1.01 - Nature of Drugs and Drug Development & Regulation

Question 1

Reliance on observation and experimentation

Answer 1

17th Century

Question 2

They developed the methods of experimental physiology and pharmacology.

Answer 2

François Magendie & Claude Bernard

Question 3

When was controlled clinical trials reintroduced to medicine?

Answer 3

About 60 years ago

Question 4

The study of substances that interact with living systems through chemical processes

Answer 4

Pharmacology

Question 5

The science of substances used to prevent, diagnose, and treat disease.

Answer 5

Medical Pharmacology

Question 6

A branch of pharmacology that deals with the undesirable effects of chemicals on living systems, from individual cells to humans to complex ecosystem.

Answer 6

Toxicology

Question 7

The study of genetic variations that cause differences in drug response among individuals or population.

Answer 7

Pharmacogenetics or Pharmacogenomics

Question 8

Enumerate the 1st domain in the major areas of study in Pharmacology. (3)

Answer 8

1. Medical Pharmacology & Toxicology
2. Pharmacokinetics
3. Pharmacodynamics

Question 9

It is the understanding the actions of drugs as chemicals on individual organisms, especially humans and domestic animals.

The beneficial and toxic effects.

Answer 9

Medical Pharmacology and Toxicology

Question 10

Deals with the absorption, distribution, and elimination of drugs

Answer 10

Pharmacokinetics

Question 11

Concerns the actions of the chemical on the organism.

Answer 11

Pharmacodynamics

Includes:

• Mechanism of Action (MOA) of the drug
• Therapeutic and Toxic effects

Question 12

Deals with the effects of chemicals on all organisms and their survival in groups and as species.

Answer 12

Environmental Toxicology

Question 13

• any substance that brings about a change in biologic function through its chemical actions.
• agent used in mitigation, diagnosis, prevention, and cure of diseases in man and animal and has the ability to modify the body structure and function.

Answer 13

Drug

Question 14

“activator”

Answer 14

Agonist

Question 15

“Inhibitor”

Answer 15

Antagonist

Question 16

“Target molecule”

Answer 16

Receptor

Question 17

Drugs that may interact directly with other drugs.

Answer 17

Chemical antagonist

Question 18

Interact almost exclusively with water molecules.

Answer 18

Osmotic agents

Question 19

Drugs may be synthesized within the body.

Answer 19

Hormones

Question 20

Chemicals that are NOT synthesized in the body.

Answer 20

Xenobiotics

Question 21

Drugs that have almost exclusively harmful effects.

Answer 21

Poisons

Question 22

Are usually defined as poisons of biologic origin, ie, synthesized by plants or animals, in contrast to inorganic poisons

Answer 22

Toxins

Question 23

Give examples of inorganic poisons

Answer 23

Lead & Arsenic

Question 24

To interact chemically with the receptor, a drug molecule must have __(1)__, __(2)__, __(3)__ and __(4)__.

Answer 24

appropriate size
electrical charge
shape
atomic composition

Question 25

True or False. A drug is often administered at a location near its intended site of action.

Answer 25

False. A drug is often administered at a location DISTANT from its intended site of action.

Question 26

What is the molecular weight of lithium ion?

Answer 26

7 MW

Question 27

What is the molecular weight of alteplase?

Answer 27

59,050

Question 28

Most of the drugs have molecular weights between?

Answer 28

100 to 1000

Question 29

For selective binding, the MW must be at least __ MW units in size.

Answer 29

100

Question 30

Drugs much larger than MW ____ DO NOT diffuse readily between the compartments of the body (Permeation).

Answer 30

1000

Question 31

A very strong bond and in many cases, irreversible under biologic conditions.

Answer 31

Covalent bond

Question 32

Much more common than covalent bonding in drug-receptor interactions.

Answer 32

Electrostatic bond

Question 33

Usually quite weak and important for the interactions of highly lipid-soluble drugs with the lipids of cell membranes and in the interaction of drugs with the internal walls of receptor “pockets.”

Answer 33

Hydrophobic

Question 34

Drugs that bind to the same receptor molecule but do not prevent binding of the agonist.

Answer 34

Allosteric drugs

Question 35

when administered at concentrations sufficient to saturate the receptor pool, it can activate their receptor effector systems to the maximum extent of which the system is capable.

Answer 35

Full Agonist

Question 36

➢binds to the same receptors and activate them in the same way but do not evoke as great a response, no matter how high the concentration. ➢ Low intrinsic efficacy

Answer 36

Partial Agonist

Question 37

Presence of the antagonist at the receptor site will block access of agonists to the receptor and prevent the usual agonist effect.

Answer 37

Neutral Antagonism

Question 38

The drug will reduce any constitutive activity -> resulting in effects that are the opposite of the effects produced by conventional agonists at that receptor.

Answer 38

Inverse Agonists

Question 39

Specific regions of receptor molecules provide the local areas responsible for drug binding.

Answer 39

Receptor sites or Recognition sites

Question 40

Drugs bind to some non-regulatory molecules in the body without producing a discernible effect.

Answer 40

Inert Binding Sites

Question 41

To function as a receptor, an endogenous molecule must? (2)

Answer 41

1. be selective in choosing ligands to bind | 2. must change its function upon binding

Question 42

The _____ characteristic is required to avoid constant activation of the receptor by promiscuous binding of many different ligands.

Answer 42

selectivity

Question 43

The action of the body on the drug.

Answer 43

``` ADME: Absorption Distribution Metabolism Excretion/elimination ```

Question 44

an inactive precursor chemical that is readily absorbed and distributed must be administered and then converted to the active drug by biologic processes—inside the body.

Answer 44

Prodrug

Question 45

From a movement of drug molecules into and within the biological environment

Answer 45

Permeation

Question 46

Permeation common in aqueous or lipid medium is.

Answer 46

Passive Diffusion

Question 47

Movement of molecules through watery extracellular and intracellular spaces. Occurs within occurs within the larger - aqueous compartments of the body - across epithelial membrane tight junctions and the - endothelial lining of blood vessels through aqueous pores

Answer 47

Aqueous diffusion

Question 48

The most important limiting factor for drug permeation because of the large number of lipid barriers that separate the compartments of the body.

Answer 48

Lipid diffusion

Question 49

Exist for many substances that are important for cell function and too large or too insoluble in lipid to diffuse passively through membranes.

Answer 49

Transport by special carriers

Question 50

The process by which the substance is bound at a cell-surface receptor, engulfed by the cell membrane, and carried into the cell by pinching off of the newly formed vesicle inside the membrane.

Answer 50

Endocytosis

Question 51

iron is transported into hemoglobin-synthesizing red blood cell precursors in association with the protein ____?

Answer 51

transferrin

Question 52

Reverse process, expulsion of material that is membrane-encapsulated inside the cell from the cell.

Answer 52

Exocytosis

Question 53

Commonly causes a respiratory alkalosis metabolic acidosis.

Answer 53

Aspirin (ASA) Overdose

Question 54

Important in the management of ASA overdose.

Answer 54

Sodium Bicarbonate