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M3 Pharm B3 > Anti-neoplastic Agents > Flashcards

Anti-neoplastic Agents Flashcards

1
Q

Cancer (Malignant neoplasia) Defined (3)

A

Uncontrolled growth and spread of abnormal cells

Tumors may be benign or malignant (cancer)

In cancer, cell proliferation (cell renewal and replacement (becomes unbalanced)

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2
Q

Goal of cancer treatment (2)

A
  1. Total cell kill

2. To kill cancer without destroying normal cells

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3
Q

First order kinetics: Fractional Cell Kill (2)

A

Cancer drugs kill a fixed percentage (proportion) of tumor cells and not a fixed number of cells

This means that the same dose which decreases tumor burden from 10^6 to 10^3 cells will be needed to decrease the burden from 10^3 to 10^0 cells

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4
Q

Log-cell kill hypothesis (3)

A

Magnitude of a tumor cell kill is a logarithmic function

A dose of an effective drug will reduce the cancer cell load from trillion cells to billion cells: 3-log-kill

One of the reason for use of drug combination

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5
Q

Generation Time

A

Time to complete one cycle

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6
Q

Growth Fraction

A

% of cell which are actively dividing

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7
Q

2 Types of Drugs Against Cancer `

A
  1. Cell-cycle specific

2. Cell-cycle non specific

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8
Q

Cell-Cycle Specific (CCS) Drugs (2)

A

Acts on cell undergoing division

In general, CCS drugs are MOST effective in high growth fraction tumors

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9
Q

Cell-Cycle Non Specific Drugs (2)

A

Acts on cell during any phase

Useful in LOW growth fraction sold tumors as well as high growth fraction tumors

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10
Q

Cell Cycle: 1 - Non phase specific (5)

A
  1. Alkylating agents
  2. Nitrosourea
  3. Dacarbazine
  4. Cisplatin
  5. Antitumor antibiotics
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11
Q

Cell Cycle: 2. Phase specific (CCS) - a: G1 phase defined and drugs (2)

A

Synthesis of cells components needed for DNA synthesis

L-asparaginase
Mitomycin

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12
Q

Cell Cycle: 2. Phase specific (CCS) - b: S-phase (7)

A

Period of DNA synthesis

  1. Cytarabine
  2. 6-mercaptopurine (6MP)
  3. 6-thioguanine (6TG)
  4. Methotreaxate (MTX)
  5. Hydroxyurea
  6. Etoposide
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13
Q

Cell Cycle: 2. Phase specific (CCS) - c: G2 phase (2)

A

Preparation for mitosis

Bleomycin

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14
Q

Cell Cycle: 2. Phase specific (CCS) - d: M phase (4)

A

Mitosis

  1. Vinblastine
  2. Vincristin
  3. Paclitaxel
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15
Q

Cell Cycle: 1 - Non phase specific: Alkylating Agents (6)

A
  1. Cyclophosphamide
  2. Ifosfamide
  3. Mechrorethamine
  4. Melphalan
  5. Chlorambucil
  6. Busulphan
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16
Q

Cell Cycle: 1 - Non phase specific: Alkylating Agents - Cyclophosphamide Activation

A

Converted in liver to 4 hydroxyl CP to form 2 metabolites, where when they reach normal cells, get converted into active to 2 active metabolites: acrolein

17
Q

Cell Cycle: 1 - Non phase specific: Alkylating Agents MOA (2)

A

Donate alkyl groups to guanine N7 of DNA –> making it non-functional DNA

Bifunctional alkylating agents can cause intrastrand linking and cross-linking

18
Q

Cell Cycle: 1 - Non phase specific: Alkylating Agents MOA 2 (1)

A

Alkylation of guanine can result in miscoding through abnormal base pairing with thymine

19
Q

Cell Cycle: 1 - Non phase specific: Alkylating Agents - a. Cyclophosphamide Adverse Effect (1) and Prevention (1)

A

Hemorrhagic cystitis

Prevent it by Mesna

20
Q

Cell Cycle: 1 - Non phase specific: Alkylating Agents - b. Nitrosurea Drugs (2) and MOA

A
  1. Carmustine
  2. Lomustine
  3. Semustine

Crosses BBB

21
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - c. Platinum Agents - Cisplatin Side effects (3) and Prevention (1)

A
    1. Renal toxicity
      1. Peripheral sensory neuropathy
      2. Ototoxicity
  • Prevention: Amifostine (cytoprotectant) for renal toxicity
22
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - c. Platinum Agents - Carboplatin Side Effect (1)

A

Myelosuppression

23
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - c. Platinum Agents - Oxaliplatin (1)

A

Peripheral sensory

24
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - d. Others (3)

A
  1. Procarbazine
  2. Dacarbazine
  3. Altretamine
25
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - d. Others - Procarbazine MOA

A

Depolymerizes DNA

26
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - d. Others - Procarbazine Use

A

Hodgkin’s, NHL

27
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - d. Others - Procarbazine Adverse Effects (1)

A

Increased risk of secondary cancers - acute leukemia

28
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - e. Busulphan Use (1)

29
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - e. Busulphan Adverse effects (4)

A
  1. Skin pigmentation
  2. Acute lung injury
  3. Chronic interstitial fibrosis
  4. Alveolar hemorrhage (busulphan lung)
30
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - e. Busulphan - Chlorambucil Use

31
Q

Cell Cycle: 1 - Non phase specific: Alkylating agents - e. Busulphan - Chlorambucil Adverse Effects (4)

A
  1. Bone marrow suppression
  2. Anemia
  3. Neutropenia
  4. Thrombocytopenia

M3 Pharm B3 (10 decks)

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