35 Questions
What is the term for the maximal response a drug can produce?
Emax
What type of antagonist is characterized by the ability to bind to a receptor and block the action of an agonist, but can be reversed by increasing the concentration of the agonist?
Competitive reversible antagonist
What is the term for the concentration of a drug required to produce 50% of its maximal response?
EC50
What type of modulation involves the binding of a molecule to a site on the receptor, other than the active site, resulting in a conformational change that affects the activity of the receptor?
Allosteric modulation
What is the term for a drug that binds to a receptor and produces a response, but with less efficacy than a full agonist?
Partial agonist
What is the term for the dose of a drug required to produce 50% of its maximal response?
ED50
What type of molecule is most commonly targeted by drugs?
Proteins
What is the term for the ability of a drug to produce a desired response?
Efficacy
What type of receptor is modulated by benzodiazepines?
GABA receptor
What is the term for a molecule that binds to a receptor but cannot activate it?
Antagonist
What is the term for the attraction between a drug and its target molecule?
Affinity
What type of receptor is targeted by salbutamol?
Beta-2 adrenoceptor
What is the primary focus of pharmacodynamics?
The study of the action of drugs on the physiology or pathology of the body
What is the primary goal of a curative drug?
To remove the underlying physiological cause of a condition
Why is it recommended to use generic names when referring to drugs?
Because they are more specific to the active ingredient
What is the primary difference between a therapeutic drug and a curative drug?
A therapeutic drug treats symptoms, while a curative drug treats the cause
What is pharmacokinetics primarily concerned with?
The movement of drugs within the body
Why is it important to understand the difference between a therapeutic drug and a curative drug?
Because it affects the patient's understanding of the treatment
The type of antagonist that binds to a receptor and cannot be reversed by increasing the concentration of the agonist is referred to as a non-competitive antagonist.
True
The EC50 of a drug is the concentration required to produce 100% of its maximal response.
False
L-dopa is converted to dopamine in the brain and is used to treat Parkinson's disease.
True
The Kd of a drug is the concentration of ligand at 50% of receptor occupancy.
True
GABA is an inhibitory neurotransmitter that is enhanced by benzodiazepines.
True
Captopril is an SSRI that is used to treat depression.
False
Nitrates are commonly used as calcium channel antagonists.
False
Benzodiazepines are a type of G-protein coupled receptor agonist.
True
Phenylephrine is a β2 adrenoceptor antagonist.
False
Atenolol is a β2 adrenoceptor antagonist.
False
Salbutamol is a β1 adrenoceptor agonist.
False
Pharmacodynamics is the branch of pharmacology concerned with the movement of drugs within the body.
False
Anti-cancer agents are an example of curative drugs.
False
Brand names should be used when referring to drugs in a pharmacology context.
False
All therapeutic drugs are also curative drugs.
False
Pharmacology is the study of the movement of drugs within the body.
False
Insulin is an example of a curative drug for diabetes.
False
Study Notes
What is Pharmacology?
- Pharmacology is the study of medicines and drugs, including their action, their use, and their effects on living systems.
- It consists of two branches: pharmacodynamics (action of drugs on the body) and pharmacokinetics (movement of drugs within the body).
Key Principles of Pharmacology
- Pharmacology involves the study of how drugs work, including their interactions with receptors.
- There are different types of drugs, including agonists, antagonists, and partial agonists.
Drug Targets and Receptors
- Drug targets include nuclear receptors, enzymes, ion channels, and protein carriers.
- Examples of drugs and their targets include:
- Steroid hormones and glitazone drugs (nuclear receptors)
- Captopril (ACE inhibitor)
- Flurouracil (uracil replacement, anti-cancer)
- L-dopa (converted to dopamine)
- SSRI (inhibits reuptake of 5-HT)
- Lithium (mood stabilizer)
Types of Antagonists
- Competitive, reversible antagonist
- Competitive, irreversible antagonist
- Non-competitive antagonist
- Competitive, irreversible antagonist
Allosteric Modulation
- Allosteric modulation involves the binding of a molecule to a receptor, altering its activity.
- Examples of allosteric modulation include benzodiazepines (GABA receptor modulator) and glutaminase.
Partial Agonists
- A partial agonist is a drug that binds to and activates a receptor, but with only partial efficacy.
- Partial agonists can have varying levels of efficacy at different receptors.
Concentration-Response Curve
- The concentration-response curve is a graph that shows the relationship between the concentration of a drug and its response.
- The EC50 is the concentration of a drug required to produce 50% of its maximal response (Emax).
- Examples of EC50 values include:
- Histamine on guinea pig heart: 9 x 10^(-7) mol/l = 900 nM
- ACh on frog rectus muscle: 1 x 10^(-5) mol/l = 10 μM
Drug Binding
- Drug binding involves the interaction between a drug and a biological molecule, such as a receptor or enzyme.
- Agonists bind to receptors and activate them, while antagonists bind to receptors but do not activate them.
- Affinity refers to the attraction between a drug and its target, while efficacy refers to the ability of a drug to produce a desired response.
Types of Receptors
- Ion channel receptors: Nifedipine (calcium channel blocker) and nitrazepam (benzodiazepine, GABA receptor modulator)
- G protein-coupled receptors: Phenylephrine (α1 adrenoceptor agonist), Propranolol (β adrenoceptor antagonist)
- Enzyme-linked receptors: Insulin and cytokines (used as therapy for various conditions)
Learn about the fundamentals of pharmacology, including key principles, types of drugs, and how they interact with receptors. Understand the study of medicines and drugs, their action, use, and effects on living systems.
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