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M2 Fall > Pharmocology Unit 1 > Flashcards

Pharmocology Unit 1 Flashcards

1
Q

cimetidine

A

inhibit drug metabolism (CYPs), inhibit excretion (competitive inhibitor organic cation transport in kidney tubule and liver)

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2
Q

phenobarbitol

A

stimulate drug metabolism

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3
Q

probenicid

A

competitive inhibitor organic anion transporter, inhibit drug secretion into kidney tubule and liver and excretion

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4
Q

ethanol

A

stimulate drug metabolism (CYPs)

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5
Q

bethanechol

A

synthetic choline ester; M selective; increase action time; stimulate smooth muscle post/op (GI, bladder, saliva)

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6
Q

carbachol

A

synthetic choline ester; increased action time; wide-angle glaucome -> increase humour drainage

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7
Q

methacholine

A

synthetic choline ester; M selective; decrease tachycardia, test bronchiol hyperactivity

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8
Q

muscarine

A

natural alkaloid; Muscarinic agonist

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9
Q

pilocarpine

A

natural alkaloid; muscarinic agonist; wide-angle glaucoma, increase saliva (anti-parkinson)

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10
Q

nicotine

A

natural alkaloid; nicotinic agonist

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11
Q

varenicline

A

nicotinic selective agonist

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12
Q

Contraindications of cholinergic activation

A

asthma, hyperthyroid, coronary insufficiency, acid peptic disease

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13
Q

adverse effects of cholinergic stimulation

A

flushing, sweating, cramps, bladder tightness, visual changes, headache, salivation

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14
Q

ambenonium

A

competitive ChE inhibitor

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15
Q

edrophonium

A

Competitive ChE inhibit; Q; alcohol-short acting; neuromusclar block reversal; myasthenia gravis

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16
Q

neostigmine

A

Competitive ChE inhibit; Q; carbamate-intermediate; ileus (GI motility); myasthenia gravis; neuromuscular block reversal

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17
Q

physostigmine

A

Competitive ChE inhibit; T; carbamate-inter; topical, wide-angle glaucoma

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18
Q

pyridostigmine

A

competitive ChE inhibit; Q; carbamate-inter; myasthenia gravis

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19
Q

diisopropylfluorophosphate (DFP)

A

noncompetitive ChE inhibit; organo-phosphate-long lasting; very toxic

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20
Q

Echothiophate

A

OP noncompetitive ChE inhibit; long lasting; emergency IOP reduction; only OP with therapeutic value

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21
Q

carbaryl

A

OP insecticide; ChE inhibitor

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22
Q

malathion

A

OP insecticide; ChE inhibitor; least toxic-used for head lice

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23
Q

parathion

A

OP insecticide; ChE Inhibitor; common agent in OP poisoning

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24
Q

tetraethylpyrophosphate

A

OP insecticide; ChE inhibitor

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25
Q

sarin

A

OP nerve gas; ChE inhibitor

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26
Q

Soman

A

OP nerve gas; ChE inhibitor

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27
Q

pralidoxime (2-PAM)

A

Q; AChE reactivator after OP poisoning (before aging) Step 2.

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28
Q

Cholinergic antogonist effects

A

alleviate GI hypermotility, diarrhea; decrease sweating, salivation, acid production; anti-parkinson; anti-motion sickness, amnesia

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29
Q

cholinergic anatgonist toxicities (CNS)

A

hallucinations, amnesia, sedation/excitment

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30
Q

cholinergic antagonist toxicities (PNS)

A

mydriasis, cycloplegia, photophobia, dry eyes, xerostomia, , urinary retention, tachycardia, atropine flush/fever.

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31
Q

atropine

A

cholinergic anatoginist; M selective; T; long; step 1 OP poision; cardiac collapse; anti-parkinson; bronchodilation; decreased secretions; high dose -> lower acid production

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32
Q

homatropine

A

cholinergic anatgonist; M selective; T; inter; topical - mydriasis, cycloplegia

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33
Q

scopolamine

A

cholinergic anatgonist; M selective; T; long; amnesia; motion sickness

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34
Q

methscopolamine

A

cholinergic anatgonist; M selective; Q; long; GI diseases, decrease motility/secretions

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35
Q

trihexyphenidyl

A

cholinergic anatgonist; M selective; T; Inter; anti-parkinson

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36
Q

tropicamide

A

cholinergic anatgonist; M selective; T; short; topical - mydriasis, cycloplegia

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37
Q

cyclopentolate

A

cholinergic anatgonist; M selective; T; inter; topical - mydriasis, cycloplegia

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38
Q

ipratropium

A

cholinergic anatgonist; M selective; Q; aerosol form; bronchodilaton, less mucociliary clearance problems (does not decrease fluidity) for patients with airway problems; tachycardia, decrease salivation; used for B2 intolerance, less effective

