Anxiolytics lorazepam

Pregabalin produced anxiolytic effects similar to lorazepam, alprazolam, and venlafaxine in acute trials. Sedation and dizziness were the most common adverse effects, and the dose should be tapered over 1 week upon discontinuation. 

In the presence of cirrhosis or other liver impairment, lorazepam or oxazepam should be utilized for detoxification. These two benzodiazepines have no active hepatic metabolites and are generally considered safer choices for patients with liver damage. Once the starting point for the taper is determined, the dose is decreased by 10-20% per day. It is important to note that this rate of taper is much faster than that used for patients treated chronically with benzodiazepines who are discontinuing their anxiolytic in order to determine if it is still needed for control of symptoms. In that case, the rate of decrease is 10-20% per week. Should the patient display... 

Anxiolytics. The use of anxiety-reducing medications has not been systematically assessed in the treatment of AN. Nevertheless, many clinicians anecdotally report that the use of short-acting benzodiazepine such as lorazepam (Ativan) prior to mealtime diminishes anticipatory anxiety and thereby facilitates refeeding. 

The synthesis of these compounds will be described in Section 3.1, Opioid analgesics. Besides opioids, benzodiazepines (diazepam, lorazepam, and midazolam), which have anxiolytic, sedative, and anticonvulsant effects, that cause amnesia and muscle relaxation, are frequently used to relieve patients anxiety during anesthesia. 

Lorazepam (Ativan, Others) [C-IV] [Anxiolytic, Sedative/ Hypnotic/Benzodiazepine] Uses Anxiety preprocedure sedation control Szs Action Benzodiazepine Dose Adults. Preprocedure sedation 2.0-4.0 mg... 

The speciflc clinical use of the numerous available benzodiazepines depends on their individual pharmacokinetic and pharmacodynamic properties. Drugs with a high affinity for the GABAa receptor (alprazolam, clonazepam, lorazepam) have high anxiolytic efficacy drugs with a short duration of action (temazepam) are used as hypnotics to minimise daytime sedative effects. Diazepam has a long half-life and duration of action and may be favoured for long-term use or when there is a history of withdrawal problems oxazepam has a slow onset of action and may be less susceptible to abuse. 

Benzodiazepines are highly effective anxiolytics and sedatives. They also have muscle relaxant, amnestic, and anticonvulsant properties. Benzodiazepines effectively treat both acute and chronic generalized anxiety and panic disorder. The high-potency benzodiazepines alprazolam and clonazepam have received more attention as antipanic agents, but double-blind studies also have confirmed the efficacy of diazepam and lorazepam in the treatment of panic disorder. Although only a few benzodiazepines are specifically approved by the... 

Nevertheless, the GABAergic properties of benzodiazepines remain their most important clinical application. Over the past 30 years, the most widely used benzodiazepine drug has been diazepam (1.6). It is an anxiolytic, sedative, and muscle relaxant the anxious, depressed person becomes more outgoing and relaxed. There have been many diazepam analogs. Oxazepam (4.177) and lorazepam (4.178) have similar effects. Temazepam (4.179), flunitrazepam (4.180), and flurazepam (4.181) are useful sedative-hypnotics. Clonazepam (4.182) is a clinically useful anticonvulsant. Brotizolam (4.183), a novel benzodiazepine analog, seems to be an effective sedative-hypnotic. Midazolam (4.184) is an imidazolo-benzodiazepine that is water soluble and thus easily injectable. It is a hypnotic sedative with marked amnestic (i.e., memory loss) properties and is used in dentistry, endoscopic procedures, and induction to anesthetics in the elderly and in... 

A BZD s pharmacokinetics may play a role in the occurrence, in part accounting for the increase in its incidence after the advent of short-acting BZD anxiolytics and hypnotics (e.g., lorazepam, alprazolam, and triazolam). 

Other than slow taper, no consistently effective treatment to alleviate withdrawal symptoms has been reported. Although several compounds have been studied (e.g., b-blockers, clonidine, carbamazepine, abercamil, ondansetron), results have been contradictory ( 250). Carbamazepine, however, may be useful in seizure-prone patients (251). Valproate (VPA) has also been reported to benefit patients undergoing BZD discontinuation after long-term dependence ( 252), which may be related to VPA s potential anxiolytic properties, its ability to alleviate withdrawal phenomena, or both. The azaspirone anxiolytic buspirone has been reported ineffective in suppressing withdrawal symptoms, particularly in long-term BZD users (253, 254). Hydroxyzine has also been found beneficial in treating patients for lorazepam withdrawal (255). 

