Pharm 1.1-5 Basic Principles Of Pharmacology I-5

Front 1

Drug Action

Back 1

Molecular action - invisible

Front 2

Drug effect

Back 2

pharmacologic effect- visible response

Front 3

pharmacokinetics

Back 3

time course of absorption, action, and elimination

Front 4

pharmacodynamics

Back 4

physiochemical or receptor interactions

Front 5

reversible receptor bonds

Back 5

ionic, Van der waals, Hydrogen

Front 6

irreversible receptor bonds

Back 6

covalent

Front 7

EC50 (definition) (tells you what about the agonist?)

Back 7

effective concentration for 50% response

Hint 7

relates to affinity of agonist for receptor

Front 8

graded response graph (for drug effects)

Back 8

linear format

Front 9

dose-response graph (for drug effects)

Back 9

logarithmic

Front 10

threshold of dose-response graphs (definition) (gives you what info about the agonist?)

Back 10

dose of agonist at which response begins

Hint 10

relates the affinity of agonist for the receptor

Front 11

Effect = (of certain dose of drug)

Back 11

E(max) [D] ---------------- K(D) + [D]

Hint 11

K(D) = EC50

Front 12

intrinsic activity (definition) (influences?)

Back 12

ability to stimulate a receptor once bound

Hint 12

efficacy and potency

Front 13

E(max) (definition) (what % of receptor occupancy needed?)

Back 13

maximum response

Hint 13

not all receptors need to be occupied

Front 14

More efficacious agonists need ______ receptors occupied than less efficacious agonist to achieve the same effect.

Back 14

less

Front 15

Less efficacious agonists need ______ receptors occupied than more efficacious agonist to achieve the same effect.

Back 15

more

Front 16

secondary receptors

Back 16

outside target tissue - mediate side-effects

Front 17

strongest agonist has ______ intrinsic activity

Back 17

strongest

Front 18

These agonists differ by their _____ but not in _____
(how can you tell?)

Back 18

binding, activating the receptor

Hint 18

different EC50's but same E(max)

Front 19

three agonists with the same?

Back 19

intrinsic activity

Front 20

two agonists with different?
(but the same?)

Back 20

intrinsic activity

Hint 20

receptor binding affinity (K(D) is the same)

Front 21

Efficacy
(depends on the?)

Back 21

the ability of the drug to activate the effector portion of the receptor once bound

Hint 21

structure of the drug

Front 22

Potency
(depends on?)

Back 22

relates to the amount of drug that is needed for an effect

Hint 22

3)Biologic System (receptor density, efficiency of stimulus-response mech)
2)Interaction with the Receptor (affinity, efficacy)

Front 23

double-headed arrows represent differences in?

Back 23

A- relative potency (amount of drug needed)

Hint 23

B- relative efficacy (maximum effect)

Front 24

adding of a competative antagonist to a dose of agonist inc/dec the ____ of the Log Dose-response curve of the agonist?

Back 24

increases

Hint 24

K(D) or EC50

Front 25

what type of antagonism?

Back 25

non-competitive

Front 26

(T/F) Non-competitive inhibitors inactivate the effector

Back 26

(T)

Front 27

(T/F) Noncompetitive antagonists interfere with agonist binding.

Back 27

(T)

Front 28

(T/F) Competitive antagonists interfere with agonist binding.

Back 28

(F)

Front 29

(T/F) Competitive inhibitors inactivate the effector.

Back 29

(F)

Front 30

characteristics of Simple Diffusion

Back 30

Lipid Soluble, small, nonionized

Front 31

Characteristics of Facilitated Diffusion

Back 31

selective, can be saturated

Front 32

Characteristics of Filtration

Back 32

driven by hydrostatic pressure, transported through pores or channels between cells, size limiting

Front 33

Amount of:
Intracellular Fluid
Interstitial Fluid
Plasma

Back 33

28L
9L
3L

Front 34

What characteristics do drug molecules have that can pass through the capillary membrane?

Back 34

small molecule, lipid-(in)soluble

Front 35

weak acids ____ a proton

Back 35

give up

Front 36

weak bases ___ a proton

Back 36

accept

Front 37

Henderson-Hasselbach Equation

Back 37

pH= pKa + log A-/HA

Front 38

which is greatly absorbed in the stomach, weak acids or weak bases?