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39
Q

tiotropium

A

cholinergic anatgonist; M selective; Q; aerosol form; like ipratropium but longer lasting; less mucociliary clearance problems (does not decrease fluidity) for patients with airway problems

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40
Q

derafinicin

A

cholinergic anatgonist; M3 selective (smooth muscle, gland); slow micturition, bladder spasms, urinary urgency

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41
Q

solifenacin

A

cholinergic anatgonist; M3 selective (smooth muscle, gland); slow micturition, bladder spasms, urinary urgency

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42
Q

tolterodine

A

cholinergic anatgonist; M3 selective (smooth muscle, gland); slow micturition, bladder spasms, urinary urgency

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43
Q

mecamylamine

A

cholinergic nondepolarizing competitive antagonist; N1 selective (ganglionic blocker); S- increase GI absorption; 12hrs; hypertensive emergency; adjunct for PVD, HTN; control bleeding through hypotension.
CNS effects- tremors, confusion, mania, depression

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44
Q

trimethaphan

A

cholinergic nondepolarizing competitive antagonist; N1 selective (ganglionic blocker); IV, minutes; hypertensive emergency; control bleeding through hypotension

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45
Q

N1 gangion blocker effects

A

orthostatic hypotension, low CO, low TPR, fainting, xerostomia, urinary retention, mydriasis, cycloplegia, low sex function, low GI motility

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46
Q

succinylcholine

A

cholinergic anatogonist; N2 selective noncompetitive depolarizing;rapid hydrolysis by plasma ChE; neuromuscular block.

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47
Q

d-tubocurarine (curare)

A

N2 selective nondepolarizing competitive antagonist; long; no vagal block, some histamine release

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48
Q

cisatracurium

A

N2 selective nondepolarizing competitive antagonist; like curare; intermediate

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49
Q

mivacurium

A

N2 selective nondepolarizing competitive antagonist; like curare; short

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50
Q

atracurium

A

N2 selective nondepolarizing competitive antagonist; like curare

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51
Q

pancuronium

A

ammonia steroid; N2 selective nondepolarizing competitive antagonist; long

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52
Q

vecuronium

A

ammonia steroid; N2 selective nondepolarizing competitive antagonist; long; some ganglion/vagal block, tachycardia, no histamine release

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53
Q

nondepolarizing N2 selective anatgonist contraindications

A

liver/renal dysfunction (impaired drug clearing); myasthenia gravis; may induce hypotension from cross-react with N1, histamine release

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54
Q

depolarizing N2 selective anatgonist (succinylcholine) contraindications

A

ChE mutations; OP poisioning; high EC K+ (CHF, burns, trauma); eye trauma, hi IOP.

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55
Q

alpha-1 selctive agonists

A

contraction/constriction/GI relaxation; vasoconstriction, mydriasis, ejaculation, piloerection, glycogenolysis

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56
Q

metaraminol

A

a1 selective agonist

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57
Q

methoxamine

A

a1 selctive agonist; hypotensive crisis

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58
Q

phenylephrine

A

a1 selective agonist; hypotensive crisis, reduce diffusion of anesthetic from site, alleviate congestion; mydriasis

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59
Q

alpha-2 selective agonists

A

presynaptic (-)feedback on NE release

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60
Q

a-methyldopa

A

a2 selective agonist (adrenergic antagonist); lower NE release from terminal; low TPR, anti-HTN, low HR, low CO; conversion to a-methylNE (false neurotransmitter), stimulate brainstem; CNS adverse effects: sedation, dizziness, xerostomia, congestion, hypotension, anemia, hepatitis, lupus

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61
Q

clonidine

A

a2 selective agonist (adrenergic antagonist); lower NE release from terminal; low TPR, hypotension, low HR, low CO;

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62
Q

guanebenz

A

a2 selective agonist (adrenergic antagonist); lower NE release from terminal; low TPR, elicit hypotension, low HR, low CO;

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63
Q

alpha-2 agonist adverse effects

A

sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation

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64
Q

amphetamine

A

mixed a1,B1 agonist; vasopressor; increase NE release from terminal

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65
Q

ephedrine

A

mixed a1,B1, mild B2 agonist; stress incontinece, orthostatic hypotension, decongestant, brochodilation, increase NE release from terminal

