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Flashcards in First Aid - Pharm Deck (233)
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 ___

(-)1/K_m

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

5 weak acid drugs
treat overdose of weak acid with ___

phenobarbital
MTX
TCAs
aspirin
bicarbonate

26

weak base drug
__a__
treat overdose wtih _b__

a. amphetamine
b.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

therapeutic index

TI = LD_50/ED_50

where LD_50 is median toxic dose,
ED_50 is median effective dose

31

the first synapse in a parasympathetic pathway is ___

nicotinic

32

the second synapse in a parasympathetic pathway is ___

muscarinic

33

the first synapse in a sympathetic pathway is ___

nicotinic

34

the second synapse in most sympathetic pathways is ___
2 exceptions are ___

noradrenergic

sweat gland
renal vascular smooth muscle

35

2nd synapse in sweat gland pathway is ___

muscarinic

36

2nd synapse in renal vascular smooth muscle pathway is ___

D1 dopaminergic

37

nicotinic receptor is ___tropic
muscarinic receptor is ___tropic

iono
metabo

38

nicotinic receptor is a ___-gated ___ channel

ligand
Na+/K+

39

alpha1 major functions

inc. vascular smooth muscle contraction
inc. pupillary dilator muscle contraction (mydriasis)
increase intestinal and bladder sphincter muscle contraction

40

alpha_1 adrenergic receptor type

G_qPCR

41

alpha_2 major function

decrease sympathetic outflow
decrease insulin release
decrease lipolysis
increase platelet aggregation

42

alpha_2 adrenergic receptor type

G_iPCR

43

beta 1 adrenergic major functions

increase heart rate
increase contractility
increase renin release
increase lipolysis

44

beta_1 adrenergic receptor type

G_sPCR

45

beta_2 adrenergic major functions

vasodilation
bronchodilation
increase contractility
increase HR
increase insulin release
increase lipolysis
ciliary muscle relaxation
increase aqueous humor production
decrease uterine tone

46

beta_2 adrenergic recetor type

GsPCR

47

M1 muscarinic receptor is ___
M2 muscarinic receptor is ___
M3 muscarinic receptor is ___

G_qPCR
G_iPCR
G_qPCR

48

M1 major functions

CNS, ENS

49

M2 major functions

decrease HR and contractility of atria

50

M3 major functions

increase exocrine gland secretion
increase gut peristalsis
increase bladder contraction
bronchocontriction
increase pupillary sphincter muscle contraction (miosis)
ciliary muscle contraction (accomodation)

51

D1Rs: receptor type and
major functions

G_sPCR
renal vascular smooth muscle relaxation

52

D2Rs: receptor type and
major functions

G_iPCR
neurotransmitter modulation

53

H1Rs: receptor type and
major functions

G_qPCR
nasal and bronchial mucus secretion
vascular permeability
bronchoconstriction
itching
pain

54

H2Rs: receptor type and
major functions

G_sPCR
gastric acid secretion

55

ADH V1Rs: receptor type and major functions

G_qPCR
vasoconstriction

56

ADH V2Rs: receptor type and major functions

G_sPCR
H2O reabsorption in collecting duct

57

Y is converted to ___ by ___.
this is blocked by ___, which works as a ___

DOPA
Y hydroxylase
metyrosine
antihypertensive

58

DOPA is converted to ___ by ___.
cofactor is ___

DA
DOPA decarboxylase (AAADC)
B6

59

DA is imported to vesicles by ___.
this is blocked by ___

VMAT (vesicular monoamine transporter)
reserpine

60

DA is converted to ___ by ___.
cofactor is ___

NE
DBH (DA beta hydroxylase)
vitamin C

61

In ___, NE is converted to ___ by ___, in the ___.
___ is required

adrenal medulla
E
PNMT (phenylethanolamine N-methyl transferase)
cytoplasm
SAM

62

After MAO-COMT in either order, DA becomes ___

HVA (homovanillic acid)

63

After MAO-COMT in either order, E becomes ___ and NE becomes ___

both become MHPG (methoxyhydroxyphenylglycol)

64

After COMT, E becomes ___ and NE becomes ___.

metanephrine
normetanephrine

65

adrenal pheochromocytomas make more ___ than ___, but other ones do the opposite

E
NE

66

catecholamine exocytosis is potentiated by ___ (2) and inhibited by ___

amphetamine
ephedrine
guanethidine

67

___ (3) blocks catecholamine reuptake

cocaine
amphetamine
TCAs

68

2 presynaptic receptors which inhibit catecholamine release

alpha_2
M2

69

1 presynaptic receptor which facilitates catecholamine release

AII (angiotensin)

70

rate limiting step of cholinergic neurotransmission is ___
this is inhibited by ___

