Dosing & Uses
Dosage Forms & Strengths
powder for injection
- 10mg/vial
Cancers
Leukemia/Lymphomas/Polycythemia Vera/Mycosis Fungoides/Bronchogenic Carcinoma
0.4 mg/kg IV divided over 2 or 4 days
Combo treatment (MOPP regimen): 6 mg/m²/day IV days 1 and 8 q4Weeks
Do not repeat course until WBC >1000/mm³ & platelets >50 k/mm³
Metastatic Carcinoma
Intrapericardial: 0.2 mg/kg once
Mycosis Fungoides (Orphan)
Orphan indication sponsor
- Yaupon Therapeutics, Inc; 259 Radnor Chester Road; Radnor, PA 19087
Administration
Monitor
- CBC, renal, hepatic, & bone marrow functions
- Adjust subsequent dose based on WBC, platelet counts
Other Indication & Uses
Intrapleural, intraperitoneal, intrapericardial
Off-label: Cutaneous mycosis fungoides (topical application)
Safety & efficacy not established
Cancers
Leukemia/Lymphomas/Polycythemia Vera/Mycosis Fungoides/Bronchogenic Carcinoma
0.4 mg/kg IV divided over 2 or 4 days
Combo treatment (MOPP regimen): 6 mg/m²/day IV days 1 and 8 q4Weeks
Do not repeat course until WBC >1000/mm³ & plateletes >50 k/mm³
Metastatic Carcinoma
Intrapericardial: 0.2 mg/kg once
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
> 10%
Severe nausea/vomiting (90%)
Frequency Not Defined
Vertigo
Chills
Fever
Tinnitus
Thrombosis
Angioedema
Dyspnea
Hemolytic anemia
Hyperuricemia
Myelosuppression
Jaundice
IV site pain
Skin rash
Dermatitis
Erythema multiforme
Urticaria
Fertility impairment
Amenorrhea
Oligomenorrhea
Azoospermia
Oligozoospermia
Allergic reactions
Anaphylaxis
Alopecia
Aggravation of amyloidosis
Warnings
Black Box Warnings
Caution in handling and disposing of the drug
The drug should be administered under the supervision of an experienced cancer chemotherapy physician
If extravasation occurs, it may cause severe tissue damage, leading to ulceration and necrosis
Avoid exposure during pregnancy
Contraindications
Hypersensitivity, history of anaphylaxis
Active infection
Cautions
Amyloidosis
Blood coagulation disorder may occur
Bone marrow depression (leukopenia, thrombocytopenia, anemia)-potential contraindication in CLL
Risk of hyperuricemia
Bone & nervous tissue tumors have responded poorly to therapy
Vesicant (avoid extravasation)
Avoid pregnancy
Pregnancy & Lactation
Pregnancy Category: D
Lactation: not known if excreted in breast milk, do not nurse
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibits DNA & RNA synthesis, via formation of carbonium ions; cross links DNA strands (interstrand and intrastrand crosslinking) causing miscoding breakage and subsequently DNA replication failure
Pharmacokinetics
Half-life elimination: <1 min
Metabolism: Extensive (within minutes; rapid demethylation and hydrolysis)
Excretion: Urine
Administration
IV Incompatibilities
Solution: D5W, NS
- However only 10% drug loss in both fluids
Additive: methohexital
Y-site: allopurinol, cefepime
IV Compatibilities
Y-site: amifostine, aztreonam, filgrastim, fludarabine, granisetron, melphalan, ondansetron, sargramostim, teniposide, vinorelbine
IV Preparation
Must be used fresh, solution is stable for only 1 hr after dilution & must be administered within 1 hr
Do not use if solution is discolored or if water droplets visible prior to reconstitution
Dilute powder with 10 mL SWI to a final concentration of 1 mg/mL; may be diluted in up to 100 mL NS for intracavitary administration
Standard dilution
- IV push: dose/syringe (concentration: 1 mg/mL)
- Maximum syringe for IVP is 30 mL & syringe should be <75% full
IV Administration
Vesicant, do not give IM/SC
Margin of error is very slight
Administer IVP through sidearm of free flowing IV (preferred) or direct injection into vein over a few min
Flush with 5-10 mL NS
Extravasation Management
Sodium thiosulfate1/6 M is specific antidote for nitrogen mustard extravasations
- Mix 4 mL of 10% sodium thiosulfate with 6 mL SWI (or 1.6 mL 25% Na-thiosulfate with 8.4 mL SWI)
- Aspirate residual drug & remove needle
- Inject antidote (2 mL for every 1 mg of drug extravasated) into SC tissue clockwise into infiltrated area using 25 gauge needle
- Time is essential in treating extravasation
- Heat & cold not proven effective
Storage
Store intact vials at room temp
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
