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Chemotherapy > Chemo > Flashcards

Chemo Flashcards

1
Q

Targets of HIV treatment

A

reverse transcriptase

Protease

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2
Q

NRTI

A

zidovudine
didanosine
zalcitabine

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3
Q

NNRTI

A

efavirenz
nevirapine
etravirine
delaviridine

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4
Q

PI

A

saquinivir

nelfinivir

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5
Q

NS3 Inhibitors

A

1- telaprevir, boceprevir

2- simeprevir, voxilaprevir

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6
Q

NS5A Inhibitors

A

1- daclatavir, ledipasvir

2- velpatsvir

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7
Q

NS5B Inhibitors

A

sofosbuvir

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8
Q

Hepatitis C

A

single stranded RNA genome

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9
Q

function of NS5B inhibitors

A

inhibit RNA dependent RNA polymerase

–>prevents RNA replication

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10
Q

genital herpes

A

HHV1+2

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11
Q

herpes zoster

A

HHV3

shingles and chickenpox

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12
Q

cidofovir

A

new and treats herpes zoster
selectively inhibits DNA polymerase
–>prevents viral DNA replication and transcription
it is phosphorylated by cellular kinases- toxicity

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13
Q

HA receptor

A

it recognises sialic acid on epithelial cells and binds to the cell
cell is internalised in an endosome

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14
Q

M2 receptor

A

acts as an ion channel
influx of H+ breaks down the matrix layer
segments go into cytosol

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15
Q

antigenic drift

A

virus makes mistakes when copying its genes

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16
Q

antigenic shift

A

one cell is infected by 2 viruses so the segments are mixed around

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17
Q

targets for influenza antiviral

A

M2- endosome escape

NA- release from the cell

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18
Q

M2 channel inhibitors

A

amantadine and rimantadine

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19
Q

neuraminidase inhibitors

A

zanamir (relenza)

oseltamivir (tamiflu)

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20
Q

ribavirin FDA approved to treat

A

hepatitis C

human respiratory syncytial virus

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21
Q

antibiotic

A

natural substance made by a microorganism which prevents/ stops the growth of another

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22
Q

antibacterial

A

compounds capable of killing/ inhibiting bacteria

can be synthetic or semi-synthetic

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23
Q

disinfectants

A

kill microorganisms but are too toxic to be used in humans

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24
Q

mupirocin

A

narrow spectrum
gram +ve bacteria
topical ointment
inhibits iso-leucyl tRNA synthetase

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25
Q

linezolid and tedizolid

A

oxazolidinone
bacteriostatic
bind to 50S subunit of Gram +ve

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26
Q

lipophilic tetracyclines

A

minocycline

doxycycline

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27
Q

hydrophilic tetracycline

A

tetracycline

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28
Q

aminoglycosides treat:

A

severe sepsis by Enterobacteriaceae
plague and tularaemia
enterococcal endocarditis
combination- anaerobic infections and TB

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29
Q

30S and 50S aminoglycosides

A

tobramycin

kanamycin

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30
Q

chloramphenicol treats

A

used in the treatment of typhoid and paratyphoid fever

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31
Q

adverse effects of tetracycline

A

GI disturbances

deposits in calcium- pregnant and young children

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32
Q

adverse effects of aminoglycosides

A

ototoxicity

nephrotoxicity

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33
Q

adverse effects of chloramphenicol

A

myelosuppression

Gray syndrome

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34
Q

macrolides

A

erythromycin

azithromycin

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35
Q

what effects erthyromycins availability

A

it is acid labile

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36
Q

targets for drugs for bacterial cell membrane

A

synthesis of peptidoglycan

bacterial membranes

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37
Q

transglycosylation

A

disaccharide incorporated into existing glycan strand

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38
Q

transpeptidation

A

stem peptides undergo cross linking to give rigidity in the cell wall
final amino acid is cleaved from the peptide

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39
Q

what does clavulanic acid do?

