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1.
West Afr J Med ; 40(8): 779-785, 2023 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-37638969

RESUMO

BACKGROUND: Coronary computed tomography angiography (CCTA) allows for non-invasive visualization of the coronary arteries which is promising in diagnosing coronary artery disease. OBJECTIVES: To determine the prevalence, morphology, anatomic distribution pattern and correlates of CAD in our environment. METHODS: This cross-sectional study was conducted on the first cohort of patients referred for CCTA in our hospital. The patients were examined with 160-slice Toshiba® CT scanner. Their demographic data, relevant clinical information as well as the findings on CCTA were extracted and documented. The data were analysed using the R programming software version 4.0.4. RESULTS: Out of a total of 153 patients who presented for CCTA within the study period, 133 (84.7%) were eligible for analysis. Their age ranged from 22-78 years with a mean ± SD of 55.8 ± 11.7 years. A total of 33 (24.8%) had normal CCTA, while 100 (75.2%) had either stenosis or total occlusion. There was a significantly higher (p-value of 0.00001) calcium score among those with stenosis compared to those with normal CCTA. The severity of the stenotic lesion was associated with the calcium score. The logistic regression analyses showed a statistically significant (P = 0.0415, OR = 1.0569, 97.5% CI =1.078152-1.123240) association between age and the presence of coronary stenosis. In addition, most of the stenotic lesions were in the left anterior descending artery (LAD). CONCLUSION: Majority of the patients had coronary artery disease of variable severity and the LAD was the most involved artery. There was no significant association between sex and severity of the disease; however, old age and higher number of lesions were associated with severe disease.


CONTEXTE: L'angiographie coronaire par tomodensitométrie (ATCC) permet une visualisation non invasive des artères coronaires, ce qui est prometteur pour le diagnostic de la maladie coronarienne. OBJECTIFS: Déterminer la prévalence, la morphologie, le modèle de distribution anatomique et les corrélats de la maladie coronarienne dans notre environnement. MÉTHODES: Cette étude transversale a été menée sur la première cohorte de patients envoyés pour un CCTA dans notre hôpital. Les patients ont été examinés à l'aide d'un tomodensitomètre Toshiba® à 160 coupes. Leurs données démographiques, les informations cliniques pertinentes ainsi que les résultats de l'ACTC ont été extraits et documentés. Les données ont été analysées à l'aide du logiciel de programmation R version 4.0.4. RÉSULTATS: Sur un total de 153 patients qui se sont présentés pour une ACTC pendant la période de l'étude, 133 (84,7 %) étaientéligibles pour l'analyse. Leur âge était compris entre 22 et 78 ans,avec une moyenne + écart-type de 55,8 + 11,7 ans. Au total, 33 (24,8%) avaient une CCTA normale, tandis que 100 (75,2 %) présentaient une sténose ou une occlusion totale. Le score calcique était significativement plus élevé (valeur p de 0,00001) chez les patients présentant une sténose que chez ceux dont l'ACTC était normale. La gravité de la lésion sténosée était associée au score calcique. Les analyses de régression logistique ont montré une association significative (P=0,0415, OR= 1,0569, 97,5% CI=1,078152-1,123240) entre l'âge et la présence d'une sténose coronaire. En outre, la plupart des lésions sténosées se trouvaient dans l'artère descendante antérieure gauche (LAD). CONCLUSION: La majorité des patients présentaient une maladie coronarienne de gravité variable et l'artère LAD était l'artère la plus touchée. Il n'y avait pas d'association significative entre le sexe et la sévérité de la maladie ; cependant, l'âge avancé et le nombre plus élevé de lésions étaient associés à la sévérité de la maladie. Mots-clés: Angiographie, Tomodensitométrie, Artères Coronaires, Stenose.


