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HDT 3.2 > Chemotherapy Drugs > Flashcards

Chemotherapy Drugs Flashcards

1
Q

Name the 4 types of antimetabolite drugs?

A

a) Folate Antagonist
b) Pyrimidine analogues
c) Purine analogues
d) Ribonucleotide reductase inhibitors

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2
Q

How do antimetabolites work?

A

Structurally similar to naturally occurring metabolites involved in nucleic synthesis.

Similar to DNA and RNA bases.

Cell mistakes for normal metabolite so
- inhibition of enzymes involved in nucleic acid synthesis -Incorporation into nucleic acid leading to incorrect codes

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3
Q

How do Folate antagonists work?

A

Folates essentials for synthesis of purines

Folates exist as polyglutamates –> reduced to dihydrofolate –> tetrahydrofolate which important for purine synthesis

Reduction enzymes: thymidylate (TS), dihydrofolate reductase (DHFR) & glycinamide ribonucleotide transformylase (GARFT) responsible for this transformation

FA inhibit these enzymes.

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4
Q

Name some Folate Antagonists

A

MTX
Pemetrexed
Raltitrexed

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5
Q

What are Pyrimidine Analogues

A

Act as fraudulent nucleotides - structurally similar to cytosine, thymine and uracil. Interacts with thymidylate synthetase & folate co-factors –> incoorporation into DNA and RNA. Disrupts DNA synthesis, aa codes incorrect

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6
Q

Name some Pyrimidine Analogues

A 
5- Flourouracil
Capecitabine
Gemcitabine
Gytarabine 
Azacitidine
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7
Q

Name some purine analogues

A

6-Mercaptopurine

Fludrabine

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8
Q

What are purine analogues

A

Fraudulent nucleotides. Incorporated into growing DNA chain, in place of adenine and guanine. Inhibits enzymes involved in purine synthesis.

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9
Q

Name the Ribonucleotide reductase inhibitors

A

Hydroxycarbamide

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10
Q

How do Ribonucleotide reductase inhibitors work?

A

Inhibitor of ribonucleotide reductase - enzyme essential for generation of deoxyribonucleotides

Prevents manufacture of purines and pyrimidines –> decreased cellular levels of DNA

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11
Q

How do Alkylating agents and Nitrosureas work?

A

ovalently link an alkyl group (R-CH2) to chemical moieties in nucleic acids and proteins

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12
Q

What are some Alkylating agents and Nitrosureas?

A

a) Nitrogen Mustards
b) Alkyl Sulfonates
c) Triazines
d) Nitrosoureas
e) Metal salts

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13
Q

What are some Nitrogen Mustards?

A

Melphalan

Mechlorethamine (Mustine)

Cyclophosphamide

Bendamustine

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14
Q

What is the name of the Alkyl Sulfonates?

A

Busulfan

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15
Q

What are the names of the Triazines?

A

Decarbazine

Temozolomide -

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16
Q

What are the names of Nitrosoureas?

A

BCNU - Carmustine

CCNU - Lomustine

17
Q

What are the names of the metal salts?

A

Cisplatin, Carboplatin and Oxaliplatin

18
Q

How do metal salts work?

A

inhibit DNA synthesis through intra and inter-strand cross links.

19
Q

What are the Natural Products drugs?

A

Vinca Alkyloids

Taxanes

(Mitotic inhibitors)

20
Q

How do Vinca Alkyloids work?

A

Prevent construction of microtubules

21
Q

How do Taxanes work?

A

allow tubulin to be built up in microtubules but inhibit breakdown of microtubules back into tubulin

22
Q

What are the names of some vinca alkyloids?

A 
Vincristine
Vinblistine
Vindesine
Vinorelbine
Brentuximab vedotin
DM1/Emtansine
Kadcyla
23
Q

What are some names of the Taxanes?

A

Paclitaxel

Docetaxel

Abraxane

Cabazitaxel

Eribulin

Trabectedin

24
Q

What are the different types of antitumour antibiotics?

A

Major class: anthracyclines:

Doxorubicin, daunorubicin, idarubicin, epirubicin

Mixantrone

Antinomycin D

Mutomycin C

Bleomycin

25
Q

How do anthracyclines work?

A

Inhibit topoisomerase II

  • DNA intercalation
  • Free radical formation - alkylation
26
Q

How does Mutomycin C work?

A

Cross linking between complementary DNA strands inhibits replication.

27
Q

How does Bleomycin work?

A

DNA strand scisson - fragmentation of DNA

28
Q

How do Topoisomerase Inhibitors work?

A

Nuclear enzymes that cause DNA strand breaks and therefore allow it to unwind during cell division.

29
Q

How do Topoisomerase I work?

A

causes single nick in DNA

30
Q

How does Topoisomerase II work?

A

cleaves both strands

31
Q

what are the examples of Topoisomerase I inhibitors?

A

Topotecan

Irinotecan

32
Q

what are the examples of Topoisomerase II inhibitors?

A

Etoposide

Teniposide

HDT 3.2 (10 decks)

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