Ch uptake
hemicholinium

71

ACh is synthesized by ___ from ___ and ___

choline acetyltransferase (ChAT)
choline
Ac CoA

72

uptake of ACh into vesicule is inhibited by ___
vesicular exocytosis is inhibited by ___

vesamicol
botulinum

73

direct agonists: cholinomimetics

bethanechol, carbachol, pilocarpine, methacholine

74

direct cholinomimetic for GI motility

bethanechol

75

2 indications for bethanechol

ileus (post op, neurogenic)
urinary retention
b/c it activates bladder and bowel

76

2 direct cholinomimetics for glaucoma

pilocarpine
carbachol

77

pilocarpine causes contraction of ___ (2)
and secretion of ___ (3)

pupillary sphincter
ciliary body
saliva
sweat
tears

78

contraction of ___ helps open angle glaucoma
contraction of ___ helps closed angle glaucoma

ciliary body
sphincter pupillae

79

direct cholinomimetic for testing asthma

methacholine

80

indirect cholinomimetics are ___s

AChEI

81

Indirect agaonists (cholinomimetics)

neostigmine, pyridostigmine, physostigmine, donepezil, rivastigmins, galantamine

82

indirect cholinomimetic for GI motility

neostigmine

83

neostigmine has high/low CNS penetration

low

84

4 neostigmine indications

ileus (post op, neurogenic)
urinary retention
MG
post op NMJ block reversal

85

cholinomimetic for MG dx

edrophonium

86

cholinomimetic for MG tx

pyridostigmine

87

2 indirect cholinomimetics for glaucoma

echothiophate
physiostigmine

88

CNS penetrations of
a. pyridostigmine
b. physiostigmine
c. echothiophate

a. low
b. high
c. low

89

what indirect agonist do you use for alzheimer's?

donepezil, rivastigmine, galantamine

90

cholinesterase inhibitor poisoning

DUMBBELSS:
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skeletal and CNS
Lacrimation
Sweating
Salivation

91

2 antidotes for cholinergic intoxication

atropine
pralidoxime

92

pralidoxime functions in cholinergic intoxication by ___

regenerating active ChE

93

antimuscarinic for eye

atropine
homatropine
tropicamide

94

atropine causes ___ (2)

mydriasis
cycloplegia

95

cycloplegia means ___

inability to accomodate

96

antimuscarinic for Parkinson's disease

benztropine

97

antimuscarinic for motion sickness

scopolamine

98

2 antimuscarinic for asthma and COPD

ipratropium
tiotropium

99

2 antimuscarinics for bladder spasticity

oxybutynin
darifenacin
solifenacin

100

glycopyrrolate used for ___ (3)

reduce airway secretions
drooling
peptic ulcers

101

atropine effects

eye: pupil dilation, cycloplegia
respiratory: decreased secretions from airway
stomach: decreased acid secretion
gut: decreased motility
bladder: decreased urgency in cystitis

102

atropine toxicity

hot
dry
red
blind (cycloplegia)
mad (disoriented)

may cause acute angle-closure glaucoma, urinary retention (in BPH men or hyperthermic infants)

103

E effects which receptor

beta > alpha (with alpha at higher doses)

104

E is indicated for ___ (4)

anaphylaxis
open angle glaucoma
asthma
hypoTN

105

NE effects which receptor

alpha_1 > alpha_2 > beta_1

106

NE is indicated for ___

hypoTN (*decreases renal perfusion)

107

isoproterenol effects which receptor

beta_1 = beta_2

108

isoproterenol is indicated for ___

evaluation of tachyarrhythmias

109

DA effects which receptor

D1 = D2 > beta > alpha

110

DA is indicated for ___ (3)

shock
heart failure
unstable bradycardia

111

DA's effects on the heart

+ inotrope
+ chronotrope
at high doses

112

dobutamine effects which receptor

beta_1 > beta_2 > alpha

113

dobutamine is indicated for ___ (3)

heart failure
cardiac stress testing

114

dobutamine's effects on the heart

inotropic > chronotropic

115

phenylephrine effects which receptor

alpha_1 > alpha_2

116

phenylephrine is indicated for ___ (3)

pupil dilation
nasal decongestion
hypotension

117

5 beta_2-selective agonists

metaproterenol
albuterol
salmetrol
terbutaline
ritodrine

118

2 beta_2 agonists for acute asthma

metaproterenol
albuterol

119

beta_2 agonist for chronic asthma tx

salmetrol

120

2 tocolytic beta_2 agonist

terbutaline
ritodrine

121

3 indirect sympathomimetics
of these ___ (2) are secretagogues

amphetamine
ephedrine
cocaine

amphetamine
ephedrine

122

3 amphetamine indications

narcolepsy
obesity
ADD

123

3 ephedrine indications

nasal decongestion
urinary incontinence
hypoTN

124

what drug should you avoid prescribing in patients with cocaine intoxication?

