1. Intro to Pharmocology

Question 1

What is Pharmacology?

Answer 1

• The study of drugs:
  
  • their sources/origin
  • their appearance/nature
  • their chemistry/composition
  • their actions/effects
  • their uses

Question 2

What does Pharmocology consist of? ex. topics

Answer 2

• Multi-faceted
• General principles of drug action (pharmacodynamics/pharmacokinetics)
• Systems/Organ pharmacology
  
  • Neuropharmacology
  • Cardiovascular pharmacology
• Clinical pharmacology
• Pharmacoepidemiology
• Pharmacogenomics
• Toxicology

Question 3

What is the difference between Pharmacology and Pharmacy?

Answer 3

• Pharmacologist: produces and understands hoe the drugs work
• Pharmacist: gives drugs to public and tells them how it works // more public facing

Question 4

What is a drug? And can it be an endogenous?

Answer 4

• Definition: any biologically active compound taken with the ability to produce a change in biologic function through its chemical function
• Medically speaking: “drug” is a term usually reserved for compounds of an exogenous source. However, when talking about basic principles, drug may refer to endogenous and exogenous compounds.
  • drugs may be identical to endogenously (inside body) produced compounds
  • ex. adrenaline can be endogenously created as your body produces it. It can also be exogenously produced by an epi-pen.

Question 5

What are the 4 core principles of Drugs and Receptors?

Answer 5

• Receptors are used by endogenous drugs as a core element of day-to-day physiology
• There are 100s of different receptors in the body, and compounds/drugsare selective in which receptors they can bind
• Exogenous drugs, such as those taken for medical conditions, act tomodify these processes
• In terms of biological (drug-receptor interaction) effect, drugs fall into one of 3 different categories/mechanisms
  
  • Replacement
  • Interruption
  • Potentiation

Question 6

How are receptors used by the body as a core element of day-to- day physiology (1st core principle)?

Answer 6

• Receptors are a crucial mechanism of communication:
  
  • Translate drug binding into biological response
    
    • 2nd messenger cascade (system)
  • Nervous System
  • Endocrine System
  • Local Regulation

Question 7

What are 2 kinds of structures receptor can be?

Answer 7

• Transmembrane structure –> relates msg to other side
  
  • e.g. G protein coupled receptor
• Intracellular complex
  
  • important implications for drug accessibility
  • e.g. transcription factors in DNA replication

Question 8

What is a specialized receptor?

Answer 8

• Definition: a specialized structure (usually protein) designed to bind an endogenous signal molecule (hormone, neurotransmitter, antacid, etc.) for the purpose of facilitating cell-to-cell communication

*Referred to as a specialized receptor: bind to the drugs and take that msg into the cell

Question 9

What is a generalized receptor?

Answer 9

• Definition: a molecule standard to a cell’s function or regulation, whose activity can incidentally be modified by (exogenous) drug interaction.
  
  • basically drugs can bind to and repair their function
  • still impacted by drugs
  • not specified receptors because their job isn’t communicating. It’s performing some other function
• ex. example pic on slide 22

Question 10

Explain how Receptor numbers vary and its selectivity (2nd core principle).

Answer 10

• Many different receptor families throughout body, vary in…
  
  • structure
  • 2nd messenger cascade (what they do when activated)
  • expression (locations/number)
• Drugs will preferentially bind to certain receptors over others, oftendue to how “snugly” they fit in binding site
  
  • “chemical-structure dependent” interactions
  • enzymatic “lock and key” model

–> ex. on slide 25

Question 11

Explain Drug-Receptor Interaction (lock and key model).

Answer 11

*look on slide 24

Question 12

Explain how receptors can be “hijacked” (3rd core principle).

Answer 12

• Exogenous molecules can bind to endogenous receptors and affect biochemical processes
  
  • IF they can reach the tissue where the receptor is located
  • Molecules will often have similar chemical structure to endogenous “drug” in order to work

Question 13

What is an Antagonist?

Answer 13

• can act on specialized or generalized receptors
• Exogenous drugs that bind to an endogenous receptor without activation
• “Produces a response” by occupying site, meaning any endogenous drugs are unable to bind and activate
• Often chemically similar to agonists, but lack crucial part of the “key” for that “lock”
• ex. Claritin® (loratidine) –>Histamine receptor antagonist
  
  • Prevents allergic response to endogenously-produced histamine

Question 14

What is an Agonist?

Answer 14

• act on specialized receptors
• Mimic an endogenous molecule, binding to and activating a receptor
• Usually very chemically similar to endogenous drug, making it a good fit for the receptor “lock”
• ex. VentolinTM (salbutamol) –> for asthma
  
  • β2-adrenoreceptor agonist
    
    • Stimulates receptors
    • Located primarily in lungs
    • Relaxation of bronchial smooth muscle
    • Easier breathing

Question 15

Explain the 3 mechanisms/types of Biological effects. (4th core principle).
- (can give in terms of blood pressure control)

Answer 15

*refer back to Lecture 1, slides 28-34