Alkylating-like drugs
Carboplatin, cisplatin, and
oxaliplatin are heavy metal complex-es that contain platinum. Because their
action resembles that of a bifunctional alkylating drug, they are referred to
as alkylating-likedrugs.
The distribution and metabolism of carboplatin aren’t defined clearly.
After I.V. administration, carboplatin is eliminated primari-ly by the kidneys.
The elimination of carboplatin is biphasic. It has an initial half-life of 1 to
2 hours and a terminal half-life of 21⁄2 to 6 hours. In patients
with decreased renal function, the ter-minal half-life of carboplatin may last
from 30 to 300 hours.Oxali-platin is 70% to 90% bound to plasma proteins, and
the protein-binding increases over time. It’s widely distributed into most body
tissues and is eliminated in phases.
When administered intrapleurally (into the pleural
space around the lung) or intraperitoneally (into the peritoneum), cisplatin
may exhibit significant systemic absorption. Highly protein bound, cis-platin
reaches high concentrations in the kidneys, liver, intestines, and testes but
has poor central nervous system (CNS) penetra-tion. The drug undergoes some
liver metabolism, followed by ex-cretion through the kidney.
Platinum is detectable in tissue for at least
4 months after admin-istration.
Like alkylating drugs, carboplatin, cisplatin, and oxaliplatin are cell
cycle–nonspecific and inhibit DNA synthesis. They act likebifunctional alkylating drugs by cross-linking
strands of DNA andinhibiting DNA synthesis.
These alkylating-like
drugs are used in the treatment of severalcancers.
• Carboplatin is used
primarily to treat ovarian and lung cancer.
• Cisplatin is prescribed
to treat bladder and metastatic ovarian
• Cisplatin is the drug of
choice to treat metastatic testicular cancers.
• Cisplatin may also be
used to treat head, neck, and lung cancer (although these indications are clinically
accepted, they’re currently unlabeled uses).
• Oxaliplatin is used in combination with
other agents to treatcolorectal cancer.
Alkylating-like drugs interact with a few
other drugs:
• When carboplatin,
oxaliplatin, or cisplatin is administered with an aminoglycoside, the risk of toxicity to the
kidney increases
• Carboplatin or cisplatin
taken with bumetanide, ethacrynic acid,or furosemide increases the risk
of ototoxicity (damaging the organs of hearing and balance)gans of hearing and balance).
• Cisplatin may reduce
serum phenytoin levels. (See Adverse reactions to alkylating-like drugs.)
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