Block 3 Flashcards
Where are oral drugs mostly absorbed? and why?
Upper part of small intestine because it is rich and blood and has a lot of surface area
What is the rate limiting step of absorption?
The drug dissolving
T/F: When bound to proteins, drugs are inactive
True
Potentiation
When there is drug competition and if a drug is being booted from being bound to protein, more drug is free, so more drug is able to be processed, potentially causing toxicity.
Half life
Time required for the body to clear half of the drug
Eliminate rate constant
The speed at which a drug or substance is removed from the body through various processesT
Total body clearance
Rate of drug eliminate from the body by ALL routes (renal + non-renal)
Zero-order kinetics
Elimination is constant regardless of the concentration, leading to a linear decrease in drug level over time. Graph is LINEAR.
First-order kinetics
Rate of elimination is proportional to the concentration, resulting in a constant percentage reduction per unit of time. Graph is LOGARITHMIC.
Elimination rate constant (Kel)
The speed at which a drug or substance is removed from the body the body through various processes –> gradient/slope of the curve
Half-life
Time required for the body to clear half of the drug
How many half lives before a drug is almost completely eliminated from the body?
5-6 half lives
Extraction ratio
Measure that indicates the fraction of a drug that is removed from the bloodstream by an organ while passing through
Pharmacodynamics
The study of how drugs interact with the body at a molecular and cellular level to produce their therapeutic effects
Drug action
The mechanisms by which a drug acts to produce effects in a patient
Drug effect
The tangible consequence of the drug’s action
Agonist
Substance that activates or stimulates a receptor in the body, mimicking the effects of a naturally occurring compound
Antagonist
Substance that blocks or inhibits the action of a receptor
Inverse Agonist
Substance that not only blocks the activation of a receptor but also produces an opposite or “negative” response compared to the receptor’s natural state
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A drug that acts on the same receptor as an agonist and produces an opposite effect (opposes through the same pathway)
Mixed agonist-antagonist
Substance that can act as both an agonist and an antagonist, depending on the specific receptor or tissue it interacts with (binds to more than 1 receptor)
Full agonist
Compound that binds to a receptor and activates it to its maximum potential, does NOT reach a ceiling and you can keep upping the concentration indefinitely due to there being spare receptors (can give as much of a drug as you want and keep increasing the concentration)
Partial agonist
Compound that binds to a receptor and only activates it partially, it reaches a ceiling effect
Competitive antagonist
Competes with agonists for binding to the same receptor, reducing the receptor’s activation by agonists, and its effects can be overcome by increasing agonist concentration, restoring normal receptor activity
Non-competative antagonism
The opposite of competitive antagonists, irreversible reaction and is NOT dose dependent (no matter how many agonists you give this will still work as an antagonist)
Physiological Antagonist
A drug that counters the effect of another drug by binding to a different receptor and causing an opposite effect (opposes through a different pathway)
EC50
The concentration of a drug needed to produce 50% of a response.
Most potent drug is the one with the lowest EC50
Drug specificity
How precisely a drug interacts with a particular target or receptor in the bodyD
Drug selectivity
The degree to which a drug acts on a given site as well as other sites dependent on the concentration range