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KN-Pharm Block 2- Anticancers > Alkylating Agents and Antimetabolites > Flashcards

Alkylating Agents and Antimetabolites Flashcards

2
Q

What is tumor lysis syndrome? (TLS)

A

tumor cells killed and cellular materials dumped into circulation. Adverse effects in kidney. Can cause gout. Often prophylactically treat with hydration, acid/base correction, and sodium bicarbonates.

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3
Q

What do alkylating agents do?

A

leave a chemical moiety bound to DNA to prevent cell division.

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4
Q

What do bis(chloroetyl)amine alkylating agents usually bind to on DNA?

A

N7 guanine. Messes Up DNA enough to trigger apoptosis and halt cell division.

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5
Q

What are the unique negative effects of bis(chloroethyl)amine alkylating agents?

A

IV administration causes vascular damage and irritation. Pulmonary fibrosis.Ifosfamide causes CNS toxicity.Acrolein production, which can cause renal failure and urotoxicity. Treat with MESNA

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6
Q

What is MESNA

A

prophylactic to treat the acrolein production from cyclophosphamide and alkylating agents.

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7
Q

What is busulfan?

A

and alkyl sulfonate.

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8
Q

What unique toxicities does busulfan have?

A

veno-occlusive disease of liver as well as pulmonary fibrosis.

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9
Q

What are nitrosoureas? What is unique about them?

A

BCNU and CCNU - both alkylators. They can penetrate the CNS and brain (unique).

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10
Q

What anticancer drug becomes active in hypoxic locations (such as necrotic tumor centers)?

A

Mitomycin C.

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11
Q

What is a unique toxicity of cisplatin?

A

ototoxicity from accumulation in ear. Also persistant peripheral neuropathy that can worsen even after cessation of treatment.

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12
Q

What is disulfiram-like effect?

A

disulfiram is a drug that makes alcoholic patients feel sick when they drink. Drugs like hprocarbazine can mimick this effect.

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13
Q

How does methotrexate work?

A

dihydrofolate reductase inhibition. Deny availability of DHF to provide carbon groups for DNA and RNA synthesis. It is polyglutamated so it becomes trapped inside cell and increases duration of function.

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14
Q

What is a unique side effect of 5-fluorouacil?

A

foot and hand neuropathy.

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15
Q

What drug can erase fingerprints over time?

A

capecitabine (very similar to 5-fluorouacil.)

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16
Q

What is the mechanism of cyclophoshamide and is there anything unique about it?

A

nitrogen mustard, alkylate DNA, intra or inter crosslinks.Creates acrolein so protect by using MESNA with it.Lung fibrosis

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17
Q

What is the mechanism of ifosfmaide and is there anything unique about it?

A

nitrogen mustard, alkylate DNA, intra or inter crosslinks.Creates acrolein so prevent toxicity with MESNA

18
Q

What is the mechanism of mechlorethamine and is there anything unique about it?

A

nitrogen mustard, alkylate DNA, intra or inter crosslink

19
Q

What is the mechanism of melphalan and is there anything unique about it?

A

alkylate DNA, produce intra or inter crosslinks.Lung fibrosis

20
Q

What is the mechanism of chlorambucil and is there anything unique about it?

A

nitrogen mustard, alkylate DNA intra or inter crosslinks.Lung fibrosis

21
Q

What is the mechanism of busulfan and is there anything unique about it?

A

alkyl sulfonate, alkylate DNA intra or inter crosslinks.Hepatic veno-occlusive diseaseAddison-like syndrome

22
Q

What is the mechanism of carmustine (BCNU) and is there anything unique about it?

A

nitrosoureas, alkylate DNA, intra or inter crosslinkshepatic veno-occlusiveCNS issues

23
Q

What is the mechanism of lomustine (CCNU) and is there anything unique about it?

A

nitrosoureas, alkylate DNA, intra or inter crosslinks.CNS (seizures, dementia)

24
Q

What is the mechanism of thiotepa and is there anything unique about it?

A

aziridine, alkylate DNA, intra or inter crosslinksCNS

25
Q

What is the mechanism of mitomycin C and is there anything unique about it?

A

antibiotic, alkylate DNA, intra or inter crosslinks.

26
Q

What is the mechanism of cisplatin and is there anything unique about it?

A

platinu, alkylate DNA, inter or intra crosslinks.Renal and oto-toxicity.Severe peripheral neuropathy, reduce with Amifostine

27
Q

What is the mechanism of carboplatin and is there anything unique about it?

A

platinum, alkylate DNArenal toxicity, thrombocytopenia

28
Q

What is the mechanism of oxaliplatin and is there anything unique about it?

A

platinum, alkylate DNA

29
Q

What is the mechanism of dacarbazine and is there anything unique about it?

A

methylating, triazene, methylate on 06 guanine on DNA

30
Q

What is the mechanism of procarbazine and is there anything unique about it?

A

methylating, hydrazine, DNA methylator via CYP activation on 06 guanine.Disulfiram-effect (makes you feel bad with alcohol)

31
Q

What is the mechanism of methotrexate, pemetrexed, trimetrexate and is there anything unique about it?

A

antimetabolite, folic acid analog, DHFR.GI toxicity.Give Leucovorin AFTER for metabolic rescue to save non cancer cells.

32
Q

What is the mechanism of 5-fluorouracil and is there anything unique about it?

A

antimetabolite, pyrimidine analog, inhibits Thymidylate synthase and DNA synthesis by thymine absence. Inhibits mRNA translation.Hand-foot syndrome.Give Leucovorin WITH it to ‘enhance’ uptake and effect.

33
Q

What is the mechanism of capecitabine and is there anything unique about it?

A

antimetabolite, pyrimidine analog. It is converted to 5-FU. inhibits Thymidylate synthase and DNA synthesis by thymine absence. Inhibits mRNA translation.Hand-foot syndrome.

34
Q

What is the mechanism of cytarabine (ARA-C) and is there anything unique about it?

A

antimetabolite, pyrimidine analog, inhibits DNA polymerase and prevents DNA cain elongation.Foot-hand syndrome

35
Q

What is the mechanism of gemcitabine and is there anything unique about it?

A

antimetabolite, pyrimidine analog, inhibits DNA polymerase and prevents DNA cain elongation.Foot-hand syndrome

36
Q

What is the mechanism of 6-MP (mercaptopurine), thiogaunine and is there anything unique about it?

A

antimetabolite, purine analog, RNA and DNA inhibitors by incorporating into them.6-MP dose must be reduced if allopurinol present or if TPMT enzyme absent.

37
Q

What is the mechanism of pentostatin, caldribine, fludarabine and is there anything unique about it?

A

antimetabolites, purine analogs, inhibit DNA synthesis and ribonucleotide reductase.

KN-Pharm Block 2- Anticancers (3 decks)

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