66
Q

epinephrine

A

B»>a agonist; cardiac simulant, vasoconstrictor, tachycardia, up arterial pressure, up flow to muscle, up blood glucose, anaphylaxis, cardiac arrest, hemostasis in surgery, congestion

67
Q

norepinephrine

A

a, B1»>B2 agonist, up BP, CO, HR, vasoconstriciton, FFA; congestion,

68
Q

B1 selective agonist

A

increase HR, contractility, CO, lipolysis

69
Q

dobutamine

A

B1 selective agonist; heart failure

70
Q

isoproterenol

A

B nonselective agonist; vasodilator, B1 -> up CO; B2 -> down MAP

71
Q

B2 selective agonist

A

dilation/relaxation; skeletal muscle/coronary artery vasodilation; bronchodilation, myometrial relax, GI relax

72
Q

albuterol

A

B2 selective agonist; asthma, bronchodilation

73
Q

metaproterenol

A

B2 selective agonist; asthma, bronchodilation

74
Q

terbutaline

A

B2 selective agonist; asthma, bronchodilation; relax pregnant uterus

75
Q

D1 agonist

A

renal splnachnic vasodilation

76
Q

D2 agonist

A

presynaptic (-)feedback on NE release; postsynaptic in CNS

77
Q

bromocriptine

A

CNS D2 agonist; anti-parkinson; PNS effects: postural hypotension, cardiac arrhythmia

78
Q

dopamine

A

a1,B1,D1,2 agonist; shock therapy

79
Q

fenoldapam

A

D1»>D2 agonist; renal, splanchnic vasodilaton

80
Q

a1 selective blockers

A

vasodilaton, decrease MAP, urinary obstruction, pheochromocytoma

81
Q

doxazosin

A

a1 selective blocker; urinary obstruction relief

82
Q

prazosin

A

Highly selective a1 selective blocker; elicits no tachycardia; oral, 12hrs; mild/moderate hypertension; urinary obstruction from BPH

83
Q

tamsulosin

A

a1 selective blocker; urinary obstruction relief

84
Q

terazosin

A

a1 selective blocker; urinary obstruction relief

85
Q

phenoxybenzamine

A

noncompetitive a1 blocker; long lasting (day); alkylates a1,2 and blocks Aminte I transport; low MAP (-> reflex tachycardia, no B1 block); pheochromocytoma preoperatively or inoperative/metastatic conditions, severe hypertension

86
Q

phentolamine

A

a1 competitive blocker; pheochromocytoma (preoperative/inoperative/metastatic), hypertension; a2 block -> up NE release -> up CO, tachy; “dirty drug” cross react with muscarinic and histamine

87
Q

labetolol

A

mix adrenergic antagonist

88
Q

B1 selective antagonist

A

used with diuretics from hypertension therpay

89
Q

atenolol

A

B1 blocker; inter-long; anti-hypertensive

90
Q

betaxolol

A

B1 blocker; long; glaucoma

91
Q

metaprolol

A

B1 blocker; inter; anti-hypertensive; angina pectoris; recurrent MI protection

92
Q

nadolol

A

B nonselective blocker; long; anti-HTN

93
Q

pindolol

A

B nonselective blocker; inter; anti-HTN

94
Q

propranolol

A

B nonselective blocker; inter; Anti-HTN, angina, anti-arrhythmia, migraine, recurrent MI protection

95
Q

timolol

A

B nonselective blocker; inter; anti-htn; angina; lower IOP, recurrent MI protection

96
Q

guanethidine

A

prejunctional transport into neuron by Amine I; oral; long; depletes NE stores (minimal effect on other biogenic amines, (epi, da); block exocytosis of NT; anti-HTN and severe HTN. not cross BBB

97
Q

reserpine

A

Transported to neuron by Amine I, depletes stores of all biogenic amines, (NE, epi, DA, serotonin) PNS and CNS; CNS affects: sedation, depression, parkinson, GI motility

98
Q

cocaine

A

Amine I tronsport inhibitor; vasoconstriction, tachycardia, mydriasis; hemostasis during surgery

99
Q

DMI (tricyclic antidepressant)

A

Aminte I transport inhibitor; target: CNS. increase NE in synapse

100
Q

tyramine

A

NE releasing agent by displacing from vesicle. found in cheeses, can raise BP when on MAO inhibitors.

