Kaplan Chapter 1

Question 1

Name some popular weak acid drugs to remember?

Answer 1

1. aspirin
2. loops
3. thiazides
4. warfarin
5. pens
6. many “ate” drugs like valproate

Question 2

Name some popular drugs that are considered weak bases?

Answer 2

Many of the easily abused drugs
1. local anesthetics (cocaine)
2. amphetamines (methamphetamine)
3. PCP
4. morphine
5. narcotics (ex: codeine)

Question 3

What is the indication for warfarin usually?

Answer 3

anti-coagulant

Question 4

What are some factors that make a drug safer for pregnancy?

Answer 4

1. large
2. water soluble
3. highly protein bound

Question 5

What is the calculation for Volume of distribution?

Answer 5

Vd = (amount of drug injected)/(blood concentration extrapolated at t = 0)

Vd= dose/C₀

Question 6

When is Vd low?

Answer 6

when bound to plasma protein

Question 7

When is Vd high?

Answer 7

When sequestered in tissue

Question 8

Give typical plasma volume?

Answer 8

3L

Question 9

Give typical blood V?

Answer 9

5L

Question 10

Give typical extracellular fluid volume?

Answer 10

ECF = 12-14 L

Question 11

Give typical TBW volume?

Answer 11

40-42 L

Question 12

Give common CYP inducers and pneumonic to remember 3 of them.

Answer 12

rifampin
St. John’s Wort
carbamazepine
phenytoin

St. John Rifin in the Car

or Chronic Smoker and Chronic Drinking in Barbs Car Ruins Passengers Seats

Chronic smoking
chronic drinking
Barbituates
Carbamazepines
Rifampin (antibiotic)
Phenytoin
St. Johns Wort

Question 13

Give the most common CYP 450 inhibitors and best pneumonic to remember them.

Answer 13

ketoconazole
amiodarone
cimetidine
macrolides (especially erythromycin)
grapefruit juice
omeprazole

Ami’s COKE and Grapefruit juice

or AA CCOKE and Grapefruit Juice w/ Pie

acute alcohol
Amiodarone
Cimetidine
Chloramphenicol/ciprofloxacin as well
Omeprazole
Ketoconazole (azoles/ antimicrobials)
Erythromycin (macrolide/antimicrobials)
Grapefruit Juice
Protease Inhibitor: Ritonavir, indinavir etc.

Question 14

Give the 3 macrolides azithromycin, erythromycin, and clarithromycin in order of least to greatest P450 inhibitor effect?

Answer 14

Remember alphabetical order.
1. azithromycin
2. clarithromycin
3. erythromycin

Question 15

Suffix to remember macrolides?

Answer 15

“thromycin”

Question 16

Name substances that can acidify urine?

Answer 16

NH4Cl (ammonium chloride), Vit. C, cranberry juice

Question 17

Name substances that can alkalinize urine?

Answer 17

NaHCO3, acetazolamide

Question 18

What are some drugs that at high doses exhibit zero order kinetics?

Answer 18

Zero PEAs

phenytoin
ethanol
salicylate acid (aspirin)

Zero WATT Power

W = warfarin
A = alcohol and aspirin
T = tolbutamide
T = theophylline
P = Phenytoin

Question 19

Formula for volume of distribution.

Answer 19

V_d =dose/C⁰

C₀ = conc. at time 0

Question 20

Formula for half-life.

Answer 20

t_1/2 = 0.7 x (V_d / Cl)

Question 21

Loading dose formula?

Answer 21

LD = (V_d x C_p)/f

Cp; concentration in plasma

Question 22

Maintenance dose formula?

Answer 22

MD = Cl x C^ss x † /f

t (tau): dosing interval

Question 23

Infusion rate formula?

Answer 23

k₀ = Cl x C^ss

Question 24

Most common class CYPP450 drugs are metabolized?

Answer 24

3A4

Question 25

Phase I Metabolism examples?

Answer 25

cytochrome P450, MAO, alcohol metabolism

Question 26

What usually takes place in Phase I metabolism?

Answer 26

drug goes through either oxidation, reduction, or hydrolysis rxns

Question 27

What usually takes place in Phase II Metabolism?

Answer 27

conjugation

Question 28

What are examples of Phase II Metabolism?

Answer 28

glucuronidation, acetylation, glutathione

Question 29

Drugs that cause drug induced SLE because of genetic variability in acetylation of the body? (slow acetylators)?

Answer 29

hydralazine procainamide isoniazid (INH) SHIPP sulfasalazine hydralazine isoniazid (INH) procainamide penicillamine

Question 30

What drug can induce glucuronyl transferase to distinguish Crigler-Najjar Type 1 and Crigler-Najjar Type 2

Answer 30

barbituates (ex: phenobarbital)

Question 31

What enzyme is needed to cause Phase II metabolism?

Answer 31

transferases

Question 32

What is phase 1 biotransformation?

Answer 32

modification of drug molecule via oxidation, reduction, or hydorlysis

Question 33

Describe the process of microsomal metabolism.

Answer 33

Usually done by oxidation reactions Major enzyme systems are involved CYP450 which are localized in SER of cells mostly in liver but can also be found in GI tract, lungs, and kidney.

Question 34

Examples of non microsomal metabolism in Phase I biotransformation?

Answer 34

hydrolysis, MAO, alcohol metabolism

Question 35

Describe hydrolysis in non microsomal metabolism?

Answer 35

phase I reaction involving addition of water molecule with subsequent bond breakage and includes esterases (pseudocholinesterase) and amidases

Question 36

Glucuronidation requires what major enzyme for conjugation?

Answer 36

glucuronyltransferase