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These Pharm Cards Have Been Compromised > Exam IV > Flashcards

Exam IV Flashcards

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
Q

rilonacept

mech, use, admin, SE

A

binds to IL-1 molecule!

admin subQ

RA; admin with methotrexate

NOT USED with TNF inhibitors (synergistic)

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19
Q

bleomycin

mech, SE

A

intercalates with DNA→strand breakage

pulmonary fibrosis

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20
Q

hydroxychloroquine

mech, SE (3)

A

taken up by macrophages, concentrated in lysosomes, and interferes with antigen processing

GI dysfunction, dermatitis,
irreversible retinal damage

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21
Q

ergot alkaloids (2)

mech, SEs (2)

A

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

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21
Q

imitinib

mech, use, admin, SE

A

protein kinase inhibitor of a kinase which turns off cell apoptosis

tx chronic myelogenous leukemia (CML)

given orally→causes edema

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21
Q

trastuzumab

mech, use

A

blocks a HR2 receptor (a tyrosine kinase)

tx breast cancer

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22
Q

tocilizumab

mech, use

A

binds to IL-6 receptors on T-cells

RA

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23
Q

5-fluorouracil

mech

A

pyrimidine analog inhibiting thymidylate syntetase→inhibits thymidine synthesis

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24
Q

ixabepilone

mech

A

binds to microtubules

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25
Q

natalizumab

mech, use, SE

A

inhibits to α-integrins (INHIBITS RECEPTORS) on CD4 T-Cells

Crohn’s Dx, MS

linked with progressive multifocal leukoencephalopathy (viral dx of CNS)

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25
Q

anastrozole

mech, use

A

inhibits aromatase enzyme (which converts testosterone to estrogen)

treats ladycancers

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26
Q

specific H2 blockers (4)

mech, SE

A

blocks peripheral H2 receptors (doesn’t cross BBB)

cimetidine (has antiandrogenic efx→gynecomastia/galactorrhea)

ranitidine
tamotidine
nizatidine

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27
Q

aspirin

where most readily absorbed? mech?

A

most readily absorbed in stomach (weak acid)

inhibits cyclooxygenase (both COX1 adn COX2)→ ↓prostaglandin synthesis

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28
Q

golimumab

mech, use

A

binds to TNF molecule

ulcerative colitis, psoriatic arthritis, RA

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29
Q

What are the desired effects of aspirin and other NSAIDs (4)? What are the SE/toxicities (8)? Where is it contraindicated (2)?

A

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
Q

What is the mechanism of action for glucocorticoids?

A

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
Q

NIBs

mechanism

A

kinase inhibitors

32
Q

etoposide

mech

A

inhibits topoisomerase II→irreperable DNA breaks

34
Q

propionic acid derivatives (7)

mech, SE

A

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
Q

irinotecan

mech

A

topoisomerase I inhibitor

37
Q

omalizumab

mech, admin?

A

anti IgE mAB

IV only

37
Q

tacrolimus

mech, use, SE (5)

A

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
Q

non propionic acid, non acetic acid derived (6)

mech, SE

A

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
Q

inhibitors of leukotriene system (3)

mech

A

zileuton inhibits E2 5-lipoxygenase in immune cells

zafirlukast, montelukast block leukotriene receptors on pulmonary smmm

40
Q

bortezomib

mech, use

A

inhibits proteasome→inhibits antigen presentation by APCs

tx multiple myeloma

41
Q

prednisone

mech, use

A

inhibits immune functioning

treats neoplasia of immune system (like leukemias, lymphomas)

42
Q

basiliximab

mech, use, SE (4)

A

mAB that blocks IL-2 receptor

used with cyclosporine A

hypersensitivity rxns (chimeric)
HTN, bronchospasms, pulmonary edema
43
Q

leuprolide

mech, use

A

stimulates GnRH receptor→initially ↑testosterone, then downregulates receptor and then ↓↓↓testosterone synthesis

tx prostate tumors

45
Q

infliximab

mech, use, SE (5), admin

A

mAB binding to TNF molecule

RA, Chrohn’s disease

admin IV

hypersensitivity (chimeric MAB);
itching, hypotension, fever
worsens TB/fungus infections

46
Q

tamoxifen

mech, use, SE (2)

A

blocks estrogen receptor

treats ladycancers

retinal changes, ↑cataract formation

48
Q

longer acting agents for asthma treatment

mech, admin, SE (3)

A

formoterol, arformoterol, salmeterol, indicaterol

specific ß2 agonist

inhaled usually

tremor, tachycardia, ♥ palpitations (due to ß1 effect)

50
Q

Cholinergic blockers for COPD treatment (2)

mech? SE?

