PARACETAMOL, UM AINE PARTICULAR
Resumo
Este estudo visa fazer uma análise comparativa do paracetamol com a classe de fármacos a qual pertence, os anti-inflamatórios não-esteroidais (AINES) tradicionais. São abordadas as principais diferenças do paracetamol com seugrupo farmacológico, fazendo uma revisão atualizada do seu mecanismo de ação, metabolismo e efeitos tóxicos.Palavras-Chave: paracetamol, anti-inflamatórios não-esteroidais (AINES), antitérmico, analgésico.Referências
BEASLEY, R.; CLAYTON, T.; CRANE, J.; VON MUTIUS, E.; LAI, C.K.W.; MONTEFORT, S.; STEWART, A. Associa-tion between paracetamol use in infancy and childhood, and risk of asthma, rhinoconjunctivitis, and eczema in children aged 6-7 years: analysis from phase three of the isaac programme. The Lancet, v. 372, n. 9643, p. 1039-1048, 2008.
BELTRAMO, M.; STELLA, N.; CALIGNANO, A.; LIN, S. Y.; MAKRIYANNIS, A.; PIOMELLI, D. Functional role of high-affinity anandamide transport, as revealed by selective inhibition. Science, v. 277, p. 1094 -1097, 1997.
BONNEFONT, J.; CHAPUY, E.; CLOTTES, E.; ALLOUI, A.; ESCHALIER, A. Spinal 5-HT1A receptors differentially influence nociceptive processing according to the nature of the noxious stimulus in rats: effect of WAY-100635 on the antinociceptive activities of paracetamol, venlafaxine and 5-HT. Pain, v. 114, p. 482–490, 2005.
BOUTAUD, O.; ARONOFF, D.M.; RICHARDSON, J.H.; MARNETT, L.J.; OATES, J.A. Determinants of the cellular specificity of acetaminophen as an inhibitor of prostaglandin H(2) synthases. Proceedings of the National Acad-emy of Sciences of the United States of America, v. 99, p. 7130 –7135, 2002.
CABALLERO, F.J.; NAVARRETE, C.M.; HESS, S., FIEBICH, B.L.; APPENDINO, G.; MACHO, A.;
MUÑOZ, E.; SANCHO, R. The acetaminophen-derived bioactive N-acylphenolamine AM404 inhib-its NFAT by targeting nuclear regulatory events. Biochemical Pharmacology, v. 73, n. 7, p. 1013-1023,2007.
CHANDRASEKHARAN, N.V.; DAI, H., LAMAR TUREPU ROOS, K.; EVANSON, N.K.; TOMSIK,J.; ELTON, T.S.; SIMMONS, D.L. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: Cloning, structure, and expression. Proceedings of the National Academy of Sciences of the United States of America (PNAS), v. 99, n.21, p. 13926 – 13931, October, 2002.
CHOI, S.S.; LEE, J.K.; SUH, H.W. Antinociceptive profiles of aspirin and acetaminophen in formalin, substance P and glutamate pain models. Brain Research, v. 921, p. 233–239, 2001.
FOOD AND DRUG ADMINISTRATION. Department of Health and Human Services. CFR Parts 201 and 343[Docket No. 1977N–0094L] RIN 0910-AF36 Internal Analgesic, Antipyretic, andAnti-rheumatic Drug Products for Over-the-Counter Human Use; Proposed Amendment of the Tentative Final Monograph.[base de dados na
internet].
Disponível em:http://www.accessdata.fda.gov/scripts/oc/ohrms/frbydocket.cfm
HÖGESTÄTT, E.D.; JÖNSSON, B.A.G.; ERMUND, A.; ANDERSSON, D.A.; BJÖRK, H.; ALEXANDER, J.P.; CRA-VATT, B.F.; BASBAUM, A.I.; ZYGMUNT, P.M. Conversion of Acetaminophen to the Bioactive N-Acylphenolamine AM404 via Fatty Acid Amide Hydrolase-dependent Arachidonic Acid Conjugation in the Nervous System. The Journal of Biological Chemistry, v. 280, n. 36, p. 31405–31412, 2005.
HOWLETT, A.C. Pharmacology of cannabinoid receptors. Annual Review of Pharmacology and Toxicology, v. 35, p. 607– 634, 1995.
