Shared Flashcard Set

Details

Pharm 8/2 Anti-Cancer
Antineoplastic drugs
25
Pharmacology
Professional
04/18/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
Mechlorethamine (Mustargen®)
Definition

Anti-CA; Alkylating Agent

Use: Hodgkin's disease

Mechanism: Alkylates DNA, casuing miscoding, breakage and cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells

Major Side Effects: ARF; vesicant (tissue damage at injection site) hyperuricema, hematologic tox., other rapidly proliferating cells i.e. BM, GI, sperm, hair; nausea/vomiting (CTZ and local); BM suppression, immuno suppression, teratogenesis, reproduction

Term
Cyclophosphamide (Cytoxan®), Ifosfamide (Ifex®)
Definition

Anti-CA; Alkylating Agent; KNOW THIS GUY!!!

Use: Broad spectrum; breast, lung, ovarian, endometrial, cervical carinomas; for immunosuppression in RA, organ transplant, lupus nephritis; leukemia, lymphomas, Hodgkin's disease, testicular cancer

Mechanism: Pro-drug (CYP450 activates)Alkylates DNA, casuing miscoding, breakage and cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells

Major Side Effects: Acrolein is breakdown product -> hemorrhagic cystitis (MESNA sulhydryl donor blocks); alopecia, hematogic, SIADH 

Other Drugs: Chlorambucil (Leukeran®) - CLL, given for months/years, low tox

Thiotepa - Bladder cancer

Bendamustine (Treanda)- CLL, non-hodgkins lymphoma

Busulfan (Busulfex®) - CML, hyperuricema side effect


Term
Carmustine (BCNU)
Definition

Anti-CA drug: Alkylating Agent (Nitrosurea)

Uses: brain tumor

Mechanism: Enters CNS (highly lipid soluble)Alkylates DNA, casuing miscoding, breakage and cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells

Major Side Effects: PROFOUND MYELOSUPPRESSION

Other Drugs: Lomustine (CCNU) - PROFOUND MYELOSUPPRESSION (also brain tumors)

Streptozocin (Zanosar®) - pancreatic cancer

 

Term
Dacarbazine
Definition

Anti-CA drug; Alkylating agent

Mechanism: Alkylates DNA, causing cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells

Major Side Effects: 

Other Drugs: Procarbazine (Matulane®)

Temozolamide (Temodar®)

Term
Cisplatin (Platinol)
Definition

Anti-CA drug: Alkylating Agent

Uses: testicular cancer

Mechanism: bifunctional alkylating agents, most effective in S phase; Alkylates DNA, casuing cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells

Major Side Effects: renal (amifostin antagonises tox), acoustic nerve damage (HEARING LOSS)

Other Drugs: Carboplatin (Paraplatin®)

Oxaliplatin (Eloxatin®)

Term
Methotrexate (Methotrexate®)
Definition

Antimetabolite

Uses: Leukemia, chriocarcinoma, immunosuppression (RA, psoriasis); burkitt's, non-hodgkins lymphoma, breast carcinoma, head and neck squamous cell carcinoma

Mechanism: inhibits dihydrofolate reductase, blocks synth of tetrahydrofolate from folic acid; blocks DNA, RNA and protein synthesis (as a result); chemotherpeutic effect DECREASED by folinic acid

Side effects: Leucovorin rescues from toxicity of methotrexate, must hydrate (decreased precipitations in renal tubules), hepatotoxicity (long term), pulmonary infiltrates; Apthos ulcer and pancytopenia

Other Drugs: Pemetrexed (Alimta®)

Term
6-Mercaptopurine (Purinethol®)
Definition

Antimetabolite: BIG drug

Uses: Leukemias

Mechanism: Purine analogue; converted by Hypoxanthine guanine phosphoribosyl transferase (HGPRT), interferes with DNA and RNA synthesis

Resistance develops through HGPRT

Metabolized by xanthine oxidase, allopurinol blocks breakdown

Side effects: BM depression, cholestatic jaundice, hyperuricemia (may need allopurinol)

Other Drugs: Thiogaunine - unaffected by allopurinol (not metabolized by xanthine oxidase; causes myelosuppression

Fludarabine (Fludara)

Cladribine (Leustatin®)

Term
5-Fluorouracil (Adrucil®)
Definition

Antimetabolite; BIG drug

Uses: Solid tumors (breast, stomach, esophagus, pancrease); hepatomas, ovarian cancer, cervical cancer, bladder and prostate; topical creame for premalignant keratoses and basal cell carcinomas; Colorectal cancer (combo with leucovorin)

Mechanism: G1 and S phase specific; a Pyrimidine that binds thymidylate synthase (rate limiting step in DNA synth) inhibiting it, blocking DNA synthesis; chemotherapeutic effect ENHANCED by folinic acid

Side effects: GI ulcers, BM depression

Other Drugs: Capecitabine (Xeloda®) - 5 fluorouracil pro-drug; 

Cytarabine

Gemcitabine (Gemzar®)

Hydroxyurea (Hydrea®- radiation recall (if you give this to a person who had radiation before, will get pigmentation at the site of radiation)

Term
Daunorubicin (Cerubidine®)
Definition

Abx

Rationale: Bind DNA base pairs, causing DNA strand scission; interferes with cell replication

Side effects: red urine, cardiomyopathy (dexrazoxane for iron chelation), radiation recall

Term
Doxorubicin (Adriamycin®
KNOW
Definition

Abx; BIG drug

Use: Lymphoma, leukemia, Hodgkin's disease; solid tumors (breast)sarcomas, thyroid carcinoma

