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Foundations > Antineoplastics > Flashcards

Antineoplastics Flashcards

1
Q

Mechlorethamine

A

Cell-cycle nonspecific.

Nitrogen Mustard, Alkylating Agent: Bifunctional alkylation; produces DNA crosslinks. Highly reactive and not measurable in blood after seconds

Tx

  1. Rarely used
  2. Hodgkin’s Lymphoma
  3. Non-Hodgkin’s Lymphoma

IV only, will not enter CNS.

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2
Q

Cyclophosphamide

A

Cell-cycle specific, phase non-specific

Nitrogen Mustard, Alkylating Agent

Tx
1. Broad spectrum

Oral or Parenteral, will not enter CNS

SE
1. Bladder toxicity (Sterile Hemorrhagic Cystitis), caused by other product made during activation (Acrolein. Treat acrolein toxicity with mesna.)

Prodrug, activated by liver cytochrome P450s

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3
Q

Carmustine

A

Cell-cycle nonspecific

Nitrosureas, Alkylating Agent

Tx

  1. Brain Tumors
  2. Multiple Myeloma
  3. Melanoma

This class can penetrate CNS

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4
Q

Methotrexate MTX

A

Cell-cycle S-Phase specific
Antimetabolite

Folate Analog: Binds DHF Reductase, preventing THF production. This blocks pyrimidine and purine synthesis.

Tx

  1. Acute lymphocytic leukemia (ALL)
  2. Choriocarcinoma

SE

  1. Intestinal epithelium damage (diarrhea, bleeding)
  2. Bone marrow suppression
  3. Renal tubular necrosis (limited by maintaining alkaline urine)
  4. High serum album binding, can thus increase plasma plasma concentration of other album-binding drugs by competing for binding
  5. Hepatotoxic
  6. CNS abnormality

Methotrexate is given in high doses. Normal cells are rescued with leucovorin, which is a fully reduce folate (folinic acid) that does not need DHFR conversion. Normal cells are better suited to uptake leucovorin than tumor cells, leading to preferential killing.

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5
Q

Fluorouracil (5-FU)

A

Cell-cycle S-Phase specific
Antimetabolite

Pyrimidine Analog: Activated in cells to F-UTP, which limits RNA synthesis, and to FdUMP, which interferes with thmidylate synthase and ultimately DNA synthesis

Tx (very broad, but especially colon and breast)

  1. Stomach, colon, pancreas, ovary, head and neck, breast and bladder.
  2. Basal cell carcinoma

SE

  1. Nausea, anorexia, diarrhea
  2. Myelosuppression
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6
Q

Cytarabine

A

Cell-cycle S-Phase specific
Antimetabolite

Pyrimidine (Cytidine) Analog: Competes for phosphorylation of Cytidine. Causes chain termination as it competes for DNA incorporation

Tx
1. Acute Leukemias (especially acute myelocytic leukemia)

SE

  1. Myelosuppression (dose-limiting)
  2. Neurotoxicity
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7
Q

Mercaptopurine

A

Cell-cycle S-Phase specific
Antimetabolite

Purine Analog: Converted in cells to ribonucleotide that inhibits RNA and DNA synthesis

Tx
1. Acute Leukemias

SE

  1. Bone Marrow Suppression
  2. Vomiting, Nausea, Anorexia
  3. Jaundice

***Careful with people with TPMT deficiencies (severe bone marrow suppression, aplastic anemia)

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8
Q

Hydroxyurea

A

Cell-cycle G1-S interface specific
Antimetabolite

Substituted urea: Blocks ribonucleotide reductase, preventing dNTP formation and DNA synthesis

Tx
1. Granulocytic Leukemia

SE
1. Hematopoietic Depression, GI Disturbances

Useful in conjunction with radiation (cells need dNTPs to repair radiation-induced DNA damage)

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9
Q

Vinblastine

A

Cell-cycle M-phase specific
Vinca Alkaloid

Bind tubulin, block microtubule/mitotic spindle formation

Tx

  1. Lymphomas
  2. Breast Cancer

SE

  1. Strong myelosuppressive (dose-limited)
  2. Epithelial ulcerations
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10
Q

Vincristine

A

Cell-cycle M-phase specific
Vinca Alkaloid

Bind tubulin, block microtubule/mitotic spindle formation

Tx

  1. Acute lymphocytic leukemia (ALL)
  2. Lymphomas
  3. Wilm’ Tumor
  4. Neuroblastoma

SE

  1. Alopecia
  2. Neuromuscular abnormalities
  3. Peripheral Neuropathy
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11
Q

Paclitaxel

A

Cell-cycle late G2 (G2/M interface) specific
Taxane

Enhances stability of microtubules and their assembly by binding the beta-subunit.

