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Fundamentals of Pathological Processes > FPP-Drugs > Flashcards

FPP-Drugs Flashcards

1
Q

Alkylating Agents

A

Introduce alkyl groups into DNA, causes crosslinks and strand breaks
cell-cycle non-specific:
Mechlorethamine, Carmustine
cycle specific, phase non-specific:
Cyclophosphamide
Sides: bone marrow suppression, GI effects, alopecia

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2
Q

Mechlorethamine

A

Alkylating agent
cell-cycle non-specific
limited use today, highly reactive
Lymphomas

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3
Q

Cyclophosphamide

A

Alkylating agent
Prodrug, activated by P450s
cycle-specific, phase non-specific, oral, poor CNS
side product-> bladder toxicity (treated w Mesna)
broad spectrum, wide uses

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4
Q

Carmustine

A

Alkylating agent
cycle non-specific
crosses blood brain barrier
used for brain tumors, multiple myeloma, melanoma

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5
Q

Antimetabolites

A

Most effective in rapidly proliferative
S-phase specific
Analogs of compounds for nucleic acid biosynthesis
Mercaptopurine, Methotrexate, Hydroxyurea, Fluorouracil, Cytarabine

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6
Q

Methotrexate

A

Folate analog
Binds DHFR and prevents FH4 synthesis
sides: GI epithelial damage, bone marrow suppression, renal tubular necrosis, displaces other albumin-bound drugs
Acute lymphocytic leukemia (ALL), Choriocarcinoma (can cure)

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7
Q

Leucovorin

A

folate rescue

with high-dose Methotrexate, this can be used to rescue normal cells

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8
Q

Fluorouracil

A

5-FU
Inhibits RNA synthesis and DNA synthesis via thymidylate synthase
Sides: nausea, anorexia, diarrrhea, myelosuppression
Uses: GI cancers (1st), colon, breast, basal cell carcinoma

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9
Q

Cytarabine

A

Pyrimidine (cytidine) analog competes for phosphorylation
causes DNA chain termination
Sides: myelosuppression, neurotoxicity
Phase-specific dose kinetics (continuous infusion)
Acute leukemias

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10
Q

Mercaptopurine

A

purine analog, inhibits RNA and DNA synthesis
Sides: bone marrow supp, vomiting, nausea, anorexia, Jaundice
Acute leukemias
TPMT polymorphisms in some pts need to adjust dose or not use

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11
Q

Hydroxyurea

A

Inhibits ribonucleotide reductase, blocks DNA synthesis
arrests cells at G1-S
Uses: granulocytic leukemia
Sides: hematopoietic depression, GI issues

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12
Q

Vinca Alkaloids

A

Bind tubulin, inhibits microtubule and mitotic spindle assembly
Vincristine, Vinblastine

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13
Q

Vinblastine

A

Vinca Alkaloid
Sides: strongly myelosuppressive, epithelial ulcerations
Use: lymphomas, breast cancer

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14
Q

Vincristine

A

Vinca Alkaloid
Sides: less bone marrow supp, alopecia, neuromuscular abnormalities, peripheral neuropathy
Use: acute lymphocytic leukemia, lymphomas, Wilm’s tumor, neuroblastoma, etc

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15
Q

Taxanes

A

Enhances assembly and stability of microtubules, binds tubulin
Arrests in G2-M (radiosensitizer)
Paclitaxel

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16
Q

Paclitaxel

A

Taxane
use: refractory ovarian cancer, breast cancer
Sides: leukopenia, peripheral neuropathy, myalgia

17
Q

Doxorubicin

A

Intercalates in DNA, distorts, causes lipid preoxidation and free radicals, binds DNA+topoisomerase II
cycle-specific, phase non-specific
among most active anti-tumor
wide spectrum, lymphomas, breast, ovary, small cell lung
also anti-angiogenic
sides: cardiomyopathy, bone marrow supp, alopecia, GI effects

18
Q

Bleomycin

A

iron-containing glycopeptides bind to DNA, causes oxidative damage, strand breaks
Needs chelated Fe
G2-phase specific
germ cell tumors, head, neck, lung, lymphomas
sides: minimal myelosupp, pulmonary toxicity, skin vesiculation/hyperpigment

19
Q

Etoposide

A

Stabilizes DNA-topoisomerate II
Arrests G2-M interface
use: lymphomas, acute leukemia, small cell lung, testis
sides: leukopenia, nausea, vomiting, diarrhea, alopecia

20
Q

Filgrastim

A

Granulocyte colony stimulating factor
limits chemo-induced neutropenia
sides: bone pain

21
Q

Trastuzumab

A

HER2 receptor antibody

use: breast cancer that ovexpresses HER2
sides: cardiomyopathy (reversible), hypersensitivity, infusion rxn

22
Q

Cisplatin

A

Platinum coordination complex
actived to cause DNA crosslinks
cell-cycle-specific, phase non-specific
testicular cancer, ovarian, head, neck, bladder, small cell lung, esophagus, etc
sides: nephrotoxicity, ototoxicity, peripheral neuropathy, electrolyte probs, nausea, myelosupp

23
Q

Procarbazine

A

Activated by liver to methylating agent, causes chromosomal damage
atypical alkylating agent
Hodgkin’s Lymphoma
sides: myelosupp, nausea, vomiting

24
Q

Prednisone

A 
Binds steroid receptors
arrests in G1
depress growth-related genes
induces nucleases-> cell-lysis
lymphoma, leukemia, breast cancer
also anti-emetic and anti-inflammatory, immunosuppressive, weight gain, fluid retiention, psychological
25
Q

Tamoxifen

A

non-steroidal anti-estrogen receptor in breast tissue
cytostatic (tumor regrows when removed)
use: post-menopausal breast cancer, pre-menopausal metastatic breast CA, breast CA prohylaxis
Activated by CYP2D6
sides: nausea, hot flashes, fatigue, bone pain

26
Q

Letrozole

A

blocks conversion of androgens to estrogens by inhibiting aromatase (CYP19)
1st line for post-menopausal or metastatic breast CA
Better effects than Tamoxifen, sides similar

27
Q

Leuprolide

A

GnRH analog
after initial surge, decreases LH/FSH, which decreases testosterone
use: prostate CA
sides: hot flashes, impotence

28
Q

Flutamide

A

non-steroidal anti-androgen, blocks androgen receptors

use: metastatic prostate CA
sides: gynecomastia, diarrhea, hepatotoxicity

29
Q

Multi-drug resistance (MDR)

A

ATP-dependent drug efflux pumps (P-glycoprotein, MRP)

Vincristine, Vinblastine, Doxorubicin, Bleomycin, Etoposide, Paclitaxel

30
Q

Natural Products

A

Vinblastine, Vincristine, Paclitaxel

31
Q

Anti-tumor Antibiotics

A

Doxorubicin, Bleomycin, Etoposide

32
Q

Misc Agents

A

Cisplatin, Procarbazine

33
Q

Biological response modifiers

A

Filgrastin, Trastuzumab

34
Q

Hormones and Antagonists

A

Prednisone, Tamoxifen, Letrozole, Leuprolide, Flutamide

Fundamentals of Pathological Processes (3 decks)

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