Exam 1 Flashcards
Study of the effects of drugs on the body and how the body responds to the drugs
Pharmacology
Collection of botany and medicinal substances, precursor to pharmacology, around 40 BCE
Materia Medica
Considered the father of toxicology, known for the phrase ‘The dose makes the poison’
Paracelsus
Describes what a drug does to the body
Pharmacodynamics
Describes what the body does to a drug, involving absorption, distribution, metabolism, and excretion (ADME)
Pharmacokinetics
Study of how a person’s genetic profile can influence their response to drugs
Pharmacogenomics
Study of harmful effects of chemicals, substances, or situations on living organisms and the environment
Toxicology
What is an agonist?
A drug that binds to a receptor and activates a response
How does an agonist compare to the native ligand?
It may have a response greater or lesser than the native ligand
What is an antagonist?
A drug that binds to a receptor and prevents the binding of the native ligand without activating a response.
What is the function of an antagonist?
To block the receptor and inhibit the biological response that would normally occur upon ligand binding.
Drug binding occurs at a site other than the active site on a receptor
Allosteric
Drug binding occurs at the active site of a receptor
Orthosteric
Toxins vs. Poisons
Toxins are biological substances, poisons are non-biological substances like arsenic or lead
Drugs act at different receptors to counteract the effects of other drugs
Physiologic Antagonism
Drugs that favor the inactive form of a receptor, effectively acting as stronger antagonists
Inverse Agonists
Strongest type of bond, followed by ionic, hydrogen, and hydrophobic bonds
Covalent Bond
Combination of optical isomers, mirror images of each other, can have different effects
Racemic Mixtures
Large protein on cell surface that can bind to drugs or endogenous ligands
Receptor
Specific site on a receptor where a drug or ligand binds to elicit a response
Receptor Site
Maximum number of receptors available for a drug to bind to
Bmax
Maximum effect or response achievable by a drug
Emax
Dissociation constant, drug concentration at which 50% of receptors are occupied
Kd
Effective concentration for 50% of the maximum effect, indicates drug potency
EC50
Drug that competes for the active site with the agonist (surmountable)
Competitive Inhibitor
Drug that binds to a different site on the receptor, preventing agonist binding (insurmountable)
Allosteric Inhibitor
What is allosteric inhibition?
Inhibition that cannot be surmounted by increasing the dose of an antagonizing drug due to binding on a different site than competitive inhibition.
How does allosteric inhibition differ from competitive inhibition?
Allosteric inhibition cannot be surmounted by increasing the dose of an antagonizing drug due to binding on a different site.
What is physiologic antagonism?
It is a situation where two drugs/native ligands bind to different receptors with opposite effects.
Give an example of physiologic antagonism in the cardiovascular system.
Epinephrine increases heart rate via beta receptors, while acetylcholine decreases heart rate via muscarinic receptors.
Refers to the amount of drug required to produce a specific effect.
Potency
Extent to which a drug produces a maximum effect regardless of dose.
Efficacy
What is a partial agonist?
Binds like an agonist but produces a partial response.
How does a partial agonist act in the presence of a full agonist?
Acts as an antagonist by preventing full agonist binding.
What is the role of an inverse agonist?
It favors inactive receptors, acting as a stronger form of antagonist by lowering the constitutive form of the receptor.
How does an inverse agonist differ from an antagonist?
An inverse agonist favors inactive receptors and acts as a stronger form of antagonist by lowering the constitutive form of the receptor.
What are drug carriers?
Molecules like albumin in blood that bind drugs.
How do drug carriers affect drug distribution and pharmacokinetics?
They alter drug response based on patient albumin levels.
Ratio of toxic dose to therapeutic dose, indicating drug safety margin.
Therapeutic index
Relates pH to pKa for weak acids and bases, determining their charged state in a solution.
Henderson Hasselbach equation
How are monoclonal antibodies produced?
From a single clone of B cells, created by fusing B cell with myeloma cell.
What defines monoclonal antibodies?
Identical antibodies binding to a specific antigen.
Regulatory body ensuring drug safety and efficacy in the United States, overseeing drug development from pre-clinical studies to post-marketing surveillance.
FDA
Steps to bring a prescription drug to market
Include pre-clinical studies, IND application, Phase I-III trials, NDA submission, FDA review, and post-marketing surveillance.
Receptor types based on molecular structure
Include G protein-coupled receptors, ligand-gated ion channels, catalytic receptors, nuclear receptors, transporters, and enzymes.
Define G protein-coupled receptors (GPCRs)
Receptors with seven transmembrane spanning domains, an extracellular ligand-binding site, and an intracellular G protein-binding site.
Ion channels that open in response to the binding of a specific ligand.
Ligand-gated ion channels
Receptors that have intrinsic enzymatic activity upon ligand binding.
Catalytic receptors
Receptors that regulate gene expression upon ligand binding.
Nuclear receptors
Proteins responsible for the movement of ions, small molecules, or macromolecules across biological membranes.
Transporters
Biological molecules that catalyze biochemical reactions.
Enzymes
Molecules that amplify and propagate the signal initiated by the first messenger.
Second messengers
What is desensitization?
The process where a cell reduces its responsiveness to a stimulus over time.
The space available in the body to contain the drug.
Volume of distribution (Vd)
The ability of the body to eliminate the drug.
Clearance (CL)
The amount of drug in the body.
Concentration (C)
The rate at which the drug is eliminated from the body.
Rate of Elimination (ROE)
The desired concentration of the drug in the body to achieve the desired effect.
Target concentration (TC)
The time it takes for the drug concentration to decrease by 50%.
Half-life (T1/2)
The fraction of the administered dose that reaches the systemic circulation.
Bioavailability (F)
