Introduction

Question 1

Mechanism of action

Answer 1

Pharmacodynamics

Question 3

Type of passive diffusion for large molecules

Answer 3

Aqueous diffusion

Question 4

Type of passive diffusion that is the most important limiting factor for drug permeation

Answer 4

Lipid diffusion

Question 5

Absorption, distribution, metabolism, excretion

Answer 5

Pharmacokinetics

Question 7

Type of antagonist that binds reversibly

Answer 7

Competitive antagonist

Question 8

Type of antagonist that binds at the active site or allosteric site

Answer 8

Noncompetitive antagonist

Question 9

Type of antagonist that inactivates the agonist by modifying or sequestering it

Answer 9

Chemical antagonist (Protamine)

Question 10

Type of antagonist that either blocks or activates a receptor

Answer 10

Physiologic antagonist (adrenergic antagonists)

Question 11

Measure of the ability of the body to eliminate a drug

Answer 11

Clearance

Question 12

Measure of apparent space in the body available to contain a drug

Answer 12

Volume of distribution (Vd)

Question 13

Type of antagonist that binds to a receptor, competes with, and prevents binding of other molecules

Answer 13

Pharmacologic antagonist (Atropine)

Question 15

Type of agonist that binds at the active site but only produces a partial response

Answer 15

Partial agonist (buprenorphine)

Question 16

Type of transport that requires energy and a carrier; is saturable (low to high)

Answer 16

Active transport

Question 17

Fractional extent to which a dose of a drug reaches its site of action

Answer 17

Bioavailability

Question 18

Type of drug transport that does not require energy nor a carrier; is non-saturable (high to low)

Answer 18

Passive diffusion

Question 19

A portion of the drug goes to the portal circulation and is metabolized in the liver resulting to a decreased drug effect before it reaches the systemic circulation

Answer 19

First-pass effect

Question 20

Enumerate the CYP inhibitors (decrease in drug metabolism = increase in drug effect)

Answer 20

Sodium Valproate, Isoniazid, Cimetidine, Ketoconazole, Fluconazole, Alcohol (acute), Chloramphenicol, Erythromycin, Sulfonamides, Ciprofloxacin, Omeprazole, Metronidazole, Grapefruit juice, Amiodarone, Quinidine (SICKFACES.COM/GAQ)

Question 21

Type of transport that does not require energy but requires a carrier; is saturable (high to low)

Answer 21

Facilitated diffusion

Question 22

Principal organ in metabolism

Answer 22

Liver

Question 23

Enumerate the CYP inducers (increase in drug metabolism = decrease in drug effect)

Answer 23

Barbiturates, St. John’s Wort, Carbamazepine, Rifampin, Alcohol (chronic), Phenytoin, Griseofulvin, Phenobarbital, Sulfonylureas (BullShit CRAP GPS)

Question 24

Type of agonist that acts by abrogating the intrinsic activity of the free receptor

Answer 24

Inverse agonist

Question 25

Rate and extent of disappearance of a drug from the site of administration and entry into systemic circulation

Answer 25

Drug absorption

Question 26

Route of administration that has a 100% bioavailability

Answer 26

Intravascular

Question 27

Route of administration that has a less than 100% bioavailability (has a lag phase)

Answer 27

Oral

Question 28

The effect where a drug goes into portal circulation and gets metabolized in the liver leading to a decreased drug effect before it reaches systemic circulation

Answer 28

First-pass effect

Question 29

A type of preparation that produces a slow, uniformed absorption of the drug for 8 hours or longer

Answer 29

Controlled-release preparations (extended-release, sustained-release, prolonged-action)

Question 30

Route of administration that has a direct access to the systemic circulation via SVC (bypasses the liver, protecting it from first-pass effect)

Answer 30

Sublingual (Isosorbide dinitrate tablets for angina)

Question 31

Route of administration that has a 50% bioavailability

Answer 31

Rectal (Diazepam suppositories for seizures in children)

Question 32

Route of administration used for diagnostic agents

Answer 32

Intra-arterial

Question 33

Route of administration to surpass the BBB and blood-CSF barrier

Answer 33

Intrathecal

Question 34

Route of administration for non-irritating drugs (has a constant and slow rate of absorption to produce a prolonged effect)

Answer 34

Subcutaneous

Question 35

Route of administration where fat composition is a factor in absorption (more fat = less blood vessels = delayed absorption)

Answer 35

Intramuscular

Question 36

Route of administration where access to circulation is rapid

Answer 36

Inhalation (pulmonary absorption; lungs have a large surface area; salinase for nasal congestion, salbutamol metered-dose inhaler or nebulization for asthma)

Question 37

When 2 (or more) drugs have the same active ingredients, have identical strength or concentration, and are given in the same route of administration

Answer 37

Pharmaceutical equivalents

Question 38

Drugs converted into _ _ are more water-soluble and are more readily excreted

Answer 38

Inactive metabolites

Question 39

Drugs converted into _ _ have the same effect but of longer duration

Answer 39

Active metabolites (Diazepam to Nordiazepam)

Question 40

A compound that has no activity

Answer 40

Prodrug (Salicylic acid undergoes acetylation into AcetylSalicylic Acid or Aspirin)

Question 41

Phase I of metabolism

Answer 41

Oxidation, reduction, hydrolysis -> addition of a functional group -> drug inactivation

Question 42

Phase II of metabolism

Answer 42

Conjugation -> use of phase I by-product -> increased hydrophilicity -> elimination

Question 43

Enzyme system for microsomal metabolism

Answer 43

Cytochrome P450 enzyme system (found in the liver, GIT, lungs, kidneys)

Question 44

The time when half of the initial drug's dose or concentration is reached or decreased

Answer 44

Half-life (t1/2)

Question 45

The amount of drug present inside the body

Answer 45

Area Under the Curve (AUC)

Question 46

Organ in drug excretion

Answer 46

Kidneys (also bile duct, lungs, skin)

Question 47

A constant fraction of the drug is eliminated per unit time and t1/2 is constant (half of the drug is eliminated every x hours)

Answer 47

First-order elimination (most drugs follow this)

Question 48

A constant amount of the drug is eliminated per unit time and t1/2 is variable (a specific amount of the drug is eliminated every x hours)

Answer 48

Zero-order elimination (ethanol in high blood levels, phenytoin in high doses, salicylates in toxic doses)

Question 49

Refers to the volume of blood cleared of drug per unit time

Answer 49

Clearance (Cl) (constant in first-order)

Question 50

The rate when the drug comes in which is equal to the rate the drug goes out (availability rate = elimination rate)

Answer 50

Steady state (usually 4-5 half-lives)