Anticancer agents Flashcards

(36 cards)

1
Q

Cancer statistics

A

Major cause of death in pets (40-45% of all dogs >10 yrs of age)
23% of all dogs die of cancer

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2
Q

Hallmarks of cancer

A

Sustaining proliferative signaling
Evading growth suppression
Resisting cell death
Inducing angiogenesis
Enabling replicative immortality
Activating invasion and metastasis

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3
Q

Treating cancer

A

Surgery
Radiation therapy
Chemmotherapy
Hyperthermia
Photodynamic therapy

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4
Q

Chemotherapy

A

Mono-therapy for systemic cancers
Adjuvant therapies
Neo-adjuvant therapies (prior to surgery to shrink tumor)

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5
Q

Chemotherapy activation of immune system

A

Activates macros, T cells and monos → release pro-inflammatory and activation of apaptotic pathways → cell death

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6
Q

Chemotherapy on microtubules

A

Vincristine inhibition of microtubule aggreggation and Paclitaxel inhibition of microtubule disaggregation → altered function of microtubules → cell arrest

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7
Q

Chemotherapy on the nucleus

A

Oxaliplatin, cisplatin inhibition of DNA replication and mRNA transcription → DNA/RNA polymerase → cell arrest and death

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8
Q

Chemotherapy on the mitochondria

A

Oxaliplatin, cisplatin, Vincristine, pacliaxel alter function of resp. chain→ ↑ ROS
OR
→ altered mitochondrial function → activation of apoptosis

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9
Q

Sustained proliferation

A

Replicative immortality
Cancer cells constantly divide and cycle

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10
Q

What are the subclasses of alkalizing agents?

A

Nitrogen mustards
Nitrosoureas
Alkyl sulphonates
Atypical

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11
Q

Alkalizing agents MOA

A

Add alkyl group to the N7 atom of guanine base of the DNA molecule → cross linking of DNA and strand breaks

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12
Q

Alkaline agents in the cell cycle

A

Binds to DNA in the S-phase

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13
Q

Nitrogen mustards

A

Cyclophosphamide
Ifosfamide
Melphalan
Chlorambucil

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14
Q

Ifofsamide

A

Isomer of Cyclophosphamide
Slow IV infusion
Toxicity: Neutropenia, hemorr. cystitis, CNS

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15
Q

MESNA (Mesnex)

A

Rescue agent for hemorr. cystitis
Well tolerated, could cause N/V

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16
Q

Cyclophosphamide

A

Most used nitrogen mustard in vet med
Prodrug given IV or oral
Lymphomas K9 and cats
Malignant mammary gland tumors

17
Q

Cyclophosphamide toxicity

A

Myelosuppression, alopecia, neutropenia, hemorr cystitis
GI (cats)
Bladder irritation

18
Q

Amelioration of Ifofsamide and Cyclophosphamide toxicity

A

Adequate hydration
Diuresis by IV furosemide
Co-admin of MESNA

19
Q

Melphalan

A

Orally and IV
Multiple myeloma in K9 and cats, plasma cells tumors, extramedullary plasmacytoma, relapsed lymphoma in K9

20
Q

The main side effect of melphalan is ____________

A

Myelosupression

21
Q

Chlorambucil (Leukran)

A

One of the most common
Slow acting and least toxic
PO on empty stomach of IV
Replace Cyclophosphamide to avoid hemorr. cystitis

22
Q

Chlorambucil toxicity

A

Myelosuppression with neutropenia and thrombocytopenia
Reversible BM suppression

23
Q

Chlorambucil uses

A

Slower growing tumors like Chronic lymphocytic leukemia, Small cell lymphoma, GI lymphoma in cats

24
Q

Anticancer ABX

A

Doxorubicin
Bleomycin
Mitoxantrone

25
Doxorubicin MOA
From Streptomyces peucetius Intercalates to DNA, inhibits topoisomerase 2, interferes with RNA synthesis Produces free radicals Act on cells deficient in superoxide dismutase (cardiac and tumor cells)
26
Doxorubicin uses
Most effective Lymphoma and leukemia of K9s and cats Combo with cyclophosphamide to treat lymphosarcoma in K9s and cats
27
Doxorubicin toxicity
Cardiotoxicity is K9s Anorexia and nephrotoxicity in cats Palmer-planta erythrodysesthesia syndrome (treated with B6)
28
Bleomycin
From S. verticillus IV, IM, SC Cell specific: G2 and M phase Treats squamous cell carcinoma
29
Bleomycin toxicity
Causes cytoxicity by binding to DNA Pulmonary toxicity (rales, cough, fatal fibrosis)
30
Mitoxantrone
Synthetic athracenedione Treats lymphoproliferative disorders (lymphomas and leukemias) Transitional cells carcinoma of urinary bladder
31
Mitoxantrone toxicity
Extravasation necrosis Mild BM depression Bluish- green sclera and urine
32
Antimetabolites
Prevents biosynthesis of cell metabolism S-phase specific Metabolized to active form Used for leukemias
33
Antimetabolite drugs
Pteridines (methotrexate) Pyrimidine analogs (fluoroacil) Purine analogs (6- mercaptopurine)
34
Methotrexate
Inihibits dihydrofolate reductase IV, IM, IV, oral Limited veterinary use
35
Microtubule inhibitors and the cell cycle
Stope cell separation during division during the G2 phase
36
Vinca alkaloids taxols and the cell cycle
Stop cell separation during divison during the M phase