTMENT OPEN MODEL | CHARACTERISTICS** ABSORPTION

NO absorption

# **TWO COMPARTMENT OPEN MODEL | CHARACTERISTICS** distribution of drug between **blood stream & tissue**

SLOW

# **TWO COMPARTMENT OPEN MODEL | CHARACTERISTICS** EQUILIBRIUM is obtained ____ after administration

some later time

# **TWO COMPARTMENT OPEN MODEL | CHARACTERISTICS** STEEP FALL on first part of blood level curve is due to ____

DISTRIBUTION

# **TWO COMPARTMENT OPEN MODEL | CHARACTERISTICS** PHARMACOKINETIC PARAMETERS THAT CAN BE DETERMINED: * for drugs administered via **INTRAVASCULAR route**

Elimination rate constant (ke) or β and Distribution rate constant (α)

# **TWO COMPARTMENT OPEN MODEL | CHARACTERISTICS** PHARMACOKINETIC PARAMETERS THAT CAN BE DETERMINED: * for drugs administered via **EXTRAVASCULAR route**

Absorption rate constant (ka) Elimination rate constant (ke) ro β Distribution rate constant (α)

# **TWO COMPARTMENT OPEN MODEL: IV BOLUS** * also known as **FEATHERING** or **PEELING** * A useful procedure for **fitting a curve** to the experimental data of a drug when the drug does not clearly follow a one-compartment model

METHODS OF RESIDUAL

# **TWO COMPARTMENT OPEN MODEL: IV BOLUS** METHODS OF RESIDUAL is also known as

FEATHERING or PEELING

# **TWO COMPARTMENT OPEN MODEL: IV BOLUS** what PAPER should be used

SEMI-LOG PAPER | or plot logC

# **TWO COMPARTMENT OPEN MODEL: IV BOLUS** it has a ____ behavior

BIPHASIC

# **TWO COMPARTMENT OPEN MODEL: IV BOLUS** the **plasma concentration-time curve** will NOT be a ____ for two-compatment models

NOT STRAIGHT LINE

# **TWO COMPARTMENT OPEN MODEL: IV BOLUS** how to identify the **Terminal (Elimination) phase**

select the last 3-4 data points when the curve becomes linear

as compared to **IV bolus injection**, this allows **PRECISE CONTROL** of **plasma drug concentrations** to fit the individual needs of the patient

IV INFUSION

# **ONE-COMPARTMENT OPEN MODEL: IV INFUSION** maintains an **effective constant plasma concentration** of drugs with ____ by e**liminating fluctuations** between the peak anf trough

narrow therapeutic index

# **ONE-COMPARTMENT OPEN MODEL: IV INFUSION** the **UPHILL CURVE** represents the **constant amount** of the drug that **enters SLOWLY** into the body until sucj time that a ____ is obtained

STEADY STATE CONC.

# **ONE-COMPARTMENT OPEN MODEL: IV INFUSION** the **RATE OF INPUT** is said to follow a ____ since the drug is **delivered CONSTANTLY** at a specific time

ZERO ORDER PATTERN

# **ONE-COMPARTMENT OPEN MODEL: IV INFUSION** the **ELIMINATION RATE** depends on the **concentration of the drug available in the bodt**, thus is said to follow ____

FIRST ORDER

# **ONE-COMPARTMENT OPEN MODEL: IV INFUSION** * the **rate** of drug **LEAVING** the body is **EQUAL** to the rate of drug **ENTERING** the body

STEADY STATE PLASMA CONC. (Css)

used to obtain concentrations as **rapidly as possible** since the steady state plasma concentration is NOT attained in a relatively short period of time

LOADING DOSE or INITIAL DOSE