Chemotherapy Drugs

Front 1

3 broad categories of alkylating agents

Back 1

Nitrogen mustards
Nitrousureas
Platinum analogs

Front 2

5 toxicities of alkylating agents

Back 2

1. myelosuppression (febrile neutropenia)
2. mucositis
3. n/v
4. alopecia
5. secondary malignancies

Front 3

mechlorethamine
(class)

**AE

Back 3

alkylating agent:
nitrogen mustard

**potent vesicant!

Front 4

cyclophosphamide
(class)

**AE

Back 4

alkylating agent:
nitrogen mustard (IV or PO)

**Prodrug, when converted by liver, also produces ACROLEIN --> irritates bladder wall --> hemorrhagic cystitis!
Thus, dose with lots of fluids & Mesna

Front 5

Ifosfamide
(class)

**Ifosfamide vs its analog?

Back 5

alkylating agent:
nitrogen mustard (analog of cyclophosphamide; also activated by liver to the same active metabolites)

**LESS POTENT than cyclophosphamide, thus need 4x the dose to get the same effect. This is problematic because it creates 4x more ACROLEIN --> more hemorrhagic cystitis!
Dose w/ fluids & Mesna

Front 6

Melphalan
(class & indication)

Back 6

alkylating agent:
nitrogen mustard

High dose Melphalan - for autologous HSCT (IV or PO)

Front 7

Bendamustine
(class)

Back 7

COMBINATION AGENT:

Alkylating agent (nitrogen mustard) + Purine analog

Front 8

Carmustine & Lomustine (class)

Back 8

alkylating agent:
nitrousureas

Front 9

Nitrousureas - their PRO?

Back 9

Carmustine & Lomustine are lipophilic, thus have good CNS penetration

Front 10

Nitrousureas - 1 CON and 3 AE's?

Back 10

CON of Carmustine & Lomustine:
DELAYED (4 wk) myelosuppression

AE:
Severe N/V, pulmonary toxicity, hepatotoxicity

Front 11

Cisplatin
(class + 3 AE's)

Back 11

Alkylating Agent: Platinum Analog

NEPHROTOXICITY
Ototoxicity
N/V (Ci-SPLAT-in)
**Thus, dose w/ fluids & anti-emetics!

Front 12

Carboplatin
(class + main AE + AE's compared to Cisplatin)

Back 12

Alkylating Agent: Platinum Analog

Main AE: MYELOSUPPRESSION!!

LESS n/v, neuropathy, & nephrotoxicity vs Cisplatin

Front 13

Carboplatin - how is it dosed?

Back 13

Dosed based on renal function w/ Calvert formula (NOT by body surface area):

Dose = Target AUC (CrCl + 25)

Front 14

Oxaliplatin
(class + 2 AE's)

Back 14

Alkylating Agent: Platinum Analog

AE:
Acute - Cold-induced neuropathy
Cumulative - Peripheral neuropathy

Front 15

Dacarbazine
Class + its use (pro)

Back 15

Alkylating Agent

CNS penetration!

Front 16

Temozolomide
Class + route of administration

Back 16

Alkylating Agent

ORAL; converted to Dacarbazine

Front 17

2 Topoisomerase I inhibitors

Back 17

Irinotecan
Topotecan

"-TECAN"

Front 18

3 Topoisomerase II inhibitors
(1 of them have 4 drug names)

Back 18

1. Anthracyclines (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin)
2. Mitoxantrone
3. Etoposide

Front 19

Anthracyclines
- 4 names
- toxicity (3)

Back 19

Daunorubicin, Doxorubicin, Epirubicin, Idarubicin ("RUBICIN")

AE:
1. CHF after a cumulative dose is reached
2. High, delayed emetogenicity
3. Vesicants

Front 20

Topotecan
- class
- dose-limiting toxicity (1)

Back 20

Topotecan: Topo-I inhibitor

Dose-limiting marrow suppression

Front 21

Irinotecan (CPT-11)
- class
- early & late toxicities (1 each), and how AE's are treated

Back 21

Irinotecan (CPT-11): Topo-I inhibitor

EARLY: cholinergic syndrome --> treat with IV Atropine
LATE: direct GI toxicity (may cause serious dehydration) --> treat with Loperamide
**Diarrhea is a dose-limiting side effect!**

Front 22

Bleomycin - MOA

Back 22

Single & double-stranded breaks in DNA by forming reactive free radicals

Front 23

Bleomycin - MAIN TOXICITY to remember? (+4 others...)

