streptozocin: profile and news

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Other information

Indication
For the treatment of malignant neoplasms of pancreas (metastatic islet cell carcinoma)

Pharmacology
Streptozocin is an antitumour antibiotic consisting of a nitrosourea moiety interposed between a methyl group and a glucosamine. Streptozocin is indicated in the treatment of metastatic islet cell carcinoma of the pancreas. Streptozocin inhibits DNA synthesis in bacterial and mammalian cells. In bacterial cells, a specific interaction with cytosine moieties leads to degradation of DNA. The biochemical mechanism leading to mammalian cell death has not been definitely established; streptozocin inhibits cell proliferation at a considerably lower level than that needed to inhibit precursor incorporation into DNA or to inhibit several of the enzymes involved in DNA synthesis. Although streptozocin inhibits the progression of cells into mitosis, no specific phase of the cell cycle is particularly sensitive to its lethal effects.

Mechanism Of Action
Although its mechanism of action is not completely clear, streptozocin is known to inhibit DNA synthesis, interfere with biochemical reactions of NAD and NADH, and inhibit some enzymes involved in gluconeogenesis. Its activity appears to occur as a result of formation of methylcarbonium ions, which alkylate or bind with many intracellular molecular structures including nucleic acids. Its cytotoxic action is probably due to cross-linking of strands of DNA, resulting in inhibition of DNA synthesis.

Drug Category
Antibiotics; Antineoplastic Agents; ATC:L01AD04

Brand Names/Synonyms
Rcra Waste Number U206; STREPTOZOTOCIN; STRZ; STZ; Streptozocin; Streptozocin [Usan:Inn]; Streptozocine [Inn-French]; Streptozocinium [Latin]; Streptozocinum [Inn-Latin]; Streptozoticin; Streptozotocin; U 9889; U-9889; Zanosar

Dosage Forms
POWDER FOR SOLUTION

Absorption
Poor oral absorption (17-25%)

Interactions
-->Interactions for Streptozocin:

ZANOSAR may demonstrate additive toxicity when used in combination with other cytotoxic drugs. Streptozocin has been reported to prolong the elimination half-life of doxorubicin and may lead to severe bone marrow suppression; a reduction of the doxorubicin dosage should be considered in patients receiving ZANOSAR concurrently. The concurrent use of strep-tozocin and phenytoin has been reported in one case to result in reduced streptozocin cytotoxicity.

Chemical IUPAC Name
1-methyl-1-nitroso-3-[2,4,5-trihydroxy-6-(hydroxymethyl)oxan-3-yl]-urea

Chemical Formula
C8H15N3O7

Half Life
5-15 minutes

Drug Type
Approved Drug

# Accession No
APRD00209

CAS Registry Number
18883-66-4