Parent drug and/or metabolite? Which of them is most appropriate to establish bioequivalence of two oral oxcarbaxepine formulations in healthy volunteers?

Expert Opinion on Pharmacotherapy

Volumn 8, Issue 10, 2007, Pages 1415-1423

  Di Girolamo, Guillermo ^a,d   Opezzo, Javier A W ^b   Schere, Daniel ^b   Gonzalez, Claudio D ^c   Moncalvo, Juan J Rodriguez ^d  

^a UNIVERSIDAD DE BUENOS AIRES   (Argentina)

^b Laboratory of Clinical Tests and Nuclear Medicine   (Argentina)

^c Instituto Universitario   (Argentina)

^d Instituto Universitario ^*  (Argentina)

Author keywords

Bioequivalence; Metabolite; MHD; Oxcarbazepine; Parent drug

Indexed keywords

AURENE; LICARBAZEPINE; OXCARBAZEPINE; UNCLASSIFIED DRUG;

ABSENCE OF SIDE EFFECTS; ADULT; ANTICONVULSANT ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CLINICAL TRIAL; CONFIDENCE INTERVAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG HALF LIFE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; QUANTITATIVE ANALYSIS; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUNTEER;

ADMINISTRATION, ORAL; ADULT; ANTICONVULSANTS; AREA UNDER CURVE; BIOTRANSFORMATION; CALIBRATION; CARBAMAZEPINE; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CROSS-OVER STUDIES; HALF-LIFE; HUMANS; LINEAR MODELS; MALE; METABOLIC CLEARANCE RATE; MODELS, BIOLOGICAL; REFERENCE VALUES; REPRODUCIBILITY OF RESULTS; RESEARCH DESIGN; THERAPEUTIC EQUIVALENCY;

EID: 34447513706     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656566.8.10.1415     Document Type: Article

References (42)