Assuntos
Angiografia por Tomografia Computadorizada , Doença da Artéria Coronariana , Humanos , Adulto Jovem , Adulto , Pessoa de Meia-Idade , Idoso , Doença da Artéria Coronariana/diagnóstico por imagem , Doença da Artéria Coronariana/epidemiologia , Cálcio , Constrição Patológica , Estudos Transversais , Nigéria/epidemiologia , Tomografia Computadorizada por Raios X , Angiografia
2.
Artigo em Inglês | AIM (África) | ID: biblio-1512895

RESUMO

Contrary to the old dictum that central obesity is more common among men than women, recent reports have shown a gradual reversal of this trend, as suggested by some studies. Objective: To compare the prevalence of central obesity among men and women with Diabetes mellitus in NorthCentral Nigeria. Methods: This multi-centred, cross-sectional study was conducted across 20 hospitals in Abuja, Nasarawa State, and Niger State, involving 1040 participants. Some obesity indices (body mass index, waist circumference and waist-toheight ratio) were measured. Results: The prevalence of central obesity (waist circumference criterion) was significantly higher in the females compared to male participants (89.6% vs 51.6%, χ2 = 1231.37, p<0.001), similar to the prevalence determined by waistheight ratio criterion (female vs male, 88.8% vs 71.5%, χ2 = 58.83, p<0.001). Following correction for age, duration of diabetes mellitus, blood pressure, blood glucose, and glycated haemoglobin using logistic regression, female gender remained a significant determinant of central obesity (OR = 2.76, 95% CI 1.81-3.83, p = 0.004). Conclusion: The prevalence of central obesity was higher among women than men in a cross-section of patients with diabetes mellitus in North-Central Nigeria


Assuntos
Humanos , Pressão Sanguínea , Diabetes Mellitus , Obesidade Abdominal , Glicemia , Prevalência , Estudos Transversais , Circunferência da Cintura , Razão Cintura-Estatura , Diversidade de Gênero
3.
J Med Imaging Radiat Sci ; 53(3): 429-436, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-35717379

RESUMO

OBJECTIVES: To evaluate and compare image quality and radiation dose between the helical and wide-volume scans to determine the protocol that provides a lower radiation dose without loss in image quality. METHODS: The study was prospectively conducted on consented adult patients that presented for routine brain CT. Image quality and radiation dose were compared between the helical and wide-volume scans on the Toshiba 160-slice Aquilion Prime CT scanner. The volume computed tomography dose index (CTDIvol) and dose length product (DLP) for each scan mode were collected and compared. Image quality was quantitatively and qualitatively evaluated using the unenhanced brain CT images. The data were analysed using a statistical package for social sciences (SPSS) software version 20 for both the descriptive and inferential statistics. A significant difference in image quality and radiation dose between the helical and wide-volume scans was determined based on a p-value of <0.05. RESULTS: A total of 54 participants were included, with two groups of 27 participants. The CTDIvol and DLP values were significantly p < 0.05 higher in the helical scan (CTDIvol: 65 mGy; DLP: 1597 mGy.cm) compared to the wide-volume scan (CTDIvol: 54 mGy; DLP: 1133 mGy.cm). The grey and white matters show a better signal-to-noise ratio (SNR) for the helical scan. Meanwhile, the contrast-to-noise ratio (CNR) was significantly p < 0.05 higher in the wide-volume scan. The results from the visual grading methods were compared and showed superior image quality in helical over the wide-volume scan. CONCLUSION: Wide-volume provides a lower dose compared to helical and therefore, could be adopted as the routine protocol for brain CT for in house dose optimisation. Where clinical conditions warrant the need for a helical scan, the protocol should be optimised in line with the as low as reasonable achievable (ALARA) principle.


Assuntos
Tomografia Computadorizada de Feixe Cônico , Tomografia Computadorizada por Raios X , Adulto , Encéfalo , Humanos , Doses de Radiação , Razão Sinal-Ruído
4.
Heliyon ; 7(10): e08108, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34660925

RESUMO

To meet the rising demand for uninterrupted high-speed broadband internet services, the deployment of high-frequency bands for the transmission of radio signals is inevitable. Unfortunately, attenuation due to rain droplets remains the most challenging factor impeding effective radio wave propagation especially in earth-space satellite links operating at Ka and V bands. It is important to understand the attenuation and the parameters that determine its magnitude in order to provide an effective solution to this problem. Rain height as one of the attenuation input parameters was examined in detail. A study of its temporal evolution reveals that seasonal variation is insignificant while the spatial variation shows that it increases from the Sahel to the Coastal Zone of Nigeria. The work provides comprehensive rain height and rain-induced attenuation contour maps. These maps are expected to serve as a database for link budget calculations for different areas in Nigeria. Rain-induced attenuation maps for 1%, 0.1%, and 0.01% of time exceedance are provided at 20 GHz and 40 GHz for Ka and V band signals respectively.

