Shared Flashcard Set

Details

Haem/Onc Drugs
Relevant drugs for BPT revision
31
Other
Post-Graduate
01/12/2021

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Cards

Term
Examples of Alkylating Agents
Definition
  • Cyclophosphamide
  • Melphalan
  • Busulfan
Term
Mechanism of Action of Alkylating Agents
Definition
Interfere with DNA synthesis by cross-linking DNA strands --> strand breaks; inhibit DNA replication/repair
Term
Side Effects of Cyclophosphamide
Definition
  • Haemorrhagic cystitis
  • Bladder TCC
Term
Side Effects of All Alkylating Agents
Definition
  • Infertility
  • Myelosuppression
  • Teratogenic (never in pregnancy unless the life of the mother is at stake)
  • Secondary malignancy (AML, lymphoma)
Term
What class of anti-neoplastic agents confers risk of secondary malignancy?
Definition
Alkylating agents (AML, lymphoma)
Term
Indications for Cyclophosphamide
Definition
  • Haematological malignancies
Term
Examples of platinum-based chemotherapeutics
Definition
  • Cisplatin
  • Carboplatin
  • Oxaliplatin
Term
Mechanism of action of platinum-based chemotherapeutics
Definition
Causes cross-links of DNA
Term
Side effects common to all platinum-based chemotherapeutics
Definition
  • Infertility
  • Hypomagnesaemia
  • Peripheral neuropathy with cumulative dosing
Term
Side effects of cisplatin
Definition
  • Severe nausea & vomiting
  • Ototoxicity
  • Nephrotoxicity
Term
Examples of Taxanes
Definition
  • Paclitaxel
  • Docetaxel
Term
Mechanism of action of Taxanes
Definition
Prevents microtubule formation by binding to tubulin dimers (M phase of cell cycle)
Term
Side effects of Taxanes
Definition
  • Peripheral neuropathy
  • Fluid retention
  • Neutropaenia
  • Infertility, amenorrhoea
  • Hypersensitivity reaction
  • Need to dose reduce in liver impairment
Term
Mechanism of Action of, and indications for Tamoxifen
Definition

ER+ competitive antagonism

ER+ Breast Ca (pre- and post-menopausal)

Term
Mechanism of action of, and indications for, Aromatase Inhibitors
Definition
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Term
Side effects of Tamoxifen
Definition
  • Hot flushes
  • Low libido
  • DVT (2-3x risk)
  • Endometrial cancer (2-3x risk)
Term
Side effects of Aromatase Inhibitors
Definition
  • Hot flushes
  • Low libido
  • Arthralgias
  • Osteopaenia
Term
Examples of ALK-Inhibitors
Definition
  • Alectinib (2nd gen, new standard of care, brain penetration)
  • Crizotinib (1st gen, lots of side effects)
  • Others: Ceritinib, lorlatinib (brain penetration)
Term
What is the function of ALK?
Definition

Transmembrane tyrosin kinase receptor

Activates a whole bunch of pathways (JAK, STAT, mTOR, sonic hedgehog & more) to stimulate cell growth, transformation, and anti-apoptotic signalling

Term
What malignancies are ALK-Inhibitors used for?
Definition
NSCLC (5% of adenocarcinomas are ALK+, typically younger patients, non-smokers)
Term
Side effects of ALK-Inhibitors
Definition

First generation (crizotinib) is the worst

  • Nausea, vomiting, diarrhoea (mild)
  • Hepatitis (severe, rare)
  • Pneumonitis (severe, rare)
  • Visual phenomena
  • Low testosterone (universal)
  • Bradycardia
Term
What are some examples of intracellular EGFR inhibitors?
Definition
  • Erlotinib, gefitinib (1st gen)
  • Afatinib (2nd gen)
  • Osimertinib (3rd gen)
Term
Side effects of EGFR inhibitors
Definition

Acneform rashmeans that it's working!

Diarrhoea

Hepatitis, pneumonitis (rare)

Term
Why would you use Osimertinib rather than an earlier generation EGFR inhibitor?
Definition

Overcomes resistance to earlier generation EGFR inhibitors

  • 50% of patients develop T790M mutation - change to structure of binding pocket meaning older EGFR-i's can't bind
  • Osimertinib overcomes this
Term
What is the mechanism of action of Imatinib?
Definition
Multi-kinase inhibitor, including BCR-Abl and cKIT
Term
What are some other multi-kinase inhibitors similar to Imatinib?
Definition

Dasatinib

Nilotinib

Term
Mechanism of Action of Durvalumab
Definition
  • Anti PDL-1 inhibitor
Term
Indications for Durvalumab
Definition
  • Stage 3 Lung Ca - Neoadjuvant (PACIFIC trial)
Term
Mechanism of action of Capecitabine
Definition

Anti-metabolite (pyrimidine analogue)

Plantar-palmar erythema

Term
What are some examples of extracellular EGFR inhibitors?
Definition

MABs

  • Cetuximab
  • Panitumumab
Term
Side effects of VEGF inhibitors
Definition
  • Hypertension - means that it's working!
  • Proteinuria/nephrotic syndrome
  • Bleeding/increased risk of haemorrhage
  • Delayed wound healing
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