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Pharm 2060 > Module 1 > Flashcards

Module 1 Flashcards

1
Q

Pharmacology is…

A

The study of drugs

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2
Q

3 Routes of Administration

A

Enteral
Parental
Topical

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3
Q

Enteral Administration includes…

A

Oral

Rectal

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4
Q

Parenteral administration includes…

A

Intravenous
Intramuscular
Subcutaneous

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5
Q

Topical administration includes…

A

Creams

Patches

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6
Q

Canadian Drug Legistlation

A

Foods and Drugs Act & Regulations
Health Canada
Health Canada Products & Food Brand
- Therapeutic Products Directorate - Biologics & Genetic Therapies Directorate - Natural Health Products Directorate -

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7
Q

Drugs in the simplest sense are…

A

Chemicals, not pills or capsules

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8
Q

What are the 3 types of drug names and what do they describe?

A

Chemical Name - used by chemists to describe chemical structure
Generic Name - unique drug name that we use most commonly
Trade Name - drug name assigned by company (too many different names for the same drug)

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9
Q

List the 7 step order of approval for marketed drugs in Canada

A
  1. ) Preclinical Testing
  2. ) Clinical Trial Application
  3. ) Phase I Clinical Trial
  4. ) Phase II Clinical Trial
  5. ) Phase III Clinical Trial
  6. ) New Drug Submission (NDS) submitted to Health Canada
  7. ) Phase IV Clinical Trial
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10
Q

Preclinical Testing

A
  • Tested in cultured cells, living tissue or experimental animals
  • Evaluates the biological effects, pharmacokinetics and toxicology
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11
Q

Clinical Trial Application

A
  • Application submitted to Health Canada before any human studies can take place
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12
Q

Phase I Clinical Trial

A

20-100 Healthy “Volunteers”

- Evaluation of pharmacokinetics and pharmacodynamics

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13
Q

Phase II Clinical Trial

A

300 - 500 “patients” with the target disorder

- Therapeutic effectiveness, side effects and dosing information is gathered

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14
Q

Phase III Clinical Trial

A

500 - 5000 Patients with the target disorder

- Therapeutic effectiveness verified, long term side effects assessed

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15
Q

New Drug Submission (NDS) submitted to Health Canada

A
  • A report that details therapeutic effectiveness and safety, includes results from all pre-clinical and clinical studies
  • If approved Health Canada issues a Notice of Compliance (NOC) and a Drug Information Number (DIN)
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16
Q

Phase IV Clinical Trial

A
  • Post marketing surveillance

- Health Canada monitors the efficacy and safety of the drug after it has been marketed

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17
Q

Pharmacokinetics

A

What the body does to the drug

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18
Q

ADME

A

Absorption, Distribution, Metabolism, and Excretion

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19
Q

Absorption occurs…

A

Stomach
Small Intestine
Portal Vein

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20
Q

Metabolism occurs…

A

Liver -> Gall Bladder/Common Bile Duct -> Small + Large Intestine

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21
Q

Distribution occurs…

A

Systemic Circulation -> Heart, Brain, Muscle, Kidney/Bladder

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22
Q

Excretion includes…

A

Biliary - Gall Bladder/Common Bile Duct
Feces - Large Intestine
Renal - Kidney + Bladder

23
Q

Role of intestinal villi

A

Barrier against ingested drugs, toxins and nutrients

24
Q

Role of tight junctions

A

Prevent molecules from passing between cells

25
Q

Nucleus

A

Contains genetic material (DNA)

26
Q

Smooth Endoplasmic Reticulum

A

Metabolizes drugs, carbohydrates and steroids

27
Q

Rough Endoplasmic Reticulum

A

Synthesizes proteins

28
Q

Golgi Apparatus

A

Processes and packages proteins and lipids

29
Q

Mitochondria

A

Produces ATP (cell’s source of energy)

30
Q

Cell Membrane

A

Separates the intracellular and extracellular environments

31
Q

Composition of cell membrane

A

Phospholipids which have a polar (water soluble), phosphate containing head and two fatty acid (lipid soluble) tails. Often called a lipid bilayer.
- Also contains proteins embedded in the phospholipids

32
Q

3 ways drugs cross the membrane…

A
  1. ) Direct penetration of the cell membrane
  2. ) Through ion channels and pores
  3. ) Specific transport proteins (Drug Transporters)
33
Q

Direct penetration of the cell membrane requires…

A

Drugs must be lipid soluble (lipophilic)
-> Cell membranes are composed primarily of lipid, therefore we want drugs to dissolve into the lipids of the cell membrane to pass through. Hydrophobic drugs cannot directly pass through the cell membrane.