Back 23

Bleomycin AE:
1. PULMONARY FIBROSIS
2. hyperpigmentation
3. rash
4. fever
5. allergic reaction

Front 24

3 main subclasses of Anti-Microtubule agents

Back 24

1. Vinca Alkaloids
2. Taxanes
3. Epothilones

Front 25

MOA of anti-microtubules (3 subclasses)

Back 25

ALL: affect M phase of cell cycle

Vinca alkaloids: inhibit formation of tubulin --> no polymerization into microtubules

Taxanes & Epothilones: prevent breakdown of microtubules

Front 26

Names of the 3 Vinca's

Back 26

Vinblastine
Vincristine
Vinorelbine

Front 27

Which of the vinca alkaloids has the worst neurotoxicity?

Back 27

Vincristine

Front 28

Toxicities of Vinca alkaloids

Back 28

Vincristine: Neurotoxicity & Constipation
Vinblastine / Vinorelbine: Myelosuppression (less neurotoxicity)

ALL 3 are vesicants

Front 29

Names of 3 Taxanes

Back 29

Paclitaxel
Docetaxel
Cabazitaxel

("TAX")

Front 30

Paclitaxel
- class
- AE

Back 30

Taxane (anti-microtubules)

- Neuropathy

**ALL Taxanes & Epothilones require premedication w/ steroids due to solubilizing agents**

Front 31

Docetaxel
- class
- AE

Back 31

Taxane (anti-microtubules)

- Fluid retention syndrome

**ALL Taxanes & Epothilones require premedication w/ steroids due to solubilizing agents**

Front 32

Cabazitaxel
- class
- unique effect

Back 32

Taxane (anti-microtubules)

Crosses BBB, NOT affected by P-glycoprotein

**ALL Taxanes & Epothilones require premedication w/ steroids due to solubilizing agents**

Front 33

Ixabepilone
- class
- unique effect

Back 33

Epothilone

has distinct tubulin binding site --> NOT affected by P-glycoprotein!

**ALL Taxanes & Epothilones require premedication w/ steroids due to solubilizing agents**

Front 34

Anti-Metabolites - which phase of the cell cycle do they affect?

Back 34

S phase

(vs. Anti-microtubules: M phase)

Front 35

3 main classes of anti-metabolites

Back 35

1. Folate antagonists
2. Purine analogs
3. Pyrimidine analogs

Front 36

Methotrexate - class

Back 36

Anti-metabolite: Folate antagonist

Front 37

Thioguanine (6-TG) - class

Back 37

Anti-metabolite: Purine Analog

Front 38

Mercaptopurine (6-MP) - class

Back 38

Anti-metabolite: Purine Analog

Front 39

Nelarabine, Fludarabine, Cladrabine - class

Back 39

Anti-metabolite: Purine Analog

Front 40

Pentostatin - class

Back 40

Anti-metabolite: Purine Analog

Front 41

Capecitabine - class

Back 41

Anti-metabolite: Pyrimidine Analog

Front 42

Cytarabine (ARA-C) - class

Back 42

Anti-metabolite: Pyrimidine Analog

Front 43

Fluorouracil - class

Back 43

Anti-metabolite: Pyrimidine Analog

Front 44

Methotrexate (folate blocker) -
Elimination & where in body does it accumulate?

Back 44

Cleared renally
Accumulates in third-space fluids

Front 45

Methotrexate HIGH DOSE therapy - 3 guidelines?

Back 45

1. Hydrate with bicarbonate-containing fluids until urine pH >7
2. Leucovorin rescue (folinic acid)
3. Monitor MTX blood levels <0.05 uM

Front 46

Methotrexate toxicities (4)

Back 46

Mucositis
Pneumonitis
Renal failure
Increased LFT

Front 47

Which of the purine analogs are oral?

Back 47

Thioguanine (6-TG) & Mercaptopurine (6-MP)

Front 48

Mercaptopurine - what metabolizes it? (MUST REMEMBER THIS)

Back 48

Mercaptopurine is metabolized by Xanthine Oxidase!

