Cancer Chemotherapy Flashcards by Jamaira Belmes

Drugs that act on S Phase

Cytarabine
6-MP
6-Thioguanine
Methotrexate
Hydroxyurea
Etoposide

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Drugs that act on G2 Phase

Bleomycin

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Drugs that act on M Phase

Vinblastine
Vincristine
Paclitaxel

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Drugs that act on G0 Phase (cell cycle non specific)

Alkylating agents
Antitumor
Antibiotics
Nitrosoureas (Lomustine, Carmustine)
Cisplatin

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Use of chemotherapy in patients with localized cancer before performing local therapy (surgery)

Neoadjuvant Chemotherapy

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Chemotherapy done after local treatment procedures such as surgery or radiation

Adjuvant Chemotherapy

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Rescue therapy for Methotrexate

Leucovorin

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Rescue therapy for Cyclophosphamide

2-mercaptoethane sulfonate sodium (MESNA)

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Rescue therapy for Doxorubicin

Dexrazoxane

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Rescue therapy for Cisplatin

Amifostine

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ALKYLATING AGENTS

forms DNA cross links – (-) of DNA synthesis and function

cell cycle non specific

USES:
NHL
breast and ovarian ca
neuroblastoma
CLL
Wilms tumor
Rhabdomyosarcoma

Cyclophosphamide
Ifosfamide
Chlorambucil
Mechlorethamine

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SE of Cyclophosphamide

HEMORRHAGIC CYSTITIS
bone marrow suppression
hepatotoxicity
alopecia
SIADH
cardiac dysfunction
pulmonary toxicity

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ALKYLATING AGENTS

USES:
testicular ca
ovarian and bladder ca
lung and advanced colon ca
pancreatic ca
breast ca
H and N ca
gastroesophageal ca

Cisplatin
Carboplatin
Oxaliplatin

SE:
neurotoxicity (peripheral neuritis, acoustic nerve damage)

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Part of the FOLFOX and FOLFIRI regimen used in the treatment of SOLID tumors that are RESISTANT to Cisplatin and Carboplatin in the basis of mismatch repair defect

Oxaliplatin

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ALKYLATING AGENTS

forms hydrogen peroxide – generates free radicals – DNA strand scission

cell cycle non specific

USES:
HL and NHL
brain tumors

Has the HIGHEST CARCINOGENIC POTENTIAL amongst alkylating agents

Procarbazine

Dacarbazine

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ALKYLATING AGENTS

forms DNA cross links – (-) of DNA synthesis and function

cell cycle non specific

USES:
CML

Busulfan

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SE of Busulfan

PULMONAR FIBROSIS
adrenal insufficiency
skin pigmentation

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ALKYLATING AGENTS

forms DNA cross links – (-) of DNA synthesis and function

cell cycle non specific

USES:
brain tumor
melanoma, skin cancer
CLL

Special alkylating agent because they are DESIGNED for BRAIN TUMORS

lipophilic – cross BBB

NITROSUREAS

Carmustine
Lomustine
Bendamustine

SE:
CNS toxicity (dizziness, ataxia)
N/V
Bone marrow suppression
Skin flushing

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ANTIMETABOLITES

(-) DIHYDROFOLATE REDUCTASE – decreases synthesis of thymidylate, AA< purine nucleotides

(-) AICAR transformylase

S phase

USES:
CHORIOCARCINOMA
acute leukemias
NHL
Primary CNS lymphoma
Breast cancer
H & N cancer
Bladder cancer
RA
Psoriasis 
Ectopic pregnancy

Methotrexate

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SE of Methotrexate

BONE MARROW SUPPRESSION
Pulmonary infiltrates and fibrosis
Mucositis
Crystalluria
Diarrhea

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ANTIMETABOLITES

Inhibits de novo purine nucleotide synthesis

Activated by HGPRT

USES:
AML, ALL
CML
Lymphomas

PURINE

6-Mercaptourine
6-Thioguanine
Azathioprine

SE:
bone marrow suppression
immunosuppression
hepatotoxicity (cholestasis, jaundice, necrosis)

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ANTIMETABOLITES

Inhibits thymidylate synthase, Dihydrofolate reductase and Purine nucleotide synthesis

USES:
mesothelioma
NSCLC

PURINE

Pemetrexed

SE:
hand-foot syndrome (palmar-plantar erythrodysesthesia)

ANTIMETABOLITES

Inhibits thymidylate synthase – inhibition of DNA synthesis and function

THYMINELESS DEATH

USES:
BREAST Ca
COLORECTAL Ca
H & N Ca
bladder ca
anal ca

PYRIMIDINE

5-Fluorouracil

Chemotherapeutic prodrug of 5-FU

TEGAFUR

ANTIMETABOLITES Inhibits DNA synthesis and repair Inhibits ribonucleotide reductase w/ reduced formation of dNTPs USES: AML, ALL CML in blast crisis MOST SPECIFIC for the S PHASE of the CELL CYCLE

PYRIMIDINE Cytarabine

ANTIMETABOLITES Inhibits DNA synthesis and repair Inhibits ribonucleotide reductase w/ reduced formation of dNTPs USES: PANCREATIC Ca NSCLL, Bladder Ca NHL Capecitabine - COLORECTAL ca, HCC, gastroesophageal

Gemcitabine | Capecitabine - oral

NATURAL ANTICANCER DRUGS Prevents microtubule assembly Causes cell arrest at METAPHASE Acts primarily in M phase of cell cycle ``` USES: Acute leukemia Lymphoma Wilms tumor Neuroblastoma Rhabdomyosarcoma ```

