Antineoplastics - Alkylating Agents Flashcards

1
Q

Prodrug activated by CYP450-2B6

AE: hemorrhagic cystitis due to toxic metabolite Acrolein

A

Alkylating Agent

Cyclophosphamide, nitrogen mustard

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2
Q

Vesicant; no longer used

A

Alkylating Agent

Mechlorethamine

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3
Q

Used for Brain tumors and Lymphomas

A

Carbustine (IV) and Lomustine (oral); highly lipophilic –> cross BBB

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4
Q

AE: pulmonary fibrosis and Renal failure

Used for CML

A

Busulfan

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5
Q

Prodrug metabolized by CYP450-3A4 to Chloroacetaldehyde

A

Ifosfamide

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6
Q

AE of Ifosfamide

A

Neurotoxicity, nephrotoxicity, hemorrhagic cystitis

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7
Q

AE: oral ulceration, pulmonary fibrosis, hepatotoxicity

A

Melphalan

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8
Q

Given with Amifostine to reduce nephrotoxicity

A

Cisplatin

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9
Q

AE of Platinum compounds

A

Peripheral neuropathy, electrolyte disturbances, anaphylactic rxns

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10
Q

Alkylating Agent MOA

A

Alkylation at N7 position of Guanine; on single or both via cross-linking (intrastrand or b/t both)

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11
Q

Curative therapy for Testicular Cancer

A

Vinblastine + Cisplatin + Bleomycin

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12
Q

A Methylhydrazine

A

Procarbazine

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13
Q

AE of Procarbazine

A

Disulfiram-like rxn, metabolite is MAOI

Leukemogenic, mutagenic, teratogenic

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14
Q

Are Alkylating Agents cell-cycle specific or cell cycle non-specific?

A

Cell cycle non-specific

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15
Q

Alkylating agents that cause pulmonary fibrosis

A

Busulfan
Melphalan
Carmustine
Lomustine

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16
Q

Causes Oral ulceration

A

Melphalan

17
Q

Cause hemorrhagic cystitis

A

Ifosfamide

Cyclophosphamide

18
Q

Cross BBB

A

Carmustine

Lomustine

19
Q

Vesicant

A

Mechlorethamine

Decarbazine

20
Q

Given with Mesna to prevent?

A

Mesna prevents Hemorrhagic cystitis by Cyclophosphamide

21
Q

Metabolite of Ifosfamide

A

Chloroacetaldehyde

22
Q

Metabolite of Cyclophosphamide

A

Acrolein: irritates bladder mucosa

23
Q

Nitrogen Mustards

A

Cyclophosphamide, Ifosfamide, Mechlorethamine, Melphalan

24
Q

Used for Multiple Myeloma

A

Melphalan

25
Q

Nitrosureas

A

Carmustine, Lomustine

26
Q

Alkyl Sulfonates

A

Busulfan

27
Q

Methylhydrazines

A

Procarbazine

28
Q

Triazine

A

Dacarbazine

29
Q

Platinum Analogs

A

Cisplatin, Carboplatin

30
Q

Indications for Platinum Analogs

A

Testicular, Ovarian, and Bladder Cancer