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1.
Anesth Essays Res ; 7(1): 116-22, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-25885732

RESUMO

BACKGROUND: Nasal packing after the nasal surgery can be extremely hazardous and can lead to airway complications such as dyspnea and respiratory obstruction. OBJECTIVE: The present study aimed at comparing the traditional nasal packing with nasal airway during the immediate postoperative period in patients undergoing fibreoptic endoscopic sinus surgery (FESS) under general anaesthesia (GA) with regards to airway management. MATERIALS AND METHODS: The study groups consisted of 90 ASA grade I and II patients aged 16 to 58 years who underwent FESS under GA. Patients were randomly assigned into three groups: Group NP, UA and Group BA of 30 patients each. At the end of surgery, Group NP patients were managed with traditional bilateral nasal packing while a presterilized 5 mm ID uncuffed ETT was cut to an appropriate size and inserted into one of the nostrils in UA and bilaterally in BA group patients. During postoperative period following parameters and variables were observed over the next 24 hours: Any respiratory distress or obstruction, pain and discomfort, oxygen saturation, heart rate, blood pressure, bleeding episode, ease of suctioning through nasal airway, anaesthesiologists and surgeons satisfaction during postoperative period, discomfort during removal of nasal airway and any fresh bleeding episode during removal of nasal airway. The data was compiled and analyzed using Chi-square test and ANOVA with post-hoc significance. Value of P < 0.05 was considered significant and P < 0.0001 as highly significant. RESULTS: The post-op mean cardio-respiratory parameters showed significant variations among NP group (P < 0.05) and the patient of UA and BA groups while intergroup comparison between UA and BA was non-significant (P > 0.05). Pain and discomfort, bleeding episode, ease of suctioning through nasal airway, pain and bleeding during removal of nasal airway (P < 0.0001) as well as surgeons and anaesthesiologists satisfaction criteria showed significant results among the NP group as compared to UA and BA groups (P < 0.05). CONCLUSION: The present intervention to maintain airway patency can be termed as excellent with additional benefits like ease of suctioning; oxygen supplementation and a possible haemostatic effect due to pressure on the operated site. The low cost of the modified nasal airway and easily replicable design were the standout observations of the present study.

2.
Saudi J Anaesth ; 5(4): 365-70, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22144922

RESUMO

BACKGROUND AND AIMS: Opioids as epidural adjunct to local anesthetics (LA) have been in use since long and α-2 agonists are being increasingly used for similar purpose. The present study aims at comparing the hemodynamic, sedative, and analgesia potentiating effects of epidurally administered fentanyl and dexmedetomidine when combined with ropivacaine. METHODS: A total of one hundred patients of both gender aged 21-56 years, American Society of Anaesthesiologist (ASA) physical status I and II who underwent lower limb orthopedic surgery were enrolled into the present study. Patients were randomly divided into two groups: Ropivacaine + Dexmedetomidine (RD) and Ropivacaine + Fentanyl (RF), comprising 50 patie nts each. Inj. Ropivacaine, 15 ml of 0.75%, was administered epidurally in both the groups with addition of 1 µg/kg of dexmedetomidine in RD group and 1 µg/kg of fentanyl in RF group. Besides cardio-respiratory parameters and sedation scores, various block characteristics were also observed which included time to onset of analgesia at T10, maximum sensory analgesic level, time to complete motor blockade, time to two segmental dermatomal regressions, and time to first rescue analgesic. At the end of study, data was compiled systematically and analyzed using ANOVA with post-hoc significance, Chi-square test and Fisher's exact test. Value of P<0.05 is considered significant and P<0.001 as highly significant. RESULTS: The demographic profile of patients was comparable in both the groups. Onset of sensory analgesia at T10 (7.12±2.44 vs 9.14±2.94) and establishment of complete motor blockade (18.16±4.52 vs 22.98±4.78) was significantly earlier in the RD group. Postoperative analgesia was prolonged significantly in the RD group (366.62±24.42) and consequently low dose consumption of local anaesthetic LA (76.82±14.28 vs 104.35±18.96) during epidural top-ups postoperatively. Sedation scores were much better in the RD group and highly significant on statistical comparison (P<0.001). Incidence of nausea and vomiting was significantly high in the RF group (26% and 12%), while incidence of dry mouth was significantly higher in the RD group (14%) (P<0.05). CONCLUSIONS: Dexmedetomidine seems to be a better alternative to fentanyl as an epidural adjuvant as it provides comparable stable hemodynamics, early onset, and establishment of sensory anesthesia, prolonged post-op analgesia, lower consumption of post-op LA for epidural analgesia, and much better sedation levels.

