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Pharmacology II > Anti-Neoplastics #3 > Flashcards

Anti-Neoplastics #3 Flashcards

1
Q

Most chemotherapeutic drugs exert their effect against ______ dividing ______ cell. However, some normal cells in the body also divide rapidly including?

A

rapidly, cancer, cells lining the GI tract, hair cells, blood cells

Pay attention to what is happening in GI system re: therapeutic drugs

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2
Q

What are Cell Cycle Specific (CCS) chemotherapeutic drugs?

A

❖ Cell Cycle NonSpecific (CCNS)
- Act on the specific phases of the cell cycle.
▪ Antimetabolites act on (S phase)

▪ Vinca alkaloids
▪ Taxanes
- Plant Alkaloids or Microtubule Targeting Agents (M phase)

▪ Topoisomerase I and II inhibitors (G1-S, G2-M phases)
▪ Anti-tumor Antibiotics (G2-M phase)

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3
Q

What are Cell Cycle NonSpecific (CCNS) chemotherapeutic drugs?

A

▪ Alkylating agents: Typical and Atypical
▪ Platinum analogs
▪ Antibiotics (aka Anthracyclines)

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4
Q

What are Miscellaneous Anticancer Agents chemotherapeutic drugs?

A
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5
Q

Name the Cell Cycle Specific (CCS) chemotherapeutic drugs. What phase of the cell cycle do they act on?

A

microtubule inhibitors = taxanes and vinca alkaloids.

Etoposide can also act at G!-S phase

Etopo = topo II, irino = inhibit action of topo I

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6
Q
  1. What is the function of Antimetabolites? Explain.
  2. What is their MOA?
  3. What phase of the cell cycle do they act on?
A
  1. Antimetabolites are structural analogs of DNA and RNA Components. They are inserted in place of nucleotides during replication. This inhibits the process and ultimately leads to cell death. [Some of them are also able to get inserted in NA and that insertion makes abnormal structural abnormalities causing DNA breakage leading to cell death. ]
  2. Mechanism of action: interfere with DN or RNA biosynthesis and prevent normal nucleotide production.
  3. Antimetabolite are primarily S phase specific.
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7
Q

Name the different classes of antimetabolites.

A
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8
Q

Methotrexate
Therapeutic uses?
Adverse effects ?
Animals used in ?

A
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9
Q

5-Fluorouracil
Therapeutic uses?
Adverse effects ?
Animals used in ?

A
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10
Q

Cytarabine, Gemcitabine
Therapeutic uses?
Adverse effects ?
Animals used in ?

A

crosses BBB so used for neuro cancer

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11
Q

6-Mercaptopurine, 6-Thioguanine
Therapeutic uses?
Adverse effects ?
Animals used in ?

A
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12
Q

What is the MOA of CCS drugs?

A

Cell cycle specific drugs act on the mitotic spindle during the process of mitosis. During mitosis, the chromosomes move to opposite “poles” of the cell via microtubules. These tubules are made up of alpha and beta subunits and need to be assembled and disassembled before and after the mitotic process and play role in cell shape, structure, division, mitosis, etc.

Microtubule targeting agents either inhibit assembly or prevent disassembly. Vinca alkaloids prevent microtubule assembly, specifically _____ tubulin. Taxanes prevent deassembly, specifically _____ tubulin.

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13
Q

Vincristine
Therapeutic uses?
Adverse effects ?
Animals used in ?

A

Most commonly used in vet med

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14
Q

Vinblastine
Therapeutic uses?
Adverse effects ?
Animals used in ?
Can this be absorbed orally?

A

No, it can’t be absorbed orally. It is administered IV.
Only CNS?

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15
Q

Vinorelbine
Therapeutic uses?
Adverse effects ?
Animals used in ?

A
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16
Q

Paclitaxel
Therapeutic uses?
Adverse effects ?
Animals used in ?

A
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17
Q

MOA of CCS: Anti-tumor Antibiotics

A

MOA: Bind to DNA and cause DNA fragmentation via generation of free radicals
Mitotic inhibitor and topoisomerase II inhibitor
➢ Bleomycin (G2 specific, DNA damage). Used for electrochemotherapy, especially in cats; this local treatment is a way to get chemodrugs into cancer cells; after injecting drug, deliver chains of electric impulses create holes in cell membrane.
- Poorly characterized in dogs. Effective against benign gingival tumor –> invades bone so that is why not used in dogs
➢ Etoposide (G2-M specific, Topoisomerase II inhibitor) ( limited information in animals and is used less).

antibiotic, poisonous to cells?

Free radicals damage DNA which is why it is used. Used for lymphoma, cervicla cnera, head and neck, testicular cancer,

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18
Q

Cell Cycle Non-Specific (CCNS) Chemo Drugs - Alkylating agents

A

➢ Cyclophosphamide (CytoxanR) = most used in vet med
➢ Chlorambucil
➢ Melphalan
➢ Mechlorethamine
➢ Ifosfamide
➢ Procarbazine
➢ Lomustine
➢ Carmustine
➢ Streptozocin
➢ Dacarbazine
➢ Hydroxyurea

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19
Q

Cell Cycle Non-Specific (CCNS) Chemo Drugs - Platinum analogs

A

➢ Cisplatin
➢ Carboplatin

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20
Q

Cell Cycle Non-Specific (CCNS) Chemo Drugs - Antibiotics (Anthracyclines)

A

➢ Doxorubicin (AdriamycinR)
➢ Epirubicin
➢ Actinomycin D
➢ Mitoxantrone

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21
Q

What is Extracted from streptomyocin bacteria ?