VINCA ALKALOIDS Vincristine ``` SE: NEUROPATHY areflexia peripheral neuritis paralytic ileus ```

NATURAL ANTICANCER DRUGS ``` USES: Lymphomas Neuroblastoma Testicular ca Kaposi sarcoma Germ cell tumor Breast ca ```

VINCA ALKALOIDS Vinblastine Vinorelbine SE: BONE MARROW SUPPRESSION alopecia GI distress

NATURAL ANTICANCER DRUGS Inhibits DNA topoisomerase II (DNA gyrase) Inhibits mitochondrial electron transport

PODOPHYLLOTOXIN -TOPO Etoposide Teniposide

NATURAL ANTICANCER DRUGS Inhibits DNA topoisomerase I USES: Tepotecan - advanced ovarian ca, SCLC Irinotecan - metastatic colorectal cancer

CAMPTOTHECIN -TECAN Tepotecan Irinotecan

NATURAL ANTICANCER DRUGS Interferes with MITOTIC SPINDLE Prevents microtubule DISASSEMBLY into tubulin monomers ``` USES: ADVANCED BREAST CANCER and ovarian ca lung ca gastroesophageal ca gastric ca prostate ca ```

TAXANES Paclitaxel Docetaxel Cabazitaxel

SE of Paclitaxel

Neutropenia Thrombocytopenia Peripheral neuropathy

SE of Docetaxel

Neurotoxicity Bone marrow suppression Fluid retention

ANTITUMOR ANTIBIOTICS Intercalates b/w base pairs Inhibits topoisomerase II Generates free radicals -- single and double stranded DNA breaks ``` USES: breast ca HL and NHL lymphoma soft tissue sarcoma endometrial cancer SCLC NSCLC ovarian ca AML, ALL Wilms tumor neuroblastoma ```

ANTHRACYCLINE ``` Doxorubicin Daunorubicin Idarubicin Epirubicin Mitoxantrone ``` SE: DILATED CARDIOMYOPATHY

ANTITUMOR ANTIBIOTICS Generates free radicals -- DNA strand breaks Intercalates with DNA MOST SPECIFIC for G2 phase

Bleomycin Mitomycin SE: PULMONARY FIBROSIS

ANTITUMOR ANTIBIOTICS Binds to double stranded DNA Inhibits DNA dependent RNA synthesis USES: Wilms tumor Rhabdomyosarcoma

Actinomycin | Dactinomycin

HORMONAL ANTICANCER DRUGS Suppresses inflammation and immune response May trigger APOPTOSIS and work on NON DIVIDING cancer cells USES: CLL HL

GLUCOCORTICOID Prednisone

HORMONAL ANTICANCER DRUGS Estrogen antagonist - breast tissue and CNS Estrogen agonist - uterus, liver and bone USES: Hormone sensitive breast ca

SERMS Tamoxifen Toremifene

HORMONAL ANTICANCER DRUGS Competitive antagonist at androgen receptor USES: PROSTATE Ca Surgical castration

ANDROGEN ANTAGONIST Flutamide Bicalutamide Nilutamide

Must be co-administered with flutamide to prevent acute flare-up of prostate cancer

GnRH analogs (Leuprolide)

HORMONAL ANTICANCER DRUGS Increased LH and FSH secretion with INTERMITTENT administration Decreased LH and FSH secretion with PROLONGED CONTINUOUS administration ``` USES: Controlled ovarian hyperstimulation Endometriosis Myoma uteri Precocious puberty Prostate cancer ```

GnRH ANALOG Leuprolide Gonadorelin Nafarelin

HORMONAL ANTICANCER DRUGS Reduces estrogen synthesis by (-) aromatase USES: breast ca (esp in menopausal state) precocious puberty

ESTROGEN SYNTHESIS INHIBITOR Anastrozole Letrozole

Effective against breast cancers that have become resistant to tamoxifen

Anastrozole | Letrozole

Tyrosine kinase inhibitors USES: Chronic Myelogenous Leukemia GIST

``` Imatinib Dasatinib Nilotinib Crizotinib Afatinib Nintedanib Regorafenib ```

TKI also used for idiopathic pulmonary fibrosis

Nintedanib

Acts against breast cancer cells that overexpress the HER-2/neu receptor for epidermal growth factor USES: metastatic breast cancer

Trastuzumab Pertuzumab Lapatinib SE: CHF

Inhibits binding of VEGF to VEGFR -- inhibition of VEGF signaling Inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery

``` Bevacizumab Sorafenib Sunitinib Pazopanib Lenvatinib ```

Binds to a surface protein in NHL cells Induces complement mediated lysis, direct cytotoxicity and induction of apoptosis CD20 (-) USES: NHL (low grade)

Rituximab

Binds to EGFR and (-) downstream EGFR signaling, enhances response to chemotherapy and radiotherapy USES: COLORECTAL Ca H&N Ca NSCLC

Cetuximab Panitumumab Nimotuzumab ``` SE: infusion reaction skin rash hypomagnesemia fatigue interstitial lung disease ```

Inhibits EGFR tyrosine kinase -- inhibition of EGFR signaling USES: NSCLC Pancreatic ca

Erlotinib | Gefitinib

Endogenous glycoproteins with antineoplastic immunosuppressive and antiviral actions USES: Hairy cell leukemia CML T-cell lymphomas

Interferon-alpha

Hydrolyzes circulating L asparaginase -- rapid (-) protein synthesis USES: ALL

Asparaginase

Allows DNA transcription and differentiation of immature leukemic promyelocytes into mature granulocytes

All Trans Retinoic Acid (ATRA)