Introduction

Question 1

Do drugs modify or confer new functions?

Answer 1

Modify

Question 2

What are pharmacodynamics?

Answer 2

what the drug does to the body

Question 3

What are pharmacokinetics?

Answer 3

What the body does to the drug

Question 4

What is a specialized target that binds a drug or endogenous ligand and mediates the pharmacologic action?

Answer 4

drug receptor

Question 5

What is it called when a drug is bound to the receptor and as a result has binding that leads to the biological response?

Answer 5

drug-receptor complex

Question 6

Why are there a large variety of receptors and channels at the membrane?

Answer 6

Because most drugs are lipid soluble

Question 7

What is the compound that binds to the receptor and mimics the response of the endogenous ligand?

Answer 7

agonist

Question 8

What is the compound that blocks or reverses the affect of agonists and have no effect on their own?

Answer 8

antagonist

Question 9

The ____ _____ is not as effective because it occupies all receptors but doesn’t activate the ligand binding site, opens ion channels differently or incompletely, and can act as antagonist if given with full antagonist

Answer 9

partial agonist

Question 10

What is a competitive antagonist?

Answer 10

Compete for the same site on the receptor that the agonist wants (increasing dose can overcome this)

Question 11

What are noncompetitive antagonists?

Answer 11

Bind to different site to reduce maximal response that an agonist can produce, not overcome by increased potency

Question 12

What is an inverse agonist?

Answer 12

Opposite effect than agonist :)

Question 13

What is the maximal response a drug can produce?

Answer 13

Efficacy

Question 14

What is the measure of dose required to produce a response?

Answer 14

Potency

Question 15

Lethal dose 50 / effective dose 50

Answer 15

Therapeutic index

Question 16

What is it called when two drugs with opposite effects are given together?

Answer 16

Functional antagonism

Question 17

What is it called when an antagonist is administered with an agonist?

Answer 17

Competitive antagonism

Question 18

What is a diminished response to the same drug over time?

Answer 18

Tolerance

Question 19

What are different ways of tolerance?

Answer 19

receptor desensitization, down-regulation (less receptor synthesis)

Question 20

What is tachyphylaxis?

Answer 20

body quickly develops reduced response to drug, requiring higher doses

Question 21

What is an enhanced response to a drug?

Answer 21

Hyperactivity

Question 22

What is the enhancement of one drug by another which has no effect on its own?

Answer 22

Potentiation

Question 23

What is the production of a greater response by two drugs when given together than each individually?

Answer 23

synergism

Question 24

What are some adverse effects of drugs?

Answer 24

Overextension, organ-directed toxicities, fetal toxicities

Question 25

What is the amount of the drug absorbed after oral administration compared with after IV?

Answer 25

bioavailability

Question 26

AUCoral/AUCiv=f

Answer 26

bioavailability

Question 27

Does a smaller or bigger molecule absorb faster?

Answer 27

smaller

Question 28

Does a smaller or bigger particle absorb faster?

Answer 28

smaller particle

Question 29

Does a drug dissolve faster in aqueous or oily solutions?

Answer 29

aqueous

Question 30

Can ionized or unionized drugs cross membrane?

Answer 30

unionized

Question 31

Does lower or larger surface area absorb faster?

Answer 31

larger

Question 32

Less or more blood flow for absorption?

Answer 32

More

Question 33

What is it called when oral drugs are metabolized by the liver before reaching systemic circulation?

Answer 33

first pass effect

Question 34

What are the inactive drugs metabolized by the liver to make an active form?

Answer 34

prodrugs

Question 35

What is albumin's role in drug distribution?

Answer 35

Binds to drug like other plasma proteins, sequesters drugs in blood, slows transfer, prolongs their duration of action

Question 36

What happens when drugs bind to tissue proteins?

Answer 36

accumulate in certain tissues which makes it stay in the body for weeks after stopped

Question 37

What is the process of converting a drug into another chemical called a metabolite?

Answer 37

drug metabolism, mostly by the liver!

Question 38

What are the minor metabolizing organs?

Answer 38

GI tract, lungs, kidneys, skin

Question 39

How does drug metabolism work?

Answer 39

by making the molecule more water soluble to enhance removal

Question 40

What phase involves introducing a polar functional group to up renal elimination?

Answer 40

Phase I with the cytochrome P-450 enzymes

Question 41

What enzyme metabolizes over 50% of the medications?

Answer 41

CYP3A4

Question 42

What phase involves conjugating to make it more polar to up renal elimination?

Answer 42

phase II

Question 43

What's the most common form of drug deactivation?

Answer 43

active drug to inactive metabolite

Question 44

What is the kidney's role in drug elimination?

Answer 44

excrete most drugs and metabolites into urine, depends on renal function involving: glomerular filtration, proximal tubular secretion, distal tubular reabsorption

Question 45

What is enterohepatic recycling?

Answer 45

drugs secreted into the bile --> reabsorption in small intestine --> systemic circulation or back to bile (prolonged amount of time the drug is in the body)

Question 46

dose (mg)/plasma concentration (mg/mL)

Answer 46

volume of distribution (assuming it is evenly distributed throughout the body with no metabolism or elimination)

Question 47

what is the rate at which a drug is cleared from the body?

Answer 47

Clearance

Question 48

Rate of drug (mg/min)/plasma concentration (mg/mL)

Answer 48

clearance

Question 49

What order kinetics is the elimination rate of the drug is concentration dependent?

Answer 49

PERCENTAGE -- first order (exponential)

Question 50

What is the fraction of a substance that is removed per unit time measured?

Answer 50

elimination rate constant

Question 51

What is the time it takes for half blood level concentration of a drug?

Answer 51

half life

Question 52

What is the steady state concentration?

Answer 52

5 half lives (3-4 to start to feel the effect)

Question 53

What is a loading dose?

