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Flashcards in Cancer Drugs Deck (49)
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1

Methotrexate

Subclass
Antifloate

MOA:
Inhibit Dihyrofolate reductase (DHFR)

Phase of Action
S-Phase

Schedule or Dose Dependent:
Schedule

DLTs
Mylo

Notable ADEs
Renal dysfunction
Mucositis
CNS toxicity
Hepatotoxicity


DIs
NSAIDs
PPIs
Penicillins


Clinical Pearls:
Distributes into third spaces
Renally eliminated
Requires MTX level monitoring, leucovorin rescue, and sodium bicarbonate with high-doses

2

Pemetrexed

Subclass
antifloate

MOA:
DHFR

Phase of Action
s-phase

Schedule or Dose Dependent:
schedule

DLTs
Mylo

Notable ADEs
rash


DIs
avoid nsaids


Clinical Pearls:
Supplement with folic acid and vitamin B12 to prevent myelosupp. And dexamethasone to prevent rash

3

5-FU

Subclass
Antipyrimidine

MOA:
Uracil Analog
Inactivates thymidylate synthase (TS)
Incorporates into DNA/RNA as a false nucleotide


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Bolus = Myelosupp.
CIV = Diarrhea, hand-food syndrome, mucositis


Notable ADEs
Skin toxicities
Photosensitivity
Ocular toxicity
Myocardial ischemic symptoms
Alopecia


DIs
Inhibitor of CYP2C9 (warfarin)


Clinical Pearls:
Leucovorin needed to increase binding affinity of FdUMP to TS (increases efficacy)

4

Capecitabine

Subclass
Antipyrimidine

MOA:
Uracil Analog
Inactivates thymidylate synthase (TS)
Incorporates into DNA/RNA as a false nucleotide


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Diarrhea, hand-food syndrome, mucositis

Notable ADEs
Skin toxicities
Photosensitivity
Ocular toxicity
Myocardial ischemic symptoms
Alopecia



DIs
Inhibitor of CYP2C9 (warfarin)


Clinical Pearls:
Oral prodrug of 5-FU

5

Cytarabine
(Ara-c)

Subclass
Antipyrimidine

MOA:
Cytosine Analog
Inhibits DNA polymerase



Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Flu-like symptoms
High dose Ara-C causes cerebellar toxicity and conjunctivitis

DIs
N/A


Clinical Pearls:
Corticosteroids prevent flu-like symptoms and topical corticosteroids prevent conjunctivitis

6

Gemcitabine

Subclass
Antipyrimidine

MOA:
Cytosine Analog
Inhibits DNA polymerase and ribonucleotide reductase

Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Flu-like syndrome
Elevated LFTs
Rash


DIs
N/A


Clinical Pearls:
Topical corticosteroids help with rash

7

6-MP

Subclass
Antipurine

MOA:
Guanine analog
Incorporates into DNA as a false purine


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Hepatotoxicity
Jaundice

DIs
Allopurinol
warfarin

Clinical Pearls:
Metabolized by xanthine oxidase

8

Fludarabine

Subclass
Antipurine

MOA:
Adenine analog
Incorporates into DNA as a false purine
Inhibits DNA polymerase
Inhibits ribonucleotide reductase

Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
CNS toxicity
Peripheral neuropathies
Pulmonary toxicity
Seizures
Opportunistic infections

DIs
N/A

Clinical Pearls:
Requires prophylaxis against PCP and HSV

9

Cladribine

Subclass
Antipurine

MOA:
Adenine analog
Incorporates into DNA as a false purine
Inhibits DNA polymerase
Inhibits ribonucleotide reductase

Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Fever
Opportunistic infections


DIs
N/A


Clinical Pearls:
Requires prophylaxis against PCP

10

Clofarabine

Subclass
Antipurine

MOA:
Adenine analog
Incorporates into DNA as a false purine
Inhibits DNA polymerase
Inhibits ribonucleotide reductase


