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PCM Exam 1 > Anticancer Drugs 2 > Flashcards

Anticancer Drugs 2 Flashcards

1
Q

Mechanism of action of 6 Mercaptopurine

A

It is an analog of hypoxanthine and guanine
Converted to thio-IMP by HGPRT and thio-IMP inhibits first step of de novo purine ring biosynthesis and blocks formation of AMP and GMP from IMP

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2
Q

Function of thio-IMP

A
  • inhibits first step of de novo purine ring biosynthesis

- blocks formation of AMP and GMP from IMP

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3
Q

6 mercaptopurine is metabolized to _____________ by __________

A

Thiouric acid; xanthine oxidase

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4
Q

What does administering allopurinol do to the levels of 6 mercaptopurine

A

↑ so must ↓ the dose of 6 mercaptopurine given

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5
Q

Adverse effects of 6 mercaptopurine

A

Nausea, vomiting, diarrhea, bone marrow suppression, hepatotoxicity

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6
Q

6 thioguanine is converted to thioguanine monophosphate (TGMP) which then inhibits _______ and _______

A

Purine synthesis; phosphorylation of GMP to GDP

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7
Q

What is 6 thioguanine used for?

A

Acute non lymphocytic leukemia

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8
Q

What is the effect of allopurinol when given with 6 thioguanine

A

Allopurinol DOES NOT potential it’s action because very little is metabolized to thiouric acid

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9
Q

Mechanism of action of 5- fluorouracil

A
  1. Converted to 5- FdUMP which inhibits thymidilate synthase and so DNA synthesis is inhibited
  2. Converted to 5-FUTP and incorporated to RNA interfering with RNA processing and function
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10
Q

Name the pyrimidine analogs

A

5- Fluorouracil
Capecitabine
Cytarabine

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11
Q

5-FU is mainly metabolized by ____ and what are some adverse effects in patients with that enzyme deficiency

A 
Dihydropyrimidine dehydrogenase (DPD) 
Myelosuppresion, neurotoxicity and life threatening diarrhea
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12
Q

5-FU + leucovorin is used as a chemotherapy for ________

A

Colorectal cancer

Leucovorin potentiates the activity of 5-FU because it ↑ the levels of N5,N10 methylene THF

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13
Q

How does 5-FU inhibit thymidylate synthase?

A

Forms a ternary complex involving thymidylate synthase, 5 FdUMP and N5,N10 methylene THF

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14
Q

Adverse effects of 5-FU

A

Nausea, voting, alopecia and bone marrow suppression; very toxic to the GI tract so people with a DPD deficiency are at risk for life threatening diarrhea

Can also see hand-foot Syndrome in which there is an erythematous desquamation of the palms and soles

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15
Q

What is capecitabine

A

Orally availabe prodrug of 5-FU and has the same cytotoxic activity as 5-FU

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16
Q

Mechanism of action of cytarabine

A

It is an analog of deoxycytidine and is phopshoryatled into a triphoshate and when it gets incorporated into DNA, it inhibits DNA polymerase

given via IV

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17
Q

cytarabine inhibits _______

A

DNA polymerase

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18
Q

Mechanism of action of antitumor antibiotics

A

Binds to DNA between bases and blocks synthesis of new RNA/DNA and causes DNA strand breakage and interferes with replication

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19
Q

Name antitumor antibiotics

A

Anthracyclines : doxorubicin and daunorubicin

Bleomycin

20
Q

____________ an anthracyline, is one of hte most widely used anti cancer drug

A

Doxorubicin

21
Q

Anthracyclines inhibit the enzyme __________

A

Topoisomeriase II (DNA gyrase)

22
Q

Name the 4 mechanisms of anthracyclines

A
  • Inhibition of toposiomersae II
  • intercalation in DNA with blcokade of DNA and RNA synthesis and strand breakage
  • binding to cell membranes to alter fluidity and ion transport
  • generation of free radicals
23
Q

What is the cause of cardiac toxicity when taking anthracyclines and what do you give to reduce the cardiotoxicity

A

Generation of free radicals; dexrazoxane

24
Q

Bleomycin is cell cycle specific and arrests cells in ___________

A

G2

25
Q

Mechanism of bleomycin

A

Has 2 binding sites: one for DNA and another for ferrous iron
DNA-bleomycin Fe2+ is oxidized to Fe3+ and the liberated electrons form free radicals which causes strand breaks in DNA

26
Q

Adverse effects of bleomycin

A

Most important and serious: pulmonary toxicity (pneumonitis, fibrosis)
Little myelosuppression

27
Q

____________ is the most widely used alkylating agent

A

Cycophosphamide

28
Q

Which group of anti cancer drugs are mutagenic and carcinogenic

A

Alkylating agents

29
Q

List alkylating agents

A

Nitrogen mustards: melphalan, cyclophosphamide, mechlorethamine

Nitrosureas

Other

Platinum coordination complexes

30
Q

____________ is an unstable alkylating agent that is a powerful vessicant and must be given via _______

A

Mechlorethamine; IV

31
Q

Cyclophosphamide is a product that is activated by

A

CYP2B

32
Q

What is the metabolite that is responsible for the hemorrhagic cystitis that can result from using cyclophosphamide

A

Acrolein

33
Q

Adverse effects of melphalan and what kind of drug is it

A

Bone marrow suppression;

Alkylating agent

34
Q

What makes nitrosureas unique for certain cancer treatments

A

Useful in treating brain tumors

It is very lipophilic so it can cross the blood brain barrier

35
Q

Adverse effects of busulfan

A 
Myelosuppresion (main) 
Pulmonary fibrosis (also caused by bleomycin)
36
Q

Mechanism of dicarbazine

A

Methylation agent after it is activated in the liver

37
Q

Procarbazine’s adverse effects

A

Bone marrow depression, weak MAOI which can cause hypertensive reactions if gtibvne sympathomimetic agents or tyramine containing foods, disulfiram like reactions, mutagenic and teratogenic (alkylating agent)

38
Q

Examples of platinum coordination complexes

A

Cisplatin and carboplatin

39
Q

Mechanism of platinum coordination complexes

A

Does not alkylate DNA but binds to DNA and inhibits DNA synthesis by forming cross links

40
Q

Adverse effects of cisplatin

A

Myelosuppresion, ototoxicity, peripheral neuropathy, and nephrotoxicity

41
Q

_________ is given to reduced the renal toxicity associated with cisplatin

A

Amifostine

42
Q

What is the dose limiting toxicity for carboplatin?

A

Myelosuppresion

43
Q

What are some additional adverse effects you see in a patient taking I-Phosphamide that you dont see in someone taking cyclophosphamide

A
  • neurotoxicity

- nephrotoxicity

44
Q

describe the effects of 6-MP on someone with Lesch Nyan Syndrome

A

6 MP would not be as effective and there would be more resistance to it because these patients have low levels of HGPRT

45
Q

6-MP and 6-TG are also metabolized by _______ and patients with a deficiency in this enzyme are at risk for ________

A

TPMT (thiopurine methyltransferase);

myelosuppression

PCM Exam 1 (22 decks)

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