Lecture 1 Part 1

Question 1

pharmacology is the science that…

Answer 1

pharmacology is the science that deals with the ACTION and USE of drugs

Question 2

learning pharmacology is among the most important steps in becoming a ____, ____, or _____

Answer 2

physician, pharmacist, or biomedical researcher

Question 3

rather than simply ordering a medication to treat a symptom or disease, modern therapeutics requires an understanding of……

Answer 3

the underlying MECHANISM OF ACTION of a pharmacologic agent, how it is influenced and influences the disease, and its capacity to cause beneficial/harmful clinical effects

Question 4

pharmacology is uniquely positioned among the ___ and ___ sciences

Answer 4

biomedical and pharmaceutical

Question 5

pharmacology depends on and contributes to……

Answer 5

genetics
biochemistry
cell biology
organ physiology
clinical medicine

Question 6

modern pharmacology is divided into what 5 branches

Answer 6

biochemical pharmacology
molecular pharmacology
immunological pharmacology
genetic pharmacology
clinical pharmacology

Question 7

the development of ____ and ____ pharmacology helps us to understand the MOA from system to organ to molecular level

Answer 7

biochemical and molecular

Question 8

define pharmacology

Answer 8

the study of substances that interact with living systems through chemical processes, esp through binding to regulatory molecules and activating/inhibiting normal body processes

Question 9

“pharmacology is the study of SUBSTANCES that interact with living systems through chemical processes, esp through………

what are these “SUBSTANCES”

Answer 9

-chemicals given to achieve a benficial/therapeutic effect

-chemicals that have TOXIC effects on regulatory processes in parasites that have infected the patient

Question 10

define medical pharmacology

Answer 10

the science of substances used to PREVENT, DIAGNOSE, AND TREAT diseases

this is what physicians study

Question 11

“basic principles in therapeutics”

Answer 11

clinical pharmacology

designed to illustrate a consistent approach to qualitative and quantitative decision making in therapeutics

used in clinical trials

Question 12

define toxicology

Answer 12

the branch of pharmacology that deals with the undesirable effects of chemicals on living systems (from individual cells to complex ecosystems)

Question 13

define pharmacodynamics

Answer 13

the study of the biochemical and physiological effects of drugs (ON THE BODY)

Question 14

define pharmacokinetics

Answer 14

the study of ADME of drugs or disposition of drugs in the body

EFFECT OF THE BODY ON THE DRUG

Question 15

define pharmacotherapeutics

Answer 15

the use of drugs to prevent and treat disease

Question 16

_________ knew the beneficial or toxic effects of many plant and animal materials

give 2 examples of this

Answer 16

prehistoric people

rhubarb was used as a cathartic (purgative - laxative) - beneficial (INDIA)

arsenate was used for cancer treatment in China (harmful)

Question 17

in the last 2500 years, the predominant schools of thought did not rely on…..

Answer 17

experimentation and observation, but rather on untested notions (like that disease is caused by excess blood/bile)

this was a lack of experimental medicine, and therefore many treatments were unhelpful and even worse than no treatment at all

Question 18

in which century did medicine begin to rely on observation and experimentation?
these principles were first established by….

Answer 18

around the end of the 17th century

principles first established by the physical sciences

Question 19

around the end of the 17th century, physicians in _____ and elsewhere in Europe began to apply….

this began what is termed as……..

Answer 19

Great Britain

began to apply the methods of observation and experimentation to study the effects of traditional drugs used in their practices

materia medica – the science of drug preparation and the medical use of drugs.

Question 20

what is the precursor of modern pharmacology

Answer 20

materia medica

Question 21

during the era of the start of materia medica, was the mechanism of action of drugs being understood?
why or why not

Answer 21

NO

this was prevented bc there were no methods for purifying active agents from the crude materials, AND there were no methods for testing hypotheses about the nature of drug actions

Question 22

in the late 18th and early 19th centuries, who developed methods of experimental animal physiology and pharmacology

Answer 22

Francois Magendie and Clause Bernard

Question 23

what laid the groundwork for learning how drugs work at the organ and tissue levels?
what century was this?

Answer 23

late 18th early 19th

developments in chemistry and physiology

Question 24

Paradoxically, real advances in basic pharmacology in the 19th centru were accompanies by…..

