ORG MED CHAP 1

Question 1

It is 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

___________ is a substance to which a drug needs to interact with to elicit a pharmacological response
___________proteins, some are nucleic acids and lipids

Answer 3

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

Question 4

___________ ability of drug to bind to the receptor

Answer 4

Affinity

Question 5

___________ ability of a drug to exert a pharmacologic action

Answer 5

INTRINSIC ACTIVITY ability of a drug to exert a pharmacologic action

Question 6

_______
Affinity only

Answer 6

ANTAGONIST

Question 6

_________
Affinity + Intrinsic activity

Answer 6

AGONIST

Question 6

WHAT ARE THE FOUR FUNDAMENTAL PATHWAYS OF DRUG PHARMACOKINETICS?

Answer 6

(ADME) ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION

Question 7

_____________________
site other than the binding site

Answer 7

ALLOSTERIC SITE

Question 8

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

Answer 8

ABSORPTION

Question 9

WHAT ARE THE FACTORS THAT INFLUENCE THE
ABSORPTION?

Answer 9

Chemical structure
Variation in particle size
Nature of the crystal form (Amorphous >
Crystalline)

Question 10

____________ = 100% crystalline (long-acting)

Answer 10

Ultra-lente

Question 11

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

Answer 11

Lente insulin

Question 12

_________ = 100% amorphous (short-acting)

Answer 12

Semi lente

Question 13

What is the minimum value of Pre- Diabetes?

Answer 13

100

Question 14

what is the maximum value of Diabetes?

Answer 14

above 126

Question 15

what is the maximum value of Pre-Diabetes?

Answer 15

125

Question 16

what is the minimum value of Diabetes?

Answer 16

126

Question 17

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

Answer 17

Bioavailability

Question 18

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

Answer 18

DISTRIBUTION

Question 19

________________
- serves as a reservoir
-may limit access to certain body
compartments
- Prolongs drug duration of action

Answer 19

PLASMA PROTEIN BINDING

Question 20

___________binds acidic drugs

Answer 20

Albumin

Question 21

__________binds basic drugs

Answer 21

α-1-acid-glycoprotein

Question 22

___________________
* converts drugs into polar form, water-soluble products that are readily excretable
* detoxification process but not all the time

Answer 22

METABOLISM

Question 23

compounds that are inactive in their native form, but are easily metabolized to the active agent
Ex:
– Enalapril to Enalaprilat
– Chloramphenicol palmitate to Chloramphenicol
– Primidone to Phenobarbital
– Phenacetin to Paracetamol

Answer 23

PRODRUGS

Question 24

GIVE ME ONE EXAMPLE OF FIRST PASS EFFECT

Answer 24

NITROGLYCERIN

Question 25

______________
* drugs may be metabolized by hepatic enzymes to inactive chemicals (drug is metabolized prior to absorption)
* only _________ administered orally and
rectally undergo first pass metabolism (CYP 450)

Answer 25

FIRST PASS EFFECT
DRUGS

Question 26

__________________
* the main route of excretion of a drug and its metabolite is through the kidney (for LMW & polar drugs)

Answer 26

EXCRETION

Question 27

WHAT ARE THE OTHER TYPES OF EXCRETION?

Answer 27

Biliary/Fecal, Breastmilk, Sweat (for HMW & lipophilic drugs)

Question 28

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

Answer 28

ENTEROHEPATIC RECIRCULATION