beta blockers because of the unopposed alpha 1 activation leading to extreme hypertension

125

2 alpha_2 agonists

clonidine
alpha-methyldope

126

alpha_2 agonists are indicated for ___ with ___

HTN
renal disease

127

clonidine toxicity symptoms

CNS depression, bradycardia, hypotension, respiratory depression, small pupil size

128

alpha-methyl dopa toxicity symptoms

direct coombs + hemolytic anemia, SLE-like syndrome

129

2 non-selective alpha blockers
___ is reversible blocker

phenoxybenzamine
phentolamine

phentolamine

130

phenoxybenzamine use:

HTN
prevention in heochromocytoma

131

phenoxybenzamine toxicity:

orthostatic hypotension, reflex tachycardia

132

phentolamine use:

MAO inhibitor patients who ate too much tyramine

133

alpha_1 selective blockers end in ___

zosin

134

alpha_1 blockers are indicated for

HTN
urinary retention from BPH
PTSD

135

3 alpha_1 SEs

1st dose orthostatic hypoHTN
dizziness
headache

136

alpha_2 selective blocker

mirtazapine

137

mirtazapine is indicated for ___

depression

138

3 mirtazapine SEs

sedation
hyperlipidemia
hyperphagia

139

beta blockers effects

decrease heart rate and contractility
decrease MI mortality
decrease AV conduction velocity in SVT
decrease cardiac output and renin secretion
decrease progression of CHF
decrease aqueous humor

140

2 beta blockers for SVT

propranolol
esmolol

141

sexual SE of beta blocker

impotence

142

acebutolol is ___-selective beta blocker

beta_1

143

atenolol is ___-selective beta blocker

beta_1

144

betaxolol is ___-selective beta blocker

beta_1

145

esmolol is ___-selective beta blocker

beta_1

146

labetalol is ___-selective beta blocker

non

147

metoprolol is ___-selective beta blocker

beta_1

148

nadolol is ___-selective beta blocker

non

149

pindolol is ___-selective beta blocker

non

150

propranolol is ___-selective beta blocker

non

151

timolol is ___-selective beta blocker

non

152

2 non-selectve alpha + beta blockers

carvedilol
labetalol

153

2 partial beta agonists

pindolol
acebutolol

154

tx for acetaminophen poisoning

N-acetyl cysteine

155

tx for salicylate poisoning (2)

bicarbonate
dialysis

156

purpose of bicarbonate in salicylate poisoning

alkalinize urine

157

tx for amphetamine poisoning

ammonium chloride

158

purpose of ammonium chloride in amphetamine poisoning

acidify urine

159

tx for anticholinesterase poisoning (2)

atropine
pralidoxime

160

tx for antimuscarinic toxicity

physiostigmine salicylate

161

tx for beta blocker toxicity

glucagon

162

tx for digitalis toxicity (5)

stop digitalis
normalize K+
lidocaine
anti-dig Fab
Mg2+

163

tx for Fe toxicity

desferoxamine

164

tx for Pb toxicity (4)

CaEDTA
dimercaprol
succimer
penicillamine

165

tx for As/Au/Pb toxicity (4)

dimercaprol
succimer
penicillamine
CaEDTA

166

tx for Cu toxicity

penicillamine

167

tx for CN- toxicity (3)

nitrite
hydroxocobalamin
thiosulfate

168

tx for methemoglobinemia (2)

methylene blue
vitamin C

169

tx for CO toxicity (2)

100% O2
hyperbaric O2

170

tx for MeOH/ethylene glycol toxicity (3)

ethanol
dialysis
fomepizole

171

tx for opioid toxicity

naloxone

172

tx for benzo toxicity

flumazenil

173

tx for TCA toxcity

bicarbonate

174

purpose of bicarbonate in TCA toxicity

alkalinize serum

175

tx for heparin toxicity

protamine

176

tx for warfarin toxicity (2)

vitamin K
FFP

177

tx for tPA/streptokinase toxicity

aminocaproic acid

178

tx for theophylline toxicity

beta blocker

179

Fe poisoning is particularly common with ___

kids

180

Fe is cytotoxic because of ___

membrane lipid peroxidation

181

acute Fe poisoning presents with ___

gastric bleeding

182

chronic Fe poisoning presents wtih ___ (2)

