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1. Pharmacology > Anticancer agents > Flashcards

Anticancer agents Flashcards

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
Q

Doxorubicin MOA

A

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
Q

Doxorubicin uses

A

Most effective
Lymphoma and leukemia of K9s and cats
Combo with cyclophosphamide to treat lymphosarcoma in K9s and cats

27
Q

Doxorubicin toxicity

A

Cardiotoxicity is K9s
Anorexia and nephrotoxicity in cats
Palmer-planta erythrodysesthesia syndrome (treated with B6)

28
Q

Bleomycin

A

From S. verticillus
IV, IM, SC
Cell specific: G2 and M phase
Treats squamous cell carcinoma

29
Q

Bleomycin toxicity

A

Causes cytoxicity by binding to DNA
Pulmonary toxicity (rales, cough, fatal fibrosis)

30
Q

Mitoxantrone

A

Synthetic athracenedione
Treats lymphoproliferative disorders (lymphomas and leukemias)
Transitional cells carcinoma of urinary bladder

31
Q

Mitoxantrone toxicity

A

Extravasation necrosis
Mild BM depression
Bluish- green sclera and urine

32
Q

Antimetabolites

A

Prevents biosynthesis of cell metabolism
S-phase specific
Metabolized to active form
Used for leukemias

33
Q

Antimetabolite drugs

A

Pteridines (methotrexate)
Pyrimidine analogs (fluoroacil)
Purine analogs (6- mercaptopurine)

34
Q

Methotrexate

A

Inihibits dihydrofolate reductase
IV, IM, IV, oral
Limited veterinary use

35
Q

Microtubule inhibitors and the cell cycle

A

Stope cell separation during division during the G2 phase

36
Q

Vinca alkaloids taxols and the cell cycle

A

Stop cell separation during divison during the M phase

1. Pharmacology (29 decks)

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