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Heme Pharm > Pharm RR > Flashcards

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
Q

Binds to the CD20 antigen

A

Rituximab

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26
Q

chimeric (mouse-human) monoclonal antibody

A

Rituximab

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27
Q

reduction in FAS-mediated apoptosis

A

Imatinib

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28
Q

Competitively binds to the ATP binding site on the bcr-abl

A

Imatinib

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29
Q

inhibits phosphorylation of proteins involved in CML clone proliferation

A

Imatinib

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30
Q

Resistance results from mutations in the kinase domain

A

Imatinib

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31
Q

normal tissues are able to synthesize 1) for protein synthesis

A

1) L-asparagine

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32
Q

depriving malignant cells of the asparagine necessary for 1) –> leads to cell death

A

1) protein synthesis

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33
Q

suppress mitosis in the lymphocytes

A

Glucocorticoids

Prednisone, Dexamethasone

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34
Q

displaces the repressor and promotes degradation of the PML-RAR-fusion gene.

A

Tretinoin

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35
Q

Induces lipocortins

A

Glucocorticoids

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36
Q

↓PLA2→ ↓AA

A

Glucocorticoids

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37
Q

Down-regulates expression of cytokines (IL-1,

IL-4 and TNF-α which leads to immunosuppression

A

Glucocorticoids

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38
Q

prevents activation of calcineurin phosphatase activity by Ca2+/calmodulin

A

Cyclosporine (Cs) and Tacrolimus

39
Q

↓IL-3; IL-4, IFN-γ

A

Tacrolimus

40
Q

immunosuppressant for transplantation

A

Tacrolimus

41
Q

hypertension, hyperlipidemia

A

Cyclosporine

42
Q

hepato-, nephro-,

and neuro—toxicity

A

Cyclosporine

43
Q

↓Calcineurin phosphatase activity by

Ca2+/Calmodulin

A

Cyclosporine and Tacrolimus

44
Q

Tacrolimus inhibits

A

↓IL-3; IL-4, IFN-γ

45
Q

binds to FKBP → S-FKBP complex

→ ↓mTOR → ↓Protein synthesis

A

Sirolimus

46
Q

↓mTOR–> Arrest of T-cell division in G1 phase

A

Sirolimus

47
Q

use: coronary artery

disease

A

Sirolimus-eluting stents

48
Q

binds to cyclophilin

A

CYCLOsporin

49
Q

Prevention of graft versus host

disease

A

Methotrexate

50
Q

inosine monophosphate

dehydrogenase (IMPDH) inhibitor

A

Mycophenolic Acid & Mycophenolate Mofetil

51
Q

rate-limiting enzyme in the

synthesis of guanosine in the PURINE syntheis

A

IMPDH

52
Q

↓NO production by immune cells

A

Mycophenolic Acid & Mycophenolate Mofetil

53
Q

↓Hydrobiopterin [BH4] levels, which

regulates iNOS in neutrophils

A

Mycophenolic Acid & Mycophenolate Mofetil

54
Q

autoimmune hemolytic anemia

A

Mycophenolate Mofetil

55
Q

inhibits dihydroorotate dehydrogenase

A

Leflunomide

56
Q

inhibition of pyrimidine synthesis

A

Leflunomide

57
Q

inhibits purine synthesis and proliferation of B cells by inhiting IMPDH

A

Mycophenolic Acid & Mycophenolate Mofetil

58
Q

Depletion of pyrimidine pool → ↓Lymphocyte expansion

A

Leflunomide

59
Q

Lymphocytes depend on de novo 1) synthesis for cell replication &
clonal expansion after immune cell activation

A

1) pyrimidine

60
Q

Leukopenia, cardiotoxicity, & ↑Risk of cancer,

A

Cyclophosphamide

61
Q

Promotes transition from G1 to S phase

A

mTOR

62
Q

non-specific (binds TNF-α and TNF-β)

A

Etanercept

63
Q

TNF-α-specific

A

Infliximab and Adalimumab

64
Q

stimulates IL-6
production → ↑Expression of adhesion molecules → ↑Cell
proliferation

A

IL-1

65
Q

↓IL-1 activity

A

Anakinra

66
Q

IL-1 Receptor antagonist

A

Anakinra

67
Q

Blocks IL-1-induced metalloproteinase release from synovial fluid; use for RA

A

Anakinra

68
Q

Blocks IL-2 receptor aka CD25

A

Basiliximab

Daclizumab

69
Q

inhibits purine synthesis

A

MMF (Mycofenolate mofetil)

Azathioprine

70
Q

Induction therapy for renal transplantation

A

Basiliximab

Daclizumab

71
Q

targets all T cells → Broad

immuno-suppression

A

Anti-thymocyte globulin (ATG)

72
Q

do not compete with nucleoside triphosphates nor

require phosphorylation to be active

A

Nonnucleoside: Efavirenz

73
Q

bind directly to reverse transcriptase resulting in allosteric
inhibition of RNA- and DNA-dependent DNA polymerase.

A

Nonnucleoside: Efavirenz

74
Q

Rash which could progress to Stevens-Johnson syndrome

A

Nonnucleoside: Efavirenz

75
Q

Fetal abnormalities (neural tube defects

A

Nonnucleoside: Efavirenz

76
Q

boost levels of protease inhibitors

A

Ritonavir

77
Q

use in pregnant women with HIV

A

Zidovudine (NRTI)

78
Q

competitive inhibitors of

dihydrofolate reductase

A

Trimethoprim and pyrimethamine

79
Q

structural
analogs of para-aminobenzoic acid
(PABA)

A

Sulfonamides (sulfamethoxazole; sulfadiazine)

80
Q

inhibit incorporation
of PABA into dihydropteroic acid
interfering with folate metabolism

A

Sulfonamides (sulfamethoxazole; sulfadiazine)

81
Q

inhibits squalene epoxidase; squalene not converted to lanosterol

A

Terbinafine

82
Q

Inhibits lanosterol demethylase (LD); ___ to ___

A

azoles; lanosterol to ergosterol

83
Q

converted to 5-fluorouracil, an

antimetabolite, by fungi

A

Flucytosine

84
Q

Inhibits GS = β-(1,3)-glucan

synthase;

A

echinocandins e.g Capsofungin

NOTE: selectively toxic because human cells do not contain β-(1,3)-D-glucan

85
Q

inhibits fungal mitosis by interacting with polymerized microtubules

A

Griseofulvin

86
Q

Binds to ergosterol in fungal cell membranes forming pores or
channels

A

Polyene such as Amphotericin B

87
Q

remains the therapy of choice for many systemic fungal

infections despite its significant side effects

A

Polyenes: Amphotericin B

88
Q

not absorbed form the GI tract so it must be

administered intravenously

A

Amphotericin B

89
Q

insoluble in water so it is available as a

complex with the bile salt deoxycholate or as a lipid preparation

A

Amphotericin B

90
Q

Amphotericin B Antifungal activity

A

(a) Aspergillus spp.
(b) Candida spp.
(c) Cryptococcus neoformans

91
Q

adverse affects less with 1) of

amphotericin B than with the deoxycholate salt

A

1) lipid preparations

92
Q

Amphotericin B:
Infusion reactions (fever, chills); can be prevented with
1)

A

1) antiinflammatory drugs or meperidine

93
Q

Mutation in ERG11

A

gene encoding for 14-α-demethylase; fungi becomes resistant to AZOLES

94
Q

Mechanism of fungal resistance

Occurs rapidly if used alone!

A

flucytosine

Heme Pharm (13 decks)

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