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Exam IV Flashcards

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1
Q

daunorubicin

mech, admin, SE

A

intercalates with DNA→produces free radicals

given IV

♥ muscle degeneration

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2
Q

migraine agents (7)

mech, admin, SE

A

TRIPTANS (sumatriptan, rizatriptan, zomitriptan, naratriptan, almotriptan, eletriptan, frovatriptan)

serotonin receptor agonist

admin oral/IV/nasal spray

synergistic effect with MAOIs or SSRIs→serotonin syndrome
(hyperthermia, muscle twitching)

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2
Q

abatacept

mech, use

A

inhibits CD80 and CD86 receptors

treats RA

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3
Q

vincristine

mech, admin

A

binds to microtubules→blocks cell mitosis

given IV

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4
Q

behavioral changes associated with glucocorticoid uses (3)

A

euphoria/depression, psychosis, emotional lability

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4
Q

ustekinumab

mech, use

A

binds to IL-12 and IL-23 molecules

psoriasis

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4
Q

Cyclosporine

mech, use, SE (7)

A

binds to CYCLOPHYLLIN protein→COMPLEX inhibits calcineurin phosphatase
eventually incapacitates T-Cells

tx transplants, psoriasis, dry eye

metab by CYP450
nephrotoxicity, hepatotoxicity
cosmetic changes: hypertrichosis, gingival hyperplasia
↑cholesterol, mild HTN

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4
Q

leucovorin

mech

A

a tetrahydrofolic acid analog which requires DHF Reductase
rescues cells methotrexate toxicity

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5
Q

middle potency glucocorticoids

A

prednisone (a prodrug→no topical admin), prednisolone, triamcinolone

ISA:4
MCA: 0.25
duration 18-36h

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6
Q

ATGAM antithymocyte globulin

mech, use, SE

A

polyclonal antibody

treats acute renal transplant rejection

↑risk for allergic response

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6
Q

methotrexate

mech, SE

A

folic acid antimetabolite inhibiting dihydrofolate reductase

myelosuppression (inhibition of blood cell formation)→fixed with leucovorin

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6
Q

erbulin

mech

A

inhibits microtubules→prevents mitosis, causes apoptosis

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7
Q

GI side effects of glucocorticoids (3)

A

↑risk of ulcers, gastritic, GI bleeding

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9
Q

the methylxanthine used for asthma

mech, SE (5)

A

theophylline

inhibits cAMP phosphodiesterase ENZYME (relaxes smmm by ↓cAMP breakdown)

♥ arrythmias (from heart stimulation)
CNS: tremors, insomnia, seizures
GI upset

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9
Q

ibritumomab

SE

A

its pure mouse, so superduper antigenic

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10
Q

etanercept

mech, admin, use

A

binds to TNF

given subq

RA

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11
Q

certolizumab

mech, use

A

binds to TNF molecule

RA, Chrohn’s Dx

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13
Q

first generation antihistamines (6)

mech? clinical use for each? tox? SE (4)

A

block both central and peripheral H1 receptors

diphenhydramine (sedative, motion sickness)
clemastine (motion sickness)_
chlorpheniramine (NOT A SEDATIVE, uticaria, motion sickness)
hydroxyzine (sedative, uticaria)
promethazine (STRONG sedative, STRONG antiemetic)
tripelennamine (sedative, local anaesthetic)

high TI

dry mouth, blurred vision, constipation (antimuscarinic efx)
synergistic with CNS depressants

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13
Q

topotecan

mech

A

topoisomerase I inhibitor

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14
Q

everolimus

mech, use, SE (3)

A

BINDS to FK-BINDING PROTEIN→COMPLEX inhibits a kinase required for IL-2 induced transcription of cytokines

tx transplantation, psoriasis

renal toxicity
lung toxicity
metab by CYP 450

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15
Q

adalimumab

mech, use

A

binds to TNF molecule

RA

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16
Q

Which agent for asthma treatment is the least selective in its method of action? Which receptors does it bind? What are some side effects (2)? How is it administered?

