Antineoplastic Agents II Flashcards

1
Q

Cyclophosohamide MOA
Uses (2)
Primary toxicity and antidote

A

Nitrogen mustard alkylating agent
Solid tumors and hematological malignancies
Hemorrhagic cystitis…antidote is mesna

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

Carmustine (BCNU) MOA
Use
Primary toxicity

A

Nitrosource alkylating agent
Brain tumors (wafers and stuff)
Myelosuppression

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

4 adverse effects of alkylating agents

A
  1. Mutagenic
  2. Myelosuppressive
  3. Leukemia
  4. Strong vesicant properties
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Common resistance mechanisms to alkylating agents

A
  1. Inactivation by glutathione
  2. Reduced uptake
  3. Accelerated DNA repair
  4. Increased expression of MGMT (removed alkyl groups from guanine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

MOA of non-classical alkylating agents

A

Lead to DNA cross-linkages but do NOT have alkyl groups

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

3 common non-classical alkylating agents (Platinum compounds)

A
  1. Cisplatin
  2. Carboplatin
  3. Oxaliplatin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Adverse effects of Cisplatin (2)

A
  1. Peripheral motor and sensory neuropathy

2. Nephrotoxicity

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

Primary differences between Cisplatin and Carboplatin (2)?

A
  1. Carboplatin causes less nausea, neurotoxicity, ototoxicity, and nephrotoxicity than cisplatin
  2. Dose-limiting toxicity for carboplastin is myelosuppresion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Vinacristine MOA

Primary toxicity

A

Inhibits microtubule formation preventing mitotic spindle formation. This causes cell to arrest in mitosis causing cell death
Primary toxicity is neurological

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Vinablastine MOA

Primary toxicity

A

Inhibits microtubule formation preventing mitotic spindle formation. This causes cell to arrest in mitosis causing cell death
Primary toxicity is myelosuppresion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Paclitaxel MOA

Primary toxicity

A

Kills tumor cells by preventing depolymerization of microtubules thereby arresting cells in mitosis
Primary toxicity is peripheral neuropathy

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

What drug is commonly given with paclitaxel to reduce myelosuppression?

A

Filgrastin (G-CSF)

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

Topoisomerase I inhibitors (2)

Topoisomerase II inhibitor

A
  1. Irinotecan and Topotecan

2. Etoposide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q
Doxorubicine MOAs (2)
Primary toxicity and antidote
A
  1. Intercalates with DNA and inhibits topoisomerase II thereby causing DNA damage
  2. Also binds to iron and generates free radicals which cause DNA and protein damage
  3. Primary toxicity is irreversible cardiomyopathy. Antidote is dexrazoxane
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Bleomycin MOA

Primary toxicity

A
  1. Small peptide that binds to DNA and causes single and double strand breaks. It causes cells to arrest in G2
  2. Primary toxicity is irreversible pulmonary toxicity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Prednisone and dexamethasone MOA for cancer

A

Inhibit lymphocyte proliferations and decreases intracranial pressure

17
Q

Tamoxifen MOA

Primary toxicity

A

Partial competitive estrogen receptor antagonist that decreases growth of estrogen dependent breast cancers

Patients are at increased risk of endometrial cancer

18
Q

Anastrozole MOA

A

Aromatase inhibitor which lowers estrogen levels

19
Q

Flutamide MOA

A

Prevents dihydrotestosterone from binding to androgen receptors. Useful for prostate cancers

20
Q

GnRH agonists

GnRH antagonist

A

Leuprolide an goserelin are GnRH agonists

Degarelix is an GnRH antagonist

21
Q
Trastuzumab MOAs (2)
Primary toxicity
A

HER-2 inhibitor and blocks HER-2 mediated signaling. Can also induce antibody dependent cytotoxicity
Toxicity: Irreversible cardiac toxicity (CHF)

22
Q

Cetuximab MOA

Primary use

A

Monoclonal antibody that binds to EGFR and blocks signaling.

Useful for colorectal cancers

23
Q

Bevacizumab MOA

A

Monoclonal antibody directed against VEGF…prevents angiogenesis

24
Q

Lapatinab MOA

Primary use

A

Small molecule that inhibits both EGFR and HER-2 kinase activity.
Used to treat HER-2 amplified, trastuzumab-refractory breast cancer

25
Q

Erlotininb

Primary use

A

Oral, small molecule EGFR inhibitor

First line treatment of metastatic nonsmall cell lung carcinoma with EGFR mutations at exon 19 or 21

26
Q

Imatinib MOA
Primary use
Resistance mechanism

A

Small molecule inhibitor of BCR-ABL and thereby inhibits growth signaling
Treats chronic myelogenous leukemia caused by Philadelphia chromosome translocation
Point mutations in BCR-ABL cause a reduced affinity for Imatinib

27
Q

Asparaginase MOA
Use
Adverse effect

A

Hydrolyzes L-asparagine into L-aspartate
Treats Acute Lymphoblastic leukemia (ALL)
Primary adverse effect is allergic reaction

28
Q

Bortezomib MOA
Use
Toxicity

A

Inhibits proteasome causing increases in p53
Treats relapsed or refractory multiple myeloma
Peripheral neuropathy

29
Q

Temsirolimus MOA

Use

A

Inhibition of mTOR complex 1 which reduces protein translation, promotes cell cycle inhibition, and promotes apoptosis
Treats renal cell carcinoma