Regulatory review of acetaminophen clinical pharmacology in young pediatric patients

Journal of Pharmaceutical Sciences

Volumn 101, Issue 12, 2012, Pages 4383-4389

  Ji, Ping ^a   Wang, Yaning ^a   Li, Zhihong ^a   Doddapaneni, Suresh ^a   Hertz, Sharon ^a   Furness, Scott ^a   Sahajwalla, Chandrahas G ^a  

^a CENTER FOR DRUG EVALUATION AND RESEARCH   (United States)

Author keywords

ADME; Clinical pharmacokinetics; Disposition; Metabolism; Pediatric; Pharamcokinetics; Pharmacodynamics; Pharmacokinetics pharmacodynamics

Indexed keywords

EID: 84868206413     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23331     Document Type: Review

References (55)

1. Internal analgesic, antipyretic, and antirheumatic drug products for over-the-counter human use; Tentative final monograph. Federal Register, Vol. 53, No. 221, 1988. (Docket No. 77N-0094).
2. Temple AR. 1983. Pediatric dosing of acetaminophen. Pediatric Pharmacol 3:321-327.
3. Internal analgesic, antipyretic, and antirheumatic drug products for over-the-counter human use: Proposed amendment of the tentative final monograph: Required warnings and other labeling, 74 FR 77314-52 (April 29, 2009) (Docket No.1977N-0094L).
4. Bagnall WE, Kelleher J, Walker BE, Losowsky MS. 1979. The gastrointestinal absorption of acetaminophen in the rat. J Pharm Pharmacol 31:157-60.
5. Kalantzi L, Reppas C, Dressman JB, Amidon GL, Junginger HE, Midha KK, Shah VP, Stavchansky SA, Barends DM. 2006. Biowaiver monographs for immediate release solid oral dosage forms: Acetaminophen (paracetamol). J Pharm Sci 95:4-14.
6. Prescott LF. 2001. Paracetamol (acetaminophen): A critical bibliographic review. 2nd ed. Boca Raton, Florida: CRC, 1001 p.
7. Gelotte CK, Auiler JF, Lynch JM, Temple AR, Slattery JT. 2007. Disposition of acetaminophen at 4, 6, and 8 g/day for 3 days in healthy young adults. Clin Pharmacol Ther 81:840-848.
8. Rostami-Hodjegan A, Shiran MR, Ayesh R, Grattan TJ, Burnett I, Darby-Dowman A, Tucker GT. 2002. A new rapidly absorbed acetaminophen tablet containing sodium bicarbonate. I. A four way crossover study to compare the concentration-time profile of acetaminophen from the new acetaminophen/sodium bicarbonate tablet and a conventional acetaminophen tablet in fed and fasted volunteers. Drug Dev Ind Pharm 28:523-531.
9. Stillings M, Havlik I, Chetty M, Clinton C, Schall R, Moodley I, Muir N, Little S. 2000. Comparison of the pharmacokinetic profiles of soluble aspirin and solid acetaminophen tablets in fed and fasted volunteers. Curr Med Res Opin 16:115-124.
10. Gupta M, Brans YW. 1978. Gastric retention in neonates. Pediatrics 62:26-29.
11. Carlos MA, Babyn PS, Marcon MA, Moore AM. 1997. Changes in gastric emptying in early postnatal life. J Pediatr 130:931-937.
12. Liang J, Co E, Zhang M, Pineda J, Chen JD. 1998. Development of gastric slow waves in preterm infants measured by electrogastrography. Am J Physiol 274:G503-G508.
13. Clissold SP. 1986. Acetaminophen and phenacetin. Drugs 32:46-59.
14. Bannwarth B, Netter P, Lapicque F, Gillet P, Péré P, Boccard E, Royer RJ, Gaucher A. 1992. Plasma and cerebrospinal fluid concentrations of acetaminophen after a single intravenous dose of propacetamol. Br J Clin Pharmacol 34:79-81.
15. Levy G, Garrettson LK, Soda DM 1975. Letter: Evidence of placental transfer of acetaminophen. Pediatrics 55:895.
16. Berlin Jr, CM, Yaffe SJ, Ragni M. 1980. Disposition of acetaminophen in milk, saliva, and plasma of lactating women. Pediatr Pharmacol (New York) 1:135-41.
