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MODA MVST1b > Chemotherapy > Flashcards

Chemotherapy Flashcards

1
Q

D-cycloserine

A

Structural analogue of D-ala, prevents synthesis of pentapeptide by inhibiting L-Ala racemase, D-Ala-D-Ala synthetase and D-Ala-D-Ala/muramyl tripeptide ligase

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2
Q

Fosfomycin

A

Inhibits pyruvyl transferase required fro the conversion of NAG to NAM.
Treat UTIs

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3
Q

Bacitracin

A

Cyclic polypeptide antibiotic. Forms a tight complex with Mg2+ and bactoprenol pyrophosphate, inhibits the dephosphoylation to bactoprenol phosphate (lipid carrier for NAM-NAG unit). Active for gram + bacteria.

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4
Q

Penicillin, Ampicillin, Amoxicillin, Methicillin

A

Beta-lactam antibiotics. Inhibit peptidoglycan crosslinking transpeptidase enzymes by covalent and irreversible binding as a pseudosubstrate.

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5
Q

Augmentin/Co-amoxiclav

A

Amoxicillin (beta-lactam antibiotic) and beta-lactamase inhibitor clavulanate combination

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6
Q

Clavulanate

A

Beta-lactamase inhibitor

forms a slowly hydrolysing acyl-enzyme intermediate

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7
Q

Vancomycin

A

Glycopeptide antibiotic, binds to D-Ala-D-Ala termini of the pentapeptide in peptidoglycan, so prevents its cross-linking to a neighbouring pentapeptide in another peptidoglycan strand. Effective against C. diff and used IV against gram + cocci such as Enterococcus and Staphylococcus.

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8
Q

Tetracycline

A

Polyketide antibiotic, binds to 16S rRNA in 30S subunit of ribosome. Inhibits movement of aminoacyl-tRNA into the A site.
Effective against a wide range of bacteria - first line against mycoplasma and cholera (also against plasmodium). Drug toxicity associated with binding of calcium in bones and teeth.

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9
Q

Erythromycin

A

14-membered macrolide antibiotic. Binds to 23S rRNA in 50S subunit, and blocks the polypeptide exit tunnel. Drug has a similar antibacterial spectrum as penicillin, suitable second line drug for patients allergic to penicillin.

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10
Q

Clindamycin

A

A lincosamide
Interacts with A and P sites to compete with the binding of loaded tRNA molecules at these positions. Shows activity against certain protozoa including plasmodium too.

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11
Q

Chloramphenicol

A

Blocks aminoacyl tRNA binding to 50S subunit of ribosome. Very effective broad-spectrum antibiotic, but use is restricted because of bone marrow suppression in some cases. Indicated in life threatening infections such as meningitis.

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12
Q

Fusidic Acid

A

Inhibits elongation factor G, and hence the movement of the 30S subunit by one codon along the mRNA. Narrow spectrum against staphylococcal infections.

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13
Q

Synercid

A

Synergistic nonribosomal peptide combination (quinupristin + dalfopristin), blocks polypeptide translocation at 50S subunit of the ribosome by binding to 23S rRNA sites partially overlapping with those targeted by macrolides.

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14
Q

Streptomycin, gentamycin

A

Aminoglycoside antibiotcs, target 30S subunit near A site, decrease fidelity of mRNA translation. Streptomycin nephrotoxic and ototoxic (ear). These effects are reduced for gentamycin. Used against gram - rods Pseudomonas and Proteus. Most streptococci gram + are resistant as gentamycin can’t penetrate the cell, but penicillin and gentamycin have a synergistic effect against some streptococci.

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15
Q

Ciprofloxacin

A

Fluoroquinolone antibiotic, inhibits type II DNA topoisomerases (DNA gyrase and topo IV), and hence inhibits changes in supercoiling required for replication and gene expression
Ciprofloxacin is an FDA-approved drug for Bacillus anthracis, also Pseudomonas infections where oral therapy is preferred (e.g. cystic fibrosis respiratory tract infections)

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16
Q

Rifampin

A

Binds to beta subunit of the DNA-dependent RNA pol, and inhibits initiation of RNA synthesis. Often used to treat Mycobacterium.

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17
Q

Daunorubicin

A

Binds non-covalently. Planar polycyclic anthracycline antibiotic, intercalates in dsDNA and causes local unwinding. Used as anticancer agent. also topoisomerase II inhibitor.

