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THER 201 Therapeutics > Cancer Therapy & Immunomodulators > Flashcards

Cancer Therapy & Immunomodulators Flashcards

1
Q

Heterogenous group of drugs

Induces cellular damage thru GENERATION OF INTRA-STRAND CROSSLINKS IN DNA

Covalent binding to nucleic acids is facilitated by the generation of ____________ –> affects DNA/RNA synthesis

Is cell cycle non-specific?

A

Alkylating Agents

Covalent binding to nucleic acids is facilitated by the generation of CARBONIUM ION GROUPS –> affects DNA/RNA synthesis

Cell cycle non-specific (exert maximum cytotoxicity at late G1 and S phase)

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2
Q

PD of nitrogen mustards

A

Cyclophosphamide

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3
Q

PD of nitrosoureas

A

Lomustine

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4
Q

PD of platinum agents

A

Cisplatin

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5
Q

PD of platinum agents

A

Cisplatin

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6
Q

Toxic effect of nitrogen mustards due to ACROLEIN

Other toxic effects:
Nausea/vomiting
Bone marrow depression

A

Hemorrhagic cystitis

Can be precvented by (1) hydration and (2) use of sulfhydryl donors (eg MESNA and NAC - N-acetylcysteine)

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7
Q

PD of nitrosoureas: Lomustine

Lipid soluble — CONSEQUENCE?
Used in CNS tumors
PO given
Used to treat hodgkin’s lymphoma

A

Lipid solubility of lomustine enables cumulative delayed myelosuppression, lowers bioavailabiloty of the drug

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8
Q

PD of platinum agent: Cisplatin

Water-soluble complex build around a central Pt atom (reacts with water to release Cl- –> Pt complex binds w/ DNA)

Given IV

What are the multiple indications of administering Cisplatin?

A

Head and neck tumors
Thoracic, germ cell/testicular cancers
Genitourinary cancers

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9
Q

PD of platinum agent: Cisplatin

Water-soluble complex build around a central Pt atom (reacts with water to release Cl- –> Pt complex binds w/ DNA)

Given IV

What are the toxic effects of Cisplatin?

A

Nausea - use 5HT3 receptor antagonists
Renal - hydration and diuresis needed
Neurologic (paresthesia of feet and hands)
Ototoxicity (high freq hearing loss and tinnitus)
Low myelotoxicity

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10
Q

Give other alkylating agents apart from

N mustards - cyclophosphamide
Nitrosoureas - lomustine
Pt agent - cisplatin

A

Dacarbazine
Temozolomide
Procarbazine

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11
Q

Analogs of natural compounds that inhibit purine synthesis

A

Antimetabolites

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12
Q

How do antimetabolites interfere with nucleic acid synthesis? Give 2 hehe

A

Competition of binding sites of enzymes

Incorporation into nucleic acids –> inhibits normal function –> apoptosis

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13
Q

Stage of cell cycle in which antimetabolites has high specificity?

Are alkylating agents non-specific?

A

S phase

Alkylating agents are cell cycle non-specific (exert maximum cytotoxicity at G1 and S)

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14
Q

Stage of cell cycle in which antimetabolites has high specificity?

Are alkylating agents non-specific?

A

S phase

Alkylating agents are cell cycle non-specific (exert maximum cytotoxicity at G1 and S)

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15
Q

PD of antifolate angents

A

Methotrexate

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16
Q

PD of pyrimidine analogues

A

Fluorouracil

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17
Q

PD of purine analogue

A

Fludarabine

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18
Q

What is the PD of antifolate?

What is its main function?

A

Methotrexate

Main function: interfere with THYMIDYLATE SYNTHESIS

Competitive antagonist of DHFR - dihydrofolate reductase

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19
Q

Does methotrexate have high lipid solubility?

A

Methotrexate, PD of antifolate agents, has poor lipid solubility, can’t cross BBB, no high dose regimen to treat primart CNS lymphoma is needed

But high dose regimens may cause nephrotoxicity, need for folinic acid rescue

20
Q

Give 2 antimetabolites that inhibit thymidylate synthase

A

Methotrexate and Fluorouracil

21
Q

Indication for fluorouracil use?

