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2060B: Pharmacology > Module 1: Intro to Pharmacology > Flashcards

Module 1: Intro to Pharmacology Flashcards

1
Q

Define pharmacology

A

The word pharmacology is derived from the Greek words pharmakon meaning remedy and logos meaning study.
- Generally, pharmacology is considered the study of drugs.

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2
Q

What 4 aspects does pharmacology include?

A
  1. How a drug is delivered (it’s route of administration).
  2. How a drug works (it’s mechanism of action).
  3. The therapeutic effect of drugs on patients.
  4. The adverse effects of drugs on patients.
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3
Q

How are drugs classified? (3)

- Give an example of each

A
  1. Drugs – Traditional drugs (i.e. chemical agents).
  2. Biologics – Ex. Antibodies, and hormones.
  3. Natural Health Products – Ex. Herbals, vitamins, minerals.
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4
Q

Before a drug reaches the market there is research to determine if it is (2):

A

1) Safe

2) Effective

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5
Q

Define drug

A

Typically, we think of a drug as a “pill” or “capsule”.

  • Drugs are actually chemicals.
  • Within every pill are many molecules of a chemical.
  • It is the chemical that actually produces the pharmacological effect.
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6
Q

How does one name drugs? (3)

A
  1. Chemical Name
    - Describes the chemical structure of the molecule
    - Is used by chemists but not by many others.
  2. Generic Name
    - A unique name that identifies a drug.
    - The generic name is the name most often used in Pharmacology.
    - It is the name that should be used by health care professionals (although it often isn’t).
  3. Trade name
    - The name assigned by a drug company.
    - It is usually easy to remember and marketable.
    - The major problem with trade names is many companies may make the same drug, therefore it may have many different trade names.
    - Ambiguous so use generic name.
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7
Q

Briefly describe drug development:

A
  • Approval of marketed drugs in Canada takes ~15 years
  • Drug development moves through several different levels
  • Total cost of new drug can be as high as ~800 million
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8
Q

Describe (7) steps of approval of marketed drugs in Canada

A

1) Pre-clinical Testing
- Cultured cells, living tissue, experimental animals
- Evaluate biological effects, pharmacokinetics, and toxicity

2) Clinical Trial Application
- Submitted to Health Canada prior to human studies

3) Phase I: Clinical Trial
- 20-100 healthy volunteers
- Evaluation of pharmacokinetics and pharmacodynamics

4) Phase II: Clinical Trial
- 300-500 patients with target disorder
- Therapeutic effectiveness, side effects, dosing info

5) Phase III: Clinical Trial
- 500-5000 patients with target disorder
- Therapeutic effectiveness verified, long term side effects assessed

6) New Drug Submission (NDS) submitted to Health Canada
- Report = effectiveness/safety
- Pre-clinical and clinical study results

7) Phase IV: Clinical Trial
- Post-marketing surveillance
- Efficacy and safety of drug

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9
Q

What are the (3) methods to administering drugs into people? Explain each.

A

1) Enteral - “involves GI Tract”
- Oral
- Rectal

2) Parenteral - “does not involve GI tract”
- Intravenous
- Intramuscular
- Subcutaneous

3) Topical
- Creams
- Patches

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10
Q

Define pharmacokinetics:

A

It is what the body does to the drug:

  • Absorption
  • Distribution
  • Metabolism
  • Excretion
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11
Q

During oral administration of a drug, where does most of the absorption occur?

A

Small intestine

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12
Q

During oral administration of a drug, how does the drug travel to the liver?

A

Carried by the portal blood supply

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13
Q

During oral administration of a drug, where is the primary site of metabolism?
- What are the 2 “fates”, explain each, and how the drug is excreted?

A

Liver

1) Systemic Circulation
- Brain, heart, muscle, kidney (primary excretion via urine)

2) Bile Duct
- Back into the intestine
- Excretion via feces

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14
Q

During parenteral injection of a drug, where is the primary site of absorption?

A

Systemic circulation

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15
Q

What are two physiological barriers to drug transport?

A

1) Intestinal Villi

2) Tight junctions

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16
Q

What does a drug need to exert its effects (2) ? Why?

A

Physical and chemical properties

- To pass through barriers

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17
Q

What does the nucleus contain?

A

Genetic material

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18
Q

What does the smooth ER do?

A

Metabolizes drugs, carbohydrates, and steroids

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19
Q

What does the rough ER do?

A

Synthesizes proteins

20
Q

What does the golgi apparatus do?

A

Processes and packages proteins and lipids.

21
Q

What does the mitochondria do?

A

Produces ATP (cell’s source of energy).

22
Q

What does the cell membrane do (2)?

