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[PMID]:28612633
[Au] Autor:Doggrell SA
[Ad] Endereço:a Faculty of Health , Queensland University of Technology , Brisbane , Australia.
[Ti] Título:Granisetron in the treatment of chemotherapy-induced nausea and vomiting (CINV) - is there still a role after comparison with palonosetron?
[So] Source:Expert Opin Pharmacother;18(10):1019-1026, 2017 Jul.
[Is] ISSN:1744-7666
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Chemotherapy-induced nausea and vomiting (CINV) has a negative impact on the lives of subjects receiving chemotherapy. In 2009, the second generation 5-HT -receptor antagonist, palonosetron, which is longer-acting than granisetron, was shown, as part of dual therapy with dexamethasone, to be superior to intravenous granisetron in the delayed phase of CINV. Area covered: In an attempt to maintain plasma levels of granisetron during the delayed phase of CINV, longer-acting preparations of granisetron have been manufactured. In addition to comparing intravenous/oral granisetron with palonosetron, this review considers the new longer-acting preparations of granisetron (transdermal and subcutanous) with emphasis on whether they are effective in the delayed phase of CINV. Expert opinion: Comparison of intravenous/oral granisetron and palonosetron, as part of triple therapy against the delayed phase of CINV, do not give clear-cut results as to non-inferiority or superiority of either agent. Subcutaneous granisetron is more convenient to use than transdermal granisetron, and has been shown to be non-inferior to palonosetron, as part of dual therapy, in the treatment of the acute and delayed phases of CINV. At present, it seems likely that there will be ongoing roles for intravenous and subcutaneous granisetron in CINV, but further data is required to ascertain the future of transdermal granisetron.
[Mh] Termos MeSH primário: Antieméticos/uso terapêutico
Antineoplásicos/efeitos adversos
Náusea/tratamento farmacológico
Vômito/induzido quimicamente
Vômito/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Cutânea
Antieméticos/farmacocinética
Antieméticos/farmacologia
Ensaios Clínicos como Assunto
Dexametasona/farmacocinética
Dexametasona/farmacologia
Dexametasona/uso terapêutico
Granisetron/farmacocinética
Granisetron/farmacologia
Granisetron/uso terapêutico
Seres Humanos
Isoquinolinas/farmacocinética
Isoquinolinas/farmacologia
Isoquinolinas/uso terapêutico
Náusea/induzido quimicamente
Quinuclidinas/farmacocinética
Quinuclidinas/farmacologia
Quinuclidinas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antiemetics); 0 (Antineoplastic Agents); 0 (Isoquinolines); 0 (Quinuclidines); 5D06587D6R (palonosetron); 7S5I7G3JQL (Dexamethasone); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170822
[Lr] Data última revisão:
170822
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170615
[St] Status:MEDLINE
[do] DOI:10.1080/14656566.2017.1342809


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[PMID]:28211304
[Au] Autor:Ahmed YM; Messiha BA; Abo-Saif AA
[Ad] Endereço:a Department of Pharmacology and Toxicology, Faculty of Pharmacy , Nahda University , Beni-Suef , Egypt.
[Ti] Título:Granisetron and carvedilol can protect experimental rats againstadjuvant-induced arthritis.
[So] Source:Immunopharmacol Immunotoxicol;39(2):97-104, 2017 Apr.