5.
J Med Imaging Radiat Sci ; 52(3): 435-442, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-33896746

RESUMO

BACKGROUND: Mammography involves the use of low energy X-rays to image the breast tissue. Although low dose radiation is used, the use of ionising radiation implies the risk of inducing breast cancer. Thus, the study established local DRLs for digital mammography for in-house dose optimisation. METHODS: This was a retrospective study that had a total of 240 women that presented for mammography at the two tertiary institutions located in the Northwest region of Nigeria. Patient demographic information including compressed breast thickness (CBT), which is the breast tissue thickness across the imaging plate, and mean glandular dose (MGD) were recorded. Data were analysed based on descriptive and inferential statistics using SPSS statistical software. The DRLs based on MGD and CBT were established and compared with the relevant data in the literature. RESULTS: Local DRLs based on MGD and CBT were established at the 75th percentile (craniocaudal (CC): 1.50 mGy; 57 mm; mediolateral (MLO): 1.60 mGy; 63 mm) and 95th percentile (CC: 3.74 mGy; 69 mm; MLO: 3.61 mGy; 76 mm). The MGD based on manual exposure was significantly (p < 0.005) higher compared to the automatic optimisation parameter (AOP) mode which suggests the need to continuously adhere to the use of AOP mode for in-house dose optimisation. CONCLUSION: The study established local DRLs for the digital mammography systems at the 75th and 95th percentiles which compared well with the values established in the literature. Manual selection of parameters should only be employed where there are legitimate indications as it is associated with high exposure. Also, manual selection of parameters should be based on preset tables as a function of compressed breast thickness.


Assuntos
Níveis de Referência de Diagnóstico , Mamografia , Feminino , Hospitais , Humanos , Nigéria , Doses de Radiação , Estudos Retrospectivos
6.
West Afr J Med ; 38(3): 287-291, 2021 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-33767235

RESUMO

In trauma and orthopaedic practice, the management of segmental bone loss constitutes a major challenge to the surgeon. Several methods have been employed in bone reconstruction with varying objectives depending on the size of the defect in question. A gap of not more than 2cm may benefit from acute docking and fixation, 4cm gap can be managed by non-vascularized structural or non-structural graft with fixation. Gaps of more than 4cm can be managed by numerous options which include allograft, vascularized structural graft and distraction osteogenesis with either linear rail system (LRS) or Ilizarov device. Masquelet technique of induced membrane formation is used to bridge a gap of more than 5cm and up to 25cm using bone cement as a spacer in first stage and use of autologous cancellous bone graft in the second stage.


En traumatologie et en orthopédie, la prise en charge de la perte osseuse segmentaire constitue un défi majeur pour la chirurgien. Plusieurs méthodes ont été employées dans la reconstruction d'os avec des objectifs variables en fonction de la taille du défaut en question. Un écart de pas plus de 2 cm peut en bénéficier de l'amarrage et de la fixation aigus, un écart de 4 cm peut être géré par structurelle non vascularisée ou greffe non structurelle avec fixation. Les espaces de plus de 4 cm peuvent être gérés par de nombreux options qui incluent allogreffe, greffe structurelle vascularisée et ostéogenèse par distraction avec l'un ou l'autre des systèmes de rails linéaires (LRS) ou appareil Ilizarov. Technique de Masquelet d'induit la formation de la membrane est utilisée pour combler un espace de plus de 5 cm et jusqu'à 25 cm en utilisant du ciment osseux comme espaceur dans la première étape et l'utilisation d'une greffe d'os spongieux autologue dans la deuxième étape. Mots clés: Défaut osseux segmentaire, ostéogenèse par distraction, technique de membrane induite, espaceur de ciment osseux.