A

1) Separates the intracellular and extracellular environments
2) Controls which drugs can enter

23
Q

What is the cell membrane composed of?

A

Composed of phospholipids which have a polar (water soluble), phosphate containing head and two fatty acid (lipid soluble) tails.

24
Q

Why is the cell membrane also called the lipid bilayer?

A

The cell membrane is often called a lipid bilayer because of the arrangement of the phospholipids.

25
Q

Is the cell membrane fluid?

A

The cell membrane is “fluid” because the phospholipids are flexible allowing them to undulate back and forth.

26
Q

What else is embedded in the phospholipid membrane?

A

The cell membrane also contains proteins embedded in the phospholipids.

27
Q

How do drugs cross the cell membrane (3)?

A
  1. Direct penetration of the cell membrane.
  2. Through ion channels and pores.
  3. Specific transport proteins (drug transporter’s).
28
Q

What type of cells can penetrate the cell membrane directly?

A

Lipid soluble cells (lipophilic)

29
Q

What type of cells can pass through ion channels and pores?

A

Channels and pores are very small - Therefore, only very small compounds

30
Q

What are the 2 types of drug transporters? What are they important for?

A

1) Uptake: Move drugs from the outside to inside of cell
- Mediating intestinal absorption, renal excretion, and reaching target sites of action inside cells

2) Efflux: Move drugs from inside cell to outside
- They are important for protecting cells and are present in the intestine, placenta, kidney and at the blood brain barrier.

31
Q

What are the (6) different types of drug molecules

A
  1. Polar Molecules
  2. Ions
  3. Quaternary Ammonium Compounds
  4. Ionizable Molecules
  5. Lipophilic Molecules
32
Q

What are (2) characteristics of polar molecules? Provide an example.

A

1) Water soluble
2) Uneven distribution of electrical charge = no net charge

Examples:

  • H2O
  • Glucose
  • Kanamycin
33
Q

What are (2) characteristics of ions? Provide an example.

A

1) Total number of electrons do not equal total number of protons = negative/positive charge
2) Due to charge, cannot directly pass through cell membrane (only small ions)

Examples:

  • Na+
  • K+
  • CL-
  • Li+
34
Q

What are (3) characteristics of quaternary ammonium compounds?

A

1) Have at least 1 N atom
2) Positive charge at all times
3) Unable to cross membranes due to positive charge

35
Q

What are (2) characteristics of ionizable molecules?

How do you determine whether a weak acid or a weak base carries a charge?

How do we know if it is ionized or unionized?

A

1) Exist in charged/uncharged forms
2) Weak acids or weak bases

Determination of whether a weak acid or a weak base carries a charge depends on the pH of the surrounding medium.

Ionized/Unionized - Depends on the medium

a) Weak acid + Acidic medium (i.e. stomach) = non-ionized
b) Weak acid + Alkaline medium (i.e. small intestine) = ionized
c) Weak base + Acidic Medium (i.e. stomach) = ionized
d) Weak base + alkaline medium (i.e. small intestine) = non-ionized

36
Q

What is a characteristic of lipophilic molecules?

A
  • Lipid soluble
37
Q

What is the impact of pH on drug movement?

A

Only non-ionized drugs can directly penetrate the cell membrane.

38
Q

Most drugs are weak bases, meaning they can cross the membranes easier if they are what type of medium?

A

Alkaline

39
Q

The acidic drug is unionized and therefore can/cannot cross the cell membrane?

A

Can

40
Q

The basic drug is ionized and therefor can/cannot cross the cell membrane?

A

Cannot

41
Q

What is ion trapping?

Provide an example.

A

Ion trapping occurs when there is a difference in pH on different sides of a membrane
- Drugs accumulate on the side of the membrane where they are ionized.

Example:

  • An acidic drug is placed into an acidic environment. - Since acidic drugs are unionized in acidic environments, the drug is able to cross the membrane.
  • The other side of the membrane is basic, therefore when the drug crosses the membrane is becomes ionized
  • Since ionized drugs are unable to cross cell membranes, the drug is now “trapped” on the basic side of the membrane.
42
Q

How do molecules pass through capillaries?

A

Fenestrations

- Small holes within the endothelial cells of the capillary

43
Q

Can hydrophilic drugs penetrate endothelial cell wall?

A

No but, they can pass through the fenestrations to leave the capillaries

44
Q

How do lipophilic drugs pass through capillaries?

A

Either between fenestrations, tight junctions, or directly through plasma membrane

45
Q

How do drugs enter the brain?

A

The brain has a blood brain barrier which has tight junctions and no fenestrations
- Drugs must be lipophilic or have specific proteins that carry them into the brain

2060B: Pharmacology (18 decks)

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