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Chlorambucil
4-[bis(2-chlorethyl)amino]benzenebutanoic acid
2. 維持量:1天2~6mg,不可超過1天0.1mg/kg,可低至1天0.03mg/kg。
3. 孩童:1天0.1~0.2mg/kg,或1天4.5mg/㎡。
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.
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).



