First Aid Pharmacology Flashcards

(261 cards)

1
Q

K_m reflects ___

A

substrate affinity for enzyme (inversely)

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2
Q

V_max is a function of ___

A

enzyme concentration

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3
Q

low ___ means high enzyme affinity

A

K_m

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4
Q

inhibitors are studied with graph of ___ vs. ___

this is aka ___ plot (2)

A

1/V
1/[S]
double reciprocal
Lineweaver-Burk

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5
Q

x intercept of double reciprocal plot is ___

A

NAME?

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6
Q

y intercept of double reciprocal plot is ___

A

1/V_max

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7
Q

K_m is the ___ at which V is ___

A

substrate concentration

V_max/2

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8
Q

competitive/noncompetitive inhibitors do not change V_max

A

competitive

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9
Q

competitive/noncompetitive inhibitors do not change K_m

A

noncompetitive

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10
Q

efficacy change means ___ of dose response curve

A

vertical shift

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11
Q

potency change means ___ of dose response curve

A

horizontal shift

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12
Q

competitive inhibitors change ___

A

potency

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13
Q

non-competitive inhibitors change ___

A

efficacy

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14
Q

V_d in terms of plasma drug concentration

A

V_d = (amount of drug in body)/(plasma concentration)

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15
Q

drugs with low V_d distribute in ___
drugs with medium V_d distribute in ___
drugs with high V_d distribute in ___

A

blood
ECF or TBW
tissues

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16
Q

low V_d means ___ L

A

4–8

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17
Q

clearance (CL) in terms of plasma drug concentration (C_p)

A

CL = (rate of drug elimination)/(C_p)

