Pharmocology Unit 1 Flashcards
1
Q
cimetidine
A
inhibit drug metabolism (CYPs), inhibit excretion (competitive inhibitor organic cation transport in kidney tubule and liver)
2
Q
phenobarbitol
A
stimulate drug metabolism
3
Q
probenicid
A
competitive inhibitor organic anion transporter, inhibit drug secretion into kidney tubule and liver and excretion
4
Q
ethanol
A
stimulate drug metabolism (CYPs)
5
Q
bethanechol
A
synthetic choline ester; M selective; increase action time; stimulate smooth muscle post/op (GI, bladder, saliva)
6
Q
carbachol
A
synthetic choline ester; increased action time; wide-angle glaucome -> increase humour drainage
7
Q
methacholine
A
synthetic choline ester; M selective; decrease tachycardia, test bronchiol hyperactivity
8
Q
muscarine
A
natural alkaloid; Muscarinic agonist
9
Q
pilocarpine
A
natural alkaloid; muscarinic agonist; wide-angle glaucoma, increase saliva (anti-parkinson)
10
Q
nicotine
A
natural alkaloid; nicotinic agonist
11
Q
varenicline
A
nicotinic selective agonist
12
Q
Contraindications of cholinergic activation
A
asthma, hyperthyroid, coronary insufficiency, acid peptic disease
13
Q
adverse effects of cholinergic stimulation
A
flushing, sweating, cramps, bladder tightness, visual changes, headache, salivation
14
Q
ambenonium
A
competitive ChE inhibitor
15
Q
edrophonium
A
Competitive ChE inhibit; Q; alcohol-short acting; neuromusclar block reversal; myasthenia gravis
16
Q
neostigmine
A
Competitive ChE inhibit; Q; carbamate-intermediate; ileus (GI motility); myasthenia gravis; neuromuscular block reversal
17
Q
physostigmine
A
Competitive ChE inhibit; T; carbamate-inter; topical, wide-angle glaucoma
18
Q
pyridostigmine
A
competitive ChE inhibit; Q; carbamate-inter; myasthenia gravis
19
Q
diisopropylfluorophosphate (DFP)
A
noncompetitive ChE inhibit; organo-phosphate-long lasting; very toxic
20
Q
Echothiophate
A
OP noncompetitive ChE inhibit; long lasting; emergency IOP reduction; only OP with therapeutic value
21
Q
carbaryl
A
OP insecticide; ChE inhibitor
22
Q
malathion
A
OP insecticide; ChE inhibitor; least toxic-used for head lice
23
Q
parathion
A
OP insecticide; ChE Inhibitor; common agent in OP poisoning
24
Q
tetraethylpyrophosphate
A
OP insecticide; ChE inhibitor
25
sarin
OP nerve gas; ChE inhibitor
26
Soman
OP nerve gas; ChE inhibitor
27
pralidoxime (2-PAM)
Q; AChE reactivator after OP poisoning (before aging) Step 2.
28
Cholinergic antogonist effects
alleviate GI hypermotility, diarrhea; decrease sweating, salivation, acid production; anti-parkinson; anti-motion sickness, amnesia
29
cholinergic anatgonist toxicities (CNS)
hallucinations, amnesia, sedation/excitment
30
cholinergic antagonist toxicities (PNS)
mydriasis, cycloplegia, photophobia, dry eyes, xerostomia, , urinary retention, tachycardia, atropine flush/fever.
31
atropine
cholinergic anatoginist; M selective; T; long; step 1 OP poision; cardiac collapse; anti-parkinson; bronchodilation; decreased secretions; high dose -> lower acid production
32
homatropine
cholinergic anatgonist; M selective; T; inter; topical - mydriasis, cycloplegia
33
scopolamine
cholinergic anatgonist; M selective; T; long; amnesia; motion sickness
34
methscopolamine
cholinergic anatgonist; M selective; Q; long; GI diseases, decrease motility/secretions
35
trihexyphenidyl
cholinergic anatgonist; M selective; T; Inter; anti-parkinson
36
tropicamide
cholinergic anatgonist; M selective; T; short; topical - mydriasis, cycloplegia
37
cyclopentolate
cholinergic anatgonist; M selective; T; inter; topical - mydriasis, cycloplegia
38
ipratropium
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
39
tiotropium
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
40
derafinicin
cholinergic anatgonist; M3 selective (smooth muscle, gland); slow micturition, bladder spasms, urinary urgency
41
solifenacin
cholinergic anatgonist; M3 selective (smooth muscle, gland); slow micturition, bladder spasms, urinary urgency
42
tolterodine
cholinergic anatgonist; M3 selective (smooth muscle, gland); slow micturition, bladder spasms, urinary urgency
43
mecamylamine
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
44
trimethaphan
cholinergic nondepolarizing competitive antagonist; N1 selective (ganglionic blocker); IV, minutes; hypertensive emergency; control bleeding through hypotension
45
N1 gangion blocker effects
orthostatic hypotension, low CO, low TPR, fainting, xerostomia, urinary retention, mydriasis, cycloplegia, low sex function, low GI motility
46
succinylcholine
cholinergic anatogonist; N2 selective noncompetitive depolarizing;rapid hydrolysis by plasma ChE; neuromuscular block.
