Antineoplastic Agents Flashcards

1
Q

Alkylating agents used as Antineoplastic

A

Nitrosoureas (Carmustine, Lomustine, Semustine)
Nitrogen Mustards (Cyclophosphamide, Ifosfamide)
Thiotepa
Busulfan
Mechlorethamine
Chlorambucil

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2
Q

MOA of Nitrosoureas

A

Form covalent bonds with nucleophilic groups present on DNA – alkylation of DNA leads to cell death

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3
Q

Nitrosoureas undergo spontaneous 1. _______ ______ with the formation of the 2. _______ ______ ____ from diazohydroxide formed.

A
  1. non-enzymatic degradation

2. 2-chloroethyl carbonium ion

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4
Q

Nitrosoureas activates DNA by liberating isocyanate that attach carboxyl groups to the lysine residues of proteins.

True or False

A

False!!

Nitrosoureas INACTIVATES DNA by liberating isocyanate that attach CARBAMOYL groups to the lysine residues of proteins.

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5
Q

An alkylating agent that is used for the treatments of Hodgkin’s Lymphoma and Chronic lymphocytic leukemia (CLL) with prednisone.

A

Chlorambucil

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6
Q

Utilizes two sulfonate functionalities as leaving grps separated by a four-carbon chain that reacts with DNA.

A

Busulfan

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7
Q

MOPP treatment of Hodgkin’s Lymphoma

A

Mechlorethamine, Oncovin (vincristine), procarbazine, and prednisone

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8
Q

A member of aziridines that is an active alkylating agent.

A

Thiotepa

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9
Q

Platinum-Based Antineoplastic Agents

A

Cisplatin, Oxaliplatin, Carboplatin

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10
Q

Antineoplastic Agents that are structurally related to natural metabolite necessary for cellular growth, Inhibit the production of utilization of these metabolites.

A

Antimetabolites

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11
Q

Drugs under Purine Analogs (M,T,A,P)

A

Mercaptopurine, Thioguanine, Azathioprine, Pentostatine

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12
Q

Pyrimidine Analogs (F,F,C,G)

A

Fluorouracil, Fluxuridine, Cytarabine, Gemcitabine

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13
Q

Folic Acid Analog

A

Methotrexate

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14
Q

These antibiotics disrupt DNA function and cell division.

A

Cytotoxic Antibiotics

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15
Q

MOA of Cytotoxic Antibiotics

A

Planar molecule inserts itself between base pair of DNA (-) topoisomerase

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16
Q

Drugs that are Cytotoxic Antibiotics. (-cin, -mycin)

A
Daunorubicin
Doxorubicin
Dactinomycine
Idarubicin
Valrubicin
Bleomycin
Mitomycine
Plicamycin
Streptozocin
17
Q

Antineoplastic obtained from plants (Plants Products)

A

Epipodophyllotoxins (Etoposide, Tenoposide)
Camptothecins
Vinca alkaloids
Taxanes

18
Q

A semi-synthetic derivative derived from mayapple which inhibits microtubule functions.

A

Epipodophyllotoxins (Etoposide, Tenoposide)

19
Q

Inhibits topoisomerase I and treat various cancers

A

Camptothecins (Topotecan, Irinotecan)

20
Q

MOA of vinca alkaloids

A

Inhibit microtubule synthesis

21
Q

Vinka Alkaloids drugs

A

Vincristine, Vinblastine, vinorelbine

22
Q

Vinka alkaloids are composed of _______ moiety containing the ____ subunit and the ____ moiety containing the ______ subunit joined by a C-C bond

A

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.

23
Q

Paclitaxel, a taxane, is derived from what plant?

Common Name and Scientific Name

A

Pacific Yew (Taxus brevifolia)

24
Q

This antineoplastic agent cause inactivation of asparaginase, depriving all of these important substance

A

L-asparaginase

25
Q

Hormones used under antineoplastic agents

A

Tamoxifen, Goserelin, Trifluoromethylaniline, Mitotane

26
Q

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

A

D. IV

27
Q

Goserelin is an analog of?

A

Gonadotropin-releasing hormone

28
Q

Gonadotropin-releasing hormone receptor inhibits Follicle-stimulating hormone (FSH) and Luteinizing Hormone.

T or F

A

True

29
Q

Selective for adrenal glands

A

Mitotane

30
Q

Drugs under Trifluoromethylaniline

A

Flutamide, Nilutamide, Bicalutamide

31
Q

Trifluoromethylaniline is an __________ and it blocks the effects of _________ and __________.

A

Antiandrogen

Testosterone and Androgens

32
Q

What is the subunit in the cantharanthine moiety of vinca alkaloids?

A

Vinblastine

33
Q

Derivative of 6-Mercaptopurine that is used as an immunosuppressive agent

A

Azathioprine (Imuran)