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2021 Origins > Chemodrugs > Flashcards

Chemodrugs Flashcards

1
Q

What is the mechanism of action of Carboplatin/Cisplatin?

A

Cross-links DNA

Adverse effects: Nephrotoxicity, peripheral neuropathy, ototoxicity.

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2
Q

What is the mechanism of action of Oxaliplatin?

A 
Forms intrastrand
and interstrand
DNA cross-links;
binding to nuclear
and cytoplasmic
proteins
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3
Q

What is the mechanism of action of Dacarbazine?

A

Methylates DNA
and inhibits DNA
synthesis and
function

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4
Q

What is the mechanism of action of Cyclophosphamide?

A

Forms DNA crosslinks at guanine
resulting in
inhibition of DNA
synthesis and

Adverse effects: Myelosuppression; SIADH; hemorrhagic cystitis,
function

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5
Q

What is the mechanism of action of 5-Fluorouracil?

A

Inhibits TS = inhibition of DNA synthesis and function. Pyrimidine analog bioactivated to 5-FdUMP, which covalently complexes with thymidylate synthase and folic acid.

Adverse effects: Myelosuppression, palmar- plantar erythrodysesthesia (hand-foot syndrome).

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6
Q

What is the mechanism of action of Methotrexate?

A

Inhibits DHFR; inhibits TS; inhibits de novo
purine nucleotide synthesis. Decreases dTMP and DNA synthesis

Adverse effects: Myelosuppression, Hepatotoxicity.
Mucositis (eg, mouth ulcers). Pulmonary fibrosis.
Folate deficiency, which
may be teratogenic (neural tube defects) without supplementation.
Nephrotoxicity (rare).

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7
Q

What is the mechanism of action of Cytarabine?

A

Inhibits DNA chain elongation

Adverse effects: Myelosuppression with megaloblastic anemia. CYTarabine causes panCYTopenia.

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8
Q

What is the mechanism of action of Vincristine?

A

Inhibits mitosis via microtubules. prevent mitotic spindle formation (M-phase arrest).

Adverse effects: neurotoxicity (areflexia, peripheral neuritis), constipation (including paralytic ileus). Crisps the nerves.

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9
Q

What is the mechanism of action of Bleomycin?

A

Oxygen free radicals bind
to DNA causing single- and
double-strand DNA breaks

Adverse effects: Cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia.

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10
Q

What is the mechanism of action of Doxorubicin?

A

Generate free radicals. Intercalate in DNA = breaks in DNA = decrease in replication

Interferes with topoisomerase II enzyme.

Adverse effects: Cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia.

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11
Q

What is the mechanism of action of Etoposide?

A

Inhibits topoisomerase II = increase DNA degradation

Adverse effects: Myelosuppression, alopecia

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12
Q

What is the mechanism of action of Irinotecan/topotecan

A

Inhibits topoisomerase I

Adverse effects: Severe myelosuppression, diarrhea.

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13
Q

What is the mechanism of action of Mitomycin?

A

Acts as an alkylating agent and forms cross-links with DNA; formation
of oxygen free radicals,
which target DNA

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14
Q

What is the mechanism of action of Paclitaxel?

A

Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur).

Myelosuppression, neuropathy, hypersensitivity.
Taxes stabilize society.

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15
Q

What is the mechanism of action of Erlotinib?

A

Inhibits EGFR tyrosine kinase leading to inhibition of EGFR signaling

Adverse effects: Rash

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16
Q

What is the mechanism of action of Imatinib?

A

Tyrosine kinase inhibitor of BCR-ABL (Philadelphia chromosome fusion gene in CML).

Adverse: Fluid retention.

17
Q

What is the mechanism of action of Cetuximab?

A

Monoclonal antibody against EGFR.

Adverse effects: Rash, elevated LFTs, diarrhea.

18
Q

What is the mechanism of action of Bevacizumab?

A

Monoclonal antibody against VEGF. Inhibits angiogenesis (BeVacizumab inhibits Blood Vessel formation).

Adverse effects: Hemorrhage, blood clots, and impaired wound healing

19
Q

What is the mechanism of action of Sorafenib?

A

Inhibits multiple RTKs, including raf kinase, VEGF-R2, VEGF-R3, and PDGFR-β leading to inhibition of angiogenesis, invasion, and metastasis

20
Q

What is mechanism of action of hydroxyurea?

A

Inhibits ribonucleotide reductase = decrease DNA synthesis (s-phase)

Adverse effects: myelosuppression

2021 Origins (7 decks)

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