Streptozocin


Generic Medicine Info
Indications and Dosage
Intravenous
Neuroendocrine tumours of pancreatic origin
Adult: Treatment in patients with metastatic islet cell carcinoma of the pancreas (progressive or symptomatic): Alone or in combination with other antineoplastic agents: Daily regimen: 500 mg/m2 once daily for 5 consecutive days every 6 weeks until disease progression or unacceptable toxicity occurs. Dose escalation is not recommended. Weekly regimen: Initially, 1,000 mg/m2 once weekly for the 1st 2 weeks, then may escalate subsequent dose according to patient’s therapeutic response and tolerability up to Max single dose of 1,500 mg/m2. Alternative dosing regimen: Three-weekly regimen: 500 mg/m2 daily for 5 consecutive days during cycle 1, then 1,000 mg/m2 every 3rd week during the subsequent cycles. Doses may be given via IV inj or infusion over 30 minutes to 4 hours. Premedication with antiemetics is recommended. Dosage and treatment protocol recommendations may vary among individual products and between countries (refer to detailed product guideline).
Elderly: Initiate at the lower end of the dosing range.
Renal Impairment
eGFR ≤30 mL/min/1.73 m2: Contraindicated. eGFR >30-≤45 mL/min/1.73 m2: Evaluate the benefit/risk ratio. eGFR >45-≤60 mL/min/1.73 m2: Reduce dose by 50%. Dosage recommendations may vary among individual products and between countries (refer to detailed product guideline).
Hepatic Impairment
Dose reduction may be required.
Reconstitution
Reconstitute vial labelled as containing 1 g with 9.5 mL of 0.9% NaCl solution for inj or dextrose 5% in water to achieve a concentration of 100 mg/mL. If more dilute infusion solutions are desirable, may further dilute the reconstituted solution in the same vehicles.
Contraindications
Renal impairment (eGFR ≤30 mL/min/1.73 m2). Concomitant use with other potentially nephrotoxic drugs, or live and live-attenuated vaccines.
Special Precautions
Patient with pre-existing renal disease and diabetes. Provide adequate hydration before administration to help reduce the risk of nephrotoxicity. Avoid extravasation. Renal (eGFR >30-≤60 mL/min/1.73 m2) and hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Severe nausea and vomiting; hepatotoxicity (e.g. hypoalbuminaemia, elevated transaminases and lactate dehydrogenase), mild to moderate glucose intolerance (reversible); CNS effects (e.g. lethargy, confusion); severe tissue lesions and necrosis (following extravasation). Rarely, mild bone marrow suppression (e.g. mild anaemia or haematocrit reduction).
Gastrointestinal disorders: Diarrhoea.
General disorders and administration site conditions: Inj site reactions (e.g. burning sensation, erythema, oedema, tenderness), fever.
Psychiatric disorders: Depression.
Renal and urinary disorders: Urinary disorders, nephrogenic diabetes insipidus.
Potentially Fatal: Dose-related and cumulative renal toxicity (e.g. proteinuria, hypophosphataemia, anuria, glycosuria, renal tubular acidosis). Rarely, severe haematological toxicity (e.g. substantially decreased leucocyte and platelet count).
IV/Parenteral: D
Patient Counseling Information
This drug may cause confusion or lethargy, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor renal function (including BUN, serum creatinine, serial urinalysis, creatinine clearance or eGFR) and serum electrolytes at baseline, weekly during and for 4 weeks following therapy; LFTs and CBC with differential and platelets weekly. Obtain 24-hour urine collection if proteinuria is detected on urinalysis. Closely monitor infusion site to prevent extravasation, and glucose levels (in patients with diabetes).
Drug Interactions
Increased immunosuppression with risk of lymphoproliferative disorders with immunosuppressive drugs. May prolong the elimination half-life of doxorubicin and result in severe bone marrow suppression; consider doxorubicin dose reduction when used concurrently with streptozocin. Phenytoin may reduce the cytotoxic effect of streptozocin. Coadministration with carmustine may synergistically increase the haematological toxicity of both drugs.
Potentially Fatal: May cause severe cumulative renal toxicity when given concurrently with other potentially nephrotoxic agents. May increase the risk of severe infections with live and live-attenuated vaccines.
Action
Description: Streptozocin is an antineoplastic antibiotic nitrosourea. Its exact mechanism has not been fully established; however, it has been shown to undergo spontaneous decomposition to produce reactive methylcarbonium ions that inhibit deoxyribonucleic acid (DNA) synthesis by alkylation and cross-linking of DNA strands, and possibly by protein modification. Although it inhibits the progression of cells into mitosis, no specific cell cycle phase is particularly sensitive to its lethal effects.
Onset: Therapeutic response: Approx 17 days (1,500 mg/m2 once weekly regimen).
Pharmacokinetics:
Distribution: Distributed to body tissues, specifically in the liver, kidneys, pancreas, and intestines.
Metabolism: Extensively and rapidly metabolised, primarily in the liver and possibly in the kidneys.
Excretion: Via urine (approx 60-70%; 30% as nitrosourea containing metabolites, 10-20% as unchanged drug); faeces (<1%). Elimination half-life: <1 hour.
Chemical Structure

Chemical Structure Image
Streptozocin

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 29327, Streptozocin. https://pubchem.ncbi.nlm.nih.gov/compound/Streptozocin. Accessed June 24, 2021.

Storage
Store intact vials between 2-8°C. Protect from light. Reconstituted solution must be used within 12 hours. Storage recommendations may vary among individual products or between countries (refer to product-specific guidelines). This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
MIMS Class
Cytotoxic Chemotherapy
ATC Classification
L01AD04 - streptozocin ; Belongs to the class of alkylating agents, nitrosoureas. Used in the treatment of cancer.
References
Anon. Streptozocin. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/06/2021.

Anon. Streptozocin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/06/2021.

Buckingham R (ed). Streptozocin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/06/2021.

Joint Formulary Committee. Streptozocin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/06/2021.

Zanosar 1 g Powder for Concentrate for Solution for Infusion (Keocyt). MHRA. https://products.mhra.gov.uk. Accessed 08/06/2021.

Zanosar Powder for Solution (Teva Parenteral Medicines, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/06/2021.

Disclaimer: This information is independently developed by MIMS based on Streptozocin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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