1 Flashcards

1
Q

Alemtuzumab

A

Recombinant humanised monoclonal antibody
Anti-CD52
CD52 is found on most B cells, T cells, monocytes, macrophages and some granulocytes
Rx: CLL, multiple sclerosis
Caution: may cause transient and severe hypotension caution with IHD

May cause hypotension, infusion related reactions, profound lymphopenia, pancytopenia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Bevacizumab

A

Recombinant humanised
binds to VEGF inhibiting angiogenesis
Risk of heart failure
Hypertension, impaired wound healing, thromboembolic events,

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Blinatumomab

A

Recombinant, bispecific mAb
Binds to CD19 (B cells ) and CD3 (T cells)
Forms link that results in activation of T cells and the elimination of CD-19 positive B cells
Indicated: B cell ALL
Cytokine release syndrome, neurological toxicity, infection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Brentuximab vedotin

A

Conjugte - toxic payload: chimeric antibody (CD30) + monomethyl auristatin E (MMAE) a microtubule poison > cell cycle arrest and apoptosis
Containdicated with bleomycin
Renal avoid: <30mL/min
Hepatic avoid: Child B and C
Peripheral neuropathy, infusion related, PML, pneumonitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Cetuximab

A
Recombinant chimeric 
Binds to EGFR 
inhibits proliferation, 
Skin reactions: acne, rash,
infusion reaction, VTE, mucositis,
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

EGFR inhibitors

A
Cetuximab
Panitumumab
Afatinib
Erlotinib
Gefitinib
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

EGFR inhibitor skin reactions

A

Papulopustular rash
Face and upper body
Occurrence/severity may be associated with response to treatment
Rx doxycycline prophylaxis and steroids
Other skin signs: itch, dry skin, fissures, paronychia, nail disorders, abnormal hair growth

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Ipilimumab

A

Human monoclonal Ab

CTLA-4 (cytotoxic T lymphocyte-associated antigen 4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

CYP450 inducers

A
SCRAP GPS
St. John's Wort
Carbamazipine
Rifampicin
Alcohol (chronic)
Phenytoin
Griseofulvin
Phenobarbital
Sulphonylureas
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

CYP450 inhibitors

A
SICKFACES.COM GQ
Sodium valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Alcohol (acute)/amiodarone
Chloramphenicol
Erythromycin
Sulphonamides
Ciprofloxicin
Omeprazole
Metronidazole
Grapefruit juice
Quinidine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Omalizumab

A

Recombinant humanised
Monoclonal antibody against IgE
Reduces the immune systems response to allergen exposure
Rx: asthma, chronic spontaneous urticaria
Thrombocytopenia, ? association with Churg-Strass syndrome
SE: injection site reactions, bleeding, headache, MSS pain, anaphylaxis , serum sickness-like reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Anti-CD20 antibodies

A

Rituximab
Ofatumumab
Obinutuzumab

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Basilixumab

A

Chimeric monoclonal antibody against IL-2
Blocks IL-2 inhibiting T-lymphocyte proliferation
Rx: prevention of acute renal transplant rejection (also liver and lung)
Caution if previous Rx with basilixumab, may increase risk of hypersensitivity; ?increase in surgical wound complications
SE: hypersensitivity, cytokine release syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Crizotinib

A

Tyrosine kinase inhibitor
Inhibits anaplastic lymphoma kinase (ALK) and hepatocyte growth factor (HGFR, c-Met)
Rx: anaplastic lymphoma (AKL +); non-small cell lung cancer (ALK+)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Afatinib

A

TKI
EGFR
HER2, HER4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Axitinib

A

VEGF 1-3

17
Q

Dasatinib

A
BCR-ABL
Src family
c-KIT
PDGFR
ephrin receptor
18
Q

Erlotinib

A

EGFR

19
Q

Gefitinib

A

EGFR

20
Q

Ibrutinib

A

Bruton’s tyrosine kinase (BTK)

21
Q

Imatinib

A

bcr-abl, c-KIT, PDGFR

22
Q

Nilotinib

A

bcr-abl, c-KIT, ephrin receptor, PDGFR

23
Q

Tofacitinib

A

JAK1, JAK2, JAK3

24
Q

Sunitinib

A

VEGFR 1-3
PDGFR
c-KIT
FLT-3

25
Q

Sorafenib

A
VEGFR 2-3
PDGFR
c-kit
FLT-3
also Raf kinase
26
Q

Pertuzumab

A

Recombinant humanised
Monoclonal antibody against HER2
Prevents HER2 paring with other members of the HER family, arrests cell growth and induces apoptosis
Activates immune response that lyses tumour cells
Rx: HER2 positive breast cancer
Caution: risk of cardiac failure/LV dysfunction caution if underlying heart disease, or other cardiotoxic agents
SE: infusion related reactions, LV dysfunction, diarrhoea, oral mucositis, headache, neutropenia, rash, itch