[Is] ISSN:1532-2513
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Rheumatoid arthritis (RA), a disabling autoimmune disorder of the joints as well as other organs, affects about 1% of population. Unfortunately, all current treatments of RA cause severe gastrointestinal, renal and other complications. OBJECTIVE: We aimed to evaluate the possible antiarthritic effects of a serotonin 5-HT receptor blocker, granisetron, and a nonselective adrenergic receptor blocker, carvedilol, on complete Freund's adjuvant-induced RA in adult female albino rats. MATERIALS AND METHODS: Rats were allocated into a normal control group, an arthritis control group, two reference treatment groups receiving dexamethasone (1.5 mg/kg/day) and methotrexate (1 mg/kg/day), and two treatment groups receiving granisetron (2.5 mg/kg/day) and carvedilol (10 mg/kg/day). Serum-specific rheumatoid, immunological, inflammatory and oxidative stress biomarkers were assessed. A confirmatory histopathological study on joints and spleens was performed. RESULTS: Granisetron administration significantly improved all the measured biomarkers, with the values of rheumatoid factor, matrix metalloproteinase-3, cartilage oligomeric matrix protein, immunoglobulin G, antinuclear antibody and myeloperoxidase being restored back to normal levels. Carvedilol administration significantly improved all biomarkers, with serum MPO value restored back to normal levels. DISCUSSION AND CONCLUSIONS: Serotonin 5-HT receptor blockers and adrenergic receptor blockers, represented by granisetron and carvedilol, may represent new promising protective strategies against RA, at least owing to immune-modulator, anti-inflammatory and antioxidant potentials.
[Mh] Termos MeSH primário: Artrite Experimental/tratamento farmacológico
Carbazóis/farmacologia
Granisetron/farmacologia
Propanolaminas/farmacologia
[Mh] Termos MeSH secundário: Animais
Artrite Experimental/sangue
Artrite Experimental/imunologia
Biomarcadores/sangue
Proteína de Matriz Oligomérica de Cartilagem/sangue
Proteína de Matriz Oligomérica de Cartilagem/imunologia
Feminino
Imunoglobulina G/sangue
Imunoglobulina G/imunologia
Metaloproteinase 3 da Matriz/sangue
Metaloproteinase 3 da Matriz/imunologia
Peroxidase/sangue
Peroxidase/imunologia
Ratos
Ratos Wistar
Fator Reumatoide/sangue
Fator Reumatoide/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (Carbazoles); 0 (Cartilage Oligomeric Matrix Protein); 0 (Immunoglobulin G); 0 (Propanolamines); 0K47UL67F2 (carvedilol); 9009-79-4 (Rheumatoid Factor); EC 1.11.1.7 (Peroxidase); EC 3.4.24.17 (Matrix Metalloproteinase 3); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170321
[Lr] Data última revisão:
170321
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170218
[St] Status:MEDLINE
[do] DOI:10.1080/08923973.2017.1286502


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[PMID]:28137449
[Au] Autor:Ruepp MD; Wei H; Leuenberger M; Lochner M; Thompson AJ
[Ad] Endereço:Department of Chemistry and Biochemistry, University of Bern, Bern, Switzerland.
[Ti] Título:The binding orientations of structurally-related ligands can differ; A cautionary note.
[So] Source:Neuropharmacology;119:48-61, 2017 Jun.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Crystal structures can identify ligand-receptor interactions and assist the development of novel therapeutics, but experimental challenges sometimes necessitate the use of homologous proteins. Tropisetron is an orthosteric ligand at both 5-HT and α7 nACh receptors and its binding orientation has been determined in the structural homologue AChBP (pdbid: 2WNC). Co-crystallisation with a structurally-related ligand, granisetron, reveals an almost identical orientation (pdbid; 2YME). However, there is a >1000-fold difference in the affinity of tropisetron at 5-HT versus α7 nACh receptors, and α7 nACh receptors do not bind granisetron. These striking pharmacological differences prompt questions about which receptor the crystal structures most closely represent and whether the ligand orientations are correct. Here we probe the binding orientation of tropisetron and granisetron at 5-HT receptors by in silico modelling and docking, radioligand binding on cysteine-substituted 5-HT receptor mutants transiently expressed in HEK 293 cells, and synthetic modification of the ligands. For 15 of the 23 cysteine substitutions, the effects on tropisetron and granisetron were different. Structure-activity relationships on synthesised derivatives of both ligands were also consistent with different orientations, revealing that contrary to the crystallographic evidence from AChBP, the two ligands adopt different orientations in the 5-HT receptor binding site. Our results show that even quite structurally similar molecules can adopt different orientations in the same binding site, and that caution may be needed when using homologous proteins to predict ligand binding.
