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Fpp > Chemo Drugs > Flashcards

Chemo Drugs Flashcards

1
Q

Alkylating agents

A
  • nitrogen mustards –> Mechlorethamine, Cyclophosphamide

- nitrosureas –> Carmustine

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2
Q

Mechlorethamine

A

MECH: induce alkyl groups in dna; causes dna crosslinks and strand breaks

Cell cycle non specific

USE: Hodgkin’s lymphoma

TOX: hematopoiesis suppression; damage to intestinal mucosa; nausea, vom

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3
Q

Cyclophosphamide

A

MECH: induce alkyl groups in dna; cause dna crosslinks and strand breaks; ACTIVATED IN LIVER by cytoP450

Cycle specific/phase nonspecific

USE: v broad spectrum–> hodgin’s lymphoma, non hodgkins lymphoma, multiple myeloma, neuroblastoma, leukemia, carcinoma of endometrium/breast/lung

TOX: hematopoiesis suppression; damage to intestinal mucosa; nausea, vom; STERILE HEMORRAGIC CYSTITIS

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4
Q

Carmustine

A

MECH: induce alkyl groups into dna; cause dna crosslinks, strand breaks; HIGHLY LIPOPHILIC - CROSSES BBB

Cell cycle non specific

USE: BRAIN tumors; multiple myeloma; melanoma

TOX: hematopoiesis suppression; damage to intestinal mucosa; nausea, vom

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5
Q

Antimetabolites

A
  • folate analogs: Methotrexate
  • pyrimidine analogs: Fluorouracil, Cytarabine
  • purine analogs: Mercaptopurine, Hydroxyurea
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6
Q

Methotrexate

A

MECH: binds dihydrofolate reductase; prevents formation of THF

S phase specific

USE: acute lymphocytic leukemia; choriocarcinoma

TOX: intestinal epithelium; bone marrow suppression; renal tubular necrosis

**REQ rescue of host cells w/ LEUCOVORIN

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7
Q

Fluorouracil

A

MECH: activated in cells to FUTP to inhib rna syn and FdUMP to interfere w/ thymidylate synthetase and dna syn

S phase specific

USE: carcinoma of stomach, colon, pancreas, ovary, head and neck, breast, bladder; topical cream for basal cell carcinomas

TOX: nausea; anorexia; diarrhea; myelosuppression

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8
Q

Cytarabine

A

MECH: cytidine analog; competes w/cytidine for all 3 phosphorylation steps to dCTP; cytarabine tri phosphate competes w/ dCTP for incorporation into dna –> dna chain termination

S phase specific

USE: acute leukemias

TOX: myelosuppression; neurotox

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9
Q

Mercaptopurine

A

MECH: purine analog; converted in cells to ribonucleotide –> inhib rna and dna syn

S phase specific

USE: acute leukemias

TOX: bone marrow depression; vomiting, nausea; anorexia; jaundice

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10
Q

Hydroxyurea

A

MECH: inhib ribonucleotide reductase –> blocks dna syn

S phase specific (arrest at G1-S interface)

USE: chronic granulocytic leukemia; head and neck cancer

TOX: hematopoietic depression; GI disturbances

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11
Q

Natural Products

A
  • vinca alkaloids –> vinblastine, vincristine

- taxanes –> paclitaxel

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12
Q

Vinblastine

A

MECH: binds to tubulin –> inhib proper formation of microtubules and mitotic spindle

M phase specificity

USE: Hodgkins, non hodgkins; breast cancer

TOX: STRONGLY myelosuppressive; epithelial ulcerations

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13
Q

Vincristine

A

MECH: binds to tubulin –> inhib proper formation of microtubules and mitotic spindles

M phase specificity

USE: acute lymphocytic leukemia; Hodgkins and non hodgkins lymphoma; Wilm’s tumor; neuroblastoma; rhabdomyosarcoma

TOX: alopecia; neuromusc abnorm (incl peripheral neuropathy); significantly LESS bone marrow suppression

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14
Q

Paclitaxel

A

MECH: enhances assembly and stability of microtubules by binding to beta subunit of tubulin

Late in G2 phase

USE: refractory ovarian cancer; breast cancer

TOX: dose limiting leukopenia; peripheral neuropathy; myalgia/arthralgia

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15
Q

Antitumor antibiotics

A

Doxorubicin

Belomycin

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16
Q

Doxorubicin

A

MECH: intercalates btwn dna base pairs –> distorting dna helix; causes lipid peroxidation and free radical gen; binds to dna and Topo II