A

epinephrine

activates ALL α and ß receptors

inhaled or IV

SE: ↑HR (from ß1) and ↑BP (from α1 induced vasoconstriction)

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17
Q

ocular side effects of glucocorticoids (2)

A

cataracts, glaucoma

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18
Q

rituximab

mech, use

A

blocks CD20 receptor

tx Chronic lymphocytic leukemia, RA

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19
rilonacept mech, use, admin, SE
binds to IL-1 molecule! admin subQ RA; admin with methotrexate NOT USED with TNF inhibitors (synergistic)
19
bleomycin mech, SE
intercalates with DNA→strand breakage pulmonary fibrosis
20
hydroxychloroquine mech, SE (3)
taken up by macrophages, concentrated in lysosomes, and interferes with antigen processing GI dysfunction, dermatitis, irreversible retinal damage
21
ergot alkaloids (2) mech, SEs (2)
ergotamine, dihydroergotamine partial 5HT receptor agonists synergistic with 5HT agonists (MAOIs/SSRIs)→serotonin syndrome (HTN, fever, confusion, muscle twitch/rigidity, severe vasospasm) pregnancy category X
21
imitinib mech, use, admin, SE
protein kinase inhibitor of a kinase which turns off cell apoptosis tx chronic myelogenous leukemia (CML) given orally→causes edema
21
trastuzumab mech, use
blocks a HR2 receptor (a tyrosine kinase) tx breast cancer
22
tocilizumab mech, use
binds to IL-6 receptors on T-cells RA
23
5-fluorouracil mech
pyrimidine analog inhibiting thymidylate syntetase→inhibits thymidine synthesis
24
ixabepilone mech
binds to microtubules
25
natalizumab mech, use, SE
inhibits to α-integrins (INHIBITS RECEPTORS) on CD4 T-Cells Crohn's Dx, MS linked with progressive multifocal leukoencephalopathy (viral dx of CNS)
25
anastrozole mech, use
inhibits aromatase enzyme (which converts testosterone to estrogen) treats ladycancers
26
specific H2 blockers (4) mech, SE
blocks peripheral H2 receptors (doesn't cross BBB) cimetidine (has antiandrogenic efx→gynecomastia/galactorrhea) ranitidine tamotidine nizatidine
27
aspirin where most readily absorbed? mech?
most readily absorbed in stomach (weak acid) inhibits cyclooxygenase (both COX1 adn COX2)→ ↓prostaglandin synthesis
28
golimumab mech, use
binds to TNF molecule ulcerative colitis, psoriatic arthritis, RA
29
What are the desired effects of aspirin and other NSAIDs (4)? What are the SE/toxicities (8)? Where is it contraindicated (2)?
antipyretic effects (for fever px only) limited analgesia (due to ↓prostaglandins) antiinflammatory anticlotting (irreversible inhibitor of platelet COX2→↓TXA2) GI upset (gastric irritant→↓PG production via intestinal mucosa) tinnitus ↑respiration ↓miosis, ↓kidney perfusion, hypersensitivity, bronchospasms, inhibits labor contrx with clotting deficiencies contrx in children with viral infections (→Reyes sx)
30
What is the mechanism of action for glucocorticoids?
enter target cell and binds to cytoplasmic receptor steroid-receptor complex dimerizes and binds to steroid response element in DNA lipocortin I is induced→activity of phospholipase A2 is inhibited ↓↓synthesis of prostaglandins and leukotrienes→inhibits immune response
31
NIBs mechanism
kinase inhibitors
32
etoposide mech
inhibits topoisomerase II→irreperable DNA breaks
34
propionic acid derivatives (7) mech, SE
PROs (ibuPROfen, naPROxyn, fenoPROfen, ketoPROfen, flurbiPROfen, oxaPROzin, suPROfen) cyclooxygenase inhibitors (COX1 and COX2) [see aspirin] also in ↑doses: ↑MI, ↑stroke (due to greater effect on PGI prod. than TXA2)
35
irinotecan mech
topoisomerase I inhibitor
37
omalizumab mech, admin?
anti IgE mAB IV only
37
tacrolimus mech, use, SE (5)
binds to FK-BINDING PROTEIN→COMPLEX inhibits calcineurin phosphatase tx transplants nephrotoxic neurotoxic alopecia, diabetes metab by CYP450 | (ultimately prevents activation of Tcells; more efficacious than cyclosporin)
38
non propionic acid, non acetic acid derived (6) mech, SE