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18
Q

CL in terms of V_d

A

CL = V_d x K_e

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19
Q

t_1/2 in terms of V_d

A

t_1/2 = (0.7 x V_d)/CL

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20
Q

loading dose in terms of V_d

A

LD = (C_p x V_d)/F

where F is bioavailability

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21
Q

maintenance dose in terms of C_p

A

MD = (C_p x CL)/F

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22
Q

zero order kinetics means

A

constant elimination per unit time

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23
Q

3 drugs with zero order kinetics

A

phenytoin
ethanol
aspirin

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24
Q

first order kinetics means

A

constant fraction of drug eliminated per unit time

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25
4 weak acid drugs | treat overdose of weak acid with ___
``` phenobarbital MTX TCAs aspirin bicarbonate ```
26
weak base drug___ | treat weak base overdose with ___
amphetamine | ammonium chloride
27
phase I metabolism is done by ___ its products are active/inactive 3 phase I reactions
``` CYP450 active reduction oxidation hydrolysis ```
28
phase II metabolism products are active/inactive, polar/nonpolar 3 phase II reactions
``` inactive very polar glucuronidation acetylation sulfation ```
29
geriatric patients lose phase ___ metabolism first
I
30
a partial agonist has higher/lower potency and higher/lower efficacy than full agonist.
higher OR lower OR same | lower
31
therapeutic index
TI = LD_50/ED_50 where LD_50 is median toxic dose, ED_50 is median effective dose
32
the first synapse in a parasympathetic pathway is ___
nicotinic
33
the second synapse in a parasympathetic pathway is ___
muscarinic
34
the first synapse in a sympathetic pathway is ___
nicotinic
35
the second synapse in most sympathetic pathways is ___ | 2 exceptions are ___
noradrenergic sweat gland renal vascular smooth muscle
36
2nd synapse in sweat gland pathway is ___
muscarinic
37
2nd synapse in renal vascular smooth muscle pathway is ___
D1 dopaminergic
38
nicotinic receptor is ___tropic | muscarinic receptor is ___tropic
iono | metabo
39
nicotinic receptor is a ___-gated ___ channel
ligand | Na+/K+
40
alpha1 adrenergic effect on eye
dilator muscle contraction
41
alpha_1 adrenergic receptor type
G_qPLR
42
alpha_1 adrenergic affect on GIT
increased sphincter contraction
43
alpha_2 adrenergic receptor type | alpha 2 effect on metabolism
G_iPLR | decreased insulin release
44
beta_1 adrenergic receptor type
G_sPLR
45
beta_1 adrenergic affect on kidney
increased renin release
46
beta_1 adrenergic affect on metabolism
increased lipolysis
47
beta_2 adrenergic affect on vessels
vasodilation
48
both beta_1 and beta_2 affect the heart but ___ is stronger | only ___ affects the lungs, causing ___
beta_1 beta_2 bronchodilation
49
beta_2 adrenergic affect on metabolism (3)
increased lipolysis increased glycogenolysis increased insulin release
50
beta_2 adrenergic affect on eye
increased aqueous humor production
51
M1 muscarinic receptor is ___ M2 muscarinic receptor is ___ M3 muscarinic receptor is ___
G_qPLR G_iPLR G_qPLR
52
M2Rs are expressed by ___ and do ___
cardiomyocytes | negative inotropism and chronotropism
53
M3Rs do ___ to exocrine glands
increase secretion
54
M3Rs do ___ to GIT smooth muscle
increase peristalsis
55
M3Rs do ___ to lungs
bronchoconstriction
56
M3Rs do ___ (2) to eye
pupillary sphincter contraction (miosis) | ciliary muscle contraction (accomodation)
57
M3Rs do ___ to bladder
detrusor contraction
58
D1Rs are ___ | they do ___
G_sPLR | renal vascular smooth muscle relaxation
59
D2Rs are ___ | they do ___
G_iPLR | neurotransmitter modulation
60
histamine H1Rs are ___
G_qPLR
61
H1Rs do ___ (4)
RT mucus secretion bronchoconstriction itching pain
62
histamine H2Rs are ___ | they do ___
G_sPLR | gastric acid secretion
63
ADH V1Rs are ___ | they do ___
