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Heme Pharm > Mechanism > Flashcards

Mechanism Flashcards

1
Q

replaces clotting factors, fibrinogen, protein S, protein C, and antithrombin

A

Fresh frozen plasma

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2
Q

disrupt DNA and RNA synthesis, converted to 5-fluorouracil, by fungi

A

Flucytosine

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3
Q

chlorinated to form nitrenium ion; toxic to bone marrow precursors

A

clozapine

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4
Q

These drugs form a ternary complex with topoisomerase II and DNA

A

Doxorubicin, daunorubicin - anthracyclines

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5
Q

inhibits dihydroorotate dehydrogenase, leading to inhibition of pyrimidine synthesis

A

Leflunomide

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6
Q

Direct Factor Xa inhibitor not requiring antithrombin

A

Rivaroxaban

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7
Q

inhibits the re-ligation of the broken DNA strands, leading to apoptosis

A

Doxorubicin, daunorubicin - anthracyclines

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8
Q

concentrates in parasite food vacuoles; increases free heme and toxicity to parasite

A

Chloroquine

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9
Q

monoclonal to T cells

A

Alemtuzumab

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10
Q

monoclonal to B cells

A

rituximab

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11
Q

competitive inhibitors of dihydrofolate reductase

A

Trimethoprim and pyrimethamine

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12
Q

binds to both the active site and a second site on the thrombin molecule

A

Lepirudin

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13
Q

Incorporates into the growing viral DNA chain results in premature chain termination due to inhibition of binding with the incoming nucleotide, cytosine

A

Lamivudine (nucleoside analog of cytosine), Emtricitabine (fluorinated analog of lamivudine)

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14
Q

complex of ferric oxyhydroxide with polymerized dextran; The complex must be phagocytized by (1) cells before iron becomes available

A

Iron dextran 1. reticuloendothelial

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15
Q

inhibit incorporation of PABA into dihydropteroic acid interfering with folate metabolism

A

Sulfonamides: sulfamethoxazole and sulfadiazine

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16
Q

binds DNA and chelates iron, leading to formation of free radicals that cause single- and double-strand DNA breaks

A

Bleomycin

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17
Q

bind to antithrombin and accelerate the rate at which it inhibits various coagulation proteases, but less effective in inhibiting thrombin

A

Enoxaparin: low molecular weight heparin

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18
Q

Delivered to transferrin more readily

A

Sodium Ferric gluconate and iron sucrose

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19
Q

active triphosphate derivative inhibits DNA polymerase, DNA primase, DNA ligase, and ribonucleotide reductase, and is incorporated into DNA and RNA

A

Fludarabine (antimetabolite, purine analog)

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20
Q

drugs bind β-tubulin blocking its ability to polymerize with α-tubulin into microtubules

A

Antimitotic drugs - Vincristine and vinblastine (vinca alkaloids)

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21
Q

concentrates in parasite food vacuoles; increases free heme and toxicity to parasite

A

Amodiaquine

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22
Q

Active drug = Cycloguanil, a triazine metabolite

A

Proguanil

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23
Q

inhibits vitamin K epoxide reductase which is the enzyme that regenerates reduced vitamin K; action occurs in liver

A

warfarin

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24
Q

inhibits synthesis of phosphoribosylamine by inhibiting phosphoribosylpyrophosphate synthetase and phosphoribosylpyrophosphate aminotransferase

A

Mercaptopurine (antimetabolite, purine analog)

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25
Q

bind only to the active site of thrombin

A

Argatroban and dabigatran

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26
Q

bind competitively to plasminogen blocking the binding of plasminogen to fibrin and subsequent conversion fo plasmin

A

Aminocaproic acid; Tranexamic acid

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27
Q

The false nucleotide also causes DNA damage upon intercalation

A

Mercaptopurine (antimetabolite, purine analog)

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28
Q

“Erythrocytic forms of all four human malarial species Folate synthesis blockade ‐ selective ↓ of plasmodial dihydrofolate reductase activity”

A

Pyrimethamine Proguanil

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29
Q

displaces the repressor, activating the differentiation program, and promoting degradation of the PML-RAR- fusion gene

A

Tretinoin

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30
Q

“Active against hepatic-stage schizonts Gametocidal “

A

Primaquine

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31
Q

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

A

Anakinra

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32
Q

block the enzyme lanosterol 14-α-demethylase inhibiting the conversion of lanosterol to ergosterol

