Caldwell
Drug receptors must be what
what form will an antagonist bind to
both active and inactive
what receptor controls thermoregulation -- is it PNS or SNS
M3
sympathetic-- only time this happens
what is the order of how catecholamines are made
is ep made throughout the body
dopamine --> NE --> Ep
only in adrenal medulla
what is the difference between acetylcholine, methacholine, and bethanechol
A: easily broken down by ACh esterase
shortest DofA
M: 3X less susceptible to being broken down
B: not susceptible
what is associated with Kd and EC50
binding-- affinity
effect -- efficacy
whats the difference between a competitive and non competitive inhibitor
can emax be reached with either one?
competitive- binds reversibly to active site-- can be overcome
noncompetitive-- binds irreversibly to active site or allosteric site-- cannot be overcome
how does mirabegron work
B3 agonist-- relaxes smooth muscle in detrusor muscle of bladder
treats overactive bladder
what are the enzymes that break down catecholamines?
what is entacapone?
MAO and COMT
COMT inhibitor
prevent breakdown of dopamine-- good drug for Parkinson's
what pesticides were shown to have a link to Parkinson's
what causes parkinsons?
rotenone and paraquat
neurons are destroyed in the substantia nigra and corpus striatum-- responsible for motor control
antacids
metamucil
both act on stomach directly
what is the difference between therapeutic window and therapeutic index
window= range of doses of a drug that gives a therapeutic response without toxicity-- determined by population data
index= drug selectivity in giving the desired vs undesired effect
ratio of TD or LD50 : ED50
want high number= safer
how does Timolol work
B1 receptor blocker
blocks NE from binding on ciliary body
decreases production of aqueous humor= decrease in intraocular pressure= treats glaucoma
what are the receptors for Gs, Gi, and Gq
Gq= A1, M1, M3, M5
Gs= B1, B2, B3, A2
Gi= M2, M4, A2
what the difference between atropine and scopolamine
atropine-- strong affinity for Muscarinic receptors- blocks ACh from binding competitively -- doesnt go into CNS
Scopolamine-- marketed as patches-- rapidly and fully distributes into CNS- greater effect than a lot of other antimuscarinics
what is an inverse agonist
binds to inactive state of receptors
decreases constitutive activity
sometimes described as antagonist
has negative efficacy
if you take an agonist all the time what will the body do to its receptors to help maintain homeostasis -- what about an antagonist
down regulate
up regulate
how does clonidine work
A2 agonist
sympathomimetic
dilates arteries= treats HTN
dampens SNS= treats ADHD
what are the four antiepileptics that we should know
Valproic Acid
Ethosuximide
Carbamazepine
Levetiracetam
atropine
what is constitutive activity and what are examples
activity of a receptor-effector system in the absence of an agonist ligand -- the equilibrium determines the degree of constitutive activity
histamines in CNS
Cancer
how can the body down regulate its receptors
turning off signals --
remove receptors
turning off genes to make receptors
what is the visceral sensory checkpoint in the medulla that signals must go through
nucleus tractus solitarius
what three drugs work in a similar way to Myrbetric? what kind of drugs are they
anticholinergics
oxybutynin, solifenacin, darifenacin
what kind of test is used for diagnosing CF
sweat test