G_qPLR | vasoconstriction
64
ADH V2Rs are ___ | they do ___
G_sPLR | H2O reabsorption in collecting duct
65
Y is converted to ___ by ___. | this is blocked by ___, which works as a ___
DOPA Y hydroxylase metyrosine antihypertensive
66
DOPA is converted to ___ by ___. | cofactor is ___
DA DOPA decarboxylase (AAADC) B6
67
DA is imported to vesicles by ___. | this is blocked by ___
VMAT (vesicular monoamine transporter) | reserpine
68
DA is converted to ___ by ___. | cofactor is ___
NE DBH (DA beta hydroxylase) vitamin C
69
In ___, NE is converted to ___ by ___, in the ___. | ___ is required
``` adrenal medulla E PNMT (phenylethanolamine N-methyl transferase) cytoplasm SAM ```
70
After MAO-COMT in either order, DA becomes ___
HVA (homovanillic acid)
71
After MAO-COMT in either order, E becomes ___ and NE becomes ___
both become MHPG (methoxyhydroxyphenylglycol)
72
After COMT, E becomes ___ and NE becomes ___.
metanephrine | normetanephrine
73
adrenal pheochromocytomas make more ___ than ___, but other ones do the opposite
E | NE
74
catecholamine exocytosis is potentiated by ___ (2) and inhibited by ___
amphetamine ephedrine guanethidine
75
___ (3) blocks catecholamine reuptake
cocaine amphetamine TCAs
76
2 presynaptic receptors which inhibit catecholamine release
alpha_2 | M2
77
1 presynaptic receptor which facilitates catecholamine release
AII (angiotensin)
78
rate limiting step of cholinergic neurotransmission is ___ | this is inhibited by ___
Ch uptake | hemicholinium
79
ACh is synthesized by ___ from ___ and ___
choline acetyltransferase (ChAT) choline Ac CoA
80
uptake of ACh into vesicule is inhibited by ___ | vesicular exocytosis is inhibited by ___
vesamicol | botulinum
81
direct cholinomimetic for GI motility
bethanechol
82
2 indications for bethanechol
ileus (post op, neurogenic) urinary retention b/c it activates bladder and bowel
83
2 direct cholinomimetics for glaucoma
pilocarpine | carbachol
84
pilocarpine causes contraction of ___ (2) | and secretion of ___ (3)
``` pupillary sphincter ciliary body saliva sweat tears ```
85
contraction of ___ helps open angle glaucoma | contraction of ___ helps closed angle glaucoma
ciliary body | sphincter pupillae
86
direct cholinomimetic for testing asthma
methacholine
87
indirect cholinomimetics are ___s
AChEI
88
indirect cholinomimetic for GI motility
neostigmine
89
neostigmine has high/low CNS penetration
low
90
4 neostigmine indications
ileus (post op, neurogenic) urinary retention MG post op NMJ block reversal
91
cholinomimetic for MG dx
edrophonium
92
cholinomimetic for MG tx
pyridostigmine
93
2 indirect cholinomimetics for glaucoma
echothiophate | physiostigmine
94
pyridostigmine has high/low CNS penetration physiostigmine has high/low CNS penetration echothiophate has high/low CNS penetration
low high low
95
cholinergic intoxication causes CNS ___ | and skeletal muscle ___
excitation | excitation
96
2 antidotes for cholinergic intoxication
atropine | pralidoxime
97
pralidoxime functions in cholinergic intoxication by ___
regenerating active ChE
98
antimuscarinic for eye
atropine homatropine tropicamide
99
atropine causes ___ (2)
mydriasis | cycloplegia
100
cycloplegia means ___
inability to accomodate
101
antimuscarinic for Parkinson's disease
benztropine
102
antimuscarinic for motion sickness
scopolamine
103
2 antimuscarinic for asthma and COPD
ipratropium | tiotropium
104
2 antimuscarinics for bladder spasticity
oxybutynin darifenacin solifenacin
105
glycopyrrolate used for ___ (3)
reduce airway secretions drooling peptic ulcers
106
atropine effects
eye: pupil dilation, cycloplegia respiratory: decreased secretions from airway stomach: decreased acid secretion gut: decreased motility bladder: decreased urgency in cystitis
107
atropine toxicity
``` hot dry red blind (cycloplegia) mad (disoriented) ``` may cause acute angle-closure glaucoma, urinary retention (in BPH men or hyperthermic infants)
108
at low doses E agonizes ___ | at higher doses it agonizes ___