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Elevated LFTs

DIs
N/A

Clinical Pearls:
N/A

11

Hydroxyurea

Subclass
Hydroxyurea

MOA:
Inhibits ribonucleotide diphosphate reductase


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Secondary malignancies
Rash


DIs
N/A

Clinical Pearls:
N/A

12

Vincristine

Subclass
Vinca Alkaloid

MOA:
Microtubule destabilizer


Phase of Action
M Phase

Schedule or Dose Dependent:
Schedule

DLTs
Peripheral neuropathies,
Constipation


Notable ADEs
Alopecia (Severe)

DIs


Clinical Pearls:
LETHAL if administered intrathecally
Doses capped at 2 mg (typically)

13

Vinblastine

Subclass
Vinca Alkaloid

MOA:
Microtubule destabilizer


Phase of Action
M Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp

Notable ADEs
Peripheral neuropathies

DIs


Clinical Pearls:
LETHAL if administered intrathecally

14

Vinorelbine

Subclass
Vinca Alkaloid

MOA:
Microtubule destabilizer

Phase of Action
M Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp

Notable ADEs
Peripheral neuropathies

DIs


Clinical Pearls:
LETHAL if administered intrathecally

15

Paclitaxel

Subclass
Taxanes

MOA:
Microtubule stabilizer


Phase of Action
M Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Hypersensitivity reaction
Peripheral neuropathies
Alopecia (Severe)


DIs


Clinical Pearls:
Contains CREMOPHOR
Premedicate with dexamethasone, diphenhydramine, ranitidine to decrease hypersensitivity reactions
Requires PVC-free bag, tubing and 0.2 micron filter

16

Docetaxel

Subclass
Taxanes

MOA:
Microtubule stabilizer


Phase of Action
M Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Fluid retention, edema, pleural effusions, ascites
Peripheral neuropathies
Alopecia (Severe


DIs


Clinical Pearls:
Contains Polysorbate 80
Premedicate with dexamethasone day before, day of and day after treatment to minimize fluid retention

17

Irinotecan

Subclass
Camptothecins

MOA:
Inhibits topoisomerase I


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Diarrhea

Notable ADEs
Myelosupp.,

DIs


Clinical Pearls:
Acute diarrhea is treated with atropine
Delayed diarrhea is treated with loperamide
Patients with UGT1A1 deficiencies area at high risk of diarrhea

18

Topotecan

Subclass
Camptothecins

MOA:
Inhibits topoisomerase I


Phase of Action
S Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs

DIs


Clinical Pearls:

19

Etoposide

Subclass
Epipodophyllotoxin

MOA:
Inhibits topoisomerase II


Phase of Action
G2 Phase

Schedule or Dose Dependent:
Schedule

DLTs
Myelosupp.

Notable ADEs
Nausea/vomiting, alopecia, mucositis, secondary malignancies,
Alopecia (Severe

DIs


Clinical Pearls:
Oral or IV

20

Bleomycin

Subclass


MOA:
Generates oxygen free radicals leading to DNA strand breaks


Phase of Action
G2 Phase

Schedule or Dose Dependent:
Schedule

DLTs
Pulmonary toxicity

Notable ADEs
Anaphylaxis/ Hypersensitivity reactions, fever, flulike symptoms,

DIs


Clinical Pearls:
PFTs are required to monitor pulmonary toxicity
Maximum lifetime dose >360 units

21

L-asparaginase

Subclass


MOA:
Inactivate asparagine formation, starving leukemic cells of asparagine


Phase of Action
G1 Phase

Schedule or Dose Dependent:
Schedule

DLTs
Hypersensitivity Reactions

Notable ADEs
Pancreatitis
Decreased synthesis of proteins and clotting factors
Hyperglycemia
Hepatotoxicity

