Exam one: antineoplastic agents MOA, AE, TU etc Flashcards

1
Q
  • Therapeutic Use: Hodgkin’s Disease
  • MOA: Alkylating agent (Nitrogen Mustard)
  • AE: bone marrow and GI mucosa
  • Notes: most reactive alkylating agent.
A

Mechlorethamine

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2
Q
  • Therapeutic Use: Broad spectrum
  • MOA: Alkylating agent; prodrug; hydroxylated by CYP2B
  • AE: bone marrow and GI mucosa; renal toxicity
  • Notes: most widely used alkylating agent. Use with mesna.
A

Cyclophosphamide

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3
Q
  • Carmelo penetrates the lane (BBB)
  • Therapeutic Use: Highly lipophilic to treat malignant gliomas
  • MOA: Alkylating agent (Nutrosoureas)
  • AE: Severe cumulative myelosuppression. Long term Tx leads to renal failure.
  • Notes:
A

Nitrosoureas

  • Carmustine
  • Lomustine
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4
Q
  • Therapeutic Use: malignant myeloma, Hodgkin’s disease (ABVD)
  • MOA: Triazene Alkylating agent. Methylating agent. Prodrug CYP demethylation in liver
  • AE: myelosuppression, N/V and flu-like symptoms.
  • Notes:
A

Dacarbazine

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5
Q
  • Therapeutic Use: Hodgkin’s and non-hodgkin’s, brain tumors.
  • MOA: Methylhydrazine; Prodrug; monofunctional – produces chromosomal damage.
  • AE: bone marrow suppression; neurotoxicity
  • Notes: Only the PROs can handle the brain tumors.
A

Procarbazine

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6
Q
  • Therapeutic Use: testicular, ovarian, head/neck, bladder, esophageal, lung, colon cancers.
  • MOA: Platinum Complex alkylating agent. React with nucleophilic sites on DNA and proteins to produce apoptosis. Monofunctional (produces chromosome damage)
  • AE: nephrotoxicity and neurotoxicity. Myelosuppression
  • Notes: Carboplatin is much less toxic.
A

Platinum Complexes

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7
Q
  • Therapeutic Use: colorectal cancer combined with FOLFOX
  • MOA: React with nucleiohilic sites on DNA and proteins to produce apoptosis.
  • AE: peripheral neuropathy
  • Notes: No cross resistance with other platinum agents.
A

Oxaliplatin

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8
Q

• Drugs: 6-thiopurine; 6-mercaptopurine; 6-thioguanine
• Therapeutic Use: inhibits purine synthesis.
o 6-MP: ALL; works with allopurinol (xanthine oxidase inhibitor)
o 6-TG: acute granulocytic leukemia
• MOA: Antimetabolites; inhibit purine synthesis
• AE: can become lethal if drug accumulates.
• Notes:

A

6-Mercaptopurine (6-MP)

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9
Q
  • Therapeutic Use: non-hodgkin lymphoma, CLL, hairy cell leukemia (Cladribine).
  • MOA: Antimetabolite; Adenosine analogs causing DNA problems => apoptosis.
  • AE: Myelosuppression
  • Notes:
A

6-Thioguanine (6-TG)

Fludarabine-5’- phosphate

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10
Q

• Therapeutic Use: hard tumors; RA, ALL, Burkitt’s lymphoma, non-Hodgkin’s, carcinomas, oseteogenic sarcomas, choriocarcinomas, breast cancer.
• MOA: Folic acid inhibitor; inhibits dihydrofolate reductase
• AE: toxicity prevented or reversed by leucovorin; bypasses blocked DHFR. Renal damage.
• Notes: Structurally very similar to tetrahydrofolate.
crystal METH is LEUCrative!!!

A

Methotrexate

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11
Q

• Therapeutic Use: colorectal cancer; Breast cancer (CMF; no estrogen receptor).
• MOA: Antimetabolite; Uracil analog (prodrug) causing a decrease in DNA synthesis => impaired RNA translation.
• AE: Myelosuppresion and GI
• Notes: Commonly given drug.
o 5-fluorouracil makes ur Colon FLUOw.

A

5-Fluorouracil (5-FU)

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12
Q
  • Therapeutic Use: AML
  • MOA: antimetabolite; cytosine deoxyriboside analog, prodrug (met to AraCTP)
  • AE: myelosuppresion
  • Notes:
A

Cytarabine (AraC)(Cytosine arabinoside)

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13
Q
  • Therapeutic Use: metastatic pancreatic cancer; non small cell lung and bladder cancer.
  • MOA: Antimetabolite; Cytosine deoxyriboside analog; prodrug
  • AE: myelosuppresion is dose limiting.
  • Notes:
A

Gemcitabine

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14
Q

o Treatment of choice with glucocorticoids for ALL (MOPP); Given with Actinomycin D.

o Curative therapy for metastatic testicular tumors, in combination w/ bleomycin and cisplatin.
o Note: Ball Blaster!