LAVONAS, E.J.; REYNOLDS,K.M.; DART, R.C. Therapeutic Acetaminophen Is Not Associated With Liver Injury in Children: A Systematic Review. Pediatrics, v.126, p.1430-1444, 2010
LIAO, H.T.; LEE, H.J.; HO, Y.C.; CHIOU, L.C. Capsaicin in the periaqueductal gray induces analgesia via metabo-tropic glutamate receptor-mediated endocannabinoid retrograde disinhibition. British Journal of Pharmacology, v.163, n. 2, p. 330 – 345, 2011.
MAIONE S, BISOGNO T, DE NOVELLIS V, PALAZZO E, CRISTINO L, et al. Elevation of Endocannabinoid Levels in the Ventrolateral Periaqueductal Grey through Inhibition of Fatty Acid Amide Hydrolase Affects Descending Nociceptive Pathways via Both Cannabinoid Receptor Type 1 and TransientReceptor Potential Vanilloid Type-1 Receptors. Journal of Pharmacology and Experimental Therapeutics, v. 316, p. 969–982, 2006.
MALLET, C.; BARRIÈRE, D.A.; ERMUND, A.; JÖNSSON, B.A.G.; ESCHALIER, A.; ZYGMUNT, P.M.; HÖGESTÄTT, E.D. TRPV1 in brain is involved in acetaminophen-induced antinociception. PLoS one, v. 5, n. 9, p. 1 – 11, 2010.
OUELLET, M.; PERCIVAL, M.D. Mechanism of acetaminophen inhibition of cyclooxygenase isoforms. Archives of Biochemistry and Biophysics, v. 387, p. 273–280, 2001.
PALAZZO E, DE NOVELLIS V, MARABESE I, CUOMO D, ROSSI F, et al. Interaction between vanilloid and gluta-mate receptors in the central modulation of nociception. European Journal of Pharmacology, v. 439, p. 69–75,
2002.
PARANÁ, R; WAKSMAN, J.C. Mecanismos da hepatotoxicidade medicamentosa – Acetaminofen/Paracetamol.
GED gastroenterol. endosc.dig.vol 30(Supl.1):06-47, 2011
PINI, L.A.; SANDRINI, M.; VITALE, G. The antinociceptive action of paracetamol is associated with changes in the serotonergic system in the rat brain. European Journal of Pharmacology, v. 308, p. 31–40, 1996. PIOMELLI, D.; GIUFFRIDA, A.; CALIGNANO, A.; RODRIGUEZ DE FONSECA, F. Review: The endocannabinoid system as a target for therapeutic drugs. Trends in Pharmacological Sciences, v. 21, n. 6, p. 2218 – 2224, 2000.
POLSON, J.; LEE, W.M. The management of acute liver failure. Hepatology, p. 1179-1197, 2005.
RANG, H.; DALE, M.M.; RITTER, J.; FLOWER, R.; HENDERSON, G. Rang & Dale Farmacologia. 7 ed. Rio de Janeiro: Elsevier, 2011.
REZENDE, R.M.; FRANÇA, D.S.; MENEZES, G.B.; REIS, W.G.P. dos; BAKHLE, Y.S.; FRANCISCHI, J.N. Different mechanisms underlie the analgesic actions of paracetamol and dipyrone in a rat model of inflammatory pain. Br J Pharmacol., v.153, n.4, p.760-768, feb., 2008.
RUMACK, B.H.; MATTHEW, H. Acetaminophen Poisoning and Toxicity. Pediatrics, v. 55, n. 6, p. 871-876, 1975. SOCIEDADE BRASILEIRA DE HEPATOLOGIA. GED Gastroenterologia Endoscopia Digestiva. Rev. Suplemento Hepatotoxicidade, v.30, supl.1, p. 6-47, 2011.
STAROWICZ, K.; MAIONE, S.; CRISTINO, L.; PALAZZO, E.; MARABESE, I. ET AL. Tonic endovanilloid facilitation of glutamate release in brainstem descending antinociceptive pathways. The Journal of Neuroscience, v. 27, p.13739–13749, 2007.
TOTH A, BOCZAN J, KEDEI N, LIZANECZ E, BAGI Z, et al. Expression and distribution of vanilloid receptor 1 (TRPV1) in the adult rat brain. Brain Res Mol Brain Res., v. 135, p.162–168, 2005.
VANE, J.R.; BOTTING, R.M. A better understanding of anti-inflammatory drugs based on isoforms of cyclooxy-genase (COX-1 and COX-2). Advances in Prostaglandin, Thromboxane and Leukotriene Research, v. 23, p.41-48,1995.