7.
West Afr J Med ; 37(2): 189-196, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32150639

RESUMO

Extremity gangrene is a fairly common pathology, which complicates systemic vascular and endocrine diseases. Most often, it is encountered in diseases like uncontrolled Diabetes Mellitus, presenting as diabetic foot gangrene, severe peripheral arteriosclerosis with gangrene of the extremity complicating severe uncontrolled systemic hypertension and meningococcal septicaemia with peripheral gangrene. It also occurs in some cases of snake bite as well as frost bite (in regions with extreme cold weather conditions). Some of them present as monolateral extremity gangrene. However, others present as bilateral symmetrical peripheral gangrene (SPG) characterized by bilateral extremity ischaemia resulting in gangrene in which there is no major vascular occlusive disease. There is disseminated intravascular coagulation with the gangrene being considered as a cutaneous marker and some of the patients that survive ultimately require amputation of the affected limb(s) in the severe cases. The mild cases end up losing some of the digits or just exfoliation of the dead cutaneous layer. The effects are generally more severe in the lower limbs than in upper limbs. Notable among these are some of those complicating meningococcal sepsis resulting from peripheral intravascular coagulation. We present here, five patients who presented with varying degrees of peripheral gangrene during an epidemic of meningitis and the treatments that were carried out depending on the severity of their cases.


Assuntos
Amputação Cirúrgica , Coagulação Intravascular Disseminada/cirurgia , Gangrena/etiologia , Meningite Meningocócica/complicações , Infecções Meningocócicas/cirurgia , Sepse/microbiologia , Coagulação Intravascular Disseminada/complicações , Coagulação Intravascular Disseminada/diagnóstico , , Gangrena/cirurgia , Humanos , Perna (Membro) , Infecções Meningocócicas/complicações , Sepse/complicações
8.
West Afr J Med ; 36(1): 83-87, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30924122

RESUMO

BACKGROUND: Back pain due to prolapsed intervertebral disc accounts for two thirds of all visits to the orthopaedic clinic. The incidence of this disease is increasing with the increased sports activities in the young and due to degeneration in the elderly. Open lumbar microdiscectomy remains the gold standard amongst surgical procedures for herniated discs with or without instrumentation. However, percutaneous/ endoscopic microdiscectomy is gaining popularity. In our environment, high cost and paucity of instrumentation and skills militate against the use of such technique. In the western world, improvement in the mentioned skills and instrumentation and shorter rehabilitation time make minimal access surgeries more appealing than open microdiscectomy in recent times. MATERIALS AND METHODS: Patients with clinical signs and symptoms of spinal canal stenosis secondary to isolated lumbar disc herniation were investigated with plain radiographs and magnetic resonance imaging (MRI). All those with definite canal stenosis as seen on the MRI that were not responsive to conservative therapy or those with rapidly deteriorating clinical outlook without instability were included to have open Laminectomy without instrumentation. Their preoperative and postoperative walking distance, their modified Roland-Morris disability indices, Their pain numeric score (NRS), their anteroposterior distance of the spinal canal at maximal site of stenosis and finally the absence or presence of preoperative and post operative anteroposterior/instability. RESULTS: Twenty patients had open Laminectomy. There was significant improvement in the postoperative pain numeric score, the walking distance, the Roland Morris disability score. There was no evidence of postoperative instability on the plain radiograph. CONCLUSION: Open Laminectomy remains a useful tool in the treatment of patients with lumbar spinal canal stenosis due to prolapsed intervertebral discs.


Assuntos
Deslocamento do Disco Intervertebral/cirurgia , Laminectomia/métodos , Vértebras Lombares/cirurgia , Canal Medular/diagnóstico por imagem , Estenose Espinal/cirurgia , Adulto , Idoso , Humanos , Vértebras Lombares/diagnóstico por imagem , Imageamento por Ressonância Magnética , Pessoa de Meia-Idade , Estudos Retrospectivos , Resultado do Tratamento
9.
West Afr J Med ; 35(2): 123-127, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30027998

RESUMO

BACKGROUND: Childhood injuries are often associated with fractures, and it is said to account for about 25% of all paediatrics trauma. There is a male preponderance and the peak incidence occurs among primary and secondary school age groups. The occurrence and management of these fractures are influenced by season, geographical location, educational and socio-economic status of the populace as well as time of presentation and availability of suitable facilities for treatment. OBJECTIVES: To analyse the demographic characteristics of the subjects, aetiological factors, fracture distribution, educational and occupational status of their parents, mode of treatment and their outcomes. SUBJECTS AND METHODS: We carried out a prospective study on children 0-12 years of age at the University Teaching Hospital, Zaria, Nigeria, with fractures who consented to the study from January 2013 to December, 2016. Eight-six children were recruited through the Accident and Emergency Department. Diagnosis was made by both clinical and radiological assessment. They were managed by either non-operative or operative modality. Their complications were also managed. Their follow-up was for 12 months. RESULTS: A total of 86 children with 86 fractures were enrolled with mean age of 7 years and male/female ratio of 2:1. The main aetiological factors were road traffic accidents (52.4% from cars, motorcycle and tricycle), followed by falls from heights (40.0%). Forearm bone fractures were the commonest (30.2%). Non-operative modality dominated the management (72.1%). Complication rate was 20.4%. CONCLUSION: Fractures in children have a male prepon-derance with the radius being most commonly involved. Non-operative management was the main modality of treatment.