Answer 24

an outburst of nonscientific patent medicines

Question 25

about ____ years ago, there was a major expansion of research efforts. new concepts and techniques have enabled new discoveries concerning the mechanism of action, and PHYSIOLOGICAL SUBSTRATES AND RECEPTORS

Answer 25

50 years ago

Question 26

true or false the molecular mechanisms of action of many drugs have now been identified and many receptors have been isolated and structurally characterized and cloned

Answer 26

TRUE

Question 27

The public (that consumes medication) is still exposed to inaccurate, incomplete, or unscientific information regarding the pharmacological effects of chemicals. what has this lead to

Answer 27

a huge growth in the "alternative healthcare" industry

Question 28

we want a _____- therapeutic window for a drug. what does this mean

Answer 28

large therapeutic window this means there is a lot of space between the effective dose and lethal dose. this means the drug is safer

Question 29

explain when the significance of the kidney secretary became clear

Answer 29

during WW2 when penicillin was discovered penicillin was in short supply and was also rapidly excreted -- big problem. scientists discovered probenecid (a benzoic acid derivative) was used to prevent the rapid loss of penicillin in the urine by enhancing its reabsorption into the bloodstream probenecid is no longer used bc large scale production and semi-synthetic congeners are now available

Question 30

name the 2 general principles that students should always remember

Answer 30

-all substances under certain circumstances can be toxic -all therapy that is promoted as "health enhancing" should meet the same standards for evidence of safety and efficacy ie -- there should be no separation between scientific medicine and alternative (complementary) medicine

Question 31

any substance that ________________ is a drug

Answer 31

brings about a chemical change in biologic function

Question 32

true or false in all cases, a drug molecule interacts with a specific molecule in the biologic system that plays a regulatory role (receptor)

Answer 32

FALSE -- most cases there are some exceptions -- one of which is that antagonists may interact directly with other drugs and not a receptor

Question 33

true or false drugs cannot be synthesized within the body

Answer 33

FALSE -- they can (hormones)

Question 34

true or false drugs may be chemicals NOT made by the body

Answer 34

TRUE --- xenobiotics

Question 35

in order to chemically interact with its receptor, a drug must have the appropriate (4 things---)

Answer 35

size electrical charge shape atomic composition

Question 36

can drugs be poisons? define poisons

Answer 36

yes a substance that through its chemical action kills, injures, or impairs an organism

Question 37

how are toxins usually defined?

Answer 37

as poisons of biological origin synthesized by plants or animals OR inorganic poisons such as cyanide, lead, arsenic

Question 38

true or false a drug is often administered at a location DISTANT from its intended site of action

Answer 38

TRUE -- pill given orally to relieve headache

Question 39

as mentioned, a drug is often administered at a location distant from its intended site of action. therefore....

Answer 39

a drug must have the necessary properties to be transported from its site of administration to site of action

Question 40

what property must a drug have to ensure that its actions will only be of an appropriate duration?

Answer 40

should be inactivated or excreted from the body at a reasonable rate

Question 41

true or false only the liver has capacity for metabolism

Answer 41

FALSE every cell/tissue has to capacity for metabolism, but the liver is the main

Question 42

after a drug has been absorbed, where is the drug?

Answer 42

in the plasma

Question 43

from the plasma (after absorption), where can the drug go?

Answer 43

Drug can reversibly leave the bloodstream and be distributed into intracellular fluids and be metabolized by liver kidney or other tissues

Question 44

3 ways that drugs can be excreted

Answer 44

urine feces bile

Question 45

true or false at room temp, drugs may be solids liquids or gases

Answer 45

TRUE solid - aspirin liquid - nicotine, ethanol gas - nitrous oxide

Question 46

what influences the best route of administration? give an example

Answer 46

the physical nature of the drug at room temp (solid, liquid, gas) liquid drugs are easily vaporized and can be inhaled as gas form (ie: halothane)

Question 47

p.r

Answer 47

rectal

Question 48

s.c

Answer 48

subcutaneous

Question 49

the vast majority of drug have a molecular weight of _____? why??

Answer 49

between 100-1000 at least 100 is needed to acheive selective binding to its receptor -- drug must be sufficiently unique in shape, charge, etc to prevent binding to other receptors

Question 50

true or false the molecular size of drugs varies from very small to very large

Answer 50

TRUE lithium MW = 7 alteplase = 59,050

Question 51

how is the upper limit of MW determined?