A

bind more efficiently to beta lactamase and make it inactive so beta-lactam can still work

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40
Q

4 types of beta lactam

A

penicillins
cephalosporins
monobactams
carbapenems

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41
Q

applications of vancomycin

A

gram +ve infections caused by S.aureus and MRSA
can be given orally for diarrhoea as will stay there
given to patients hypersensitive to b-lactam

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42
Q

MAO of polymyxin B and E

A

1- initially through lipopolysaccharide
2- goes through outer membrane into inner membrane
3- destabilisation and affects depolarisation so leakage of proteins

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43
Q

adverse effects of vancomycin

A

red man syndrome due to release of histamines

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44
Q

MAO for ribavirin

A

1- inhibits inosine monophosphate deyhydrogenase- reduces RNA synthesis
2- induces errors/ mutations- can bind to C or U
3- slows down RNA dependent RNA polymerase- longer for immune response

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45
Q

linezolid treats

A

community and hospital acquired pneumonia

skin and soft tissue infections

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46
Q

tedizolid treats

A

reduced myelosuppression

increased antibacterial potency

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47
Q

what does azithromycin treat?

A

chlamydia and respiratory tract infections

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48
Q

what is benzylpenicillin used to treat?

A

syphillis by streptococci

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49
Q

what is daptomycin used to treat?

A

complicated skin and soft tissue infections (S.aureus and MRSA)

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50
Q

what is tetrahydrofolate important for?

A

it is an essential precursor to DNA

–>if blocked, DNA synthesis is prevented

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51
Q

target for sulphonamides

A

competitive inhibitors of dihydropteroate synthase

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52
Q

target for trimethoprim

A

inhibitor of dihydrofolate reductase

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53
Q

applications of sulphonamides and trimethoprim

A

short-term and prophylaxis of respiratory, urinary or digestive tract infections
pneumonia in HIV
together they are cotrimoxazole

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54
Q

what is cotrimoxazole

A

sulphonamide and trimethoprim combined

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55
Q

what does topoisomerase 4 do?

A

creates a transient double stranded break in one chromosome to allow the other to pass through

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56
Q

what does gyrase do?

A

mediates negative supercoiling

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57
Q

MAO of quinolones

A

bind to 5’ end of enzymes topoisomerase and gyrase
traps the enzymes on DNA so the enzymes keep breaking up DNA
this blocks DNA replication and transcription

58
Q

MAO of nitroheterolytic drugs

A

nitro group acts as an electron donor

oxygen free environments

59
Q

MAO of rifamycin

A

interferes with RNA polymerase

occludes the entrance of RNA exit channel, RNA cannot leave the enzyme

60
Q

Applications of rifamycin

A

Gram positive infections
tuberculosis
leprosy
penicillin resistant S.pneumoniae

61
Q

saprophytism

A

usually from dead organic material

62
Q

dermatophytes

A

exploit keratin found in skin, hair and nails

63
Q

risk factors for candidosis

A 
gut surgery
antibiotics
central venous catheters
IV drug abuse
immune suppression
prematurity
diabetes 
cancer
64
Q

30S aminoglycosides

A

streptomycin and spectinomycin

65
Q

daptomycin

A

gram +ve

IV

66
Q

MAO of daptomycin

A

uses Ca2+ and lipophilic tail to enter membrane
then aggregates
causes depolarisation so contents leak

67
Q

Daptomycin applications

A

skin and soft tissue infections (S.aureus and MRSA)

68
Q

Polymyxin applications

A

inhalation therapy for cystic fibrosis

burns

69
Q

Nitroheterolytic drugs

A

metrodizaole and tinizaole

need oxygen free environment

70
Q

what does cryptococcus cause

A

pulmonary disease

meningitis

71
Q

what is aspergillis terreus resistant to?

A

amphotericin B

72
Q

MAO of 5-fluorocytosine

A

converted to fluorouracil

either: - disrupts translation by incorporated into RNA
or: - inhibit DNA synthesis by inhibiting thymidylate synthetase

73
Q

what does 5-flurocytosine and Amphotericin B treat?