To be used with oxiplatin and irinotecan

A

Colorectal cancer

22
Q

Give two prodrugs of fluorouracil

Are these administered PO?

A

Capecitabine and Tegafur (coffee and toga)

Administered PO (fluorouracil is administered Iv or topically)

23
Q

Toxic effects of pyrimidine analogues

A

Cytopenias - anemia, thrombocytopenia

GI disturbances - diarrhea, abdominal pain, nausea

Stomatitis - oral ulcers, usu treated with ice chips

24
Q

What enzyme is inhibited by fludarabine, purine analogue PD?

What enzyme is inhibited by methotrexate and fluorouracil?

A

Ribonucleotide reductase - inhibited by fludarabine

Thymidylate synthase - inhibitrd by methotrexate and fluorouracil

25
Q

Phosphate prodrug converted to ribonucleotide upon entering cell

A

Fludarabine

26
Q

Used to treat chronic lymphocytic leukemia

A

Fludarabine

27
Q

Plant-derived cytotoxic agents

A

Vinca alkaloids
Taxanes
Camptothecins

28
Q

Bind to tubulin, preventing polymerization

M-phase specific

A

Vinca alkaloids

VINcristine
VINblastine
VINdesine
VINorelbine

29
Q

Indications for vinca alkaloids use

A

Lymphoma
Sarcoma
CNS tumors

30
Q

Toxic effects of vinca alkaloid use

A

Neurotoxicity (peripheral myopathy)
Myelotoxicity
Alopecia

31
Q

Bind to polymerized microtubules, preventing dissociation

M-phase specific

A

Taxanes

PacliTAXel
DoceTAXel

32
Q

Indications for taxanes use

A 
Sarcoma
Breast cancer
Lung cancer
H&N tumora
Gynecologic malignancies
33
Q

Toxic effects of taxanes use

A

Neurotoxicity
Myelosuppression
Fluid retention (particularly with Docetaxel)
Hypersensitivity (requires pre-medications w/ steroids and anti-histamines)

34
Q

Act on topoisomerase 1

G1-S phase specific

A

Camptothecins

IrinoTECAN
TopoTECAN

35
Q

Indications for camptothecins use

A

Colorectal cancer (CRC)
CNS tumors
Small cell lung cancer (SCLC)

36
Q

Toxicities of camptothecins

A

Diarrhea (more of irinotecan)

  • acute: due to cholinergic effect of drug: treat w/ atropine
  • => 24 hrs: due to tissue damage: treat w/ loperamide

Myelosuppression

37
Q

Heterogenous group
Exert effect mainly on DNA
Cell cycle non-pspecific except for BLEOMYCIN

A

Anti-tumor cytotoxic agents

38
Q

First approved topoisomerase 2 poison

Alkylator

A

Anthracyclines: Doxorubicin

39
Q

Only approvrd treatment to amelioraye extravasation of doxorubicin

A

Dexrazoxane

40
Q

Intercalates in the minor groove of DNa betweem adjacent G-C pairs and interferes with movement of RNA pol, preventing transcription

A

Dactinomycin

41
Q

Indications for dactinomycin use

A

Ewing’s sarcoma

Pediatric cancers

42
Q

Degrades preformed DNA through chelation of Fe2+, producing ROS

G2 and M phase, also in G0

Used kn Hodgkin’s lymphoma

Toxicity: pulmonary fibrosis

A

Bleomycin

43
Q

Bifunctional alkylating agent, binds to O6 of guanine

May also degrade DNA through ROS generation

A

Mitomycin

44
Q

Used in treatment of anal cancer w/ fluoroucracil and radiation therapy (Nigro protocol)

A

Mitomycin

45
Q

Toxicities of mitomycin

A

Pulmonary fibrosis
Delayed myelosuppression
Nephrotoxicity

THER 201 Therapeutics (7 decks)

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