Answer 51

primarily by the requirement that drugs be able to move within the body (from the site of administration to the site of action)

Question 52

VERY LARGE DRUGS must be administered how and why

Answer 52

directly to the compartment where they have their effect bc they may have issues moving throughout the body to reach the site of action from site of administration

Question 53

very large drugs are usually ________

Answer 53

proteins

Question 54

what is alteplase and how is it administered

Answer 54

a very large MW clot-dissolving enzyme it is administered directly into the vascular compartment by IV infucion

Question 55

drugs interact with receptors by means of.......

Answer 55

chemical forces/bonds (3 types) covalent (strongest) electrostatic hydrophobiv

Question 56

true or false covalent bonds are very strong and in most cases not reversible under biologic conditions

Answer 56

TRUE

Question 57

give 2 examples of drugs that use covalent bond forces and explain their mechanism

Answer 57

activated form of phenoxybenzamine covalently binds to the alpha receptor for norepinephrine -- results in the receptor being blocked. this effect lasts long after the free drug has disappeared from the bloodstream and is reversed ONLY by the synthesis of new alpha receptors (~48 hrs) DNA alkylating agents used in chemo -- disrupts chemical division in neoplastic tissue

Question 58

phenoxybenzamine is used to treat what kind of condition?

Answer 58

if there is a tumor on the adrenal gland more epinephrine will be produced. this causes vasoconstricition and high blood pressure. phenoxybenzamine helps this condition bc it binds to the alpha receptor for norepinephrine and thus blocks its production

Question 59

_________ is much more common than covalent bonding in drug-receptor interactions

Answer 59

electrostatic bonds

Question 60

are electrostatic bonds strong or weak? explain

Answer 60

they can be relatively strong in the case of permanently charged ionic molecules to wear hydrogen bonds OR these weaker H bonds can have a very weak dipole induced interaction such as Van der Waals forces

Question 61

true or false hydrophobic bonds are usually quite weak

Answer 61

true

Question 62

hydrophobic bonds are important for which drugs

Answer 62

highly lipid soluble drugs woth the lipids of cell membranes and perhaps in the interaction of drugs with the internal walls of receptor pockets

Question 63

which bonds are usually more selective: -drugs which bind through WEAK bonds to their receptors -drugs which bind through very strong bonds to their receptors

Answer 63

weak bonds are usually more selective this is bc a weak bond requires a very precise fit if an interaction is to occur -- only a few receptor types are likely to provide such a precise fit

Question 64

"attraction between opposite charges"

Answer 64

electrostatic forces

Question 65

"fluctuation in electron clouds around molecules oppositely polarize neighboring atoms"

Answer 65

van der waals forces

Question 66

"hydrophobic groups interact with each other to exclude water molecules"

Answer 66

hydrophobic forces

Question 67

"hydrogen shared between electronegative atoms"

Answer 67

hydrogen bonds

Question 68

more than _____ of all useful drugs in biology are chiral molecules that exist as enantiomeric pairs

Answer 68

MORE THAN HALF

Question 69

drugs with 2 asymmetric centers have how many diastereomers? give an example

Answer 69

4 diastereomers labetalol -- an alpha and beta receptor blocking drug

Question 70

chiral refers to a molecule with....

Answer 70

a center of 3D asymmetry

Question 71

define stereoisomers

Answer 71

compounds that have the same MF but differ in arrangement of atoms in space

Question 72

"mirror images"

Answer 72

enantiomers

Question 73

"chiral"

Answer 73

4 different groups attached

Question 74

true or false chemical identity is associated with true enantiomers

Answer 74

TRUE (only have 1 asymmetric center) if there's more than 1 - it's a diasteromer and does NOT have the same physical chemical properties

Question 75

R,R and S,S

Answer 75

enantiomers

Question 76

S,R and R,S

Answer 76

diasteriomers

Question 77

explain the significance of enantiomers and drug metabolism

Answer 77

1 drug enantiomer is often more susceptible than the other to drug-metabolizing enzymes (bc they're usually stereospecific) therefore, the duration of 1 enantiomer may be quite different from the other

Question 78

most studies of clinical efficacy and drug elimination have been carried out with...... as a result......

Answer 78

RACEMIC MIXTURES many pts are receiving drug doses in which 50% or more is either inactive or actively toxic

Question 79

skipped slides 29-31

Answer 79

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