cisplatin

Brand: Platinol

⚠ BBW ISMP High Alert Prototype Drug
Drug Class: platinum-based alkylating agent
Drug Family: antineoplastic
Subclass: first-generation platinum antineoplastic
Organ Systems: hematology-oncology

Mechanism of Action

Undergoes hydrolysis to form reactive platinum species; forms intrastrand and interstrand DNA cross-links (primarily at adjacent guanine residues), distorting DNA helix; triggers apoptosis via p53 pathway; cells in all phases of cell cycle are susceptible.

DNA (intrastrand and interstrand cross-links)

Indications

  • testicular cancer (curative)
  • ovarian cancer
  • bladder cancer
  • lung cancer (NSCLC and SCLC)
  • head and neck cancer
  • cervical cancer

Contraindications

  • cisplatin hypersensitivity
  • pre-existing significant renal impairment
  • pre-existing severe hearing loss (ototoxicity)
  • myelosuppression

Adverse Effects

Common

  • severe nausea/vomiting (most emetogenic of all chemotherapies)
  • nephrotoxicity
  • peripheral neuropathy
  • electrolyte wasting (hypomagnesemia, hypokalemia, hypocalcemia)

Serious

  • nephrotoxicity (dose-limiting, cumulative)
  • ototoxicity (irreversible high-frequency hearing loss)
  • peripheral neuropathy (cumulative, sometimes irreversible)
  • myelosuppression
  • severe nausea and vomiting (most emetogenic agent)
  • anaphylaxis

Pharmacokinetics (ADME)

Absorption IV only
Distribution extensively binds to plasma proteins (>90%) and tissue proteins; distributes widely
Metabolism non-enzymatic conversion to reactive species in plasma
Excretion renal (primarily platinum — 90% within 24 hours of administration); dose reduction with renal impairment
Half-life 58–73 hours (terminal)
Onset immediate (IV)
Peak end of infusion
Duration variable per cycle
Protein Binding >90%
Vd moderate-large

Drug Interactions

Drug / Agent Mechanism Severity
aminoglycosides/vancomycin/loop diuretics additive ototoxicity and nephrotoxicity major
NSAIDs increase nephrotoxicity risk by reducing renal prostaglandin-mediated vasodilation major
phenytoin cisplatin reduces phenytoin absorption and increases metabolism; subtherapeutic phenytoin levels major

Nursing Considerations

  1. Pre-hydration with at least 1–2 L of 0.9% NaCl over 2–4 hours before and after cisplatin is mandatory to prevent nephrotoxicity; maintain urinary output >100 mL/hr during infusion.
  2. Aggressive antiemetic prophylaxis is required — the most emetogenic chemotherapy regimen demands a 5-HT3 antagonist + NK1 antagonist + dexamethasone combination.
  3. Monitor BMP (electrolytes, creatinine) before each cycle; replace magnesium aggressively (hypomagnesemia is universal and can be severe).
  4. Audiogram testing at baseline and periodically; instruct patients to report tinnitus, decreased hearing, or dizziness immediately.

Clinical Pearls

  • Cisplatin's discovery was accidental — an American researcher studying the effects of electric current on bacterial growth noticed that platinum electrodes were producing platinum compounds that inhibited bacterial division, leading to its development as an anti-cancer drug.
  • The combination of bleomycin, etoposide, and cisplatin (BEP) is curative for advanced testicular cancer in >80% of cases — one of oncology's greatest success stories and a testament to cisplatin's importance.

Safety Profile

Pregnancy contraindicated
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required