Monograph
L01XA01 - Cisplatin |
Not porphyrinogenic |
NP |
Rationale
Non-CYP metabolism. However, side effects such as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Cisplatin is an inorganic complex that contains a platinum atom surrounded in a plane by 2 chloride atoms and 2 ammonia molecules in the cis position.
Therapeutic characteristics
Cisplatin is a platinum-containing antineoplastic agent used in the treatment of cancer such as ovarial cancer, vescical cancer, testis tumours with metastases, cancers in the head/neck region, and lungcancer. It is administered as an intravenous injection or infusion. Common adverse reactions of cisplatin that can be confused with an acute porphyric attack are vomiting, and nausea. Side effects such as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Hepatic exposure
Metabolism and pharmacokinetics
Cisplatin has a non-enzymatic metabolism. Excretion is mainly in the urine: up to about 50% of a dose has been reported to be excreted in urine over 5 days, and platinum may be detected in tissue for several months afterwards. The unbound fraction, which is more rapidly cleared, may be actively secreted by the renal tubules. Interactions with CYP metabolism of other drugs not observed. Not listed as CYP-inducer or inhibitor (Rendic 2002). Cisplatin did not exert a significant effect on the PXR-mediated induction of CYP3A4 (Harmsen, 2009). Cisplatin was without inhibitory effect on CYP3A4 (Baumhakel, 2001).
Published experience
Used uneventfully by AIP man in the treatment of testicular cancer (Arbus, 1981).
IPNet drug reports
No.
References
# | Citation details | PMID |
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* | Scientific articles | |
1. | Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448.
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2. | Relationship between porphyria and the use of antineoplastics.
Arbus MH. Am J Hosp Pharm. 1981;38(5):631. |
7282689 |
3. | Screening for inhibitory effects of antineoplastic agents on CYP3A4 in human liver microsomes.
Baumhäkel M, Kasel D, et al. Int J Clin Pharmacol Ther. 2001 Dec;39(12):517-28. |
|
4. | Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor.
Harmsen S, Meijerman I, et al. Cancer Chemother Pharmacol. 2009;64(1):35-43. |
18839173 |
* | Drug reference publications | |
5. | McEvoy GK, editor. Cisplatin. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (10.05.10).
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6. | Sweetman SC, editor. Martindale: The complete drug reference. Cisplatin. Pharmaceutical Press 2009.
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Similar drugs
Tradenames and packages
From some sources, we get a list of packages (United Kingdom, Ireland, Estonia).
Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway).
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Netherlands
Cisplatine · Cisplatine 0,5 mg/ml PCH, concentraat voor oplossing voor infusie · Cisplatine 1 mg/ml PCH, concentraat voor oplossing voor infusie · Cisplatine Accord 1 mg/ml concentraat voor oplossing voor infusie · Cisplatine Hikma 1 mg/ml concentraat voor oplossing voor infusieBelgium
Cisplatin · Cisplatin Accord Healthcare 1 mg/ml sol. perf. (à diluer) i.v. flac. · Cisplatine · Cisplatine Teva 1 mg/ml sol. perf. (à diluer) i.v. flac.United Kingdom
Cisplatin · Cisplatin 100mg/1000ml in Sodium chloride 0.9% infusion bags · Cisplatin 100mg/100ml concentrate for solution for infusion vials · Cisplatin 100mg/100ml solution for infusion vials · Cisplatin 10mg/10ml concentrate for solution for infusion vials · Cisplatin 10mg/10ml solution for infusion vials · Cisplatin 113mg/1000ml in Sodium chloride 0.9% infusion bags · Cisplatin 128mg/1000ml in Sodium chloride 0.9% infusion bags · Cisplatin 145mg/1000ml in Sodium chloride 0.9% infusion bags · Cisplatin 164mg/1000ml in Sodium chloride 0.9% infusion bags · Cisplatin 185mg/1000ml in Sodium chloride 0.9% infusion bags · Cisplatin 33mg/250ml in Sodium chloride 0.9% infusion bags · Cisplatin 36mg/250ml in Sodium chloride 0.9% infusion bags · Cisplatin 40mg/250ml in Sodium chloride 0.9% infusion bags · Cisplatin 45mg/250ml in Sodium chloride 0.9% infusion bags · Cisplatin 50mg powder for solution for infusion vials · Cisplatin 50mg/500ml in Sodium chloride 0.9% infusion bags · Cisplatin 50mg/50ml concentrate for solution for infusion vials · Cisplatin 50mg/50ml solution for infusion vials · Cisplatin 70mg/500ml in Sodium chloride 0.9% infusion bags · Cisplatin 89mg/500ml in Sodium chloride 0.9% infusion bags · Platinex · Platinex 100mg/100ml solution for infusion vials · Platinex 50mg/50ml solution for infusion vialsDenmark
Cisplatin · Cisplatin "Accord" · Cisplatin "Ebewe" · Cisplatin "Pfizer"Norway
Cisplatin AccordPoland
Cisplatin - Ebewe · Cisplatinum AccordLuxembourg
CISPLATINE · CISPLATINE TEVA-1MG/MLFinland
Cisplatin Accord · Cisplatin EbeweLatvia
Cisplatin · Cisplatin AccordSerbia
Cisplatin · Cisplatin Ebewe® · Cisplatin Pfizer · Cisplatinum · Cisplatinum Accord · Sinplatin · Sinplatin®
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