The flumazenil analogue, Ro 16-0154, a benzodiazepine partial inverse agonist, has been labeled by halogen exchange to enable SPECT investigations of central benzodiazepine receptors in the human brain. The purified 123I-Ro 16-0154 was found to be stable in rat brain preparations and to be metabolized in rat liver preparations. Its pharmacologic properties were comparable to those of flumazenil...

Delirium tremens might last for weeks and treatment requires massive benzodiazepine doses, yet it is possible to manage patients with this condition successfully. In this case of delirium tremens, standard agents at the usual recommended doses were not sufficient to achieve control of confusion and agitation or to stabilize neurologic and cardiovascular parameters. The patient required extraord...

Rhesus monkeys were trained to discriminate injections of saline from those of 8-carboline-3-carboxylic acid ethyl ester (8-CCE), a compound that binds to the benzodiazepine receptor, but often has actions opposite to those of the benzodiazeplnes. A benzodlazepine agonist midazolam and low doses of a specific benzodiazepine antagonist, Ro 15-1788, reversed the discriminative effects of 8-CCE. H...

Cross-reactivities of some over-the-counter and uncontrolled prescription drugs with the immunoassays of some classes of drugs of abuse have been reported (1–17). Chemical structure similarity is a cause for cross-reactivity in immunoassays because the cross-reacting compound can fit onto the active sites in the antibody that has been developed for the drug of abuse or its chemical class. Howev...

Data from a hospital-based drug surveillance programme were used to determine how often benzodiazepine drugs were used in general medical wards. Benzodiazepines were the drugs most commonly used as hypnotics and were given to 32% of these patients. Concomitant use of more than one benzodiazepine drug or of benzodiazepines with other psychoactive drugs was common and often irrational. A series o...

QSAR of the binding affinities of [2-phenylimidazo[1,2-a]pyridin-3-yl]acetamide derivatives (Fig. 1) with central and peripheral (from cortex and ovary) benzodiazepine receptors has been explored using physico-chemical parameters. Attempt has been made to explore the structural and/or physico-chemical requirements of the compounds that are responsible for the selective action against peripheral...

We report two serious and unusual complications of benzodiazepine withdrawal in a single patient: takotsubo cardiomyopathy and catatonia. This 61-year-old female patient was brought to the emergency department with lethargy and within hours had declined into a state of catatonia. Although there was never a complaint of chest pain, ECG showed deep anterior T-wave inversions and cardiac enzymes w...

I report how some adulterants affect results for drugs of abuse in urine as measured by Roche RIA, Syva emit d.a.u., and Abbott TDx fpia (fluorescence polarization immunoassay) for the following drugs: amphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine, opiates, and phencyclidine (PCP). Sodium chloride interfered negatively with all of these drugs when assayed by emit and caused...

Benzodiazepines and benzodiazepine receptor agonists (e.g., zaleplon [Sonata], zolpidem [Ambien]) are widely used to treat anxiety and insomnia, even though antidepressants are first-line therapy for anxiety disorders based on the evidence.1 In this issue of American Family Physician, Drs. Ramar and Olson review the management of insomnia and other sleep disorders.2 When benzodiazepines are use...

Ventilatory response to CO2 was measured before and after two different benzodiazepine hypnotics in both chronic bronchitics and patients without chest disease. Flurazepam, but not nitrazepam, produced a significant decrease in CO2 sensitivity, although there was no significant change in FEV1 or mixed venous PCO2. This is the first unequivocal evidence of central depression of respiration by a ...