3.
J Emerg Trauma Shock ; 4(4): 494-500, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22090744

RESUMO

BACKGROUND AND CONTEXT: Polytrauma is a leading cause of mortality in the developing countries and efforts from various quarters are required to deal with this increasing menace. AIMS AND OBJECTIVES: An attempt has been made by the coordinated efforts of the intensive care and trauma team of a newly established tertiary care institute in designing and improving the trauma care services to realign its functions with national policies by analyzing the profile of polytrauma victims and successfully managing them. MATERIALS AND METHODS: A retrospective analysis was carried out among the 531 polytrauma admissions in the emergency department. The information pertaining to age and gender distribution, locality, time to trauma and initial resuscitation, cause of injury, type of injury, influence of alcohol, drug addiction, presenting clinical picture, Glasgow Coma score on admission and few other variables were also recorded. The indications for various operative interventions and intensive care unit (ICU) admissions were analyzed thoroughly with a concomitant improvement of our trauma care services and thereby augmenting the national policies and programs. A statistical analysis was carried out with chi-square and analysis of variance ANOVA tests, using SPSS software version 10.0 for windows. The value of P<0.05 was considered significant and P<0.0001 as highly significant. RESULTS: Majority of the 531 polytrauma patients hailed from rural areas (63.65%), riding on the two wheelers (38.23%), and predominantly comprised young adult males. Fractures of long bones and head injury was the most common injury pattern (37.85%) and 51.41% of the patients presented with shock and hemorrhage. Airway management and intubation became necessary in 42.93% of the patients, whereas 52.16% of the patients were operated within the first 6 hours of admission for various indications. ICU admission was required for 45.76% of the patients because of their deteriorating clinical condition, and overall,ionotropic support was administered in 55.93% of the patients for successful resuscitation. CONCLUSIONS: There is an urgent need for proper implementation ofpre-hospital and advanced trauma life support measures at grass-root level. Analyzing the profile of polytrauma victims at a national level and simultaneously improving the trauma care services at every health center are very essential to decrease the mortality and morbidity. The improvement can be augmented further by strengthening the rural health infrastructure, strict traffic rules, increasing public awareness and participation and coordination among the various public and private agencies in dealing with polytrauma.

4.
Saudi J Anaesth ; 5(3): 345-7, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21957424

RESUMO

Noonan syndrome is a genetically transmitted autosomal dominant disorder characterized by various anatomic anomalies and pathophysiologic derangements. Anesthetic management in such cases poses a multitude of challenges, especially related to the airway management and maintenance of cardiovascular stability. We report a case of a 9-year-old male child weighing 24 kg, who was diagnosed as a case of Noonan syndrome and had undergone ligation of patent ductus arteriosus during early childhood. The child was operated on for release of bilateral neck bands under general anesthesia. The case report pertains to the successful airway and anesthetic management in the background of difficult airway and existence of various cardiac lesions.

5.
Saudi J Anaesth ; 5(1): 82-4, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21655024

RESUMO

An 11-month-old male child weighing 8 kg was brought to the plastic surgery out-patient department by his parents with chief complaints of sudden increase in size of a swelling over the upper lip and difficulty in feeding for the last 7 days. It was diagnosed as a case of hemangioma of the upper lip. All the routine and special investigations including coagulation profile of the child were normal. The child was planned for ablation of feeding vessels along with intralesional steroid injection. Airway management of the child posed the challenge for us as the size and site of the lesion carried the risk of difficult intubation and possible risk of extensive hemorrhage. All the requisite equipment for difficult airway management was made ready. We were able to intubate the child with miller number-2 blade from the left angle of mouth without putting much pressure on the swelling. The surgical and postoperative period was uneventful and the child was discharged the next day to be followed up after 2 weeks.

