Pharmacokinetics/dynamics Flashcards
small hydrophobic molecules diffuse across plasma membranes
Co2, O2
specific protein that is the site of binding
receptor
a compound that is specific for reach receptor and activates it
ligand
molecules neutral in charge
non-polar
molecule with partial negative and positive charge
polar
strongest bond strength
covalent
weakest bond strength
van der waals
receptor most prevalent in the body
G-protein
name the four receptor types
ion channel, g-protein, intrinsic enzyme, intracellular
ligand-gated ion channel examples
nicotinic, glutamate, GABA-A, glycine
play an important role in muscle contraction and propagation of action potential
voltage-gated
contains the alpha, beta, and gamma subunits
g-protein
second messenger actions are
tissue specific
long term treatment with agonist leads to
desensetization
long term treatment with antagonist leads to
hypersensitization
located in the CNS and peripheral tissues, and responsible for fight or flight response
adrenergic receptors
located in vascular smooth muscle and post-synaptic CNS
alpha 1
both pre and post synaptic, in pancreatic islet cells, platelets, and nerve terminals
alpha 2
post synaptic activation of alpha 2 receptors leads to
vasoconstriction and platelet aggregation
pre synaptic alpha 2 receptors
inhibit norepi release
activation of this receptor increases cAMP
beta
increases cAMP leading to vasodilation
D1, D5
decreases cAMP leading to vasoconstriction
D2, D3, D4
two main cholinergic receptors
nicontinic and muscarinic
ligand gated cholinergic receptor
nicontinic
g protein coupled cholinergic receptor
muscarinic
Nm found
post-synaptic skeletal neuromuscular
Nn found
autonomic ganglia postganglonic
acetylcholine opens sodiuma and potassium ion channels
cholinergic
M2 located
cns, heart, smooth muscle, autonomic nerve terminals
Gaba a receptor family
ligand gated
gaba a ion
chloride
gaba a located in
CNS
gaba b located in
peripheral tissues
gaba b receptor family
g protein
both gaba receptor subtypes cause inhibition
post-synaptically
gaba a meds
benzos, barbs
gaba b meds
baclofen
gaba chloride activation leads to
CNS depression
all serotonin receptors are g-protein receptors except
5HT3- ligand gated
serotonin ions
sodium and potassium
zofran receptor family
serononin
which histamine receptors are clinically pertinent
h1 h2
histamine receptor family
g protein
h1 location
CNS
cause hives, bronchoconstriction, vasodilation
h1
located in parietal cells of the stomach
h2
regulates acid production
h2
causes muscle relaxation
h2
vasopressin receptor family
g protein
causes vasodilation in pulmonary circulation
v1
increase in calcium leads to vasoconstriction
v1
v2 MOA
increase cAMP leads to water reabsorption, causes regulation of plasma volume, inducing the release of von-willebrand factor and factor vii
found in the pituitary gland, involved in acth release and body temperature regulation
v3
activation leads to dysphoria
kappa
cyp2d6 rapid metabolizers experience
high morphine levels and toxicity
most abundant cytochrome
3a4
