Study Guide Chapter 1: Intro

Question 2

What is the history of pharmacology?

Answer 2

Early Medicine (ancient Egypt-Imhotep, ancient Greek-Hippocrates, traditional Chinese medicine) → Materia Medica → Paracelsus (father of toxicology) → Modern Pharmacology (scientific principles, controlled drug trials)

Materia Medica refers to the ancient European system of writing and body of knowledge on botany and medical substances.

Question 3

Define pharmacodynamics.

Answer 3

How the drug affects the body.

Question 4

Define pharmacokinetics.

Answer 4

How the body affects the drug, including absorption, distribution, metabolism, and elimination.

Question 5

Define pharmacogenomics.

Answer 5

How genes determine drug interactions with the body.

Question 6

Define toxicology.

Answer 6

Study of harmful effects.

Question 7

What is an agonist?

Answer 7

Mimics endogenous ligand; binds to the active site.

Question 8

What is an antagonist?

Answer 8

Blocks the active site; competitive inhibitor.

Question 9

Define allosteric.

Answer 9

Binds outside the active site; can be an allosteric agonist or inhibitor.

Question 10

Define orthosteric.

Answer 10

Binds to the active site.

Question 11

What is the difference between toxins and poisons?

Answer 11

Toxins are produced by living organisms (botox); poisons are produced by non-living organisms (anthrax).

Question 12

List the different types of drugs based on their state.

Answer 12

• Solid/Liquid/Gas
  *organic compounds (carbohydrates/lipids/proteins)
  *inorganic compounds (lithium/Fe)

Question 13

What are the factors affecting drug interactions with receptors?

Answer 13

• Appropriate size
• Electrical charge
• Shape
• Bonding

Question 14

Describe the bond strengths in pharmacology.

Answer 14

• Covalent: strongest bond (50-1150 kcal/mol)
• Ionic: 5-10 kcal/mol
• Hydrogen: 2-5 kcal/mol
• Van der Waals forces
• Hydrophobic: 0.5-1 kcal/mol (weakest bond)

Question 15

What is a racemic mixture?

Answer 15

A mixture that is 50/50 (e.g., R-ketamine, S-ketamine).

Question 16

Define stereoisomerism.

Answer 16

chiral compounds. molecules that have the same molecule formula, but have mirror image arrangements.

Question 17

What is a receptor and a receptor site?

Answer 17

*Receptor is the protein
*Receptor site is the site where the drug binds to elicit an effect.

Question 18

What does Emax represent in drug response curves?

Answer 18

Maximal effect a drug can have.

Question 19

What does EC50 represent?

Answer 19

Concentration at which 50% of the maximum effect is achieved.

Question 20

Differentiate between a competitive inhibitor and an allosteric inhibitor.

Answer 20

• Competitive inhibitor: competes directly with the agonist for the active site; can be outcompeted.
• Allosteric inhibitor: binds outside of the active site; cannot be outcompeted.

Question 21

What is physiologic antagonism?

Answer 21

Drugs act at different receptors to counteract each other’s effects.
*Ex: Epi and Clonidine- work in different areas against each other

Question 22

Differentiate between potency and efficacy.

Answer 22

• Potency can be concentration (EC50) or dose (ED50) where 50% of drug’s maximal effect is achieved.
• Efficacy: greatest possible response a drug can deliver.

Question 23

Define a partial agonist.

Answer 23

Produces a lower response at full receptor occupancy; acts as a full agonist alone, acts as antagonist in the presence of an agonist

Question 24

What is an inverse agonist?

Answer 24

“An antagonist on steroids!” Brings the constitutive activity below the baseline; favors the inactive form

Question 25

What is the most common drug carrier in the blood? Names the other drug carriers and what they bind to.

Answer 25

Albumin, which binds mostly to acidic drugs. Alpha 1 acid glycoproteins- basic drugs lipoproteins (ldl,hdl)-neutral drugs

Question 26

What does the Therapeutic Index (TI) measure?

Answer 26

A measure of safety; TI = TD50/ED50 or LD50/ED50.

Question 27

How does pH affect the charge on a drug?

Answer 27

*If pH < pKa, it favors the protonated form *if pH > pKa, it favors the un-protonated form

Question 28

List the four main causes of drug variation.

Answer 28

* Amount of drug available at receptor * Presence or absence of endogenous ligand * Increase or decrease of functional receptors * Increase or decrease in downstream effectors

Question 29

How does the Henderson-Hasselbalch equation relate to drug charge?

Answer 29

It relates pH to pKa, helping to determine if a drug is charged or uncharged.

Question 30

Define monoclonal antibodies.

Answer 30

Antibodies that seek out a specific target and can activate or inactivate it.

Question 31

How are monoclonal antibodies produced?

Answer 31

Forming a Hybridoma by fusing a plasma cell producing antibodies with a cancer cell. *Steps- isolate an antigen, inject a small proportion into a mounse, mouse makes antibodies, mouse is dissected, spleen is removed. B-cells of the spleen are used and fused with cancer cells (hybridoma), the hybridoma is grown and cultured to find the desired antibody. antibody is isolated, grown and cultured. every culture is a clone of the original cell

Question 32

What do the naming conventions for monoclonal antibodies signify?

Answer 32

* -mab: monoclonal antibody * -umab: human * -momab: mouse * -ximab: chimeric * -zumab: humanized

Question 33

Draw the structure of a monoclonal antibody

Answer 33

Question 34

What is the role of the FDA?

Answer 34

Regulatory body overseeing drug development, ensuring drugs are safe and effective.

Question 35

What is the difference in regulation between prescription and OTC drugs?

Answer 35

* Prescription: available only by recommendation of authorized health professionals. * OTC: freely available to the general public.

Question 36

List the steps to bring a prescription drug to market.

Answer 36

* In-vitro studies * Animal testing * IND (investigational new drug) application * Phase I: safety 20-100 * Phase II: efficacy in patients 100-200 * Phase III: double-blind efficacy 1000-6000 * NDA (New drug application) submission * Phase IV: Marketing, Profit