Assuntos
Acidentes de Trânsito/estatística & dados numéricos , Fraturas Ósseas/epidemiologia , Criança , Pré-Escolar , Feminino , Humanos , Incidência , Lactente , Recém-Nascido , Masculino , Nigéria/epidemiologia , Estudos Prospectivos
10.
Niger J Clin Pract ; 17(3): 366-9, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24714019

RESUMO

INTRODUCTION: The use of drains in trauma and Orthopaedic practice has been affected by the concept of evidence based medicine that has become accepted as standard of care for all surgical or medical practice, which questions all care processes that cannot be backed by evidence to be beneficial to the patient. There have been a large number of multi centre meta-analytical studies that found drains to be of little or no benefit in trauma and Orthopaedic operations. Because of these studies, there are few situations where drains are routinely used e.g. Calcaneal fractures in developed countries. Even major procedures like total knee and arthroplasties are being performed without drains. We set to find out whether such evidence can be found in our practice. MATERIALS AND METHODS: Between 2004 and 2012, eighty six patients matched for sex and type of injury and operative procedures to be done were prospectively selected and assigned to use or no use of drains in their operations. Complications like haematoma, drain migration, infection, inadvertent drain stitching were observed in the two groups. RESULTS: Eighty six major orthopaedic operations were studied. There was no evidence of occurrence of complication arising from non use of drains in the undrained group. Those patients whose wounds were drained had no need for drain change thus making the wound care less eventful CONCLUSION: Postoperative wound drains make for neat postoperative period with less tissue swelling. There was no statistically significant differences between the drained and undrained wounds in terms of infection rates, haematoma or seroma formation.


Assuntos
Drenagem/efeitos adversos , Drenagem/métodos , Procedimentos Ortopédicos/efeitos adversos , Procedimentos Ortopédicos/métodos , Adolescente , Adulto , Idoso , Drenagem/instrumentação , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Procedimentos Ortopédicos/instrumentação , Complicações Pós-Operatórias/etiologia , Estudos Prospectivos , Adulto Jovem
11.
Niger J Clin Pract ; 14(2): 245-8, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21860149

RESUMO

Gangrene of the extremities in the newborn is extremely rare at birth. Less than 100 cases have been reported worldwide. Its etiology is obscure in many cases; however, some factors have been associated with it in the newborn, which include vascular injury and embolism. We report a case of a baby with congenital bilateral lower limb gangrene caused by thromboembolic phenomenon from retroplacental hematoma following abruptio placentae and highlight the challenges of managing such condition in resource-poor setting.


Assuntos
Gangrena/congênito , Perna (Membro)/diagnóstico por imagem , Descolamento Prematuro da Placenta , Angiografia , Evolução Fatal , Feminino , Gangrena/etiologia , Humanos , Recém-Nascido , Perna (Membro)/irrigação sanguínea , Gravidez , Tromboembolia/complicações , Tomografia Computadorizada por Raios X
12.
Ann Afr Med ; 10(1): 1-5, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21311147

RESUMO

Physicians and other professionals in the field of medicine have to perform invasive and non-invasive procedures on patients as part of their duties. There is a legal basis upon which these procedures are done; this is called 'informed consent.' Sociocultural factors have strong influence on the sick role. These factors influence the application of informed consent in Nigeria.


