Carmustine - How It Works
Clinical pharmacology details from the US FDA-approved label: how Carmustine works in your body, how it's absorbed, how long it stays active, and how it's eliminated.
Mechanism of Action
12.1 Mechanism of Action The activity of GLIADEL Wafer is due to release of cytotoxic concentrations of carmustine, a DNA and RNA alkylating agent, into the tumor resection cavity. On exposure to the aqueous environment of the resection cavity, the anhydride bonds in the copolymer are hydrolyzed, releasing carmustine, carboxyphenoxypropane, and sebacic acid into the surrounding brain tissue.
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The activity of GLIADEL Wafer is due to release of cytotoxic concentrations of carmustine, a DNA and RNA alkylating agent, into the tumor resection cavity.
On exposure to the aqueous environment of the resection cavity, the anhydride bonds in the copolymer are hydrolyzed, releasing carmustine, carboxyphenoxypropane, and sebacic acid into the surrounding brain tissue.
12.3 Pharmacokinetics Carmustine concentrations delivered by GLIADEL Wafer in human brain tissue have not been determined.
Following wafer insertion, the mean whole blood C max (± SD) is 10.2 ng/mL ± 4.8 ng/mL.
Absorption Systemic absorption of carmustine is measurable for approximately 24 hours after wafer insertion.
Carmustine C max was reached approximately 3 hours after wafer insertion.
Elimination Metabolism Carmustine degrades both spontaneously and metabolically.
12.6 Wafer Biodegradation GLIADEL Wafers are biodegradable when implanted into the human brain.
Wafer remnants were visible on CT scans obtained 49 days after implantation of GLIADEL Wafer.
More than 70% of the copolymer degrades within three weeks.
Wafer remnants have been present at re-operation and autopsy up to 7.8 months after GLIADEL Wafer implantation and consisted mostly of water and monomeric components with minimal detectable carmustine present.
Pharmacokinetics
12.3 Pharmacokinetics Carmustine concentrations delivered by GLIADEL Wafer in human brain tissue have not been determined. Following wafer insertion, the mean whole blood C max (± SD) is 10.2 ng/mL ± 4.8 ng/mL. Absorption Systemic absorption of carmustine is measurable for approximately 24 hours after wafer insertion. Carmustine C max was reached approximately 3 hours after wafer insertion. Elimination Metabolism Carmustine degrades both spontaneously and metabolically.