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18
Q

Bleomycin

A

Metal-chelating glycopeptide antibiotic, generates superoxide and hydroxyl radicals, causing single and double strand breaks in DNA. Covalently binding

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19
Q

Mitomycin C

A

Aziridine-containing antibiotic. Alkylates and cross-links at GC. so preventing strand separation during DNA replication and transcription. Covalent binding. Antibiotic and anticancer. G base

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20
Q

Sulfamethoxazole

A

Sulfa drug. P-aminobenzoate analogue that competitively inhibits DHPS in the biosynthesis of tetrahydrofolate (a methyl carrier required for synthesis of dTMP)

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21
Q

Trimethoprim

A

Inhibits DHFR in the biosynthesis of tetrahydrofolate

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22
Q

Co-trimoxazole

A

Combination of sulfamethoxazole and trimethoprim. Co-trimoxazole has been withdrawn as a routine anti-bacterial agent in this country, as result of its being implicated in cases of Stevens-Johnson syndrome (a severe and sometimes fatal allergic reaction). Used in AIDS patients with fungal Pneumocystitis carinii infections.

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23
Q

Valinomycin

A

Cyclic peptide antibiotic that binds K+ and facilitates K+ diffusion across the membrane

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24
Q

Gramicidin A

A

Linear polypeptide antibiotic, forms a homodimeric complex that acts as an ion channel in the membrane

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25
Q

Polymixin

A

Cationic detergent antibiotic containing cyclic peptide and hydrophobic tail, binds to membrane and alters its ion permeability

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26
Q

Amphotericin C

A

Polyene antifungal and antiparasitic, forms pores in the membrane by an ergosterol-dependent mechanism. Drug of choice for most systemic mycoses: Cryptococcus, candida, aspergillus. Also antiprotozoal

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27
Q

Fluconazole

A

Triazole antifungal. Inhibit ergosterol biosynthesis. Used in treatment of athlete’s foot and vaginal candidiasis.

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28
Q

Miconazole

A

Imidazole antifungal and antiprotozoal. Inhibit ergosterol biosynthesis

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29
Q

Melarsen oxide

A

Arsenic compound. Selectively accumulated in Trypanosoma species. Inhibits metabolism. Treat sleeping sickness

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30
Q

Suramin

A

Trypanosomiasis drug of choice. Doesn’t contain toxic metal, so therapeutic index much higher than melarsen. Might act on glycolytic enzymes

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31
Q

Chloroquine and mefloquine

A

Antimalarial 4-aminoquinoline drug - inhibits heme polymerisation in food vacuole of Plasmodium.

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32
Q

Artemisinin

A

Prodrug of dihydroartemisinin, which is active during the stage where the parasite is inside erythrocytes. MODA might be based on production of oxygen radicals

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33
Q

Sulfadoxin

A

Sulfa drug that inhibits DHPS in Plasmodium. Sulfamethoxazole analogue.

34
Q

Pyrimethamine

A

Inhibits DHFR reductase in Plasmodium. Trimethoprim analogue.

35
Q

Fansidar

A

Comibination of sulfadoxin and pyrimethamine analogous to cotrimoxazole. Used in treatment of patients with P.falciparum malaria when chloroquine resistance is suspected and oral treatment is appropriate.

36
Q

Amantadine

A

Blocks fusion of M2 ion channel protein involved in nucleocapsid uncoating of influenza virus. Used predominantly in prophylaxis and treatment of infections by Influenza A virus. Not effective against Influenza B

37
Q

Oseltamivir and Zamanivir

A

Inhibit neuraminidase, a glycoprotein enzyme that plays an essential role in the release of the virion progeny from infected cells and that assists in the movement of the virus particles through the upper respiratory tract.

38
Q

Ganiciclovir

A

Purine analogue. Competitive inhibitor of DA pol but has 3’OH that permits chain extension. Phosphorylated by a phosphotransferase specific to cytomegalovirus.