101
Q

pseudoehpedrine

A

a,B agonist; NE releasing agent; decongestant

102
Q

azothioprine

A

immunosupressant; block purine synthesis by incorporating nucleotide thio-gaunine. uses: renal transplant, AI; adverse: myelosuppression, nausea, vomiting

103
Q

cyclophsophamide

A

immunosuppressant; DNA linking -> damage to proliferating cells; uses: AI disease, bone marrow transplant; adverse: meylosuppression

104
Q

leflunomide

A

immunosuppressant; blockk pyrimidine synthesis; uses: RA, AI disease; adverse: myelosuppression,heptatotoxicity, diarrhea

105
Q

methotrexate

A

immunosuppressant; dihydrofolate reducatese inhibitor; block thymidine and purine synthesis; uses: RA, AI; adverse: myelosuppression, heptotoxicity

106
Q

mycophenolate-mofetil

A

immunosuppressant; inosine monophasphate dehydrogenase inhibitor, block purine synthesis; uses: solid organ transplant, alternative to cyclosporin, some AI diseases; adverse: myelosuppression, nausea, vomiting

107
Q

prednisone (immunosuppression)

A

blocks activated transcription factor NF-AT and IL-2, IL-4, INF-g, decrease TH response, ab production, cytotoxic response; uses: solid organ trasnplant and hematopeitic stem cell transplant; adverse: cushings, hyperglycemia, htn, osteoporosis,

108
Q

sirolimus (rapamycin)

A

immunosuppressant; + FKBP12 inhibit mTOR -> blcok translation of cell cycle progression mRNA; uses: solid organ transplant, graft vs host; adverse: antagonizes tacrolimus, synergizes with cyclosporin, myelosuppression, hld, htn, hepatotoxicity

109
Q

cyclosporin

A

immunosuppressant; + cyclophilin -> inactivate calcineurin -> no activation of NF-AT; uses: kidney, liver, cardiac transplant, AI disease, some inflammatory diseases; advrese: nephrotoxicity, hyperglycemia, htn, liver failure

110
Q

tacrolimus

A

immunosuppressant; + FKBP12 inactivate calcineurin -> no activation of NF-AT; uses: same as cyclosporin, 100x potency; adverse: same as cyclosporin

111
Q

Anti-Tcell globulin (ATG)

A

immunosuppressant; purified animal anti-Tcell Ig; prolonged T cell depletion (1 year); adverse: cytokine release syndrome, potential anaphylaxis

112
Q

muromonab-CD3 (OKT3)

A

anti-CD3 (tcell) Ig; target all circulation T cells; uses: acute organ rejection; adverse: massive cytokine release syndrome, potential anaphylaxis,

113
Q

alentuzumab

A

anti-CD52 Ig; target circulation leukocytes (lymphocytes, macrophages, neutrophils, NK cells) proloned immune suppression; adverse: myelosuppression

114
Q

basiliximab

A

anti-CD25 (IL-2r) Ig: target all circulation ACTIVATED T cells; uses: moderate effect compared to ATG, for low to moderate risk or rejection; adverse: well tolerated

115
Q

Rh(d) Ig

A

Prevention of fetal hemolytic syndrome by passive immunity of Rh- mother

116
Q

belatecept

A

fusion protein B7 ligand/Ig Fc domain; blocks co-stimulation -> anergy; uses: kidney transplant; adverse: anemia, neutropenia, susceptible to EBV infection

117
Q

IL-2

A

Immune stimulant; increase T cell proliferation; uses: metastatic melanoma, renal cell carcinoma; adverse: capillary leak syndrome, hypotension, low perfusion, lack of specificity

118
Q

INF-gamma

A

immune stimulant; increase Th1 response, macrophage activation, cytotoxicity for severe recurrent infections (intracellular)

119
Q

bacillus calmette-guerin (BCG)

A

immune stimulant adjuvant; attenuated live bacillus; increase antigen presentation activity; adverse: potential systemic inflammation (shock)

120
Q

ceterizine

A

2nd gen H1 antagonist; reduced CNS effects; reduced non H1 effects

121
Q

Non-H1 effects of anti-histamines

A

antagonost: cholinergic, adrenergic, seretonin, promethazine (anesthesia)

122
Q

cyclizine

A

1st gen H1 antagonist; motion sickness; adverse: CNS sedation, nonH1 effects

123
Q

dimenhydrinate

A

1st gen H1 antagonist; motion sickness; (dramamine); adverse: CNS sedation, nonH1 effects

124
Q

diphenhydramine

A

1st gen Hq antagonist; motion sickness (benadryl); advese: CNA sedation, nonH1 effects

