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238 Cards in this Set
- Front
- Back
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 ___
|
-1/K_m
|
|
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 wtih ___ |
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 |
|
glycopyrrolate used for ___ (3)
|
reduce airway secretions
drooling peptic ulcers |
|
atropine effects
|
eye: pupil dilation, cycloplegia
respiratory: decreased secretions from airway stomach: decreased acid secretion gut: decreased motility bladder: decreased urgency in cystitis |
|
atropine toxicity
|
hot
dry red blind (cycloplegia) mad (disoriented) may cause acute angle-closure glaucoma, urinary retention (in BPH men or hyperthermic infants) |
|
at low doses E agonizes ___
at higher doses it agonizes ___ |
beta_1
all adrenergic receptors |
|
E is indicated for ___ (4)
|
anaphylaxis
open angle glaucoma asthma hypoTN |
|
NE agonizes ___
|
alpha_1 > alpha_2 > beta_1
|
|
NE is indicated for ___
|
hypoTN (*decreases renal perfusion)
|
|
isoproterenol agonizes ___
|
beta_1 = beta_2
|
|
isoproterenol is indicated for ___
|
evaluation of tachyarrhythmias
|
|
DA agonizes ___
|
D1 = D2 > beta adrenergic > alpha adrenergic
|
|
DA is indicated for ___ (3)
|
shock
heart failure unstable bradycardia |
|
DA's effects on the heart
|
+ inotrope
+ chronotrope at high doses |
|
dobutamine agonizes ___
|
beta_1 > beta_2 > alpha
|
|
dobutamine is indicated for ___ (3)
|
heart failure
cardiac stress testing |
|
dobutamine's effects on the heart
|
inotropic > chronotropic
|
|
phenylephrine agonizes ___
|
alpha_1 > alpha_2
|
|
phenylephrine is indicated for ___ (3)
|
pupil dilation
nasal decongestion hypotension |
|
5 beta_2-selective agonists
|
metaproterenol
albuterol salmetrol terbutaline ritodrine |
|
2 beta_2 agonists for acute asthma
|
metaproterenol
albuterol |
|
beta_2 agonist for chronic asthma tx
|
salmetrol
|
|
2 tocolytic beta_2 agonist
|
terbutaline
ritodrine |
|
3 indirect sympathomimetics
of these ___ (2) are secretagogues |
amphetamine
ephedrine cocaine amphetamine ephedrine |
|
3 amphetamine indications
|
narcolepsy
obesity ADD |
|
3 ephedrine indications
|
nasal decongestion
urinary incontinence hypoTN |
|
what drug should you avoid prescribing in patients with cocaine intoxication?
|
beta blockers because of the unopposed alpha 1 activation leading to extreme hypertension
|
|
2 alpha_2 agonists
|
clonidine
alpha-methyldope |
|
alpha_2 agonists are indicated for ___ with ___
|
HTN
renal disease |
|
2 non-selective alpha blockers
___ is reversible blocker |
phenoxybenzamine
phentolamine phentolamine |
|
non-selective alpha blockers are used for ___ in context of ___
phentolamine is used for ___ phenoxybenzamine is used for ___ |
HTN
pheochromocytoma hypertensive crisis chronic (& preop) management |
|
alpha_1 selective blockers end in ___
|
zosin
|
|
alpha_1 blockers are indicated for
|
HTN
urinary retention from BPH |
|
3 alpha_1 SEs
|
1st dose orthostatic hypoHTN
dizziness H/A |
|
alpha_2 selective blocker
|
mirtazapine
|
|
mirtazapine is indicated for ___
|
depression
|
|
3 mirtazapine SEs
|
sedation
hyperlipidemia hyperphagia |
|
SBP effects of low dose E are via ___ R
low dose E ___s SBPDBP effects of low dose E are via ___ R low dose E ___s DBP low dose E does ___ to MAP |
beta_1
raises beta_2 lowers no change |
|
SBP effects of NE are via ___ R
E ___s SBPDBP effects of E are via ___ R E ___s DBP E does ___ to MAP |
beta_1
