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Pharm RR Flashcards

1
Q

what is phosphoribosylamine

A

needed for synthesis of purines; mercaptopurine inhibits the enzymes needed to synthesize phosphoribosylamine

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2
Q

form a ternary complex with topoisomerase II and DNA

A

Doxorubicin + Daunorubicin

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3
Q

produce free radicals

A

Doxorubicin + Daunorubicin

Bleomycin

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4
Q

Binds DNA and chelates iron

A

Bleomycin

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5
Q

degraded by a specific hydrolase low in skin and lungs–

A

Bleomycin

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6
Q

highly reactive alkyl groups that forms covalent bonds between guanines

A

Cyclophosphamide

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7
Q

cross-linking between two DNA strands

A

Cyclophosphamide

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8
Q

Acrolein is a metabolite

A

Cyclophosphamide

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9
Q

mesna

A

conjugates acrolein

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10
Q

prodrug that is converted in the liver to MTIC

A

Dacarbazine

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11
Q

Interrupts DNA replication by causing methylation of guanine

A

Dacarbazine

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12
Q

methylation of guanin

A

Dacarbazine

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13
Q

potent inhibitor of DNA polymerase

A

Cytarabine

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14
Q

cytidine analog

A

Cytarabine

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15
Q

Resistance: Occurs due to increased drug inactivation or decrease formation of monophosphate.

A

Cytarabine

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16
Q

severe leukopenia, thrombocytopenia, and anemia.

A

Cytarabine

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17
Q

Inhibits DNA polymerase, DNA primase, DNA ligase, and ribonucleotide reductase

A

Fludarabine

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18
Q

Purine analog; biotransformed into false purine nucleotide

A

Mercaptuopurine

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19
Q

false nucleotide also causes DNA damage upon intercalation.

A

Mercaptuopurine

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20
Q

Degraded by xanthine oxidase and thiopurine methyltransferase

A

Mercaptuopurine

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21
Q

biotransformed to polyglutamate

A

Methotrexate

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22
Q

inhibits dihydrofolate reductase

A

Methotrexate

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23
Q

Drug Interactions:aspirin or piperacillin delay drug excretion and lead to severe myelosuppression.

A

Methotrexate

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24
Q

Drug Interactions: nonsteroidal antiinflammatory agents delay drug excretion and lead to severe myelosuppression.

