Week 1: Chapter 2,3,4,5,6,8,9,10 Overview ~ Ray Flashcards
Please add and edit as you see fit :) Week 1 objectives: Differentiate between pharmacodynamics and pharmacokinetics. Recall/employ main concepts of rational drug selection and cost when prescribing. Summarize special drug treatment considerations in pediatric and geriatric patients. Recall mechanisms that cause drug interactions. Recall various herbal therapies and their uses. (143 cards)
What are the stages of drug development? Could you describe each phase?
Preclinical: The drug is targeted, and ingredients are isolated. Medical chemists can create compounds and slightly adjust them to evaluate the perfect combination of properties. Studies are performed on cells, isolated tissues, and organs. Toxicology and safety testing determine the potential risk a compound poses to people and the environment.
Clinical phase I: establishes biological effects (safe dosages and pharmacokinetics) on healthy people at different doses.
Clinical Phase 2: drugs are used to treat diseases in a small number of sick patients. Outcomes are evaluated. <100 people.
Clinical Phase 3: The drug is compared with current medications in the market to evaluate outcomes—larger population group (~1000).
Explain the Dose-Response Curves
The higher the concentration of a drug at its site of action, the more the drug will bind to its receptor and the greater the response will be. With a greater number of drug molecules in the vicinity, more are likely to interact with the receptor and produce a response. Note: far fewer receptors may be needed to produce maximal effect.
IE a graph to show the concentration or dose of a drug in relation to that drugs percent of maximum response.
Explain Graded Response
Biological effects that can be measured continually up to the maximal capacity of the biological system (For example, the use of BP to monitor the effectiveness of Anti-HTNs)
Explain Quantal Response
Quantal Responses: Effects are present or absent. Examples are seizures, pregnancy, or death. NOTE:s can be both. For example, antiseizure medications can be graded by the decrease in seizures, whereas Some medicines can be quantal when there is an absence.
What is potency?
Potency is how much drug is needed to produce a biological response. Describes the difference in concentration of dosage of different drugs required to make the same effect. Higher potency requires less dose/concentration.
What is efficacy? Provide examples.
The maximal effect a drug can produce.
Example: Mild pain relief meds, such as Tylenol, cannot relieve the same pain as Oxy regardless of the dose.
What is intrinsic activity?
the ability of a drug to produce a response ONCE IT HAS OCCUPIED specific receptors.
Some drugs can occupy receptors and provide little to no response. The lower the intrinsic activity the lower efficacy the drug has.
What is Therapeutic Index (TI)? What is the formula?
It is the ratio of the lethal dose to the therapeutic dose. The higher the TI, the safer it is considered.
TI= LD50/ED50
What is Structure-Activity Relationship (SAR)
The correlation of chemical structure with pharmacological activity. Chemical interactions determine a drug’s activity at a particular receptor type, and changes in chemical structure result in changes in pharmacological activity.
What is a receptor?
Receptors are large molecules, usually proteins, that interact with and mediate the action of drugs.
Receptors provide a theoretical framework for understanding and predicting drug actions and the relationship between dose (or concentration) and effect. Also, receptors within the same “superfamily” often share properties.
What are Ion Channel Receptors?
Ion Channel receptors transmit signals across the cell membrane by increasing the flow of ions and altering the electrical potential or separation of charged ions across the membrane. Responses are rapid onset and short duration.
For example, when Acetylcholine (ACh) binds on TWO (2) nicotinic ion receptor sites, the channel opens, and Sodium and Potassium cross the cell membrane to initiate a response.
If you have pro can someone as a pic please
What types of Ion Channel Receptors are there?
ACh (nicotinic)
Gamma-aminobutyric acid (GABA)
Excitatory amino acids (glycine, aspartate, glutamate, etc.).
What are G-protein coulpled receptors? Explain the structure.
G-protein–coupled receptors are proteins that cross the cell membrane seven (7) times, creating a pocket in which drugs can interact. There is a “tail” intracellularly.
What happens when G-proteins are activated?
When a drug is attached to the binding site, the G protein undergoes a conformational change like a “twist”. The G-protein is then released. The, now-activated, G-protein can interact with effector proteins. These effector proteins then make second messengers.
How many subunits are in G-proteins? What are their names?
Alpha, Beta, Gamma.
What is Phosphorylation?
Placing a phosphate group on a protein is a way of marking it for activation or inactivation.
What is a Transmembrane Receptor?
Transmembrane receptors consist of extracellular hormone-binding domain and an intracellular enzyme domains that phosphorylates the amino acid tyrosine
How do transmembrane receptors get activated? What happens?
The hormone binds to the extracellular binding site, the receptor conformation changes, and two receptors bind to each other, activating the enzyme and sustaining the effect. Different receptors catalyze the phosphorylation of tyrosine residues on various downstream signaling proteins.
What are intracellular receptors? what happens when they are activated?
Intracellular receptor resides in the cytoplasm until it binds with a drug that has glucocorticoid activity. Binding of the drug displaces a stabilizing protein and permits the folding of the receptor into its active conformation. The receptor then moves to the nucleus, where it controls the transcription of genes by binding to specific DNA sequences
What are enzymes?
biological molecules that encourage specific chemical reactions in the body.
I think of enzymes as action tasks. Enzymes are the lock, and drug is the key.
What is full agonist
drugs that produce receptor stimulation and conformation change every time they are bonded. they do not need all the available receptors to produce maximum effect.
what are antagonists
Drugs that occupy a receptor without stimulating them and prevent other molecules from occupying the same site to produce a response.
what are the two types of antagonists (explain both)
Competitive: compete for the same binding site. Drugs can overcome antagonistic effects with higher concentrations of competing agonists.
Non-competitive: antagonist irreversibly bind somewhere else in the enzyme, changing it and making it unusable. Increasing drug does not increase effectiveness.
what are partial agonists?
Bind to receptors but when they occupy the receptor sites, they stimulate only some of the receptors. They trigger a lower maximal response than a full agonist. This is sometimes called intrinsic activity