27
Q

Secukinumab

A

Recombinant human monoclonal antibody
IL-17
Inhibits the activity of IL-17 which is involved in inflammatory and immune responses
Rx: psoriatic arthritis, ankylosing spondylitis
Caution with IBD, may cause new cases or exacerbate
SE: menstrual disorders, infection, hypersensitivity reactions, neutropenia
May develop anti-drug antibodies

28
Q

Abiraterone

A

Inhibits CYP17
Results in reduction of androgen synthesis in testicular, adrenal and prostate tumour tissue
Rx: prostate cancer
May cause mineralocorticoid excess - give with supplemental prednisolone
Caution if CVD, heart failure
Contraindicated in severe liver impairment
SE: fluid retention, hypokalaemia, hypertension, UTI, fracture, hot flushes

29
Q

Methotrexate

A

Folic acid antagonist
Inhibits DNA synthesis and cell replication by competitively inhibiting the conversion of folic acid to folinic acid
Rx: cancer, psoriasis, RA, Crohn’s
Caution: immunosuppressive, GI ulcers, third spacing, hepatic and renal
Teratogenic
Toxicity: myelosuppression, pulmonary, hepatic

30
Q

Cyclosporine

A

Calcineurin inhibitor
Forms complex with cyclophilin which blocks the action of calcineurin in activated T cells. Prevents production of IL-2 and other cytokines
Rx: transplant rejection, nephrotic syndrome, RA, psoriasis
Caution: uncontrolled hypertension, renal impairment, immunosuppressive
SE: “get more”
gingival hyperplasia, hypertension, hypercholesterolaemia, hyperkalaemia, hyperglycaemia, raised bilirubin + aminotransferases BUT hypomagnesaemia
Reversible posterior leucoencephalopathy syndrome
Level C0 and C2, calculate AUC

31
Q

Leflunomide

A

Inhibits pyramiding synthesis in leucocytes and other rapidly dividing cells by inhibiting activity of dihydro-orotate dehydrogenase
Rx: RA, psoriatic arthritis
Contraindicated: lymphoproliferative disease in last 5 years, myelodysplasia
Infection (TB, HBV), ILD
Hepatotoxic: avoid if ALT+AST >2 ULN
Teratogenic
SE: abdominal pain, cholelithiasis, ILD, hypersensitivity, peripheral neuropathy
Washout-cholestyramine

32
Q

Sulfasalazine

A

MOA is unclear
Exerts local anti-inflammatory action on bowel wall
Rx: UC, Crohn’s (better for distal disease)
Caution: G6PD deficiency, asthma
Renal <20mL/min, hepatic clearance
Safe in pregnancy, give folic acid supplement.
SE: haemolytic, oligospermia, vomiting, yellow-orange discolouration of fluids, pancreatitis, interstitial nephritis.

33
Q

Ustekinumab

A

Recombinant human monoclonal antibody
Inhibits activity of cytokines, IL-12 and IL-23, which are involved in inflammatory and immune response
Rx: chronic psoriasis, psoriatic arthritis if unresponsive to TNFa
Caution: malignancy of history of malignancy, infection (TB, HBV)
May exacerbate psoriasis or psoriatic arthritis
SE: pustular psoriasis, exfoliative dermatitis, hypersensitivity, injection site reaction

34
Q

Apremilast

A

Inhibits phosphodiesterase 4
Reduces proportion of pro-inflammatory cytokines (e.g. TNFa, IL-17, IL 23 and increasing anti-inflammatory cytokines (e.g. IL -10)
Rx: chronic psoriasis, psoriatic arthritis
Caution: depression
Renal: <30mL/min
Avoid pregnant
SE: GI (esp. diarrhoea), depression, rebound psoriasis, weight loss

35
Q

Cyclophosphamide

A

Alkylating agent
Immunosuppressive properties are considered due to cytotoxic effect on lymphocytes
Interfere with cellular replication by forming cross-linkages between DNA strands
Rx: autoimmune disease, cancer, vasculitis
Caution: myelosuppression, haemorrhaging cystitis, cardiotoxicity
Teratogenic
SE: alopecia, hyperpigmentation heart failure, pulmonary fibrosis, hyponatraemia + seizures

36
Q

Mycophenolate

A

Mofetil and sodium are both converted to mycophenolic acid
Selectively suppressed lymphocyte proliferation and antibody formation by inhibiting unisons monophosphate dehydrogenase
Depletion of guanosine nucleotides results
More lymphocyte selective than azathioprine
Rx: prevent transplant rejection, autoimmune disease
Caution: GI ulceration (increased risk bleeding), reduced absorption of MMF with low gastric acid (e.g. PPI use), use sodium in this context
Renal:
Teratogenic
SE: myelosuppression, oesophagitis, gastritis, colitis, infection, aplastic anaemia, pure red cell aplasia, photosensitivity