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carmustine (BiCNU, Gliadel)

 

Classes: Antineoplastics, Alkylating

Dosing and uses of BiCNU, Gliadel (carmustine)

 

Adult dosage forms and strengths

powder for injection

  • 100mg

wafers

  • 7.7mg

 

Brain Tumors, Multiple Myeloma, Hodgkin's Disease, NHL

BiCNU

  • 150-200 mg/m² IV (single dose or divided 2 days) q6Weeks OR
  • 75-100 mg/m²/day IV for 2 days q6Weeks

 

Adjunct to Surgery in Patients with Recurrent Glioblastoma Multiforme

GliadeL

  • Up to 8 wafers placed in surgical resection cavity of brain

 

Adjunct to Surgery & Radiation in Patients with Maligmant Glioma

GliadeL

  • Up to 8 wafers placed in surgical resection cavity of brain

 

Intracranial Malignancies (Orphan)

Orphan indication sponsor

  • Direct Therapeutics, Inc; 460 Seaport Court, Suite 220; Redwood, CA 94063

 

Renal Impairment

CrCl 46-80 mL/min: Administer 80% of regular dose

CrCl 31-45 mL/min: Administer 75% of regular dose

CrCl ≤ 30 mL/min: Not recommended

 

Hepatic Impairment

Dose adjustment may be necessary; not studied

 

Other Indications & Uses

Off-label: Mycosis fungoides

 

Pediatric dosage forms and strengths

Safety & efficacy not established

 

Geriatric dosage forms and strengths

BiCNU

 

Brain Tumors, Multiple Myeloma, Hodgkin's Disease, NHL

150-200 mg/m² IV (single dose or divided 2 days) q6Weeks Or

75-100 mg/m²/day IV for 2 days q6Weeks

Monitor CBC, pulmonary function, LFTs, renal function

GliadeL

 

Adjunct to Surgery in Patients with Recurrent Glioblastoma Multiforme

Up to 8 wafers placed in surgical resection cavity of brain

Monitor CBC, pulmonary function, LFTs, renal function

 

Adjunct to Surgery & Radiation in Patients with Maligmant Glioma

Up to 8 wafers placed in surgical resection cavity of brain

Monitor CBC, pulmonary function, LFTs, renal function

 

BiCNU, Gliadel (carmustine) adverse (side) effects

>10%

Convulsions (19%)

Hemiplegia (19%)

Headache (15%)

Metabolic disorder (14%)

Somnolence (14%)

Fever (12%)

 

1-10%

Confusion (10%)

Aphasia (9%)

Nausea (8%)

Vomiting (8%)

Pain (7%)

Rash (5%)

Abscess (4%)

Cranial edema (4%)

ICP elevation (4%)

Meningitis (4%)

Hyperglycemia (3%)

HTN (3%)

Constipation (2%)

Diarrhea (2%)

Dizziness (2%)

Depression (2%)

 

Frequency not defined

Greater myelotoxicity reported when coadministered with cimetidine

 

Warnings

Black box warnings

The drug should be administered under the supervision of an experienced cancer chemotherapy physician

Bone marrow suppression (notably thrombocytopenia and leukopenia) is the most common and severe of the toxic effects that may result from carmustine administration. It may contribute to bleeding and infections. Monitor blood counts for at least 6 weeks after a dose. Do not give recommended dosage more frequently than every 6 weeks. Adjust dose based on nadir blood counts from prior dose

Pulmonary toxicity is dose related. Risk increases with cumulative doses > 1400 mg/m², history of lung disease and duration of therapy. Delayed cases of pulmonary fibrosis that can result in death have been reported 15 years after administration in children

 

Contraindications

Hypersensitivity

 

Cautions

Do not give more frequently than q6-8wk due to delayed myelosuppression

Risk of irreversible pulmonary fibrosis on long-term treatment

Injection site reactions may occur during administration; rapid infusion may cause burning along the vein and flushing of skin

Extravasation risk, monitor closely during infusion

Intra-arterial administration may cause ocular toxicity

Monitor renal function regularly during treatment

Avoid pregnancy

 

Pregnancy and 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 of BiCNU, Gliadel (carmustine)

Mechanism of action

Alkylates and crosslinks DNA and RNA intefering with normal DNA function; may also inhibit enzyme processes by carbamylation of aminoacids in protein

 

Pharmacokinetics

Half-life elimination: 1.4 min (initial); 22 min (secondary)

Vd: 3.25 L/kg

Distribution: Readily crosses blood-brain barrier

Clearance: 56 mL/min/kg

Excretion: Urine (60-70%)

 

Administration

IV Incompatibilities

Solution: D5W (may be used in shorter time periods)

Additive: sodium bicarbonate

Y-site: allopurinoL

 

IV Compatibilities

Solution: Ns

Y-site: amifostine, aztreonam, cefepime, etoposide PO4, filgrastim, fludarabine, gemcitabine, granisetron, melphalan, ondansetron, piperacillin/tazobactam, sargramostim, teniposide, thiotepa, vinorelbine

 

IV Preparation

Initially dilute with 3 mL of supplied diluent (dehydrated alcohol); further dilute aseptically with 27 mL SWI to result in a concentration of 3.3 mg/mL in 10% alcohoL

Standard dilution: dose/150-500 mL D5W or Ns

 

IV Administration

Significant absorption to PVC containers; should be administered in either glass or Excel container

Infuse over 1-2 hr

High dose carmustine: maximum rate of infusion <3 mg/sq.meter/min to avoid excessive flushing, agitation, & hypotension; infusions should run over at least 2 hr

 

Extravasation Management

Elevate extremity

Inject long-acting dexamethasone or by hyaluronidase throughout tissue with a 25- to 37-gauge needle

Apply warm, moist compresses

 

Storage

Store intact vials under refrigeration