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2 - MODA > Chemotherapy > Flashcards

Chemotherapy Flashcards

1
Q

Isoniazid

A

Limited spectrum antibiotic. First-line drug for prevention/treatment of TB
Inhibits mycolic acid synthesis

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2
Q

D-cycloserine

A

Antibiotic: structural analogue of D-Ala, prevents D-Ala-D-Ala & therefore pentapeptide inhibiting cell wall cross-linking

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3
Q

Fosfomycin

A

Antibiotic: inhibits pyruvyl transferase (required to convert NAG to NAM)
Approved in USA to treat UTI

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4
Q

Penicillin, Amoxicillin

A

Beta-lactam antibiotics irreversibly covalently bind to transpeptidases inhibiting cell wall peptidoglycan cross-linking

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5
Q

Methicillin

A

Beta-lactamase resistant beta-lactam antibiotic

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6
Q

Vancomycin

A

Glycopeptide antibiotic binds D-Ala-D-Ala preventing transpeptidase activity & cell wall cross-linkage formation
Effective against C. difficile & IV against Gram +ve cocci

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7
Q

Tetracycline

A

Broad spectrum polyketide antibiotic: binds 16 rRNA of 30S subunit
Inhibits tRNA entry to A-site & thus protein synthesis
Destroys gut flora (secondary infection) & stains/impairs structure of bone/teeth
Bacteriostatic

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8
Q

Streptomycin

A

Narrow spectrum aminoglycoside antibiotic: binds 30S subunit & decrease fidelity of translation
Effective against aerobic Gram -ve rods eg Pseudomonas/Proteus (& some Gram +ve bacteria)
Exhibits nephro/ototoxicity (reduced in gentamycin)
Bactericidal

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9
Q

Erythromycin

A

Macrolide antibiotic: binds 50S subunit & blocks polypeptide exit tunnel
Similar spectrum to penicillin so suitable second-line drug for patients with penicillin allergy

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10
Q

Chloramphenicol

A

Very effective broad-spectrum antibiotic: binds 50S subunit & blocks peptidyl transferase activity
Uses limited by bone marrow suppression
Used in life-threatening infections (meningitis, typhus)

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11
Q

Fusidic acid

A

Narrow spectrum antibiotic: inhibits elongation factor G & thus movement of 30S subunit along mRNA
Used in staphylococcal infections (Gram +ve skin/eye infections)

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12
Q

Ciproflaxin

A

Synthetic, broad spectrum fluoroquinolone antibiotic: inhibits type II topoisomerases
Used in anthrax & Pseudomonas infections where oral therapy preferred (eg respiratory tract infections in cystic fibrosis)
Relatively expensive
Bacteriocidal

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13
Q

Rifampin

A

Antibiotic: binds beta-subunit of DNA-dependent RNA polymerase blocking initiation of RNA synthesis
Does not inhibit synthesis in progress
Used in TB
Can be bactericidal

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14
Q

Daunomycin

A

Planar polycyclic anthracycline antibiotic: intercalates in dsDNA and causes local unwinding
Also fragments DNA via ROS formation (gives cardiovascular toxicity)
Used as an anticancer agent

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15
Q

Mitomycin C

A

Aziridine-containing antibiotic: alkylates and cross-links (at guanines) DNA
Prevents strand separation in DNA replication & transcription

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16
Q

Sulfamethoxazole

A

Sulfa drug antibiotic: competitive inhibitor of dihydropteroate synthase in tetrafolate biosynthesis

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17
Q

Trimethoprim

A

Antibiotic: inhibits dihydrofolate reductase in tetrafolate biosynthesis

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18
Q

Co-trimoxazole

A

Combination drug of sulfamethoxazole & trimethoprim causing rapid bactericidal effects (either on own have slow bactericidal effects)
Use discontinued in UK because implicated in Stevens-Johnson syndrome (severe & potentially fatal allergic reaction)
Still used in AIDS patients with fungal Pneumocystis carinii infections

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19
Q

Valinomycin

A

Cyclic peptide ionophore antibiotic: binds K+ ion and causes membrane depolarisation by facilitating diffusion across membrane
Compromises homeostasis, growth & cell viability

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20
Q

Amphotericin B

A

Polyene antifungal: forms pores in membrane dependent on ergosterol
Used in most systemic mycoses
Some Leishmania species have ergosterol in their membranes so active against these (antiprotozoal)

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21
Q

Miconazole

A

Imidazole antifungal: inhibits ergosterol biosynthesis

Some Leishmania species have ergosterol in their membranes so active against these (antiprotozoal)

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22
Q

Fluconazole

A

Triazole antifungal: inhibits ergosterol biosynthesis

Used in athlete’s foot & vaginal candidiasis

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23
Q

Chloroquine

A

Antiprotozoal drug: active against Plasmodium in red blood cell
Inhibits haem polymerisation to haemozoin causing toxic build of haem & generation of ROS

24
Q

Artemisinin

A

Antiprotozoal: rapidly acting antimalarial (Plasmodium) thought to act on production of ROS in RBC
Prodrug converted to dihydroartemisinin

