ANTINEOPLASTICS Flashcards by Karrizze Basto

Q

1 gram of tumor is equivalent to

A

10^9 or 1 billion cells

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Q

A very common adverse reaction of alkylating agents used in the tx of cancer

A

Alopecia

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

Alkylating agents replace H with an alkyl group, which causes ____.

A

DNA strand breakage

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

Mainstay therapy for solid tumors followed by autologous bone marrow transplantation

A

Thiotepa

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

Dialkylating agent drug of choice for Hodgkin’s disease

A

Mechlorethamine

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

For germ cell testicular cancer

A

Ifosfamide

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

Causes sulfur stripping

A

Busulfan

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

Cell cycle non-specific phosphoramide mustard (major metabolite)

A

Cyclophosphamide

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

For multiple myeloma

A

Melphalan

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Q

ALKYLATING AGENTS: NITROGEN MUSTARDS

1st line agent for chronic lymphocytic leukemia and macroglobulinemia

A

Chlorambucil

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Q

ALKYLATING AGENTS: ORGANOPLATINUM

MOA of organoplatinum

A

DNA strands cross-linking

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Q

ALKYLATING AGENTS: ORGANOPLATINUM

Most reactive and most effective in platinating DNA

A

Cisplatin

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Q

ALKYLATING AGENTS: ORGANOPLATINUM

Carboplatin is administered with ____ to reduce toxicity

A

1,1-cyclobutane-dicarboxylate

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Q

ALKYLATING AGENTS: ORGANOPLATINUM

____ is administered with 1,1-cyclobutane-dicarboxylate to reduce toxicity

A

Carboplatin

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Q

ALKYLATING AGENTS: ORGANOPLATINUM

Activated in low chloride environment, not recognized by MMR

A

Oxaliplatin

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Q

ALKYLATING AGENTS

Alkylates DNA with restricted uncoiling and replication of strands

A

Nitrosoureas

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Q

ALKYLATING AGENTS: NITROSOUREAS

1st line agent for metastatic brain tumor

A

Lomustine

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Q

ALKYLATING AGENTS: NITROSOUREAS

2nd line agent for Hodgkin’s disease

A

Lomustine

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Q

ALKYLATING AGENTS: NITROSOUREAS

For brain tumors and can penetrate BBB

A

Carmustine

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Q

ALKYLATING AGENTS: OTHERS

3 agents for Hodgkin’s lymphoma

A

Mechlorethamine
Lomustine
Procarbazine

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Q

ALKYLATING AGENTS: OTHERS

2 agents that form DNA adducts

A

Dacarbazine
Temozolomide

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Q

ALKYLATING AGENTS: OTHERS

Involved in hydroxylation of methyl group

A

Altretamine

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Q

ALKYLATING AGENTS: OTHERS

2nd line agent for ovarian cancer

A

Altretamine

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Q

ALKYLATING AGENTS: OTHERS

Induces hyperglycemia on animal model

A

Streptozocin

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# ALKYLATING AGENTS: OTHERS Source of streptozocin

Streptomyces achromogenes subsp. Strepzoticus

# ALKYLATING AGENTS: OTHERS Antineoplastic that is not considered an anti-metabolite

Etoposide

Compounds closely related in structure to a cellular precursor (N-base)

Anti-metabolites

# ANTI-METABOLITES MOA of anti-metabolites

Prevention of biosynthesis by enzyme inhibition

# ANTI-METABOLITES Designed to interact at cofactor sites for enzymes involve in the biosynthesis of nucleic acid bases

Folates (Anti-folates)

# ANTI-METABOLITES: FOLATES First drug to produce substantial remissions in leukemia

Methrotrexate (MTX)

# ANTI-METABOLITES: FOLATES MOA of Methrotrexate (MTX)

1. Dihydrofolate reductase binding (DHFR) 2. Thymidylate synthase (TS) interference

# ANTI-METABOLITES: FOLATES A pyrrolopyrimidine analog

Pemetrexed

# ANTI-METABOLITES: FOLATES MOA of Pemetrexed

Thymidylate synthase (TS) inhibition

# ANTI-METABOLITES: FOLATES Structually similar to MTX and approved for the tx of pneumocystis carinii pneumonia (PCP) in HIV/AIDS patients

