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FPP Exam 1 > Anti-Neoplastic Drugs > Flashcards

Anti-Neoplastic Drugs Flashcards

1
Q

Classification of Anti-Neoplastic Drugs

A

Alkylating Agents Antimetabolites Natural Products Misc. Agents Hormone and Hormone Antagonists

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2
Q

Alkylating Agents: Cell Cycle Specificity

A

Cell cycle non-specific: also affects G0 ex: mechlorethamine, carmustine (nitrosoureas)

cell-specific phase non-specific: ex: cyclophosphamide

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3
Q

Alkylating Agents: Side effects

A

“typical” side effects: Hematopoiesis suppression GI Effects Alopecia

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4
Q

Mechlorethamine

A

Alkylating Agent – Prototype cell-cycle nonspecific produces DNA cross-linking Does not cross CNS Hodgkin’s and non-Hodgkin’s lymphoma

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5
Q

Cyclophosphamide

A

Alkylating Agent– cell-cycle phase nonspecific Pro-drug activated by liver cP450s Bladder toxicity: sterile hemorrhagic cystitis (can be partially prevented with mesna)

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6
Q

Carmustine

A

Akylating Agent - cell-nonspecific

crosses BBB very well

Treatment of: brain tumors, multiple myeloma, melanoma

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7
Q

Antimetabolites

A

many are phase specific (usually S-phase)

structural ananlogs of compounds required for itermediary metabolism.

Folate Analogs: Methotrexate

Pyrimidine Analongs: Flourouricil (5-FU)

Cytarabine

Purine Analongs: Mercaptopurine (6-MP)

Misc. Antimetabolites: Hydroxyurea

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8
Q

Methotrexate (MTX)

A

Antimetabolite: Binds to dihydrofolate reductase and prevents formation of tetrahydrofolate

High doses necessary to bind all DHFR followed by rescue of host cells with Leucovorin

Side Effects: intestinal epithelium damage

bone marrow suppression

**renal tubular necrosis **

**displaces other drugs from serum albumin **

Indications: Acute Lymphocytic Leukemia (ALL)

Choriocarcinoma

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9
Q

Fluorouracil (5-FU)

A

Antimetabolite : pyrimadine analog

interferes with thymidylate synthesis and ultimately DNA synthesis

**S-Phase Specific **

Broad spectrum of uses: stomach, **colon, **pancreas, ovary head and neck, **breast, **bladder

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10
Q

Cytarabine

A

Antimetabolite : pyrimadine analog

competes for integration into DNA and causes chain termination

**S-Phase Specific **

Side Effect: **myelosuppression, neurotoxicity **

Uses: Acute Leukemias, Acute Myelocytic Leukemia (AML)

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11
Q

Mercaptopurine (6-MP)

A

Antimetabolite: Purine Analog

Inhibits DNA and RNA synthesis

**S Phase Specific **

treatment of acute leukemias

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12
Q

Hydroxyurea

A

Antimetabolite

inhibits ribonucleotide reductase – prevent DNA synthesis

**Arrests Cells at G1-S interfaces **

Useful in conjunction with radiation

Major use: ** granulocytic leukemia **

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13
Q

Vinca Alkaloids

A

Vincristine

Vinblastine

Bind to tubulin, inhibiting proper formation of microtubules and mitotic spindles

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14
Q

Taxanes

A

enhances assembly and stability of microtubules by binding to the Beta subunit of tubulin

**blocks late in G2 phase **

Paclitaxel

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15
Q

Epipodophyllotoxins

A

Etoposide

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16
Q

Monoclonal Antibodies

A

Trastuzumab

17
Q

Antibiotics

A

Doxorubicin

Bleomycin

18
Q

Vinblastine

A

Blocks tubulin and spindle formation

Strongly myelosuppressive

side effects: epithelial ulcerations

uses: **lymphomas, breast cancer **

19
Q

Vincristine

A

Blocks tubulin and spindle formation

side effects: alopecia, **neuromuscular abnormalities **

uses: **ALL, lymphomas. Wilm’s Tumor, neuroblastoma **

20
Q

Paclitaxel

A

Taxane

interfere with DNA repair, intensifying the effects of DNA damage by cisplatin or cyclophosphamide