A

Doxorubicin is an anthracycline antibiotic derived from the actinobacteria Streptomyces peucetius var.

22
Q

CCNS: Alkylating Agents
MOA?

A

Addition alkylating agents damage DNA which is why cancer cell dies

23
Q

Guanine: Alkylating Site of DNA

A

Alkylating agents that do this are typical alkylating agents.
Nitro = a-typical alkylating agent.
Alkylating of guanine = breakage of DNA strands, other damage, (she said a few others - relisten).

24
Q
  1. Alkylation of guanine occurs at which location?
    1A. What does this result in?
    1B. What is the MOA?
A
  1. N-7
    1A. Abnormal nucleotide sequences,
    miscoding of mRNA, cross-linked DNA strands that cannot replicate, breakage of DNA strands, and other damage to the transcription, and translation of genetic material.
    1B. Cross-linking DNA and preventing its replication, Breakdown of DNA, Alkylation of proteins and RNA
25
Q

CCNS: Alkylating Agents
Name the Typical ones.

A

❑ Nitrogen mustards (N-7)
➢ Cyclophosphamide (CytoxanR)
➢ Chlorambucil
➢ Melphalan
➢ Mechlorethamine
➢ Ifosfamide

26
Q

Name the atypical CCNS Alkylating Agents

A

❑ Nitrosoureas (O-6)
➢ Lomustine
➢ Carmustine
➢ Streptozocin (acts via GLUT2)

27
Q

Name the other CCNS Alkylating Agents.

A

MOA is unknown. It is know that they alkylating DNA both N7 and Oxygen 6.

28
Q

Cyclophosphamide
MOA?

A

Cyclophosphamide
- Typical
✓ The cytotoxic effects are directly related to the alkylation of DNA,
which causes cross linking of base pairs.
✓ The 7th nitrogen atom of guanine is suitable for formation of
covalent bond with alkylating agen

29
Q

Lomustine
MOA?

A

Atypical
✓ The chemotherapeutic and cytotoxic effects are directly related
to the alkylation of DNA. The 6-oxygen atom of guanine is suitable
for formation of covalent bond with bifunctional alkylating agent
✓ Highly lipid-soluble, can cross BBB

30
Q

Cyclophosphamide
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
31
Q

Chlorambucil
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A

b/c less myelo can be used mroe often.

Less effective by less toxic which is important in some cases. Monitor blood cells more closely in cases of myelosuppression.

32
Q

Melphalan
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
33
Q

Mechlorethamine
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
34
Q

Ifosfamide
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
35
Q

Lomustine
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
36
Q

Carmustine
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
37
Q

Streptozocin
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
38
Q

Dacarbazine
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
39
Q

Procarbazine
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
40
Q

Hydroxyurea
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
41
Q

Platinum Analogs
MOA?

A

Cause cross-links in DNA and prevent DNA replication (similar to alkylating agents)
➢ Cisplatin: an inorganic metal complex that inhibits cell division
➢ Carboplatin (2nd generation, significantly less renal and GI
toxicity, better in combination therapies)
* Oxaliplatin (3rd generation, no cross-resistance, neurotoxicity
is reversible)

Generation = more efficacy, less toxicity.?

42
Q

Cisplatin
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
43
Q

Carboplatin
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
44
Q

Cytotoxic Antibiotics
MOA?

A

MOA: Inhibition of topoisomerase II and free radical-mediated DNA damage. They inhibit both DNA and RNA synthesis
* Cell cycle non-specific but most active during the S phase
* Derived from the fungus Streptomyces
➢ Doxorubicin (AdriamycinR)
➢ Epirubicin (Dox analog)
➢ Actinomycin D (blocks RNA polymerase)
➢ Mitoxantrone = both antibiotic and topo inhibitor; used in many cancers, particularly for prostate cancer. used in combo with other drugs b/c it has different characteristics

45
Q

Doxorubicin
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A

can cause chronic crdiomyopathy in dogs and neuropathy and immunodeficiency? in cats.

46
Q

Epirubicin
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
47
Q

Actinomycin D
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
48
Q

Mitoxantrone
(Topo II inhibitor)
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
49
Q

Glucocorticoids
(CCNS, G1, inh. mitosis in lymphocytes)
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A
50
Q

L-Asparaginase
(G1 phase, Asparagine inhibitor)
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A

depleted circulating level of asparagine –> ?

When don’t get it = die.

Works as aparagine inhibitor and is used in some dogs and cats. when given alone = no myelosuppression. Acting on protein needed for synthesis. ?

51
Q

Piroxicam
(NSAID, COX-2 inhibitor, tumor angiogenesis)
Therapeutic uses?
PK?
Adverse Effects?
Animals used in?

A

Angiogenesis is important for tumor to grow.

52
Q
A

Summary of what we discussed.
antibiotics - are also often topoisomerase inhibitors

Pharmacology II (27 decks)

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