Test 4 - Module 10: Pharmacology Basics Flashcards
Pharmacology is _____.
A. The study of how a drug affects the organism
B. The study of how the organism affects the drug
C. The study of the interactions between a drug and an organism
C
Pharmacodynamics is _____
A. The study of how a drug affects the organism
B. The study of how the organism affects the drug
C. the study of the interactions between a drug and an organism
A
Pharmacokinetics is _____
A. The study of how a drug affects the organism
B. The study of how the organism affects the drug
C. the study of the interactions between a drug and an organism
B
The study of the biochemical, physiological and molecular effects of drugs on the body is ____
Pharmacodynamics
When looking at pharmacodynamics what is included? (5)
- Site of action
- Mechanism of action
- receptor binding
- post receptor effects
- chemical interactions
What three things can affect pharmacodynamics
- age
- disease/disorder
- drug-drug interactions
What three receptor subtypes are included in pharmacodynamics
- Enzymes
- Ion channels
- Membrane receptors
How do drugs bind due to chemical reactions? (4)
- Electrostatic interactions (intermolecular forces)
- Hydrophobic interactions
- Covalent bonds
- stereospecific interactions (enantiomers)
Why do we avoid covalent bonds with drugs
Because it is an intramolecular force. Makes that receptor completely unavailable
What can happen with stereospecific interactions if you have the wrong enantiomers
it might not bind, or it might bind and have negative or no effects
Drugs act as a ____ that bind to the receptor
ligand
Affinity is ____
A. Term used to compare the relative affinity of competing drugs
B. How well the drug binds to the receptor
C. How well the drug produces its desired effect
B
Efficacy is ____
A. Term used to compare the relative affinity of competing drugs
B. How well the drug binds to the receptor
C. How well the drug produces its desired effect
C
Potency is ____
A. Term used to compare the relative affinity of competing drugs
B. How well the drug binds to the receptor
C. How well the drug produces its desired effect
A
If we have a higher affinity we would be able to do what to the dose?
Have a lower dose/not take as much of the drug
What is a competitive antagonists
bind reversibly
what is a non-competitive antagonists?
Either binds irreversibly or binds to create allosteric effects that diminish an agonists ability to bind to a different receptor
The study of the ADME of drugs from the body
Pharmacokinetics
______ effects the ability of the drug to give its desired effect
concentration
_____ helps us to better understand:
1. drug administration
2. therapeutic dosing
3. time intervals between drug dosing
4. toxic dosing
pharmacokinetics
What determines time to maximal concentration at the receptor to produce peak effect?
absorption rate
_____ tells us how much of the administered drug is actually absorbed
Bioavailability
What factors affect bioavaliability (8)
- Drug molecular weight
- Drug formulation
- Drug stability (esp pH sensitivity)
- Drug interactions
- Intestinal motility
- Gastric emptying (food slows this process)
- Blood flow
- First pass metabolism (typically in the liver)
_____ is the effectiveness of the movement of the drug throughout the body
distribution
Distribution is influenced by what? (6)
- blood
- total body water
- ECF
- lymphatic fluids
- CSF
- protein-binding
What drug property help determine ability of a drug to be distributed to the desired receptor site?
Drug solubility
_____ is the breakdown of drugs into metabolites
metabolism
_____ convert from inactive form to active form
prodrug
True/false: metabolism typically does not inactivate the drug ahead of excretion
false. It DOES typically inactivate ahead of secretion
what are common processes of metabolism?
Hydrolysis and REDOX
esters, amides and nitriles are metabolized via ____
hydrolysis
If a drug is being broken down with CP450 enzymes in the liver that would be an example of a ______ reaction
REDOX
What is Lipinski Rule of 5?
Used as a tool to measure a NCE’s (new chemical entity) potential bioavailability
How does the lipinski rule of 5 apply to H bond acceptors/donors
keep them less than 10
Lipinski rule of 5 for molecular weight
less than 500
Lipinski rule of 5 for calculated partition coefficient (cLogP)
less than 5. if it is less than 5 then it can cross membrane easily
Violation of ______ “rule” predicts a NCE is non-orally available
one or more
Structure of an amino acid
- amine group
- carboxcylic acid
- side chain (polar, non-polar, acid/base)
What part of an amino acid can form an H bond?
the polar and acid/base part of the side chain
Why do we like H bonds in drugs
they increase affinity
Potential drug compounds must have a mix of _______ and ______ groups
hydrophillic and lipophillic
What functional groups have been linked to increased toxicity due to their metabolites
- aromatic anilines
- nitroaromatics
- aliphatic halides
- polycyclic aromatic hydrocarbons
- thiophenes
What do these functional groups have in common?
1. aromatic anilines
2. nitroaromatics
3. aliphatic halides
4. polycyclic aromatic hydrocarbons
5. thiophenes
They have been linked to an increased toxicity due to their metabolites
Drug efficacy is directly related to the ______ of the drug at its site of action
concentration
True/false. Drug concentration must be high enough to elicit the desired effect but not too high to cause negative effects
true
Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for absorption?
when they enter the bloodstream
Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for distribution
contact with a receptor
Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for metabolism
when they leave receptor and move to liver
Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for excretion
passage to kidneys for removal
absorption of drugs into the bloodstream is dependent on the _____ properties of the drug and the ______ at the site of absorption
acid/base
pH
_____ transport requires no energy while _____ transport requires energy
passive; active
Active transport: At high drug concentrations, transport _____ due to limited number of transport proteins
plateaus
true/false. active transport can lead to competition with structurally similar compounds.
true
Small drugs (<50Da) and lipophilic drugs (50-500 Da) are transported via
passive
Drugs that have an ionized charge and are (>50 Da) are transported via
active
