Week 7 Flashcards

1
Q

Alkylating agents

A
  • transfer alkyl groups to various cellular constituents
  • general MOA involves intramolecular cyclization forming an ethylene imonium ion that may directly or through formation of a carbonium ion transfer an alkyl group to a cellular constituent
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2
Q

Antimetabolites

A

have similar chemical structure to essential substances in the cell and interfere with utilization of these substances which adversely affects cell function and growth

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3
Q

Anti-tumor antibiotics

A

bind to DNA through intercalation between specific bases and block the synthesis of RNA, DNA, or both

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4
Q

Treatment strategies

A
  • Surgery
  • Radiotherapy
  • Chemotherapy
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5
Q

Primary chemotherapy

A

Chemo is the only thing that can be helpful

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6
Q

Neoadjuvant chemotherapy

A

prior to surgery to reduce tumor size

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7
Q

Adjuvant chemotherapy

A

after surgery

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8
Q

Combination chemotherapy

A

multiple drugs used

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9
Q

Why use combo therapy

A
  • Way to get around resistance
  • Increase cell kill while limiting toxicity (Do not want to overlap toxicity- do not double down on cardio-toxic effects)
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10
Q

Models of cell kinetics

A
  • murine

- gompertzian

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11
Q

Murine

A

-exponential cell growth; so there is a constant faction of cells being killed instead of a certain number

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12
Q

Gompertzian

A
  • slow in beginning, increases exponentially and then plateaus
  • tumor will proliferate rapidly until it gets to a certain size, this will cause more cells to stay in G0
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13
Q

What cell cycle phase do anticancer cancer agents inhibit?

  • Antimetabolites
  • Vinca Alkaloids
  • Bleomycin
  • Taxanes
A

Antimetabolites: S phase
Bleomysin: G2 phase
Vinca alkaloids and taxanes: M phase

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14
Q

Agents not cell cycle specific

A
  • Alyklating agents
  • MAB
  • TK receptor inhibtors
  • Anthro-cyclines
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15
Q

Mechanisms of anti-cancer drug resistance

A

-P53- tumor suppressor gene: If mutated, unable to suppress cell cycle
-Anti-metabolites: Methylate DNA and cross link DNA so that it cannot be replicated and cancer cells can resist
by increasing the amount of enzyme that degrades anti-cancer therapeutic of blocking enzyme that would turn on medication

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16
Q

Treatment for Hodgkins lymphoma

A
  • Blemoycin
  • Doxorubicin
  • Vinca alkaloids
  • Decarbazine
17
Q

Blemoycin

A
  • anti-tumor antibiotic w/ pulmonary toxicity
  • Binding to DNA, which results in single- and double-strand breaks following free radical formation, and inhibition of DNA biosynthesis
18
Q

Doxorubicin

A
  • Oxygen free radicals bind to DNA causing single- and double-strand DNA breaks; inhibits topoisomerase II; intercalates into DNA; w/
  • Cardio toxicity (all anthro cyclines)
  • Rescue therapy: dexresosan which inhibits generation of free radicals- before
19
Q

Vinca alkaloids

A

-Micro-tubule de-stabalizer, from periwinkle plant, toxicity Nausea, vomiting, allopecia,

20
Q

Breast Cancer

A
  • Trestuzamab
  • Cyclophosphamide (alkylating agent)
  • Tamoxifen
  • Anastrozole
  • Methotrexate (anti-metabolite)
21
Q

Trestuzamab

A

HER2 receptor blocker

22
Q

Cyclophosphamide (alkylating agent)

A
  • Great bio-availability
  • Hemorrhagic cystitis: Metabolite (acarlyn) is toxic to bladder because it is excreted through urine
  • Rescue therapy: mesna; Prior- not after, because it prevents from happening but does not help with symptoms after it occurs
23
Q

Tamoxifen

A
  • SERM: antagonist for estrogen receptor. Given for years
24
Q

Anastrozole

A
  • aromatase inhibitor; Given for years
25
Q

Methotrexate (anti-metabolite)

A
  • Works on di-hydro folate reductase
  • Inhibition of thymalade synthase
  • Inhibits purine nucleotides
  • High dose: Mucocytis; harsh on GI system,
  • Can be overdosed: rescue is leucovorin which produces felonic acid so cells are able to use that instead of folic acid to make DNA
26
Q

Colon cancer treatment

A
  • FU-5P
  • Oxaloplatin
  • Bevizisumab
27
Q

5- Fluorauracil

A
  • antimetabolite
  • inhibits thymidylate synthase; incorporation of FUTP (5-fluorouridine-5′-triphosphate)into RNA and DNA which inhibits RNA processing and DNA synthesis and function
28
Q

Oxaloplatin

A

-alkylating agent, cross-links DNA

29
Q

Bevizisumab

A
  • growth factor receptor inhibitor
  • Inhibits angiogenesis through VEGF
  • Can cause bleeding
  • Have to have wild type RAS or drug is ineffective because it effects TKR
30
Q

Squamous non-small cell carcinoma

A

-Alkylating agent: cysplatin
Growth Factor Receptor
-Inhibitor: cetizumab

31
Q

plactotaxel

A
  • Taxanes
  • Microtubule stabilizer that act at M phase and prevent cell from continuing in cell cycle
  • Allergic reaction, peripheral neuropathy