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Flashcards in First Aid Pharmacology Deck (261)
1

K_m reflects ___

substrate affinity for enzyme (inversely)

2

V_max is a function of ___

enzyme concentration

3

low ___ means high enzyme affinity

K_m

4

inhibitors are studied with graph of ___ vs. ___
this is aka ___ plot (2)

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

5

x intercept of double reciprocal plot is ___

#NAME?

6

y intercept of double reciprocal plot is ___

1/V_max

7

K_m is the ___ at which V is ___

substrate concentration
V_max/2

8

competitive/noncompetitive inhibitors do not change V_max

competitive

9

competitive/noncompetitive inhibitors do not change K_m

noncompetitive

10

efficacy change means ___ of dose response curve

vertical shift

11

potency change means ___ of dose response curve

horizontal shift

12

competitive inhibitors change ___

potency

13

non-competitive inhibitors change ___

efficacy

14

V_d in terms of plasma drug concentration

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

15

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

16

low V_d means ___ L

4--8

17

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

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

18

CL in terms of V_d

CL = V_d x K_e

19

t_1/2 in terms of V_d

t_1/2 = (0.7 x V_d)/CL

20

loading dose in terms of V_d

LD = (C_p x V_d)/F

where F is bioavailability

21

maintenance dose in terms of C_p

MD = (C_p x CL)/F

22

zero order kinetics means

constant elimination per unit time

23

3 drugs with zero order kinetics

phenytoin
ethanol
aspirin

24

first order kinetics means

constant fraction of drug eliminated per unit time

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