pyroxicam, diclofenac, bromfenac, nepafenac, etodolac, nabumetone cyclooxygenase inhibitors (COX1 and COX2) [see aspirin] also in ↑doses: ↑MI, ↑stroke (due to greater effect on PGI prod. than TXA2)
39
inhibitors of leukotriene system (3) mech
zileuton inhibits E2 5-lipoxygenase in immune cells zafirlukast, montelukast block leukotriene receptors on pulmonary smmm
40
bortezomib mech, use
inhibits proteasome→inhibits antigen presentation by APCs tx multiple myeloma
41
prednisone mech, use
inhibits immune functioning treats neoplasia of immune system (like leukemias, lymphomas)
42
basiliximab mech, use, SE (4)
mAB that blocks IL-2 receptor used with cyclosporine A ``` hypersensitivity rxns (chimeric) HTN, bronchospasms, pulmonary edema ```
43
leuprolide mech, use
stimulates GnRH receptor→initially ↑testosterone, then downregulates receptor and then ↓↓↓testosterone synthesis tx prostate tumors
45
infliximab mech, use, SE (5), admin
mAB binding to TNF molecule RA, Chrohn's disease admin IV hypersensitivity (chimeric MAB); itching, hypotension, fever worsens TB/fungus infections
46
tamoxifen mech, use, SE (2)
blocks estrogen receptor treats ladycancers retinal changes, ↑cataract formation
48
longer acting agents for asthma treatment mech, admin, SE (3)
formoterol, arformoterol, salmeterol, indicaterol specific ß2 agonist inhaled usually tremor, tachycardia, ♥ palpitations (due to ß1 effect)
50
Cholinergic blockers for COPD treatment (2) mech? SE?
ipratropium, tiotropium muscarinic receptors blockers on pulmonary smmm dry mouth
51
highest potency glucocorticoids
dexamethasone, betamethasone ISA:25 MCA: 0.01 duration 36-54h
52
carfilzomib mech, use
inhibits proteosomes→inhibits antigen presentation by APCs tx multiple myeloma
53
fulvestram mech, use, SE (2)
blocks estrogen receptor treats ladycancers retinal changes, cataract formation
55
mast cell inhibitors (2) mech
cromolyn sodium, nedocromil inhibits release of mediators from immune cells by INHIBITING Cl- CHANNELS, which ↓Ca++ uptake
55
azathioprine mech, use, SE
prodrug converted to 6-mercaptopurine→inhibits synthesis of purines; inhibits enzymes responsible for GMP synthesis transplants, RA, Crohns Bone marrow depression (→thrombocytopoenia, megaloblastic anemia, leukopenia)
56
leflunomide mech, SE (4)
antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase diarrhea, abdominal pain teratogen (especially for lymphocytes) inhibits CYP450
57
sirolimus mech, use, SE (3)
BINDS to FK-BINDING PROTEIN→COMPLEX inhibits a kinase required for IL-2 induced transcription of cytokines tx transplantation, psoriasis renal toxicity lung toxicity metab by CYP 450
58
skeletal side effects of glucocorticoids (3)
osteoporosis osteonecrosis ↓growth in children
59
vinblastine mech, admin
binds to microtubules→blocks cell mitosis given IV
60
Shorter acting agents for treatment of asthma (1+5) mech? admin? SE (3)?
isoproterenol (less selective) albuterol, pirbuterol, bitolterol, levalbuterol, terbutaline specific ß2 agonists (RECALL: any agent which acts to activate a receptor can cause downregulation and loss of effect!) admin via inhalation tremor, tachycardia, ♥ palpitations (due to ß1 effect)
62
teriflunomide mech, SE
prodrug; converted to antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase diarrhea, abdominal pain teratogen (especially for lymphocytes)
62
flutamide mech, use
blocks intracellular androgen receptor tx prostate tumors
62
abiraterone mech, use
inhibits 17-hydroxylase lyase (CYP17)→ ↓testosterone synthesis tx prostate tumors
63
THE non-narcotic analgesic mech, tox (2)
acetaminophen NOT AN NSAID→NO antiinflammatory or NO antiplatelet efx specific COX2 inhibitor? fewer GI upset than NSAIDs acute liver failure (↓↓glutathione tx with N-acetyl cysteine)
64
bevacizumab mech
blocks VEGF (vascular endothelial growth factor)→inhibits formation of blood supply to tumors
65
glucocorticoids used for asthma tx (7) mech? clinical use? admin? SE (2)?
