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1.
Acta Anaesthesiol Scand ; 45(1): 59-64, 2001 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-11152035

RESUMEN

BACKGROUND: Strabismus correction in children is associated with a high incidence of postoperative nausea and vomiting. The purpose of this prospective, double-blind study was to examine the influence of the surgical method for correction of squint on the incidence of postoperative vomiting. METHODS: One hundred and twenty consecutive children aged 2-12 years, scheduled for elective strabismus surgery, were enrolled in this prospective, double-blind study. A standardised total intravenous anaesthesia was given to all children. The development of perioperative oculocardiac reflex was noted and the number of episodes of vomiting during the first 48 h postoperatively was recorded. At the completion of the study, the children who were operated with myopexy according to Faden, were allocated to a Faden group, those without a myopexy to the non-Faden group. All the patients included in this study were operated on by the same surgeon with standardised techniques. RESULTS: The Faden group was younger, lighter and the operation time was longer (P<0.05). The incidence of vomiting was greater in the Faden group; 53% versus 12% (P<0.05). The incidence of oculocardiac reflex was similar in both groups; 40% in the Faden versus 28% in the non-Faden group, respectively. The total dose of propofol and alfentanil was similar between the groups. Requirement of analgesics for postoperative pain was similar in both groups. The only independent risk factor for postoperative vomiting was the Faden operation. CONCLUSION: The surgical method used for strabismus correction in children has a great influence on the incidence of postoperative vomiting. The Faden operation is associated with a very high incidence of postoperative vomiting; this particular group of patients has to be considered as a high risk group for postoperative vomiting and deserves an antiemetic prophylaxis.


Asunto(s)
Procedimientos Quirúrgicos Oftalmológicos , Náusea y Vómito Posoperatorios/epidemiología , Estrabismo/cirugía , Alfentanilo , Analgésicos Opioides , Anestesia Intravenosa , Anestésicos Intravenosos , Niño , Preescolar , Método Doble Ciego , Femenino , Humanos , Masculino , Proyectos Piloto , Propofol , Estudios Prospectivos , Reflejo Oculocardíaco/fisiología
2.
J Med Chem ; 38(16): 3086-93, 1995 Aug 04.
Artículo en Inglés | MEDLINE | ID: mdl-7636872

RESUMEN

A series of 2 beta-alkyl-3 beta-phenyltropanes (i.e., the 2 beta-alkyl analogues of the WIN series) were prepared as analogues of cocaine and tested for their ability to displace [3H]mazindol binding and to inhibit high-affinity dopamine uptake into striatal nerve endings (synaptosomes). These 2 beta-alkyl analogues were readily prepared in optically pure form starting from cocaine by proceeding through the 2 beta-phenyl-bearing aldehyde 6 as a key intermediate. Wittig reaction of 6 with the appropriate phosphorane and hydrogenation delivered the final products. All new compounds with the exception of 8e were found to exhibit nanomolar or subnanomolar affinity for the cocaine binding site in the rat striatum. These results are in apparent opposition to the binding model previously proposed which suggests a hydrogen bond donor-acceptor interaction to be present in the vicinity of the C-2 substituent. Taken together with our previous reports and recent findings from other laboratories, we suggest a new pharmacophore model in which 2 beta-substituents lacking H-bond acceptors enhance affinity to the binding site through hydrophobic interactions. The new SAR data contained herein may be relevant to the design of possible cocaine antagonists.


Asunto(s)
Cocaína/análogos & derivados , Glicoproteínas de Membrana , Proteínas de Transporte de Membrana , Proteínas del Tejido Nervioso , Tropanos/metabolismo , Animales , Proteínas Portadoras/metabolismo , Cocaína/metabolismo , Cuerpo Estriado/metabolismo , Dopamina/metabolismo , Proteínas de Transporte de Dopamina a través de la Membrana Plasmática , Ligandos , Mazindol/metabolismo , Ratas , Receptores de Droga/metabolismo , Relación Estructura-Actividad , Sinaptosomas/metabolismo , Tropanos/química
4.
J Med Chem ; 37(20): 3440-2, 1994 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-7932572

RESUMEN

Six new N-sulfonylated analogs of cocaine have been prepared, and these compounds have been evaluated for their ability to inhibit [3H]mazindol binding and [3H]dopamine uptake into striatal synaptosomes. The N-sulfonyl compounds still inhibited binding and uptake at low micromolar concentrations despite the neutral character of the tropane nitrogen, thus suggesting that the binding of cocaine to the dopamine transporter may not require protonation of its nitrogen and ionic interaction with its recognition site.


