Pharm Exam 1 Flashcards
What term refers to an exogenous chemical agent used to modify physiology?
Drug
What term refers to the study of the use of chemical agents for therapeutic purposes?
Pharmacology
What term refers to adverse effects of a drug?
Toxicology
What term refers to a site of action/target of a drug?
Receptor
What is a drug that mimics/stimulates a biological effect called?
Agonist
What is a drug that inhibits a biological effect called?
Antagonist
What term describes what the drug does to the body?
Pharmacodynamics
What are examples of pharmacodynamics?
Therapeutic effect and toxic effect
What term describes what the body does to the drug?
Pharmacokinetics
What are examples of pharmacokinetics?
Absorption, distribution, metabolism, and elimination
What term refers to the study of how a drug acts to achieve a response by altering or modifying existing physiologic or pathologic processes?
Pharmacodynamics
Drug actions are ___________
Specific
Basic principle: drugs have _______ molecular targets/receptors in the body
Specific
What are the 5 classifications of receptors?
- Ion channel-linked receptor
- G-protein coupled receptor (GPCR)
- Receptor with intrinsic enzyme activity
- Receptor with associated enzyme activity
- Intracellular receptor
What are the 2 types of ion channel-linked receptors?
- Voltage gated ion channel
- Ionotropic (ligand-gated) ion channel
What do ion channel-linked receptors control?
Flow of ions from outside cell to inside cell
Where are ion channel-linked receptors found?
On cell surface
What determines if the ion channel is open or closed?
Whether or not the ligand is bound to the ion channel-linked receptor
What are ion-channel linked receptors made up of?
Multiple subunits
How does binding of the ligand to an ion channel-linked receptor effect the cell membrane?
The membrane either depolarizes or hyperpolarizes
What mediates the signaling of a G protein-coupled receptor (GPCR)e?
G proteins
How many times does a GPCR span the membrane?
7 times (it has 7 transmembrane domains)
What is the largest family of receptors?
GPCR
What kind of receptor is a target for 50-70% of drugs?
GPCR
What kind of receptors are GPCRs?
Metabotropic receptors
Where is a GPCR found?
Part of it is outside the cell, part of it is inside the cell
What determines the activity of a G protein?
Whether or not a diphosphate or triphosphate is bound to it
How many subunits does the G protein have?
3 (alpha, beta, gamma)
The A subunit binds to _______. It activates effectors when ________ is bound; dissociated from BY subunits
guanine; GTP
The B and Y subunits activate upon dissociation from _______ subunit. It activates effectors when ________.
alpha; free
What are the 3 possible effectors?
adenylate cyclase
PI3-kinase
protein kinase C
Have enzymatic activity that is part of the receptor itself
receptor with intrinsic enzyme activity
Have enzymatic activity that is separate from the ligand binding domain
receptor with associated enzyme activity
Which receptor has the following enzyme activities:
tyrosine kinase
tyrosine phosphate
serine/threonine kinase
guanylyl cyclase
receptor with intrinsic enzyme activity
Which receptor has the following enzyme activities:
janus kinase (JAK)
signal transducers and activators of transcription (STAT)
receptor with associated enzyme activity
For both receptors with intrinsic and associated enzyme activity, these receptors span the membrane with a ______________. The ligand binding domain is _______ the cell; the signaling domain is __________ the cell.
single stretch of amino acids
outside; inside
Where are intracellular receptors found?
inside the cell
Ligand for intracellular receptors must be _______ so it can pass through the membrane to bind to the receptor
lipophilic
Intracellular receptors mediate _____ ________
DNA transcription
Activation time of ion channel
milliseconds
Activation time of GPCR
seconds to minutes
Activation time of receptor with intrinsic and associated enzyme activity
minutes to hours
Activation time of intracellular receptor
hours to days
Get _______ affinity from multiple points of interaction
higher
Hydrophobic bonds are ________
weakest
Hydrogen bonds _______ and mediated by ______
weak; H+
Ionic bonds are most _________. They are also ______ and _______
common
intermediate, reversible
Covalent bonds are _________ and __________
strongest, irreversible
What are the results of drug binding?
- change in intracellular ions (thru ion channels)
- produce small molecules (thru GPCRs)
- protein phosphorylation (activates proteins)
- DNA transcription (intracellular receptors)
What are some small molecules that can be produced as a result of drug binding?
cAMP/cGMP
PIP2
IP3
PKC
intracellular Ca2+
Elicits max. effect
full agonist
Elicits less than max. effect (therefore less efficacious)
partial agonist
Competes with ligand (agonist) for binding to receptor
competitive antagonist
Binds to receptor with high affinity; there is no dissociation
non-competitive/irreversible antagonist
Emax = no change
EC50 = increases
competitive anatagonist
Emax = decreases
EC50 = no change
non-competitive/irreversible antagonist
Acts like an antagonist, blocks tonic activity of a receptor, and reduces basal activity of a receptor
inverse agonist
What describes the principal that not every receptor needs to be occupied to achieve maximal effect?
spare receptor theory
What describes the physiology of amplification of signal transduction pathways
spare receptor theory
Attenuated response that occurs with sustained stimulation with a drug (physiological)
tolerance
Modifications of the receptor to minimize signaling (cellular)
desensitization
Process by which the number of receptors is decreased (molecular)
downregulation