125
Q

H1 antagonist uses

A

allergic rhinitis, urticaria; motion sickness, emesis

126
Q

fexofenedine

A

2nd gen H1 antagonist; reduced CNS, nonH1 effects

127
Q

loratadine

A

2nd gen H1 antagonist; reduced CNS, nonH1 effects

128
Q

adalimumab

A

human anti-TNFa; RA, Chrons disease, inflammation

129
Q

infliximab

A

humanized anti-TNF1; RA Chrons, inflammation

130
Q

etanercept

A

fusion protein; TNFa receptor + Fc domain IgG; RA, Chrons, inflammation

131
Q

anakinra

A

competitive IL-1r antagonist; RA and other inflammatory diseases; short half-life, daily injection

132
Q

Aspirin

A

NSAID; analgesic/antipyretic, cardiovascular prophylaxis

133
Q

diclofenac

A

NSAID; Rx arthritis/anti-inflammatory

134
Q

ibuprofen

A

NSAID; analgesic/antipyretic

135
Q

indomethacin

A

NSAID; RX arthritis/anti-inflammatory; Intolerance: GI effects

136
Q

ketorolac

A

NSAID; post surg analgesic

137
Q

naproxen

A

NSAID; analgesic/antipyretic; RX anti-inflammatory

138
Q

Aspirin Intolerance

A

Salicilysm: hyperventilation, tinnitus, vertigo, emesis, sweating
Reye’s Syndrome: viral disease/vaccination -> acute encephalopathy, fatty liver disease

139
Q

NSAID toxicity

A

Acute renal failure, GI ulceration, prolonged bleeding (aspirin), increased CV event (not aspirin)

140
Q

misoprostol

A

PGE analog; protective against NSAID-indiced GI ulcers; given with diclofenac

141
Q

Celecoxib

A

COX2 selective inhibitor; analgesic/antipyretic; less GI, platelet effects; for chronic NSAID use; increased CV/stroke

142
Q

acetominephen

A

nonselective COX inhibitor; inhibited by peroxides at inflammation; not anti-inflammatory; no GI, CV, platelet effects; analgesic/antipyretic; hepatotoxicity

143
Q

rofecoxib

A

COX2 selective inhibitor; analgesic/antipyretic; less GI, platelet effects; for chronic NSAID use; increased CV/stroke; OFF MARKET

144
Q

prednisone (anti-inflammatory)

A

increased production of annexins -> inhibition of PLA2 and AA->leukotriene/prostaglandin production
repressed expression of IL-1, TNFa and IL-8 (chemotaxin)

145
Q

PGE

A

relax smooth muscle: GI circular, bronchial, vasodilation; constrict smooth muscle: GI long., uterine; hyperalgesia

146
Q

PGI/prostacyclin

A

relax bronchial, uterine, vasodilation; inhibit aggregation; antogonize TXA; hyperalgesia

147
Q

TXA

A

vasoconstriction; promote aggregation; antagonize PGI

148
Q

Salmeterol

A

long acting aerosolized B2 agonist; maintenance therpay with fluticasone

149
Q

beclomethasone

A

aerosolized corticosteroid; long term reduction of asthma symmptoms

150
Q

budesomide

A

aerosolized corticosteroid; long term reduction of asthma symmptoms

151
Q

fluticasone

A

aerosolized corticosteroid; long term reduction of asthma symmptoms

152
Q

triamcinolone

A

aerosolized corticosteroid; long term reduction of asthma symmptoms

153
Q

montelukast

A

LTD4 receptor antagonist; reduce bronchoconstriction and edema; leukotriene modulator; allows reduction of steroid dose; asthma prophylaxis

154
Q

zafirlukast

A

LTD4 receptor antagonist; reduce bronchoconstriction and edema; leukotriene modulator; allows reduction of steroid dose; asthma prophylaxis

155
Q

zileuton

A

Lipoxygenase inhibitor; blocks productino of leukotrienes from AA; hepatotoxic

156
Q

cromolyn

A

inhibit degranulation from mast cells; Ca channel blocker?; Cl channel clocker

157
Q

nedocromil

A

inhibit degranulation from mast cells; Ca channel blocker?; Cl channel blocker

158
Q

theophylline

A

methyxanthine; inhibitor of phosphdiesterase degredation of cAMP (B2 pathway to smooth muscle relaxation) -> brochodilation

159
Q

LTB4

A

neutrophil chemotaxis

160
Q

LTD4

A

increased capillary permeability, bronchoconstriction, eosinophil chemotaxis, degranulation

M2 Fall (5 decks)

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