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Drugs/Immuno > Antineoplastics > Flashcards

Antineoplastics Flashcards

1
Q

Imatinib

A
  • t(9,22) Philadelphia chromosome
  • lipophilic, metabolized by CYP450 (CYP3A4)
  • binds inactive kinase receptor, inhibits ATP binding site
  • causes: N,V,D,skin rxns,hepatotoxicity,hypertension,myelosuppression, edema,CH
  • use: GI strongly tumors
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2
Q

Gefitinib/Erlotinib

A
  • deletions in exon 19, L858R
  • blocks EGFR-ERB1, tyrosine kinase inhibitor
  • EGFR has 4 family receptors (ERbB1-4) which may compensate for one
  • causes:rash,diarrhea, hypertension,hepatotoxicity,GI perforation,lung diseas
  • use: NSCLC
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3
Q

Trastuzumab (Herceptin)

A
  • EGFR HER2 inhibitor, blocks dimerization
  • mediates receptor blockade, receptor internalization and apoptosis
  • causes:N,V,D,rigors,cardiac dys,CHF,hypotension,edema
  • use: breast cancer with taxol
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4
Q

Bevacizumab

A
  • anti-VEGF, inhibits angiogenesis

- uses:colon cancer,vasculopathy of eyes

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5
Q

Ipilimumab

A
  • anti CTLA4(cytotoxic T lymphocyte associated protein 4)
  • CTLA4 downregulates immune system
  • use: melanoma, NSCLC
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6
Q

Pembrolizumab, Nivolumab

A
  • against PD1 (programmed death receptor 1)
  • expressed on subset of NK cells
  • effective in pts with biomarker,mismatch repair deficiency
  • use:melanoma, NSCLC,Hodgkins lymphoma
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7
Q

Thalidomide

A
  • inhibits VEGF and bFGF
  • arrests myeloma cells at G1, decrease of IL1,IL6,lessen cell adhesion, disruption of BCL2 antiapoptosis, increase IL2 and NK activity
  • teratogenic, peripheral neuropathy
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8
Q

Bortezomib

A
  • inhibits ubiquitin-proteasome pathway
  • disregulates protein turnover in cell and NK inflammatory pathways
  • sensitizes cells to apoptosis via ER stress and unfolded protein response
  • VERY toxic, toxic dose=therapeutic dose
  • causes:peripheral neuropathy, hypotension,GI dys,myelosuppression
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9
Q

What are the Classical Toxicities?

A

Bone marrow suppression, ulcers of oral/GI mucosa,alopecia,impaired wound healing, crystalluria

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10
Q

Mechlorethamine - Alkylating agent

A
  • binds directly to DNA
  • spontaneous activation to reactive carbonium ions
  • given by IV near tumor site
  • classical toxicity, bone marrow suppression is limiting
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11
Q

Cyclophosphamide - Alkylating agent

A
  • bind directly to DNA
  • prodrug activated by CYP450
  • given orally, wide distribution, metabolities/active drug in urine
  • causes: classical toxicity, myocarditis, hemorrhagic cystitis
  • use: hematogenous tumors and solid tumors
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12
Q

Allopurinol

A
  • reduces hyperuricemia and crystalluria associated with massive cell death and purine release
  • helps with classical toxicity from drugs
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13
Q

MOPP and COP

A

M-mechlorethamine, O-Oncovin(vincristine), procarbizine, prednisone
C-cyclophosphamide, Oncovin, prednisone

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14
Q

Cisplatin - platinum analogs

A
  • bind directly to DNA
  • crosslinkers, only cis is active, fixed positive charge
  • exchange Cl group for electrons in O,N,P, and DNA
  • strongly bind tissue, eliminated unchanged in urine
  • causes:nephrotoxicity,N,V,neuropathy,ototoxicity
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15
Q

Actinomycin D - antibiotics

A
  • bind directly to DNA
  • generates free radicals to tear DNA apart, specific bind deoxyguanine
  • IV, multiple half lives, excreted unchanged in urine and bile
  • causes: classical toxicity
  • use: carcinomas, Wilm’s tumor, Kaposi’s sarcoma, curative in testicular
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16
Q