25
Q

Sulfadoxin

A

Sulfa drug antiprotozoal: inhibits dihydropteroate synthase in Plasmodium inhibiting tetrahydrofolate biosynthesis

26
Q

Pyrimethamine

A

Antiprotozoal: inhibits dihydrofolate reductase in Plasmodium inhibiting tetrahydrofolate biosynthesis

27
Q

Fansidar

A

Antiprotozoal: combination of sulfadoxin & pyrimethamine especially effective against P. falciparum when chloroquine resistance is suspected

28
Q

Melarsoprol

A

Antiprotozoal arsenic compound: prodrug converted to melarsen oxide active against Trypanosomes
Inhibits glycolytic & TCA enzymes inhibiting ATP synthesis
Actively accumulates in Trypanosomes

29
Q

Suramin

A

Antiprotozoal: first useful agent against Trypanosomes which doesn’t contain a toxic metal ion
Only effective in early stage of infection
May act on glycolytic enzymes (mechanism unknown)

30
Q

Zanamivir

A

Antiviral drug: active against influenza inhibits NA

31
Q

Oseltamivir

A

Antiviral drug: active against influenza inhibits NA

Pro-drug broken down by esterases in plasma

32
Q

Amantidine

A

Antiviral drug: active against influenza blocks M2 channel (proton channel) involved in the uncoating of the nucleocapsid (requires acidification of virion interior)

33
Q

Aciclovir

A

Antiviral drug: active against Herpes simplex & zoster
Purine analogue phosphorylated by viral thymidine kinases then acts as chain terminator and inhibits viral DNA polymerase (30x more potent than host DNA pol)

34
Q

Niverapine

A

Antiviral drug: non-nucleoside inhibitor of reverse transcriptase in HIV

35
Q

AZT

A

Antiviral drug: nucleoside inhibitor (thymidine analogue) of reverse transcriptase in HIV

36
Q

Saquinavir

A

Antiviral drug: HIV protease inhibitor preventing viral replication & release of virions from infected cells

37
Q

Cyclophosphamide

A

Nitrogen mustard anticancer drug: alkylates DNA causing crosslinks within or between strands
Prodrug: activated in liver
Mainly used in lymphomas

38
Q

Lomustine

A

Nitrosourea anticancer drug: alkylates DNA causing crosslinks with other DNA strands or proteins
Commonly used in lymphoma (especially cutaneous), melanoma & tumours of kidney/lung
Can cross BBB so can be used in cancers in the brain
Use limited due to decreases in WBC/platelets & damage to multiple organs

39
Q

Cisplatin

A

Platinum-based anticancer drug: crosslinks DNA and revolutionised treatment of testicular cancer
Bone marrow suppression and renal toxicity limit use

40
Q

Mitoxantrone

A

Anthracycline anticancer drug: intercalates within DNA

Used in metastatic breast cancer, acute myeloid leukaemia & non-Hodgkin’s lymphoma

41
Q

Methotrexate

A

Antimetabolite anticancer drug: inhibits dihydrofolate reductase preventing tetrahydrofolate synthesis (& thus purine synthesis)

42
Q

Leucovorin

A

Adjuvant used in methotrexate chemotherapy used to salvage normal cells from folate depletion

43
Q

Etoposide

A

Anticancer drug: type II topoisomerase inhibitor

Used to treat lung & testicular cancer, lymphoma

44
Q

Topotecan

A

Anticancer drug: type I topoisomerase inhibitor

Used to treat lung & ovarian cancer

45
Q

Vinblastine

A

Vinca alkaloid anticancer drug: antimitotic which binds tubulin dimers causing disassembly of microtubule
Used in Hodgkin’s lymphoma

46
Q

Taxol

A

Taxane anticancer drug: antimitotic which binds microtubules and stabilises them
Used in advanced forms of Kaposi’s sarcoma

47
Q

Tamoxifen

A

Anticancer drug: oestrogen receptor antagonist used in breast cancer

48
Q

Anastrozole

A

Anticancer drug: aromatase inhibitor causing a reduction in oestrogen synthesis

49
Q

Goseraline

A

Anticancer drug: analogue of GnRH which is an agonist at its receptor. Sustained agonism shuts down testosterone production
Used in prostatic cancer

50
Q

Prednisone

A

Glucocorticoid prodrug converted into prednisolone in the liver
Used in the treatment of acute lymphoblastic leukaemia

51
Q

Cetuximab

A

Monoclonal antibody against the epidermal growth factor receptor
Used in colorectal cancer

52
Q

Erlotinib

A

Small molecule inhibitor of EGFR (RTK)

Used in lung cancer

53
Q

Imatinib

A

Receptor tyrosine kinase inhibitor

Inhibits Bcr-Abl so used in chronic myeloid leukaemia

54
Q

Clavulanate

A

Augmentin: inhibits beta-lactamases by forming slowly hydrolysing acyl-enzyme intermediate
Used to recapture use of beta-lactams in resistant strains

55
Q

Cephalosporin

A

Beta-lactam antibiotic

2 - MODA (8 decks)

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