  • MOA: Plant Alkaloids; anti-mitotic; M-phase specific; binds tubulin blocking polymerization activity
  • AE: peripheral neuropathy and myelosuppresion.
A

Vinca Alkaloids (Vin-)

Vinblastine
Vincristine

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15
Q
  • Therapeutic Use: metastatic cancers, abraxane is albumin-bounds taxol
  • MOA: Plant alkaloid; Anti-mitotic M-phase specific; promotes MT polymerization and stabilization blocking mitosis.
  • AE: Hypersensitivity & neutropenia.
  • Notes: Mitosis is a TAXANE process!
A

Taxanes

  • Paclitaxel
  • Abraxane
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16
Q
  • Therapeutic Use: FYI
  • MOA: Plant alkaloids; S-phase specific; binds and stabilizes TOPO-1 DNA complex (allows breakage but not resealing)
  • AE: Myelosuppression.
  • Notes: Toco interacts with Topo!
A

Camptothecins

=Topotecan

17
Q
  • Therapeutic Use: FYI
  • MOA: Plant alkaloids; Complexes with TOPO-II
  • AE: Myelosuppression
  • Notes: eTOPOside interacts with TOPO-II
A

Epipodophyllotoxins

Etoposide

18
Q
  • Therapeutic Use: anti-tumor antibiotic
  • MOA: binds to DNA by intercalating (sandwiching) between GC base pairs.
  • AE: Myelosuppression
  • Notes: one of most potent anti-tumor agents known. Curative in regimen with Vincristine and Cyclophosphamide.
A

Actinomycin D (Dactinomycin)

19
Q

• Therapeutic Use: FYI. Antitumor antibiotic
• MOA: Intercalate with DNA and binds to the backbone of DNA
• AE: FYI
• Notes: can be cardiotoxic, epirubin is less cardiotoxic.
o Adrian Peterson is the backbone of offense/DNA cause he can intercalate through the gaps… Ya buddy!

A

Anthracyclines
Adriamycin (Doxorubicin)
-Bleomycin

20
Q
  • Therapeutic Use: APL with high rate of complete remission
  • MOA: Retinoids; stimulate transcription of genes that have retinoic acid receptors induces differentiation.
  • AE: Vitamin A toxicity
  • Notes: tRETINoin is a RETINoid which affects RETINol (vitamin A)
A

Tretinoin (ATRA)

21
Q
  • Therapeutic Use: CML
  • MOA: inhibits BRC/ABL Tyr kinase and c-kit receptor protein kinase.
  • AE: Non-severe
  • Notes: concerned with drug interactions that use P450 isoforms.
A

Imatinib mesylate (Gleevac)

22
Q
  • Therapeutic Use: cancer (esp. lung)
  • MOA: inhibits EGFR tyrosine kinase, blocks signal transduction pathways required for cell proliferation and survival
  • AE: possible diarrhea and acne-like rash
  • Notes: induces of P450 decrease plasma gefitinib.
A

Gefitinib

23
Q
  • Therapeutic Use: Refractory multiple myeloma
  • MOA: acts as a reversible inhibitor of 26S proteasome  silences NF-KB.!!!
  • AE: FYI
  • Notes: She stressed this in class! –Zomib is a proteasome inhibitor.
A

Bortezomib

24
Q
•	Therapeutic Use: breast cancer
•	MOA: blocks Her2/neu receptor
•	AE: FYI
•	Notes: Not for pt who expresses ER.  Pt tumor must express HER2/neu marker
o	Be sure to treat HER boobs!
A

Trastuzumab (Herceptin)

25
Q
  • Therapeutic Use: B cell non-hodgkin lymphoma
  • MOA: binds CD20 of normal and malignant B cells causing lysis
  • AE: N/F/C on 1st infusion
  • Notes:
A

Rituximab

26
Q
  • Therapeutic Use: colon cancer
  • MOA: binds EGFR; inhibits cell growth  apoptosis
  • AE: acne-like rash
  • Notes: Cetux sounds like cecum which is near the colon.
A

Cetuximab

27
Q
  • Therapeutic Use: metastatic colorectal cancer
  • MOA: angiogenesis inhibitor binding VEGF
  • AE: HTN
  • Notes: Often used in combination therapy.
A

Bevacizumab

28
Q
  • Therapeutic Use: leukemias and cancers
  • MOA: immunomodulatory, antiproliferative, and antiviral. Cytokines binding JAK-STAT.
  • AE: F/C, myelosuppresion; neurotoxicity.
  • Notes:
A

Interferon-alfa

29
Q
  • Therapeutic Use: melanoma and renal cell cancer
  • MOA: induces a T-cell response that is cytolytic for tumor cells.
  • AE: Flu-like symptoms
  • Notes: two starts with a “T” so it stimulates Tc cells.
A

Interleukin-2 (IL-2)

30
Q
  • Therapeutic Use: prophylaxis of chemotherapy-induced neutropenia
  • MOA: increases production of neutrophils and stimulates phagocytic and cytotoxic activity.
  • AE: bone pain in lower back, sternum, and pelvis.
  • Notes
A

Granulocyte Colony-Stimulating Factor (G-CSF)

31
Q
  • Therapeutic Use: good for bone marrow problems
  • MOA: increases neutrophils and monocytes
  • AE: fever and bone pain
  • Notes:
A

Granulocyte/Macrophage Colony-Stimulating Factor (GM-CSF