[Mh] Termos MeSH primário: Ligação Competitiva/efeitos dos fármacos
Modelos Moleculares
Receptores 5-HT3 de Serotonina/química
Receptores 5-HT3 de Serotonina/genética
[Mh] Termos MeSH secundário: Sítios de Ligação/efeitos dos fármacos
Ligação Competitiva/genética
Cristalografia por Raios X
Granisetron/química
Granisetron/farmacologia
Células HEK293
Seres Humanos
Indóis/química
Indóis/farmacologia
Ligantes
Estrutura Molecular
Mutação/genética
Antagonistas da Serotonina/farmacologia
Relação Estrutura-Atividade
Trítio/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indoles); 0 (Ligands); 0 (Receptors, Serotonin, 5-HT3); 0 (Serotonin Antagonists); 10028-17-8 (Tritium); 6I819NIK1W (tropisetron); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170201
[St] Status:MEDLINE


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[PMID]:27671323
[Au] Autor:Pandhare A; Pappu AS; Wilms H; Blanton MP; Jansen M
[Ad] Endereço:Department of Cell Physiology and Molecular Biophysics, School of Medicine, Texas Tech University Health Sciences Center, Lubbock, TX, USA; Center for Membrane Protein Research, School of Medicine, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USA. Electronic address: akash.pandha
[Ti] Título:The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors.
[So] Source:Neuropharmacology;113(Pt A):89-99, 2017 Feb.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The FDA-approved antidepressant and smoking cessation drug bupropion is known to inhibit dopamine and norepinephrine reuptake transporters, as well as nicotinic acetylcholine receptors (nAChRs) which are cation-conducting members of the Cys-loop superfamily of ion channels, and more broadly pentameric ligand-gated ion channels (pLGICs). In the present study, we examined the ability of bupropion and its primary metabolite hydroxybupropion to block the function of cation-selective serotonin type 3A receptors (5-HT Rs), and further characterized bupropion's pharmacological effects at these receptors. Mouse 5-HT Rs were heterologously expressed in HEK-293 cells or Xenopus laevis oocytes for equilibrium binding studies. In addition, the latter expression system was utilized for functional studies by employing two-electrode voltage-clamp recordings. Both bupropion and hydroxybupropion inhibited serotonin-gated currents from 5-HT Rs reversibly and dose-dependently with inhibitory potencies of 87 µM and 112 µM, respectively. Notably, the measured IC value for hydroxybupropion is within its therapeutically-relevant concentrations. The blockade by bupropion was largely non-competitive and non-use-dependent. Unlike its modulation at cation-selective pLGICs, bupropion displayed no significant inhibition of the function of anion-selective pLGICs. In summary, our results demonstrate allosteric blockade by bupropion of the 5-HT R. Importantly, given the possibility that bupropion's major active metabolite may achieve clinically relevant concentrations in the brain, our novel findings delineate a not yet identified pharmacological principle underlying its antidepressant effect.
[Mh] Termos MeSH primário: Antidepressivos de Segunda Geração/farmacocinética
Bupropiona/análogos & derivados
Bupropiona/farmacocinética
Receptores 5-HT3 de Serotonina/metabolismo
Antagonistas do Receptor 5-HT3 de Serotonina/farmacocinética
Serotonina/metabolismo
[Mh] Termos MeSH secundário: Regulação Alostérica
Animais
Relação Dose-Resposta a Droga
Granisetron/farmacocinética
Células HEK293
Seres Humanos
Camundongos
Oócitos/efeitos dos fármacos
Oócitos/metabolismo
Serotonina/análise
Serotonina/farmacocinética
Xenopus laevis
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents, Second-Generation); 0 (Htr3a protein, mouse); 0 (Receptors, Serotonin, 5-HT3); 0 (Serotonin 5-HT3 Receptor Antagonists); 0 (hydroxybupropion); 01ZG3TPX31 (Bupropion); 333DO1RDJY (Serotonin); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170902
[Lr] Data última revisão:
170902
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE


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[PMID]:28061543
[Au] Autor:Yang LQ; Sun XC; Qin SK; Chen YX; Zhang HL; Cheng Y; Chen ZD; Shi JH; Wu Q; Bai YX; Han BH; Liu W; Ouyang XN; Liu JW; Zhang ZH; Li YQ; Xu JM; Yu SY
[Ad] Endereço:Department of Clinical Medicine, Nanjing Medical University, Nanjing 211166, China; Department of Medical Oncology, Nanjing Bayi Hospital, Nanjing 210002, China.