47
d-tubocurarine (curare)
N2 selective nondepolarizing competitive antagonist; long; no vagal block, some histamine release
48
cisatracurium
N2 selective nondepolarizing competitive antagonist; like curare; intermediate
49
mivacurium
N2 selective nondepolarizing competitive antagonist; like curare; short
50
atracurium
N2 selective nondepolarizing competitive antagonist; like curare
51
pancuronium
ammonia steroid; N2 selective nondepolarizing competitive antagonist; long
52
vecuronium
ammonia steroid; N2 selective nondepolarizing competitive antagonist; long; some ganglion/vagal block, tachycardia, no histamine release
53
nondepolarizing N2 selective anatgonist contraindications
liver/renal dysfunction (impaired drug clearing); myasthenia gravis; may induce hypotension from cross-react with N1, histamine release
54
depolarizing N2 selective anatgonist (succinylcholine) contraindications
ChE mutations; OP poisioning; high EC K+ (CHF, burns, trauma); eye trauma, hi IOP.
55
alpha-1 selctive agonists
contraction/constriction/GI relaxation; vasoconstriction, mydriasis, ejaculation, piloerection, glycogenolysis
56
metaraminol
a1 selective agonist
57
methoxamine
a1 selctive agonist; hypotensive crisis
58
phenylephrine
a1 selective agonist; hypotensive crisis, reduce diffusion of anesthetic from site, alleviate congestion; mydriasis
59
alpha-2 selective agonists
presynaptic (-)feedback on NE release
60
a-methyldopa
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
61
clonidine
a2 selective agonist (adrenergic antagonist); lower NE release from terminal; low TPR, hypotension, low HR, low CO;
62
guanebenz
a2 selective agonist (adrenergic antagonist); lower NE release from terminal; low TPR, elicit hypotension, low HR, low CO;
63
alpha-2 agonist adverse effects
sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation
64
amphetamine
mixed a1,B1 agonist; vasopressor; increase NE release from terminal
65
ephedrine
mixed a1,B1, mild B2 agonist; stress incontinece, orthostatic hypotension, decongestant, brochodilation, increase NE release from terminal
66
epinephrine
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
norepinephrine
a, B1>>>B2 agonist, up BP, CO, HR, vasoconstriciton, FFA; congestion,
68
B1 selective agonist
increase HR, contractility, CO, lipolysis
69
dobutamine
B1 selective agonist; heart failure
70
isoproterenol
B nonselective agonist; vasodilator, B1 -> up CO; B2 -> down MAP
71
B2 selective agonist
dilation/relaxation; skeletal muscle/coronary artery vasodilation; bronchodilation, myometrial relax, GI relax
72
albuterol
B2 selective agonist; asthma, bronchodilation
73
metaproterenol
B2 selective agonist; asthma, bronchodilation
74
terbutaline
B2 selective agonist; asthma, bronchodilation; relax pregnant uterus
75
D1 agonist
renal splnachnic vasodilation
76
D2 agonist
presynaptic (-)feedback on NE release; postsynaptic in CNS
77
bromocriptine
CNS D2 agonist; anti-parkinson; PNS effects: postural hypotension, cardiac arrhythmia
78
dopamine
a1,B1,D1,2 agonist; shock therapy
79
fenoldapam
D1>>>D2 agonist; renal, splanchnic vasodilaton
80
a1 selective blockers
vasodilaton, decrease MAP, urinary obstruction, pheochromocytoma
81
doxazosin
a1 selective blocker; urinary obstruction relief
82
prazosin
Highly selective a1 selective blocker; elicits no tachycardia; oral, 12hrs; mild/moderate hypertension; urinary obstruction from BPH
83
tamsulosin
a1 selective blocker; urinary obstruction relief
84
terazosin
a1 selective blocker; urinary obstruction relief
85
phenoxybenzamine
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
phentolamine
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
labetolol
mix adrenergic antagonist
88
B1 selective antagonist
used with diuretics from hypertension therpay
89
atenolol