beclomethasone, budesonide, fluticasone, mometasone, ciclesonide (all inhaled) prednisone, dexamethasone (not inhaled) bind to intracellular receptors→alter DNA trxn→↑lipocortin→inhibits PLA2 synth DOC for chronic asthma infections in mouth (thrush), dysphonia (abnormal speech)
67
CV side effects of glucocorticoids (5)
stroke, CHF, MI, HTN, ↑intracranial pressure
68
celecoxib mech, use, SE
specific COX2 inhibitor used to treat arthritis ↑MI, ↑stroke due to greater effect of drug on PGI2 than TXA2
70
second generation antihistamines (4) mech? difference from first gen? tox? SE (3)?
loratadine, fexofenadine, desloratadine, cetirizine block peripheral H1 receptors ONLY do not cause drowsiness (don't enter CNS) high TI dry mouth, blurred vision, constipation (antimuscarinic efx)
72
least potent glucocorticoids
cortisone (a prodrug→no topical admin), hydrocortisone ISA:1 MCA: 1 duration 8-12h
72
cisplatin mech, SE(2)
alkylates DNA renal damage, ototoxicity
74
paclitaxel mech
forms abnormal microtubules
76
doxorubicin mech, admin, SE
intercalates with DNA→produces free radicals given IV ♥ muscle degeneration
77
What are the clinical uses of antihistamines (4)? What are they ineffective in treating?
dermatoses (itching, insect bites) allergic rhinitis/conjunctivitis→ ↓ congestion, sneezing antiemetic/antinausea→tx motion sickness sedatives DO NOT TREAT ASTHMA or COMMON COLD
79
What is the synthetic path for glucocorticoids? Which reactions require P450?
cholesterol → pregnenolone → 17-OH pregnenolone → 17-OH progesterone →11-deoxycortisol → cortisol all require CYP450 except the pregnenolone→17OHpregnenolone reaction
80
What are the effects of the H1 blockers (6) and H2 blockers (1)?
H1 Blockers: CNS: sedation, anti-nausea drying of mucous membranes local anaesthesia dilates bronchial smmm inhibits secretion of interleukins→ ↓↓immune/inflammation H2 Blockers: inhibits acid secretion from parietal cells
82
betalacept mech, use, SE
inhibits CD80, CD86 receptors for renal transplants ↑malignancy associated
84
cyclophosphamide mech, admin
prodrug which alkylates DNA oral/IV
85
N-acetyl cysteine mech
used to treat acetaminophen overdose a reducing agent to ↑glutathione (GSH) levels in liver
86
metabolic side effects of glucocorticoids (3)
weight gain fat redistribution (to abdomen, moon face, buffalo hump) muscle wasting (thin arms, growth inhibition in children)
87
methotrexate mech, use, SE
antimetabolite for folic acid inhibiting dihydrofolate reductase DOC for early tx of RA affects cells with rapid turnover (GI, bone marrow, fetal development) | (eventually ihiits cell division)
88
acetic acid derivatives (3) mech, SE
indomethacin, tolmetin, sulinadac cyclooxygenase inhibitors (COX1 and COX2) [see aspirin] also in ↑doses: ↑MI, ↑stroke (due to greater effect on PGI prod. than TXA2) Indomethacin is extremely potent COX inhibitor: used for newborns with patent ductus arteriosus causes thrombocytopoenia, aplastic anemia, corneal opacities
89
dactinomycin mech
intercalates with DNA→interferes with RNA synthesis
90
cytarabine mech
pyrimidine analog inhibiting DNA polymerase
91
Skin/mucosal damage associated with glucocorticoids (4)
easy bruising (skin thinning) poor wound healing acne increased incidence of infection (eg: thrush)
92
anakinra mech, admin, use, SE
blocks IL-1 receptor admin subcutaneously RA; admin with methotrexate NOT USED with TNF inhibitors (synergistic)
93
6-mercaptopurine mech
prodrug purine analog inhibiting enzymes required for purine synthesis
94
mycophenolate mofetil mech, use, SE
specific antimetabolite inhibiting inosine monophosphate dehydrogenase →inhibiting guanosine synthesis transplants, lupus ``` GI cell disruption bonemarrow depression (→thrombocytopoenia, megaloblastic anemia, leukopenia) ```
95
lomustine mech, admin
prodrug which alkylates DNA given IV
96
tolfacitinib mech, SE
inhibits Janus Kinase→prevents effect of cytokines on gene expression (JAK-STAT) ↑infection chance, ↑malignancy

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