A

cryptococcal meningitis

74
Q

examples of polyene antifungals

A

Amphotericin B and nystatin

75
Q

MAO of polyene antifungals

A

bind to sterols (ergosterol)

increases cell permeability

76
Q

what is amphotericin B used to treat

A

empirical treatment in immunocomprised patients
treatment where fungi isn’t known
candidosis etc.
IV

77
Q

what is nystatin used to treat?

A

vaginal and oral candidosis

it is a topical cream (too toxic for IV)

78
Q

yeast fungi

A

candida

cryptococcus

79
Q

mould fungi

A

Aspergillosis

mucromycosis

80
Q

dimorphic fungi

A

histoplasmosis

81
Q

MAO of echinocandins

A

bind to FKS1P subunit of gluten synthase and inhibit

–>inhibit the cell wall synthesis

82
Q

spectrum of activity for echinocandins

A

Aspergillosis and candida

narrow spectrum

83
Q

examples of echinocandins

A

caspofungin
anidulafungin
micafungin

84
Q

MAO for terbinafine

A

inhibits squalene epoxidase

prevents ergosterol synthesis

85
Q

What is terbinafine used for?

A

treats dermatophyte infections of skin and nail

topical/oral/inhalation

86
Q

neuroplasia

A

another name for cancer

87
Q

metastasis

A

process of formation of distant secondary products

88
Q

angiogenesis

A

tumours and cancer cells forming stroma

including blood and lymphatic vessels

89
Q

palliative chemotherapy

A

when cancers resistant to all drugs and treatment

–>offer care- quality of life maintained

90
Q

MAO of methotrexate

A

competitive inhibitor of dihydrofolate reductase

91
Q

how can methotrexate toxicity be rescued?

A

leucovorin

92
Q

MAO of 6-mercaptopurine

A

inhibits purine synthesis

gets incorporated into DNA and RNA–> non-functional molecules

93
Q

Gemcitabine

A

analogue of deoxycytidine

used in the treatment of advanced metastatic pancreatic cancer

94
Q

MAO of cytarabine

A

chain terminator of DNA synthesis
phosphorylated and incorporated into DNA
inhibits DNA polymerases

95
Q

MAO of antimetabolites

A

inhibit or interfere with DNA/RNA synthesis

96
Q

MAO of antibiotics

A

bind to DNA

disrupt function of DNA

97
Q

MAO dactinomycin

A

Intercalates into minor groove of DNA- more sensitive to strand breaks and chromosomal rearrangements
binds to DNA and interferes with transcription and replication
resistance due to P-glycoprotein

98
Q

MAO anthrayclines

A

intercalate into DNA
generates free radicals that break DNA strands
targets cells in S and G2 phases
form cross links with GG making DNA unstable

99
Q

examples of anthracyclines

A

doxorubicin and daunorubicin

100
Q 
mechlorethamine
cyclophosphamide
ifosphamide
carmustine
dacarbazine
temzolamide
A

alkylating agents

101
Q

MAO platinum drugs

A

form intra and inter strand cross links
interfere with DNA replication and transcription
act in G1 and S phases

102
Q

Topoisomerase 1 inhibitors

A

topotecan- ovarian and lung cancer

irinotecan- colon and rectal cancer

103
Q

MAO of topoisomerase 1 inhibitors

A

prevent re-ligation of DN strands
S phase specific
need to be activated in cancer cells

104
Q

Topoisomerase 2 inhibitors

A

daunorubicin and doxorubicin- break DNA strands that cannot be repaired
Etoposide and teniposide- double strand breaks in DNA

105
Q

Telomerase Inhibitors

A

Imetelsat- direct enzyme inhibitors

compete for binding with telomerase RNA

106
Q

Mitosis inhibitors

A

bind to tubin and inhibit polymerisation into microtubules

–>induce spindle dysfunction

107
Q

Vinca alkaloids

A

block mitosis in metaphase by binding to tubular and preventing polymerisation into microtubules
induce spindle dysfunction

108
Q

Taxanes

A

active in G2/M phase of cell cycle
stabilise microtubules, preventing chromosome segregation
used to treat ovarian and breast cancers

109
Q

what are anthracyclines used for?

