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Respiratory Drugs > Treatment for Lung Cancer > Flashcards

Treatment for Lung Cancer Flashcards

1
Q

What are the localised symptoms and signs of lung cancer?

A

Cough and fatigue
Breathing problems
Blood in phlegm
Chest pain and tightness
Hoarseness & hiccups

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2
Q

What are the generalised signs and symptoms of lung cancer?

A

Bone pain
Headaches
Weight loss
Abdominal pain
Hepatomegaly
GI disturbances

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3
Q

What are the available treatment methods for lung cancer?

A

Surgery
Radiation
Pharmacotherapy

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4
Q

What are the two options under pharmacotherapy of lung cancer?

A

Chemotherapy
Targeted or Biologic therapy

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5
Q

What are the kinds of drugs given in chemotherapy?

A

Alkylating agents
Antimetabolites
Topoisomerase inhibitors
Microtubule inhibitors

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6
Q

What are the examples of alkylating agents?

A

Cisplatin (1st gen)
Carboplatin (2nd gen)

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7
Q

What is the mechanism of action of alkylating agents?

A

Kill tutor cells at all stages of cycle
Form intra-strand and inter-strand crosslinks –> inhibition of DNA synthesis

Bind both to cytoplasmic and nuclear proteins

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8
Q

Pharmacokinetics of alkylating agents?

A

Administered via IV

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9
Q

What is a contraindication of cisplatin?

A

Aluminium, it reacts and inactivates it

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10
Q

What are the adverse effects of alkylating agents?

A

Nephrotoxicity
Ototoxicity
Neurotoxicity
Nausea & Vomiting
Myelosuppression

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11
Q

What are the examples of antimetabolites (folate antagonists)?

A

Pemetrexed and Pralatrexate

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12
Q

What is the mechanism of action for antimetabolites (folate antagonists)?

A

Inhibits DHFR and enzymes involved in de novo purine nucleotide biosynthesis

Inhibits thymidylate synthase –> lower risk of resistance

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13
Q

What is the function of the DHFR enzyme?

A

Converts folic acid into DHF which is then converted into THF

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14
Q

What is the function of thymidylate synthase?

A

Converts dUMP into dTMP

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15
Q

What are the pharmacokinetics of antimetabolites (folate antagonists) ?

A

Excited in urine
Dose modification is required if renal dysfunction

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16
Q

What are the adverse effects of antimetabolites (folate antagonists)?

A

Myelosuppression
Skin rash
Neutropenic sepsis leading to death

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17
Q

What is an example of antimetabolites (pyrimidine analogs)?

A

Gemcitabine

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18
Q

What is the mechanism of action of Gemcitabine?

A

Gemcitabine diphosphate inhibits ribonuclease reductase required to convert ribonucleotides into deoxyribonucleotides

Gemcitabine triphosphate inhibits DNA polymerase –> blockade of DNA synthesis and repair

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19
Q

How does Gemcitabine triphosphate go by unrecognised?

A

It is incorporated into DNA and it is followed by one more normal nucleotide

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20
Q

What are the adverse effects of Gemcitabine?

A

Myelosuppression
Hepatic toxicity
Flu-like symptoms !!
GI disturbances
Elevations of serum transaminases
Proteinuria

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21
Q

What does inhibition of DNA repair by Gemcitabine do to the other agents?

A

It may increase cytotoxicity

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22
Q

What are examples of topoisomerase inhibitors?

A

Irinotecan and Topotecan

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23
Q

What is Irinotecan?

A

It is a prodrug that is converted mainly in the liver to a more potent metabolite

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24
Q

What is Irinotecan converted into?

A

SN-38 metabolite

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25
Q

What are the pharmacokinetics of camptothecins?

A

Irinotecan and SN-38 mainly eliminated in the bile and feces

Dose reduction is required in liver dysfunction

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26
Q

Mecanism of action of camptothecins?

A

Inhibit topoisomerase I –> S phase

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27
Q

What are the adverse effects of camptothecins?

A

Myelosuppression
Diarrhea

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28
Q

What is an example of topoisomerase inhibitor (epipodophylolotoxins)?

A

Etoposide

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29
Q

What is etoposide?

A

A semisynthetic derivative of podophyllotoxin

30
Q

What is the mechanism of action of Etoposide?

A

Inhibits DNA enzyme topoisomerase II
Cell - cycle phase specific and arrests cells in S phase (or early G2)

31
Q

Pharmacokinetics of Etoposide?

A

Administered IV or orally
Excreted in urine,
Dose reduction in patients with renal dysfunction

32
Q

Adverse effects of Etoposide?

A

Myelosuppression
GI disturbances
Alopecia

33
Q

What is an example of microtubule stabilisers?

A

Texans

34
Q

What are examples of taxanes?

A

Paclitaxel and Docetaxel

35
Q

Which is more potent: Paclitaxel or Docetaxel?

A

Docetaxel

36
Q

What does the original taxmen drug contain?