[Ti] Título:Transdermal granisetron for the prevention of nausea and vomiting following moderately or highly emetogenic chemotherapy in Chinese patients: a randomized, double-blind, phase III study.
[So] Source:Chin Clin Oncol;5(6):79, 2016 Dec.
[Is] ISSN:2304-3873
[Cp] País de publicação:China
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The granisetron transdermal delivery system (GTDS) has been demonstrated effectiveness in the control of chemotherapy-induced nausea and vomiting (CINV) in previous studies. This is the first phase III study to evaluate the efficacy and tolerability of GTDS in patients receiving moderately emetogenic chemotherapy (MEC) or highly emetogenic chemotherapy (HEC) in China. METHODS: A total of 313 patients were randomized into the GTDS group (one transdermal granisetron patch, 7 days) or the oral granisetron group (granisetron oral 2 mg/day, ≥2 days). The primary endpoint was the percentage of patients achieving complete control (CC) from chemotherapy initiation until 24 h after final administration (PEEP). Chi-square test and Fisher's exact test were used for statistical analysis. RESULTS: Two hundred eighty-one patients were included in the per protocol analysis. During PEEP, CC was achieved by 67 (47.52%) patients in the GTDS group and 83 (59.29%) patients in the oral granisetron group. There was no statistical significance between the groups (P=0.0559). However, the difference of the CC percentage mainly occurred on the first day of chemotherapy between the groups. The CC was 70.13% on day 1 in the GTDS group, which was significantly lower than that of 91.03% in the oral granisetron group in the full analysis set. In the following days of chemotherapy, the CC was similar between the groups. In terms of cisplatin-contained regimen and female, there was statistical significance between the groups. Both treatments were well tolerated and safe. The most common adverse event was constipation. CONCLUSIONS: GTDS provided effective and well-tolerated control of CINV in Chinese patients, especially to non-cisplatin-contained regimen.
[Mh] Termos MeSH primário: Antieméticos/administração & dosagem
Antineoplásicos/efeitos adversos
Granisetron/administração & dosagem
Náusea/prevenção & controle
Vômito/prevenção & controle
[Mh] Termos MeSH secundário: Administração Cutânea
Adolescente
Adulto
Idoso
Antineoplásicos/uso terapêutico
Método Duplo-Cego
Feminino
Seres Humanos
Masculino
Meia-Idade
Náusea/tratamento farmacológico
Vômito/tratamento farmacológico
Adulto Jovem
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE III; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antiemetics); 0 (Antineoplastic Agents); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170331
[Lr] Data última revisão:
170331
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170108
[St] Status:MEDLINE
[do] DOI:10.21037/cco.2016.12.04


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[PMID]:28002447
[Au] Autor:Louca Jounger S; Christidis N; Hedenberg-Magnusson B; List T; Svensson P; Schalling M; Ernberg M
[Ad] Endereço:Department of Dental Medicine, Section of Orofacial Pain and Jaw Function, Karolinska Institutet, and the Scandinavian Center for Orofacial Neurosciences (SCON), Huddinge, Huddinge, Sweden.
[Ti] Título:Influence of Polymorphisms in the HTR3A and HTR3B Genes on Experimental Pain and the Effect of the 5-HT3 Antagonist Granisetron.
