Intro to Pharmacology Flashcards
What is the difference between Pharmacology and Therapeutics?
Pharmacology = drug action Therapeutics = drug prescribing and treatment (patient-focused)
What is the difference between pharmacodynamics and pharmacokinetics?
Pharmacodynamics = what the drug does to the body Pharmacokinetics = what the body does to the drug
What 3 questions can be asked about a drug to understand its pharmacodynamics?
e.g. what would you comment on the pharmacodynamics of cocaine?
Where is this effect produced?
What is the target for the drug?
What is the response that is produced after interaction with this target?
Cocaine: effect = euphoria; target = dopamine reuptake protein on the pre-synaptic terminal; response = blocks dopamine reuptake
Drug target sites tend to be proteins.
What are the 4 main drug target sites in the body? Give an example of a drug for each type of target site:
Receptors - nicotine
Enzymes - aspirin
Ion channels - local anaesthetis
Transport proteins - prozac (anti-depressant)
What is selectivity?
Why do drugs require high levels of selectivity?
Why is it hard to achieve complete selectivity for drugs?
The degree to which a drug acts on a given site relative to other sites
To reduce the number of side effects
A lot of drugs and chemicals are structurally quite similar
How does the selectivity of a drug affect the dosage given? e.g. if a drug is 50 times more selective for target A than target B?
A specific dosage of a drug will begin to show effects at its primary target site e.g. target A. If the drug is 50x more selective for target site A than B, then 50x that dosage will be required to start seeing effects at target B
So why is it important to keep drug dosages as low as possible but still treating the issue?
At a low dose, the effect you see is more specific, due to the fact that the drug will only interact with one target. As the dose increases, the effect becomes less specific, because the drug starts to interact with other drug targets producing other unwanted effects
Pergolide is a drug used to treat Parkinson’s.
What receptor does it primarily act on and what other receptors can it affect at higher doses?
Dopamine receptors primarily
Can also bind to serotonin receptors and adrenergic receptors
What are the 4 different chemical interactions drugs can use to interact with target sites?
(HINT: think chemistry - bonding)
- Electrostatic interactions - most common, includes hydrogen bonds and Van der Waals forces.
- Hydrophobic interactions -lipid soluble drugs
- Covalent bonds - least common, interactions tend to be irreversible
- Stereospecific interactions - many drugs exist as stereoisomers and interact stereospecifically with receptors
What is the equilibrium formed by drugs, receptors, and drug-receptor complexes?
How does an increase or decrease in drug affect this equilibrium?
Drugs + receptors –> drug-receptor complex
Increase in drugs shifts equilibrium to the right as more complexes are formed
Decrease in drugs shifts equilibrium to the left as more receptors are remain unoccupied
What is the difference between agonists and antagonists?
Both fit the target site
Agonists = activate the target site
Antagonists = occupy the target site, so the true molecule cannot bind to the target site to activate it
What is meant by the affinity of a drug?
Strength of binding of the drug to the receptor
Higher affinity = stronger bond
What is meant by the efficacy of a drug?
Ability of an individual drug molecule to produce an effect once bound to a receptor
Higher efficacy = more complete response
So how does efficacy of drugs relate to antagonist / agonist effects?
No response from drug binding to target site = antagonist
Partial response from drug binding to target site = partial agonist
Complete response from drug binding to target site = complete agonist
What is meant by the potency of a drug?
So what is the standard measure of potency?
The concentration or dose of a drug required to produce a defined effect - higher potency = lower dosage required
Standard measure of potency is to determine the concentration (EC50) or dose (ED50) of a drug required to produce a 50% tissue response
What is the difference between EC50 and ED50?
The concentration that produced a 50% response would be the EC50
When responses are vague e.g. reduction in breathlessness, the dose of drug that produced the desired effect in 50% of the individuals tested