Rationale: Bind DNA base pairs, causing DNA strand scission; interferes with cell replication

Side effects: forms free radicals/CARDIOTOXICITY!! (iron makes worse i.e. fenton)

Dexrazoxane chelates iron, decreases toxicity

Other Drugs: Idarubicin (Idamycin®)

Epirubicin (Ellence®)

Valrubicin (Valstar®)

Mitoxantrone (Novantrone®)

Term
Bleomycin Sulfate (Blenoxane®)
KNOW
Definition

Abx

Doesn't suppress BM very much (advantage)

Uses: testicular carcinoma, ovarian carcinoma

Rationale: Directly damages DNA (breaks up DNA) fragmentationmost toxic in late G2 and early M phase

Side effects: PULMONARY FIBROSIS (lance armstrong refused it); anaphylactoid reactions

Other drugs: Dactinomycin (Cosmegen®) - wilm's tumor and rhagdomyosarcoma, choriocarcinoma; vesicant; radiation recall

Mitomycin (Mutamycin®) - has to be activated by CYP 450

Term
Vinblastine Sulfate (Velban®)
KNOW
Definition

Microtubule Agent

Use: Widely used; hodgkin's disase, leukemia in children, non-hodgkin's lymphoma

Mechanism: binds tubulin disrupting mitotic spindle apparatus/prevents segregation of chromosome lined up in metphase/metaphase arrest; M phase specific

Side effect profile: less neurotoxicity but MORE BM depression (blasts bone marrow)

Term
Vincristine Sulfate (Oncovin®)
KNOW
Definition

Microtubule Agent

Use: Testicular carcinoma (bleomycin and cisplatin combo)

Mechanism: binds tubulin disrupting mitotic spindle apparatus/prevents segregation of chromosome lined up in metphase/metaphase arrest; M phase specific

Side effect profile: WORSE for neurotoxicity, peripheral neuropathy (crisps nerves) but little myelosuppression

Term
Paclitaxel (Taxol®)
Definition

Microtubule Agent

Use: breast/ovary carcinoma, lung head and neck carcinomas; kaposi's sarcoma

Mechanism: binds AND STABILIZES tubulin and microtubulin - arresting mitosisG2 and M phase specific (mitosis!); axonal transport disruption

Side effect profile: Peripheral neuropathy, highly myelosuppressive, myalgias, severe hypersensitivity

Other Drugs: Docetaxel (Taxotere) - MORE TOXIC

Term
Etoposide (Vepesid®)
Definition

Anti-CA drug; Topoisomerase Inhibitor

Use: Testicular cancer

Mechanism: forms comples with topoisomerase II resulting in strand breakage of DNA and cell death

Tox: leukopenia, BM suppression

Other Drug: Tenoposide (Vumon®)

Term
Topotecan (Hycamtin®)
Definition

Anti-CA drug: Topoisomerase Inhibitor

Use: Ovarian cancer

Mechanism: topoisomerase I inhibitor

Toxicity:  BM myelosuppressionanemia, leukopenia, thrombocytopenia and neutropenia

Other Drugs: Irinotecan (Camptosar®)

Asparaginase (Elspar®) - ALL, asparagine only used by neoplastic cells, hydrolysis asparagine, leading to hypersensitivity

Term
Imatinib (Gleevec®)
Definition

Tyrosine Kinase Inhibitor

PROTOTYPE

Use: CML

Mechanism: Inhibits Bcr-Abl tyrosine kinase (CML causing)

metabolized by CYP3A4 

Side effects: GI, Diarrhea

Other Drugs: Dasatanib

Erlotinib

Gefinitib

Term
Cetuximab (Erbitux®)
Definition

Growth Factor Receptor Inhibitor

Mechanism: Binds to epidermal growth factor receptor (EGFR), blocking signals for cell growth and survival

Other Drugs: Panitimumab (Vectibix®)

Term
Bevacizumab (Avastin)
KNOW
Definition

Growth Factor Receptor Inhibitor

Use: clear cell renal carcinoma, blioblastoma; injected in eye for macular degeneration

Mechanism: inhibits angiogenesis by blocking vascular endothelial growth factor (VEGF)

Side effect: HTN, proteinuria, thromboembolism; vessel injury and bleeding, delay Sx in pts on this drug

Other Drugs: Sorafenib

Sunitinib - kidney

Pazopanib

Term
Prednisone (Deltasone®)
Definition

Hormone or antagonist

Use (which CA): Leukemia and lympoma

Mechanism: suppresses mitosis in lymphocytes

 

Term
Tamoxifen (Novaldex®)
Definition

Hormone or Antagonist

Use (which CA): prevention of breast CA (prior Hx); therapy of breast cancer

Mechanism: estrogen antagonist in breast

Activated by CYP2D6

Term
Trastuzumab (Herceptin®)
Definition

Hormone or Antagonist

Use (which CA): Metastatic breast cancer

Mechanism: Ab against HER2 protein; only used in pts with HER2 overexpression

Side effect: Cardiomyopathy (DON'T COMBINE WITH DOXIRUBICIN)

Term
Flutamide (Eulexin®)
Definition

Hormone or antagonist

Use (which CA): Metastatic prostate carcinoma

Mechanism: blocks androgen receptor of androgen sensitive tissue or tumors

Term
Rituximab
Definition

Monoclonal Antibody

Use:

Term
Alemtuzumab (Campath®)
Definition

Monoclonal antibody

Use:

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