streptozocin

Absorption: IV administration results in complete bioavailability.

Distribution: Rapidly distributed. High concentrations in liver, pancreas, kidneys, and intestine. Active metabolite enters the CSF.

Metabolism/Excretion: Highly metabolized in liver and kidneys. 10–20% excreted unchanged by the kidneys. Small amounts excreted in expired air (5%) and feces (1%).

Half-Life: 35–40 min.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IV (effects on blood counts)	unknown	1–2 wk	unknown
IV (tumor response)	17 days	35 days	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Renal impairment (dose ↓ recommended);
Hepatic impairment;
Active infection;
↓bone marrow reserve;
Pedi: Safety and effectiveness not established in children;
Geri: Consider body mass, age-related in renal/hepatic/cardiac function as well as concurrent illness and drug therapies in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Endo: hyperglycemia, HYPOGLYCEMIA (FIRST DOSE)

F and E: hypophosphatemia

GI: nausea, vomiting, diarrhea, duodenal ulcer, HEPATITIS

GU: nephrotoxicity, gonadal suppression, proteinuria

Hemat: anemia, eosinophilia, leukopenia, thrombocytopenia

Local: phlebitis, injection site reactions

Neuro: confusion, depression, lethargy

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

↑myelosuppression with other antineoplastics.
↑risk of nephrotoxicity with other nephrotoxic agents, including aminoglycosides.
Toxicity may be ↑ by concurrent phenytoin therapy.
May ↑ toxicity of doxorubicin.
May ↓ antibody response to live-virus vaccines and ↑ risk of adverse reactions.

Route/Dosage ⬆ ⬇

IV (Adults ): 500 mg/m²once daily for 5 days every 4–6 wk or 1 g/m²once weekly for 2 wk; then may be ↑ (not to exceed 1.5 g/m²/dose) and given once weekly for 4–6 doses.

Availability ⬆ ⬇

Powder for injection: 1 g/vial

Assessment ⬆ ⬇

Monitor vital signs prior to and periodically during therapy.
Monitor intake and output and daily weight. Report significant discrepancies or dependent edema; may indicate nephrotoxicity. Encourage fluids to 3000 mL/day to ↓ risk of renal damage.
Monitor IV site carefully and ensure patency. Discontinue infusion immediately if severe discomfort, erythema along vein, or infiltration occurs. Apply cool packs above injection site. Tissue ulceration and necrosis may result from infiltration. Resume infusion in another vein and notify physician or other health care professional.
Monitor for bone marrow depression. Assess for bleeding (bleeding gums, bruising, petechiae, guaiac stools, urine, and emesis) and avoid IM injections and rectal temperatures if platelet count is low. Apply pressure to venipuncture sites for 10 min. Assess for signs of infection during neutropenia. Anemia may occur. Monitor for ↑ fatigue, dyspnea, and orthostatic hypotension.
Monitor hydration status, appetite, and nutritional intake. Adequate hydration may ↓ the risk of nephrotoxicity by ↓ urine/renal concentration of the drug and its metabolites. Severe, protracted nausea and vomiting may occur 1–4 hr after beginning infusion. Nausea and vomiting may worsen with subsequent doses. Administration of an antiemetic and adjustment of diet as tolerated may help maintain fluid and electrolyte balance and nutritional status.

Lab Test Considerations:

Monitor renal status prior to and frequently during therapy and for 4 wk after course of therapy. Nephrotoxicity is common and may be manifested by ↑ BUN and serum creatinine, ↓ CCr, and presence of protein in urine. Reduction or discontinuation of streptozocin may allow reversal of renal damage.
- Monitor for hepatotoxicity—evidenced by ↑ AST, ALT, LDH, serum bilirubin, and alkaline phosphatase or ↓ serum albumin—at least weekly.
- May cause hypoglycemia. Monitor serum glucose prior to and after initial dose and periodically during therapy.
- Monitor serum uric acid prior to and periodically during therapy.
- Monitor CBC and differential prior to and weekly during therapy. Report significant ↓.
- Serial fasting insulin concentrations may be used to determine response to therapy.

Implementation ⬆ ⬇

IV dextrose should be immediately available, because hypoglycemia may occur in response to initial dose.
- Solution should be prepared in a biologic cabinet. Wear gloves, gown, and mask while handling medication. Discard equipment in designated containers.

IV Administration:

Intermittent Infusion: Diluent: Reconstitute vial with 9.5 mL of D5W or 0.9% NaCl. May be further diluted in 10–200 mL of D5W or 0.9% NaCl. Admixed solution stable for 12 hr.Concentration: 100 mg/mL.
Rate: Infuse over 10–15 min. Slower infusion rates (45–60 min) have been used to ↓ venous irritation. May also be infused over 6 hr.
- May be administered via rapid IV injection.

Patient/Family Teaching ⬆ ⬇

Instruct patient to notify nurse immediately if pain or redness develops at IV site.
Instruct patient to notify nurse immediately if symptoms of hypoglycemia occur (anxiety; chills; cold sweats; confusion; cool, pale skin; difficulty in concentration; drowsiness; excessive hunger; headache; irritability; nausea; nervousness; shakiness; unusual tiredness; or weakness).
Instruct patient to notify health care professional if ↓ urine output; swelling of lower extremities; yellowing of skin; fever; chills; sore throat; signs of infection; bleeding gums; bruising; petechiae; or blood in urine, stool, or emesis occurs. Caution patient to avoid crowds and persons with known infections. Instruct patient to use soft toothbrush and electric razor. Caution patient not to drink alcoholic beverages or take products containing aspirin or NSAIDs.
Instruct patient not to receive any vaccinations without advice of health care professional.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during therapy and to avoid breastfeeding during therapy.
Advise patient of need for medical follow-up and frequent lab tests.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