[So] Source:PLoS One;11(12):e0168703, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to investigate experimentally if 5-HT3 single nucleotide polymorphisms (SNP) contribute to pain perception and efficacy of the 5-HT3-antagonist granisetron and sex differences. Sixty healthy participants were genotyped regarding HTR3A (rs1062613) and HTR3B (rs1176744). First, pain was induced by bilateral hypertonic saline injections (HS, 5.5%, 0.2 mL) into the masseter muscles. Thirty min later the masseter muscle on one side was pretreated with 0.5 mL granisetron (1 mg/mL) and on the other side with 0.5 mL placebo (isotonic saline) followed by another HS injection (0.2 mL). Pain intensity, pain duration, pain area and pressure pain thresholds (PPTs) were assessed after each injection. HS evoked moderate pain, with higher intensity in the women (P = 0.023), but had no effect on PPTs. None of the SNPs influenced any pain variable in general, but compared to men, the pain area was larger in women carrying the C/C (HTR3A) (P = 0.015) and pain intensity higher in women with the A/C alleles (HTR3B) (P = 0.019). Pre-treatment with granisetron reduced pain intensity, duration and area to a lesser degree in women (P < 0.05), but the SNPs did not in general influence the efficacy of granisetron. Women carrying the C/T & T/T (HTR3A) genotype had less reduction of pain intensity (P = 0.041) and area (P = 0.005), and women with the C/C genotype (HTR3B) had less reduction of pain intensity (P = 0.030), duration (P = 0.030) and area compared to men (P = 0.017). In conclusion, SNPs did not influence experimental muscle pain or the effect of granisetron on pain variables in general, but there were some sex differences in pain variables that seem to be influenced by genotypes. However, due to the small sample size further research is needed before any firm conclusions can be drawn.
[Mh] Termos MeSH primário: Granisetron/uso terapêutico
Mialgia/tratamento farmacológico
Mialgia/genética
Receptores 5-HT3 de Serotonina/genética
Antagonistas do Receptor 5-HT3 de Serotonina/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Alelos
Método Duplo-Cego
Feminino
Genótipo
Voluntários Saudáveis
Seres Humanos
Masculino
Mialgia/induzido quimicamente
Mialgia/prevenção & controle
Limiar da Dor/fisiologia
Efeito Placebo
Polimorfismo de Nucleotídeo Único
Fatores Sexuais
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (HTR3A protein, human); 0 (HTR3B protein, human); 0 (Receptors, Serotonin, 5-HT3); 0 (Serotonin 5-HT3 Receptor Antagonists); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170703
[Lr] Data última revisão:
170703
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161222
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0168703


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[PMID]:27915445
[Au] Autor:Deeks ED
[Ad] Endereço:Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand. demail@springer.com.
[Ti] Título:Granisetron Extended-Release Injection: A Review in Chemotherapy-Induced Nausea and Vomiting.
[So] Source:Drugs;76(18):1779-1786, 2016 Dec.
[Is] ISSN:1179-1950
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:An extended-release (ER) subcutaneously injectable formulation of the first-generation 5-HT receptor antagonist granisetron is now available in the USA (Sustol ), where it is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) following moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide combination chemotherapy regimens in adults. Granisetron ER is administered as a single subcutaneous injection and uses an erosion-controlled drug-delivery system to allow prolonged granisetron release. Primary endpoint data from phase III studies after an initial cycle of chemotherapy indicate that, when used as part of an antiemetic regimen, granisetron ER injection is more effective than intravenous ondansetron in preventing delayed CINV following highly emetogenic chemotherapy (HEC); is noninferior to intravenous palonosetron in preventing both acute CINV following MEC or HEC and delayed CINV following MEC; and is similar, but not superior, to palonosetron in preventing delayed CINV following HEC. The benefits of granisetron ER were seen in various patient subgroups, including those receiving anthracycline plus cyclophosphamide-based HEC, and (in an extension of one of the studies) over multiple MEC or HEC cycles. Granisetron ER injection is generally well tolerated, with an adverse event profile similar to that of ondansetron or palonosetron. Thus, granisetron ER injection expands the options for preventing both acute and delayed CINV in adults with cancer receiving MEC or anthracycline plus cyclophosphamide-based HEC.