Back 38

weak acids

Front 39

Two fluid compartments, 1: pH=7.4, 2: pH=1.4. Which direction will equilibrium shift for a weak acid?

Back 39

Toward compartment 1.

Front 40

Two fluid compartments, 1: pH=7.4, 2: pH=1.4. Which direction will equilibrium shift for a weak base?

Back 40

Toward compartment 2

Front 41

What is trapped in the stomach, weak acids or weak bases?

Back 41

weak bases

Front 42

Enteral drug administration.

Back 42

GI tract

Front 43

Parenteral Drug Administration.

Back 43

any route of administration not through the GI tract.

Front 44

Which is less painful and more rapid in reference to absorption, S.C. or intramuscular injections?

Back 44

intramuscular

Front 45

label routes of administration. Between which two is inhalation?

Back 45

A-IV
B-IM
C-SC
D-PO
and between A and B

Front 46

Bioavailability
(definition)
(equation)

Back 46

fraction of dose available for biologic action

Hint 46

AUC (oral)
--------------- X100
AUC (iv)

Front 47

Equation to predict plasma concentration of drug- IV
(pill)

Back 47

Cp = Dose/Vd
(Vd = volume of distribution)

Hint 47

Cp = (F x Dose)/Vd
(F = fraction absorbed)

Front 48

Volume of Distribution
(equation)
(values)

Back 48

Vd = Dose / Plasma Concentration

(D/Cp)

Hint 48

40L - sml molec. & lipid-soluble
12L- lipid-soluble
3L- protein bound

Front 49

Why might the Volume of Distribution of a drug appear to be more than 40?

Back 49

Tissue Binding or plasma protein binding

Front 50

what are the two components of volume distribution of a drug?

Back 50

a = drug distribution
b = drug elimination

Front 51

Factors affecting distribution of a drug:

Back 51

Blood flow
Ability to enter fluid space (pH, binding, transport, solubility...)
Time after administration
Redistribution
Size of Pt

Front 52

label initial compartments of drug distribution

Back 52

Top- Plasma
Dashed- Brain
Dotted- Muscle
lowest- fat

Front 53

What do you do with an overdose of a weak acid drug for CNS toxicity? (aspirin/barbiturates)

Back 53

increase plasma pH (with NaHCO3)

Front 54

What do you do with an overdose of a weak base drug for CNS toxicity?

Back 54

decrease pH (with HCl)

Front 55

What can cause a smaller apparent Vd for a drug?

Back 55

reporting of total measured drug in the plasma with drug plasma protein binding

Front 56

loading dose

Back 56

needing to fill the storage sites of a drug before enough free drug is available to interact with its target tissue... where are these storage sites?

Hint 56

short term- protein binding
long term- lipid or bone

Front 57

why is it dangerous to give both antibiotics and anticoagulants?

Back 57

drug displacement- the antibiotic will displace some of anticoag attached to plasma proteins, releasing more free drug

Front 58

Purpose of Biotransformations

Back 58

to clear a drug from the plasma

Front 59

Basics of preparing a drug for excretion

Back 59

make it larger, charged, and more water soluble

Front 60

What are the reactions that compose the first two Phases of biotransformation?

Back 60

Phase 1: oxidation, reduction, hydrolysis

Hint 60

Phase 2: conjugation

Front 61

term used to describe an increase in metabolism of the primary drug or other drugs in the Liver?

what is the consequence of this?

Back 61

induction

Hint 61

you may need to increase the dose of the drug to achieve the desired effect

Front 62

term used to describe when a pt on antibiotics and cardiac drugs experiences an overdose of the cardiac drugs due to the antibiotics blocking the metabolism of the cardiac drugs

Back 62

inhibition

Front 63

(T/F) The hepatic microsomal drug metabolizing system performs both Phase 1 and Phase II processes

Back 63

True

Front 64

(T/F) The non-microsomal systems perform both Phase 1 and Phase II processes.

examples of non-microsomal systems?

Back 64

False- usually phase I (acetyl cholinesterase, alcohol dehydrogenase)

plasma, red cells

Front 65

What is the most common Phase 1 reaction for the biotransformation of drugs?

Back 65

drug oxidation

Front 66

What is the most common Phase 1 reaction for the biotransformation of drugs?

