Aminocamptothecin
Pronunciation
(a min o camp to THE sin)
Synonyms
9-AC; 9-Aminocamptothecin; NSC-603071
Generic Available
No
Use - Unlabeled/Investigational
Phase II trials: Relapsed lymphoma, refractory breast cancer, nonsmall cell lung cancer, untreated colorectal carcinoma
Contraindications
Hypersensitivity to aminocamptothecin or any component of the formulation
Adverse Reactions
Frequency not defined.
Central nervous system: Fatigue
Dermatologic: Alopecia
Gastrointestinal: Nausea, vomiting, diarrhea, mucositis, anorexia
Hematologic: Neutropenia (may be dose-limiting), thrombocytopenia (reversible, but may be dose-limiting depending on administration schedule), anemia
Drug Interactions
Patients taking anticonvulsants that induce hepatic enzymes have less toxicity and can tolerate higher doses of aminocamptothecin.
Stability
Store ampuls at room temperature. Contents of ampul are added to vial (supplied) containing 24.5 mL of special diluent. Resulting aminocamptothecin concentration is 100 mcg/mL. Further dilution with special diluent for administration via syringe pump is acceptable. May further dilute with NS if resulting concentration is <1 mcg/mL. Diluted solutions are stable for 28 hours at room temperature. Undiluted aminocamptothecin should not contact plastic items.
Mechanism of Action
Aminocamptothecin binds to topoisomerase I, stabilizing the cleavable DNA-topoisomerase I complex, resulting in arrest of the replication fork and inhibition of DNA synthesis.
Pharmacodynamics/Kinetics
Ratio of lactone to total drug is 8.7 ± 4.7% because of instability of aminocamptothecin lactone in plasma.
Distribution: Vd: 46-92 L
Metabolism: None identified
Half-life elimination: Terminal: 8-17 hours for total aminocamptothecin
Excretion: Urine (32% of total drug delivered)
Dosage
I.V.: Adults: 45-59 mcg/m
2
/hour for 72 hours as a continuous infusion; repeat every 2 weeks
or
35 mcg/m
2
/hour as a 72-hour continuous infusion
Administration
Administer by continuous I.V. infusion.
Monitoring Parameters
WBC with differential, platelet count
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause sedation
Mental Health: Effects on Psychiatric Treatment
May cause GI side effects; concomitant use with SSRIs, lithium, or vaproic acid may produce additive effects; monitor. May cause neutropenia and thrombocytopenia; monitor if using concomitantly with clozapine, valproic acid, and carbamazepine.
Oncology: Emetic Potential
Moderate (30% to 60%)
Oncology: Vesicant
No
Dosage Forms
Injection: 5 mg ampul
References
Grossman SA, Hochberg F, Fisher J, et al, "Increased 9-Aminocamptothecin Dose Requirements in Patients on Oral Anticonvulsants. NAPTT CNS Consortium. The New Approaches to Brain Tumor Therapy,"
Cancer Chemother Pharmacol
, 1998, 42(2):118-26.
Iyer L and Ratain MJ, "Clinical Pharmacology of Camptothecins,"
Cancer Chemother Pharmacol
, 1998, 42(Suppl):31-43.
Potmesil M, Arbuck SG, Takimoto CH, et al, "9-Aminocamptothecin and Beyond. Preclinical and Clinical Studies,"
Ann N Y Acad Sci
, 1996, 803:231-46.
Takimota CH, Wright J, and Arbuck SG, "Clinical Applications of the Camptothecins,"
Biochim Biophys Acta
, 1998, 1400(1-3):107-19.
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