Adriamycin (Doxorubicin) - antibiotics

A
  • bind directly to DNA
  • intercalated quionone redox center binds Fe2+ oxidizes to Fe3+
  • passes electron to oxygen to make free radicals
  • IV,wide distribution except CNS,metabolized by liver,excreted in bile
  • classic toxicity and cardiotoxicity, free radicals have no buffer in heart
  • solid and hematogenous tumors
  • Idarubicin and epirubicin
17
Q

Bleomycin - antibiotics

A
  • glycopeptides intercalate and make free radicals by binding iron
  • NO bone marrow suppression
  • cause: skin lesions,hyperpigmentation,pulmonary fibrosis
  • IV or IM
  • use: lymphoma,germ cell cancers, head and neck cancer
  • caution when giving to smokers
18
Q

Etoposide (Teniposide) - topoisomerase inhibitors

A
  • bind directly to DNA/topoisomerase II
  • cause dsDNA breaks
  • renal elimination, some hepatic and biliary excretion
  • use: lymphomas, lung, gastric cancer
  • cause:N,V,bone marrow suppression, hepatic toxicity,increased leukemia
  • resistance occurs by MDR1 gene, ABC transporter P170 pumps drug out
19
Q

Methotrexate - antimetabolites

A
  • do not directly bind DNA
  • depletes folic acid, unable to make dTMP from dUMP
  • DNA synthesis fails and causes apoptosis
  • excreted unchanged in urine, NSAIDs compete/ reduce polyglutamation
  • classic toxicity, hepatotoxicity, nephrotoxicity
  • use: choriocarcinoma,lymphoma,sarcoma,leukemia
20
Q

6-Mercaptopurine - purine analog

A
  • phosphorylated via salvage pathway
  • inhibits enzymes for ATP/GTP synthesis, disturb DNA structure
  • metabolized by xanthine oxidase/thiopurine methyltransferase
  • unchanged in urine
  • classic toxicity, hepatotoxicity, must decrease allopurinol dose
  • use: childhood cancers, leukemia, lymphoma, Hodgkins
21
Q

5-Fluorouracil - pyramidine analogs

A
  • phosphorylated via salvage pathway to 5FdUMP
  • parental, hepatic metabolism by DPD, genotyping to prevent toxicity
  • classical toxicity, ataxia, GI, skin
  • capacitabine is prodrug
22
Q

Vinblastine, Vincristine - mitotic spindle inhibitors

A
  • bind tubulin to disaggregate mitotic spindles - mitotic arrest
  • widely followed by CCS agents
  • IV, distribute widely except CNS
  • metabolized by CYP3A4
  • use: lymphoma, sarcoma, solid tumors
  • cause: myelosuppression, peripheral neuropathy
23
Q

Paclitaxel (Taxol) - mitotic spindle inhibitor

A
  • mitotic arrest by binding tubulin, stabilizes microtubules
  • metabolized by CYP3A4, resistance from MDR1 gene
  • use: breast, ovarian, head/neck, lung, bladder, prostate, melanoma
  • cause:myelosuppression, peripheral neuropathy,cardiac block, arrhythmia
24
Q

Docetaxel

A
  • mitotic spindle inhibitors

- NSCLC, breast, head/neck,gastric,prostate

25
Q

Leuprolide - GnRH Agonist

A
  • chronic treatment causes decrease in GnRH receptor

- causes decrease in LH and FSH, decrease in androgen/estrogen at first

26
Q

Degarelix/Cetrorelix - GnRH antagonist

A
  • cause decrease in LH and FSH

- decrease in androgens and estrogen, no surge

27
Q

Estradiol/ tamoxifen

A

Estrogen agonist/antagonist

28
Q

Danazol/flatamide

A

-androgen agonist/antagonist

29
Q

Vorozole, Letrozole - aromatase inhibitors

A
  • better ER(+) tumor shrinkage, better relapse prevention

- used for premenopausal women with ovarian suppression

30
Q

Retinoic Acid

A
  • APL associated w/ t(15,17) and broken RAR-alpha
  • effective treatment with increase levels of RA
  • increase RA: stimulate broken RAR by releasing corepressors from receptor
31
Q

Cytotoxic drugs that interfere with DNA replication by cross linking DNA strands and DNA strand breaking are classified as _______________.

A

Alkylating agents

-Mechlorethamine and Cyclophosphamide

Drugs/Immuno (9 decks)

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