17. Kumpulainen E, Kokki H, Halonen T, Heikkinen M, Savolainen J, Laisalmi M. 2007. Paracetamol (acetaminophen) penetrates readily into the cerebrospinal fluid of pediatrics after intravenous administration. Pediatrics 119:766-771.
18. Anderson BJ, van Lingen RA, Hansen TG, Lin YC, Holford NH. 2002. Acetaminophen developmental pharmacokinetics in premature neonates and infants: A pooled population analysis. Anesthesiology 96:1336-1345.
19. Prescott LF. 1980. Kinetics and metabolism of acetaminophen and phenacetin. Br J Clin Pharmacol 10:291S-298S.
20. Patel M., Tang B.K., Kalow W. 1992. Variability of acetaminophen metabolism in Caucasians and Orientals. Pharmacogenetics 2:38-45.
21. Miners JO, Osborne NJ, Tonkin AL, Birkett DJ. 1992. Perturbation of acetaminophen urinary metabolic ratios by urine flow rate. Br J Clin Pharmacol 34:359-362.
22. Burchell B, Brierley CH, Rance D. 1995. Specificity of human UDP-glucuronosyltransferases and xenobiotic glucuronidation. Life Sci 57:1819-1831.
23. Court MH. 2001. Acetaminophen UDP-glucuronosyltransferase in ferrets: Species and gender differences, and sequence analysis of ferret UGT1A6. J Vet Pharmacol Ther 2:415-422.
24. Mutlib AE, Goosen TC, Bauman JN, Williams JA, Kulkarni S, Kostrubsky S. 2006. Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity. Chem Res Toxicol 19:701-709.
25. Manyike PT, Kharasch ED, Kalhorn TF, Slattery JT. 2000. Contribution of CYP2E1 and CYP3A to paracetamol reactive metabolite formation. Clin Pharmacol Ther 67:275-282.
26. Dahlin DC, Miwa GT, Lu AY, Nelson SD. 1984. N-acetyl-p-benzoquinone imine: A cytochrome P-450-mediated oxidation product of acetaminophen. Proc Natl Acad Sci U S A 81:1327-1331.
27. Lauterburg BH, Mitchell JR. 1987. Therapeutic doses of acetaminophen stimulate the turnover of cysteine and glutathione in man. J Hepatol 4:206-211.
28. van der Marel CD, Anderson BJ, van Lingen RA, Holford NH, Pluim MA, Jansman FG, van den Anker JN, Tibboel D. 2003. Paracetamol and metabolite pharmacokinetics in infants. Eur J Clin Pharmacol 59:243-251.
29. Miller RP, Roberts RJ, Fischer LJ. 1976. Acetaminophen elimination kinetics in neonates, children, and adults. Clin Pharmacol Ther 19:284-294.
30. Vieira I, Sonnier M, Cresteil T. 1996. Developmental expression of CYP2E1 in the human liver. Hypermethylation control of gene expression during the neonatal period. Eur J Biochem 238:476-483.
31. Palmer GM, Atkins M, Anderson BJ, Smith KR, Culnane TJ, McNally CM, Perkins EJ, Chalkiadis GA, Hunt RW. 2008. I.V. acetaminophen pharmacokinetics in neonates after multiple doses. Br J Anaesth 101:523-530.
32. Piñeiro-Carrero VM, Piñeiro EO. 2004. Liver. Pediatrics 113:1097-1106.
33. Windoder A, Vogel C. 1976. Untersuchungen über serumkonzentrationen und temperaturverlauf nach einer neuen oral applizier baren tIussigen acetaminophenzübereitung. Klinische Pädiatrie 188:430-434
34. Peterson RG, Rumack BH. 1981. Age as a variable in acetaminophen overdose. Arch Internal Med 141:390-393.
35. Wilson JT, Brown RD, Bocchini Jr JA, Kearns GL. 1982. Efficacy, disposition and pharmacodynamics of aspirin, acetaminophen and choline salicylate in young febrile pediatrics. Ther Drug Monit 4:147-180.
36. Nahata MC, Powell DA, Durrell DE, Miller MA. 1984. Acetaminophen accumulation in pediatric patients after repeated therapeutic doses. Eur J Clin Pharmacol 27:57-59.
