Antineoplastic Agents Flashcards
Alkylating agents used as Antineoplastic
Nitrosoureas (Carmustine, Lomustine, Semustine)
Nitrogen Mustards (Cyclophosphamide, Ifosfamide)
Thiotepa
Busulfan
Mechlorethamine
Chlorambucil
MOA of Nitrosoureas
Form covalent bonds with nucleophilic groups present on DNA – alkylation of DNA leads to cell death
Nitrosoureas undergo spontaneous 1. _______ ______ with the formation of the 2. _______ ______ ____ from diazohydroxide formed.
- non-enzymatic degradation
2. 2-chloroethyl carbonium ion
Nitrosoureas activates DNA by liberating isocyanate that attach carboxyl groups to the lysine residues of proteins.
True or False
False!!
Nitrosoureas INACTIVATES DNA by liberating isocyanate that attach CARBAMOYL groups to the lysine residues of proteins.
An alkylating agent that is used for the treatments of Hodgkin’s Lymphoma and Chronic lymphocytic leukemia (CLL) with prednisone.
Chlorambucil
Utilizes two sulfonate functionalities as leaving grps separated by a four-carbon chain that reacts with DNA.
Busulfan
MOPP treatment of Hodgkin’s Lymphoma
Mechlorethamine, Oncovin (vincristine), procarbazine, and prednisone
A member of aziridines that is an active alkylating agent.
Thiotepa
Platinum-Based Antineoplastic Agents
Cisplatin, Oxaliplatin, Carboplatin
Antineoplastic Agents that are structurally related to natural metabolite necessary for cellular growth, Inhibit the production of utilization of these metabolites.
Antimetabolites
Drugs under Purine Analogs (M,T,A,P)
Mercaptopurine, Thioguanine, Azathioprine, Pentostatine
Pyrimidine Analogs (F,F,C,G)
Fluorouracil, Fluxuridine, Cytarabine, Gemcitabine
Folic Acid Analog
Methotrexate
These antibiotics disrupt DNA function and cell division.
Cytotoxic Antibiotics
MOA of Cytotoxic Antibiotics
Planar molecule inserts itself between base pair of DNA (-) topoisomerase
Drugs that are Cytotoxic Antibiotics. (-cin, -mycin)
Daunorubicin Doxorubicin Dactinomycine Idarubicin Valrubicin Bleomycin Mitomycine Plicamycin Streptozocin
Antineoplastic obtained from plants (Plants Products)
Epipodophyllotoxins (Etoposide, Tenoposide)
Camptothecins
Vinca alkaloids
Taxanes
A semi-synthetic derivative derived from mayapple which inhibits microtubule functions.
Epipodophyllotoxins (Etoposide, Tenoposide)
Inhibits topoisomerase I and treat various cancers
Camptothecins (Topotecan, Irinotecan)
MOA of vinca alkaloids
Inhibit microtubule synthesis
Vinka Alkaloids drugs
Vincristine, Vinblastine, vinorelbine
Vinka alkaloids are composed of _______ moiety containing the ____ subunit and the ____ moiety containing the ______ subunit joined by a C-C bond
Vinca alkaloids are composed of CATHARANTHINE moiety containing the INDOLE subunit and the VINDOLINE moiety containing the DIHYDROINDOLE subunit joined by a C-C bond.
Paclitaxel, a taxane, is derived from what plant?
Common Name and Scientific Name
Pacific Yew (Taxus brevifolia)
This antineoplastic agent cause inactivation of asparaginase, depriving all of these important substance
L-asparaginase
Hormones used under antineoplastic agents
Tamoxifen, Goserelin, Trifluoromethylaniline, Mitotane
Which of the following is true about Tamoxifen?
I. Tamoxifen is an estrogen antagonist
II. It is a treatment of estrogen receptor
III. Toremifene, a tamoxifen analog, is used with Chlorine
IV. All of the above
a. I only
b. I and II
c. III only
d. IV
D. IV
Goserelin is an analog of?
Gonadotropin-releasing hormone
Gonadotropin-releasing hormone receptor inhibits Follicle-stimulating hormone (FSH) and Luteinizing Hormone.
T or F
True
Selective for adrenal glands
Mitotane
Drugs under Trifluoromethylaniline
Flutamide, Nilutamide, Bicalutamide
Trifluoromethylaniline is an __________ and it blocks the effects of _________ and __________.
Antiandrogen
Testosterone and Androgens
What is the subunit in the cantharanthine moiety of vinca alkaloids?
Vinblastine
Derivative of 6-Mercaptopurine that is used as an immunosuppressive agent
Azathioprine (Imuran)