B1 blocker; inter-long; anti-hypertensive
90
betaxolol
B1 blocker; long; glaucoma
91
metaprolol
B1 blocker; inter; anti-hypertensive; angina pectoris; recurrent MI protection
92
nadolol
B nonselective blocker; long; anti-HTN
93
pindolol
B nonselective blocker; inter; anti-HTN
94
propranolol
B nonselective blocker; inter; Anti-HTN, angina, anti-arrhythmia, migraine, recurrent MI protection
95
timolol
B nonselective blocker; inter; anti-htn; angina; lower IOP, recurrent MI protection
96
guanethidine
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
reserpine
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
cocaine
Amine I tronsport inhibitor; vasoconstriction, tachycardia, mydriasis; hemostasis during surgery
99
DMI (tricyclic antidepressant)
Aminte I transport inhibitor; target: CNS. increase NE in synapse
100
tyramine
NE releasing agent by displacing from vesicle. found in cheeses, can raise BP when on MAO inhibitors.
101
pseudoehpedrine
a,B agonist; NE releasing agent; decongestant
102
azothioprine
immunosupressant; block purine synthesis by incorporating nucleotide thio-gaunine. uses: renal transplant, AI; adverse: myelosuppression, nausea, vomiting
103
cyclophsophamide
immunosuppressant; DNA linking -> damage to proliferating cells; uses: AI disease, bone marrow transplant; adverse: meylosuppression
104
leflunomide
immunosuppressant; blockk pyrimidine synthesis; uses: RA, AI disease; adverse: myelosuppression,heptatotoxicity, diarrhea
105
methotrexate
immunosuppressant; dihydrofolate reducatese inhibitor; block thymidine and purine synthesis; uses: RA, AI; adverse: myelosuppression, heptotoxicity
106
mycophenolate-mofetil
immunosuppressant; inosine monophasphate dehydrogenase inhibitor, block purine synthesis; uses: solid organ transplant, alternative to cyclosporin, some AI diseases; adverse: myelosuppression, nausea, vomiting
107
prednisone (immunosuppression)
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
sirolimus (rapamycin)
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
cyclosporin
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
tacrolimus
immunosuppressant; + FKBP12 inactivate calcineurin -> no activation of NF-AT; uses: same as cyclosporin, 100x potency; adverse: same as cyclosporin
111
Anti-Tcell globulin (ATG)
immunosuppressant; purified animal anti-Tcell Ig; prolonged T cell depletion (1 year); adverse: cytokine release syndrome, potential anaphylaxis
112
muromonab-CD3 (OKT3)
anti-CD3 (tcell) Ig; target all circulation T cells; uses: acute organ rejection; adverse: massive cytokine release syndrome, potential anaphylaxis,
113
alentuzumab
anti-CD52 Ig; target circulation leukocytes (lymphocytes, macrophages, neutrophils, NK cells) proloned immune suppression; adverse: myelosuppression
114
basiliximab
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
Rh(d) Ig
Prevention of fetal hemolytic syndrome by passive immunity of Rh- mother
116
belatecept
fusion protein B7 ligand/Ig Fc domain; blocks co-stimulation -> anergy; uses: kidney transplant; adverse: anemia, neutropenia, susceptible to EBV infection
117
IL-2
Immune stimulant; increase T cell proliferation; uses: metastatic melanoma, renal cell carcinoma; adverse: capillary leak syndrome, hypotension, low perfusion, lack of specificity
118
INF-gamma
immune stimulant; increase Th1 response, macrophage activation, cytotoxicity for severe recurrent infections (intracellular)
119
bacillus calmette-guerin (BCG)
immune stimulant adjuvant; attenuated live bacillus; increase antigen presentation activity; adverse: potential systemic inflammation (shock)
120
ceterizine
2nd gen H1 antagonist; reduced CNS effects; reduced non H1 effects
121
Non-H1 effects of anti-histamines
antagonost: cholinergic, adrenergic, seretonin, promethazine (anesthesia)
122
cyclizine