Front 49

AE of Fludarabine, Cladrabine, Pentostatin (purine analogs)

Back 49

Immunosuppression - lymphopenia

Front 50

AE of Nelarabine (purine analog)

Back 50

Neurotoxicity

Front 51

Cytarabine (ARA-C) - 3 high-dose AE's

Back 51

1. Marrow suppression
2. Cerebellar (ataxia)
3. Conjunctivitis (treat w/ steroid eye drops)

Front 52

Fluorouracil - AE's with intermittent vs continuous boluses

Back 52

Intermittent bolus (high dose): myelosuppression
Continuous bolus (low dose): hand-food syndrome, GI

Front 53

Which drugs cause hand-foot syndrome?

Back 53

Fluorouracil (pyrimidine analog)
Capecitabine (pyrimidine analog)

Front 54

The 2 DNA hypomethylators?

Back 54

5-Azacitidine
Decitabine

Front 55

Monoclonal Antibodies:

Target of Rituximab / Ofatumumab?

Back 55

CD20

- on B lymphocytes
- >90% of B cell NHL & Leukemias

Front 56

Monoclonal Antibodies:

Target of Alemtuzumab?

Back 56

CD52

- Most NL & Malignant B & T lymphocytes, NK cells, Monocytes, Macrophages
- Refractory CLL
- T-cell Leukemia

Front 57

Monoclonal Antibodies:

Target of Ibritumomab & Tositumomab?

Back 57

CD20, conjugated to radioactive molecules

- for Relapsed and/or refractory CD20+, Follicular NHL
- NOT for pt w/ >25% BM involvement!!!

Front 58

Monoclonal Antibodies:

Target of Brentuximab Vedotin?

Back 58

CD30 + radioactive MMAE (mitotic spindle poison)

- Hodgkin's lymphoma
- anaplastic large cell lymphoma

Front 59

Monoclonal Antibodies:

Target of Denileukin Diftitox? (clue: it's all in the name!)

Back 59

CD25 (IL-2 receptor: DeniLEUKIN), attached to Diphtheria toxin (DIFTitox sounds like DIPHtheria)

- persistent/recurrent cutaneous T cell lymphoma

Front 60

Monoclonal Antibodies:

Target of Trastuzumab / Pertuzumab?

Back 60

HER2/NEU-Receptor (blocks signal)

- Breast cancer

Front 61

What is a serious AE of Trastuzumab / Pertuzumab (HER2/Neu-receptor Ab)?
This AE is made worse when used w/ which 2 drugs?

Back 61

Cardiotoxic!! (CHF)

Especially when used with Cyclophosphamide or Anthracycline

Front 62

Monoclonal Antibodies:

Target of Cetuximab / Panitumumab?

Back 62

EGFR

- overexpressed in many SOLID tumors

Front 63

2 Serious/unique AE of Cetuximab/Panitumumab (EGFR-Ab)?

Back 63

Skin rsh
Electrolyte imbalances

Front 64

Monoclonal Antibodies:

Target of Bevacizumab?

Back 64

VEGF

Front 65

3 Serious AE's of Bevacizumab (Anti-VEGF Ab)?

Back 65

1. PERFORATIONS - GI, TE-Fistulas
2. BLEEDING - impaired wound healing
3. CIRCULATORY - arterial thrombosis, HTN, CHF

Front 66

Monoclonal Antibodies:

Target of Ipilimumab?

Back 66

CTLA-4 (cytotoxic T-lymphocyte-associated antigen 4)

--> blocking CTLA-4 augments T cell activation & proliferation

Front 67

Serious AE of Ipilimumab?

Back 67

T-cell activation can cause fatal immune-mediated AE

Front 68

Which subclasses of monoclonal antibodies are commonly associated w/ infusion-related reactions (urticaria, chills, hypotension, dysrhythmias)?

1. -Momab
2. -Zumab
3. -Umab
4. -Ximab

Back 68

INFUSION REACTIONS are common in:

-MOMAB
-XIMAB

The other 2 are RARE (zumab, umab)

Front 69

Serious AE of Alemtuzumab (Anti-CD52 Ab)?

Back 69

Myelosuppression --> Opportunistic infections (PCP, HSV, CMV)

Front 70

All Tyrosine Kinase Inhibitors are metabolized by...

Back 70

ALL TKI are CYP3A4 substrates!!

Front 71

Common suffix of TKI's

Back 71

"-inib"