Trimetrexate

# ANTI-METABOLITES: FOLATES MOA of hydroxyurea

Ribonucleotide Reductase inhibition

# ANTI-METABOLITES: PURINES MOA of 6-mercaptopurine

De Novo Purine synthesis blocking

# ANTI-METABOLITES: PURINES Primary treatment for acute leukemia

6-mercaptopurine + 6-thioguanine

# ANTI-METABOLITES: PURINES For chronic lymphocytic leukemia and non-Hodgkin's lymphoma

Fludarabine

# ANTI-METABOLITES: PURINES Deoxyadenosine analog for hairy cell leukemia

Cladribine

# ANTI-METABOLITES: PURINES MOA of Pentostatin

Adenosine deaminase inhibition -> increase dATP

# ANTI-METABOLITES: PYRIMIDINES Palliative tx of carcinoma of the breast, colon, pancreas, rectim, and stomach

5-Fluorouracil (5-FU)

# ANTI-METABOLITES: PYRIMIDINES Fluoropyrimidine deoxynucleoside analog for GI adenocarcinoma metastatic to the liver

Floxuridine (FUDR)

# ANTI-METABOLITES: PYRIMIDINES MOA of 5-FU and FUDR

Thymidylate synthase (TS) inhibition -> DNA synthesis inhibition

# ANTI-METABOLITES: PYRIMIDINES Fluoropyrimidine carbamate prodrug of 5-FU for metastatic breast and colorectal cancer

Capecitabine

# ANTI-METABOLITES: PYRIMIDINES Drug of choice for locally advanced or metastatic adenocarcinoma of the pancreas

Gemcitabine | (+) Cisplatin

# ANTI-METABOLITES: PYRIMIDINES Drug of choice for inoperable locally advanced or metastatic NSCLC

Gemcitabine

# ANTI-METABOLITES: PYRIMIDINES A potent radiosensitizer

Gemcitabine

# ANTI-METABOLITES: PYRIMIDINES Cytosine arabinoside tx for acute agranulocytic leukemia

Cytarabine

# ANTIBIOTICS Antibiotic that do not possess clinically useful anti-malignant property

Streptomycin

# ACTINOMYCIN Source of dactinomycin

Strep. parvilus

# ACTINOMYCIN Tx of rhabdomyosarcoma and Wilms' tumor in children

Dactinomycin

# ACTINOMYCIN Lifesaving tx for women with choriocarcinoma resistant to MTX

Dactinomycin

# ANTHRACYCLINES MOA of anthracyclines

1. Topoisomerase II inhibition 2. Intercalation of the planar ring system

# ANTHRACYCLINES Isolated from Strep. peucetius for non-lymphocytic and lymphocytic leukemia

Daunorubicin

# ANTHRACYCLINES Cardiotoxic isolated from Strep. peucetius var. caesius

Doxorubicin

# ANTHRACYCLINES No 4-methoxy group and terminal side chain for blast phase chronic myelogenous carcinoma | Less cardiotoxic than doxorubicin

Idarubicin

# ANTHRACYCLINES 4'-epimer of doxorubicin

Epirubicin

# ANTHRACYCLINES BCG-refractory carcinoma of urinary bladder

Valrubicin

# ANTHRACYCLINES Tint urine blue

Mitoxantrone

# GLYCOPEPTIDES Isolated from Streptomyces verticillus

Bleomycin

# GLYCOPEPTIDES Palliative treatment of squamous cell carcinoma with no myelotoxicity (bone marrow)

Bleomycin

# GLYCOPEPTIDES Isolated from Streptomyces caespitosus

Mitomycin C

# GLYCOPEPTIDES Bioreductive alkylating agents

Mitomycin C

# EPIPODOPHYLLOTOXIN (PLANT PRODUCTS) Source of epipodophyllotoxins

Mayapple (Mandrake) Root

# EPIPODOPHYLLOTOXIN (PLANT PRODUCTS) MOA of epipodophyllotoxins

Inhibition of microtubule function (topoisomerase II)

