Dental Pharmacology Exam 1 Flashcards
xenobiotics
chemicals not synthesized in the body
pharmacodynamics =
Pharmacokinetics =
what the drug does to the body
what the body does to the drug
pharmacovigilance =
pharmacogenenics =
the safetly of the drug
variations in response due to genetic differences
examples of drugs that do not follow the receptor method of action
antacids
osmotic diuretics
most drug/receptor bonds are (weak or strong) and are classified as ______ type.
weak
van der waals
name 6 receptor types
transmembrane ion channel transmembrane G protein transmembrane enzymatic cytosolic domains intracellular adhesion extracellular enzyme
explain the nicotinic Ach receptor
- ligand gated ion channel
- the ligand binds to the channel
- allows permeability to Na
G protein activation steps (4)
- Agonist binds
- GTP attaches to Alpha unit, displacing GDP
- alpha-GTP diffuses to the effector
- effector activation
activating adenyl cyclase is (inhibitory or stimulatory)?
stimulatory
major G proteins and their actions (5)
- G(s) = stimulatory = activates adenyl cyclase
- G(I) = inhibitory = inhibits adenyl cyclase
- G(0) = inhibits Ca channes
- G(q) = activates phospholipase C
- G(12/13) = ion transport interactions
Adenyl cyclase reaction
ATP —–[adenyl cylase]——> cAMP——>PKA———> Protein phosphorylation
Phospholipase C reaction
PIP3——-[PLC]——–> DAG + IP3
DAG——–> PKC——–> protein phosphorylation
IP3———-> Ca————> protein phosphorylation
Intracellular receptor example = ______
important characteristics to know about the ligand
steroid hormone, thyroid hormone
- lipohillic
- binds a transcription
- causes changes in genome/protein translation
Ligand A increases cAMP and Ligand B decreases cAMP
Net result?
they cancel each other out
tachyphylaxis
RAPID/REPEATED administration of the SAME DOSE of a drug, resulting in REDUCED effect over time
desensitization
decreased ability of a receptor to respond to stimulation
homologous desensitization vs. heterologous
homo = one receptor has decreased response
hetero = 2 or more receptors have decreased response
inactivation of receptor =
refractory =
down- regulation =
inactivation = loss of ability for a receptor to respond to stimulation by drug or ligand
refractory = a period of time before the next drug/receptor interaction can produce an effect
down-regulation = less receptors available due to persistent drug-receptor interaction
describe down regulation of a receptor
- LESS receptors available due to CHRONIC drug interaction
- the receptor is INTERNALIZED in the cell and SEQUESTERED or DEGRADED
Kd =
K(off)/K(on)
affinity and Kd relationship
inc Kd
dec affinity
Drug A: 3 mg binds 50% of ther receptors
Drug B: 1 mg binds 50% of the receptors
Which has higher affinity? Kd?
Drug B = higher affinity, lower Kd
Kd occurs at ____% binding.
50%
KNOW : graphs on Lecture 1/2 slide 32
:)
On the drug-receptor binding curve:
- 0 LR/R0 =
- 5 LR/R0 =
- 0 = 100% binding
0. 5 = 50% binding
dose-dependent response =
as you increase the dose, you increase the effect
Kd = EC50 means that
at 50% receptor/drug binding, you get 50% of the effect
- does not always occur
ED50
TD50
LD50
- effective (therapeutic) dose = 50% of the pop has a therapeutic response
- toxic dose = same but toxic response
- lethal dose = same but lethal response
which statement is correct?
- The receptor must be bound to the ligand in order for the response can occur
- The receptor may not be bound to the ligand and can till cause a response
2
“some receptors can spontaneously activate with binding of a drug”
CHECK!!!!!
antagonist (2)
- no intrinsic activity
- cause no response
Competitive antagonist binds ____ on the receptor and is (IRREVERSIBLE or REVERSIBLE)?
at the active site
reversible
Non-competitive antagonists bind _____ on the receptor and are (IRREVERSIBLE or REVERSIBLE)?
at the ACTIVE SITE or ALLOSTERICALLY
active site = irreversible
allosteric = both irreversible and reversible
full agonists have an intrinsic activity =
Pure antagonists have an intrinsic activity =
1
0
potency =
efficacy =
potency = response of a drug over a given range of concentrations
- the effective CONCENTRATION (of the agonist) leading to its high maximal effect
efficacy = effect of a drug
define intrinsic activity
maximal effect of a drug or EFFICACY