[Mh] Termos MeSH primário: Antieméticos/administração & dosagem
Preparações de Ação Retardada/administração & dosagem
Granisetron/administração & dosagem
Náusea/tratamento farmacológico
Vômito/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/efeitos adversos
Antineoplásicos/uso terapêutico
Seres Humanos
Injeções/métodos
Náusea/induzido quimicamente
Neoplasias/tratamento farmacológico
Vômito/induzido quimicamente
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antiemetics); 0 (Antineoplastic Agents); 0 (Delayed-Action Preparations); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171114
[Lr] Data última revisão:
171114
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161205
[St] Status:MEDLINE


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[PMID]:27895421
[Au] Autor:Nacci C; Fanelli M; Potenza MA; Leo V; Montagnani M; De Salvia MA
[Ad] Endereço:Carmela Nacci, Maria Assunta Potenza, Valentina Leo, Monica Montagnani, Maria Antonietta De Salvia, Department of Biomedical Sciences and Human Oncology - Pharmacology Section, Medical School, University of Bari "Aldo Moro", Piazza G. Cesare, 70124 Bari, Italy.
[Ti] Título:Carbon monoxide contributes to the constipating effects of granisetron in rat colon.
[So] Source:World J Gastroenterol;22(42):9333-9345, 2016 Nov 14.
[Is] ISSN:2219-2840
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:AIM: To investigate the mechanisms underlying the potential contribution of the heme oxygenase/carbon monoxide (HO/CO) pathway in the constipating effects of granisetron. METHODS: For studies, gastrointestinal motility was evaluated in male rats acutely treated with granisetron [25, 50, 75 µg/kg/subcutaneous (sc)], zinc protoporphyrin IX [ZnPPIX, 50 µg/kg/intraperitoneal (ip)] and hemin (50 µmol/L/kg/ip), alone or in combination. For studies, the contractile neurogenic response to electrical field stimulation (EFS, 3, 5, 10 Hz, 14 V, 1 ms, pulse trains lasting 10 s), as well as the contractile myogenic response to acetylcholine (ACh, 0.1-100 µmol/L) were evaluated on colon specimens incubated with granisetron (3 µmol/L, 15 min), ZnPPIX (10 µmol/L, 60 min) or CO-releasing molecule-3 (CORM-3, 100, 200, 400 µmol/L) alone or in combination. These experiments were performed under co-treatment with or without atropine (3 µmol/L, a muscarinic receptor antagonist) or N -nitro-L-Arginine (L-NNA, 100 µmol/L, a nitric oxide synthase inhibitor). RESULTS: Administration of granisetron (50, 75 µg/kg) significantly increased the time to first defecation ( = 0.045 vehicle-treated rats), clearly suggesting a constipating effect of this drug. Although administration of ZnPPIX or hemin alone had no effect on this gastrointestinal motility parameter, ZnPPIX co-administered with granisetron abolished the granisetron-induced constipation. On the other hand, co-administration of hemin and granisetron did not modify the increased constipation observed under granisetron alone. When administered , granisetron alone (3 µmol/L) did not significantly modify the colon's contractile response to either EFS or ACh. Incubation with ZnPPIX alone (10 µmol/L) significantly reduced the colon's contractile response to EFS ( = 0.016) but had no effect on contractile response to ACh. Co-administration of ZnPPIX and atropine (3 µmol/L) abolished the ZnPPIX-mediated decrease in contractile response to EFS. Conversely, incubation with CORM-3 (400 µmol/L) alone increased both the contractile response to EFS at 10 Hz (10 Hz: 71.02 ± 19.16 116.25 ± 53.70, = 0.01) and the contractile response to ACh (100 µmol/L) ( = 0.012). Co-administration of atropine abolished the CORM-3-mediated effects on the EFS-mediated response. When granisetron was co-incubated with ZnPPIX, the ZnPPIX-mediated decrease in colon contractile response to EFS was lost. On the other hand, co-incubation of granisetron and CORM-3 (400 µmol/L) further increased the colon's contractile response to EFS (at 5 Hz: = 0.007; at 10 Hz: = 0.001) and to ACh (ACh 10 µmol/L: = 0.001; ACh 100 µmol/L: = 0.001) elicited by CORM-3 alone. L-NNA co-administered with granisetron and CORM-3 abolished the potentiating effect of CORM-3 on granisetron on both the EFS-induced and ACh-induced contractile response. CONCLUSION: Taken together, findings from and studies suggest that the HO/CO pathway is involved in the constipating effects of granisetron.
