Evidence of lowest brain penetration of an antiemetic drug, metopimazine, compared to domperidone, metoclopramide and chlorpromazine, using an in vitro model of the blood-brain barrier.

PURPOSE: The objective of the current study was to determine the ability of some antiemetic compounds to cross the blood-brain barrier (BBB) and thereby to determine possible side effects of compounds for the central nervous system (CNS). METHODS: We compared the brain penetration of some antiemetic compounds using an in vitro BBB model consisting in brain capillary endothelial cells co-cultured with primary rat glial cells. RESULTS: This study clearly demonstrated that the metopimazine metabolite, metopimazine acid, has a very low brain penetration, lower than metopimazine and even less than the other antiemetic compounds tested in this study. CONCLUSIONS: The poor brain penetration of metopimazine acid, metopimazine biodisponible form, seems very likely related to the clinically observed difference in therapeutic and safety profile.     

Opioid receptor binding in parahippocampus of patients with temporal lobe epilepsy: its association with the antiepileptic effects of subacute electrical stimulation.

Opioid receptor binding was evaluated in parahippocampal cortex (PHC) obtained from patients with intractable mesial temporal lobe epilepsy (MTLE) with and without subacute high frequency electrical stimulation (HFS) in this brain area. Mu, delta and nociceptin receptor binding was determined by autoradiography in PHC of five patients (ESAE group) with MTLE history of 14.8 +/- 2.5 years and seizure frequency of 11 +/- 2.9 per month, two of them (40%) with mesial sclerosis. This group demonstrated antiepileptic effects following subacute HFS (130 Hz, 450 micros, 200-400 microA), applied continuously during 16-20 days in PHC. Values were compared with those obtained from patients with severe MTLE (history of 21.7 +/- 2.8 years and seizure frequency of 28.2 +/- 14 per month) in whom electrical stimulation did not induce antiepileptic effects (ESWAE group, n = 4), patients with MTLE in whom no electrical stimulation was applied (MTLE group, n = 4) and autopsy material acquired from subjects without epilepsy (n = 4 obtained from three subjects). Enhanced 3H-DAMGO (MTLE, 755%; ESAE, 375%; ESWAE, 693%), 3H-DPDPE (MTLE, 242%; ESAE, 80%; ESWAE, 346%) and 3H-nociceptin (MTLE, 424%; ESAE, 217%; ESWAE, 451%) binding was detected in the PHC of all epileptic groups. However, tissue obtained from ESAE group demonstrated lower opioid receptor binding (3H-DAMGO, 44.5%, p < 0.05; 3H-DPDPE, 47%, p < 0.05; 3H-nociceptin, 39.3%, p < 0.5) when compared with MTLE group. The present results indicate that a high effectiveness to the antiepileptic effects induced by HFS is associated with reduced opioid peptide binding.     

Treatment of the Breast’s Lateral Pole: Adjuvant Maneuver to Pitanguy’s Technique

Surgical procedures for the mammary region currently are assuming an important role in body-contouring surgery. Enhancement of results is a constant challenge to the plastic surgeon. A simple and efficient maneuver for resection of the breast’s lateral pole based on the mammoplasty technique of Professor Ivo Pitanguy is described. This study realized at the Private Clinic Sérgio Carreir?o, Rio de Janeiro, RJ, Brazil.     

Postoperative pain management—clinical practice is still not optimal

Major progress in clinical pain assessment and management has been achieved in the last decade. More effective analgesic drugs and improved techniques for pain management have been introduced. However, medical reports published during the last few years on postoperative pain management (POPM) indicate that moderate or even severe pain is still rather commonly experienced by surgical patients in the early postoperative period and that worst-pain-episodes may occur even in the late postoperative phase. Insufficient relief of postoperative pain seems a more common problem on surgical wards than on a postanaesthesia care unit (PACU). The aims of POPM are to inhibit autonomic trauma-induced nociceptive impulses that may result in functional disturbances of vital organs and thereby affect the incidence of potentially severe complications influencing clinical outcome. Considering that recent studies continue to show sub-optimal pain management despite the availability of effective drugs and analgesic techniques it must be considered essential to identify possible barriers to effective pain management in clinical practice so that necessary improvements in POPM routines can be carried out.     

Unusual central chorioretinitis as the first manifestation of early secondary syphilis

Three young, otherwise healthy patients had a similar picture of unilateral central chorioretinitis associated with severe visual loss. Fluorescein angiography disclosed diffuse leakage under the neurosensory retina in the posterior pole, associated with multifocal areas of staining along the retinal vessels. Systemic examination showed a positive fluorescent treponemal antibody absorption test and a sharp increase in VDRL titers, indicative of active secondary syphilis. The patients responded dramatically to penicillin treatment, with visual recovery and resolution of the fundus lesions.