Chapter 1 Introduction

Question 1

the practice of medicinal chemistry that is devoted to the discovery and development of new drugs

Answer 1

Organic Medicinal Chemistry

Question 2

an AGENT intended for use in the diagnosis, mitigation, treatment, cure, or prevention of disease in humans or in other animals

Answer 2

DRUG

Question 3

•a substance to which a drug needs to interact with to elicit a pharmacological response
•90% proteins, some are nucleic acids and lipids

Answer 3

RECEPTOR

Question 4

•ability of drug to bind to the receptor

Answer 4

AFFINITY

Question 5

Is Receptor a macromolecules? Yes or no and why?

Answer 5

Yes! 90% proteins, some are nucleic acids and lipids

Question 6

•ability of a drug to exert a pharmacologic action

Answer 6

INTRINSIC ACTIVITY

Question 7

•Affinity + Intrinsic activity

Answer 7

AGONIST

Question 8

•Affinity only

Answer 8

ANTAGONIST

Question 9

•site other than the binding site

Answer 9

ALLOSTERIC SITE

Question 10

FACTORS THAT INFLUENCE THE ABSORPTION:
•Chemical structure
•Variation in particle size
•Nature of the crystal form (Amorphous > Crystalline)
–Example:
- Ultra-lente = 100% crystalline (long-acting)
- Lente insulin = 70% crystalline, 30% amorphous (intermediate)
- Semi lente = 100% amorphous (short-acting)

•Type of tablet coating
•Blood flow to the absorption site
•Total surface area available for absorption
•Contact time at the absorption surface

Answer 10

…

Question 11

FOUR FUNDAMENTAL PATHWAYS OF DRUG PHARMACOKINETICS

Answer 11

Absorbtion
Distributiom
Metabolism
Excretion

Question 12

the transfer of a drug from its site of administration to the systemic circulation (or to the bloodstream)

Answer 12

Absorption

Question 13

————= 100% crystalline (long-acting)

Answer 13

Ultra-lente

Question 14

—————= 70% crystalline, 30% amorphous (intermediate)

Answer 14

Lente insulin

Question 15

————-= 100% amorphous (short-acting)

Answer 15

Semi lente

Question 16

Major site of Absorption

Answer 16

Small intestine

Question 17

Small intestine was consider major site of absorption specifically due to two parts found in small intestine which is the —— and —-

Answer 17

Villi and microvilli

Question 18

Major site of metabolism

Answer 18

Liver

Question 19

Major site of excretion

Answer 19

Kidney

Question 21

Filtering unit of kidney

Answer 21

Nephron

Question 22

Drug for prevention is called ——

Answer 22

Prophylaxis

Question 23

•the fraction of administered drug that reaches the systemic circulation in a chemically unchanged form (f)

Answer 23

BIOAVAILABILITY

Question 24

Bioavalability Equation

Answer 24

F= AUC(oral)/AUC(IV) X AUC(IV) /AUC(Oral)

Question 25

AUC Means

Answer 25

Area Under the Curve

Question 26

————is used to calculate the extent of absorption of a drug. A higher ———— indicates greater bioavailability.

Answer 26

AUC

Question 27

Bioavailability is from Pharmacokinetic or Pharmacodynamic

Answer 27

Pharmacokinetic

Question 28

the process by which a drug reversibly leaves the bloodstream and enters the interstitium (extracellular fluid) and/or the cells of the tissues

Answer 28

Distribution

Question 29

•serves as a reservoir •Albumin - binds acidic drugs •α-1-acid-glycoprotein - binds basic drugs •may limit access to certain body compartments •Prolongs drug duration of action

Answer 29

PLASMA PROTEIN BINDING

Question 30

binds acidic drugs

Answer 30

Albumin

Question 31

binds basic drugs

Answer 31

α-1-acid-glycoprotein

Question 32

Prolongs drug duration of action

Answer 32

PLASMA PROTEIN BINDING

Question 33

serves as a reservoir

Answer 33

PLASMA PROTEIN BINDING

Question 34

converts drugs into polar form, water-soluble products that are readily excretable

Answer 34

METABOLISM

Question 35

detoxification process but not all the time

Answer 35

METABOLISM

Question 36

compounds that are inactive in their native form, but are easily metabolized to the active agent

Answer 36

Prodrugs

Question 37

•an inactive precursor chemical that is readily absorbed and distributed and then converted to the active drug by biologic processes inside the body Ex: –Enalapril to Enalaprilat –Chloramphenicol palmitate to Chloramphenicol –Primidone to Phenobarbital –Phenacetin to Paracetamol

Answer 37

Prodrug

Question 40

All ACE’s that end with “Pril” are Prodrug except——

Answer 40

Captopril(already active)

Question 41

•drugs may be metabolized by hepatic enzymes to inactive chemicals (drug is metabolized prior to absorption) •only drugs administered orally and rectally undergo first pass metabolism (CYP 450) •Ex: Nitroglycerin

Answer 41

FIRST PASS EFFECT

Question 42

only drugs administered——and ———- undergo first pass metabolism (CYP 450)

Answer 42

orally and rectally

Question 44

•the main route of excretion of a drug and its metabolite is through the kidney (for LMW & polar drugs) •Other types: Biliary/Fecal, Breastmilk, Sweat (for HMW & lipophilic drugs)

Answer 44

EXCRETION

Question 45

•drugs emptied via the bile duct into the small intestine can be reabsorbed in the intestinal lumen back to systemic circulation

Answer 45

ENTEROHEPATIC RECIRCULATION