raises alpha_1 raises raises |
|
SBP effects of isoproterenol are via ___ R
E ___s SBPDBP effects of E are via ___ R E ___s DBP E does ___ to MAP |
beta_1
transient raise, then lower beta_2 lowers lowers |
|
administering a mixed adrenergic agonist such as ___ after alpha blocker causes ___, whereas administering an alpha agonist such as ___ after alpha block causes ___
|
E
depressor effect phenylephrine no effect |
|
beta blockers do ___ to BP
mechanism is ___ |
reduce
reduced renin release (JGA beta adrenoceptors) |
|
2 beta blockers for SVT
|
propranolol
esmolol |
|
sexual SE of beta blocker
|
impotence
|
|
acebutolol is ___-selective beta blocker
|
beta_1
|
|
atenolol is ___-selective beta blocker
|
beta_1
|
|
betaxolol is ___-selective beta blocker
|
beta_1
|
|
esmolol is ___-selective beta blocker
|
beta_1
|
|
labetalol is ___-selective beta blocker
|
non
|
|
metoprolol is ___-selective beta blocker
|
beta_1
|
|
nadolol is ___-selective beta blocker
|
non
|
|
pindolol is ___-selective beta blocker
|
non
|
|
propranolol is ___-selective beta blocker
|
non
|
|
timolol is ___-selective beta blocker
|
non
|
|
2 non-selectve alpha + beta blockers
|
carvedilol
labetalol |
|
2 partial beta agonists
|
pindolol
acebutolol |
|
tx for acetaminophen poisoning
|
N-acetyl cysteine
|
|
tx for salicylate poisoning (2)
|
bicarbonate
dialysis |
|
purpose of bicarbonate in salicylate poisoning
|
alkalinize urine
|
|
tx for amphetamine poisoning
|
ammonium chloride
|
|
purpose of ammonium chloride in amphetamine poisoning
|
acidify urine
|
|
tx for anticholinesterase poisoning (2)
|
atropine
pralidoxime |
|
tx for antimuscarinic toxicity
|
physiostigmine salicylate
|
|
tx for beta blocker toxicity
|
glucagon
|
|
tx for digitalis toxicity (5)
|
stop digitalis
normalize K+ lidocaine anti-dig Fab Mg2+ |
|
tx for Fe toxicity
|
desferoxamine
|
|
tx for Pb toxicity (4)
|
CaEDTA
dimercaprol succimer penicillamine |
|
tx for As/Au/Pb toxicity (4)
|
dimercaprol
succimer penicillamine CaEDTA |
|
tx for Cu toxicity
|
penicillamine
|
|
tx for CN- toxicity (3)
|
nitrite
hydroxocobalamin thiosulfate |
|
tx for methemoglobinemia (2)
|
methylene blue
vitamin C |
|
tx for CO toxicity (2)
|
100% O2
hyperbaric O2 |
|
tx for MeOH/ethylene glycol toxicity (3)
|
ethanol
dialysis fomepizole |
|
tx for opioid toxicity
|
naloxone
|
|
tx for benzo toxicity
|
flumazenil
|
|
tx for TCA toxcity
|
bicarbonate
|
|
purpose of bicarbonate in TCA toxicity
|
alkalinize serum
|
|
tx for heparin toxicity
|
protamine
|
|
tx for warfarin toxicity (2)
|
vitamin K
FFP |
|
tx for tPA/streptokinase toxicity
|
aminocaproic acid
|
|
tx for theophylline toxicity
|
beta blocker
|
|
Fe poisoning is particularly common with ___
|
kids
|
|
Fe is cytotoxic because of ___
|
membrane lipid peroxidation
|
|
acute Fe poisoning presents with ___
|
gastric bleeding
|
|
chronic Fe poisoning presents wtih ___ (2)
|
metabolic acidosis
GI obstruction 2' to scarring |
|
drugs causing atropine-like SEs
|
TCA
|
|
2 drugs causing coronary vasospasm
|
cocaine
sumatriptan |
|
4 drugs causing flushing
|
vancomycin
adenosine niacin CCBs |
|
3 drugs which cause torsades
|
class Ia antiarrhythmics
class III antiarrhythmics cisapride |
|
6 drugs which cause agranulocytosis
|
clozapine
carbamazepine colchicine dapsone PTU methimazole |
|
5 drugs which cause aplastic anemia
|
chloramphenicol
benzene NSAIDs PTU methimazole |
|
drug causing direct coombs positive hemolytic anemia
|
alpha methyldopa
|
|