7.
Indian J Urol ; 27(4): 457-64, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22279309

RESUMO

AIM: Peri-operative pain relief in children can be provided by conventional general anaesthesia or by regional nerve blocks. The present study was carried out to evaluate and compare the effectiveness of penile block for penile surgery with the standard technique of general anaesthesia (GA) of short duration of less than two hours, and also to evaluate the postoperative pain relief obtained by penile block. MATERIALS AND METHODS: The study was carried out in the department of Anaesthesiology and Intensive care of our hospital, on 60 children in the age group of 1-10 years, belonging to American Society of Anesthesiologists (ASA) grades I and II, and divided randomly into two groups: Group B and group G, comprising of 30 patients each. Group B children received a penile block whereas group G children underwent a standard general anaesthetic procedure. Baseline, intra-operative and post-operative heart rate (HR), electrocardiogram (ECG), non-invasive blood pressure (NIBP) (systolic and diastolic) and pulse oximeter oxygen saturation (SpO(2)) were recorded at regular intervals. The duration of post-operative pain relief, time to rescue analgesia and time to first feed were also evaluated and recorded. Statistical analysis was carried out using statistical package for social sciences (SPSS) 11 version for windows and employing analysis of variance (ANOVA), unpaired student t test, Chi-square test and Mann Whitney U test for various parameters. Value of P<0.05 was considered as significant and P<0.0001 as highly significant. RESULTS: The demographic characteristics were comparable in both the groups. Heart rate, systolic blood pressure, diastolic blood pressure and pulse oximetry showed remarkable differences at various time intervals during intra-operative and post-operative period, which were statistically significant on comparison (P<0.05 and P<0.0001). Post-operative pain relief, time to first rescue analgesia and time to first feed also showed statistically significant differences. CONCLUSIONS: Penile block is very effective when used along with light sedation for distal penile surgeries of less than 2 hours duration as compared to standard GA as reflected by more stable haemodynamics in peri-operative period, excellent pain relief extending up to 6-8 hrs postoperatively and absence of any significant complications or side effects.

8.
Am J Obstet Gynecol ; 175(6): 1543-50, 1996 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-8987939

RESUMO

OBJECTIVE: The aim of this study was to explore the relevance of placental monoamine oxidase at the subcellular level in the etiology of the hyperserotonomic state in preeclampsia-eclampsia. STUDY DESIGN: The study was conducted on placentas from 20 normal pregnant women and 25 women with varied severity of preeclampsia-eclampsia. Placental serotonin and subcellular monoamine oxidase activity were determined. Histochemical localization of monoamine oxidase was done in placental sections and cell isolates. RESULTS: Placental serotonin increases with severity (rsystolic 0.84, rdiastolic 0.83) and monoamine oxidase decreases (rsystolic 0.86, rdiastolic 0.79). Placental monoamine oxidase showed marked changes in preeclampsia-eclampsia. Histochemical localization of monoamine oxidase showed diffused low activity evenly throughout the cytoplasm and nucleus of the syncytiotrophoblastic cells in preeclampsia-eclampsia; in contrast, normal placenta showed high activity in the cytoplasm without any activity in the nucleus of syncytiotrophoblastic cells. Detection of monoamine oxidase activity in nuclei of the placenta in preeclampsia-eclampsia is a novel finding. Monoamine oxidase activity at the subcellular level further strengthens this observation. A severity-dependent decrease was present in the nuclei of placentas with preeclampsia-eclampsia. The use of specific substrates and inhibitors revealed the presence of monoamine oxidase in mitochondria and nucleus. CONCLUSION: The study delineates an impaired catabolism of placental serotonin in preeclampsia-eclampsia. The novel appearance of monoamine oxidase in nuclei in proximity to its normal site and low activity resulting in a hyperserotonomic state may lead to preeclampsia-eclampsia.


