Chemotherapy Drugs Flashcards
Name the 4 types of antimetabolite drugs?
a) Folate Antagonist
b) Pyrimidine analogues
c) Purine analogues
d) Ribonucleotide reductase inhibitors
How do antimetabolites work?
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
How do Folate antagonists work?
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.
Name some Folate Antagonists
MTX
Pemetrexed
Raltitrexed
What are Pyrimidine Analogues
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
Name some Pyrimidine Analogues
5- Flourouracil Capecitabine Gemcitabine Gytarabine Azacitidine
Name some purine analogues
6-Mercaptopurine
Fludrabine
What are purine analogues
Fraudulent nucleotides. Incorporated into growing DNA chain, in place of adenine and guanine. Inhibits enzymes involved in purine synthesis.
Name the Ribonucleotide reductase inhibitors
Hydroxycarbamide
How do Ribonucleotide reductase inhibitors work?
Inhibitor of ribonucleotide reductase - enzyme essential for generation of deoxyribonucleotides
Prevents manufacture of purines and pyrimidines –> decreased cellular levels of DNA
How do Alkylating agents and Nitrosureas work?
ovalently link an alkyl group (R-CH2) to chemical moieties in nucleic acids and proteins
What are some Alkylating agents and Nitrosureas?
a) Nitrogen Mustards
b) Alkyl Sulfonates
c) Triazines
d) Nitrosoureas
e) Metal salts
What are some Nitrogen Mustards?
Melphalan
Mechlorethamine (Mustine)
Cyclophosphamide
Bendamustine
What is the name of the Alkyl Sulfonates?
Busulfan
What are the names of the Triazines?
Decarbazine
Temozolomide -
What are the names of Nitrosoureas?
BCNU - Carmustine
CCNU - Lomustine
What are the names of the metal salts?
Cisplatin, Carboplatin and Oxaliplatin
How do metal salts work?
inhibit DNA synthesis through intra and inter-strand cross links.
What are the Natural Products drugs?
Vinca Alkyloids
Taxanes
(Mitotic inhibitors)
How do Vinca Alkyloids work?
Prevent construction of microtubules
How do Taxanes work?
allow tubulin to be built up in microtubules but inhibit breakdown of microtubules back into tubulin
What are the names of some vinca alkyloids?
Vincristine Vinblistine Vindesine Vinorelbine Brentuximab vedotin DM1/Emtansine Kadcyla
What are some names of the Taxanes?
Paclitaxel
Docetaxel
Abraxane
Cabazitaxel
Eribulin
Trabectedin
What are the different types of antitumour antibiotics?
Major class: anthracyclines:
Doxorubicin, daunorubicin, idarubicin, epirubicin
Mixantrone
Antinomycin D
Mutomycin C
Bleomycin