A

ipratropium, tiotropium

muscarinic receptors blockers on pulmonary smmm

dry mouth

51
Q

highest potency glucocorticoids

A

dexamethasone, betamethasone

ISA:25
MCA: 0.01
duration 36-54h

52
Q

carfilzomib

mech, use

A

inhibits proteosomes→inhibits antigen presentation by APCs

tx multiple myeloma

53
Q

fulvestram

mech, use, SE (2)

A

blocks estrogen receptor

treats ladycancers

retinal changes, cataract formation

55
Q

mast cell inhibitors (2)

mech

A

cromolyn sodium, nedocromil

inhibits release of mediators from immune cells by INHIBITING Cl- CHANNELS, which ↓Ca++ uptake

55
Q

azathioprine

mech, use, SE

A

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
Q

leflunomide

mech, SE (4)

A

antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase

diarrhea, abdominal pain
teratogen (especially for lymphocytes)
inhibits CYP450

57
Q

sirolimus

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

58
Q

skeletal side effects of glucocorticoids (3)

A

osteoporosis

osteonecrosis

↓growth in children

59
Q

vinblastine

mech, admin

A

binds to microtubules→blocks cell mitosis

given IV

60
Q

Shorter acting agents for treatment of asthma (1+5)

mech? admin? SE (3)?

A

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
Q

teriflunomide

mech, SE

A

prodrug; converted to antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase

diarrhea, abdominal pain
teratogen (especially for lymphocytes)

62
Q

flutamide

mech, use

A

blocks intracellular androgen receptor

tx prostate tumors

62
Q

abiraterone

mech, use

A

inhibits 17-hydroxylase lyase (CYP17)→ ↓testosterone synthesis

tx prostate tumors

63
Q

THE non-narcotic analgesic

mech, tox (2)

A

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
Q

bevacizumab

mech

A

blocks VEGF (vascular endothelial growth factor)→inhibits formation of blood supply to tumors

65
Q

glucocorticoids used for asthma tx (7)

mech? clinical use? admin? SE (2)?

A

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
Q

CV side effects of glucocorticoids (5)

A

stroke, CHF, MI, HTN, ↑intracranial pressure

68
Q

celecoxib

mech, use, SE

A

specific COX2 inhibitor

used to treat arthritis

↑MI, ↑stroke due to greater effect of drug on PGI2 than TXA2

70
Q

second generation antihistamines (4)

mech? difference from first gen? tox? SE (3)?

A

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
Q

least potent glucocorticoids

A

cortisone (a prodrug→no topical admin), hydrocortisone

ISA:1
MCA: 1
duration 8-12h

72
Q

cisplatin

mech, SE(2)

A

alkylates DNA

renal damage, ototoxicity

74
Q

paclitaxel

mech

A

forms abnormal microtubules

76
Q

doxorubicin

mech, admin, SE

A

intercalates with DNA→produces free radicals

given IV

♥ muscle degeneration

77
Q

What are the clinical uses of antihistamines (4)? What are they ineffective in treating?

A

dermatoses (itching, insect bites)
allergic rhinitis/conjunctivitis→ ↓ congestion, sneezing
antiemetic/antinausea→tx motion sickness
sedatives

DO NOT TREAT ASTHMA or COMMON COLD

79
Q

What is the synthetic path for glucocorticoids? Which reactions require P450?

A

cholesterol → pregnenolone → 17-OH pregnenolone → 17-OH progesterone →11-deoxycortisol → cortisol

all require CYP450 except the pregnenolone→17OHpregnenolone reaction

80
Q

What are the effects of the H1 blockers (6) and H2 blockers (1)?

A

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
Q

betalacept

mech, use, SE

A

inhibits CD80, CD86 receptors

for renal transplants

↑malignancy associated

84
Q

cyclophosphamide

mech, admin

A

prodrug which alkylates DNA

oral/IV

85
Q

N-acetyl cysteine

mech

A

used to treat acetaminophen overdose

a reducing agent to ↑glutathione (GSH) levels in liver

86
Q

metabolic side effects of glucocorticoids (3)

A

weight gain

fat redistribution (to abdomen, moon face, buffalo hump)

muscle wasting (thin arms, growth inhibition in children)

87
Q

methotrexate

mech, use, SE

A

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
Q

acetic acid derivatives (3)

mech, SE

A

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
Q

dactinomycin

mech

A

intercalates with DNA→interferes with RNA synthesis

90
Q

cytarabine

mech

A

pyrimidine analog inhibiting DNA polymerase

91
Q

Skin/mucosal damage associated with glucocorticoids (4)

A

easy bruising (skin thinning)

poor wound healing

acne

increased incidence of infection (eg: thrush)

92
Q

anakinra

mech, admin, use, SE

A

blocks IL-1 receptor

admin subcutaneously

RA; admin with methotrexate

NOT USED with TNF inhibitors (synergistic)

93
Q

6-mercaptopurine

mech

A

prodrug purine analog inhibiting enzymes required for purine synthesis

94
Q

mycophenolate mofetil

mech, use, SE

A

specific antimetabolite inhibiting inosine monophosphate dehydrogenase →inhibiting guanosine synthesis

transplants, lupus

GI cell disruption
bonemarrow depression (→thrombocytopoenia, megaloblastic anemia, leukopenia)
95
Q

lomustine

mech, admin

A

prodrug which alkylates DNA

given IV

96
Q

tolfacitinib

mech, SE

A

inhibits Janus Kinase→prevents effect of cytokines on gene expression (JAK-STAT)

↑infection chance, ↑malignancy

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