Cisplatin
CISPLATIN
- Cisplatin/cisplatinum/cis-diamine dichloro platinum(II) (CDDP) – Chemotherapy drug.
- 1st member of platinum-containing anti-cancer drug class.
- Administered intravenously as short-term infusion in normal saline for treatment of solid malignancies.
MECHANISM OF ACTION:
- Following administration, one of chloride ligands is slowly displaced by water – “Aquation”.
- Aqua ligand is easily displaced allowing platinum atoms to bind to guanine base.
- Damaged DNA elicits DNA repair mechanisms –
- Inturn activate apoptosis when repair proves impossible.
DNA BINDING:
- Cisplatin binds to DNA & causes critical DNA structural change (bend of 45 degrees).
DOSAGE:
- Administered slowly by i.v. infusion 50–100 mg/m2 BSA every 3–4 weeks.
- Highly emetic drug –
- Antiemetics are routinely administered before infusing it.
INDICATIONS:
Used to treat various types of cancers,
- Sarcomas
- Small cell lung cancer.
- Oesophageal CA.
- Anal squamous cell carcinoma.
- Ovarian cancer.
- Lymphomas.
- Germ cell tumours
- Thymoma
- Dysgerminoma
- Effective against testicular cancer & ovarian cancer.
- Cure rate was improved from 10% to 85%
- In carcinoma cheek –
- Best drug for single drug chemotherapy.
SIDE EFFECT:
- Nephrotoxicity – Major side effect.
- Dose-dependent toxicity.
- Reduced by maintaining good hydration.
- Myelotoxicity – Causes profound bone marrow suppression.
- Hemolytic anemia –
- Developed after several cisplatin courses.
- An antibody reacting with a cisplatin-red-cell membrane responsible for hemolysis.
- Tacrolimus toxicity
- Neurotoxicity.
- Nausea and vomiting
- Most emetogenic chemotherapy agents.
- Ototoxicity –
- Hearing loss.
- Electrolyte disturbance:
- Causes hypomagnesaemia, hypokalemia & hypocalcaemia.
- Hypocalcaemia seems to occur secondary to low serum magnesium cisplatin, & not directly due to Cisplatin
- Secondary leukaemia.
Exam Question
- Chemotherapy for dysgerminoma is Cisplatin, etoposide, bleomycin.
- Cisplatin is used in treatment of ovarian carcinoma.
- Cisplatin is one of the most emetogenic chemotherapy agents.
- Treatment of squamous cell carcinoma of anal canal is Cisplatin-based chemotherapy followed by radical radiotherapy.
- Cisplatin is used in lung cancer is also used in ovarian carcinoma.
- Important chemotherapy agent used for the thymoma treatment is Cisplatin.
- Anticancer drug causing nephrotoxicity is cisplatin.
- Cisplatin is associated with secondary leukaemia.
- Cisplatin causes tacrolimus toxicity.
- In oesophageal ca, Cisplatin is used as a Neoadjuvant chemotherapy agent.
- Cisplatin is used in metastatic testicular carcinoma.
- In carcinoma cheek, Cisplatin is the best drug for single drug chemotherapy.
- Predominantly sensory neuropathy is caused by Cisplatin.
Don’t Forget to Solve all the previous Year Question asked on Cisplatin