WANNMACHER, L; FERREIRA, M.B.C. Paracetamol versus Dipirona: como mensurar o risco?Uso racional de medicamento. v. 2, n.5, 2005.
WARNER, T.D.; MITCHELL, J.A. Cyclooxygenase-3 (COX-3): Filling in the gaps toward a COX continuum? Pro-ceedings of the National Academy of Sciences of the United States of America, v. 99, p.13371-13373, 2002.
BELTRAMO, M.; STELLA, N.; CALIGNANO, A.; LIN, S. Y.; MAKRIYANNIS, A.; PIOMELLI, D. Functional role of high-affinity anandamide transport, as revealed by selective inhibition. Science, v. 277, p. 1094 -1097, 1997.
BONNEFONT, J.; CHAPUY, E.; CLOTTES, E.; ALLOUI, A.; ESCHALIER, A. Spinal 5-HT1A receptors differentially influence nociceptive processing according to the nature of the noxious stimulus in rats: effect of WAY-100635 on the antinociceptive activities of paracetamol, venlafaxine and 5-HT. Pain, v. 114, p. 482–490, 2005.
BOUTAUD, O.; ARONOFF, D.M.; RICHARDSON, J.H.; MARNETT, L.J.; OATES, J.A. Determinants of the cellular specificity of acetaminophen as an inhibitor of prostaglandin H(2) synthases. Proceedings of the National Acad-emy of Sciences of the United States of America, v. 99, p. 7130 –7135, 2002.
CABALLERO, F.J.; NAVARRETE, C.M.; HESS, S., FIEBICH, B.L.; APPENDINO, G.; MACHO, A.;
MUÑOZ, E.; SANCHO, R. The acetaminophen-derived bioactive N-acylphenolamine AM404 inhib-its NFAT by targeting nuclear regulatory events. Biochemical Pharmacology, v. 73, n. 7, p. 1013-1023,2007.
CHANDRASEKHARAN, N.V.; DAI, H., LAMAR TUREPU ROOS, K.; EVANSON, N.K.; TOMSIK,J.; ELTON, T.S.; SIMMONS, D.L. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: Cloning, structure, and expression. Proceedings of the National Academy of Sciences of the United States of America (PNAS), v. 99, n.21, p. 13926 – 13931, October, 2002.
CHOI, S.S.; LEE, J.K.; SUH, H.W. Antinociceptive profiles of aspirin and acetaminophen in formalin, substance P and glutamate pain models. Brain Research, v. 921, p. 233–239, 2001.
FOOD AND DRUG ADMINISTRATION. Department of Health and Human Services. CFR Parts 201 and 343[Docket No. 1977N–0094L] RIN 0910-AF36 Internal Analgesic, Antipyretic, andAnti-rheumatic Drug Products for Over-the-Counter Human Use; Proposed Amendment of the Tentative Final Monograph.[base de dados na
internet].
Disponível em:http://www.accessdata.fda.gov/scripts/oc/ohrms/frbydocket.cfm
HÖGESTÄTT, E.D.; JÖNSSON, B.A.G.; ERMUND, A.; ANDERSSON, D.A.; BJÖRK, H.; ALEXANDER, J.P.; CRA-VATT, B.F.; BASBAUM, A.I.; ZYGMUNT, P.M. Conversion of Acetaminophen to the Bioactive N-Acylphenolamine AM404 via Fatty Acid Amide Hydrolase-dependent Arachidonic Acid Conjugation in the Nervous System. The Journal of Biological Chemistry, v. 280, n. 36, p. 31405–31412, 2005.
HOWLETT, A.C. Pharmacology of cannabinoid receptors. Annual Review of Pharmacology and Toxicology, v. 35, p. 607– 634, 1995.
LAVONAS, E.J.; REYNOLDS,K.M.; DART, R.C. Therapeutic Acetaminophen Is Not Associated With Liver Injury in Children: A Systematic Review. Pediatrics, v.126, p.1430-1444, 2010
LIAO, H.T.; LEE, H.J.; HO, Y.C.; CHIOU, L.C. Capsaicin in the periaqueductal gray induces analgesia via metabo-tropic glutamate receptor-mediated endocannabinoid retrograde disinhibition. British Journal of Pharmacology, v.163, n. 2, p. 330 – 345, 2011.
