First Aid Pharmacology Flashcards
K_m reflects ___
substrate affinity for enzyme (inversely)
V_max is a function of ___
enzyme concentration
low ___ means high enzyme affinity
K_m
inhibitors are studied with graph of ___ vs. ___
this is aka ___ plot (2)
1/V
1/[S]
double reciprocal
Lineweaver-Burk
x intercept of double reciprocal plot is ___
NAME?
y intercept of double reciprocal plot is ___
1/V_max
K_m is the ___ at which V is ___
substrate concentration
V_max/2
competitive/noncompetitive inhibitors do not change V_max
competitive
competitive/noncompetitive inhibitors do not change K_m
noncompetitive
efficacy change means ___ of dose response curve
vertical shift
potency change means ___ of dose response curve
horizontal shift
competitive inhibitors change ___
potency
non-competitive inhibitors change ___
efficacy
V_d in terms of plasma drug concentration
V_d = (amount of drug in body)/(plasma concentration)
drugs with low V_d distribute in ___
drugs with medium V_d distribute in ___
drugs with high V_d distribute in ___
blood
ECF or TBW
tissues
low V_d means ___ L
4–8
clearance (CL) in terms of plasma drug concentration (C_p)
CL = (rate of drug elimination)/(C_p)
CL in terms of V_d
CL = V_d x K_e
t_1/2 in terms of V_d
t_1/2 = (0.7 x V_d)/CL
loading dose in terms of V_d
LD = (C_p x V_d)/F
where F is bioavailability
maintenance dose in terms of C_p
MD = (C_p x CL)/F
zero order kinetics means
constant elimination per unit time
3 drugs with zero order kinetics
phenytoin
ethanol
aspirin
first order kinetics means
constant fraction of drug eliminated per unit time
4 weak acid drugs
treat overdose of weak acid with ___
phenobarbital MTX TCAs aspirin bicarbonate
weak base drug___
treat weak base overdose with ___
amphetamine
ammonium chloride
phase I metabolism is done by ___
its products are active/inactive
3 phase I reactions
CYP450 active reduction oxidation hydrolysis
phase II metabolism products are active/inactive,
polar/nonpolar
3 phase II reactions
inactive very polar glucuronidation acetylation sulfation
geriatric patients lose phase ___ metabolism first
I
a partial agonist has higher/lower potency and
higher/lower efficacy
than full agonist.
higher OR lower OR same
lower
therapeutic index
TI = LD_50/ED_50
where LD_50 is median toxic dose,
ED_50 is median effective dose
the first synapse in a parasympathetic pathway is ___
nicotinic
the second synapse in a parasympathetic pathway is ___
muscarinic
the first synapse in a sympathetic pathway is ___
nicotinic
the second synapse in most sympathetic pathways is ___
2 exceptions are ___
noradrenergic
sweat gland
renal vascular smooth muscle
2nd synapse in sweat gland pathway is ___
muscarinic
2nd synapse in renal vascular smooth muscle pathway is ___
D1 dopaminergic
nicotinic receptor is ___tropic
muscarinic receptor is ___tropic
iono
metabo
nicotinic receptor is a ___-gated ___ channel
ligand
Na+/K+
alpha1 adrenergic effect on eye
dilator muscle contraction
alpha_1 adrenergic receptor type
G_qPLR
alpha_1 adrenergic affect on GIT
increased sphincter contraction
alpha_2 adrenergic receptor type
alpha 2 effect on metabolism
G_iPLR
decreased insulin release
beta_1 adrenergic receptor type
G_sPLR
beta_1 adrenergic affect on kidney
increased renin release
beta_1 adrenergic affect on metabolism
increased lipolysis
beta_2 adrenergic affect on vessels
vasodilation
both beta_1 and beta_2 affect the heart but ___ is stronger
only ___ affects the lungs, causing ___
beta_1
beta_2
bronchodilation
beta_2 adrenergic affect on metabolism (3)
increased lipolysis
increased glycogenolysis
increased insulin release
beta_2 adrenergic affect on eye
increased aqueous humor production
M1 muscarinic receptor is ___
M2 muscarinic receptor is ___
M3 muscarinic receptor is ___
G_qPLR
G_iPLR
G_qPLR
M2Rs are expressed by ___ and do ___
cardiomyocytes
negative inotropism and chronotropism
M3Rs do ___ to exocrine glands
increase secretion
M3Rs do ___ to GIT smooth muscle
increase peristalsis
M3Rs do ___ to lungs
bronchoconstriction
M3Rs do ___ (2) to eye
pupillary sphincter contraction (miosis)
ciliary muscle contraction (accomodation)
M3Rs do ___ to bladder
detrusor contraction
D1Rs are ___
they do ___
G_sPLR
renal vascular smooth muscle relaxation
D2Rs are ___
they do ___
G_iPLR
neurotransmitter modulation
histamine H1Rs are ___
G_qPLR
H1Rs do ___ (4)
RT mucus secretion
bronchoconstriction
itching
pain
histamine H2Rs are ___
they do ___
G_sPLR
gastric acid secretion
ADH V1Rs are ___
they do ___
G_qPLR
vasoconstriction
ADH V2Rs are ___
they do ___
G_sPLR
H2O reabsorption in collecting duct
Y is converted to ___ by ___.