Assuntos
Núcleo Celular/metabolismo , Eclampsia/metabolismo , Monoaminoxidase/metabolismo , Placenta/metabolismo , Pré-Eclâmpsia/metabolismo , Serotonina/metabolismo , Adulto , Feminino , Histocitoquímica , Humanos , Gravidez , Distribuição Tecidual
9.
Pharmacol Res ; 27(4): 335-47, 1993.
Artigo em Inglês | MEDLINE | ID: mdl-8103596

RESUMO

This study analyses the effects of dopamine receptor agonists and antagonists on rat gastrointestinal transit (GIT) in an attempt to identify the mechanisms involved. Dopamine (DA), apomorphine, quinpirole, bromocriptine and fenoldopam were given by subcutaneous (s.c.), intrathecal (i.t.), intracisternal (i.c.) and/or intraperitoneal (i.p.) routes. In general, DA (200 micrograms, i.t.), apomorphine (3, 5 and 10 mg/kg, s.c.; or 10, 30 and 100 micrograms, i.t.), and bromocriptine (1, 5 and 10 mg/kg, s.c.) elicited decreases in gastrointestinal transit which were significantly antagonized by the D2 receptor antagonists domperidone or alizapride (both 5 mg/kg, s.c.), but remained unaffected by the D1 receptor antagonist SCH 23390 (5 mg/kg, s.c.). Similarly, DA (50, 100 and 200 micrograms, i.c.) and apomorphine (12 and 50 micrograms; i.c.) produced dose-dependent decreases in gastrointestinal transit amenable to blockade by the classical DA receptor antagonist haloperidol (10 micrograms, i.c.). The responses to apomorphine (3, 5 and 10 mg/kg, s.c.) were unaltered by 6-hydroxydopamine (100 mg/kg, i.p.)-induced sympathectomy but were antagonized by both propranolol (1 mg/kg, s.c.) and phentolamine (5 mg/kg, s.c.). Significantly, after bilateral (cervical) vagotomy, gastrointestinal transit was markedly reduced, but apomorphine (5 mg/kg, s.c.) apparently further reduced gastrointestinal transit. The D1 agonists fenoldopam (5, 10 and 20 mg/kg, s.c.) significantly reduced GIT. Fenoldopam-induced antitransit effects were markedly modified by the D1 receptor antagonist, SCH 23390 (5 mg/kg, s.c.); only the response induced by 5 mg/kg of fenoldopam was apparently antagonized by SCH 23390. The mixed D2 and D3 receptor agonist quinpirole (4 and 8 mg/kg, s.c.; or 8 mg/kg, i.p.; 200 micrograms, i.t.) did mimic DA eliciting significant reductions in gastrointestinal transit which, however, were not antagonized by domperidone (5 mg/kg, s.c.). Taken together, the present results support the contention that the decrease in rat gastrointestinal transit induced by DA and apomorphine may be mediated by an interaction with central and/or peripheral D2 receptors. The presence of dopamine receptors (D2) in the alimentary canal are strengthened by antitransit effect of fenoldopam and bromocriptine in the gastrointestinal tract.


Assuntos
Trânsito Gastrointestinal/efeitos dos fármacos , Receptores Adrenérgicos alfa/fisiologia , Receptores Adrenérgicos beta/fisiologia , Receptores de Dopamina D2/fisiologia , Animais , Dopamina/farmacologia , Dopaminérgicos/farmacologia , Vias de Administração de Medicamentos , Feminino , Masculino , Ratos , Ratos Wistar , Simpatectomia Química , Vagotomia
10.
J Pharm Sci ; 82(2): 167-9, 1993 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-8445529