# EPIPODOPHYLLOTOXIN (PLANT PRODUCTS) For testicular cancer and small cell lung cancer

Etoposide

# EPIPODOPHYLLOTOXIN (PLANT PRODUCTS) A more potent inhibitor of topoisomerase II for acute lymphoblastic leukemia

Teniposide

# CAMPTOTHECINS (PLANT PRODUCTS) MOA of camptothecins

Inhibitors of topoisomerase I

# CAMPTOTHECINS (PLANT PRODUCTS) Source of camptothecins

Camptotheca acuminata

# CAMPTOTHECINS (PLANT PRODUCTS) Semi-synthetic analog of camptotechin

Irinotecan

# CAMPTOTHECINS (PLANT PRODUCTS) Drug of choice for metastatic colon cancer

5-FU + Leucovorin + Irinotecan

# CAMPTOTHECINS (PLANT PRODUCTS) 2nd line single agent in colorectal cancer

Irinotecan

# CAMPTOTHECINS (PLANT PRODUCTS) A/E: Microscopic hematuria (blood in urine)

Topotecan

# VINCA ALKALOIDS (PLANT PRODUCTS) Source of vinca alkaloids

Catharanthus roseus (periwinkle)

# VINCA ALKALOIDS (PLANT PRODUCTS) MOA of vinca alkaloids

Arrest of mitosis (Inhibition of microtubule polymerization)

# VINCA ALKALOIDS (PLANT PRODUCTS) Dihydroindole nitrogen attached to vincristine

Formyl

# VINCA ALKALOIDS (PLANT PRODUCTS) Dihydroindole nitrogen attached to vinblastine

Methyl

# VINCA ALKALOIDS (PLANT PRODUCTS) ABVD regimen used in the treatment of Hodgkin’s lymphoma

1. Adriamycin 2. Bleomycin 3. Vinblastine 4. Dacarbazine

# VINCA ALKALOIDS (PLANT PRODUCTS) Extravasation with the use of vincas is managed by ____.

Hyaluronic Acid + Heat

# VINCA ALKALOIDS (PLANT PRODUCTS) Semi-synthetic agent for NSCLC

Vinorelbine

# TAXANES (PLANT PRODUCTS) Source of taxanes

Taxus brevifolia or Taxus baccatta (pacific yew tree)

# TAXANES (PLANT PRODUCTS) Taxanes are administered with ____ and ____ due to poor water solubility

1. Cremophor EL 2. Ethanol

# TAXANES (PLANT PRODUCTS) MOA of taxanes

β-tubulin binding | same with vincas

# TAXANES (PLANT PRODUCTS) Highly plasma protein bound drug that promotes assembly of microtubules and may cause bradycardia

Paclitaxel

# TAXANES (PLANT PRODUCTS) Semi-synthetic taxane that can cause reversible fluid retention

Docetaxel

# TAXANES (PLANT PRODUCTS) Semisynthetic amide analog of epothilone B from Sorangium cellulosum

Ixabepilone

# PROTEIN (TYROSINE) KINASE INHIBITORS Enzymes that add a phosphate (PO4) group to a protein or other organic molecule, which can turn a protein off

