James Cology

Front 1

Determines the duration of action of Drug.

Back 1

Biotransformation

Front 2

Main Organ of biotransformation

Back 2

Liver

Front 3

Important for orally administered drugs to be metabolized.

Back 3

Gi tract, Upper Intestine

Front 4

Participates in entero-hepatic cycling of glucoronides.

Back 4

Liver and upper intestine

Front 5

Important site for basic drugs and inhaled drugs

Back 5

Lungs

Front 6

Biotransforms dermally applied drugs

Back 6

Skin

Front 7

Helps eliminate some drugs in urine

Back 7

Kidney

Front 8

May be important for CNS active drugs

Back 8

Brain

Front 9

Age and gentic make up effect on metabolism

Back 9

Internal ( intrinsic)

Front 10

How Nutrition, Food, Disease state, other drugs effect metabolism.

Back 10

External ( environmental )

Front 11

Discovered with debrisoquine, metabolizes many N-containing drugs, 1-15 % are poor metabolizers, low doses given to those who are lacking this enzyme.

Back 11

CYP2D6

Front 12

First shown with mephenytoin, Oriental poor metabolizers have less of this enzyme.

Back 12

CYP2C19

Front 13

Low rates of conjugation of bilirubin are because lack of this enzyme.

Back 13

UGT-1 family

Front 14

Newborns have low levels of this enzyme.

Back 14

UGT

Front 15

Metabolism decreases when this number increases.

Back 15

Age ( as you get older metabolism decreases.)

Front 16

First recognized polymorphism, affects the metabolism of drugs like isoniazid.

Back 16

NAT-2

Front 17

Asian and natives have a low incidence of this.

Back 17

Slow acetylators

Front 18

Swedish have 70% and US has 50 % of this.

Back 18

Slow acetylators

Front 19

Omeprazole induces this enzyme

Back 19

CYP1A2

Front 20

Phenobarbital and Carbamezpine induce this enzyme

Back 20

CYP2 and 3

Front 21

Isoniazid induces this enzyme

Back 21

CYP2E1

Front 22

What you do with hot tea or coffee

Back 22

CYP slowly

Front 23

Rifampicin induces this enzyme

Back 23

CYP3A4 and 5

Front 24

Clofibrate induces this enzyme

Back 24

CYP4

Front 25

UGT and GST are induced by this drug

Back 25

Phenobarbital and othe barbiturates

Front 26

Oltipraz can induce this enzyme

Back 26

GST

Front 27

CYP1A2 can be induced by these

Back 27

Tobacco, Charbroiled foods

Front 28

CYP1 and 2 can be induced by these

Back 28

PCBs and DDT

Front 29

Alcohol can induce this CYP

Back 29

2E1

Front 30

St. Johns wart is an inducer of this enzyme

Back 30

CYP3A4

Front 31

Bioflavaniods and garlic and onion are weak inducers of these enzymes

Back 31

CYP, GST

Front 32

Perservatives can induce these enzymes

Back 32

GST and UGT

Front 33

Green tea and black tea can induce 3 enzymes name them

Back 33

CYP, UGT, GST

Front 34

Can down regulate CYP2 and 3 family members during viral infections

Back 34

Interferons or cytokines

Front 35

This liver disease leads to lowered levels of enzymes

Back 35

Cirrhosis

Front 36

Most variable of all CYP enzymes

Back 36

2D6

Front 37

Least variable of the CYP enzymes

Back 37

2E1 and 3A4/5

Front 38

Present in higher concentration than PAPS

Back 38

UDP- glucoronic acid

Front 39

These are usually present in high concentrations

Back 39

GSH and NADPH and NADH

Front 40

GSH level decrease when this decreases

Back 40

Nutrition

Front 41

Malnutrion of aa can lead to this

Back 41

Reduced aa conjugation

Front 42

Ethanol consumptions lowers this

Back 42

NADPH

Front 43

Indinavir and saquinavir are both substrates for this enzyme

Back 43

CYP3A4

Front 44

Inhibits CYP3A4 by binding to it

Back 44

Erythromycin metabolites

Front 45

Ketoconazole and other imiidizole containing drugs inhibit this enzyme

Back 45

CYP

Front 46

The products in Grapefuit that inhibit CYP3A4

Back 46

Furnocoumarins and flavanoids

Front 47

This is when a receptor binding causes a biological activity

Back 47

Intrinsic activity (alpha factor)