drug causing gray baby syndrome
|
chloramphenicol
|
|
drugs causing hemolysis in context of G6PD deficiency
|
INH
sulfonamides primaquine aspirin ibuprofen nitrofurantoin |
|
drugs causing megaloblastic anemia
|
pheyntoin
MTX sulfa |
|
drug causing cough
|
ACEI
|
|
3 drugs causing pulmonary fibrosis
|
bleomycin
amiodarone busulfan |
|
drug causing acute cholestatic hepatitis
|
macrolide
|
|
4 drugs causing hepatic necrosis
|
halothane
VPA acetaminophen amanita phalloides |
|
drug causing hepatitis
|
INH
|
|
2 drugs causing pseudomembranous colitis
|
clindamycin
ampicillin |
|
6 drugs causing gynecomastia
|
spironolactone
digitalis cimetidine alcohol ketoconazole estrogens |
|
2 drugs causing hot flashes
|
tamoxifen
clomiphene |
|
2 drugs causing hypothyroidism
|
Li
amiodarone |
|
2 drugs causing gout
|
furosemide
thiazides |
|
3 drugs causing photosensitivity
|
sulfonamides
amiodarone tetracycline |
|
8 drugs causing Stevens-Johnson syndrome
|
carbamazepine
ethosuximide lamotrigine phenobarbital phenytoin sulfa penicillin allopurinol |
|
4 drugs causing SLE-like syndrome
|
hydralazine
INH procainamide phenytoin |
|
fluoroquinolones cause ___ (3) in kids
|
tendonitis
tendon rupture cartilage damage |
|
___ causes Fanconi's syndrome
|
expired tetracycline
|
|
Fanconi's syndrome is ___ wasting of ___ (4)
|
tubular
bicarbonate AAs glucose uric acid |
|
3 drugs causing interstitial nephritis
|
methicillin
NSAIDs furosemide |
|
2 drugs causing hemorrhagic cystitis
prevent this by giving ___ |
CTX
ifosfamide mesna |
|
2 drugs which cause cinchonism
cinchonism is ___ |
quinidine
quinine |
|
cardiovascular aspects of cinchonism
|
flushing
arrhythmia |
|
4 neurological sx of cinchonism
|
tinnitus/hearing loss
blurry vision somnolence confusion |
|
2 cutaneous sx of cinchonism
|
flushing
rash |
|
2 drugs causing DI
|
Li
demeclocycline |
|
4 drugs causing PD-like syndrome
|
haloperidol
chlorpromazine metoclopramide reserpine |
|
3 drugs causing seizures
|
buproprion
imipinem/cilastatin INH |
|
drugs causing tardive dyskinesia
|
antipsychotics
|
|
4 drugs causing disulfiram-like reaction
|
metronidazole
cephalosporins (some) procarbazine 1st generation sulfonylureas |
|
disulfiram-like reaction means
mechanism is ___ |
feeling bad after EtOH
acetaldehyde dehydrogenase inhibition |
|
drug causing nephrotoxicity + neurotoxicity
|
polymixins
|
|
4 drugs causing nephrotoxicity + ototoxicity
|
aminoglycosides
vancomycin loop diuretics cisplatin |
|
9 CYP450 inducers
|
quinidine
barbiturates st. john's wort phenytoin rifampin griseofulvin carbamazepine chronic alcholism |
|
CYP450 inhibitors
|
INH
sulfonamides cimetidine erythromycin grapefruit |
|
3 drugs metabolized by alcohol dehydrogenase
|
ethylene glycol
MeOH EtOH |
|
ethylene glycol is metabolized by alcohol dehydrogenase to ___
effects are ___ (2) |
oxalic acid
acidosis nephrotoxicity |
|
MeOH is metabolized by alcohol dehydrogenase to ___ (2)
effects are ___ (2) |
formaldehyde
formic acid acidosis retinal damage |
|
EtOH is metabolized by alcohol dehydrogenase to ___
effects are ___ (3) |
acetaldehyde
nausea vomiting hypoTN |
|
___ inhibits alcohol dehydrogenase
|
fomepizole
|
|
5 non-obvious sulfa drugs
|
celecoxib
probenecid thiazides sulfonylurea sumatriptan |
|
systemic part of sulfa allergic rxn
|
fever
|
|
cutaneous part of sulfa allergic rxn (3)
|
rash
urticaria (hives) Stevens-Johnson |
|
hematologic part of sulfa allergic rxn (3)
|
HA
thrombocytopenia agranulocytosis |