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HEME II > Antineoplastic agents > Flashcards

Antineoplastic agents Flashcards

1
Q

Alkylating Agents

Nitrogen mustards

A

Cyclophosphamide

Ifosfamide

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2
Q

Alkylating Agents

Alkyl sulfonate

A

Busulfan

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3
Q

Alkylating Agents

Platinum coordination complexes

A

Cisplatin

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4
Q

Natural Products

Vinca alkaloids

A

Vinblastine
Vinorelbine
Vincristine

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5
Q

Natural Products

Taxanes

A

Paclitaxel

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6
Q

Natural Products

Epipodophyllotoxins

A

Etoposide

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7
Q

Natural Products

Antibiotics

A

Doxorubicin

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8
Q

Natural Products

Anthracenedione

A

Bleomycin

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9
Q

Natural Products

Enzymes

A

L-Asparaginase

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10
Q

Antimetabolites

A 
Folic acid analogs
  Methotrexate
Pyrimidine analogs	
  Fluorouracil (5-fluorouracil; 5-FU)
Purine analogs
  Mercaptopurine (6-MP)
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11
Q

Rescue agents

A

Leucovorin

Mesna

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12
Q

Protein tyrosine kinase inhibitors

A

Imatinib

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13
Q

Monoclonal Antibodies

A

Trastusumab

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14
Q

Agents used to minimize adverse effects

A

Filgrastim
Erythropoietin or darbepoetin alfa
Serotonin antagonists
Ondansetron

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15
Q

Alkylating Agents MOA

A

Form covalent linkages with DNA

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16
Q

Specific alkylating agent toxicities

A

Cyclophosphamide – hemorrhagic cystitis
Cisplatin – renal tubular damage, ototoxicity
Busulfan – pulmonary fibrosis

17
Q

Antimetabolites: 3 major classes

A 
Folic acid analogs (methotrexate)
Pyrimidine analogs (5-Fluorouracil)
Purine analogs (6-mercaptopurine)
18
Q

Antimetabolites MOA

A

Structural analogs to compounds necessary for cell proliferation

Block or subvert pathways that are involved in, or lead to, cell replication (nucleotide and nucleic acid synthesis)

Cell cycle specific (S phase)

19
Q

Methotrexate

A 
Inhibits dihydrofolate reductase (DHFR)
Indications:
  Cancer
  Rheumatoid arthritis
  Psoriasis
20
Q

Methotrexate & Leucovorin Rescue

A

Leucovorin: reduced folate can bypass DHFR

Used to rescue normal cells from high-dose MTX

Antidote for accidental MTX overdose

21
Q

Pyrimidine Structural Analogs

A

Prototype: 5-Fluorouracil (5-FU)

Prodrug

22
Q

Fluorouracil: Mechanisms of Action

A

Active compound (FdUMP) covalently binds thymidylate synthetase and blocks de novo synthesis of thymidylate

Active compounds (FdUTP and FUTP) are incorporated into both DNA and RNA, respectively

Leucovorin can’t rescue

23
Q

Drug Interaction: 6-MP & Allopurinol

A

Biotransformation of 6-MP includes metabolism to the inactive metabolite 6-thiouric acid by xanthine oxidase (first pass effect)

Allopurinol, a xanthine oxidase inhibitor, is often used as supportive care in the treatment of acute leukemias to prevent hyperuricemia due to tumor cell lysis

Simultaneous administration of allopurinol and oral 6-MP results in increased levels of 6-MP and increased toxicity

Reduce oral 6-MP dose by 50-75%; IV dose unaffected

24
Q

Antimetabolites: Pharmacodynamics

A

Cell cycle specific (S-phase)
Relatively little acute toxicity after an initial dose
Oral, intravenous, intrathecal (methotrexate) are common routes of administration
Common toxicities include diarrhea, myelosuppression, nausea, vomiting, immunosuppression, thrombocytopenia, leukopenia, hepatotoxicity

25
Q

Vinca Alkaloids: Adverse Effects

A

Alopecia
Myelosuppression (vinblastine > vincristine)
Vincristine exhibits neurotoxicity (numbness and tingling of the extremities, loss of deep tendon reflexes, motor weakness, autonomic dysfunction has also been observed)

26
Q

Vinca Alkaloids: Mechanism of Action

A

Bind to β-tubulin and inhibit microtubule assembly

Cell cycle specific mitosis inhibition (M-phase)

27
Q

Taxanes: Mechanism of Action

A

Bind to β-tubulin and stabilize microtubule assembly

Cell cycle specific mitosis inhibition (M-phase)

28
Q

Taxanes: adverse effects

A

Paclitaxel
Hypersensitivity reactions in hands and toes, change in taste

Docetaxel
Greater cellular uptake; retained intracellularly longer than paclitaxel permitting smaller dose, which reduces AEs
Hypersensitivity, neutropenia, alopecia

29
Q

Topoisomerase Inhibitors

A

Type I
Type II - Inhibitors:
Epipodophyllotoxins (etoposide, teniposide)
Anthracycline antibiotics (doxorubicin, daunorubicin)

Cell cycle specific (primarily S phase, also G1 and G2)

30
Q

Anthracyclines: MOA

A

Inhibit topoisomerase II
Intercalate DNA
Oxygen free radicals bind to DNA causing single- and double-strand DNA breaks

Cell cycle nonspecific (but cycling cells are more susceptible)

Free radicals are linked to significant cardiotoxicity
Cumulative cardiac damage can lead to dysrhythmias and heart failure

31
Q

Antitumor Antibiotics: Bleomycin

A

MOA: Free radicals cause single- and double-strand DNA breaks
Cell cycle specific (G2 arrest)
Causes minimal myelosuppression – useful in combination
Can cause significant pulmonary toxicity (5-10%, usually presents as pneumonitis with cough, dyspnea, dry inspiratory crackles)

32
Q

Antineoplastic Enzymes

L-aspariginase

A

MOA: hydrolyzes circulating L-asparagine into aspartic acid and ammonia, effectively inhibiting protein synthesis
Cell cycle specific (G1)

33
Q

Antineoplastic Enzymes: Adverse effects

A

Acute hypersensitivity reaction
Delayed toxicities include an increased risk of clotting and bleeding, pancreatitis, and CNS toxicity including lethargy, confusion, hallucinations, and coma

34
Q

Antineoplastic Enzymes: Indication

A

Targeted therapy for acute lymphoblastic leukemia (ALL)

ALL tumor cells lack the enzyme asparagine synthetase and thus require an exogenous source of L-asparagine

35
Q

Erlotinib and Gefitinib

A

MOA: Inhibit Epidermal Growth Factor Receptor (EGFR), a receptor tyrosine kinase
Preferred single-agent first-line therapy for NSCLC patients with somatic activating EGFR mutations
Produce dermatologic toxicities

36
Q

Bcr-Abl, CML, and Imatinib (Gleevec)

A

The BCR-ABL fusion protein results from the t(9:22) translocation and is found in 95% of patients with CML

Imatinib is a small molecule inhibitor of the ABL tyrosine kinase and has been hailed as a conceptual breakthrough in targeted chemotherapy

Imatinib can also inhibit the RTKs PDGFR and c-KIT

HEME II (5 decks)

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