37. Brown RD, Wilson JT, Kearns GL, Eichler VF, Johnson VA, Bertrand KM. 1992. Single-dose pharmacokinetics of ibuprofen and acetaminophen in febrile pediatrics. J Clin Pharmacol 32:231-241.
38. Kelley MT, Walson PD, Edge JH, Cox S, Mortensen ME. 1992. Pharmacokinetics and pharmacodynamics of ibuprofen isomers and acetaminophen in febrile pediatrics. Clin Pharmacol Ther 52:181-189.
39. Hopkins CS, Underhill S, Booker PD. 1990. Pharmacokinetics of acetaminophen after cardiac surgery. Arch Dis Child 65:971-976.
40. Rømsing J, Ostergaard D, Senderovitz T, Drozdziewicz D, Sonne J, Ravn G. 2001. Pharmacokinetics of oral diclofenac and acetaminophen in pediatrics after surgery. Paediatr Anaesth 11:205-213.
41. Anderson BJ, Woollard GA, Holford NH. 2001. Acetaminophen analgesia in children: Placebo effect and pain resolution after tonsillectomy. Eur J Clin Pharmacol 57:559-569.
42. Wilson JT, Brown RD, Kearns GL, Eichler VF, Johnson VA, Bertrand KM, Lowe BA. 1991. Single-dose, placebo-controlled comparative study of ibuprofen and acetaminophen antipyresis in children. J Pediatr 119:803-811.
43. Gupta H, Shah D, Gupta P, Sharma KK. 2007. Role of paracetamol in treatment of childhood fever: A double-blind randomized placebo controlled trial. Indian Pediatr 44:903-911.
44. Erlewyn-Lajeunesse MD, Coppens K, Hunt LP, Chinnick PJ, Davies P, Higginson IM, Benger JR. 2006. Randomised controlled trial of combined acetaminophen and ibuprofen for fever. Arch Dis Child 91:414-416.
45. Similä S, Keinänen S, Kouvalainen K. 1975. Oral antipyretic therapy: Evaluation of benorylate, an ester of acetylsalicylic acid and paracetamol. Eur J Pediatr 121:15-20.
46. Keinänen S, Hietula M, Similä S, Kouvalainen K. 1977. Antipyretic therapy. Comparison of rectal and oral paracetamol. Eur J Clin Pharmacol 12:77-80.
47. Similä S, Kylmämaa T. 1985. Antipyretic effect of tenoxicam and paracetamol in febrile children. Drugs Exp Clin Res 11:731-734.
48. Walson PD, Galletta G, Chomilo F, Braden NJ, Sawyer LA, Scheinbaum ML. 1992. Comparison of multidose ibuprofen and acetaminophen therapy in febrile children. Am J Dis Child 146:626-632.
49. Duhamel JF, Guillot M, Brouard J, Debosque S, Consten L, Dresco I, Perret M, Rezvani Y. 1993. Antipyretic effect of tiaprofenic acid in children. Comparative study with paracetamol. Pediatrie 48:655-659.
50. Van Esch A, Van Steensel-Moll HA, Steyerberg EW, Offringa M, Habbema JD, Derksen-Lubsen G. 1995. Antipyretic efficacy of ibuprofen and acetaminophen in children with febrile seizures. Arch Pediatr Adolesc Med 149:632-637.
51. McIntyre J, Hull D. 1996. Comparing efficacy and tolrability of ibuprofen and paracetamol in fever. Arch Dis Child 74:164-167.
52. Autret E, Reboul-Marty J, Henry-Launois B, Laborde C, Courcier S, Goehrs JM, Languillat G, Launois R. 1997. Evaluation of ibuprofen versus aspirin and paracetamol on efficacy and comfort in children with fever. Eur J Clin Pharmacol 51:367-371.
53. Tréluyer JM, Tonnelier S, d'Athis P, Leclerc B, Jolivet-Landreau I, Pons G. 2001. Antipyretic efficacy of an initial 30-mg/kg loading dose of acetaminophen versus a 15-mg/kg maintenance dose. Pediatrics 108:E73.
54. Autret-Leca E, Gibb IA, Goulder MA. 2007. Ibuprofen versus paracetamol in pediatric fever: Objective and subjective findings from a randomized, blinded study. Curr Med Res Opin 23:2205-2211.
55. Celebi S, Hacimustafaoglu M, Aygun D, Arisoy ES, Karali Y, Akgoz S, Citak Kurt AN, Seringec M. 2009. Antipyretic effect of ketoprofen. Indian J Pediatr 76:287-291.