Answer 53

large dose used to raise plasma concentration to a therapeutic level more quickly

Question 54

What is the kinetics of a constant AMOUNT of drug is lost per unit time?

Answer 54

zero-order kinetics (LINEAR)

Question 55

What is a maintenance dose?

Answer 55

alternations should be made in either the dose or dosing interval according to renal or hepatic diseases

Question 56

When is maintenance dose adjustment necessary?

Answer 56

Only when hepatic disease alters clearance

Question 57

What is the hepatic extraction ratio?

Answer 57

fraction of drug removed during one pass through the liver

Question 58

Are high extraction ratio drugs or low extraction ratio drugs more affected by liver disease?

Answer 58

high extraction ratio drugs

Question 59

What is a series of alleles found in a linked locus on the chromosome?

Answer 59

haplotype

Question 60

What is the inherited variation in the DNA sequence?

Answer 60

polymorphism

Question 61

What enzyme metabolizes up to 1/4 of all drugs including beta blockers, opioids, antipsychotics?

Answer 61

CYP2D6

Question 62

What enzyme has a preference for acidic drugs, like PPI, antidepressants, antiplatelets, with polymorphism more prevalent in Asian populations?

Answer 62

CYP2C19

Question 63

What enzyme metabolizes polymorphism of east asian and oceania populations disproportionally?

Answer 63

CYP2B6

Question 64

What are the two Phase II enzymes?

Answer 64

UGT1A1 and TMPT, with clinical significance in cancer and immuno treatments

Question 65

What is the enzyme that is in the PPP, most prevalent in African/Mediterranean populations in deficiency?

Answer 65

G6PD

Question 66

What genetic component determines if sustained virologic response of anti-viral medication is likely (european populations)?

Answer 66

IFNL3

Question 67

What polymorphisms have increased sensitivity to Warfarin and are higher incidence in Asian populations?

Answer 67

CYP2C9 reduces clearance and VKORC1 decreased expression

Question 68

What drug can HIV patients with HLA-B*5701 + not take or else risk of serious/fatal hypersensitivity reactions?

Answer 68

Abacavir (ziagen)

Question 69

What drug can patients of Asian descent and + HLA-B*1502 allele not take or risk serious/fatal dermatologic reactions to use for bipolar disorder including Stevens-Johnson syndrome?

Answer 69

carbamazepine (tegretol)

Question 70

What drug for HIV patients do they need to test + for CCR5 to use it?

Answer 70

Maraviroc (selzentry)

Question 71

What drug for gout and patients of Chinese or Thai or Korean with renal impairment need to test + of HLA-B*5801 to avoid serious dermatologic reactions and DRESS syndrome?

Answer 71

allopurinol (aloprim)

Question 72

What drug needs the CYP2C19 genotype tested due to allele differences?

Answer 72

clopidogrel (plavix) 2 or 3 alleles are mostly non functional and have cardiovascular issues

Question 73

What drug needs to be tested of the CYP2D6 allele due to exaggerated responses from fast metabolization?

Answer 73

codeine

Question 74

What drug needs to have tested both CYP2C9 and VKORC1 genotypes?

Answer 74

Warfarin 2nd or 3rd alleles need lower starting dose due to increased risk of bleeding (decreased metabolism)

Question 75

What are compounds likely to be therapeutically useful?

Answer 75

lead compounds

Question 76

What is a chemical modification of a known active molecule?

Answer 76

analogue

Question 77

What did the Pure Food and Drug Act (1906) do?

Answer 77

protected from mislabeled or adulterated drugs

Question 78

What is important to know about the FDA?

Answer 78

made in 1906, pre-market safety approval in 1938, increased in 1962

Question 79

What phase is animal studies, undergoing pre-clinical safety and toxicity?

Answer 79

pre-clinical

Question 80

What is the phase of first testing in humans (healthy volunteers)?

Answer 80

phase 1

Question 81

What is the phase of drug studied in patients with target disease?

Answer 81

phase 2

Question 82

What is the phase that lasts 2-10 years and is a much bigger group?

Answer 82

phase 3

Question 83

What is the phase that is when it's approved?

Answer 83

phase 4

Question 84

What is bioequivalence?

Answer 84

A way to fast track approval for a drug with an absence of significant difference

Question 85

What drug should not be prescribed if a Chinese or Thai or Korean ancestry patient tests **positive** for HLA-B*5801?

Answer 85

allopurinol

Question 86

What gene should you test Chinese or Thai or Korean patients with renal impairment/prescription of allopurinol?

Answer 86

*5801 + is a no

Question 87

What enzyme do you need to test for clopidogrel?

Answer 87

CYP2C19...1st allele is fully functional, the others have > cardio events

Question 88

What gene should you test for codiene?

Answer 88

CYP2D6... 2nd allele has exagerrated response (scary!)

Question 89

What genes do you need to test for Warfarin (coumadin)?

Answer 89

CYP2C9 and VKORC1 2nd or 3rd allele or G>A variant in VKORC1 need to use LOWER STARTING DOSE or increased risk of bleeding

Question 90

What is the gene you need to test whether there is sustained virologic response of anti-viral medication (hypersensitivity...prevalent in European populations)

Answer 90

IFNL3

Question 91

What gene do you need to test to prescribe Abacavir (Ziagen)?

Answer 91

HLA-B*5701 ... **cannot be prescribed if positive, could be fatal**

Question 92

What gene do you need to test in order to prescribe carbamazepine (tegretol) in patients of Asian descent and make sure they are NOT POSITIVE?

Answer 92

HLA-B*1502, **if positive do not prescribe, could be fatal**

Question 93

What gene do you need to test for before prescribing Maraviroc (Selzentry)?

Answer 93

CCR5, **must be positive to take it**