side effects: **dose-limiting leukopenia, peripheral neuropathy, myalgia/arthalgia **

uses: refractory ovarian cancer; breast cancer

21
Q

Doxorubicin

A

Antibiotics

cycle-specific phase non-specific

wide spectrum of activity: most widely prescribed agent

lymphomas, breast, orvary, small cell lung cancers

_One of the few drugs with some anti-angiogenic properties _

**Interculates in DNA, distorting DNA helix **

**Causes Lipid peroxidation and free radical generation **

**Binds to DNA and Topoisomerase II **

Side Effects: ****Cardiomyopathy***

**bone marrow suppression **

alopecia

**GI issues **

22
Q

Bleomycin

A

Antibiotics

mixture of iron-contianing glycopeptides that bind to DNA

causes oxidative-like damage to DNA which leads to DNA strand breaks

Phase Specific for G2

uses: **germ cell tumors of testes and ovaries **

**head, neck, lung, lymphomas **

Side Effects: minimal myelosupression

_Pulmonary toxicity _

**skin vesiculation, hyperpigmentation **

23
Q

Etoposide

A

Irreversibily stabilized DNA-topoisomerase II complexes

results in dsDNA breaks that cannot be repaired

**Blocks in late G2 Phase **

uses: **Lymphomas, acute leukemias, small cell lung, testes **

Typical side effects

24
Q

Filgrastim

A

Biological Response Modifier

Granulocyte colony stimulating factor

**Goal is to limit chemotherapy-induced neutropenia **

**-promotes progenitors of neutrophils **

**-expands the absolute population of neutrophils, providing for quicker recovery from bone marrow suppression **

25
Q

Trastuzumab

A

Monoclonal Antibody

Binds to HER2 receptor

Use: **breast cancers that overexpress HER2 **

side effects: Cardiomyopathy , hypersensitivity , infusion reaction

26
Q

Cisplatin

A

platinum coordination complex

activated species which causes DNA crosslinks

**cycle-specific phase-nonspecific **

**wide anti-tumor spectrum **

side effects: ***Nephrotoxicity***

**ototoxicity **

**peripheral neuropathy **

**electrolyte disturbances **

27
Q

Procarbazine

A

activated in vivo to a methylating agent which causes chromosomal damage

uses: hodgkin’s lymphoma

typical side effects

28
Q

Prednisone

A

binds to steroid receptors

may arrest cells at G1

**depresses expression of many growth-related genes **

induces nucleases which may modulate cell lysis

29
Q

Antiestrogenic

A

Estrogen Receptor Antagonists: Tamoxifen, Raloxifene

Aromatase Inhibitor: Letrozole (non-steroidal)

30
Q

Tamoxifen

A

Nonsteroidal **antiestrogen that competitively blocks estrogen receptors in breast tissue **

**generally cytostatic **

uses: **advanced post-menopausal breast cancer **

pre-menopausal metastatic breast cancer

*Is Activated by CYP2D6*

side effects: nausea, menopause-like symptoms, fatigue

31
Q

Letrozole

A

Blocks conversion of androgens to estrogens by inhibiting **Aromatase **

uses: ** 1st-line treatment of post-menopausal locally advanced or metastatic breast cancer **

32
Q

Leuprolide

A

Analong of GnRH

after 2-4 weeks it desensitizes GnRH signaling, decreasing LH?FSH and decreasing testosterone to castration levels

uses: advanced hormonally responsive prostate cancer

side effects: **hot flashes, impotence **

33
Q

Flutamide

A

nonsteroidal antiandrogen that blocks androgen receptors

treatment of **metastatic prostate cancer **

side effects: **gynecomastia, diarrhea, hepatotoxicity **

34
Q

Imatinib mesylate (Gleevac)

A

Approved for CML

Blocks BCR-ABL tyrosine kinase

Inhibits cell proliferation and induced apoptosis

35
Q
A

FPP Exam 1 (1 decks)

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