RESUMO

Several 1-(4-biphenoxyacetyl)-4-substituted arylthiosemicarbazides and their corresponding cyclized 2-(4-biphenoxymethyl)-5-arylamino-1,3,4- oxadiazoles were synthesized and characterized by elemental analyses and IR, mass, and nuclear magnetic resonance spectra. All compounds were evaluated for anti-inflammatory activity by determining their ability to provide protection against carrageenin-induced edema in rat paw. The anti-inflammatory activity possessed by substituted thiosemicarbazides [100 mg/kg, intraperitoneal(ip)] ranged from 22 to 68%, whereas substituted 1,3,4-oxadiazoles (100 mg/kg, ip) provided protection of 10-76%. Hydrocortisone (10 mg/kg, ip) and oxyphenbutazone (40 mg/kg, ip), used as standard reference drugs, decreased edema in rat paw by 44.6 and 52.9%, respectively. All compounds (1 mM) possessed antiproteolytic activity that was reflected by their ability to cause in vitro inhibition of trypsin-induced hydrolysis of bovine serum albumin. This inhibition ranged between 43 and 72% for substituted thiosemicarbazides and 30 and 83% for substituted 1,3,4-oxadiazoles.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Oxidiazóis/síntese química , Tiossemicarbazonas/síntese química , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Carragenina , Fenômenos Químicos , Físico-Química , Edema/induzido quimicamente , Edema/prevenção & controle , Feminino , Masculino , Oxidiazóis/farmacologia , Ratos , Soroalbumina Bovina/metabolismo , Tiossemicarbazonas/farmacologia , Inibidores da Tripsina/farmacologia
11.
Biochem Pharmacol ; 41(3): 476-8, 1991 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-1994908

RESUMO

We observed a remarkable augmentation in the rate of hydrolytic breakdown of HCHS following exposure to corticosteroid therapy. This underscores the need for a careful reappraisal of its dosage in long term therapy. In such an event the uncharged ester may be the preferred drug of choice.


Assuntos
Hidrolases de Éster Carboxílico/metabolismo , Hidrocortisona/análogos & derivados , Hidrocortisona/farmacologia , Microssomos Hepáticos/efeitos dos fármacos , Animais , Interações Medicamentosas , Ativação Enzimática/efeitos dos fármacos , Hidrocortisona/administração & dosagem , Hidrocortisona/farmacocinética , Masculino , Microssomos Hepáticos/enzimologia , Ratos
12.
Arzneimittelforschung ; 41(2): 101-3, 1991 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-2043168

RESUMO

Sixteen new 2,3-dihydro-N-(substituted phenyl)-spiro (benzo [b] cyclopenta [e][1,4] diazepine-10(1H), 1'-cyclopentane)-9(10aH)-ethanamines, whose structures were confirmed by correct elemental analyses, IR, NMR and mass spectral studies, were synthesized and evaluated for anticonvulsant and analgesic activity in vivo and monoamine oxidase (MAO) inhibitory activities in vitro. The compounds exhibiting significant anticonvulsant and analgesic activity also showed marked inhibition of the enzyme MAO. The low toxicity of these compounds was reflected by their high approximate LD50 values.


Assuntos
Anticonvulsivantes , Benzodiazepinas/farmacologia , Inibidores da Monoaminoxidase , Analgésicos , Animais , Benzodiazepinas/síntese química , Benzodiazepinas/química , Encéfalo/efeitos dos fármacos , Encéfalo/enzimologia , Feminino , Técnicas In Vitro , Dose Letal Mediana , Masculino , Camundongos , Ratos
13.
J Pharm Sci ; 79(4): 317-20, 1990 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-2352142