A

azoles

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33
Q

incorporation into RNA inhibits RNA function, RNA processing, and mRNA translation

A

Fludarabine (antimetabolite, purine analog)

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34
Q

Alkaloid from bark of cinchona tree Rapid-acting, highly effective schizonticide against all four human malaria parasites Gametocidal against P. vivax and P. ovale but not P. falciparum

A

Quinine and Quinidine

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35
Q

blocks calcineurin and inhibits IL-2, IL-3; IL-4, IFN-γ synthesis

A

Tacrolimus (FK506)

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36
Q

Incorporates into the growing viral DNA chain results in premature chain termination due to inhibition of binding with the incoming nucleotide, adenosine

A

Tenofovir (nucleotide analog of adenosine)

37
Q

increases drug exposure, thereby prolonging the drug’s half-life and allowing reduction in frequency; in addition, thegenetic barrier to resistance is raised

A

Ritonavir

38
Q

reduced to tetrahydrofolic acid which acts as an acceptor of one-carbon units

A

folate

39
Q

causes release of factor VIII and vWF from endogenous endothelial storage site

A

DDAVP (desmopressin)

40
Q

inhibits fungal mitosis by interacting with polymerized microtubules

A

Griseofulvin

41
Q

potent inhibitor of DNA polymerase, both in replication and repair; the triphosphate form competes with the physiological substrate deoxycytidine 5’-triphosphate (dCTP) for incorporation into DNA by DNA polymerases.

A

Cytarabine (antimetabolite, a cytidine analog)

42
Q

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

A

Nonnucleoside: Efavirenz

43
Q

vitamin K1 - found in green leafy vegetables

A

Phytonadione

44
Q

causes a permanent conformational change in antithrombin

A

fondaparinux

45
Q

block HIV-1 integrase activity, preventing viral DNA from integrating with cellular DNA

A

Integrase inhibitor: raltegravir

46
Q

Binds specifically and selectively to CCR5

A

Penetration blocker: Maraviroc

47
Q

competitively binds to the ATP binding site on the bcr-abl which inhibits phosphorylation of proteins involved in CML clone proliferation

A

Tyrosine kinase inhibitor - Imatinib

48
Q

prodrug that is converted in the liver to MTIC which interrupts DNA replication by causing methylation of guanine

A

Dacarbazine

49
Q

S-FKBP complex leads to inhibition of mTOR

A

sirolimus

50
Q

inhibits dihydrofolate reductase

A

Methotrexate

51
Q

have lympholytic effects and are able to suppress mitosis in lymphocytes

A

Glucocorticoids - Prednisone, Dexamethasone

52
Q

inhibits reverse transcriptase by competing with endogenous deoxynucleotides (adenosine) for the catalytic site of the enzyme

A

Tenofovir (nucleotide analog of adenosine)

53
Q

inosine monophosphate dehydrogenase (IMPDH) inhibitors, leading to inhibition of purine synthesis

A

MPA or MMF; (Mycophenolic Acid and Mycophenolate Mofetil)

54
Q

oxidized to form reactive hydroxylamine; toxic to bone marrow precursors

A

dapsone

55
Q

Also required for the active forms of proteins C and S

A

Phytonadione

56
Q

“Disrupts plasmodia mitochondria electron transport Acts against Tissue/Erythrocytic schizonts”

A

“Atovaquone-proguanil aka Malarone”

57
Q

Xa and IIa inhibitors

A

heparin and LMWH

58
Q

production of free radicals following iron catalyzed cleavage of artemisinin endoperoxide bridge in the parasite’s food vacuole inhibition of parasite’s calcium ATPase

A

Artemisinin

59
Q

Produced using recombinant DNA technology using cultured cells transfected with the human factor VIII/IX gene

A

Recombinant factor VIII/IX

60
Q

catalyzes the hydrolysis of circulating asparagine to aspartic acid and ammonia depriving malignant cells of the asparagine necessary for protein synthesis, leading to cell death

A

Asparaginase

61
Q

contain vitamin K-dependent factors II, VII, IX, and X, activated factor VII and IX

A

Prothrombin complex concentrate (PCC) and activated PCC (aPCC)

