Pharmacology Flashcards
Km =
[S] at 1/2 Vmax
Lineweaver Burk plot formula
1/V = (Km/Vmax)(1/[S]) + 1/Vmax
A higher Y intercept on a lineweaver Burk plot means
lower vmax
the X intercept of a lineweaver burk plot is
-1/Km. Closer to zero = lower affinity
A high Km means
low affinity
Vd =
(amount of drug in body) / (plasma concentration)
CL =
Vd * Ke
number of half lives to reach 90% steady state
3.3 (first order only)
number of half lives to reach steady state
4-5 (first order only)
T 1/2 =
0.693 Vd/CL (first order)
Loading dose =
(1/F)(Cp*Vd)
Maintenance dose =
(1/F)(CpCLtime interval)
Drugs with zero-order kinetics
PEA: phenytoin, ethanol, aspirin (at high or toxic concentrations)
These are part of sympathetic system but innervated by cholinergic fibers
adrenal medulla (nicotinic) and sweat glands (muscarinic)
these are innervated by Nn (nicotinic) nerves
parasympathetic ganglia, adrenal medulla
these are innervated by Nm (nicotinic) nerves
NMJ
alpha 1 (G, function)
Gq. vascular contraction, close bladder, close GI sphincters, dilate eyes
alpha 2 (G, function)
Gi. reduced symp outflow, decrease insulin, decrease lipolysis, decrease aqueous humor production, increase platelet aggregation
beta 1 (G, function)
Gs. stimulate heart, renin, lipolysis
beta 2 (G, function)
Gs. vasodilate, bronchodilate, increase lipolysis and insulin release, increase aqueous humor, decrease uterine tone, relax ciliary muscle
beta 3 (G, function)
Gs. lipolysis, thermogenesis in SKM
M1 (G, function)
Gq. CNS, enteric
M2 (G, function)
Gi. antagonize heart
M3 (G, function)
Gq. exocrine glands/gut, contract bladder, bronchoconstriction, constrict eyes, contract ciliar muscle (accomodation)
D1 (G, function)
Gs. relax renal vasculature
D2 (G, function)
Gi. neurotransmitters
H1 (G, function)
Gq. mucus, permeability, bronchoconstriction, pruritus, pain
H2 (G, function)
Gs. gastric acid secretion
V1 (G, function)
Gq. vascular smooth muscle contraction
V2 (G, function)
Gs. increases H2O permeability in collecting tubules of kidney. “V2 found in the 2 kidneys”
Gq acts via this/these pathway(s)
Phospholipase C –> DAG and IP3
DAG –> protein kinase C
IP3 increases intracellular calcium
these GPCRs use Gq
H1, A1, V1, M1, M3 (HAVe1 M&M)
these GPCRs use Gi
M2, A2, D2 (MAD 2s)
Gs/i act via this/these pathway(s)
stimulate or inhibit adenylyl cyclase.
Adenylyl cyclase increases cAMP —> protein kinase A –> heart contraction, but muscle relaxation elsewhere
this drug blocks choline entry
hemicholinium
this drug blocks ACh incorporation into vesicles
vesamicol
this drug blocks ACh vesicle fusion/NT release
botulinum
this drug blocks tyrosine conversion to DOPA
metyrosine
this drug blocks dopamine incorporation into vesicles
reserpine
this drug prevents nore release
bretylium or guanethidine
this drug displaces NE in vesicles and reverses the NET transporter
amphetamines
indirect choline agonists used for Alzheimer disease
donepezil, galantamine, rivastigmine
this is a tertiary amine anticholinergic that crosses the BBB
pysostigmine
antispasmodics for IBS
hyoscyamine, dicyclomine (anti-muscarinic)
class of drugs for oxybutynin, solifenacin, tolterodine
muscarinic antagonists
tropicamide is similar to
atropine
albuterol, salmeterol specificity
B2 > B1
dobutamine specificity
B1 > B2, a
dopamine specificity
D1 = D2 > B > a
epi specificity
B > a
nore specificity
a1 > a2 > B1
fenoldopam specificity
D1
Isoproteronol specificity
B1 = B2
midodrine specificity
a1
phenylephrine specificity
a1 > a2
this drug increases NE release (not amphetamines)
ephedrine