39
Q

Aciclovir

A

Purine analogue, upon activation by viral thymidine kinase, phosphorylated compound inhibits vira DNA pol. In zovirax cream against herpes simplex infections of the skin and mucous membranes

40
Q

Cidofovir

A

Pyrimidine analogue of cytosine. Inhibits DNA pol of cytomegalovirus

41
Q

Foscarnet

A

Organic analogue of pyrophosphate that inhibits DNA polymerase of CMV and herpes virus

42
Q

Nevirapine

A

Anti-HIV drug, non-nt reverse transcriptase inhibitor

43
Q

Zidovudine (azidothymidine AZT)

A

Nucleoside reverse transcriptase inhibitor, thymidine analogue

44
Q

Saquinavir

A

Inhibitor of HIV protease, which is vital for both viral replication within the cell and release of mature viral particles from an infected cell

45
Q

Which drugs are part of HAART?

A

Nevirapine, Zidovudine, Saquinavir

46
Q

Interferon

A

Immunoregulatory cytokine that is synthesised in response to viral infection. used as antiviral agents against hepatitis B and C, and in AIDS related Kaposi sarcomas.

47
Q

Melphalan

A

Belongs to the class of nitrogen mustard alkylating agents. Either creates interstrand cross links, intrastrand cross links, or GC to AT transitions. Used to treat chronic myeloid leukaemia. Occasionally used against melanoma (accumulates as is a phenylalanine derivative and this is a precursor of melanin). N7

48
Q

Cyclophosphamide

A

Nitrogen mustard alkylating agent. A ‘prodrug’, converted in the liver by Cy P450 to active forms that have chemotherapeutic activity. Main use in treatment of lymphomas, some forms of leukaemia and some solid tumours. N7

49
Q

Lomustine

A

Member of the nitrosoureas class of agents. All contain at least one chloroethyl side chain. Acts by cross-linking DNA to other DNA strands or to protein in a way that dsDNA cannot be replicated. Most commonly used against lymphoma (particularly cutaneous) and melanoma, and tumours in kidney and lung. Has ability to penetrate BBB so used to treat brain cancers. N7 O6

50
Q

Cisplatin

A

Platinum-based drug used to treat various types of cancers, including sarcomas, some carcinomas (small cell lung cancer, ovarian), lymphomas and germ cell tumours. N7 G and A intrastrand cross link between pGpG (65%). Bends DNA towards major groove. Also physical block - inhibits DNA Pol

51
Q

Doxorubicin

A

Anthracycline antibiotic that intercalates in DNA. Planar polycyclic. Local injection. Non-covalent. Also topoisomerase II inhibitor

52
Q

Mitoxantrone

A

Anthracycline agent used in the treatment of certain types of cancer. Mostly metastatic breast cancer, acute myeloid leukaemia, non-Hodgkin’s lymphoma. Non-covalent. Doesn’t have property of quinone-type free radical generation.

53
Q

Actinomycin D

A

Non-covalently binding intercalating agent. Act at transcription initiation complex - stop RNA pol from binding.

54
Q

Methotrexate

A

Antimetabolite and antifolate drug. Acts by inhibiting the mechanism of folic acid - inhibits DHFR and competes with folic acid for active transport into mammalian cells. Replaced more powerful and toxic antifolate aminopterin.

55
Q

Leucovorin

A

Adjuvant used in cancer therapy involving methotrexate. Also used in synergistic combination with 5-fluorouracil. Vitamin activity equivalent to folic acid but doesn’t require DHFR. Salvages normal cells as the tetrahydrofolate requirement of normal cells is much lower.

56
Q

5-fluorouracil

A

Antimetabolites. Pyrimidine analogue. Inhibits thymidilate synthase. Typically administered with leucovorin. Principal use colorectal and pancreatic cancers

57
Q

6-mercaptopurine

A

Analogue of hypoxantine- inhibit nucleotide synthesis (and incorporated into nucleic acids)

58
Q

6-thioguanine

A

Analogue of guanine - inhibit nucleotide synthesis (and incorporated into nucleic acids)

59
Q

Etoposide, Amsacrine

A

Inhibitor of enzyme topoisomerase II. Used to treat lung cancer, testicular cancer, lymphoma, non-lymphocytic leukaemia.

60
Q

Topotecan, Camptothecins

A

Topoisomerase I inhibitor. Used to treat ovarian cancer and lung cancer.

61
Q

Vinblastine

A

Vinca alkaloid and anti-mimotic drug used to treat Hodgkin’s lymphoma, non-small cell lung cancer, breast cancer and testicular cancer. Bind to free tubulin dimers and prevent microtubule assembly –> disappearance of microtubules.