1. SCHMIDT D, ELGER CE: What is the evidence that oxcarbazepine and carbarnazepine are distinctly different antiepileptic drugs? Epilepsy Behav. (2004) 5(5):627-635 (Review).
2. WAMIL AW, SCHMUTZ M, PORTET C, FELDMANN KF, MCLEAN MJ: Effects of oxcarbazepine and 10-hydroxycarbamazepine on action potential firing and generalized seizures. Eur. J. Pharmacol. (1994) 271(2-3):301-308.
3. JENSEN PK, GRAM L, SCHMMUTZ M: Oxcarbazepine. Epilepsy Res. Suppl. (1991) 3:135-140.
4. KUBOVA H, MARES P: Anticonvulsant action of oxcarbazepine, hydroxycarbamazepine, and carbamazepine against metrazol-induced motor seizures in developing rats. Epilepsia (1993) 34(1):188-192.
5. WAMIL AW, SCHMUTZ M, PORTET C, FELDMAN KF, MCLEAN AW: Effects of oxcarbazepine and 10-hydroxycarbamazepine on action potential firing and generalized seizures. Eur. J. Pharmacol. (1994) 271(2-3):301-308.
6. TECOMA ES: Oxcarbazepine. Epilepsia (1999) 40(Suppl. 5):S37-S46.
7. MCLEAN AW, SCHMUTZ M, WAMIL AW, OLPE HR, PORTET C, FELDMAN KF: Oxcarbazepine: mechanisms of action. Epilepsia (1994) 35(Suppl. 3):S5-S9.
8. GRANT SM, FAULDS D: Oxcarbazepine: a review of its pharmacology and theapeutic potential in epilepsy, trigeminal neuralgia and affective disorders. Drugs (1992) 43(6):873-888.
9. ARROYO S: Oxcarbazepine. Neurologia (2001) 16(8):370-375.
10. WELLINGTON K, GOA KL: Oxcarbazepine: an update of its efficacy in the management of epilepsy. CNS. Drugs (2001) 15(2):137-163.
11. GLAUSER TA: Oxcarbazepine in the treatment of epilepsy. Pharmacotherapy (2001) (8):904-919.
12. BEYDOUN A, KUTLUAY E: Oxcarbazepine. Expert Opin. Pharmacother. (2002) 3(1)59-67.
13. LLOYD P, FLESCH G, DIETERLE W: Clinical pharmacology and pharmacokinetics of oxcarbazepine. Epilepsia(1994) 35(Suppl. 3):S10-S13.
14. PERUCCA E: The clinical pharmacokinetics of the new antiepileptic drugs. Epilepsia (1999)40(Suppl. 9):S7-13.
15. MAY TW, KORN-MERKER E, RAMBECK B: Clinical pharmacokinetics of oxcarbazepine. Clin. Pharmacokinet. (2003) 42(12):1023-1042.
16. THOMPSON HEALTHCARE INC.: Physician's desk reference, 57th Edition (2003):2326-2331.
17. GONZALEZ-ESQUIVEL DF, ORTEGA-GAVILAN M, ALCANTARA-LOPEZ G, JUNG-COOK H: Plasma level monitoring of oxcarbazepine in epileptic patients. Arch. Med. Res. (2000) 31(2):202-205.
18. STROLIN BENEDETTI M, RUTY B, BALTES E: Induction of endogenous pathways by antiepileptics and clinical implications. Fundam. Clin. Pharmacol. (2005) 19(5):511-529.
19. PERUCCA E: Clinically relevant drug interactions with antiepileptic drugs. Br. J. Clin. Pharmacol. (2006) 61(3):246-255.
20. MATAR KM, NICHOLLS PJ, AL-HASSAN MI, TEKLE A: Rapid micromethod for simultaneous measurement of oxcarbazepine and its active metabolite in plasma by high-performance liquid chromatography. J. Clin. Pharm. Ther. (1995) 20:229-234.
21. FDA GUIDANCE DOCUMENT: Guidance for industry: average, populations, and individual approaches to establishing bioequivalence. Rockville (MD): US Food and Drug administration, Center for Drug Evaluation and Research (CEDER) (1999).
22. STEINIJANS VW, DILETTI E: Generalization of distribution - free confidence intervals for bioavailability ratios. Eur. J. Clin. Pharmacol. (1985) 28(1):85-88.
23. DICKINSON RG, HOOPER WD, PENDLEBURY SC, MOSES D, EADIE MJ: Further clinical and pharmacokinetic observations on the new anticonvulsant, oxcarbazepine. Clin. Exp. Neurol. (1988) 25:127-133.
24. DICKINSON RG, HOOPER WD, DUNSTAN PR, EADIE MJ: First dose and steady-state pharmacokinetics of oxcarbazepine and its 10-hydroxy metabolite. Eur. J Clin. Pharmacol. (1989) 37:69-74.
25. MARZO A, BALANT LP: An updated reappraisal addresed to applications of iterchangeable multi-sourse pharmaceutical products. Arzn. Forsch. Drug Res. (1995) 45(I)2:109-115.
26. GUIDANCE FOR INDUSTRY: Bioavailability and bioequivalence studies for orally administered drug products. General Considerations, Office of Training and Communications, Division of Communications Management, Drug Information Branch, HFD-210, Rockville MD 20857, FDA. Center for Drug Evaluation and Research (CDER) March (2003).
27. BLUME HH, MIDHA KK: Bio-international 92, conference on bioavailability, bioequivalence, and pharmacokinetic studies. J. Pharm. Sci. (1993) 82(11):1186-1189.
28. BLUME HH, MCGILVERAY IJ, MIDHA KK: Bio-international '94 Conference on Bioavailability, Bioequivalence and Pharmacokinetic Studies and Pre-Conference Satellite on 'In vivo/In vitro Correlation'. Munich, Germany (14-17 June 1994). Eur. J. Drug Metab. Pharmacokinet. (1995)20(1):3-13.
29. HEALTH CANADA, THERAPEUTIC PRODUCTS DIRECTORATE (TPD): Discussion paper on 'Bioequivalence requirements - highly variable drugs and highly variable drug products: issues and options'. Expert Advisory Committee on Bioavailability and Bioequivalence (EAC-BB) Meeting (6-27 June 2003).
30. BODDY AW, SNIKERIS FC, KRINGLE RO, WEI GCG, OPPERMANN JA, MIDHA KK: An approach for widening the bioequivalence acceptance limits in the case of highly variable drugs. Pharm. Res. (1995) 12:1865-1868.
31. TOTHFALUSI L, ENDRENYI L, MIDHA KK, RAWSON MJ, HUBBARD JW: Evaluation of the bioequivalence of highly variable drugs and drug products. Pharm Res. (2001) 18:728-733.
32. COMMITTEE FOR PROPRIETARY MEDICINAL PRODUCTS (CPMP), THE EUROPEAN AGENCY FOR THE EVALUATION OF MEDICINAL PRODUCTS (EMEA): Note for guidance on the investigation of bioavailability and bioequivalence (2001).
33. JAPAN NATIONAL INSTITUTE OF HEALTH: Division of drugs. Guideline for bioequivalence studies of generic drug products (1997).
34. MEDICINES CONTROL COUNCIL, DEPARTMENT OF HEALTH, REPUBLIC OF SOUTH AFRICA: Registration of medicines: biostudies (2003).
35. HEALTH CANADA, MINISTRY OF HEALTH: Guidance for industry: conduct and analysis of bioavailability and bioequivalence studies - part A: oral dosage formulations used for systemic effects (1992).
36. TOTHFALUSI L, ENDRENYI L: Limits for the scaled average bioequivalence of highly variable drugs and drug products. Pharm. Res.(2003)20:382-389.
37. max. Int. J. Clin. Pharmacol. Ther. (2003) 41:217-225.
38. e ëddition Documed SA. Bäle, Suisse. (2003):2766-2768.
39. GUIDANCE FOR INDUSTRY: Bioavailability and bioequivalence studies for orally administered drugs products - general considerations - draft guidance-FDA. Center for drug evaluation and research (CDER) (2002). Chapter VI. Special topics: Moieties to be measured.
40. JOHANNESSEN SI, TOMSON T: Pharmacokinetic variability of newer antiepileptic drugs: when is monitoring needed? Clin. Pharmacokinet. (2006) 45:1061-1075 (Review).
41. PERUCCA E: Pharmacokinetic variability of new antiepileptic drugs at different ages. Ther. Drug Monit. (2005)27(6):714-717.
42. PERUCCA E: Clinical pharmacokinetics of new-generation antiepileptic drugs at the extremes of age. Clin. Pharmacokinet. (2006) 45(4):351-363.