Cycle specific/phase nonspecific

USE: Hodgkins and non hodgkins lymphoma; breast, ovary, small cell lung cancers

TOX: dialated CARDIOMYOPATHY; bone marrow depression; alopecia; GI disturbances

17
Q

Bleomycin

A

MECH: glycopeptides that bind dna –> oxidative like damage to dna = dna strands break

Phase specific for G2

USE: germ cell tumors of testes and ovaries; head, neck, lung lymphomas

TOX: DOSE REL PULMONARY TOX; vesiculation of skin; hyperpigmentation; MINIMAL myelosuppression/immunosuppression

18
Q

Etoposide

A

MECH: stabilizes dna topo II complexes –> double strand dna breaks

Late G2 phase

USE: lymphomas; acute nonlymphocytic leukemia; small cell carcinoma of the lung; testicular cancer

TOX: leukopenia; nausea vom; diarrhea; alopecia

19
Q

Filgrastim (G-CSF)

A

MECH: stim granulocyte (neutrophil) prod by the marrow

USE: given post myelosuppressive agents to speed neutrophil recovery

TOX: bone pain

20
Q

Trastuzumab

A

MECH: monoclonal Ab that binds to HER2 receptor

USE: breast cancers that OVEREXPRESS HER2

TOX: CARDIOMYOPATHY; hypersensitivity; infusion rxn: fever, chills

21
Q

Cisplatin

A

MECH: platinum coordination complex; hyrolation –> activated species = dna crosslinks

Cycle specific/ phase non specific

USE: WIDE ANTITUMOR SPECTRUM: testes, ovary, head, neck, bladder, colon, esophagus, small cell lung

TOX: NEPHRO, OTO, peripheral neuropathy, electrolyte disturbance; nausea, vom; mild to mod myelosuppression

22
Q

Procarbazine

A

MECH: activated in vivo to a methylating agent –> chromosomal damage

G1 and S phase

USE: Hodgkin’s lymphoma

TOX: myelosuppression; nausea, vom

23
Q

Prednisone

A

MECH: bind to steroid receptors; depresses rna syn of many growth related genes; induces nucleases which may mod cell lysis

Arrest cells at G1

USE: anti emetic effect; pallative therapy; acute and chronic lymphocytic leukemia; Hodgkin’s dz, non Hodgkin’s lymphoma; breast cancer

TOX: limited myelosuppression

24
Q

Tamoxifen

A

MECH: antiestrogen that blocks estrogen receptors; activated by CYP2D6 (**less effective if CYP2D6 is inhibited)

USE: POST MENOPAUSAL breast cancer; breast cancer PROPHYLAXIS in women at high risk

TOX: hot flashes; fatigue; nausea; bone and other musculoskeletal pain

25
Q

Letrozole

A

MECH: aromatase inhib; inhib conversion androgens to estrogens in all tissues

USE: post menopausal breast cancer

TOX: bone pain and other musculoskeletal pain; hot flashes; nausea; fatigue

26
Q

Leuprolide

A

MECH: analog of gonadotropin releasing hormone; after 2-4 wks it desensitizes GnRH signaling, inhibiting LH/FSH secretion thus decreasing testosterone syn to castration levels

USE: advanced hormonally responsive prostate cancer

TOX: hot flashes; impotence

27
Q

Flutamide

A

MECH: anti androgen that blocks androgen receptors

USE: metastatic prostate cancer

TOX: gynecomastia; diarrhea; hepatotoxicity

28
Q

Sequential blockade

A

-simultaneous ax of two inhibitors acting on different enzymes of a linear metabolic pathway

  • hydroxyurea + cytarabine
  • methotrexate + 5FU
29
Q

Concurrent inhibition

A

-inhibitors block 2 separate pathways that lead to the same end product

30
Q

Complementary inhibition

A

-one of the inhibitors affects the function of an end product, the other inhibitor affects the syn of (or use of precursors leading to the formation of) that end product

Cytarabine + doxorubicin

C - inhib dna syn

D - causes dna strand breaks

31
Q

Rescue

A

Rescue pt’s normal cells from the tx

Leucovorin to rescue cells post methotrexate exposure

32
Q

Synchronization

A

Tumor cells synchronized so they are in one phase and then use agent that is specific for that phase

33
Q

Recruitment

A

Mobilization of slowly proliferating or non proliferating cells to more rapid proliferation

-initiate therapy w/ cell cycle non specific drugs (mechlorethamine or carmustine) in order to reduce tuomr buld and slowly recruit non dividing cells into active dna syn; follow w/ cell cycle specific agents

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