Assuntos
Características Culturais , Cirurgia Geral/ética , Consentimento Livre e Esclarecido , Ética Médica/educação , Humanos , Consentimento Livre e Esclarecido/ética , Consentimento Livre e Esclarecido/legislação & jurisprudência , Nigéria
13.
Ann Afr Med ; 10(1): 25-8, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21311151

RESUMO

BACKGROUND: Fractures resulting in segmental bone loss challenge the orthopedic surgeon. Orthopedic surgeons in developed countries have the option of choosing vascularized bone transfers, bone transport, allogenic bone grafts, bone graft substitutes and several other means to treat such conditions. In developing countries where such facilities or expertise may not be readily available, the surgeon has to rely on other techniques of treatment. Non-vascularized fibula strut graft and cancellous bone grafting provides a reliable means of treating such conditions in developing countries. MATERIALS AND METHODS: Over a period of six years all patients with segmental bone loss either from trauma or oncologic resection were included in the study. Data concerning the type of wound, size of gap and skin loss at tumor or fracture were obtained from clinical examination and radiographs. RESULT: Ten patients satisfied the inclusion criteria for the study. The average length of the fibula strut is 7 cm, the longest being 15 cm and the shortest 3 cm long. The average defect length was 6.5 cm. Five patients had Gustillo III B open tibial fractures. One patient had recurrent giant cell tumor of the distal radius and another had a polyostotic bone cyst of the femur, which was later confirmed to be osteosarcoma. Another had non-union of distal tibial fracture with shortening. One other patient had gunshot injury to the femur and was initially managed by skeletal traction. The tenth patient had a comminuted femoral fracture. All trauma patients had measurement of missing segment, tissue envelope assessment, neurological examination, and debridement under general anesthesia with fracture stabilization with external fixators or casts. Graft incorporation was 80% in all treated patients. CONCLUSION: Autologous free, non-vascularized fibula and cancellous graft is a useful addition to the armamentarium of orthopedic surgeon in developing countries attempting to manage segmental bone loss, whether created by trauma or excision of tumors.


Assuntos
Alongamento Ósseo , Transplante Ósseo/métodos , Fíbula/transplante , Fraturas Ósseas/cirurgia , Osteoporose , Adulto , Feminino , Fíbula/lesões , Hospitais de Ensino , Humanos , Masculino , Pessoa de Meia-Idade , Nigéria , Transplante Autólogo , Transplante Homólogo , Resultado do Tratamento
15.
Artigo em Inglês | AIM (África) | ID: biblio-1271582

RESUMO

There is an increasing incidence of missile injury attributable to improved technology; and increased crime and conflict rates in both developing and developed nations of the world. We undertook a review of civilian gunshot injuries to the extremities in Nigeria. The pathology of these injuries as well as their implications for management are presented. The peculiar challenges they present to the orthopaedic surgeons in the management of gunshot injuries in a resource depleted country are highlighted. Community based socially and culturally acceptable conflict resolution mechanisms; control of fire arms and revision of the treatment guidelines are recommended as preventive and management strategies of gunshot injuries in Nigeria


Assuntos
Armas de Fogo , Ferimentos e Lesões
16.
J Pharmacol Exp Ther ; 297(2): 638-45, 2001 May.
Artigo em Inglês | MEDLINE | ID: mdl-11303053

RESUMO

Celecoxib pharmacokinetics was evaluated after single and multiple oral dosing; after dosing in a solution and as a solid; with and without food; and after administration into different sites of the GI tract using dog. After oral dosing in a solution, celecoxib was rapidly absorbed and reached maximum concentrations by 1 h; absorption was delayed another 1 to 2 h when administered as a solid. The absolute bioavailability of celecoxib was higher when given as a solution (64--88%) compared with capsule (22--40%). The absorption of celecoxib given in a capsule was delayed by food, although systemic exposure increased by 3- to 5-fold. The systemic availability of celecoxib given intragastrically in solution was similar to that obtained following direct instillation into the duodenum, jejunum, or colon through a chronic intestinal access port. Collectively, these data suggest that celecoxib is a highly permeable drug that can be absorbed throughout the GI tract and that dissolution may be a rate-limiting factor for absorption from solid dosage forms. Unlike dogs, celecoxib given to humans with a high fat meal exhibits only a slight increase in AUC(0--infinity) (11%) that is not clinically significant with regard to safety or efficacy. In humans, a lower dose and a longer GI residence time may promote the opportunity for absorption of a poorly soluble drug such as celecoxib that can be absorbed throughout the GI tract. This would minimize the effect of food on absorption; as such, patients with arthritis can be given celecoxib with or without food.