A

Methotrexate

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25
Binds to the CD20 antigen
Rituximab
26
chimeric (mouse-human) monoclonal antibody
Rituximab
27
reduction in FAS-mediated apoptosis
Imatinib
28
Competitively binds to the ATP binding site on the bcr-abl
Imatinib
29
inhibits phosphorylation of proteins involved in CML clone proliferation
Imatinib
30
Resistance results from mutations in the kinase domain
Imatinib
31
normal tissues are able to synthesize 1) for protein synthesis
1) L-asparagine
32
depriving malignant cells of the asparagine necessary for 1) --> leads to cell death
1) protein synthesis
33
suppress mitosis in the lymphocytes
Glucocorticoids | Prednisone, Dexamethasone
34
displaces the repressor and promotes degradation of the PML-RAR-fusion gene.
Tretinoin
35
Induces lipocortins
Glucocorticoids
36
↓PLA2→ ↓AA
Glucocorticoids
37
Down-regulates expression of cytokines (IL-1, | IL-4 and TNF-α which leads to immunosuppression
Glucocorticoids
38
prevents activation of calcineurin phosphatase activity by Ca2+/calmodulin
Cyclosporine (Cs) and Tacrolimus
39
↓IL-3; IL-4, IFN-γ
Tacrolimus
40
immunosuppressant for transplantation
Tacrolimus
41
hypertension, hyperlipidemia
Cyclosporine
42
hepato-, nephro-, | and neuro—toxicity
Cyclosporine
43
↓Calcineurin phosphatase activity by | Ca2+/Calmodulin
Cyclosporine and Tacrolimus
44
Tacrolimus inhibits
↓IL-3; IL-4, IFN-γ
45
binds to FKBP → S-FKBP complex | → ↓mTOR → ↓Protein synthesis
Sirolimus
46
↓mTOR--> Arrest of T-cell division in G1 phase
Sirolimus
47
use: coronary artery | disease
Sirolimus-eluting stents
48
binds to cyclophilin
CYCLOsporin
49
Prevention of graft versus host | disease
Methotrexate
50
inosine monophosphate | dehydrogenase (IMPDH) inhibitor
Mycophenolic Acid & Mycophenolate Mofetil
51
rate-limiting enzyme in the | synthesis of guanosine in the PURINE syntheis
IMPDH
52
↓NO production by immune cells
Mycophenolic Acid & Mycophenolate Mofetil
53
↓Hydrobiopterin [BH4] levels, which | regulates iNOS in neutrophils
Mycophenolic Acid & Mycophenolate Mofetil
54
autoimmune hemolytic anemia
Mycophenolate Mofetil
55
inhibits dihydroorotate dehydrogenase
Leflunomide
56
inhibition of pyrimidine synthesis
Leflunomide
57
inhibits purine synthesis and proliferation of B cells by inhiting IMPDH
Mycophenolic Acid & Mycophenolate Mofetil
58
Depletion of pyrimidine pool → ↓Lymphocyte expansion
Leflunomide
59
Lymphocytes depend on de novo 1) synthesis for cell replication & clonal expansion after immune cell activation
1) pyrimidine
60
Leukopenia, cardiotoxicity, & ↑Risk of cancer,
Cyclophosphamide
61
Promotes transition from G1 to S phase
mTOR
62
non-specific (binds TNF-α and TNF-β)
Etanercept
63
TNF-α-specific
Infliximab and Adalimumab
64
stimulates IL-6 production → ↑Expression of adhesion molecules → ↑Cell proliferation
IL-1
65
↓IL-1 activity
Anakinra
66
IL-1 Receptor antagonist
Anakinra
67
Blocks IL-1-induced metalloproteinase release from synovial fluid; use for RA
Anakinra
68
Blocks IL-2 receptor aka CD25
Basiliximab | Daclizumab
69
inhibits purine synthesis
MMF (Mycofenolate mofetil) | Azathioprine
70
Induction therapy for renal transplantation
Basiliximab | Daclizumab
71
targets all T cells → Broad | immuno-suppression
Anti-thymocyte globulin (ATG)
72
do not compete with nucleoside triphosphates nor | require phosphorylation to be active
Nonnucleoside: Efavirenz
73
bind directly to reverse transcriptase resulting in allosteric inhibition of RNA- and DNA-dependent DNA polymerase.
Nonnucleoside: Efavirenz
74
Rash which could progress to Stevens-Johnson syndrome
Nonnucleoside: Efavirenz
75
Fetal abnormalities (neural tube defects
Nonnucleoside: Efavirenz
76
boost levels of protease inhibitors
Ritonavir
77
use in pregnant women with HIV
Zidovudine (NRTI)
78
competitive inhibitors of | dihydrofolate reductase
Trimethoprim and pyrimethamine
79
structural analogs of para-aminobenzoic acid (PABA)
Sulfonamides (sulfamethoxazole; sulfadiazine)
80
inhibit incorporation of PABA into dihydropteroic acid interfering with folate metabolism
Sulfonamides (sulfamethoxazole; sulfadiazine)
81
inhibits squalene epoxidase; squalene not converted to lanosterol
Terbinafine
82
Inhibits lanosterol demethylase (LD); ___ to ___
azoles; lanosterol to ergosterol
83
converted to 5-fluorouracil, an | antimetabolite, by fungi
Flucytosine
84
Inhibits GS = β-(1,3)-glucan | synthase;
echinocandins e.g Capsofungin | NOTE: selectively toxic because human cells do not contain β-(1,3)-D-glucan
85
inhibits fungal mitosis by interacting with polymerized microtubules
Griseofulvin
86
Binds to ergosterol in fungal cell membranes forming pores or channels
Polyene such as Amphotericin B
87
remains the therapy of choice for many systemic fungal | infections despite its significant side effects
Polyenes: Amphotericin B
88
not absorbed form the GI tract so it must be | administered intravenously
Amphotericin B
89
insoluble in water so it is available as a | complex with the bile salt deoxycholate or as a lipid preparation
Amphotericin B
90
Amphotericin B Antifungal activity
(a) Aspergillus spp. (b) Candida spp. (c) Cryptococcus neoformans
91
adverse affects less with 1) of | amphotericin B than with the deoxycholate salt
1) lipid preparations
92
Amphotericin B: Infusion reactions (fever, chills); can be prevented with 1)
1) antiinflammatory drugs or meperidine
93
Mutation in ERG11
gene encoding for 14-α-demethylase; fungi becomes resistant to AZOLES
94
Mechanism of fungal resistance | Occurs rapidly if used alone!
flucytosine

Heme Pharm (13 decks)

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