beta_1 | all adrenergic receptors
109
E is indicated for ___ (4)
anaphylaxis open angle glaucoma asthma hypoTN
110
NE agonizes ___
alpha_1 > alpha_2 > beta_1
111
NE is indicated for ___
hypoTN (*decreases renal perfusion)
112
isoproterenol agonizes ___
beta_1 = beta_2
113
isoproterenol is indicated for ___
evaluation of tachyarrhythmias
114
DA agonizes ___
D1 = D2 > beta adrenergic > alpha adrenergic
115
DA is indicated for ___ (3)
shock heart failure unstable bradycardia
116
DA's effects on the heart
+ inotrope + chronotrope at high doses
117
dobutamine agonizes ___
beta_1 > beta_2 > alpha
118
dobutamine is indicated for ___ (3)
heart failure | cardiac stress testing
119
dobutamine's effects on the heart
inotropic > chronotropic
120
phenylephrine agonizes ___
alpha_1 > alpha_2
121
phenylephrine is indicated for ___ (3)
pupil dilation nasal decongestion hypotension
122
5 beta_2-selective agonists
``` metaproterenol albuterol salmetrol terbutaline ritodrine ```
123
2 beta_2 agonists for acute asthma
metaproterenol | albuterol
124
beta_2 agonist for chronic asthma tx
salmetrol
125
2 tocolytic beta_2 agonist
terbutaline | ritodrine
126
3 indirect sympathomimetics | of these ___ (2) are secretagogues
amphetamine ephedrine cocaine amphetamine ephedrine
127
3 amphetamine indications
narcolepsy obesity ADD
128
3 ephedrine indications
nasal decongestion urinary incontinence hypoTN
129
what drug should you avoid prescribing in patients with cocaine intoxication?
beta blockers because of the unopposed alpha 1 activation leading to extreme hypertension
130
2 alpha_2 agonists
clonidine | alpha-methyldope
131
applications of clonidine
Hypertensive urgency, ADHD, severe pain, ethanol and opioid withdrawal
132
Toxicity of clonidine
CNS depression, bradycardia, hypotension, respiratory depression, small pupil size
133
applications of alpha-methyl dopa
hypertension in pregnancy
134
Toxicity of alpha-methyl dopa
direct Coombs+ hemolytic anemia, SLE like syndrome
135
2 non-selective alpha blockers | ___ is reversible blocker
phenoxybenzamine phentolamine phentolamine
136
Phenoxybenzamine and phentolamine are (reversible/irreversible)?
phenoxybenzamine: irreversible; phentolamine: reversible
137
applications of phenoxybenzamine
pheo to prevent hypertensive crisis from too much catecholamines
138
toxicity of phenoxybenzamine
orthostatic hypotension, reflex tachycardia
139
applications of phenotolamine?
pts on MAO inhibitors that ate too much tyrosine
140
applications of a1 selective blockers
urinary Sxs of BPH, PTSD (prazosin), HTN (except tamsulosin)
141
Toxicity of a1 selective blockers
1st dose orthostatic hypoHTN dizziness H/A
142
alpha_1 selective blockers end in ___
zosin
143
alpha_2 selective blocker
mirtazapine
144
mirtazapine is indicated for ___
depression
145
3 mirtazapine SEs
sedation increased cholesterol increased appetite
146
what are the appliations of beta blockers?
angina pectoris, MI, SVT, HTN, CHF, Glaucoma
147
how do beta blockers effect angina pectoris?
decreases heart rate and contractility, resulting in decreased O2 consumption
148
which beta blockers decrease mortality in Mis?
metoprolol, carvedilol, bisoprolol
149
which beta blockers are used in SVT
metoprolol, esmolol
150
how do beta blockers effect SVT?
they decrease AV conduction velocity
151
how do beta blockers effect HTN?
decrease CO, decrease renin secretion by B1 block in JGA cells
152
How do beta blockers effect CHF?
slows progression
153
Which beta blocker effects glaucoma and how?
timolol by decreasing secretion of aqueous humor
154
what are the toxic effects of beta blockers?
impotence; CV adverse effects: bradycardia, AV block, CHF; CNS effects: seizures, sedation, sleep alterations; dyslipidemia (metoprolol), asthma or COPD exacerbation
155
acebutolol is ___-selective beta blocker
beta_1 (partial agonist)
156
atenolol is ___-selective beta blocker
beta_1
157
betaxolol is ___-selective beta blocker
beta_1
158
