Antineoplastics 1 Flashcards Preview

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Flashcards in Antineoplastics 1 Deck (39)
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0

Doubling time of proliferating cancer cells is constant, straight line on a semilog plot, cell kill 1st order kinetics

Skipper's law

1

Fraction of tumor cells in replicative phase

Growth fraction

2

Cells accumulate slowly at first then there is rapid growth, growth rate about 1/3 of max tumor volume, sigmoid curve

Gompertzian growth

3

Active in al phases except g0

Phase nonspecific

4

Active in one phase of the cycle

Phase specific

5

Active even in g0

Cell cycle nonspecific

6

Cell cycle specific agents

Antimetabolites
Bleomycin
Podophyllin alkaloids (etoposide, vp-16, teniposide, vm 26)
Plant alkaloids (vincristine, vinblastine, paclitaxel)

7

Cell cycle nonspecific

Alkylating agents (busulfan, cyclophosphamide, mechlorethamine, melphalan, thiorepa)
Antibiotics (dactinomycin, daunorubicin, doxorubicin, plicamycin, mitomycin)
Cisplatin
Nitrosureas

8

Goals of cancer treatment

Cure
Palliative
Adjuvant

9

If 1g of tumor, 10^9 cells is the min size of early detection and 10^-5 is the tumor mutation rate per gene then such a tumor might contain 10^4 clones which might be resistant to a given drug

Goldie Coldman Hypothesis

10

Drug resistance mechanisms

Decreased drug transport into cell
Reduced drug activation
Increased drug or active metabolite inactivation
Increased DNA repair
Use of alternate pathway as source of metabolite
Increased drug transport outside of cell
Gene amplification of drug target
Alteration of target to reduce binding

11

Advantages of combination chemotherapy

Higher response rate due to additive effects
Non overlapping host toxicities
Effective against broader range cell lines
May slow down development of or prevent resistance

12

Inhibits dihydrofolate reductase, inhibits purine and dtmp biosysnthesis

Methotrexate

13

Terminates dna chain elongation, incorporated into dna and rna

Cytarabine

14

Intercalates with dna disrupting its function

Dactinomycin
Daunorubicin
Doxorubicin

15

Inhibits de novo synthesis of purine ring

6 mercaptopurine thioguanine

16

Inhibits dTMP synthesis

5 fluorouracil

17

Scission of DNA by an oxidative process

Bleomycin peptide antibiotics

18

Crosslinks and fragments nucleic acids

Alkylating agents
Nitrosureas
Cisplatin

19

Alkylating agents moa

Alkylation of DNA at N7 of guanine

20

Cell cycle specific, alkylating agents?

NO! Nonspecific, but replicating cells are most susceptible

21

First of nitrogen mustard used clinically

Mechlorethamine

22

Fastest acting nitrogen mustard

Mechlorethamine

23

Hodgkin's disease MOPP

Mustargen/mechlorethamine
Oncovin/vincristine
Procarbazine
Prednisone

24

ABVD, newer for hodgkins

Adriamycin (doxorubicin/hydroxydoxorubicin)
Bleomycin
Vinblastine
Dacarbazine (like procarbazine)

25

Mechlorethamine toxicities

Nausea and vomiting
Severe myelosuppression
Inc incidence of leukemias

26

Alkylating agent that is not a vesicant, needs to be converted to active form

Cyclophosphamide

27

Very broad spectrum, component of combination therapy

Cyclophosphamide

28

Less thrombocytopenia, more alopecia, less CNS effect compared to mechlorethamine

Cyclophosphamide

29

Phenylalanine derivative of nitrogen mustard, not a vesicant, oral

Melphalan