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PHA401, Classification cancer drugs by Dr Omokhafe
PHA401, Classification cancer drugs by Dr Omokhafe
1. Alkylating agents
Mechanism of action: They transfer alkyl groups to cellular constituents, especially DNA within
the nucleus leading to cell death.
Examples: cyclophosphamide, chlorambucil, mephalan, busulfan
2. Antimetabolites
(a) Methotrexate: it binds to dihydrofolate reductase and inhibits the synthesis of
tetrahydrofolate and ultimately the synthesis of purine nucleotides.
(b) 5-fluorouracil
It inhibits the synthesis of thymidilate leading to inhibiton of synthesis of DNA.
Other examples of antimetabolites include cytarabine, fludarabine and 6-mercaptopurine.
3. Natural products
(a) Vinca alkaloids e.g. vincristine and vinblastine. They inhibit the process of tubulin
polymerisation and disrupt the assembly of microtubules involved in mitotic spindle apparatus.
(c) Epipodophyltoxin e.g. etoposide: it inhibits topoisomerase II thereby inhibiting DNA synthesis
and function
(d) Campothecins e.g. topotecan and irinotecan. They inhibit topoisomerase I thereby causing
DNA damage.
4. Anticancer antibiotics
(a) anthracyclines e.g. doxorubicin and daunorubicin, epirubicin: They inhibit topoisomerase II.
They block the synthesis of DNA and RNA.
(b) Mitomycin: It generates an alkylating agent that cross links DNA
(c) Bleomycin: It binds to DNA resulting in DNA breakage.
2. Antimuscarinic drugs
They block the bronchoconstrictor effects of acetylcholine. They are effective as bronchodilators.
Examples are ipratopium and tiotropium
3. They inhibit the production of inflammatory cytokines, reduce bronchial hyperreactivity and
redu the frequency of asthma attacks. Examples include beclomethasone and budesonide.
5. Inhibitors of leukotriene synthesis e.g. zileuton and leukotriene receptor antagonists e.g.
zafirlukast and montelukast.
Antitussives
1. Codeine: It suppresses the cough center in the brain and reduces the efferent response to the
afferent cough stimulus originating from the upper respiratory tract.