Tx

  1. Refractory ovarian cancer
  2. Breast cancer

SE

  1. Dose-limiting leukopenia
  2. Peripheral neuropathy
  3. Myalgia/arthralgia

Also harms DNA repair, intensifies DNA-damaging agents

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12
Q

Doxorubicin

A

Cell-cycle specific, phase nonspecific

Has anti-angiogenic properties. Intercalates DNA, distorts the helix. Causes lipid peroxidation and free radical generation. Binds to DNA + Topoisomerase II

Tx

  1. Wide spectrum
  2. Lymphomas
  3. Breast
  4. Ovary
  5. Small cell lung

SE

  1. Cardiomyopathy
  2. Bone marrow suppression
  3. Alopecia
  4. GI problems
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13
Q

Bleomycin

A

Cell-cycle G2/M phase specific

Mixture of iron-containing glycopeptides that binds DNA. Causes oxidative-like damage to DNA, leading to strand breakage

Tx

  1. Germ cell tumors of testes and ovaries
  2. Head and neck cancer
  3. Lung cancer
  4. Lymphomas

SE

  1. Minimal myelosuppression
  2. Pulmonary toxicity (e.g. pneumonitis, fibrosis), dose related and cumulative (potentially fatal)
  3. Skin vesiculation, hyper pigmentation

Lung and skin have lowest levels of bleomycin hydrolase needed to process drug

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14
Q

Etoposide

A

Cell-cycle G2/M interface specific (late G2)

Irrversibly stabilizes DNA-topoisomerase II complexes, leading to irrepairable dsDNA breaks

Tx

  1. Lymphomas
  2. Acute Leukemia
  3. Small Cell Lung
  4. Tetis

SE

  1. Leukopenia
  2. Nausea, Vomiting, Diarrhea
  3. Alopecia
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15
Q

Filgrastim (G-CSF)

A

Biological Response Modifier

Granulocyte colony stimulating factor: Limits chemotherapy-induced neutropenia by promoting progenitors of neutrophils and expands their population. Quicker bone marrow suppression recovery. Less infection risks and allows maintenance doses to be tolerated without a gap. (all ideal)

SE
1. Bone pain

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16
Q

Trastuzumab

A

Monocolonal antibody that binds to HER2 receptor (human epidermal growth factor receptor)

25-30% of breast cancers overexpress HER2, and these cancers are less responsive to anti-estrogen strategies except for doxorubicin and paclitaxel

Tx
1. Breast cancer

SE

  1. Cardiomyopathy
  2. Hypersensitivity
  3. Infusion reactions (fever, chills)
17
Q

Cisplatin

A

Cell-cycle specific, phase non-specific

Platinum coordination complex

Activated species causes DNA cross links

Tx

  1. Testicular cancer
  2. Ovarian cancer
  3. Head and neck cancer
  4. Small cell lung cancer
  5. Colon cancer
  6. Esophagus cancer

SE

  1. Nephrotoxicity
  2. Ototoxicity
  3. Peripheral neuropathy
  4. Electrolyte disturbances
  5. Nausea and vomiting in ALL patients (100%!)
  6. Myelosuppression
18
Q

Procarbazine

A

Atypical Alkylating Agent: Activated in vivo by liver to a methylating agent causing chromosomal damage. NO CROSS RESISTANCE with other alkylating agents!

G1/S is best

Tx
1. Hodgkin’s lymphoma

SE

  1. Myelosuppression
  2. Nausea and vomiting
19
Q

Prednisone

A

G1 arrest

Steroid: Depresses expression of many growth-related genes, induces nucleases that modulate cell lysis

Tx

  1. Lymphoma
  2. Leukemia
  3. Breast Cancer

SE
1. Immunosuppression

Palliative effects:

  1. Anti-emetic
  2. Appetite stimulant
  3. Anti-inflammatory
20
Q

Tamoxifen

A

Cytostatic; holds sells in G0/G1

Nonsteroidal antiestrogen: Competitively blocks estrogen receptors in breast tissue. Tumor regrows when the agent is withdrawn. Stops cell growth, but does not necessarily kill them. Activated by CYP2D6 (be cognizant of drug interaction and ultrafast metabolizers!)

Tx

  1. Advaned post-menopausal breast cancer
  2. Pre-menopausal metastatic breast cancer
  3. Breast cancer prophylaxis for women at high risk (reduces chance by 45%)

SE

  1. Nausea
  2. Hot flashes
  3. Fatigue
  4. Bone and other musculoskeletal pain
21
Q

Letrozole

A

Aromatase Inhibitor: Blocks conversion of androgens to estrogens.

Tx
1. First line treatment for post-menopausal locally advanced or metastatic breast cancer

SE

  1. Hot flushes
  2. Nausea
  3. Fatigue
  4. Bone and other musculoskeletal pain
22
Q

Leuprolide

A

Antiandrogen

GnRH analog: Stimulates LH and FSH, causing testostorone surge and disease flare initially. After 2-3 weeks, GnRH signaling is desensitized, LH/FSH fall off and testosterone is down to castration-type levels

Tx
1. Advanced, hormonally responsive prostate cancer

SE

  1. Hot flashes
  2. Impotence
23
Q

Flutamide

A

Nonsteroidal antiandrogen: Blocks androgen receptors

Tx
1. Metastatic prostate cancer, can be used in combination with GnRH agonist

SE

  1. Gynecomastia
  2. Diarrhea
  3. Hepatoxicity

Foundations (2 decks)

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