Sedatives Benzodiazepine

Slow gasfroinfesfinal absorption compared to other sedative benzodiazepines, so may be more effective for nocfurnal awakening fhan for initial insomnia unless dosed f-2 hours prior to bedtime... 

Anterograde amnesia may be more likely with triazolam than with other sedative benzodiazepines... 

Anxiolytics and sedatives. Benzodiazepines are safe if use is brief but prolonged use may cause somnolence or poor suckling. 

Think carefully before starting new medication. Avoid sedatives/benzodiazepines. 

CifiHijClNj. White plates m.p. 125 C. Diazepam is one of several benzodiazepines which are very widely used as minor tranquillizers for allaying anxiety, as hypnotics or, in sufficiently high dosage given intravenously, as pre-anaesthetic sedatives. 

The CCK system shares one property with the opioid system, ie, the existence of selective nonpeptide antagonists. These include aspedicine, a natural benzodiazepine (136), and Devazepide (L-364,718 MK-329) (137). Selective, potent peptide antagonists for CCK, eg, Cl-988 and PD 134308, have been developed that maybe useful as anxiolytics and as dmgs which increase the analgesic effect of morphine but at the same time prevent morphine tolerance (138) (see Hypnotics, sedatives, anticonvulsants, and anxiolytics). 

AHopregnanolone and similar A-ring-reduced pregnanes potentiate GABA effects at these receptors. These steroids mimic the effects of the benzodiazepines, changing chloride ion conductance and producing sedative and hypnotic behavioral effects (276,277). Neuroactive steroids can be therapeutically useful as anticonvulsants, anxiolytics, or anesthetics (qv) (see also Hypnotics, sedatives, anticonvulsants, and anxiolytics). 

Combinations of barbiturates and benzodiazepine tranquilizers or even antihistaminergics having sedative properties are sometimes used. Furthermore, infusion of anesthetics can be used to provide long-term anesthesia for intensive care medicine. The antagonist flumazenil (18) is available to reverse the effects of anesthetics of the benzodiazepine class. 

The benzodiazepine fused azetes (353 R = Et, Pr) have been claimed as useful tranquilizers and sedatives (76BRP1448895). However, their stability and formation from benzodiazepines (352) by reaction with an aldehyde and base is hard to reconcile with the proposed structure. 

Benzodiazepines as antianxiety agents, 1, 170 as anticonvulsants, 1, 166 organometallic complexes, 7, 604 as sedatives, 1, 166 IH- 1,2-Benzodiazepines conversion to 3H-1,2-benzodiazepines, 7, 604 synthesis, 7, 597, 598, 604 3H-1,2-Benzodiazepines acid-catalyzed reactions, 7, 601 nucleophilic reactions, 7, 604 oxidation, 7, 603 synthesis, 7, 596 thermal reactions, 7, 600 5H-1,2-Benzodiazepines photochemical reactions, 7, 599 synthesis, 7, 603... 

Anxiolytics are drugs used for the treatment of anxiety disorders. Apart from benzodiazpines, a frequently used anxiolytic is the 5HT1A (serotonin) receptor agonist buspiron, which has no sedative, amnestic or muscle-relaxant side effects, but whose action takes about a week to develop. Furthermore, it is less efficaceous than the benzodiazepines. Buspiron s mechanism of action is not fully understood. 

A class of sedative/hypnotic type drug that exert their effects through the benzodiazepine binding site on GABAa receptors. The class consists both of molecules that contain the benzodiazepine moiety, for example diazepam, lorazepam and flunitrazepam, and the newer, non-benzodiazepine compounds such as zolpidem, zopiclone, indiplon and zaleplon. BzRAs are primarily used for the treatment of anxiety, insomnia and to elicit varying levels of sedation. The wide selection of compounds currently available affords the prescribing clinician extensive options in terms of relative efficacies and durations of action. 

Benzodiazepines have found wide therapeutic applications as anxiolytics, sedatives, hypnotics, anticonvulsants, and central muscle relaxants. 

The definition of desired therapeutic and side effects in the case of the benzodiazepines very much depends on the clinical problem in question. The sedative and hypnotic actions are desired effects in the treatment of insomnia, but undesired effects in the treatment of anxiety disorders. Effects that are usually undesired include daytime drowsiness, potentiation of the sedative effects of ethanol, and anterograde amnesia. They are mediated via the benzodiazepine site of GABAa receptors, since they can be antagonized with flumazenil. 

McKernan RM, Rosahl TW, Reynolds DS et al (2000) Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAa receptor al subtype. Nat Neurosci 3 587-592... 

However, lorazepam and oxazepam are relatively safe for older adults when given in normal dosages. Buspirone (BuSpar) also is a safe choice for older adults with anxiety because it does not cause excessive sedation, and the risk of falling is not as great. Before bus-pirone therapy is begun, benzodiazepines and sedatives and hypnotics are gradually withdrawn. Buspirone, unlike most of the benzodiazepines, must be taken regularly and is not effective on an as-needed basis. 

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