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Heme & Lymph > Pharm- Alkylating Agents & CCNS Drugs > Flashcards

Pharm- Alkylating Agents & CCNS Drugs Flashcards

1
Q

Bifunctional agents

A

cross-link DNA

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2
Q

Monofunctional agents

A

insert a methyl or ethyl molecule into DNA

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3
Q

Monofunctional agents

A

triazenes, nitrosoureas

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4
Q

bifunctional agents

A

nitrogen mustards, aziridines, melphalan, chlorambucil, busulfan

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5
Q

Triazenes

A

dacarbazine, procarbazine, temozolomide

  • DNA alkylation. Methylation, guanosine O6,N7
  • donate a methyl group and alkylate the guanosine O6,N7 that is in DNA
  • Can tx advanced forms of brain tumors
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6
Q

Dacarbazine therapeutic uses

A

metastatic melanoma

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7
Q

Procarbazine therapeutic uses

A

malignant glioma

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8
Q

Temozolomide

A

tx resistant glioma & astrocytoma

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9
Q

Nitrosoureas

A

DNA alkylation. Alkylation, guanosine O6,N7

  • brain tumors or large melanomas
  • used for brain cancers bc these tend to be tumors that have cells escaping the cell cycle bc they are physically limited in their growth
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10
Q

Nitrosoureas

A

Carmustine, Lomustine, Streptozocin

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11
Q

Carmustine therapeutic uses

A

brain tumors, lymphoma, melanoma

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12
Q

Lomustine therapeutic uses

A

brain tumors, lymphoma, melanoma

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13
Q

Streptozocin

A

used as a chemical to model diabetes
-selective at islet B cells
Insulinomas -> create Type 1 diabetes

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14
Q

Nitrogen Mustards

A

Cyclophosphamide, Ifosfamide, mechlorethamine

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15
Q

Cyclohosphamide, Ifosfamide

A
  • crosslinks
  • PO, liver CYP450 activation
  • various uses
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16
Q

Mechlorethamine (vesicant)

A

spontaneous activation

Historical- MOPP regiment in lymphoma

17
Q

Melphalan

A

PO

-multiple myeloma

18
Q

Chlorambucil

A
  • PO

- CLL

19
Q

Busulfan

A
  • PO

- CML

20
Q

Aziridines

A

G-G crosslinks

Thiotepa, Mitomycin C, Altretamine

21
Q

Thiotepa therapeutic uses

A

breast, ovarian, bladder cancer

22
Q

Mitomycin C therapeutic uses

A

breast & gastrointestinal cancer

23
Q

Altretamine therapeutic uses

A

Recurrent ovarian cancer - resistant to other alkylating agents

24
Q

Cisplatin & related compounds

A

organoplatinum drugs

25
Q

Organoplatinum drugs

A

cisplatin, carboplatin, oxaloplatin

26
Q

Cisplatin distinctions

A
  • platinum-Cl complex
  • stable in plasma and high Cl milieu
  • hydrolyses in cell to active agent
  • Complex elimination due to cell uptake
27
Q

Carboplatin distinctions

A

more stable analog

-primarily renal elimation, t1/2 ~ 2hrs

28
Q

Oxaloplatin distinctions

A

complex elimination due to cell uptake

29
Q

cisplatin therapeutic uses

A

testicular cancer (w/ bleomycin, vinblastin or etoposide); ovarian cancer; NSCL

30
Q

carboplatin therapeutic uses

A

ovarian cancer

31
Q

oxaloplatin therapeutic uses

A

Colorectal cancer (FOLFOX regimen). Folinic acid, FU, Oxaliplatin

32
Q

cisplatin dose limiting toxicity

A

renal; severe nausea/vomiting; ototoxicity- acoustic nerve damage

33
Q

carboplatin dose limiting toxicity

A

neutropenia

34
Q

oxaloplatin dose limiting toxicity

A

neutropenia, neuropathy- cold induced

Heme & Lymph (8 decks)

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