RESUMO

Eight substituted quinazolonoformazans were synthesized and evaluated for anti-inflammatory activity. The degree of protection provided by seven of these compounds, at a dose of 100 mg/kg, po, against carrageenin-induced edema in rat paw ranged from 26 to 57%. The four active substituted quinazolonoformazans (1, 2, 6, 8), on further evaluation for antiwrithmogenic activity, provided 10-80% protection against the aconitine-induced writhing response in mice. The ulcerogenic liabilities of two of the most active compounds were also determined. The doses producing ulcers in 50% of the treated rats (UD50) were 155 and 260 mg/kg, ip, for 2 and 8, respectively. The low toxicities possessed by these substituted quinazolonoformazans were indicated by their LD50 values which ranged from 600 to 1300 mg/kg, ip, in mice.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Compostos Azo/síntese química , Formazans/síntese química , Quinazolinas/síntese química , Animais , Anti-Inflamatórios não Esteroides/toxicidade , Carragenina , Fenômenos Químicos , Química , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Formazans/farmacologia , Formazans/toxicidade , Masculino , Camundongos , Quinazolinas/farmacologia , Quinazolinas/toxicidade , Ratos , Úlcera Gástrica/induzido quimicamente
14.
Agents Actions ; 29(3-4): 189-95, 1990 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-2339664

RESUMO

Inflammatory processes may be suppressed by endogenous mechanisms such as release of adrenocorticosteroid hormones through stimulation of the hypothalamus-pituitary-adrenal axis. In the present study, the relationship between the temporal development of carrageenan-induced edema in the hindlimb of the rat and release in plasma of the principal endogenous adrenocorticosteroid of the rat corticosterone was investigated. Suplantar injection of carrageenan produced a biphasic increase in basal plasma corticosterone levels that was not attributed to diurnal variation. The plasma level of corticosterone increased rapidly after injection of carrageenan and peaked 12-fold at 20 min. This first phase increase was attributed to the stress of the injection since it was mimicked by subplantar injection of saline. The second phase of corticosterone release was gradual and peaked 12-fold 7 hr after injection of carrageenan. The second phase was not elicited by subplantar injection of saline. When the hypothalamus-pituitary-adrenal axis is impaired via hypophysectomy, carrageenan-induced edema is more intense and lasts longer than in control rats. The results demonstrate that adrenocorticosteroid hormones are released as a result of the stress of injection and by the inflammatory response. Release of adrenocorticosteroids acts as a feedback mechanism to suppress the inflammatory response.


Assuntos
Corticosterona/sangue , Inflamação/sangue , Animais , Carragenina , Edema/sangue , Edema/induzido quimicamente , Hipofisectomia , Inflamação/induzido quimicamente , Cinética , Masculino , Ratos , Ratos Endogâmicos
15.
J Pharm Sci ; 78(12): 999-1002, 1989 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-2614702

RESUMO

Various 2-(4-biphenoxymethyl)-5-arylamino-1,3,4-oxadiazoles were synthesized by cyclization of the corresponding 1-(4-biphenoxyacetyl)-4-substituted thiosemicarbazides. These compounds were characterized by their elemental analyses and infrared, mass, and nuclear magnetic resonance spectral data. All substituted thiosemicarbazides (100 mg/kg, ip) and cyclized substituted oxadiazoles (100 mg/kg, ip) possessed anti-inflammatory activity, as reflected by their ability to provide protection against carrageenin-induced edema in the rat paw which ranged from 28 to 68% and 36 to 76%, respectively. Cyclization of the substituted thiosemicarbazides, in general, resulted in an increase in the anti-inflammatory activity of their corresponding substituted oxadiazoles, with the exception of those containing 2,4-dimethyl and 3,4-dimethyl substituents in their molecular structure. Hydrocortisone (10 mg/kg, ip) and oxyphenbutazone (40 mg/kg, ip) were used as the standard reference drugs and these provided 45 and 53% protection, respectively. All compounds (1 mM) possessed antiproteolytic activity and the in vitro inhibition of trypsin-induced hydrolysis of bovine serum albumin ranged from 13 to 75% for substituted thiosemicarbazides and 39 to 70% for substituted oxadiazoles. There was no relationship between the anti-inflammatory activity of substituted thiosemicarbazides and substituted oxadiazoles and their antiproteolytic effectiveness. The low toxicity of these compounds was reflected by their high approximate LD50 values, ranging from 500 to 1000 mg/kg.


