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Pharm > Chemo Drugs 1/2 > Flashcards

Chemo Drugs 1/2 Flashcards

1
Q

Phase 1 clinical trials

A

Determine dose and dose limiting toxicity

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2
Q

Phase 2 clinical trials

A

determine activity

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3
Q

phase 3 clinical trials

A

determine efficacy

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4
Q

Goldi-coldman hypothesis

A

neoplastic cell resistance to chemo occurs as a chance, spontaneous, event analogous to resistance of bacterial antibiotics

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5
Q

Skipper Hypothesis

A

ability of chemotherapy to cure cancer is inversely proportional to the tumor burden

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6
Q

Ondansetron should be avoided when

A

long QT sydnrome

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7
Q

ANC

A

total white count X (fraction of PMN + fraction of bands)

-any patient who develops fever greater than 385 and has ANC less than 500 must hospitalized and started on broad spectrum antibiotics until ANC greater than 500

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8
Q 
Alkylating Agents
bis(chlorethyl)amines
Cyclophosphamide 
Mechlorethamine
Chlorambucil (oral)
Melphalan(oral) 
How do they work ?
A
  1. Drugs bind covalently to DNA
  2. cell cycle non-specific
  3. DNA drug interstrand and intrastrand crosslinks
  4. Bifunctional alkylating agents that preferentially alkylate the N-7 position of guanine
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9
Q

How do cancers develop resistance to alkylating agents?

A

enhanced DNA repair (nucleotide excision repair enzymes) or binding the alkylating agents to sulfur containing molecules

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10
Q 
Cyclophosphamide
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
Side effects:
A

Class: bifunctional alkylating agent (oxazaphosphorine)
Cycle specificity: CCNS
Macromolecular target: DNA
Bioactivation: P-450 oxidase in liver
MOA: alkylates the N7 position of guanine and forms intrastrand and interstrand crosslinks
Pharmacokinetics and metabolism: Metabolites excreted in urine
Side effects: N/V, hairloss, myelosuppression(dose limiting toxicity), hematuria

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11
Q

Special features and dose modifications of Cyclophosphamide

A
  1. Hematuria
    - administer drug in morning with 6-8 glasses water
    - continuous bladder irrigation
    - use of MENSA(uroprotective agent-thiol group of mensa binds toxic metabolites)
  2. occasional occurrence of acute leukemia due to mutagenic effects of drugs
  3. no guidelines for dose modifications due to renal or hepatic dysfunction
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12
Q

What is cyclophosphamide used for?

A
  1. Breast Cancer

2. Non-Hodgkin’s lymphoma

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13
Q 
Ifosfamide
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
Side effects:
A

Class: alkylating agent, isomer of cyclophosphamide
Cycle specificity: CCNS
Macromolecular target: DNA
Bioactivation: P-450 oxidase (same as cyclophosphamide)
MOA: DNA crosslinking
Pharmacokinetics and metabolism: excreted in urine
Side effects: Myelosuppression is dose limiting. At high doses: lethargy and confusion. N/V hairloss

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14
Q

What is always administered with ifosfamide?

A

MENSA

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15
Q

What do you use ifosfamide for?

A
  1. sarcomas

2. relapsed testicular cancer

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16
Q 
Temozolomide
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
Side effects:
A

Class: Monofunctional Alkylating agent
Cycle specificity: CCNS
Macromolecular target: DNA
Bioactivation: spontaneous hydrolysis to the DNA reactive species
MOA: DNA reactive species methylates the DNA and inhibits DNA function and DNA synthesis
Pharmacokinetics and metabolism: one third of administered dose
Side effects: Myelosuppression is dose limiting. N/V hair loss

17
Q

Special Features of Temozolomide

A
  1. dose modifications will be for myelosuppression
  2. Drug can be given orally or intravenously
    * 3. the drug can be given with radiation therapy treatments.
    * 4. prophylaxis for pneumocystis carinii pneumonia
  3. no guidelines for dose modifications due to renal or hepatic dysfunction
18
Q

What are uses of temozolomide?

A

malignant brain tumors

19
Q

Pt Coordination compounds

A

non classical DNA alkylating agents-covalently binding to DNA
Pt in the +2 oxidation state
leaving groups are cis
preferential binding to N7 position of adenine and guanine

20
Q 
Cis-diamminedichloroplatinum (2) (CISPLATIN)
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
A

Class: bifunctional alkylating agent
Cycle specificity: CCNS
Macromolecular target: DNA
Bioactivation: The parent compound is not active. In presence of low chloride ion concentration, the molecule undergoes sequential aquation
MOA: Binds covalently to DNA to produce cytotoxic intrastrand adducts and interstrand crosslinks
Pharmacokinetics and metabolism: Tightly bound to proteins in plasma. Excretion is via the kidneys

21
Q

Cisplatin

Side effects

A

Side effects:

