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MoDA Drugs > Chemotherapy > Flashcards

Chemotherapy Flashcards

(63 cards)

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1
Q

Beta lactams (penicillin)

A

Ring is similar to D-ala-D-ala
Forms covalent bond with transpeptidase but doesn’t liberate it
Only bactericidal in proliferating cells

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2
Q

Vancomycin

A

Cup fits around D-ala-D-ala forming 5 H bonds and causing steric hinderance for transglycosylation

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3
Q

Fosfomycin

A

PEP analogue

Inhibits pyruvile transferase (For making NAM)

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4
Q

Cycloserine

A

Inhibits synthesis and linking of D-ala

Must cross cell membrane to do this in cytoplasm

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5
Q

Bacitracin

A

Binds bactoprenol monophosphate (membrane carrier) to deplete cycle of lipid career

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6
Q

Valinomycin

A

Makes ion channel to dissipate PMF via K+ movement

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7
Q

Polymyxin antibiotics

A

Bind gram -ve envelop to make it leaky

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8
Q

Tetracyclines

A

Bind 16S rRNA in 30S
Inhibit aminoacyl tRNA from entering A site
Bacteriostatic

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9
Q

Aminoglycosides (streptomycin, gentamicin)

A

Binds 30S; freezes pre-imitation complex so bacteriostatic

+ causes mRNA misreading to make toxic peptides; bactericidal

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10
Q

Erythromycin

A

Binds 50S at exit tunnel to stop synthesis

Bacteriostatic (mostly)

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11
Q

Chloramphenicol

A

binds 50S to stop peptidyl transferase; time critical infections only as very toxic

NB: can’t use with erythromycin as they have overlapping binding sites

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12
Q

Fusidic acid

A

inhibits elongation factor G

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13
Q

Fluoroquinolones (ciprofloxacin for anthrax, Levofloxin for strep pneumonia)

A

Target GyrA and B to cause bactericidal DNA fragmentation

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14
Q

Rifampicin

A

Blocks elongation of RNA at initiation stage (via binding beta subunit of DNA dependent RNA pol)
Used for TB

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15
Q

Aminocuomanis and Nalidixic acid

A

Inhibit DNA gyrase II via Gyrus B

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16
Q

Daunomycin

A

Intercalates between nucleases to increase DNA length to cause local unwinding

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17
Q

Bleomycin

A

Intercalated in DNA and if binding reduced metals can react to give superoxide to cleave DNA

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18
Q

Mitomycin C

A

alkylating; cross links between guanines

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19
Q

Sulfamethoxadole

A

inhibits DHPS in folate synthesis

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20
Q

Trimethoprim

A

inhibits DHFR in folate synthesis

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21
Q

Amphotericin B

A

makes ion channels in ergosterol membranes

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22
Q

Micanozol

A

inhibits ergosterol biosynthesis

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23
Q

Chloroquinone

A

inhibits detoxification of haem in malaria so get lots of ROS

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24
Q

Artemisinin

A

anti-malaria

Makes ROS

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25
Sulfadoxine
inhibits DHPS (malaria)
26
Pyrimethamine
inhibits DHFR
27
Melarsoprol
anti-trypanosomal Actively accumulates Inhibits ATP synthesis enzymes
28
Amantidine/Rimantidine
Binds HA to prevent viral and endosomal membrane fusion + blocks M2 to prevent acidifcation CHECK WHICH
29
Ribavirin
Guanosine analogue Inhibits initiation and elongation of mRNA For hepatitis C
30
Zanamivir (Relenza)
Sialic acid analogue to inhibits NA (early stages)
31
Tamiflu (oseltamivir)
Inhibits NA
32
Aciclovir
Guanosine analogue that causes chain termination Prodrug Interacts with viral DNA pol most ANti-herpes
33
Foscarnet (anti-herpes)
pyrophosphate analogue preventing addition of new nucleotides by binding viral DNA pol
34
AZT, Zidovudine
thymidine analogue that causes chain termination | anti-HIV
35
Saquinavir/Ritonavir
Blocks HIV protease
36
Enfurvirtide
Inhibits HIV viral fusion
37
1
1
38
Nitrogen mustards (cyclophosphamide)
Cross links guanine in DNA Anti-cancer Metabolised by cytP450 to active mustard form
39
Melphalam
Nitrogen mustard that is actively accumulated in melanomas
40
Nitrosureas; Carmustin, Lomustin
Cross link DNA between guanines | Can cross BBB so used for brain tumours
41
Cis-platin
Reacts with adjacent guanines in the same strand to cause cross links, bending DNA and changing minor groove
42
Anthracyclins; doxorubicin, duanomycin, antimycin D
Intercalate in DNA, causing unwinding and oxidative DNA damage and fragmentation
43
Mitoxantrone
Less toxic anthracyclin analogue
44
Methotrexate
Folic acid analogue to inhibit DHFR | can provide folinic acid to help non cancerous cells survive
45
5-flourouracil
Pyrimidine analogue to inhibit thymidylate synthase Inhibits DNA synthesis Anti-neoplastic
46
Captothecins
Inhibiting type 1 topoisomerase
47
Mitoxantrone, Antracycline, Etoposides
Inhibit type 2 topoisomerase
48
Vinca alkaloids (vinblastine, vincristine)
Bind tubulin dimers to cause microtubule dissociation
49
Taxol
Binds microtubules to stabilise so they grow
50
Tamoxifen
Antagonises oestrogen receptor
51
Anastrazole
Blocks aromatase enzyme used to synthesis oestrogens | For use in post-menopausal women
52
Flutamide
Competitively inhibits androgen receptor for prostate cancer
53
Goserelin
Agonist of GnRH receptor; acts via desensitisation to reduces testosterone production
54
Prenisole
Converted to prednisone which agonists glucocorticoid receptor to inhibit lymphocytic growth in lymphocytic cancer
55
Cetuximab
Binds EGFR for colorectal cancer
56
Retuximab
Binds CD20 receptor to cause B cell lysis
57
Imantinib
Inhibits BCr-ABl and c-kit in chronic myeloid leukaemia
58
Methicillin resistance
MecA encodes new transpeptidase/transglycosylase with lower affinity for beta lactams Fem genes generate Gly5 as cross link which is now better substrate DONT NEED BOTH GENES FOR RESISTANCE
59
Vancomycin resistance
Van genes; change to D-ala-D-lac | Target modification
60
Beta lactam resistance
Beta lacatamase activity (blocked by clavulanic acid)
61
Aminoglycoside (tetracycline) resistance
TetA proton drug anti porter used to pump out tetracycline PSeudomonas aeruginosa
62
Fluconazole resistance
Changes in ergosterol biosynthesis
63
Multiple drug resistance
Mar regulon P glycoprotein (transporter)

MoDA Drugs (9 decks)

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