Protein kinases

# PROTEIN (TYROSINE) KINASE INHIBITORS Inhibits epidermal growth factor receptor

Erlotinib | A/E: Acne, Diarrhea

# PROTEIN (TYROSINE) KINASE INHIBITORS Inhibits BCR-ABL kinase and c-kit kinase

Imatinib

# PROTEIN (TYROSINE) KINASE INHIBITORS Inhibits HER2/NEU activity

Lapatinib

# PROTEIN (TYROSINE) KINASE INHIBITORS Inhibits intracellular and cell surface kinase like VEGFR

Sorafenib

# PROTEIN (TYROSINE) KINASE INHIBITORS Inhibits receptor tyrosine kinases

Sunitinib

# HORMONES Androgen receptor antagonist for advance prostate cancer

Bicalutamide and Flutamide

# HORMONES Binds to estrogen receptor for the tx of metastatic breast cancer

Fulvestrant

# HORMONES Inhibits gonadotropin secretion for prostate cancer

Leuprolide acetate

# HORMONES A progesterone antagonist for advanced breast or endometrial cancer

Megestrol acetate

# HORMONES Selective Estrogen Receptor Modulator (SERM) for advanced breast cancer in postmenopausal women

Tamoxifen

# HORMONES Selective Estrogen Receptor Modulator (SERM) for advanced breast cancer in postmenopausal women

Tamoxifen

# HORMONES A non-steroidal triphenylethylene agent for advanced breast cancer

Tamoxifen

# HORMONES Benzothiophene derivative SERM

Raloxifene

# HORMONES Palliative treatment for advanced prostate carcinoma, breast cancer, and endometriosis

Goserelin

# HORMONES For inoperable adrenal cortical carcinoma

Mitotane

# HORMONES Palliative treatment for metastatic breast cancer

Dromostanolone

# HORMONES Palliative treatment for advanced or disseminated breast cancer

Testolactone

# HORMONES For Cushing's syndrome

Aminoglutethimide

# HORMONES SERM for metastatic breast cancer

Toremifene

# HORMONES Blocks conversion of androgen to estrogen

Aromatase Inhibitors

# AROMATASE INHIBITORS (HORMONES) For hormone dependent breast cancer

Exemestane

# AROMATASE INHIBITORS (HORMONES) First specific aromatase inhibitor for locally advanced or metastatic breast cancer

Anastrozole

# AROMATASE INHIBITORS (HORMONES) Nonsteroidal aromatase inhibitors for locally advanced or metastatic breast cancer

Letrozole

# IMMUNOTHERAPY For hairy cell leukemia and hairy cell leukemia in patients 18 years old or older

Interferon Alfa-2A

# IMMUNOTHERAPY For hairy cell leukemia and malignant melanoma

Interferon Alfa-2B

# IMMUNOTHERAPY Stimulates T-Cell growth and regulation, proliferation and immunoglobulin production in B lymphocytes, and macrophage activity enhancement

Aldesleukin

# MONOCLONAL ANTIBODIES Binds to B and T cells

Alemtuzumab

# MONOCLONAL ANTIBODIES Binds to vascular endothelial growth factor

Bevacizumab

# MONOCLONAL ANTIBODIES Binds to CD33 on leukemic cells

Gemtuzumab

# MONOCLONAL ANTIBODIES Binds to CD20 on lymphoid cells

Tositumomab

# MONOCLONAL ANTIBODIES Genetically engineered chimeric monoclonal antibody against CD20 antigen expressed on the surfaces of malignant B lymphocytes

Rituximab

# MONOCLONAL ANTIBODIES Single agent for metastatic breast cancer

Trastuzumab

# MONOCLONAL ANTIBODIES Binds with human epidermal growth factor receptor type 2 (HER2) and neu receptor

Trastuzumab

# PROTEOSOME INHIBITOR 2 proteosome inhibitors

1. Bortezomib 2. Vorinostat

# MISCELLANEOUS For acute promyelocytic leukemia (APL)

Arsenic Trioxide

# MISCELLANEOUS For cutaneous T-cell lymphoma in patient refractory prior to systemic theraphy

Bexarotene

# MISCELLANEOUS Adjunct therapy to prevent rejection of renal heterotransplants

Azathioprine

# MISCELLANEOUS Enzyme from E. coli

Asparaginase

# MISCELLANEOUS MOA of Asparaginase

Reduces asparagine in plasma makng it unavailable for leukemic cells

# MISCELLANEOUS Promotes bone marrow recovery in patients who underwent autologous bone marrow transplantation

Sargramostim

# MISCELLANEOUS GM-CSF from Saccharomyces cerevisiae or E. Coli

Sargramostim

# CYTOPROTECTIVES For ifosfamide-induced hemorrhagic cystitis

Mesna

# CYTOPROTECTIVES Reduce accumulative toxicity from cisplatin and xerostoma

Amifostine

# CYTOPROTECTIVES Potent intracellular chelating agent to reduce doxurubicin toxicity

Dexrazoxane