Module 1 Flashcards
The study of drugs.
Pharmacology
Pharmakon means this.
Remedy
Logos means this
Study (or body of knowledge)
What are the three ways to classify therapeutics?
Drugs - traditional drugs (i.e. chemical agents)
Biologics - antibodies, hormones
Natural health products - herbals, vitamins, minerals
What branch oversees pharmacologic agents in Canada?
Health Canada Products and Food Branch
What are the different directorates of the Health Canada Products and Food Branch?
Therapeutic Products Directorate
Biologics and Genetic Therapies Directorate
Natural Health Products Directorate
Oversees traditional drugs such as pills and capsules.
Therapeutic Products Directorate
Oversees antibody and hormone-type therapeutics
Biologics and Genetic therapies directorate
What are the different ways in which a drug is named?
Trade name
Generic name
Chemical (IUPAC) name
Describes the chemical structure of the molecule. Is used by chemists but not by many others.
Chemical name
A unique name that identifies a drug. Most commonly used in pharmacology. It is the name that should be used by HCPs
Generic name
The name assigned by a drug company, usually easy to remember and marketable.
Trade name
What is the issue with trade names?
The problem with trade names is that many companies may make the same drug, therefore it may have different trade names.
Approval of marketed drugs in Canada takes approximately ___ years.
The total cost of a new drug can be as high as ___________$.
15
800 000 000$
Approval of marketed drugs in Canada goes through many stages. What are they?
Pre-clinical testing and Drug discovery Clinical trial application Phase 1 clinical trial Phase 2 clinical trial Phase 3 clinical trial New drug submission (NDS) submitted to Health Canada Phase IV clinical trial
This step of drug testing/development is done in culture cells, living tissue or experimental animals.
The goal is to evaluate biological effects, pharmacokinetics and toxicity.
Preclinical testing/Drug discovery
This must be submitted to Health Canada prior to any human studies.
Details all pre-clinical data.
Health Canada will respond within ___ days of receipt.
Clinical trial application
30
Involves testing on 20-100 healthy volunteers.
What is evaluated at this stage?
Phase 1 clinical testing
Evaluate pharmacokinetics and pharmacodynamics
Involves testing on 300-500 patients with the target disorder.
What is determined at this stage?
Phase II clinical trial
Therapeutic effectiveness, side effects and dosing information is gathered
Involves testing on 500-5000 patients with the disorder.
What is determined?
Therapeutic effectiveness is verified, long term side effects are assessed
Report detailing the therapeutic effectiveness and safety of the drug.
It includes results from pre-clinical and clinical trials.
New drug submission
If the NDS is approved, what does Health Canada issue?
Notice of Compliance (NOC) and a Drug information number (DIN)
What is needed to market a drug?
NOC and DIN
Notice of Compliance
Drug information number
Includes PMS (post-market surveillance). Health Canada monitors the efficacy and safety of the drug after it has been marketed.
Phase IV Clinical trial
What are the different, major routes of administration?
Enteral
Parenteral
Topical/other
Route of administration that involves the GI tract.
Enteral
What are the different enteral routes of administration?
Oral
Rectal
Route involving drug injection.
Parenteral route
What are the different parenteral routes?
Intravenous
Intramuscular
Subcutaneous
Study of what the body does to the drug.
Encompasses four factors, what are they?
Pharmacokinetics
ADME - absorption, distribution, metabolism, excretion
Most orally administered drugs are absorbed in the ____________, transported by the ________ blood supply to the _______.
Small intestine
Portal
Liver
Primary site of drug metabolism
Liver
After reaching the liver, what are the two fates of orally administered drugs?
Enter the systemic circulation and are distributed to different organs
Enter the bile duct and get excreted back into the intestine, and leave the body in feces
What is the primary site of drug excretion?
Kidneys
These form a barrier against orally ingested drugs, toxins and nutrients
Intestinal villi
A - Contains genetic material
B - Metabolizes drugs, carbohydrates and steroids
C - Synthesizes proteins (not ribosomes)
D - Processes and packages proteins and lipids
E - Produces ATP
F - Separates the intracellular and extracellular environments
A - nucleus B - smooth ER C - Rough ER D - Golgi apparatus E - Mitochondria F - Cell membrane
Cellular component which is the major determinant of which drugs are able to enter the cell.
Cell membrane
What is the lipid bilayer composed of? What are these composed of?
Phospholipids - contain Two fatty acids (hydrophobic tails) and a polar head group (phosphate)
Proteins and cholesterol are also embedded
What are the different ways in which drugs cross the cell membrane?
Direct penetration of the cell membrane
Through ion channels and pores
Specific transport proteins (drug transporters)
What is needed for a drug to be able to directly penetrate the cell membrane?
The drug MUST be lipophilic
Channels and pores in cell membranes are very _____.
Only very small compounds (MW < ____) can pass
Channels are very _______ - meaning only certain compounds can fit through them
small
<200 Da
selective
What is an example of a drug that passes through ion channels?
Lithium
Carrier proteins that move drugs from one side of the cell membrane to the other.
What are the two types?
Drug transporters
Uptake transporters - from outside the cell to inside
Efflux transporters - from inside the cell to outside
Important in protecting cells. Present in the intestine, placenta, kidney and BBB.
Efflux transporters
Important in mediating intestinal absorption, renal excretion and reaching target sites of action inside cells
Uptake transporters
What are the different types of drug molecules?
Polar molecules Ions Quaternary ammonium compounds Ionizable molecules Lipophilic molecules
Water soluble molecules which have an uneven distribution of electrical charge, but no net charge.
Polar molecules
Atoms or molecules in which the total number of electrons is not equal to the total number of protons, resulting in a net charge.
Ions
Have at least one nitrogen atom and have a positive charge AT ALL TIMES
Quaternary ammonium compounds
Can exist in charged (weak acid or base) or uncharged forms.
Ionizable molecules
Weak acid - determine whether non-ionized or ionized is the majority in each environment.
Acidic, basic.
Acidic - uncharged/unionized
Basic - charged/ionized
Weak base - determine whether non-ionized or ionized is the majority in each environment.
Acidic, basic.
Acidic - ionized
Basic - unionized
Able to pass through cell membranes.
Lipophilic molecules
Most drugs are weak _____ and thus cross membranes more easily in an ________ medium.
bases
alkaline
Occurs when there is a difference in pH on different sides of a membrane.
Ion trapping
In ion trapping, where do drugs accumulate?
On the side in which they are ionized.
How is ion trapping clinically relevant?
Used in treatment of overdoses
What are the large gaps in capillaries called? How is lipophilic drug movement different from hydrophilic drug movement in capillaries?
Fenestrations
Hydrophilic drugs can only pass through fenestrations (or transporters); lipophilic drugs can pass through the membrane or through fenestrations
What is different about capillaries at the BBB?>
There are no fenestrations; drugs can only enter through transporters or if lipophilic
