Pharm RR Flashcards Preview

Heme Pharm > Pharm RR > Flashcards

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

Mechanism of fungal resistance
Occurs rapidly if used alone!

flucytosine