MAIONE S, BISOGNO T, DE NOVELLIS V, PALAZZO E, CRISTINO L, et al. Elevation of Endocannabinoid Levels in the Ventrolateral Periaqueductal Grey through Inhibition of Fatty Acid Amide Hydrolase Affects Descending Nociceptive Pathways via Both Cannabinoid Receptor Type 1 and TransientReceptor Potential Vanilloid Type-1 Receptors. Journal of Pharmacology and Experimental Therapeutics, v. 316, p. 969–982, 2006.
MALLET, C.; BARRIÈRE, D.A.; ERMUND, A.; JÖNSSON, B.A.G.; ESCHALIER, A.; ZYGMUNT, P.M.; HÖGESTÄTT, E.D. TRPV1 in brain is involved in acetaminophen-induced antinociception. PLoS one, v. 5, n. 9, p. 1 – 11, 2010.
OUELLET, M.; PERCIVAL, M.D. Mechanism of acetaminophen inhibition of cyclooxygenase isoforms. Archives of Biochemistry and Biophysics, v. 387, p. 273–280, 2001.
PALAZZO E, DE NOVELLIS V, MARABESE I, CUOMO D, ROSSI F, et al. Interaction between vanilloid and gluta-mate receptors in the central modulation of nociception. European Journal of Pharmacology, v. 439, p. 69–75,
2002.
PARANÁ, R; WAKSMAN, J.C. Mecanismos da hepatotoxicidade medicamentosa – Acetaminofen/Paracetamol.
GED gastroenterol. endosc.dig.vol 30(Supl.1):06-47, 2011
PINI, L.A.; SANDRINI, M.; VITALE, G. The antinociceptive action of paracetamol is associated with changes in the serotonergic system in the rat brain. European Journal of Pharmacology, v. 308, p. 31–40, 1996. PIOMELLI, D.; GIUFFRIDA, A.; CALIGNANO, A.; RODRIGUEZ DE FONSECA, F. Review: The endocannabinoid system as a target for therapeutic drugs. Trends in Pharmacological Sciences, v. 21, n. 6, p. 2218 – 2224, 2000.
POLSON, J.; LEE, W.M. The management of acute liver failure. Hepatology, p. 1179-1197, 2005.
RANG, H.; DALE, M.M.; RITTER, J.; FLOWER, R.; HENDERSON, G. Rang & Dale Farmacologia. 7 ed. Rio de Janeiro: Elsevier, 2011.
REZENDE, R.M.; FRANÇA, D.S.; MENEZES, G.B.; REIS, W.G.P. dos; BAKHLE, Y.S.; FRANCISCHI, J.N. Different mechanisms underlie the analgesic actions of paracetamol and dipyrone in a rat model of inflammatory pain. Br J Pharmacol., v.153, n.4, p.760-768, feb., 2008.
RUMACK, B.H.; MATTHEW, H. Acetaminophen Poisoning and Toxicity. Pediatrics, v. 55, n. 6, p. 871-876, 1975. SOCIEDADE BRASILEIRA DE HEPATOLOGIA. GED Gastroenterologia Endoscopia Digestiva. Rev. Suplemento Hepatotoxicidade, v.30, supl.1, p. 6-47, 2011.
STAROWICZ, K.; MAIONE, S.; CRISTINO, L.; PALAZZO, E.; MARABESE, I. ET AL. Tonic endovanilloid facilitation of glutamate release in brainstem descending antinociceptive pathways. The Journal of Neuroscience, v. 27, p.13739–13749, 2007.
TOTH A, BOCZAN J, KEDEI N, LIZANECZ E, BAGI Z, et al. Expression and distribution of vanilloid receptor 1 (TRPV1) in the adult rat brain. Brain Res Mol Brain Res., v. 135, p.162–168, 2005.
VANE, J.R.; BOTTING, R.M. A better understanding of anti-inflammatory drugs based on isoforms of cyclooxy-genase (COX-1 and COX-2). Advances in Prostaglandin, Thromboxane and Leukotriene Research, v. 23, p.41-48,1995.
WANNMACHER, L; FERREIRA, M.B.C. Paracetamol versus Dipirona: como mensurar o risco?Uso racional de medicamento. v. 2, n.5, 2005.
WARNER, T.D.; MITCHELL, J.A. Cyclooxygenase-3 (COX-3): Filling in the gaps toward a COX continuum? Pro-ceedings of the National Academy of Sciences of the United States of America, v. 99, p.13371-13373, 2002.
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01-12-2016
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