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Ther 201 3rd Exam > Antineoplastics 1 > Flashcards

Antineoplastics 1 Flashcards

0
Q

Fraction of tumor cells in replicative phase

A

Growth fraction

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1
Q

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

A

Skipper’s law

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2
Q

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

A

Gompertzian growth

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3
Q

Active in al phases except g0

A

Phase nonspecific

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4
Q

Active in one phase of the cycle

A

Phase specific

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5
Q

Active even in g0

A

Cell cycle nonspecific

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6
Q

Cell cycle specific agents

A

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

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7
Q

Cell cycle nonspecific

A

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

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8
Q

Goals of cancer treatment

A

Cure
Palliative
Adjuvant

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9
Q

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

A

Goldie Coldman Hypothesis

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10
Q

Drug resistance mechanisms

A 
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
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11
Q

Advantages of combination chemotherapy

A

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

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12
Q

Inhibits dihydrofolate reductase, inhibits purine and dtmp biosysnthesis

A

Methotrexate

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13
Q

Terminates dna chain elongation, incorporated into dna and rna

A

Cytarabine

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14
Q

Intercalates with dna disrupting its function

A

Dactinomycin
Daunorubicin
Doxorubicin

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15
Q

Inhibits de novo synthesis of purine ring

A

6 mercaptopurine thioguanine

16
Q

Inhibits dTMP synthesis

A

5 fluorouracil

17
Q

Scission of DNA by an oxidative process

A

Bleomycin peptide antibiotics

18
Q

Crosslinks and fragments nucleic acids

A

Alkylating agents
Nitrosureas
Cisplatin

19
Q

Alkylating agents moa

A

Alkylation of DNA at N7 of guanine

20
Q

Cell cycle specific, alkylating agents?

A

NO! Nonspecific, but replicating cells are most susceptible

21
Q

First of nitrogen mustard used clinically

A

Mechlorethamine

22
Q

Fastest acting nitrogen mustard

A

Mechlorethamine

23
Q

Hodgkin’s disease MOPP

A

Mustargen/mechlorethamine
Oncovin/vincristine
Procarbazine
Prednisone

24
Q

ABVD, newer for hodgkins

A

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

25
Q

Mechlorethamine toxicities

A

Nausea and vomiting
Severe myelosuppression
Inc incidence of leukemias

26
Q

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

A

Cyclophosphamide

27
Q

Very broad spectrum, component of combination therapy

A

Cyclophosphamide

28
Q

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

A

Cyclophosphamide

29
Q

Phenylalanine derivative of nitrogen mustard, not a vesicant, oral

A

Melphalan

30
Q

Bone marrow depression but
Infrequent nausea and vomiting
No alopecia
No renal, hepatic deficits

A

Melphalan

31
Q

Slowest acting nitrogen mustard, bone marrow depression with high doses, long perio

A

Chlorambucil

32
Q

Nitrosurea, similar to bifunctional alkylating agents but with carbamoylating activity, high lipophilicity, crosses BBB

A

BCNU (carmustine)

33
Q

Alkylsulfonate

A

Busulfan

34
Q

Pulmonary infiltrates and fibrosis

A

Busulfan

35
Q

Inorganic water soluble platinum containing complex

A

Cisplatin

36
Q

Nausea and vomiting
Nephrotoxicity delayed, dose limiting
OTOTOXICITY
Mild to mod myelosuppression

A

Cisplatin

37
Q

Alkylating agents

A 
Mechlorethamine 
Cyclophosphamide 
Busulfan 
Melphalan 
Chlorambucil
BCNU (carmustine)
Cisplatin
38
Q

Nitrogen mustard

A

Mechlorethamine
Melphalan
Chlorambucil

Ther 201 3rd Exam (16 decks)

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