Monograph
L01BC01 - Cytarabine |
Propably not porphyrinogenic |
PNP |
Rationale
Primarily non-CYP metabolizm. Not inhibitor or inducer of CYP3A4 or 2C9 in clinical use. However, side effects such as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Cytarabine (cytosine arabinoside) is a synthetic pyrimidine nucleoside analog.
Therapeutic characteristics
Cytarabine is an antimetabolite antineoplastic agent used mainly in the treatment of leukemia, especially acute non-lymphoblastic leukemia. Administered intravenously by rapid injection or continuous infusion, or by subcutaneous or intrathecal injection. Common adverse reactions of cytarabine that can be confused with an acute porphyric attack are nausea, vomiting, diarrhoea and myalgia. Side effects such as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
Cytarabine is metabolized to uridinearbinoside by hepatic, gastrointestinal and leucocyte deaminases. After entry into leucemic cells cytarabine undergoes phosphorylations forming the cytotoxic cytarabine triphosphate. Found to be a substrate of CYP3A4 by Colburn et al (2004), and also found to be an inhibitor of CYP3A4, but the authors determined that the inhibition was not of clinical significance. Baumhakel (2001) found no inhibitory effect of cytarabine on CYP3A4 in human liver microsomes.
Published experience
Used uneventfully in the treatment of acute myelogenous leukemia in AIP woman (Wehmeimer, 1987). Used uneventfully in the treatment of acute lymphoblastic leukemia in PV woman (Samuels, 1984).
References
# | Citation details | PMID |
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* | Scientific articles | |
1. | Screening for inhibitory effects of antineoplastic agents on CYP3A4 in human liver microsomes.
Baumhäkel M, Kasel D, et al. Int J Clin Pharmacol Ther. 2001;39(12):517-28. |
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2. | Chemotherapy in porphyria.
Samuels B, Bezwoda WR, et al. S Afr Med J. 1984;65(23):924-6. |
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3. | Polychemotherapy of acute myelogenous leukemia in a patient with acute intermittent porphyria.
Wehmeier A, Fischer JT, et al. Klin Wochenschr. 1987;65(7):338-40. |
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* | Drug reference publications | |
4. | DrugBank. Cytarabine. Accessed:09.07.10.
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5. | McEvoy GK, editor. Cytarabine. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (09.07.10).
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6. | Sweetman SC, editor. Martindale: The complete drug reference. Cytarabine. Pharmaceutical Press 2009.
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* | Summary of Product Characteristics | |
7. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Cytarabine Pfizer.
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Similar drugs
Tradenames and packages
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Netherlands
Cytarabine · Cytarabine Accord 100 mg/ml, oplossing voor injectie of infusie · Cytarabine Fresenius Kabi 100 mg/ml oplossing voor injectie of infusie · Cytarabine Hospira 100 mg/5 ml Onco-Tain, oplossing voor injectie 20 mg/ml · Cytarabine Hospira 1000 mg/10 ml Onco-Tain, concentraat voor oplossing voor infusie 100 mg/ml · Cytarabine Hospira 2000 mg/20 ml Onco-Tain, concentraat voor oplossing voor infusie 100 mg/mlBelgium
Cytarabine · Cytarabine Accord Healthcare 100 mg/ml sol. inj./perf. s.c./i.v. flac. · Cytarabine Fresenius Kabi 100 mg/ml sol. inj./perf. s.c./i.v. flac. · Cytarabine Onco-Tain · Cytarabine Hikma Onco-Tain 100 mg/ml sol. inj. i.théc./s.c./i.v./i.m. flac. · Cytosar · Cytosar 1 g/10 ml sol. perf. (à diluer) i.v. flac. · Cytosar 100 mg/5 ml sol. inj. i.théc./s.c./i.v. flac. · Cytosar 2 g/20 ml sol. perf. (à diluer) i.v. flac.United Kingdom
Cytarabine · Cytarabine 100mg/1ml solution for injection vials · Cytarabine 100mg/5ml solution for injection Cytosafe vials · Cytarabine 100mg/5ml solution for injection vials · Cytarabine 1g/10ml solution for injection Cytosafe vials · Cytarabine 1g/10ml solution for injection vials · Cytarabine 20mg/0.2ml solution for injection pre-filled syringes · Cytarabine 20mg/1ml solution for injection pre-filled syringes · Cytarabine 2g/20ml solution for injection Cytosafe vials · Cytarabine 2g/20ml solution for injection vials · Cytarabine 4g/40ml solution for injection vials · Cytarabine 500mg/25ml solution for injection Cytosafe vials · Cytarabine 500mg/25ml solution for injection vials · Cytarabine 500mg/5ml solution for injection vials · Cytarabine 5g/50ml solution for infusion vials · Cytarabine 20mg/ml solution for injection vials · DepoCyte · DepoCyte 50mg/5ml suspension for injection vialsDenmark
Cytarabin · Cytarabin "Fresenius Kabi" · Cytarabine · Cytarabine "Accord" · Cytarabine "Pfizer"Norway
Cytarabin Fresenius Kabi · Cytarabine AccordPoland
Alexan · Cytarabina Accord · Cytarabine Kabi · CytosarLuxembourg
CYTOSARIceland
Cytarabin · Cytarabin Fresenius Kabi · Cytarabine · Cytarabine PfizerFinland
Cytarabine Accord · Cytarabine Accord Healthcare · Cytarabine StadaLatvia
Cytarabine · Cytarabine Accord · Cytarabine KabiSerbia
Alexan · Alexan® Ebewe · Cytosar · Cytosar®
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