1st gen H1 antagonist; motion sickness; adverse: CNS sedation, nonH1 effects
123
dimenhydrinate
1st gen H1 antagonist; motion sickness; (dramamine); adverse: CNS sedation, nonH1 effects
124
diphenhydramine
1st gen Hq antagonist; motion sickness (benadryl); advese: CNA sedation, nonH1 effects
125
H1 antagonist uses
allergic rhinitis, urticaria; motion sickness, emesis
126
fexofenedine
2nd gen H1 antagonist; reduced CNS, nonH1 effects
127
loratadine
2nd gen H1 antagonist; reduced CNS, nonH1 effects
128
adalimumab
human anti-TNFa; RA, Chrons disease, inflammation
129
infliximab
humanized anti-TNF1; RA Chrons, inflammation
130
etanercept
fusion protein; TNFa receptor + Fc domain IgG; RA, Chrons, inflammation
131
anakinra
competitive IL-1r antagonist; RA and other inflammatory diseases; short half-life, daily injection
132
Aspirin
NSAID; analgesic/antipyretic, cardiovascular prophylaxis
133
diclofenac
NSAID; Rx arthritis/anti-inflammatory
134
ibuprofen
NSAID; analgesic/antipyretic
135
indomethacin
NSAID; RX arthritis/anti-inflammatory; Intolerance: GI effects
136
ketorolac
NSAID; post surg analgesic
137
naproxen
NSAID; analgesic/antipyretic; RX anti-inflammatory
138
Aspirin Intolerance
Salicilysm: hyperventilation, tinnitus, vertigo, emesis, sweating
Reye's Syndrome: viral disease/vaccination -> acute encephalopathy, fatty liver disease
139
NSAID toxicity
Acute renal failure, GI ulceration, prolonged bleeding (aspirin), increased CV event (not aspirin)
140
misoprostol
PGE analog; protective against NSAID-indiced GI ulcers; given with diclofenac
141
Celecoxib
COX2 selective inhibitor; analgesic/antipyretic; less GI, platelet effects; for chronic NSAID use; increased CV/stroke
142
acetominephen
nonselective COX inhibitor; inhibited by peroxides at inflammation; not anti-inflammatory; no GI, CV, platelet effects; analgesic/antipyretic; hepatotoxicity
143
rofecoxib
COX2 selective inhibitor; analgesic/antipyretic; less GI, platelet effects; for chronic NSAID use; increased CV/stroke; OFF MARKET
144
prednisone (anti-inflammatory)
increased production of annexins -> inhibition of PLA2 and AA->leukotriene/prostaglandin production
repressed expression of IL-1, TNFa and IL-8 (chemotaxin)
145
PGE
relax smooth muscle: GI circular, bronchial, vasodilation; constrict smooth muscle: GI long., uterine; hyperalgesia
146
PGI/prostacyclin
relax bronchial, uterine, vasodilation; inhibit aggregation; antogonize TXA; hyperalgesia
147
TXA
vasoconstriction; promote aggregation; antagonize PGI
148
Salmeterol
long acting aerosolized B2 agonist; maintenance therpay with fluticasone
149
beclomethasone
aerosolized corticosteroid; long term reduction of asthma symmptoms
150
budesomide
aerosolized corticosteroid; long term reduction of asthma symmptoms
151
fluticasone
aerosolized corticosteroid; long term reduction of asthma symmptoms
152
triamcinolone
aerosolized corticosteroid; long term reduction of asthma symmptoms
153
montelukast
LTD4 receptor antagonist; reduce bronchoconstriction and edema; leukotriene modulator; allows reduction of steroid dose; asthma prophylaxis
154
zafirlukast
LTD4 receptor antagonist; reduce bronchoconstriction and edema; leukotriene modulator; allows reduction of steroid dose; asthma prophylaxis
155
zileuton
Lipoxygenase inhibitor; blocks productino of leukotrienes from AA; hepatotoxic
156
cromolyn
inhibit degranulation from mast cells; Ca channel blocker?; Cl channel clocker
157
nedocromil
inhibit degranulation from mast cells; Ca channel blocker?; Cl channel blocker
158
theophylline
methyxanthine; inhibitor of phosphdiesterase degredation of cAMP (B2 pathway to smooth muscle relaxation) -> brochodilation
159
LTB4
neutrophil chemotaxis
160
LTD4
increased capillary permeability, bronchoconstriction, eosinophil chemotaxis, degranulation