this is blocked by ___, which works as a ___
DOPA
Y hydroxylase
metyrosine
antihypertensive
DOPA is converted to ___ by ___.
cofactor is ___
DA
DOPA decarboxylase (AAADC)
B6
DA is imported to vesicles by ___.
this is blocked by ___
VMAT (vesicular monoamine transporter)
reserpine
DA is converted to ___ by ___.
cofactor is ___
NE
DBH (DA beta hydroxylase)
vitamin C
In ___, NE is converted to ___ by ___, in the ___.
___ is required
adrenal medulla E PNMT (phenylethanolamine N-methyl transferase) cytoplasm SAM
After MAO-COMT in either order, DA becomes ___
HVA (homovanillic acid)
After MAO-COMT in either order, E becomes ___ and NE becomes ___
both become MHPG (methoxyhydroxyphenylglycol)
After COMT, E becomes ___ and NE becomes ___.
metanephrine
normetanephrine
adrenal pheochromocytomas make more ___ than ___, but other ones do the opposite
E
NE
catecholamine exocytosis is potentiated by ___ (2) and inhibited by ___
amphetamine
ephedrine
guanethidine
___ (3) blocks catecholamine reuptake
cocaine
amphetamine
TCAs
2 presynaptic receptors which inhibit catecholamine release
alpha_2
M2
1 presynaptic receptor which facilitates catecholamine release
AII (angiotensin)
rate limiting step of cholinergic neurotransmission is ___
this is inhibited by ___
Ch uptake
hemicholinium
ACh is synthesized by ___ from ___ and ___
choline acetyltransferase (ChAT)
choline
Ac CoA
uptake of ACh into vesicule is inhibited by ___
vesicular exocytosis is inhibited by ___
vesamicol
botulinum
direct cholinomimetic for GI motility
bethanechol
2 indications for bethanechol
ileus (post op, neurogenic)
urinary retention
b/c it activates bladder and bowel
2 direct cholinomimetics for glaucoma
pilocarpine
carbachol
pilocarpine causes contraction of ___ (2)
and secretion of ___ (3)
pupillary sphincter ciliary body saliva sweat tears
contraction of ___ helps open angle glaucoma
contraction of ___ helps closed angle glaucoma
ciliary body
sphincter pupillae
direct cholinomimetic for testing asthma
methacholine
indirect cholinomimetics are ___s
AChEI
indirect cholinomimetic for GI motility
neostigmine
neostigmine has high/low CNS penetration
low
4 neostigmine indications
ileus (post op, neurogenic)
urinary retention
MG
post op NMJ block reversal
cholinomimetic for MG dx
edrophonium
cholinomimetic for MG tx
pyridostigmine
2 indirect cholinomimetics for glaucoma
echothiophate
physiostigmine
pyridostigmine has high/low CNS penetration
physiostigmine has high/low CNS penetration
echothiophate has high/low CNS penetration
low
high
low
cholinergic intoxication causes CNS ___
and skeletal muscle ___
excitation
excitation
2 antidotes for cholinergic intoxication
atropine
pralidoxime
pralidoxime functions in cholinergic intoxication by ___
regenerating active ChE
antimuscarinic for eye
atropine
homatropine
tropicamide
atropine causes ___ (2)
mydriasis
cycloplegia
cycloplegia means ___
inability to accomodate
antimuscarinic for Parkinson’s disease
benztropine
antimuscarinic for motion sickness
scopolamine
2 antimuscarinic for asthma and COPD
ipratropium
tiotropium
2 antimuscarinics for bladder spasticity
oxybutynin
darifenacin
solifenacin