Chlorambucil
4-[bis(2-chlorethyl)amino]benzenebutanoic acid

Absorption
Rapidly and completely absorbed. T max is within 1 h. C max is about 1 mcg/mL.

Distribution
99% protein bound (albumin). Crosses the placenta.

Metabolism
Rapidly and extensively metabolized in the liver to phenylacetic acid mustard (active).

Elimination
The t ½ is 1.5 h (chlorambucil) and 2.4 h (phenylacetic acid mustard). 15% to 60% is excreted in urine after 24 h (less than 1% as chlorambucil or phenylacetic acid mustard).

CNS
Confusion; agitation; ataxia; hallucinations; tremors; muscular twitching; flaccid paresis; peripheral neuropathy; seizures; myoclonia.

Dermatologic
Rash; urticaria; skin hypersensitivity (including rare reports of skin rash progressing to erythema multiforme, toxic epidermal necrolysis, and Stevens-Johnson syndrome).

GI
Nausea; vomiting; diarrhea; oral ulceration; mucositis.

Genitourinary
Sterile cystitis; reversible and permanent sterility.

Hematologic
Bone marrow suppression; leukemia.

Hepatic
Hepatotoxicity; jaundice.

Hypersensitivity
Angioedema.

Respiratory
Interstitial pneumonia; pulmonary fibrosis.

Miscellaneous
Acute myelogenous leukemia; drug fever; secondary malignancies.