A

Cremophor and ethanol –> hypersensitivity reaction and myelosuppression

37
Q

What does docetaxel contain?

A

Paclitaxel bound to albumin –> lower incidence of hypersensitivity reactions

38
Q

Mechanism of action of taxanes?

A

Stabilise microtubule formation
Inhibit angiogenesis

39
Q

How does resistance develop with taxanes?

A

Alteration in tubular or tubular binding sites or P-glycoprotein mediated multi drug resistance

40
Q

Pharmacokinetics of taxanes?

A

Infused
Large distribution –> cannot enter CNS
Metabolised by liver
Excreted in bile

41
Q

What are the adverse effects of taxanes?

A

Myelosuppression
Peripheral neuropathy
Fluid retention
Hypersensitivity reactions

42
Q

What are the examples of targeted or biologic therapy?

A

VEGF inhibitors
EGFR inhibitors
Immunomodulatory monoclonal antibodies
ALK inhibitors

43
Q

What is an example of VEGF inhibitors?

A

Bevacizumab

44
Q

What is the mechanism of action of Bevacizumab?

A

Binds to and inhibits VEGF A –> inhibiting angiogenesis

45
Q

Pharmacokinetics of Bevacizumab?

A

IV infusion

46
Q

What are the adverse effects of Bevacizumab?

A

Hypertension
Bleeding !!
Thrombotic Events !!
GI perforation
Proteinuria

47
Q

What are examples of the EGFR inhibitors?

A

Erlotinib and Gefitinib

48
Q

What is the mechanism of action of EGFR inhibitors?

A

Inhibition of EGFR kinase

49
Q

Pharmacokinetics of EGFR inhibitors?

A

Metabolised by the liver by the CYP3A4 enzyme

50
Q

What are the adverse effects of EGFR inhibitors?

A

Skin rash
Diarrhea
Anorexia
Fatigue

51
Q

What is the difference between Afatinib and the other EGFR inhibitors?

A

Afatinib irreversibly blocks all kinases of the ErbB family –> binding to kinase domain –> inhibition of tumor growth

52
Q

What is Osimertinib?

A

Another EGFR inhibitor which also binds irreversibly

53
Q

When is OSimertinib used?

A

1st option for patients who develop resistance to first line therapy (erlotinib and gefitinib)

54
Q

What are the adverse effects of Osimetinib?

A

GI toxicities
Dermatologic toxicities
Pulmonary toxicities

55
Q

What is Necitumumab?

A

An EGFR inhibitor which binds to the human EGFR and blocks the binding of EGFR to its ligands

56
Q

What are the adverse effects of Necitumumab?

A

Cardiopulmonary arrest
Hypomagnesemia
Thromboembolytic event
Dermatologic toxicities
Infusion reactions

57
Q

What happens if necitumumab is given with pemetrexed and cisplatin?

A

Higher morbidity

58
Q

What are the examples of the monoclonal antibodies?

A

Nivolumab and Pembrolizumab

59
Q

What is the mechanism of action of nivolumab and pembrolizumab?

A

PD1 receptor is expressed by activated T cells and serves as checkpoint
PD1 ligand is expressed on numerous human tumours
Through the interaction, T cell activity becomes limited and tumour evades
Nivolumab and pembrolizumab block PD1 from interacting with its receptor –> restoration of T-cell activity

60
Q

Pharmacokinetics of Pembrolizumab?

A

Half life of 22 days

Very minimal drug interactions

61
Q

What is a contraindication of Pembrolizumab?

A

Use of systemic corticosteroids or immunosuppressants should be avoided before the use of drug

62
Q

pharmacokinetics of Nivolumab?

A

Half life of 27 days

63
Q

Adverse effects of Nivolumab?

A

Headache, URTI, abdominal pain

64
Q

General adverse effects of monoclonal antibodies?

A

Immune-mediated toxicities, pneumonitis, colitis and thyroid dysfunction

Depending on severity corticosteroids should be started

65
Q

What is an example of ALK inhibitors?

A

Crizotinib (1st gen)
Alectinib & Ceritinib (2nd gen)

66
Q

Mechanism of action of Crizotinib?

A

Binds to the ATP intracellular domain of activated ALK –> inhibiting phosphorylation and downstream signaling

67
Q

Adverse effects of Crizotinib?

A

Visual disorders
QT prolongation

68
Q

Mechanism of action of Alectinib and Ceritinib?

A

Inhibit autophosphorylation of ALK and downward signalling

69
Q

General adverse effects of Alectinib and Ceritinib?

A

Fatigue
Bradycardia
Hepatotoxicity
Visual disturbances

70
Q

Specific adverse effects of Alectinib?

A

Anemia, constipation, edema and myalgia (alectinib)

71
Q

Specific adverse effects of Ceritinib?

A

QT interval prolongation GI toxicity, pancreatitis, hyperglycemia

Respiratory Drugs (4 decks)

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