esmolol is ___-selective beta blocker
beta_1
159
labetalol is ___-selective beta blocker
non, also nonselective alpha
160
metoprolol is ___-selective beta blocker
beta_1
161
nadolol is ___-selective beta blocker
non
162
pindolol is ___-selective beta blocker
non (partial agonist)
163
propranolol is ___-selective beta blocker
non
164
timolol is ___-selective beta blocker
non
165
2 non-selectve alpha + beta blockers
carvedilol | labetalol
166
2 partial beta agonists
pindolol | acebutolol
167
what is nebivolol?
cardiac selective B1 adrenergic blockade with stimulation of beta 3 receptors leading to activation of NOS in vasculature
168
tx for acetaminophen poisoning
N-acetyl cysteine
169
tx for salicylate poisoning (2)
bicarbonate | dialysis
170
purpose of bicarbonate in salicylate poisoning
alkalinize urine
171
tx for amphetamine poisoning
ammonium chloride
172
purpose of ammonium chloride in amphetamine poisoning
acidify urine
173
tx for anticholinesterase poisoning (2)
atropine | pralidoxime
174
tx for antimuscarinic toxicity
physiostigmine salicylate and control HTN
175
tx for beta blocker toxicity
glucagon
176
tx for digitalis toxicity (5)
anti-dig Fab
177
tx for Fe toxicity
desferoxamine, deferasirox
178
tx for Pb toxicity (4)
CaEDTA dimercaprol succimer penicillamine
179
tx for Hg/As/Au toxicity
dimercaprol (BAL), succimer
180
tx for Cu/As/Au toxicity
penicillamine
181
tx for CN- toxicity (3)
nitrite hydroxocobalamin thiosulfate
182
tx for methemoglobinemia (2)
methylene blue | vitamin C
183
tx for CO toxicity (2)
100% O2 | hyperbaric O2
184
tx for MeOH/ethylene glycol toxicity (3)
fomepizole> ethanol | dialysis
185
tx for opioid toxicity
naloxone
186
tx for benzo toxicity
flumazenil
187
tx for TCA toxcity
bicarbonate
188
purpose of bicarbonate in TCA toxicity
alkalinize serum
189
tx for heparin toxicity
protamine sulfate
190
tx for warfarin toxicity (2)
vitamin K | plasma (if active bleeding)
191
tx for tPA/streptokinase toxicity
aminocaproic acid
192
tx for theophylline toxicity
beta blocker
193
Fe poisoning is particularly common with ___
kids
194
Fe is cytotoxic because of ___
membrane lipid peroxidation
195
acute Fe poisoning presents with ___
gastric bleeding
196
chronic Fe poisoning presents wtih ___ (2)
metabolic acidosis | GI obstruction 2' to scarring
197
drugs causing atropine-like SEs
TCA
198
drugs causing coronary vasospasm
cocaine | sumatriptan, ergot alkaloids
199
drugs causing flushing
vancomycin adenosine niacin Ca2+ channel blockers
200
drugs causing dilated cardiomyopathy
doxorubicin, daunorubicin
201
drugs which cause torsades
``` class Ia antiarrhythmics (quinidine) class III antiarrhythmics (sotalol) antiarrhythmics, macrolides, antipsychotics, TCAs ```
202
drugs which cause agranulocytosis
``` clozapine carbamazepine colchicine dapsone PTU methimazole ```
203
drugs which cause aplastic anemia
``` chloramphenicol , carbamazepine benzene NSAIDs PTU methimazole ```
204
drug causing direct coombs positive hemolytic anemia
alpha methyldopa, penicilin
205
drug causing gray baby syndrome
chloramphenicol
206
drugs causing hemolysis in context of G6PD deficiency
``` INH sulfonamides , dapsone primaquine aspirin ibuprofen nitrofurantoin ```
207
drugs causing megaloblastic anemia
pheyntoin MTX sulfa
208
drugs causing thrombocytopenia
heparin, cimetidine
209
thromboti complications
OCPs
210
drug causing cough
ACEI
211
drugs causing pulmonary fibrosis
bleomycin , methotrexate amiodarone busulfan
212
drug causing acute cholestatic hepatitis, jaundice
macrolide - erythromycin
213
drugs causing diarrhea
metformin, erythromycin, colchicine, orlistat, acarbose
214
drugs causing hepatic necrosis
halothane Valproic acid acetaminophen amanita phalloides
215
drugs causing pancreatitis
didanosine, corticosteroids, alcohol, valproic acid, azathioprine, diuretics (furosemide, HCTZ)
216
drug causing hepatitis
INH
217
drugs causing pseudomembranous colitis
clindamycin | ampicillin, cephalosporins
218
drugs causing gynecomastia
