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Pharmacology Final > Antineoplastic Agents (Conventional cytotoxins) > Flashcards

Antineoplastic Agents (Conventional cytotoxins) Flashcards

1
Q

Alkylating Agents (Nitrogen mustard agents) MoA

A

Bind to nucleotides and alkylate them (add a methyl group), this forms: (Inter-strand & Intra-strand) crosslinking, interfering with DNA & RNA synthesis

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2
Q

Alkylating Agents (Nitrogen mustard agents) cell cycle target

A

Non-specific

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3
Q

Alkylating Agents (Nitrogen mustard agents) indications

A

Non-Hodgkin lymphoma
Leukemia
Sarcoma

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4
Q

Alkylating Agents (Nitrogen mustard agents) examples

A

Cyclophosphamide
Ifosfamide

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5
Q

Platinum Coordination Complexes MoA

A

Add platin group to guanine, this forms: (Inter-strand & Intra-strand) crosslinking

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6
Q

Platinum Coordination Complexes cell cycle target

A

Non-specific, but favors (G1) and (S) phases

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7
Q

Platinum Coordination Complexes examples

A

Cisplatin “Parent drug”
Carboplatin
Oxaliplatin

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8
Q

Anti-metabolites MoA

A

Inhibit the synthesis of nucleotides by competing with their precursors

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9
Q

Anti-metabolites cell cycle target

A

(S) phase

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10
Q

Anti-metabolites examples

A

5-Fluorouracil (5-FU)
Capecitabine

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11
Q

5-Fluorouracil (5-FU) cell cycle target

A

(S) phase

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12
Q

5-Fluorouracil (5-FU) synergism

A

5-FU is combined with Leucovorin → this enhances its binding to thymidine synthase

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13
Q

5-Fluorouracil (5-FU) indications

A

Colorectal cancer
Breast cancer
Ovarian cancer
Pancreas cancer
Gastric carcinoma

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14
Q

5-Fluorouracil (5-FU) mechanisms of resistance

A

(1) Cancer cells are unable to convert 5-FU into its active form (5-FdUMP)
(2) increased the levels of thymidylate synthase

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15
Q

Capecitabine RoA

A

Given orally as a prodrug that gets activated in the liver

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16
Q

Capecitabine cell cycle target

A

(S) phase

17
Q

Capecitabine MoA

A

Converted inside the cell to 5-FU; (then same MoA as 5-FU)

18
Q

Capecitabine indications

A

Colorectal cancer
Breast cancer

19
Q

Anthracyclines cell cycle target

A

non-specific

20
Q

Anthracyclines MoA

A

1) inhibits DNA helicase → it is the enzyme that separates the two DNA strands of DNA
2) inhibits Topoisomerases (II) → it the enzyme that re-joins the two DNA strands
3) produces free ROS, which causes cell injury

21
Q

Anthracyclines examples and indications

A

A. Doxorubicin: Sarcoma, Lung cancer, Breast cancer, Acute lymphocytic leukemia
B. Epirubicin: Gastric carcinoma, Esophageal carcinoma

22
Q

Topoisomerase inhibitors examples

A

Camptothecins (Irinotecan/Topotecan)
Etoposide

23
Q

Camptothecins cell cycle target and MoA

A
  • Cell cycle target: (S) phase
  • MoA: Camptothecins inhibit Topoisomerase I in DNA replication, leading to Single-strand breaks
24
Q

Camptothecins synergy

A

these drugs are used with 5-FU and leucovorin for Colorectal cancer

25
Q

Camptothecins examples

A

→ Irinotecan, a prodrug that gets converted by CYT P450 3A4 to (SN-38), a metabolite x1000 potent than Irinotecan
→ Topotecan

26
Q

Etoposide MoA and cell cycle target

A

→ MoA: Etoposide inhibits Topoisomerase II in DNA replication, leading to Double-strand breaks
→ Cell cycle target: (S) phase & (G2) phase

27
Q

Microtubule Inhibitors examples

A

→ Taxanes (Paclitaxel and Docetaxel)
→ Vinca alkaloids (Vincristine and Vinblastine)

28
Q

Taxanes (Paclitaxel and Docetaxel) cell cycle target and MoA

A

→ Cell cycle target: (M) phase
→ MoA: they bind to the mitotic spindles of the cell,
inhibiting their depolymerization so the cells will be stuck in the metaphase of the cell cycle

29
Q

Vinca alkaloids (Vincristine and Vinblastine) cell cycle target and MoA

A

→ Cell cycle target: (M) phase
→ MoA: they inhibit the polymerization of microtubules of the mitotic spindles

30
Q

Associated drug of Myelosuppression

A

5-Fluorouracil & Capecitabine “Anti-metabolites”

31
Q

Associated drug of Renal toxicity

A

Cisplatin

32
Q

Associated drug of Cardiotoxicity

A

Doxorubicin

33
Q

Associated drug of Neurotoxicity

A

Vincristine & Vinblastine “the V’s”

34
Q

Associated drug of GI toxicity

A

5-Fluorouracil & Capecitabine “Anti-metabolites”

35
Q

Associated drug of Alopecia

A

Doxorubicin & Etoposide

Pharmacology Final (6 decks)

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