Pharm Exam 2

Front 1

Total Body Water & Example of small water soluble molecule

Back 1

0.6L/Kg

e.g Ethanol

Front 2

Extracellular Water & Example of large water soluble Molecule

Back 2

0.2L/Kg

e.g Gentamicin

Front 3

Blood & Plasma & Example of Strong plasma protein bound large molecule

Back 3

Blood 0.08L/Kg
Plasma 0.04L/Kg

e.g Heparin - always kept in blood

Front 4

Fat volume & Example of highly lipid-soluble Molecule

Back 4

0.2-0.35L/Kg

e.g DDT

Front 5

Bone Volume & Example

Back 5

0.07L/Kg

e.g ions - Lead, Flouride

Front 6

Chloroquine

Back 6

Drug with very high Vd - 13,000

Front 7

3 Formulas for CL

Back 7

= Rate of Elimination / C

= Vd x Kel - Rate of elimination Constant

= Vd x 0.7 / T1/2

Front 8

Two most important sites for Drug Elimination

Back 8

Kidney & Liver

Front 9

High Extraction Drugs

Back 9

Drugs that follow flow dependent elimination and are eliminated on the first pass of drug through the organ

Front 10

Hepatic Cycling and Endogenous substances that use this path

Back 10

Drug is Glucuronidated in Liver, secreted into bile as Glucuronide into GI tract & hydrolyzed back to original drug which is reused

e.g Folic Acid, Bile Acids, Vitamin D3 & B12, Estrogens

Front 11

Accumulation Factor

Back 11

1/Fraction Lost in one dosing

Front 12

Extraction Ratio

Back 12

CL/Q

Front 13

Q

Back 13

Q = Hepatic Blood Flow = 90L/hr in a 70Kg person

Front 14

Bioavailability Equation

Back 14

F = f x (1-ER)

Front 15

Major Plasma proteins responsible for Drug Binding

Back 15

Albumin
alpha1-acidic glycoprotein

Front 16

Alpha1 - acidic glycoprotein

Back 16

Plasma protein that increases concentration following surgery, myocardial infarction, & chronic pain & Rheumatoid Arthritis

Front 17

PK factors that change with age

Back 17

Everything is reduced except total body fat

Front 18

Maintenance Dose

Back 18

A steady state where the dosing rate = rate of elimination

Dosing Rate ss = CL x Tc

Front 19

Loading Dose Formula

Back 19

LD = Tc x Vd/F

Front 20

Corrected Dose Formula

Back 20

Corrected Dose = Average Dose x Pt creatine clearance/100ml/min

Front 21

Ideal Body Weight

Back 21

Male 52 + 1.9/inch height over 5ft

Female 52 + 1.7/inch height over 5ft

Front 22

Phase I characteristics

Exception & Example

Back 22

Usually converts parent drug to a more polar substance by adding on or unmasking a functional group

Levodopa is prodrug converted into dopamine by phase I reaction in the brain by Dopa Decarboxylase

Front 23

Phase II compounds that Covalently link to parent drug

Back 23

Glutathione
Acetate
Amino Acids
Sulfate
Glucuronate

Front 24

Glucuronide metabolite exception

Back 24

Morphine is more potent analgesic after phase II glucuronidation

Front 25

Hepatic Recirculation & 3 Examples

Back 25

High molecular Weight conjugates may get their bonds cleaved by intestinal flora and become reabsorbed for circulation

Morphine, Tetracyclines, CPT-11

Front 26

Where Biotransformations Occur

Back 26

Liver
Kidney
GI tract
Lung
Skin

Front 27

Two Important Microsomal Enzymes

Back 27

NADPH Cytochrome P450 Reductase

Cytocrome P450

Front 28

3 Drugs of Glucuronidation

Back 28

Morphine
Acetaminophin
Digoxin

Front 29

Drug of Acetylization

Back 29

Isoniazid

Front 30

Drug of Glutathione Conjugation

Back 30

Ethacrynic Acid

Front 31

Drug of Glycine Conjugation

Back 31

Nicotinic Acid

Front 32

2 Drugs of Sulfate Conjugation

Back 32

Estrone
Acetaminophen

Front 33

3 Drugs of Methylation

Back 33

Dopamine
Epinephrine
Histamine

Front 34

Microsomal enzymes catalyze what types of reactions? Non-Microsomal?

Back 34

Microsomal - Glucuronidate

Non-Microsomal - everything else

Front 35

Scoline

Back 35

The only depolarizing muscular relaxant used in clinics because it doesn't have cardiorespiratory depressant effects

Front 36

N-acetylcysteine

Back 36

Precursor of GSH to form Ac-SG (Mercapturate) which is excreted harmlessly

antidote for Acetaminophen OD

Front 37

Where are drug metabolizing enzymes located?

Back 37

Found in Lipophilic hepatic smooth ER membranes

Front 38

How many cytochrome P450 in mammals? How many have meaning in humans?

Back 38

1000

50

Front 39

Primary containers of CYP450

Back 39

Hepatocyte & small Intestine Enterocyte smooth ERs

Front 40

Major Isoforms of CYP450

Back 40

1A2
2A6
2C9
2D6
2E1
3A4

Front 41

Chronic Ethanol use induces which enzyme?

Back 41

CYP2E1

Front 42

Grapefruit Juice inhibits which enzyme?

Back 42

CYP3A4

Front 43

Caucasians are poor metabolizers of what?

Asians?

Back 43

CYP2D6

CYP2C19

Front 44

Where is Albumin Synthesized?

Back 44

Synthesized in Liver

Front 45

What type of drug binds easily to Alpha 1-acidic glycoprotein?

Back 45

Basic Molecules bind easily because it is acidic

Front 46

What are Aminoglycosides?

Back 46

Antibiotics

Front 47

Teratogenesis & Examples

Back 47

Induction of developmental defects in fetus

Thalidomide, Ethanol, Warfarin

Front 48

Mutagenesis & How to find these drugs

Back 48

Induction of changes in genetic material of animals of any age & make it heritable

Ames test - use special samonella in medium to see if there is loss of dependence on the nutrients

Front 49

Carcinogenesis & 2 examples

Back 49

Induction of malignant characteristic in cells

Vinyl Chloride & Aflatoxin

Front 50

2 Drug examples of capacity limited elimination

Back 50

Ethanol
Phenytoin

Front 51

How Warfarin Works

Back 51

inhibits Vit K Epoxidase in liver & half life of clotting factor is 14hr so it takes a while to get theraputic effect

Front 52

2 drugs extensively bound to Albumin

Back 52

Phenytoin & Slicyclates

Front 53

3 Alpha 1 - acidic Glycoprotein binding drugs

Back 53

Propranolol
lidocain
Quinidine

Front 54

How does Atropine Affect stomach motion?

Back 54

Slows it down