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HDT - Pharm > Antineoplastic Drugs > Flashcards

Antineoplastic Drugs Flashcards

1
Q

Cyclophosphamide toxicity

A

Cardiotoxicity
hemorrhagic cystitis - bladder burn
Hematuria

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2
Q

Sodium 2-mercaptoethane sulfonate role is to

A

MESNA’s role is to detoxify acrolein which is causes toxicity like (hemorrhagic cystitis + hematuria)

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3
Q

Alkylating Agents MOA

A

alkylating DNA guanine = cross-linking stands –> apoptosis

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4
Q

Platinum complexes MOA

A

covalent cross-linking of G-C base pairs = bend DNA

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5
Q

Cisplatin toxicity

A 
Renal damage = reduced with hydration
Ototoxicity
Hearing loss 
Tinnitus 
Peripheral Sensory Neuropathy
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6
Q

Antimetabolites MOA

A

Block DNA formation –> abnormal DNA
Cell cycle dependent
Inhibits protein synthesis

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7
Q

Methotrexate MOA

A

competitive inhibitor of dihydrofolate reductase
blocks dTMP
stops folate-dependent enzymes of de novo purine & thymidylate synthesis

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8
Q

Methotrexate toxicity

A

nephrotoxicity
hepatic necrosis
bone marrow depression

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9
Q

What can reduce Methotrexate toxicity?

A

Leucovorin by reducing folate (5-formylretrahydrofolate)

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10
Q

Fluorouracil MOA

A

STOP DNA synthesis
converted to the fraudulent F-dUMP
F-dUMP forms a covalent complex with thymidylate synthase & methylene tetrahydrofolate (THF)

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11
Q

what impacts 5-FU levels

A

DPYD/DPD

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12
Q

Fluorouracil toxicity

A

severe ulceration of oral & GI mucosa + diarrhea

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13
Q

Leucovorin Calcium MOA

A

its folinic acid which binds & stabilizes ternary complex of 5-fdUTP & thymidylate synthase = increases fluorouracil cytotoxicity

decreases the effects of methotrexate

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14
Q

Leucovorin Calcium toxicity

A

diarrhea when given with fluorouracil

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15
Q

6-Mercaptopurine MOA

A 
blocks purine (guanine) synthesis 
Triphosphate form incorporated into DNA --> strand breaks
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16
Q

6-Mercaptopurine toxicity

A

bone marrow depression

Xanthine oxidase inhibitors (Allopurinol) = increases effects

17
Q

Xanthine oxidase & TPMT (thiopurine methyltransferase) role is to

A

metabolize 6-Mercaptopurine in the liver

18
Q

Tumor cell lysis Syndrome is treated with

A

Allopurinol

19
Q

Mutations in TPMT =

A

drug accumulation + bone marrow destruction (infection)

20
Q

What is needed for 6-mercaptopurine activation

A

HGPRT = hypoxanthine guanine phsophoribosyl transferase

21
Q

Cytarabine (Pyrimidine Analog) MOA

A

inhibits DNA chain elongation + base rotation

Inhibits DNA polymerase

22
Q

Asparaginase MOA

A

Hydrolyze asparagine to aspartic acid & ammonia

23
Q

Asparaginase toxicity

A

risk of anaphylaxis

24
Q

Microtubule Inhibitors + MOA

A

Taxanes

  • Paclitaxel (Paclitaxel)
  • Docetaxel (Taxotere)

Arrest in Metaphase = blocks cell in mitosis

25
Q

Taxanes toxicity =

A

bone marrow toxicity

peripheral sensory neuropathy (dose limiting)

26
Q

Vinca Alkaloids

A

bind to b-tubulin & blocks polyermization with a-tubulin in the microtubules

27
Q

Anthracycline Antibiotics

A

inhibits resealing of DNA nicks by blocking Topoisomerase 2

28
Q

Anthracycline Antibiotics + Doxorubicin MOA

A

inhibits resealing of DNA nicks by blocking Topoisomerase 2

29
Q

Anthracycline Antibiotics + Doxorubicin Toxicity

A

Acute cardiac = arrhythmias (ST&T waves)

chronic cardiac = (cardiomyopathy –> CHF)

30
Q

Doxorubicin MOA for toxicity

A

free radical damage = generation of Hydroxyl radicals from peroxide

31
Q

that is the role of Dexrazoxane

A

to protect from cardiotoxicity

32
Q

Irinotecan MOA + Toxicity + Usages

A

Blocks Topoisomerase 1 = ssDNA break occurring
Severe GI toxicity + 1A1 & 28 polymorphism
Colon cancer

33
Q

Blemycin MOA + Toxicity

A

OH- radicals = DNA fragmentation

No significant bone marrow toxicity but some pulmonary fibrosis

34
Q

First-line drugs for tx of breast cancer in POSTmenopausal women

A

Anastrozole & Letrozole by being competitive nonsteroidal aromatase inhibitors

35
Q

Exemestane is a

A

STEROIDAL IRREVERSIBLE inhibitor of aromatase

36
Q

Trastuzumab MOA + toxicity

A

HER2 receptors

weakening heart muscles + CHF

HDT - Pharm (7 decks)

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