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Pharmac > Anti Cancer Drugs > Flashcards

Anti Cancer Drugs Flashcards

1
Q

Non modifiable risk factors of cancer

A

Genetics
Age: eg prostate Ca
Sex related.
Race.

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2
Q

Modifiable risk factors or cancer

A

Environmental Exposure
Chemical carcinogen
Infections

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3
Q

Principle of Cancer Chemotherapy

A

-Ca chemo cause petal cytotoxic events
- attack is directed at metab sites essential for replication
-lack of specificity of current anti-cancer drugs
- proliferating cells are more susceptible to chemo than non proliferating

-Recommended in disseminated cases or minor metastases following surgery/radiation

-destruction of cells follow first order kinetics: given dose destroys constant fraction of cells

-in most cases combination therapy is more effective

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4
Q

Advantages of combination therapy of anti cancer drugs

A

Maximal effect within range of tolerable toxicity

Improve effectiveness against broader spectrum

Delay/reduce development of resistance

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5
Q

The mutagenic ability of cancer is worse when what particular anti cancer agent is used

A

Alkylating agents

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6
Q

Anti cancer drugs are classified into

A

Cell cycle specific agents
Cell cycle non specific agents

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7
Q

Cell cycle specific agents are divided into

A

Antimetabolites: S-phase eg methotrexate

Topoisomerase II inhibitors : G1 to S

Taxanes: M phase

Vinca alkaloids: M phase

Anti microtubule inhibitors: M phase

Anti Tumor antibiotics: G2 to Mphase eg bleomycin

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8
Q

Cell cycle non specific agents

A

Alkylating agents; bulsafan, camestine, cyclophosphamide
Anti tumor antibiotics
Topoisomerase I inhibitors
Platinum analogues
Antracyclins

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9
Q

AntiMetabolites are further classified into

A

Antifolates: Methrotrexate
Fluoropyrimidines: 5-fluorouracil, capacitabine
Deoxycytidine analogues: Cytarabine
Purine antagonists: Mecaptopurine, 6-thioguanine

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10
Q

What is the MOA of Methotrexate

A

Binds at the active site of dihydrofolate reductase thereby inhibiting synthesis of tetrahydrofolate and consequently thymidilate

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11
Q

Methotrexate is converted to ………… upon which it’s cytotoxic effects rests

A

Polyglutamate metabolite

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12
Q

A common side effects of anti folate’s

A

Myelosupression

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13
Q

What is used to reverse severe adverse effects in patients with methotrexate overdose

A

Leucovorin

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14
Q

What anti folate is used to treat mesothelioma and non-small cell lung cancer

A

Pemetrexate

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15
Q

Examples of antifolates used as anti cancer drugs

A

Methotrexate
Pemetraxate
Pralatrexate

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16
Q

When 5-fluorouracil is activated it gives three metabolites namely;

A

FdUMP: 5 -fluoro- 2’-deoxyuridine- 5’ monophosphate

FUTP

FdUTP

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17
Q

Function/MOA of FdUMP

A

Formation of complex with thymidilate synthase reduces production of folate

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18
Q

Function/MOA of FUTP

A

Incorporated into RNA, interferes with RNA processing

19
Q

Function/MOA of FdUTP

A

Incorporated into cellular DNA, inhibits of DNA synthesis

20
Q

Fluoropyrimidines used in anti cancer therapy

A

5-fluorouracil, capecitabine

21
Q

Capecitabine is converted to 5-fluorouracil by……….. which is found in abundance in solid tumors

A

Thymidine phosphorylase

22
Q

Citrabine is a prodrug, it is converted to its main cytotoxic metabolite by the enzyme

A

Deoxycitidine kinase

23
Q

The main cytotoxic metabolite of citarabine

A

Citrabine triphosphate

24
Q

MOA of citarabine

A

Inhibit DNA polymerase alpha and beta…blocking DNA synthesis

25
Q

Citarabine is used in the treatment of

A

Hematologic malignancy(AML)

26
Q

Purine antagonists are classified into

A

6-thiopurines
Fludarabine
Cladribine

27
Q

6-mecaptopurine is inactive and is metabolized into two forms namely:

A

Monophosphate form
Triphosphate form

28
Q

The monophosphate form of mecaptopurine functions to

A

Inhibit several enzymes of denovo synthesis of purine nucleotide

29
Q

The triphosphate form of mecaptopurine functions to

A

It’s incorporated into RNA and DNA producing defective RNA and DNA

30
Q

Mecaptopurine is metabolized to inactive forms by

A

Xanthine oxidase

31
Q

A common xanthine oxidase inhibitor prescribed with 6-mercaptopurine

A

Allopurinol

32
Q

The MOA of fludarabine and cladribine

A

Triphosphate metabolite inhibits DNA polymerase alpha and beta thereby interfering DNA synthesis

33
Q

Alkylating agents exert their cytotoxicity by

A

Transfer of their alkyl groups to cellular constituents

34
Q

The major site of alkylation within DNA is

A

N7 portion of the guanine

35
Q

Alkylation of guanine results in

A

Misreading
Depurination

36
Q

In the MOA of alkylating agents, Intramolecular cyclisation of alkylating agents form

A

Ethylene imonium ion

37
Q

When are replicating cells most susceptible to alkylating agents

A

Late G1 and S phase of cell cycle

38
Q

Resistance to alkylating agents can be acquired from

A

Increased capability to repair DNA lesions

Decreased transport of alkylating agents into the cell

Increased expression/activity of glutathione and glutathione associated proteins

Increased glutathione 5 transferase activity

39
Q

The most widely used alkylating agent

A

Cyclophosphamide

40
Q

Alkylating agents that cross blood brain barrier used in treatment of tumors are called

A

Nitrosurea

41
Q

Nitrosourea includes

A

Carmustine
Lomustine
Streptozocine
Semustine

42
Q

The nitrosurea used in the treatment of brain tumors

A

Carmustine and lomustine

43
Q

Carmustine and lomustine is used majorly to treat

A

Brain tumors

44
Q

Streptozocine a type of Nitrosourea is specifically used to treat

A

Insulinoma

Pharmac (27 decks)

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