A

breast, lung and leukaemia

IV

110
Q

telomerase

A

binds to the end of chromosome and replicates it
integrity of chromosome maintained
active in stem cells

111
Q

examples of vine alkaloid

A

vincristine and vinblastine

112
Q

examples of taxanes

A

paclitaxel and docetaxel

113
Q

if resistant to vinka alkaloids

A

also resistant to dactinomycin

114
Q

hormone responsive

A

cancer regresses on hormone treatment

115
Q

hormone dependent

A

cancer regresses when hormone removed

116
Q

tamoxifen

A

selective oestrogen receptor modulator
competitively inhibits oestrogen receptor
lowers oestrogen levels
used with leucorvorin in premenopausal

117
Q

Flutamide, nilutamide and bicalutimide

A

non steroidal anti-androgens

compete for binding with androgen for the androgen receptor

118
Q

iressa and tarceva

A

inhibit tyrosine kinase
show promise as lung cancer therapy
Japanese 3x more likely to respond to iressa than american

119
Q

BCR-ABL

A

in CML patients a fusion protein is formed
it has tyrosine kinase activity
only found in CML patients

120
Q

Gleevac

A

small molecule inhibitor of BCR-ABL

121
Q

MDM2

A

enzyme that attaches ubiquitin to p53, then directs p53 to proteasome where it gets degraded

122
Q

nutlin

A

binds to MDM2 and releases p53 and triggers apoptosis
cannot be used clinically
proof of concept

123
Q

nexavar

A

renal cancer

inhibits tyrosine kinase- could have wider applications

124
Q

herceptin uses

A

breast and ovarian cancers that do not express the oestrogen receptor

125
Q

target for herceptin

A

HER-2- tyrosine kinase

it is over-expressed in 30% breast cancers

126
Q

development of herceptin

A

linked with emtansine (toxic tubulin inhibitor)

delivers second punch to cells

127
Q

bevacizumab uses

A

given with 5-FU for colorectal cancer

128
Q

MAO of bevacizumab

A

prevents angiogenesis by binding to vascular endothelial growth factors (VEGF)

129
Q

adverse effects of bevacizumab

A

hypertension and intestinal bleeding

effects on vascular system

130
Q

Rituximab target

A

binds to CD20 on B cells of non-Hodgkin lymphoma

not other bone marrow cells–> doesn’t deplete bone marrow

131
Q

Rituximab uses

A

therapy for NHL, other lymphomas and leukaemias

also macular degeneration of the eye

132
Q

adverse effects of rituximab

A

hypotension, fever, cardiac problems

133
Q

cetuximab

A

targets EGF receptor- tyrosine kinase activity

used in colorectal cancers

134
Q

L-asparaginase

A

depletes supply of asparagine
given in cancers where dependent on exogenous sources
normal cells not affected
therapy in childhood ALL

135
Q

interferon

A

1- alpha and gamma- epithelial and fibroblast cells
2- gamma- immune system- fight pathogens
promote cell apoptosis and stimulate immune cells to recognise and kill cancer

136
Q

interferon alpha

A

can be made in bacteria- isn’t post-translationally modified

137
Q

resistance

A

situation where disease causing agents are able to survive and grow in the presence of chemotherapeutic drugs

138
Q

types of acquired antibiotic resistance

A

1- endogenous- spontaneous mutation which leads to subtle change
2- horizontal- bacteria acquire resistant gene from a bacteria that is already

139
Q

mechanisms for antibacterial resistance

A

1- altered target site
2- decreased uptake
3-enzymatic inactivation
4- bypass

140
Q

A, C and D beta-lactamases

A

have a serine which provide nucleophilic attack on the cyclic amide bond- breaking open the beta-lactam ring

141
Q

B beta-lactamase

A

zinc ions which perform reaction

Chemotherapy (1 decks)

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