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Pharmacology > Anti-Cancer Drugs > Flashcards

Anti-Cancer Drugs Flashcards

1
Q

Criteria for drugs used in combination tx

A
  1. Each drug should be active alone against the particular cancer 􏰀
  2. The drugs should have different targets/mechanisms of action 􏰀
  3. Cross-resistance between drugs should be minimal
    􏰀
  4. The drugs should have different toxicities to the patient
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2
Q

Recruitment tx

A

initial use of CCNS drug resulting in recruitment of previously resting cells into active cell division, where they are now susceptible to a CCS drug

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3
Q

Name the classes of anti-cancer drugs

A
  1. DNA-damaging drugs (CCNS)
  2. Antimetabolites (CCS)
  3. Antimitotic agents (CCS)
  4. Topoisomerase inhibitors (CCS)
  5. Hormonal Agents (Prednisone)
  6. Target-specific agents
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4
Q

DNA-damaging drugs

  1. General
  2. List drugs
A
  1. CCNS 􏰀
    -Alkylating agents
    -􏰀Platinum compounds
    􏰀-Antitumor antibiotics
    􏰀 -Cause DNA cross-linking, abnormal base pairing, strand breaks
  2. Drugs:
    - Bleomycin
    - Carboplatin
    - Doxorubicin
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5
Q

Antimetabolites

  1. General
  2. List drugs
A
  1. CCS
    􏰀 -Act mainly S phase
    􏰀 -Structurally similar to purines and pyrimidines required for nucleic acid biosynthesis, interfere with DNA synthesis
  2. Drugs:
    - 5-Fluorouracil
    - Gemcitabine
    - Methotrexate
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6
Q

Antimitotic agents

  1. General
  2. List drugs
A
  1. CCS
    􏰀 -“Spindle poisons”
    -interfere with microtubule function
    -act mainly in M phase
  2. Drugs:
    - Vincristine
    - Paclitaxel
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7
Q

Topoisomerase Inhibitors

  1. General
  2. List drugs
A
  1. CCS
  2. Drugs:
    - Etoposide
    - Irinotecan
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8
Q

Target-Specific agents

  1. What types of drugs fall into this category?
A

-Monoclonal antibodies
􏰀-mTOR inhibitors
-Tyrosine kinase inhibitors

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9
Q

Target-Specific agents:

1. Monoclonal antibodies

A

Bevacizumab
Cetuximab
Rituximab
Trastuzumab

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10
Q

Target-Specific agents:

􏰀2. mTOR inhibitors

A

Temsirolimus

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11
Q

Target-Specific agents:

  1. Tyrosine kinase inhibitors
A

Erlotinib
Imantinib
Sunitinib

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12
Q

Common adverse effects of anticancer agents:

Immediate

A
  1. Hours to days

􏰀a) Nausea, vomiting, abdominal pain, anorexia
􏰀b) Allergic, hypersensitivity reactions
• a lot with chimeric Ab or natural products by fungi or other organisms
􏰀c) Local necrosis (extravasation)

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13
Q

Common adverse effects of anticancer agents:

Early

A
  1. Days to weeks
    a) 􏰀 Impaired wound healing
    􏰀b) Myelosuppression: leukopenia, neutropenia, anemia, thrombocytopenia 􏰀
    c) Mucositis
    • inflammation and ulceration of the digestive tract
    􏰀 d) Diarrhea
    • usually symptom of mucositis
    􏰀 e) Alopecia
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14
Q

Common adverse effects of anticancer agents:

Delayed

A
  1. Weeks to months
    a) Aspermia
    b) pulmonary fibrosis
    c) Neurotoxicity
    - often w/spindle poisons
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15
Q

Common adverse effects of anticancer agents:

Late

A
  1. Months to years
    - sterility
    - secondary malignancies (5-7 years)
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16
Q

General precautions when using anticancer agents

A

􏰀1. Baseline and periodic CBCs

􏰀 2. Active infections; watch for opportunistic infections e.g.
Pneumocystis pneumonia

􏰀3. Avoid patient dehydration; aggressive hydration (~ 3 mL/kg/hr) with NS is usually beneficial

􏰀 4. Avoid vaccination during therapy because of reduced immune response

  1. 􏰀 Health care personnel should avoid accidental exposure during preparation and handling, use protective gowns, gloves, goggles
  2. Avoid extravasation!
    􏰀
  3. Pregnancy Risk Category D or X
17
Q

DNA-damaging drugs: Alkylating agents:

General mech and List drugs

A
  1. Nitrogen mustards alkylate DNA causing cross-linkages
  2. Cyclophosphamide
    Temozolomide
18
Q

Platinum Compound Drug

A

Carboplatin (paraplatin)

19
Q

Antitumor Antibiotics

A

Bleomycin

Doxorubicin

20
Q

Monoclonal Abs

General Mechanism

A
  1. Artificially produced, designed to bind to antigens expressed on the surface of malignant cells

a)􏰀 Block the growth of cancer cells and/or recruit the body’s immune system to attack the cancer cells
􏰀
c) Can be given as monotherapy, in combination with chemotherapy, and with other targeted therapies under clinical trial

21
Q

Common Infusions Reactions to mouse antigen

A 
fever
chills
NV
hypotension 
angioedema
bronchospasm
22
Q

Tyrosine Kinase Inhibitors: General

A
  1. TK in cancers become constitutively activated leading to unrestricted cell growth
  2. All of these drugs are CYP3A4 substrates so a lot of drug interactions can happen!
23
Q

Mechanisms of resistance to anticancer treatment

A 
1. 􏰀 Increased DNA repair
􏰀 a) Alkylating agents
􏰀 b) Platinum compounds
􏰀 
2. Increased inactivation
􏰀 a) Increased GSH production → trapping of electrophilic drugs 􏰀 
 --Bleomycin
􏰀 --Platinum compounds
􏰀 --Anthracyclines (doxorubicin)
 b) 􏰀 Increased enzymatic inactivation
  1. Target or suppressor mutations
    􏰀 a) DHFR overexpression (methotrexate)
    􏰀 b) Topoisomerase mutations (etoposide, irinotecan)
    c) Mutation in p53 tumor suppressor gene → decreased apoptosis
  2. 􏰀 Decreased activation of prodrugs
    􏰀 a) Purine and pyrimidine antimetabolites
  3. Decreased drug accumulation
    a) 􏰀 Increased efflux via P-glycoprotein (ABCB1; MDR1)

Pharmacology (12 decks)

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