  1. Intense nausea and vomiting.
  2. Renal Toxicity is dose limiting.
  3. Myelosuppression in less than 25%.
  4. Hypomagnesemia.
  5. Peripheral neuropathy in less than 5%.
  6. 8th cranial nerve damage -high frequency hearing loss
  7. Allergic reactions
22
Q

Special features of cisplatin

A
  1. to avoid renal damage drug is given with saline/mannitol diuresis. Chloruresis protects kidneys. —since must be given with hydration-patients with pre-existing cardiac/pulmonary problems may not be able to tolerate
  2. dose reductions of drug are necessary for patients with renal insufficiency
23
Q

Uses of cisplatin

A

Testicular cancer, bladder cancer, head and neck cancer, ovarian cancer, small cell and non small cell lung cancer

24
Q

Carboplatin vs. cisplatin

A

-cross resistant with cisplatin

  • not renal toxic
  • dose dependent on myelosuppression

-dose is calculated using target AUC
(free carboplatin plasma concentration X time)
dose=AUC X (GFR+25)

  • does not have to be given with saline hydration and is good alternative when organ dysfunction precludes cisplatin
  • testicular, bladder, head and neck, ovarian, small and non small cell lung cancer
25
Q

Oxaliplatin

A
  • 3rd generation
  • excreted via kidneys and is not nephrotoxic
  • myelosuppression is common but not severe
  • *-dose limiting toxicity is neurotoxicity: acute and chronic
    acute: cold induced shocks (last about a week)
    chronic: sensory neuropathy-stocking and glove-tends to get better with time but doesn’t completely resolve

-SIGNIFICANT activity against COLORECTAL CANCER!

26
Q 
Plant alkaloid overview
Vincristine
Vinblastine 
Taxol
Etoposide (semisynthetic)
A

Vincristine, Vinblastine, Taxol: M phase cell cycle specific

-Dependent cytotoxicity: taxol and vincristine

27
Q 
Vincristine
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
Side effects:
A

Class: Plant alkaloid, spindle poisons
Cycle specificity:CCS
Macromolecular target: Tubulin
Bioactivation: None
MOA: binds to dimeric form of tubulin and prevents polymerization and thus, microtubule assembly, and causes the dissolution of mitotic spindle
Pharmacokinetics and metabolism: Excretion is via the bile and patients with an elevated bilirubin require a dose reduction
Side effects:
1. neuropathy is dose limiting. sensory and autonomic neuropathies.
2. Stimulation of ADH release my produce hyponatremia.
3. Does not cause myelosuppression. 4. Hair Loss, Nausea and vomiting are not a problem

28
Q

What are special features of vincristine?

A

Dose reduction is necessary for elevated bilirubin

29
Q

What is vincristine used for?

A

Lymphoma, Hodgkin’s disease, lymphoblastic leukemia

30
Q

Vinacristine vs VInblastine vs. vinorelbine

not in PPT

A

Vinblastine:much less neurotoxic than vincristine
-dose limiting toxicity is myelosuppression

Vinorelbine: useful in lung cancer and breast cancer

31
Q 
Paclitaxel 
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
Side effects:
A

Class:plant alkaloid

Cycle specificity: CSS (m-phase)

Macromolecular target: tubulin

Bioactivation: None

MOA: prevents tubulin disassembly

Pharmacokinetics and metabolism: tightly bound to plasma proteins and excreted via the biliary system. Hepatic metabolism

Side effects:

  1. Myelosuppression is dose limiting
  2. Nausea/vomiting, hair loss, stomatitis
  3. peripheral sensory neuropathy, myalgias, arthralgias
32
Q

Paclitaxel special features

A
  1. Must be premedicated with steroids (diphenhydramine and H2 blocker) to decrease the incidence of allergic reactions
  2. Dose reduction in presence of hepatic dysfunction
33
Q

What are the uses of paclitaxel

A

ovarian cancer, non small cell lung cancer, gastroesophageal cancer, breast cancer

34
Q

What are other compounds in the paclitaxel class?

A

Docetaxel: prostate cancer

Albumin bound paclitaxel: no allergic reactions and less myelosuppression and less neuropathy

Cabazitaxel: prostate cancer

35
Q 
Etoposide
Class:
Cycle specificity:
Macromolecular target:
Bioactivation:
MOA:
Pharmacokinetics and metabolism:
Side effects:
A

Class: plant alkaloid, podophyllotoxin

Cycle specificity: CCS (G1-S phase)

Macromolecular target: topoisomerase 2

Bioactivation: None

MOA:Complex of drug, DNA and topoisomerase 2 produces DNA strand breakage

Pharmacokinetics and metabolism: excreted via the kidneys and to a lesser amount the bile

Side effects:

  1. N/V hairloss
  2. Dose limiting toxicity is myelosuppression
36
Q

What are special features of Etoposide

A
  1. drug is leukemogenic-increased incidence of treatment related leukemia
  2. dose reductions with abnormal kidney and hepatic function
37
Q

What are the uses of Etoposide?

A

testicular cancer, small cell lung cancer, lymphomas

Pharm (36 decks)

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