Asunto(s)
Cocaína/análogos & derivados , Cocaína/metabolismo , Glicoproteínas de Membrana , Proteínas de Transporte de Membrana , Proteínas del Tejido Nervioso , Ácidos Sulfínicos/química , Sulfonamidas/síntesis química , Animales , Sitios de Unión , Proteínas Portadoras/química , Proteínas Portadoras/metabolismo , Membrana Celular/efectos de los fármacos , Membrana Celular/metabolismo , Cocaína/química , Cuerpo Estriado/metabolismo , Dopamina/metabolismo , Proteínas de Transporte de Dopamina a través de la Membrana Plasmática , Mazindol/metabolismo , Ratas , Relación Estructura-Actividad , Sulfonamidas/metabolismo , Sulfonamidas/farmacología , Sinaptosomas/efectos de los fármacos , Sinaptosomas/metabolismo
5.
Anesth Analg ; 78(6): 1110-3, 1994 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-8198266

RESUMEN

In a prospective, randomized, double-blind clinical trial, we compared the efficacy of propofol and naloxone for the treatment of spinal-morphine-induced pruritus. Forty patients presenting with severe pruritus within 24 h of epidural morphine administration were allocated to receive either propofol 10 mg intravenously (i.v.) or naloxone 2 micrograms/kg. In the absence of a positive response, a second dose of the same treatment was given 5 min later. Pruritus and the level of post-operative pain were assessed every 5 min up to the end of the study period (45 min) using a verbal rating scale. The overall success rate in treating pruritus was similar in the two groups (80%). The rate of success after the first injection of the treatment drug was also similar (55%). The level of postoperative pain decreased after drug treatment in six patients (30%) in the propofol group versus none in the naloxone group (P < 0.05). Forty-five percent of the patients in the naloxone group had an increase in the level of postoperative pain versus none in the propofol group (P < 0.05). In conclusion, these results suggest that propofol and naloxone are equally effective in treating spinal-morphine-induced pruritus. However, the level of postoperative pain is significantly less in the propofol group.


Asunto(s)
Analgesia Epidural/efectos adversos , Morfina/efectos adversos , Naloxona/uso terapéutico , Dolor Postoperatorio/prevención & control , Propofol/uso terapéutico , Prurito/inducido químicamente , Adulto , Anciano , Método Doble Ciego , Procedimientos Quirúrgicos Electivos , Humanos , Persona de Mediana Edad , Estudios Prospectivos , Prurito/prevención & control
7.
Anesthesiology ; 76(4): 510-2, 1992 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-1550275

RESUMEN

We investigated the efficacy of subhypnotic doses of propofol for spinal morphine-induced pruritus in a prospective, randomized, double-blind, placebo-controlled study. Fifty patients, ASA physical status 1-3, with spinal morphine-induced pruritus were allocated to receive either 1 ml propofol (10 mg) or 1 ml placebo (Intralipid) intravenously after gynecologic, orthopedic, thoracic, or gastrointestinal surgery. In the absence of a positive response, a second drug treatment was given 5 min later. The persistence of pruritus 5 min after the second treatment dose was considered a treatment failure. All failures then received, in an open fashion, a supplementary dose of propofol (10 mg) and were reevaluated 5 min later. Both groups were well matched. The success rate was significantly greater in the propofol group (84%) than in the placebo (16%) group (P less than 0.05). Ninety percent of the treatment failures in the placebo group were successfully treated by a supplementary dose of 10 mg propofol. Eight percent of the patients (4% in each group) were resistant to all treatments, including naloxone 0.08 mg intravenously. Three patients had a slight increase in sedation in the propofol group versus none in control (not significant). The beneficial effect of treatment was longer than 60 min in 85% of patients in the propofol group and in 100% of the controls (not significant). These results suggest that propofol in a subhypnotic dose is an efficient drug treatment for spinal morphine-induced pruritus. At the dose administered (10 mg), side effects were rare and minor.


Asunto(s)
Morfina/administración & dosificación , Complicaciones Posoperatorias/tratamiento farmacológico , Propofol/administración & dosificación , Prurito/tratamiento farmacológico , Adulto , Anciano , Método Doble Ciego , Femenino , Humanos , Inyecciones Epidurales , Inyecciones Espinales , Masculino , Persona de Mediana Edad , Morfina/efectos adversos , Complicaciones Posoperatorias/inducido químicamente , Estudios Prospectivos , Prurito/inducido químicamente
8.
Anesth Analg ; 74(4): 539-41, 1992 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-1554120

RESUMEN

Propofol is associated with a low incidence of postoperative nausea and vomiting. In a prospective, randomized, double-blind, placebo-controlled study, we investigated the possible direct antiemetic properties of a subhypnotic dose of propofol. Fifty-two ASA physical status I or II patients, aged 15-60 yr with nausea and vomiting after minor gynecologic, orthopedic, or digestive tract surgery, were included in the study and received either propofol (10 mg = 1 mL) or placebo (1 mL Intralipid) intravenously in the postanesthesia care unit. Patients treated with propofol experienced a larger reduction in nausea and vomiting than patients treated with placebo (81% vs 35% success rate; P less than 0.05). Patients successfully treated had a similar incidence of relapse (propofol 28%; placebo 22%) within the first 30 min after therapy. Thirty-three percent of the propofol-treated patients and 44% of the placebo-treated patients showed a minor increase in sedation. The level of postoperative pain did not change in either group. Hemodynamic values remained unchanged in both groups. Pain on injection (7.6%) or dizziness (3.6%) only occurred in the propofol group. We conclude that propofol has significant direct antiemetic properties.


Asunto(s)
Antieméticos/uso terapéutico , Propofol/uso terapéutico , Adolescente , Adulto , Relación Dosis-Respuesta a Droga , Método Doble Ciego , Femenino , Humanos , Masculino , Persona de Mediana Edad , Náusea/prevención & control , Complicaciones Posoperatorias/prevención & control , Propofol/efectos adversos , Estudios Prospectivos , Vómitos/prevención & control
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