Assuntos
Anti-Inflamatórios não Esteroides/farmacocinética , Interações Alimento-Droga , Absorção Intestinal/fisiologia , Sulfonamidas/farmacocinética , Adulto , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/sangue , Área Sob a Curva , Disponibilidade Biológica , Celecoxib , Estudos Cross-Over , Gorduras na Dieta/farmacologia , Cães , Feminino , Humanos , Masculino , Pirazóis , Sulfonamidas/administração & dosagem , Sulfonamidas/sangue
17.
Xenobiotica ; 30(7): 731-44, 2000 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-10963063

RESUMO

1. The metabolism and excretion of celecoxib, a specific cyclooxygenase 2 (COX-2) inhibitor, was investigated in mouse, rabbit, the EM (extensive) and PM (poor metabolizer) dog, and rhesus and cynomolgus monkey. 2. Some sex and species differences were evident in the disposition of celecoxib. After intravenous (i.v.) administration of [14C]celecoxib, the major route of excretion of radioactivity in all species studied was via the faeces: EM dog (80.0%), PM dog (83.4%), cynomolgus monkey (63.5%), rhesus monkey (83.1%). After oral administration, faeces were the primary route of excretion in rabbit (72.2%) and the male mouse (71.1%), with the remainder of the dose excreted in the urine. After oral administration of [14C]celecoxib to the female mouse, radioactivity was eliminated equally in urine (45.7%) and faeces (46.7%). 3. Biotransformation of celecoxib occurs primarily by oxidation of the aromatic methyl group to form a hydroxymethyl metabolite, which is further oxidized to the carboxylic acid analogue. 4. An additional phase I metabolite (phenyl ring hydroxylation) and a glucuronide conjugate of the carboxylic acid metabolite was produced by rabbit. 5. The major excretion product in urine and faeces of mouse, rabbit, dog and monkey was the carboxylic acid metabolite of celecoxib.


Assuntos
Inibidores de Ciclo-Oxigenase/farmacocinética , Sulfonamidas/farmacocinética , Animais , Celecoxib , Cromatografia Líquida de Alta Pressão , Cães , Fezes/química , Feminino , Macaca fascicularis , Macaca mulatta , Masculino , Espectrometria de Massas , Camundongos , Pirazóis , Coelhos , Especificidade da Espécie
18.
Drug Metab Dispos ; 28(5): 514-21, 2000 May.
Artigo em Inglês | MEDLINE | ID: mdl-10772629

RESUMO

The pharmacokinetics, tissue distribution, metabolism, and excretion of celecoxib, 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide, a cyclooxygenase-2 inhibitor, were investigated in rats. Celecoxib was metabolized extensively after i.v. administration of [(14)C]celecoxib, and elimination of unchanged compound was minor (less than 2%) in male and female rats. The only metabolism of celecoxib observed in rats was via a single oxidative pathway. The methyl group of celecoxib is first oxidized to a hydroxymethyl metabolite, followed by additional oxidation of the hydroxymethyl group to a carboxylic acid metabolite. Glucuronide conjugates of both the hydroxymethyl and carboxylic acid metabolites are formed. Total mean percent recovery of the radioactive dose was about 100% for both the male rat (9.6% in urine; 91.7% in feces) and the female rat (10.6% in urine; 91.3% in feces). After oral administration of [(14)C]celecoxib at doses of 20, 80, and 400 mg/kg, the majority of the radioactivity was excreted in the feces (88-94%) with the remainder of the dose excreted in the urine (7-10%). Both unchanged drug and the carboxylic acid metabolite of celecoxib were the major radioactive components excreted with the amount of celecoxib excreted in the feces increasing with dose. When administered orally, celecoxib was well distributed to the tissues examined with the highest concentrations of radioactivity found in the gastrointestinal tract. Maximal concentration of radioactivity was reached in most all tissues between 1 and 3 h postdose with the half-life paralleling that of plasma, with the exception of the gastrointestinal tract tissues.


Assuntos
Anti-Inflamatórios não Esteroides/farmacocinética , Sulfonamidas/farmacocinética , Animais , Área Sob a Curva , Bile/metabolismo , Ductos Biliares/fisiologia , Biotransformação , Celecoxib , Cromatografia Líquida de Alta Pressão , Fezes/química , Feminino , Meia-Vida , Injeções Intravenosas , Masculino , Pirazóis , Ratos , Ratos Sprague-Dawley , Sulfonamidas/administração & dosagem , Distribuição Tecidual
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