[Mh] Termos MeSH primário: Monóxido de Carbono/metabolismo
Colo/efeitos dos fármacos
Constipação Intestinal/induzido quimicamente
Defecação/efeitos dos fármacos
Motilidade Gastrointestinal/efeitos dos fármacos
Granisetron/toxicidade
Antagonistas da Serotonina/toxicidade
[Mh] Termos MeSH secundário: Acetilcolina/farmacologia
Animais
Colo/metabolismo
Colo/fisiopatologia
Constipação Intestinal/metabolismo
Constipação Intestinal/fisiopatologia
Constipação Intestinal/prevenção & controle
Relação Dose-Resposta a Droga
Estimulação Elétrica
Heme Oxigenase (Desciclizante)/metabolismo
Hemina/farmacologia
Técnicas In Vitro
Masculino
Compostos Organometálicos/farmacologia
Protoporfirinas/farmacologia
Ratos Sprague-Dawley
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Organometallic Compounds); 0 (Protoporphyrins); 0 (Serotonin Antagonists); 0 (tricarbonylchloro(glycinato)ruthenium(II)); 15442-64-5 (zinc protoporphyrin); 743LRP9S7N (Hemin); 7U1EE4V452 (Carbon Monoxide); EC 1.14.14.18 (Heme Oxygenase (Decyclizing)); N9YNS0M02X (Acetylcholine); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170424
[Lr] Data última revisão:
170424
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161130
[St] Status:MEDLINE


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[PMID]:27856931
[Au] Autor:Zhou C; Zhu Y; Liu Z; Ruan L
[Ad] Endereço:1 Department of Anesthesiology, Affiliated Tumor Hospital of Guangxi Medical University, Nanning 530021, China.
[Ti] Título:5-HT3 receptor antagonists for the prevention of postoperative shivering: a meta-analysis.
[So] Source:J Int Med Res;44(6):1174-1181, 2016 Dec.
[Is] ISSN:1473-2300
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Objective We evaluated the efficacy of 5-HT3 receptor antagonists for the prevention of postoperative shivering. Methods We searched PubMed, the Cochrane Library, EMBASE and Web of Knowledge to find randomized controlled trials (RCT) of 5-HT3 receptor antagonists for the prevention of postoperative shivering. Two researchers independently screened studies, extracted data, and assessed quality in accordance with the inclusion and exclusion criteria, and then conducted a meta-analysis using RevMan 5.2. Results Ultimately, 14 RCTs that included 980 patients were included in the analysis. We found that: 1) the incidence of shivering was significantly lower in 5-HT3 groups than placebo groups (relative risk, [RR] = 0.48, 95% confidence interval [CI] 0.40 - 0.58); 2) there was no significant difference in the incidence of shivering between 5-HT3 groups and meperidine groups (RR = 0.89, 95% CI 0.60 - 1.34). Conclusion 5-HT3 receptor antagonists appear to prevent postoperative shivering, with a broadly comparable efficacy to meperidine.