34
Q

Requirements for drugs to move through ion channels and pores

A
  • Must be very small (great for ions because they are tiny!)
  • Channels are selective, so only specific compounds can get through them
    Ex. sodium, potassium and lithium
35
Q

Role of Drug Transporters

A

Carrier proteins that move drugs from one side of the cell membrane to the other

36
Q

Uptake Drug Transporters

A
  • Move drugs from outside the cell to inside

- Important in mediating intestinal absorption, renal excretion and reaching target sites of action inside cells

37
Q

Efflux Drug Transporters

A
  • Move drugs from inside the cell to outside

- Important for protecting cells and are present in the intestine, placenta, kindly and at the blood brain barrier

38
Q

5 Types of Drug Molecules

A
  1. ) Polar Molecules
  2. ) Ions
  3. ) Quaternary Ammonium Compounds
  4. ) Ionizable Molecules
  5. ) Lipophilic Molecules
39
Q

Properties of Polar Molecules

A
  • Water Soluble

- Uneven distribution of election charge, but have no net charge (think water H2O!)

40
Q

Properties of Ions

A
  • Total number of electrons is not equal to the total number of protons
  • Have a net charge
  • Charge makes them unable to pass through the cell membrane directly and require pores or ion channels
41
Q

Properties of Quaternary Ammonium Compounds

A
  • Have at least one nitrogen atom and have a positive charge at all times
  • Postive charge does not allow them to directly penetrate the cell membrane
42
Q

Properties of Ionizable Molecules

A
  • Exist in charged or uncharged form
  • Weak acids or weak bases
  • Dependent on the pH of the surrounding medium
43
Q

When will a weak acid be non-ionized?

A

When in an acidic medium such as the stomach

44
Q

When will a weak base be non-ionized?

A

When in a alkaline medium such as the small intestine

45
Q

When will a weak acid be ionized?

A

When in a alkaline medium such as the small intestine

46
Q

When will a weak base be ionized?

A

When in a acidic medium such as the stomach

47
Q

Properties of Lipophilic Molecules

A
  • Lipid soluble unlike polar molecules, ions, quaternary ammonium structures
  • Charged ionizable molecules
48
Q

Can ionized drugs directly penetrate the cell membrane?

A

NO! Only non-ionized drugs can directly penetrate the cell membrane due to their lack of charge.

49
Q

Can non-ionized drugs directly penetrate the cell membrane?

A

YES! Non-ionized drugs can directly penetrate the cell membrane.

50
Q

Ion Trapping

A

Occurs when there is a difference in pH on different sides of a membrane

  • > Drugs accumulate on the side of the membrane in which they are ionized
  • > This is useful clinically in cases such as drug overdose
51
Q

Capillaries

A
  • Smallest blood vessels in the body

- Blood flows from the heart into arteries, then narrower arterioles, which narrow further into capillaries

52
Q

Capillary Beds

A

Supply tissue with oxygenated blood and allow drugs and other molecules to move from the blood to the tissue

53
Q

Fenestrations

A

Large gaps between capillaries in which hydrophobic drugs can bass between the fenestration’s in order to leave the blood.
-> Lipophilic drugs can pass either between the fenestrations or directly through the plasma membrane of capillary endothelial cells

54
Q

How do drugs penetrate the blood brain barrier?

A

Due to the tight junctions, the blood brain barrier does not have any fenestrations. In order to penetrate the drug must be either lipophilic or have a specific transport protein that carries them into the brain.

Pharm 2060 (5 decks)

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