``` spironolactone digitalis cimetidine alcohol ketoconazole estrogens ```
219
drugs causing hot flashes
tamoxifen | clomiphene
220
drugs causing adrenocortical insufficiency
glucocorticoid withdrawal leads to HPA suppression
221
drugs causing hypothyroidism
Li | amiodarone, sulfonamides
222
drugs causing gout
furosemide , cyclosporine | thiazides, pyrizinamide, niacin
223
drugs causing photosensitivity
sulfonamides amiodarone tetracycline, 5FU
224
drugs causing Stevens-Johnson syndrome
``` anti-epileptic drugs (carbamazepine ethosuximide lamotrigine phenobarbital phenytoin ) sulfa penicillin allopurinol ```
225
drugs causing SLE-like syndrome
Sulfa, hydralazine INH procainamide phenytoin, etanercept
226
drugs causing teeth discoloration
tetracyclines
227
drugs causing fat redistribution
protease inhibitors, glucocorticoids
228
drugs causing gingival hyperplasia
phenytoin, verapamil, cyclosporine, nifedipine
229
drugs causing myopathy
fibrates, niacine, colchicine, hydroxychloroquine, interferon-alpha, penicillamine, statins, glucocorticoids
230
drugs causing osteoporosis
corticosteroids, heparin
231
drugs causing cinchonism
quinidine, quinine
232
drugs causing parkinson-like syndrome
antipsychotics, reserpine, metoclopramide
233
drugs causing seizures
INH, buproprion, imipenem/cilastatin, tramadol, enflurane, metoclopramide
234
drugs causing tardive dyskinesia
antipsychotics, metoclopramide
235
fluoroquinolones cause ___ (3) in kids
tendonitis tendon rupture cartilage damage
236
___ causes Fanconi's syndrome
expired tetracycline
237
Fanconi's syndrome is ___ wasting of ___ (4)
``` tubular bicarbonate AAs glucose uric acid ```
238
3 drugs causing interstitial nephritis
methicillin NSAIDs furosemide
239
drugs causing hemorrhagic cystitis | prevent this by giving ___
Cyclophosphamide ifosfamide mesna
240
cardiovascular aspects of cinchonism
flushing | arrhythmia
241
4 neurological sx of cinchonism
tinnitus/hearing loss blurry vision somnolence confusion
242
2 cutaneous sx of cinchonism
flushing | rash
243
drugs causing DI
Li | demeclocycline
244
drugs causing disulfiram-like reaction
metronidazole cephalosporins (some) , griseofulvin procarbazine 1st generation sulfonylureas
245
disulfiram-like reaction means | mechanism is ___
feeling bad after EtOH | acetaldehyde dehydrogenase inhibition
246
drug causing nephrotoxicity + neurotoxicity
polymixins
247
drugs causing nephrotoxicity + ototoxicity
aminoglycosides vancomycin loop diuretics cisplatin
248
drugs causing antimuscarinic effects?
atropine, TCAs, H1 blockers, antipsychotics
249
CYP450 inducers
chronic alcoholism, modafinil, St. John's wort, Phenytoin, Phenobarbital, nevirapine, rifampine, griseofulvin, carbamezepine
250
CYP450 substrates
antiepileptics, anti-depressants, antipsychotics, anesthetics, theophylline, warfarin, statins, OCPs
251
CYP450 inhibitors
acute alcohol abuse, gemfibrozil, ciprofloxacin, isoniazid, grapefruit juice, quinidine, amiodarone, ketoconazole, macrolides, sulfonamides, cimetidine, ritonavir
252
Sulfa drugs
probenacid, furoseide, acetazolamide, celecoxib, thiazides, sulfonamide antibiotics, sulfasalazine, sulfonylurea
253
3 drugs metabolized by alcohol dehydrogenase
ethylene glycol MeOH EtOH
254
ethylene glycol is metabolized by alcohol dehydrogenase to ___ effects are ___ (2)
oxalic acid acidosis nephrotoxicity
255
MeOH is metabolized by alcohol dehydrogenase to ___ (2) | effects are ___ (2)
formaldehyde formic acid acidosis retinal damage
256
EtOH is metabolized by alcohol dehydrogenase to ___ | effects are ___ (3)
acetaldehyde nausea vomiting hypoTN
257
___ inhibits alcohol dehydrogenase
fomepizole
258
5 non-obvious sulfa drugs
``` celecoxib probenecid thiazides sulfonylurea sumatriptan ```
259
systemic part of sulfa allergic rxn
fever
260
cutaneous part of sulfa allergic rxn (3)
rash urticaria (hives) Stevens-Johnson
261
hematologic part of sulfa allergic rxn (3)
Hemolytic anemia thrombocytopenia agranulocytosis