Assuntos
Anti-Inflamatórios não Esteroides , Oxidiazóis/farmacologia , Animais , Edema/induzido quimicamente , Edema/fisiopatologia , Feminino , Dose Letal Mediana , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Oxidiazóis/toxicidade , Inibidores de Proteases , Ratos
16.
Physiol Behav ; 46(1): 105-6, 1989 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2530597

RESUMO

The neuromodulatory role of serotonin in the anticonvulsant activity of methaqualone was investigated. A dose-dependent increase in the ability of methaqualone to provide protection against pentylenetetrazol (90 mg/kg SC)-induced convulsions in mice was observed. The ED50 value for the anticonvulsant activity of methaqualone was calculated and found to be 60 mg/kg, IP. Pretreatment of mice with 5-hydroxytryptophan (100 mg/kg, IP, 2 hr) and p-chlorophenylalanine (300 mg/kg, IP, 2 hr), causing an increase in brain serotonin levels, resulted in a 60% and 80% increase, respectively, in the anticonvulsant activity of methaqualone. Similar pretreatment with p-chlorophenylalanine (300 mg/kg, IP, 48 hr), causing a lowering of brain serotonin, and methysergide (10 mg/kg, IP, 0.5 hr), causing blockade of brain serotonin receptors, resulted in a 40% and 20% decrease, respectively, in the ability of methaqualone to provide protection against pentylenetetrazol-induced convulsions. These results suggest a facilitatory role of serotonin in the anticonvulsant activity of methaqualone.


Assuntos
Anticonvulsivantes , Encéfalo/efeitos dos fármacos , Metaqualona/farmacologia , Pentilenotetrazol/farmacologia , Receptores de Serotonina/efeitos dos fármacos , Convulsões/induzido quimicamente , Serotonina/fisiologia , 5-Hidroxitriptofano/farmacologia , Animais , Relação Dose-Resposta a Droga , Fenclonina/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos , Convulsões/prevenção & controle , Triptofano/farmacologia
17.
Physiol Behav ; 46(1): 35-7, 1989 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2530601

RESUMO

The role of serotonin in the mediation of the anticonvulsant activity of JAW-669 was investigated against maximal electric shock (MES)-induced seizures in mice. A dose-dependent protection against seizures was provided by JAW-669 (4, 6 and 8 mg/kg, IP) and the calculated ED50 value was 6.01 mg/kg, IP. Pretreatment of mice with 5-hydroxytryptophan (50 mg/kg, IP) 2 hr before the administration of JAW-669 (6.01 mg/kg, IP) was found to cause a 40% increase in the ability of JAW-669 to provide protection against MES-induced seizures. Similar pretreatment with tryptophan (100 mg/kg, IP, 1 hr) caused a 30% decrease in the anticonvulsant activity of JAW-669. Prior administration of p-chlorophenylalanine (300 mg/kg, IP, 48 hr) and methysergide (10 mg/kg, IP; 0.5 hr) before administration of JAW-699 caused a 66% and 74% decrease, respectively, in the ability of JAW-669 to provide protection against MES-induced seizures. These results suggest a facilitatory role of serotonin in the anticonvulsant activity of JAW-669.


Assuntos
Anticonvulsivantes/farmacologia , Compostos de Bifenilo/farmacologia , Encéfalo/efeitos dos fármacos , Excitação Neurológica/efeitos dos fármacos , Propanolaminas/farmacologia , Receptores de Serotonina/efeitos dos fármacos , Serotonina/fisiologia , 5-Hidroxitriptofano/farmacologia , Animais , Relação Dose-Resposta a Droga , Eletrochoque , Fenclonina/farmacologia , Masculino , Metisergida/farmacologia , Camundongos , Camundongos Endogâmicos , Triptofano/farmacologia
18.
Physiol Behav ; 46(1): 101-4, 1989 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2554350