Back 66

drug oxidation

Front 67

Locations (organ and cellular specific) of oxidation of drugs

Back 67

plasma, red cells, other tissues

ER, cytoplasm, mitochondria

Front 68

6 components of hepatic mixed function oxidase system

Back 68

1) NADPH
2) cytochrome P450 reductase (flavoprotein)
3) cytochrome P450 (hemoproteins)
4) Mg++
5) phospholipid
6) O2

Front 69

In the hepatic mixed oxidase system does the drug bind to Ferrous or Ferric iron-P450?

Back 69

Ferric +++ iron

Front 70

Tylenol Overdoses deplete the body of NADPH. How does this effect the drug metabolism in the liver?

Back 70

greatly reduces it. without NADPH cytochrome P-450 reductase oxidized flavoprotein can not be recycled to its reduced state, thus durg-P450-Fe+++ can not be reduced

Front 71

(T/F) 1-2% of caucasians but 5-10% of SE asians have poor metabolic activity

Back 71

False- %'s are reversed. The 4 types of phenotypes of metabolic activity are: poor, intermediate, extensive, and untrarapid

Front 72

cellular areas where drug reductions take place in the liver

Back 72

1) microsomes
2) cytoplasm
3) mitochondria

Front 73

(T/F) Phase 1 of drug biotransformation does not inactivate the drug

Back 73

False- products of Phase 1 have variable activities, some active, some inactive

Front 74

Location of Phase II biosynthetic reactions

Back 74

Liver

Front 75

The resulting molecule of a Phase II biotransformation reaction is:

Back 75

larger, charged, water soluble, and inactive

Front 76

What type of energy source is used for the Phase II conjugation reaction of glucaronide to a drug?

Back 76

UTP

Front 77

Which of the following are components of Phase I and which are Phase II biotransformation reactions?

1) acetyl Co-A
2) H20
3) Fe-+++
4) S-adenosylmethionine
5) cytochrome P-450
6) UTP
7) Flavoprotein
8) H
9) Glucuronide

Back 77

1) acetyl Co-A: Phase II
2) H20: Phase I (hydrolysis)
3) Fe-+++: Phase I (oxidation)
4) S-adenosylmethionine (Phase II)
5) cytochrome P-450: Phase I (oxidation)
6) UTP: Phase II
7) Flavoprotein: Phase I (oxidation)
8) H: Phase I (reduction)
9) Glucuronide: Phase II

Front 78

equation for enzyme reaction with a drug

Back 78

Vmax [D]
V=--------------
Km + [D]

Front 79

What order of kinetics occurs at low drug concentrations? (when [D],,Km)

Back 79

First Order

Front 80

What order of kinetics occurs when there is a large concentration of drug? ([D]>>Km)

Back 80

Zero Order

Front 81

Explain the enzyme/durg concentration relationship for zero order kinetics.

Back 81

the enzyme is at its max efficiency

Front 82

Explain the enzyme/durg concentration relationship for First order kinetics.

Back 82

enzyme is proportionately responsive to the concentration of drug

Front 83

(T/F) The hepatic microsomal drug metabolizing system experiences both induction and inhibition.

Back 83

True

Front 84

(T/F) The non-microsomal systems experience both induction and inhibition.

Back 84

False- they only experience inhibition

Front 85

what does saturation of the transport systems in the kidney due to the order of the kinetics of renal clearance?

Back 85

changes First order to Zero order (max rate)

Front 86

In manipulating the pH of urine (pH partitioning) to enhance the renal excretion of a drug, is the urine made to be more acidic or more alkaline than the plasma?

Is the plasma more acidic or alkaline than the brain?

Back 86

urine is more alkaline than the plasma (pH=8)

plasma is more alkaline than the brain (pH=7.5)

Brain pH=7.4

Front 87

What compound is used to alkalinize the urine?

1) Sodium Sulfate
2) Sodium Bicarbonate
3) Phenobarbital

Back 87

Sodium Bicarbonate

Front 88

What is the role of activated charcoal in overdoses that do not involve the ingestion of the drug?

Back 88

To stop the enterohepatic cycling that will keep the drug from being eliminated in bile.

Front 89

equation for Clearance

Back 89

Clearance Total =

C(metabolic) + C(renal)

Front 90

clearance rate of inulin =

Back 90

filtration rate

Front 91

clearance rate of glucose =

Back 91

zero

Front 92

clearance of PAH =

Back 92

active transport + filtration (~650ml/min)