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Flashcards in Anticancer Drugs II Deck (38):
1

what are the alkylating agents

MANNT

Methylhydrazines
Alkyl Sulfonates
Nitrogen Mustards
Nitrosoureas
Triazenes

2

mechanism of action of alkylating agents

-transfer of alkyl groups to DNA sites such as N7 position of guanine (there are other sites)

3

what is an additional mechanism that occurs with alkylation agents Nitrosoureas

carbamoylation of lysine residues of proteins through formation of isocyanates

4

what are the nitrogen mustards

CIMM

Cyclophosphamide
Ifosfamide
Mechlorethamine
Melphalan

5

what is cyclophosphamide converted to and by what enzyme

converted to 4 hydroxycyclophosphamide by CYP2B6, which has the most 4 hydroxylase activity

6

adverse effect of cyclophosphamide

Hemorrhage Cystitis

7

what is responsible for the hemorrhage cystitis seen with cyclophosphamide and how can it be prevented

Acrolein, metabolite of cyclophosphamide, is responsible

-prevented by parenteral administration of Mesna, sulfhydryl compound, that reacts with acrolein in the bladder

8

what is Ifosfamide

it is an analogue of cyclophoshamide hence needs Mesna to prevent hemorrhagic cystitis as well

9

what is Mechlorethamine

an alkylating agent that is also a powerful vesicant (blistering agent)

10

what is Melphalan used for

Multiple Myeloma

11

what are the Nitrosoureas

Carmustine (IV)
Lomustine (orally)

12

types of activity do nitrosoureas have (name them)

carmustine and lomustine

they have both alkylating activity and carbamoylating activity

13

clinical application of nitrosoureas (name them)

carmustine and lomustine

they are highly lipid soluble and can cross the BBB so used for brain tumors

14

what is the alkyl sulfonates

Busulfan

15

what is the methylhydrazines

Procarbazine

16

adverse effect of methylhydrazines

-MOA inhibitor and can be potentiated if given with sympathomimetic agents and tyramine containing foods

-carcinogenic: increased risk of secondary cancers as compared to other alkylating agent

17

name the triazenes

dacarbazine

18

what are the two potent vesicant

Triazene: Dacarbazine
Nitrogen mustard: Mechlorethamine

19

what are the platinum complexes

Cisplatin
Carboplatin

20

mechanism of the platinum complexes (name them)

Cisplatin and Carboplatin

inhibits DNA synthesis and binds DNA through formation of cross links

21

Cisplatin is used in combination with what drugs and to treat what

combination with Vinblastin and Bleomycin to treat nonseminomatous testicular cancer

22

adverse effects of platinum complexes (name them)

Cisplatin and Carboplatin

Ototoxicity
Nephrotoxicity
Peripheral Neuropathy

23

what can be used to prevent the Cisplatin induced nephrotoxicity

hydration and diuresis
Amifostine - thiophosphate cytoprotective agent

24

what the anticancer hormonal agents

HORMONAL AGE

Androgen Inhibitors
Glucocorticoids
Estrogen Inhibitors

25

what glucocorticoids is used in treatment of cancer and its mechanism

Prednisone: induces lymphocyte apoptosis

26

name the estrogen inhibitors according to class

-Selective Estrogen Receptor Modulators (SERMs): Tamoxifen and Raloxifene

-Selective Estrogen Receptor Downregulators (SERDs): Fulvestrant

-Aromatase Inhibitors: Anastrozole, Letrozole, Exemestane

27

what are the selective estrogen receptor modulators (SERMs)

Tamoxifen
Raloxifene

28

mechanism of tamoxifen and clinical application

anti estrogen effect at the breast but estrogen receptor agonist in the endometrium and bone

used to treat breast cancer

29

adverse effect of tamoxifen

Endometrial Hyperplasia
Hot flashes
Thromboembolic Events

30

mechanism of Raloxifene

estrogen antagonist in the breast and endometrium

estrogen agonist in the bone (prevent osteoporosis in post menopausal women)

31

what is the selective estrogen receptor downregulators (SERDs)

Fulvestrant

32

mechanism of selective estrogen receptor downregulator (name it) and when used

fulvestrant

pure estrogen antagonist with no agonist activity
-used in tamoxifen resistant breast cancer

33

what are the aromatase inhibitors

Anastrozole
Letrozole
Exemestane

34

mechanism of the aromatase inhibitors

Anastrozole and Letrozole are nonsteroidal competitive inhibitors of aromatase

Exemestane is a steroidal non competitive inhibitor of aromatase

35

what are the androgen inhibitors

Androgen inhibitor: Goserelin and Leuprolide
Androgen Receptor Inhibitor: Flutamide

36

name the androgen receptor inhibitor and its mechanism

Flutamide: non steroid competitive antagonist of the androgen receptor used for prostatic carcinoma

37

adverse of flutamide

mild gynecomastia since it is blocking androgen receptor

38

mechanism of Goserelin and Leuprolide

androgen inhibitors

-gonadotropin releasing (GnRH) analogues that stimulate the release of gonadal hormones

-Initially: 7-10 days, they increase gonadal hormone production which can be inhibited by flutamide

-delayed: with continued GnRH analogues, there becomes an inhibitory action to reduce gonadal hormone release

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