DIs


Clinical Pearls:
Derived from E.Coli – DISCONTINUED

22

Peg-asparagase

Subclass


MOA:
Inactivate asparagine formation, starving leukemic cells of asparagine


Phase of Action
G1 Phase

Schedule or Dose Dependent:
Schedule

DLTs
Hypersensitivity Reactions

Notable ADEs
Pancreatitis
Decreased synthesis of proteins and clotting factors
Hyperglycemia
Hepatotoxicity


DIs


Clinical Pearls:
Derived from E.Coli – polyethylene glycol decreases immunogenicity and prolongs duration of action

23

Erwinia asparaginase

Subclass


MOA:
Inactivate asparagine formation, starving leukemic cells of asparagine


Phase of Action
G1 Phase

Schedule or Dose Dependent:
Schedule

DLTs
Hypersensitivity Reactions

Notable ADEs
Pancreatitis
Decreased synthesis of proteins and clotting factors
Hyperglycemia
Hepatotoxicity


DIs


Clinical Pearls:
Derived from Erwinia chrysanthemi
Developed due to hypersensitivity to L-asparaginase

24

Everolimus

Subclass


MOA:
Targets mTOR preventing intracellular signaling pathways


Phase of Action
G1 Phase

Schedule or Dose Dependent:
Schedule

DLTs
Notable ADEs
hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypophosphatemia, elevated liver enzymes, elevated SCr, myelosuppression

DIs


Clinical Pearls:
Requires premedication of diphenhydramine

25

Temsirolimus

Subclass


MOA:
Targets mTOR preventing intracellular signaling pathways


Phase of Action
G1 Phase

Schedule or Dose Dependent:
Schedule

DLTs


Notable ADEs
hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypophosphatemia, elevated liver enzymes, elevated SCr, myelosuppression

DIs


Clinical Pearls:
Requires premedication of diphenhydramine

26

Chlorambucil

Subclass
Nitrogen Mustard

MOA:
Covalently binds to DNA


Phase of Action


Schedule or Dose Dependent:
Dose

DLTs
Myelosupp.

Notable ADEs
Secondary malignancies

DIs


Clinical Pearls:
Take on an empty stomach

27

Cyclophosphamide

Subclass
Nitrogen Mustard

MOA:
Covalently binds to DNA


Phase of Action


Schedule or Dose Dependent:
Dose

DLTs
Myelosupp.

Notable ADEs
Secondary malignancies
Hemorrhagic cystitis
Alopecia (Severe)

DIs


Clinical Pearls:
Hydration required to prevent hemorrhagic cystitis
MESNA may be required with high doses

28

Ifosfamide

Subclass
Nitrogen Mustard

MOA:
Covalently binds to DNA


Phase of Action

Schedule or Dose Dependent:
Dose

DLTs
Myelosupp.

Notable ADEs
Secondary malignancies
Hemorrhagic cystitis
Neurotoxicity (somnolence, confusion, disorientation)
Alopecia (Severe)

DIs


Clinical Pearls:
Mesna REQUIRED with all doses
Methylene blue may be utilized for CNS toxicities
Hydration required to prevent hemorrhagic cystitis

29

Cisplatin

Subclass
Platinums

MOA:
Covalently binds to DNA


Phase of Action


Schedule or Dose Dependent:
Dose

DLTs
Nausea/ vomiting

Notable ADEs
Secondary malignancies
Nephrotoxicity
Ototoxocity
Peripheral neuropathies
K/Mg wasting
Myelosupp

DIs


Clinical Pearls:
HIGHLY emetogenic
Hydration required prior to and after each dose

30

Carboplatin

Subclass
Carboplatin

MOA:
Covalently binds to DNA


Phase of Action


Schedule or Dose Dependent:
Dose

DLTs
Myelosupp.

Notable ADEs
Secondary malignancies Nephrotoxicity
Ototoxocity
Peripheral neuropathies


DIs


Clinical Pearls:
Dosed based on CALVERT FORMULA
Dose = AUC x (CrCl + 25)
Cap CrCl at 125 mL/min