Flashcards in Pharm RR Deck (94):
1
what is phosphoribosylamine
needed for synthesis of purines; mercaptopurine inhibits the enzymes needed to synthesize phosphoribosylamine
2
form a ternary complex with topoisomerase II and DNA
Doxorubicin + Daunorubicin
3
produce free radicals
Doxorubicin + Daunorubicin
Bleomycin
4
Binds DNA and chelates iron
Bleomycin
5
degraded by a specific hydrolase low in skin and lungs--
Bleomycin
6
highly reactive alkyl groups that forms covalent bonds between guanines
Cyclophosphamide
7
cross-linking between two DNA strands
Cyclophosphamide
8
Acrolein is a metabolite
Cyclophosphamide
9
mesna
conjugates acrolein
10
prodrug that is converted in the liver to MTIC
Dacarbazine
11
Interrupts DNA replication by causing methylation of guanine
Dacarbazine
12
methylation of guanin
Dacarbazine
13
potent inhibitor of DNA polymerase
Cytarabine
14
cytidine analog
Cytarabine
15
Resistance: Occurs due to increased drug inactivation or decrease formation of monophosphate.
Cytarabine
16
severe leukopenia, thrombocytopenia, and anemia.
Cytarabine
17
Inhibits DNA polymerase, DNA primase, DNA ligase, and ribonucleotide reductase
Fludarabine
18
Purine analog; biotransformed into false purine nucleotide
Mercaptuopurine
19
false nucleotide also causes DNA damage upon intercalation.
Mercaptuopurine
20
Degraded by xanthine oxidase and thiopurine methyltransferase
Mercaptuopurine
21
biotransformed to polyglutamate
Methotrexate
22
inhibits dihydrofolate reductase
Methotrexate
23
Drug Interactions:aspirin or piperacillin delay drug excretion and lead to severe myelosuppression.
Methotrexate
24
Drug Interactions: nonsteroidal antiinflammatory agents delay drug excretion and lead to severe myelosuppression.
Methotrexate
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