[Mh] Termos MeSH primário: Complicações Pós-Operatórias/prevenção & controle
Receptores 5-HT3 de Serotonina/metabolismo
Antagonistas do Receptor 5-HT3 de Serotonina/uso terapêutico
Tremor por Sensação de Frio/efeitos dos fármacos
Procedimentos Cirúrgicos Operatórios/efeitos adversos
[Mh] Termos MeSH secundário: Analgésicos Opioides/uso terapêutico
Granisetron/uso terapêutico
Seres Humanos
Indóis/uso terapêutico
Isoquinolinas/uso terapêutico
Meperidina/uso terapêutico
Ondansetron/uso terapêutico
Complicações Pós-Operatórias/fisiopatologia
Período Pós-Operatório
Quinuclidinas/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Tremor por Sensação de Frio/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Indoles); 0 (Isoquinolines); 0 (Quinuclidines); 0 (Receptors, Serotonin, 5-HT3); 0 (Serotonin 5-HT3 Receptor Antagonists); 4AF302ESOS (Ondansetron); 5D06587D6R (palonosetron); 6I819NIK1W (tropisetron); 9E338QE28F (Meperidine); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171004
[Lr] Data última revisão:
171004
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161119
[St] Status:MEDLINE
[do] DOI:10.1177/0300060516668776


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[PMID]:27809336
[Au] Autor:Bustos ML; Zhao Y; Chen H; Caritis SN; Venkataramanan R
[Ad] Endereço:Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, Pittsburgh, Pennsylvania.
[Ti] Título:Polymorphisms in CYP1A1 and CYP3A5 Genes Contribute to the Variability in Granisetron Clearance and Exposure in Pregnant Women with Nausea and Vomiting.
[So] Source:Pharmacotherapy;36(12):1238-1244, 2016 Dec.
[Is] ISSN:1875-9114
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Nausea and vomiting affect up to 90% of pregnant women. Granisetron is a potent and highly selective serotonin receptor antagonist and is an effective antiemetic. Findings from a prior study in pregnant women demonstrated a large interindividual variability in granisetron exposure. Granisetron is primarily metabolized by the cytochrome P450 (CYP) enzymes CYP1A1 and CYP3A and is likely a substrate of the ABCB1 transporter. Single-nucleotide polymorphisms (SNPs) in CYP3A, CYP1A1, and ABCB1 can alter drug metabolism. OBJECTIVE: This study evaluated the influence of polymorphisms in CYP3A4, CYP3A5, CYP1A1, and ABCB1 on the pharmacokinetic properties of granisetron in pregnant women. METHODS: The study enrolled 16 pregnant women (gestational age of 12-19 wks). All patients had nausea and vomiting and were treated with granisetron 1 mg. Granisetron plasma concentrations were determined using liquid chromatography tandem-mass spectrometry. The patients' genotype was determined using TaqMan SNP Genotyping Assays. The Hardy-Weinberg equilibrium was assessed by comparing observed and expected genotype frequencies, using the exact test. Intravenous granisetron clearance was used as the dependent variable for analysis of associations. RESULTS: Of 16 patients, 25% were homozygous for the allele variant CYP3A5*3 and had a significantly lower granisetron clearance and increased area under the plasma concentration-versus-time curve (AUC) compared with nonhomozygous patients. Approximately one-third of patients (n=5) were carriers for the allele variant CYP1A1*2A and had a significantly higher granisetron clearance and decreased AUC. We did not find significant differences in the AUC or clearance for any SNPs in CYP3A4 and ABCB1 genes. CONCLUSIONS: Polymorphisms in CYP3A5 and CYP1A1 account for some of the variability in systemic clearance and exposure of granisetron in pregnant women.
[Mh] Termos MeSH primário: Citocromo P-450 CYP1A1/genética
Citocromo P-450 CYP3A/genética
Granisetron/administração & dosagem
Êmese Gravídica/tratamento farmacológico
[Mh] Termos MeSH secundário: Subfamília B de Transportador de Cassetes de Ligação de ATP/genética
Adulto
Antieméticos/administração & dosagem
Antieméticos/farmacocinética
Área Sob a Curva
Cromatografia Líquida
Feminino
Genótipo
Granisetron/farmacocinética
Seres Humanos
Polimorfismo de Nucleotídeo Único
Gravidez
Espectrometria de Massas em Tandem
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABCB1 protein, human); 0 (ATP Binding Cassette Transporter, Sub-Family B); 0 (Antiemetics); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (CYP1A1 protein, human); EC 1.14.14.1 (CYP3A5 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1A1); EC 1.14.14.1 (Cytochrome P-450 CYP3A); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161104
[St] Status:MEDLINE
[do] DOI:10.1002/phar.1860



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