Front 48

GABA-A is this type of channel

Back 48

Cl- gated

Front 49

All glutamate receptor types

Back 49

Cation channels

Front 50

Inhibits Calcium channels

Back 50

Go

Front 51

Activates potassium channels

Back 51

Gi

Front 52

Activates Calcium channels

Back 52

Gs

Front 53

Gq activates this

Back 53

PLC

Front 54

PLC makes

Back 54

IP3 and DAG

Front 55

Gq uses this for of energy to activate this

Back 55

GDP becomes GTP to activate PLC

Front 56

IP3 frees this cation

Back 56

Calcium

Front 57

Calcium activates this

Back 57

Protein Kinases

Front 58

DAG activates this

Back 58

PKC

Front 59

Activates AC to increase cAMP

Back 59

Gs

Front 60

Does the opposite of Gs

Back 60

Gi

Front 61

Gs uses this ase energy form to activate AC

Back 61

GTP

Front 62

cAMP is inactivated by this (Viagra)

Back 62

Phosphodiesterases

Front 63

PKA is activated by cAMP when this energy form is used

Back 63

ATP

Front 64

Is activated by Gi to make PG

Back 64

PLA2

Front 65

When proteins are modified by this they do things

Back 65

Phosphorylation

Front 66

Decreases the chance of an AP, and is located on the dendrites or cell bodies.

Back 66

Impulse modulating autoreceptors

Front 67

Autoreceptor located on presynaptic terminals and inhibits NT syn

Back 67

Synthesis modulating autoreceptor

Front 68

Autoreceptor located on presynaptic terminals inhibits NT release

Back 68

Release modulating autoreceptors

Front 69

What the body does to the drugs (ADME)

Back 69

Pharmacokinetic

Front 70

What the body does to the drug (DDC)

Back 70

Pharmacodynamics

Front 71

Means Poison or Drug

Back 71

Pharmakon

Front 72

Drugs for different folks

Back 72

Pharmacogenomics

Front 73

Adverse effects of chemical compounds. Includes environmental exposure.

Back 73

Toxicology

Front 74

This act required that safety testing and labels be accurate and complete

Back 74

1938: Federal Food, Drug and Cosmetic Act

Front 75

Amendment responsible for the "Caution: Federal law prohibits dispensing without prescription" on Rx bottles

Back 75

1951: Durham-Humphrey

Front 76

Kefhauver-Harris Amendment: Required testing for both safety and effectiveness for new drugs and ones between1938 and _____

Back 76

1962

Front 77

Drugs come from different sources this is the main source

Back 77

Plant or Animals

Front 78

Most drugs are used to

Back 78

Treat symptoms

Front 79

13000

Back 79

RX drugs available

Front 80

2-3 weeks

Back 80

New drug approved

Front 81

Most of the times people see doctors they get this

Back 81

RX

Front 82

Old people take this

Back 82

25% of RX

Front 83

Ptenet life for a drug in US

Back 83

20 years

Front 84

To do clinical trials you submit this to fda

Back 84

IND

Front 85

When you submit NDA to FDA it takes this long for them to approve

Back 85

20-24 months

Front 86

CAST looked at

Back 86

PVC-premature ventricular contractions

Front 87

Rezulin taken of market because

Back 87

Heart and Liver failures

Front 88

Vioxx pulled of market for this

Back 88

Increased risk of MI or Heart problems

Front 89

Not approved for use by FDA

Back 89

Combo of Phen-Fen

Front 90

Full agonist
Alpha = ?

Back 90

alpha = 1

Front 91

Partial agonist
Alpha = ?

Back 91

0 < alpha < 1

Front 92

Antagonist
Alpha = ?

Back 92

alpha = 0

Front 93

Full agonist elicits?

Back 93

Emax at Bmax

Front 94

Partial agonist never elicits?

Back 94

Emax

Front 95

Noncompetitive shifts?

Back 95

Emax downward
NO effect on EC50 or slope

Front 96

Competitive shifts?

Back 96

EC50 to the right
NO effect on Emax or slope

Front 97

Inverse agonist
Alpha = ?

Back 97

-1 < alpha < 0

Front 98

Inverse agonist can resemble?

Back 98

Antagonist

Front 99

Bmax =?

Back 99

Max number of binding sites in tissue sample

Front 100

Bmax found when?

Back 100

Drug concentration has saturated the receptors

Front 101

Bmax measures?

Back 101

Occupancy
NOT activity

Front 102

Kd =?

Back 102

Drug concentration occupies half of Bmax

Front 103

2 things that can change Kd?

Back 103

Structural specificity
Stereoselectivity

Front 104

Hill Plot: ?

Back 104

Determines if dose response or binding curve has a normal slope

Front 105

Hill plot is a ?

Back 105

linear version of log-dose graph