RESUMO

PN200-110 is a recently introduced 1,4-dihydropyridine which has been demonstrated to be a potent calcium channel blocker. 3HPN has been shown to bind in a specific saturable manner to P2 fractions obtained from brain homogenates from male Sprague-Dawley rats. 3HPN binding was found to be temperature-dependent. Specific 3HPN binding was maximal at 25 degrees C; binding decreased at 2 degrees C and 37 degrees C. The KD calculated from Scatchard analysis was 0.0943 +/- 0.0038 nM while the Bmax was found to be 109.1 +/- 2.3 fmol/mg protein. A concentration dependent inhibition of 3HPN binding by various cations was determined and found to be as follows: ZN2+ greater than La3+ greater than Rh3+, Al3+ greater than Co2+, Ni2+, Mn2+ greater than Ca2+, Mg2+ greater than Ba2+ greater than Sr2+. These results provide evidence for the existence of central high affinity dihydropyridine receptor sites in rat brain.


Assuntos
Encéfalo/metabolismo , Bloqueadores dos Canais de Cálcio , Oxidiazóis/farmacocinética , Animais , Canais de Cálcio , Isradipino , Masculino , Nifedipino/farmacocinética , Ensaio Radioligante , Ratos , Ratos Endogâmicos , Receptores Nicotínicos/fisiologia , Sinaptossomos/metabolismo
19.
Physiol Behav ; 46(1): 107-8, 1989 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2554351

RESUMO

Cyclic-AMP levels in unaffected and affected cancerous portions of human lung preparations were determined by measuring displaced 3H-cyclic-AMP from the specific binding protein by unlabeled ligand. The levels of cyclic-AMP in unaffected portions of human lungs ranged between 52-116 pmoles/g protein. Significantly higher levels of cyclic-AMP were found in lung samples affected with squamous cell carcinoma, adenocarcinoma and malignant melanoma with the mean values being 251, 290, and 509 pmoles/g protein, respectively. On the other hand, a decrease in the level of cyclic-AMP to 39 pmoles/g protein was observed in portions of lungs affected with granuloma. These results suggest that the level of cyclic-AMP in lung tissue may reflect the malignant or benign nature of the pulmonary disease.


Assuntos
Adenocarcinoma/patologia , Carcinoma de Células Escamosas/patologia , Proteína Receptora de AMP Cíclico , AMP Cíclico/metabolismo , Neoplasias Pulmonares/patologia , Melanoma/patologia , Proteínas de Transporte/metabolismo , Granuloma/patologia , Humanos , Pulmão/patologia , Pneumopatias/patologia
20.
Res Commun Chem Pathol Pharmacol ; 64(3): 485-8, 1989 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-2571179

RESUMO

Apomorphine (3.5 and 10 mg/kg, s.c.) and morphine (1.3 and 10 mg/kg, s.c.) produced a dose-dependent decrease in gastrointestinal transit of charcoal dust in rats. The involvement of dopamine in such a constipatory effect was found to be mediated to a greater extent by DA2 than by DA1 receptors, using a specific DA1 antagonist (SCH 23390) and DA2 antagonists (alizapride, domperidone). The decrease in apomorphine (50 micrograms) and dopamine (100 and 200 micrograms)-induced gastrointestinal transit after intracisternal administration was antagonized by haloperidol. These results provide evidence for the involvement of dopamine receptors in the constipatory effects of apomorphine and morphine in rats.


Assuntos
Motilidade Gastrointestinal/efeitos dos fármacos , Receptores Dopaminérgicos/efeitos dos fármacos , Animais , Apomorfina/farmacologia , Benzazepinas/farmacologia , Domperidona/farmacologia , Dopaminérgicos/farmacologia , Antagonistas de Dopamina , Relação Dose-Resposta a Droga , Feminino , Trânsito Gastrointestinal/efeitos dos fármacos , Haloperidol/farmacologia , Técnicas In Vitro , Masculino , Morfina/farmacologia , Pirrolidinas/farmacologia , Ratos , Ratos Endogâmicos
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