1.1

Question 1

What is PK? Acronym?

Answer 1

how the body works on the medication:

ADME- absorption, distribution, metabolism, and elimination

Question 2

What is PD?

Answer 2

how the drug is acting upon the body

Question 3

What are the enteral routes?

Answer 3

Oral, SL, Buccal, Feeding tube

Question 4

What are the Topical routes?

Answer 4

PR, transdermal, creams

Question 5

What are the parenteral routes?

Answer 5

IV, IM, SC

Question 6

What are the 2 modes of absorption?

Answer 6

Paracellular

Transcellular

Question 7

What is paracellular absorption?

Answer 7

drug or active ingredient is absorbed between cells, goes between the gap between cells, drug in ECF

Question 8

What is transcellular absorption?

Answer 8

rug must cross through cell, passive, active txp, or endocytosis

Question 9

What is Vd? What is the formula?

Answer 9

How much volume is the drug being distributed into.

Vd = (Amount of drug in body)/ (conc. Of drug in blood or plasma)

Question 10

What does it mean for a drug to have high Vd? Examples?

Answer 10

much higher conc. in Extravascular tissue or drug extensively distribute into body tissues and fluids
i.e. Digoxin, diltiazem, imipramine, labetalol, metoprolol, meperidine, and nortriptyline

high Vd, then the drug is dissipated through body more effectively (think about the math…) may take longer to eliminate, the drug stays mostly in extravascular tissue (outside of bloodstream, eg bone, fat, liver)

Question 11

What does it mean for a drug to have a low Vd?

Answer 11

Drugs have low Vd – retained mostly within the vasculature (Intravascular) or limited drug distribution
i.e. aminoglycosides

Question 12

What is the AUC? Why is this useful?

Answer 12

area under the curve-AUC, which tells us how much drug exposure a pt has had in a given timeframe. ALSO, allows us to predict behavior of the drug, eg the level of the drug, without lab draw, and titrate to a therapeutic effect.

Question 13

In a 2 compartment model, what are the 2 compartments?

Answer 13

Central- Heart, liver, lungs, kidneys, blood

Peripheral- Fat, muscle, CSF

Question 14

What is the MEC?

Answer 14

Minimum effective concentration

Question 15

What is the first pass loss? How is this corrected for?

Answer 15

First pass loss (i.e. First pass effect): The loss of a drug before getting to site of action when it first pass through the GI and liver.
Drugs that have extensive first pass loss require much larger oral than IV doses to achieve the same effects

Question 16

What are the 4 common biochemical ways drugs are metabolized?

Answer 16

Oxidation
Reduction
Hydrolysis
Conjugation

Question 17

What three types of conjugation occur in drug metabolism?

Answer 17

“GAS”
Glucuronidation: Adding glucuronic acid to the molecule
Acetylation: Adding an acetyl group to another molecule
Sulfation: Adding a sulfate to another molecule

Question 18

What happens in phase 1 of drug metabolism?

Answer 18

Oxidation, Reduction, and Hydrolysis

Generally result in loss of pharmacological activity

Question 19

What happens in phase 2 of drug metabolism?

Answer 19

Conjugation

Covalent link functional group with endogenous glucuronic acid, sulfate, glutathione, AA, or acetate

Question 20

What is a prodrug?

Answer 20

inactive compounds designed to max the amount of active species at site of action
Metabolized into active form

Question 21

How are prodrugs activated?

Answer 21

hydrolysis of an ester or amide linkage

Question 22

What do acidic drugs bind to?

Answer 22

albumin

Question 23

What do basic drugs bind to?

Answer 23

Alpa-acid glycoprotein

Question 24

What do thyroid hormone, estrogen, and tester one bind to?

Answer 24

Thyroid- thyroxin binding globulin
Estrogen- sex-binding globulin
Testosterone- sex-binding globulin

Question 25

When is protein binding clinically relevant?

Answer 25

high clearance with narrow therapeutic index drugs

= adding a little can up the amount in the blood a lot!