The story of modern tranquilliser drugs
Adam Doble, Ian L Martin, David Nutt in Calming the Brain: Benzodiazepines and related drugs from laboratory to clinic, 2020
Benzodiazepines were discovered quite serendipitously. Following on the heels of chlorpromazine, chemists at Hoffmann-La Roche in Basel were trying to develop new major tranquilliser drugs. Bromides are unsatisfactory sedatives and no longer used to any extent due to the availability of more suitable drugs. In contrast, certain antidepressant drugs which inhibit serotonin reuptake, such as venlafaxine, have demonstrated activity in generalised anxiety disorder, and have been approved for use in this indication. Buspirone has clear anxiolytic properties, but, unlike benzodi-azepines, has a delayed onset of action that makes it less interesting in this indication than benzodiazepine anxiolytics that act immediately. Long-acting barbiturates are still, however, sometimes used in the treatment of epilepsy, since benzodiazepines are not usually of lasting benefit in this indication. Long-acting barbiturates are, however, sometimes used in the treatment of epilepsy, since benzodiazepines are not usually of lasting benefit in this indication.
Central Venous Access: Subclavian Vein
Rahul Jandial, Danielle D. Jandial in Code Blue, 2014
This chapter provides information for performing central venous access in subclavian vein. It begins with a case scenario of a 33-year-old man who is presented with a closed head injury requiring barbiturate coma. The chapter then includes details on indications, contraindications, and information about supplies, positioning and technique. Pearls and pitfalls are also incorporated, providing additional insights and practical advice not always available in other textbooks or articles. If the patient is hypotensive and health care professional are unsure whether the subclavian vein or artery has been entered, compare the color of the withdrawn blood with a specimen from an arterial line, or attach a pressure transducer and IV tubing to the needle to obtain pressure (arterial versus venous).
Assessment by Nuclear Magnetic Resonance Spectroscopy of the Effects of Cardiopulmonary Bypass, Hypothermia, and Circulatory Arrest on the Brain
Richard A. Jonas, Jane W. Newburger, Joseph J. Volpe, John W. Kirklin in Brain Injury and Pediatric Cardiac Surgery, 2019
A series of investigations were undertaken to determine the effects of cardiopulmonary bypass, hypothermia, hyperglycemia, and barbiturates on cerebral high-energy content and intracellular pH, as measured by nuclear magnetic resonance spectroscopy in an adolescent sheep model. The sheep were cooled to 15°C, subjected to one hour of circulatory arrest, which was followed by two hours of reperfusion. Barbiturates may be beneficial because of anticonvulsant and antioxidant properties and because they decrease brain oxygen consumption. Barbiturates have been advocated for cerebroprotection during cardiac surgical procedures. Barbiturates may be beneficial because of anticonvulsant and antioxidant properties and because they decrease brain oxygen consumption. Hypothermia is the mainstay of cerebral protection because it increases ischemic tolerance. Diabetic patients with hyperglycemia who have strokes have a worse outcome than normoglycemic patients. The mechanism postulated for these findings is that hyperglycemia supplies additional substrate for anaerobic metabolism during ischemia.
New barbiturates and thiobarbiturates as potential enzyme inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2015
Ashfaq M Qureshi, Saira Mumtaz, Abdul Rauf, Muhammad Ashraf, Rumana Nasar, Zahid H Chohan
A series of 27 new barbiturates and thiobarbiturates have been synthesized by a convenient multi-component reaction in overall excellent yields (87–96%). All the synthesized compounds were characterized by 1H, 13C NMR, EIMS and elemental analysis (C, H, N and S). Furthermore, all compounds were screened for in vitro antioxidant (DPPH radical scavenging), lipoxygenase, chymotrypsin, α-glucosidase and anti-urease activities. Out of the series, 23 in DPPH, 14 in lipoxygenase, 2 in chymotrypsin have shown appreciable IC50 values.
The Effects of High-dose Barbiturates on the Acoustic Reflex and Auditory Evoked Responses: Two Case Reports
Published in Acta Oto-Laryngologica, 1985
The effects of high-dose barbiturates (pentobarbital) on the acoustic reflex, and the auditory brainstem (ABR) and middle-latency (AMR) responses, are illustrated with two case reports. Auditory electrophysiologic data were recorded serially during recovery from therapeutic barbiturate coma. ABR latency remained within normal limits in barbiturate coma, but amplitude of the wave I component was abnormally augmented. Contralateral and ipsilateral acoustic reflex activity, and the Pa component of the AMR, were not observed in barbiturate coma, and reappeared with the emergence of brainstem neurologic signs. These findings suggest a fundamental difference in the neurophysiologic substrate of the ABR vs. acoustic reflex and AMR. Possible mechanisms for the differential influence of barbiturates on these three auditory electrophysiologic measures are offered.
Temperature disturbances in traumatic brain injury: relationship to secondary insults, barbiturate treatment and outcome
Published in Neurological Research, 2008
Kristin Elf, Pelle Nilsson, Elisabeth Ronne-Engström, Tim Howells, Per Enblad
Objectives: To describe the occurrence of spontaneous hyper- and hypothermia in patients with traumatic brain injury using a computerized data collecting system, to show how temperature correlates with other secondary insults, to describe how temperature affects outcome and to show how barbiturate treatment influences those analyses. Methods: Patients with ≥ 54 hours of valid monitoring within the first 120 hours after trauma (one value/min) for temperature, intracranial pressure, cerebral perfusion pressure, systolic blood pressure, mean blood pressure and heart rate were included. Correlation analyses were performed between temperature and other secondary insult variables. The non-linear relationship between temperature and outcome (measured by Glasgow outcome scale 6 months post-trauma) was illustrated using a neural network. Results: Of the 53 patients, 44 experienced hyperthermia (>38°C) and 29 experienced hypothermia (
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