62
Q

These drugs do not compete with nucleoside triphosphates nor require phosphorylation to be active

A

Nonnucleoside: Efavirenz

63
Q

bind to antithrombin and accelerate the rate at which it inhibits various coagulation proteases

A

Unfractionated heparin and fondaparinux

64
Q

biotransformed into false purine nucleotides which inhibit phosphoribosylpyrophosphate synthetase and phosphoribosylpyrophosphate aminotransferase

A

Mercaptopurine (antimetabolite, purine analog)

65
Q

prevent post-translational cleavage of the Gag-Pol polyprotein by protease resulting in the production of immature, noninfectious viral particle

A

Protease inhibitors: Atazanavir, Darunavir, Ritonavir

66
Q

potent CYP3A4 inhibitory properties used to “boost” the levels of other protease inhibitors when given in combination, thus acting as a pharmacokinetic enhancer rather than an antiretroviral agent

A

Ritonavir

67
Q

Inhibits clot lysis for treatment of oral bleeding because of the high concentration of fibrinolytic enzymes found in saliva

A

Aminocaproic acid; Tranexamic acid

68
Q

has a high affinity for ferric iron. Once bound with iron, it is excreted in the urine

A

Deferoxamine has a high affinity for ferric iron. Once bound with iron, feroxamine is excreted in the urine

69
Q

Binds to the CD20 antigen on the surface of pre-B cells and mature B cells, resulting in the depletion of B cells from peripheral blood, lymph nodes, and bone marrow

A

Rituximab

70
Q

highly reactive alkyl groups that forms covalent bonds between guanines resulting in cross-linking between two DNA strands. DNA cannot be replicated resulting in cell death

A

Cyclophosphamide

71
Q

36 amino acid peptide which binds to gp41 inhibiting fusion of HIV with the target cell

A

Fusion inhibitor: Enfuvirtide

72
Q

Antibodies against CD25 – the high affinity IL-2 receptor (CD25 – expressed only on activated T-cells)

A

Daclizumab and Basiliximab

73
Q

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

A

echinocandins (capsofungin)

74
Q

Antifibrinolytic

A

Aminocaproic acid; Tranexamic acid

75
Q

Effective for patients with adequate endogenous stores of vWF

A

DDAVP (desmopressin)

76
Q

selectively toxic because in human cells the major sterol is cholesterol rather than ergosterol

A

The polyenes, the azoles, and terbinafine

77
Q

Directly interact with the thrombin molecule; Able to inhibit circulating and clotbound thrombin

A

Direct thrombin inhibitors: Lepirudin; Argatroban and dabigatran

78
Q

Down-regulates expression of cytokines IL-1, IL-4 and TNF-α

A

Glucocorticoids

79
Q

Binds to ergosterol in fungal cell membranes forming pores or channels

A

Polyenes: Amphotericin B

80
Q

non-specific (binds TNF-α and TNF-β) and inhibits both – approved for rheumatoid arthritis

A

Etanercept

81
Q

cell-cycle-specific agents blocking cells in mitosis (M phase). Cell division is arrested in metaphase.

A

Antimitotic drugs - Vincristine and vinblastine (vinca alkaloids)

82
Q

↓Bacterial protein synthesis (also ↓Protein synthesis in plasmodial species)

A

Doxycycline

83
Q

can form radical intermediates, which in turn can react with oxygen to produce superoxide anion radicals which attack DNA and oxidize DNA bases

A

Doxorubicin, daunorubicin - anthracyclines

84
Q

integrase strand transfer inhibitor (INSTI)

A

Integrase inhibitor: raltegravir

85
Q

blocks calcineurin and inhibits IL-2 synthesis

A

cyclosporine

86
Q

inhibits reverse transcriptase by competing with endogenous deoxynucleotides (cytosine) for the catalytic site of the enzyme

A

Lamivudine (nucleoside analog of cytosine), Emtricitabine (fluorinated analog of lamivudine),

87
Q

TNF-α-specific inhibitors - approved for rheumatoid arthritis, Crohn’s disease, ulcerative colitis

A

Infliximab and Adalimumab

88
Q

Strong blood schizonticidal activity against P. falciparum and P. vivax

A

Mefloquine

89
Q

Cofactor in the activation of factors II, VII, IX, and X

A

Phytonadione

Heme Pharm (13 decks)

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