Basic Principles

Question 1

Any substance that brings about a change in biologic function

Answer 1

Drug

Question 2

Actions of a drug on the body

Answer 2

Pharmacodynamics

Question 3

Actions of the body on the drug

Answer 3

Pharmacokinetics

Question 4

Movement of drug molecules into and within biologic environments

Answer 4

Permeation

Question 5

Most important limiting factor for permeation

Answer 5

Lipid diffusion

Question 6

Aqueous solubility is __________ proportional to electrostatic charge

Answer 6

Directly

Question 7

Lipid solubility is __________ proportional to electrostatic charge

Answer 7

Inversely

Question 8

In weak acids, ___________ form is more water soluble an undergoes better clearance

Answer 8

Unprotonated

Question 9

In weak bases, ___________ form is more water soluble an undergoes better clearance

Answer 9

Protonated

Question 10

Excretion of a weak acid may be accelerated by alkalinizing the urine with _________

Answer 10

Bicarbonate

Question 11

Excretion of a base acid may be accelerated by acidifying the urine with _________

Answer 11

Ammonium chloride

Question 12

Transfer of a drug from its site of administration to the bloodstream

Answer 12

Absorption

Question 13

Most common route of drug administration

Answer 13

Oral route

Question 14

Slowest route of drug administration

Answer 14

Topical

Question 15

Undergoes significant first pass effect

Answer 15

Oral route

Question 16

Partially bypass the first pass effect

Answer 16

Rectal

Question 17

Distribution depends on 4 factors

Answer 17

Size of the organ
Blood flow
Solubility
Binding

Question 18

Drugs may undergo 3 metabolic fates

Answer 18

Termination of drug action
Drug activation
Elimination without metabolism

Question 19

Termination of drug action

Answer 19

Elimination

Question 20

Release of drugs or their metabolites in the urine, stool, bile

Answer 20

Excretion

Question 21

Rate of elimination is proportionate to the concentration

Answer 21

First order elimination

Question 22

Rate of elimination is constant regardless of concentration

Answer 22

Zero order elimination

Question 23

What drugs display zero order kinetics?

Answer 23

WHAT PET
Warfarin
Heparin
Aspirin
Tolbutamide
Phenytoin
Ethanol
Theophylline

Question 24

Translate the drug-receptor interaction into a change in cellular activity

Answer 24

Effectors

Question 25

Response of a particular receptor-effector system measured against increasing drug concentrations

Answer 25

Dose response curve

Question 26

Denotes the amount of drug needed to produce a given effect

Answer 26

Potency

Question 27

Responsiveness diminishes rapidly after administration of a drug

Answer 27

Tachyphylaxis

Question 28

What drugs display tachyphylaxis?

Answer 28

``` MED Loves CNN in HD Metoclopramide Ephedrine Dobutamine LSD Calcitonin Nitroglycerin Nicotine Hydralazine Desmopressin ```

Question 29

Continuous activation may lead to depletion of essential substrates

Answer 29

Tolerance

Question 30

Relates the rate of elimination to the plasma concentration

Answer 30

Clearance

Question 31

Condition in which the average total amount of drug in the body does not change over multiple dosing intervals. Rate of drug input is equal to the rate of elimination.

Answer 31

Steady state

Question 32

Fraction of the administered dose that reaches the systemic circulation

Answer 32

Bioavailability

Question 33

Results in the achievement of therapeutic levels of the drug in the blood without exceeding the minimum toxic concentration

Answer 33

Dosage regimen

Question 34

Safe range between the minimum therapeutic concentration and the minimum toxic concentration of a drug

Answer 34

Therapeutic window

Question 35

Phase I reactions

Answer 35

``` HORDe Hydrolysis Oxidation Reduction Deamination ```

Question 36

Arrange according to decreasing order of strength: Electrostatic bonds Hydrophobic bonds Covalent bonds

Answer 36

Covalent bonds Electrostatic bonds (ionic bonds, hydrogen bonds, van der Waals) Hydrophobic bonds

Question 37

Fick's Law of Diffusion

Answer 37

(Difference in concentration x permeability coefficient x area)/thickness

Question 38

(Volume of distribution x desired plasma concentration)/Bioavailability

Answer 38

Loading dose

Question 39

(Clearance x desired plasma concentration)/Bioavailability

Answer 39

Maintenance dose

Question 40

Standard in vitro test for mutagenicity

Answer 40

Ames test

Question 41

Phase of clinical trial that deals with the careful evaluation of dose-response relationship and pharmacokinetics among normal human volunteers

Answer 41

Phase 1 trial

Question 42

Phase of clinical trial that deals with evaluation of drug in a moderate number of patients with target disease

Answer 42

Phase 2 trial

Question 43

Phase of clinical trial that explore further the spectrum of beneficial actions of the new drug, compare it to standard of treatment and discover toxicities

Answer 43

Phase 3 trial

Question 44

Postmarketing surveillance phase

Answer 44

Phase 4 trial

Question 45

Cytochrome P450 inducers

Answer 45

``` Ethanol Barbiturates Phenytoin Phenobarbital Rifampicin Griseofulvin Carbamazepine St. John's Wort Smoking ```

Question 46

Cytochrome P450 inhibitors

Answer 46

``` Isoniazid Sulfonamides Valproic acid Venlafaxine Cimetidine Ketoconazole Erythromycin Grapefruit juice Ritonavir Amiodarone ```