drugs Flashcards

1
Q

Monoclonal antibody against CD20 B cells

A

Rituximab

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2
Q

Rituximab

A

Monoclonal antibody against CD20 B cells

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3
Q

Area of antibody that binds to CD20

A

fc region

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4
Q

type of toxicity displayed by rituximab

A

Antibody dependant cellular cytotoxicity

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5
Q

action of CD20

A

Cell cycle initiation

Ca channel

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6
Q

condition rituximab used in

A

NHL

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7
Q

mechanism of resistance to retuximab

A

downregulation of cd20- resistant clones
Poor antibody dependant cellular cytotoxicity as fc region is neutralised
mutation od CD20 c terminal by epigenetic methylation

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8
Q

vemurafinib mechanism of action

A

BRAF V600E inhibitor

serine threonine kinase inhibitor

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9
Q

SE of vemurafanib

A

QT elongation

tumouor promotion in BRAF WT

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10
Q

% of melanomas with V600E mutation

A

40-60%

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11
Q

what is the V600E mutation

A

valine for glycine at codon 600 in exon 15

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12
Q

resistance to vemurafaib

A

Loss of PTEN allows PI3K pathway
10-35% of melanomas

-LOH, methylation or deletion mutations

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13
Q

Herceptin mechanism

A

monoclonal AB against HER-2 human oestrogen receptor-2

overexpression of HER2

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14
Q

non trade name for herceptin

A

trastuzumab

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15
Q

resistence to HER2

A

Downstream mutation
-Tyrosine kinase inhibitors can overcome

obsticles for binding- truncated HER2 mutation resultsin constitutively active receptor

PTEN mutation in 50%- upregulation of PI3K

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16
Q

Ivacaftor used in…

A

used in cf

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17
Q

ivacaftor MOA

A

potentiator of CFTR, meaning it increases the length of time channels are open, allowing Chlorie ion to pass through the pore

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18
Q

How many CFTR mutation classes recognised?

A

6

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19
Q

G551D CF mutation

A

CFTR gets to the membrane, but chnnel regulation is defective, with decreased channel conductance

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20
Q

mutaion ivacaftor targets

A

G551D

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21
Q

how many cf patients will benefit from ivaaftor

A

4%

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22
Q

alternative to ivacaftor for CF patients

A

Lumacaftor

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23
Q

machanism of action of Lumacaftor

A

Acts as a chaperone during protein folding, increasing number of CFTR receptors are on the cell surface

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24
Q

mutation Lumacaftor works for

A

F508del

25
Q

drug affecting post translational modification

A

Lumacaftor

26
Q

How many CF patients have the F508del mutation

A

50%

27
Q

Imatinib used in

A

CLL

28
Q

Imatinib MOA

A

Targets BCR-ABL ATP on Bcr, inhibiting tyrosine kinase properties of Abl.

29
Q

life expectancy of CLL patient on imatinib

A

Normal

30
Q

SE imatinib

A

Pleural effusion

31
Q

how to monitor response of Imatinib

A

qPCR of BCR-ABL

32
Q

second line tyrosine kinase inhibitor

A

Nilotinib

33
Q

Brentuximab MOA

A

Monoclonal AB to cd30

34
Q

Brentuximab used in

A

HL

35
Q

cetuximab MOA

A

monoclonal antibody too EGFR

Mechanism of antineoplastic effects in vivo unknown.1 However, cetuximab binds specifically to EGFR (HER1, c-ERbB-1) on both normal and tumor cells and competitively blocks cellular action of EGF and other ligands (e.g., transforming growth factor [TGF]-α).1 6 35 Binding to EGFR blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis (programmed cell death), and decreased matrix metalloproteinase and vascular endothelial growth factor production

36
Q

Resistance to cetuximab

A

mutation of ras

37
Q

cetuximab used in…

A

NSCLC

test for EGFR expresson

38
Q

Nivolumab MOA

A

IgG4 kappa immunoglobulin that is selective for PD-1, an immune checkpoint receptor expressed in t cells, monocytes, b cells, NK T calls and dendritic cells.

PD-1 ligand overexpression results in PD-1 activity and suppression of cytotoxic t-cell activity

nivolumab blocks interaction between PD-1 and it’s ligands, resulting in enhanced immune response,

39
Q

Nivolumab used in..

A

melanoma

40
Q

Drugs metabolised by chytochrome p450

A

paracetomol

tamoxifen

41
Q

tamoxifen

A

Acts as an estrogen antagonist

increases production of inhibitory factors and decreases production of stimulatory factors that influence breast cell growth

blocks growth receptor ERB2

42
Q

tamoxifen adverse effects

A

when used for DCIS, increases uterine malignancies, stroke, PE.

43
Q

tamoxifen metabolism

A

tamoxifen is a prodrug. metabolised by cytochrome p450 CYP2D6 into afimoxifene and endoxifen

44
Q

should we genotype for tamoxifen prescribing

A

no- FDA

45
Q

SSRI impact on Cytochrome p450

A

inhibititoon, can result in phenocopy of poor metabolisers

46
Q

which CYP2D6 allele has high rate of relapse of breast cancer when on tamoxifen

A

4*- poor metabolisers

47
Q

gefetinib and erlotinib are…

A

tyrosine kinase inhibitors used in NSCLC

48
Q

Azathioprine

A

Prodrug, metabolised to 6 thiopurine and incorporated into dna- inhibits purine synthesis- cytotoxicity

Produces Reactive Oxygen species that decrease efficiency of NER

photosensitiser

49
Q

phototoxic drugs

A

Azathioprine, voriconazole (anti fungal),

50
Q

Imiquimod used in…

A

AK- prevents progression to SCC

51
Q

Imiquimod moa

A

toll like receptor 7 agonist.

involved in pathogen recognition

activates langerhans cells to activate adaptive immune response

52
Q

nicotinamide

A

amine form of vitamin b3- precurssor to NAD, cofactor in ATP synthesis

enhances NER

reduces level of UV immunosuppression.

53
Q

Pembrolizumab

A

IgG4 isotype PD-1 inhibitor monoclonal antibody

immune checkpoint inhibitor- prevents PDL-1 binding to PD-1

PD-1 checkpoint is involved in T cell Exhastion, activation and effector function.

inhibiting this checkpoint prevents t cell exhastion and prevents the cancer cell evadng the immune system.

allows t cells to maintain their effector ffunctions

in cancer cells, activated T cells can kill tumour cells and secrete cytokines that recruit other immune cells to participate in the anti tumour respsonse

54
Q

Pembrolizimab liscenced for

A

FDA lisenced for use in genetic signiture- missmatch reapir or microsatellite instability.

55
Q

Price of Pembrolizimab

A

$150,000

56
Q

adoptive cell transfer

A

immunotherapy- using pts own immune cells to target the tumour

57
Q

adoptive cell transfer prominent type

A

CAR-T cell therapy

58
Q

CAR-T cell therapy

A

chimeric antigen receptor

receptor proteins engineered to give t cells the ability to target a specific protein.

chimeric- contain both antigen-binding and t-cell-activating functions

59
Q

PARP inhibitor example

A

Olaparib