metabolic acidosis
GI obstruction 2' to scarring

183

drugs causing atropine-like SEs

TCA

184

2 drugs causing coronary vasospasm

cocaine
sumatriptan

185

4 drugs causing flushing

vancomycin
adenosine
niacin
CCBs

186

3 drugs which cause torsades

class Ia antiarrhythmics
class III antiarrhythmics
cisapride

187

6 drugs which cause agranulocytosis

clozapine
carbamazepine
colchicine
dapsone
PTU
methimazole

188

5 drugs which cause aplastic anemia

chloramphenicol
benzene
NSAIDs
PTU
methimazole

189

drug causing direct coombs positive hemolytic anemia

alpha methyldopa

190

drug causing gray baby syndrome

chloramphenicol

191

drugs causing hemolysis in context of G6PD deficiency

INH
sulfonamides
primaquine
aspirin
ibuprofen
nitrofurantoin

192

drugs causing megaloblastic anemia

pheyntoin
MTX
sulfa

193

drug causing cough

ACEI

194

3 drugs causing pulmonary fibrosis

bleomycin
amiodarone
busulfan

195

drug causing acute cholestatic hepatitis

macrolide

196

4 drugs causing hepatic necrosis

halothane
VPA
acetaminophen
amanita phalloides

197

drug causing hepatitis

INH

198

2 drugs causing pseudomembranous colitis

clindamycin
ampicillin

199

6 drugs causing gynecomastia

spironolactone
digitalis
cimetidine
alcohol
ketoconazole
estrogens

200

2 drugs causing hot flashes

tamoxifen
clomiphene

201

2 drugs causing hypothyroidism

Li
amiodarone

202

2 drugs causing gout

furosemide
thiazides

203

3 drugs causing photosensitivity

sulfonamides
amiodarone
tetracycline

204

8 drugs causing Stevens-Johnson syndrome

carbamazepine
ethosuximide
lamotrigine
phenobarbital
phenytoin
sulfa
penicillin
allopurinol

205

4 drugs causing SLE-like syndrome

hydralazine
INH
procainamide
phenytoin

206

fluoroquinolones cause ___ (3) in kids

tendonitis
tendon rupture
cartilage damage

207

___ causes Fanconi's syndrome

expired tetracycline

208

Fanconi's syndrome is ___ wasting of ___ (4)

tubular
bicarbonate
AAs
glucose
uric acid

209

3 drugs causing interstitial nephritis

methicillin
NSAIDs
furosemide

210

2 drugs causing hemorrhagic cystitis
prevent this by giving ___

CTX
ifosfamide
mesna

211

2 drugs which cause cinchonism

quinidine
quinine

212

cardiovascular aspects of cinchonism

flushing
arrhythmia

213

4 neurological sx of cinchonism

tinnitus/hearing loss
blurry vision
somnolence
confusion

214

2 cutaneous sx of cinchonism

flushing
rash

215

2 drugs causing DI

Li
demeclocycline

216

4 drugs causing PD-like syndrome

haloperidol
chlorpromazine
metoclopramide
reserpine

217

3 drugs causing seizures

buproprion
imipinem/cilastatin
INH

218

drugs causing tardive dyskinesia

antipsychotics

219

4 drugs causing disulfiram-like reaction

metronidazole
cephalosporins (some)
procarbazine
1st generation sulfonylureas

220

disulfiram-like reaction means
mechanism is ___

feeling bad after EtOH
acetaldehyde dehydrogenase inhibition

221

drug causing nephrotoxicity + neurotoxicity

polymixins

222

4 drugs causing nephrotoxicity + ototoxicity

aminoglycosides
vancomycin
loop diuretics
cisplatin

223

9 CYP450 inducers

quinidine
barbiturates
st. john's wort
phenytoin
rifampin
griseofulvin
carbamazepine
chronic alcholism

224

CYP450 inhibitors

INH
sulfonamides
cimetidine
erythromycin
grapefruit

225

3 drugs metabolized by alcohol dehydrogenase

ethylene glycol
MeOH
EtOH

226

ethylene glycol is metabolized by alcohol dehydrogenase to ___
effects are ___ (2)

oxalic acid
acidosis
nephrotoxicity

227

MeOH is metabolized by alcohol dehydrogenase to ___ (2)
effects are ___ (2)

formaldehyde
formic acid
acidosis
retinal damage

228

EtOH is metabolized by alcohol dehydrogenase to ___
effects are ___ (3)

acetaldehyde
nausea
vomiting
hypoTN

229

___ inhibits alcohol dehydrogenase

fomepizole

230

5 non-obvious sulfa drugs

celecoxib
probenecid
thiazides
sulfonylurea
sumatriptan

231

systemic part of sulfa allergic rxn

fever

232

cutaneous part of sulfa allergic rxn (3)

rash
urticaria (hives)
Stevens-Johnson

233

hematologic part of sulfa allergic rxn (3)

HA
thrombocytopenia
agranulocytosis