Chapter 1 - Pharmacology Basic Principles Flashcards
A drug that binds to the receptor, activates it, and causes a cellular response; elicits a response from the receptor
An agonist
A drug that will bind to the receptor but inhibit its activation, preventing a cellular response; blocks endogenous ligand from activating receptor
An antagonist
A drug that binds to the active site
Orthosteric
A drug that does not bind to the active site, but still binds to the receptor
Allosteric
ADME
Absorption, distribution, metabolism, excretion
Are allosteric agonists/inhibitors competitive or non-competitive?
non-competitive
What does it mean when an agonist is “non-competitive”?
It cannot be overcome by a drug binding to the active site to achieve the desired result
What does it mean when an agonist is “competitive”?
The agonist and inhibitor will bind to the same active site
Can a competitive agonist/inhibitor be “overcome”? Why?
Yes because the agonist and inhibitor are both orthosteric and bind at the active site on the receptor
When can an orthosteric antagonist be non-competitive with an agonist?
When the antagonist forms a bond, such as a covalent bond, with the active site on the receptor
Full agonists vs. partial agonists
Partial agonists bind with less affinity; partial agonists act as antagonists in the presence of agonists. In the absence of agonists, partial agonists produce small agonistic effects.
Define Agonist Mimic or Indirect Agonist
bind to intracellular receptors, blocking enzymatic breakdown, thus producing an agonistic effect.
EC50
The drug concentration necessary to achieve 50% of effectiveness
Kd
The drug concentration at which half of all receptors are bound.
Low Kd = high drug/receptor affinity
Shamanism
religious, indigenous practice where shamans communicate with the spirit world in an altered state of consciousness
Animism
the belief that objects, places, and creatures all possess a distinct spiritual essence. Practiced by indigenous people
Spiritualism
belief or religious practice based on the supposed communication with the spirits of the dead, especially through mediums
Divination
a widespread cultural practice that involves using rituals or practices to gain insight into a question or situation
Imhotep
removed the practice of magic in treating disease, instead used plants and other natural substances. Egypt circa 3,000 BCE
Ayurvedic Medicine
Hindu medicine dating back thousands of years; diet, herbal medicines, exercise, meditation, breathing, physical therapy, yoga, massage, acupuncture, and panchakarma
Hippocrates
Father of western medicine
Asclepius
The God of medicine
Paracelsus
Father of Toxicology
“All things are poison, and nothing is without poison; only the dose permits something not to be poisonous
pharmacodynamics
what the drug does to the body; the study of a drug’s molecular, biochemical, and physiologic effects or actions.
pharmacogenomics
the study of how our genes affect the way we respond to medications
pharmacokinetics
what the body does to the drug; the study of how the body interacts with administered substances for the entire duration of exposure
3 main types of bonds listed in order of strength- strongest to weakest
Covalent, electrostatic, hydrophobic
Stereoisomerism
optical isomers, isomers that are “mirror images” of each other
Racemic mixture
a 50/50 mixture of stereoisomers, or “optical isomers”