Anticancer Drugs

Preface
Agam is a group of budding medicos, who are currently doing their under graduation in
various Medical Colleges across Tamil Nadu and Pondicherry. The group was initiated on 18th
November 2017, in the vision of uniting medicos for various social and professional causes.
We feel delighted to present you Agam pharmacology notes prepared by Agam Divide and
Rule 2019 Team to guide our fellow medicos to prepare for university examinations.
This is a reference work of 2017 batch medical students from various colleges. The team
took effort to refer many books and make them into simple notes. We are not the authors of the
following work. The images used in the documents are not copyrighted by us and is obtained from
various sources.
Dear readers, we request you to use this material as a reference note, or revision note, or
recall notes. Please do not learn the topics for the 1st time from this material, as this contain just the
required points, for revision.
Acknowledgement
On behalf of the team, Agam would like to thank all the doctors who taught us Pharmacology.
Agam would like to whole heartedly appreciate and thank everyone who contributed towards the
making of this material. A special thanks to Kareeshmaa H C, who took the responsibility of leading
the team. The following are the name list of the team who worked together, to bring out the
material in good form.
 Varsha L
 Rishikkesh Ramana G
1
1. Cisplatin
 It is hydrolysed intracellularly to produce a highly reactive moiety which
causes cross linking of DNA.
 The favoured side is N 7 of guanine residue.
 It can also react with – SH groups of cystoplasmic and nuclear proteins.
 Cisplatin is very effective in metastatic testicular and ovarian carcinoma.
 It is widely used in many other solid tumours like lung, bladder,
esophageal, gastric, hepatic carcinomas.
 Administered by slow i.v infusion 50-100 mg/m2 BSA every 3-4 weeks.
 It is a highly emetic drug. Antiemetics are routinely administered.
 The most important toxicity is renal impairment. Tinnitus, deafness,
sensory neuropathy are other problems.
2. CARBOPLATIN:
Less – reactive second Generation Platinum compound that is better
tolerated than cisplatin. Mechanism of Action is similar to that of
Cisplatin.
Nephrotoxicity, Ototoxicity are low.
Nausea and Vomiting is milder and is delayed.
It is primarily indicated in ovarian carcinoma of epithelial origin and
also used in squamous cell carcinoma of head and neck.
Anticancer Agam Pharmacology

2
3. PURINE ANTAGNNISTS
 Mercaptopurine and Thioguanine.

 These are highly effective anti-neoplastic drugs. After synthesis in the
body to the corresponding monoribonucleofides.
 They inhibit the conversion of inosine monophosphate to adenine and
guanine nucleotides. Which builds DNA and RNA.
 They are especially useful in childhood acute leukaemia,
choriocarcinoma.
 All anti- purine is absorbed orally.
 Main toxic effect is Bone Marrow Depression, Nausea and vomiting.
High incidence of Reversible Jaundices.
 AZATHIOPRINE
 It acts by getting converted to 6 - MP but has more immune suppressant
action.
 Asathioprine primarily suppresses cell-mediated immunity. Used
mainly in autoimmune disease such as Rheumatoid Arthritis.
4. FLUDARABINE
 It is a newer purine anti-metabolite phosphorylated intracellularly to the

active triphosphate from which then inhibits DNA polymerase.
 It is indicated in Chronic Lymphatic leukaemia and Non-Hodgkin’s
Lymphoma.
 Adverse effects are: Chills, Fever, Myalgia, Vomiting, Opportunistic
infections.

3
5. General toxicity of cytotoxic drugs

 Bone marrow: granulocytopenia, agranulocytosis
 Lymphoreticular tissue: Lymphocytopenia, inhibition of lymphocyte function –
suppression of cell mediated and humoral immunity.
 Skin: alopecia, dermatitis
 Foetus: abortion, foetal death
6. Anticancer antibiotics
 Actinomycin D
 Daunorubicin
 Epirubicin
 Mitoxantrone
7. Vinca alkaloid drugs and its uses

 Vincristine: induce remission of childhood acute lymphoblastic leukaemia
 Vinblastine: employed in Hodgkin’s disease, Kaposi sarcoma, breast and
testicular carcinoma
8. Rationale of L-asparaginase in malignancy

 Leukaemia cells were found to be deficient in L-asparagine synthase enzyme. L-
asparaginase degrades L-asparagine to L-aspartic acid depriving the leukemic
cells of essential metabolite and causes cell death.

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Preface

Anticancer Agam Pharmacology

 Mercaptopurine and Thioguanine.

 It is a newer purine anti-metabolite phosphorylated intracellularly to the

Anticancer Agam Pharmacology

5. General toxicity of cytotoxic drugs

7. Vinca alkaloid drugs and its uses

8. Rationale of L-asparaginase in malignancy

Anticancer Agam Pharmacology

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