62
Q

Taxol (paclitaxel)

A

Belongs to drug category of the taxanes. Is a mimotic inhibitor used to treat patients with lung, ovarian, breast cancer, head and neck cancer, and advanced forms of Kaposi’s sarcoma. Shift equilibrium between free tubulin dimers and microtubules by shifting it towards assembly.

63
Q

Tamoxifen

A

Orally-active oestrogen receptor antagonist used to treat breast cancer. Problem as can act as an agonist in other tissues like bone and uterus

64
Q

Toremifine

A

Tamoxifen analogue without oestrogen agonist properties. Taken for advanced breast cancer in post-menopausal women.

65
Q

Anastrozole

A

Aromatase inhibitor, aromatase normally converts androgen precursors to estradiol. Used in postmenopausal women with breast cancer to prevent formation of estrogens from peripheral tissues like muscles and fat.

66
Q

Goserlaine

A

Decapeptide analogue of gonadotropin releasing hormone that disrupts endogenous hormonal feedback systems, resulting in the down regulation of testosterone and oestrogen production.

67
Q

Flutamide

A

Oral anti-androgen drug primarily used to treat prostate cancer. Competes with testosterone and DHT for binding to androgen receptors in the prostate gland. So prevents stimulation of growth of prostate cancer cells.

68
Q

Prednisone

A

Synthetic corticosteroid prodrug that is converted by the liver into prednisolone, which is the active agent that inhibits growth of lymphocytes in leukemias.

69
Q

Rituximab

A

anti-CD20 mAb. Hodgkin’s and non Hodgkin’s lymphoma. Can lyse CD20 cells through ADCC, activation of complement cascade, introduction of apoptosis

70
Q

Trastuzumab

A

Herceptin
Humanised mAb against HER2 human epidermal growth factor 2. Overexpressed in 25-30% breast cancers.
IV once a week.
Cardiac side effect risk increased if given with anthracyclines (also cardiotoxic)

71
Q

Bevacizumab

A

Humanised anti-VEGF mAb. Vascular endothelial growth factor. Give with 5-fluorouracil to treat metastatic colorectal cancer, non-small cell lung cancer and breast cancer.

72
Q

Cetuximab

A

Human/Mouse chimeric mAb that binds to extracellular EGFR, so prevents EGFR binding. (stim normally, via RTK, stim cell proliferation and/or cell differentiation).
Reverses resistance of colorectal cancer to irinotecan (topoisomerase inhibitor).

73
Q

Gefitinib and Erlotinib

A

Small moelcule ligand that inhibits activity of activated EGF receptor by blocking its ability to dimerise and so function as a RTK.

74
Q

Imatinib mesylate

A

2-phenylaminopyrimidine derivative that targets RTKs.
Small molecule ligand that targets BCR-ACL protein in chronic myeloid leukaemia.
Also can inhibit RTK activity of c-kit which is expressed in gastrointestinal stroma tumours.
Marketed Glivec.

75
Q

Toceranib, Mastinib

A

Mastocyomas in dog connective tissue

Also used for C-kit mutations in GISTs

76
Q

Izoniazid

A

First line medication used in prevention and treatment of TB. Inhibits the biosynthesis of mycolic acids in cell envelope of mycobacterium tuberculosis.

77
Q

Extended spectrum cephalosporin

A

Active against gram-positive bacteria with increased activity against gram-negative bacteria.

78
Q

Teixobactin

A

Active against gram + bacteria. Inhibits bacteria by binding to lipid II in the peptidoglycan biosynthesis pathway.

79
Q

Linezolid

A

Oxazolidinone. Inhibit protein biosynthesis by interaction with the 23S ribosomal RNA of the 50S ribosomal subunit on or near peptidyltransferase centre.

80
Q

Ramoplanin

A

Glycolipopdepsipeptide against vancomycin resistant enterococci. Forms a complex with lipid pentapeptide intermediates in cell wall biosynthesis to act somewhat like vancomycin.

81
Q

Oritavancin

A

Semisynthetic analogue of vancomycin. Adds biphenyl alkyl substitution so more hydrophobic. May partition the analogue more to the membrane, and alter its ratio of inhibition between transpeptidases and transglycosylases. Restores about 2 logs of efficiency.

MODA MVST1b (11 decks)

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