Diazepam, lorazepam, and midazolam are used for preanesthetic medication and as adjuvants during surgical procedures performed under local anesthesia. As a result of their sedative, anxiolytic, and amnestic properties, and their ability to control acute agitation, these compounds are considered to be the drugs of choice for premedication. (The basic pharmacology of benzodiazepines is discussed in Chapter 22.) Diazepam and lorazepam are not water-soluble, and their intravenous use necessitates nonaqueous vehicles, which cause pain and local irritation. Midazolam is water-soluble and is the benzodiazepine of choice for parenteral administration. It is important that the drug becomes lipid-soluble at physiologic pH and can readily cross the blood-brain barrier to produce its central effects. 

A simple and efficient procedure for the direct oxidation of C-3 of l,4-benzodiazepin-2-ones, applicable to the preparation of the anxiolytic agents oxazepam and lorazepam, has been developed that represents an improvement over the well-established Polonovsky rearrangement of the N-4 oxide <20060PD1192>. Iodine in AcOH at 65 °C catalyzed acetoxylation in a reaction that involved iodination at C-3 followed by a rapid nucleophilic displacement by KOAc. The liberated HI was recycled to iodine by inclusion of a stoichiometric oxidant, with K2S2O8 being the optimal compromise of cost, availability, and efficiency. 

OFFICIAL NAMES Minor tranquilizers (sedative-hyp-notics/anxiolytics)/Benzodiazepines Alprazolam (Xanax) chlordiazepoxide (Librium, Novopoxide) clonazepam (Klonopin) clorazepate (Azene, Tranxene) diazepam (Valium) estazolam (ProSom) flunitrazepam (Rohypnol/illegal in the United States) flurazepam (Dalmane) halazepam (Paxipam) lorazepam (Ativan) midazolam (Versed) oxazepam (Serax) prazepam (Centrax) quazepam (Doral) temazepam (Restoril) triazolam (Halcion)... 

Most of the minor tranquilizers in the BZD exhibit similar clinical effects they differ primarily in their duration of action and in the dosage required to achieve the same effect. The BZDs are classified as short- (triazolam [Halcion]), intermediate- (alprazolam [Xanax] and lorazepam [Ativan]), and long-acting (chlordiazepoxide [Librium] and diazepam [Valium]). Of the various BZDs available in the United States in 2002, those primarily prescribed as anxiolytics and hypnotics include the intermediate- and long-acting variety. 

As well as compounds specifically indicated for the short-term treatment of insomnia, some benzodiazepines used primarily as anxiolytics have found extensive usage as symptomatic remedies for insomnia in anxious individuals. Examples include oxazepam, lorazepam, and diazepam. Patterns of use vary from country to country and at different times. 

Corned answer = B. The anxiolytic properties of benzodiazepines, such as lorazepam, make them the drugs of choice in treating the anxiety and agitation of cocaine withdrawal. Lorazepam also has hypnotic properties. Phenobaibital has hypnotic properties but if s anxiolytic properties are inferior to those of the benzodiazepines. Cocaine itself could countered the agitation of withdrawal but its use would not be proper therapy. Hydroxyzine, an antihistaminic, is effective as an hypnotic and is sometimes used to deal with anxiety especially if emesis is a problem. Fluoxetine is an antidepressant with no immediate effects on anxiety. 

Benzodiazepines The antiemetic potency of lorazepam and alprazolam (see p. 89) is low. Their beneficial effects may be due to their sedative, anxiolytic and amnesic properties. These same properties make benzodiazepines useful in treating anticipatory vomiting. 

Diazepam produces less sedation in cigarette smokers, and higher (not lower, as stated in SEDA-20) doses may be required for the same sedative or anxiolytic effect. Owing in part to its continued widespread use, several unusual adverse effects of diazepam continue to be reported. These include cases of urinary retention and compartment syndrome, which are not explicable by its pharmacology. On the other hand, accumulation of diazepam and attendant complications of obtundation and respiratory depression may be understood in terms of its long half-life, particularly in elderly people and medically ill patients. Caution about the intravenous use of diazepam comes from a study that showed cardiac dysrhythmias (mainly ventricular extra beats) in a quarter of oral surgery patients midazolam and lorazepam were much safer (1). 

Lorazepam is a benzodiazepine with CNS, depressant, anxiolytic, and sedative properties, used as a hypnotic, sedative, and anxiolytic drug. 

Suriclone, a cyclopyrrolone analogue of zopiclone, has similar pharmacology to the benzodiazepines, binding close to the same site of the GABA receptor-chloride channel complex. It is effective as an anxiolytic and has the notable advantages of minimal sedation and cognitive toxicity, and milder withdrawal effects than those of diazepam or lorazepam (1). Its withdrawal from further development is a mystery. 

OPIOIDS ANXIOLYTICS AND HYPNOTICS 1. t sedation with BZDs 2. Respiratoiy depressant effect of morphine antagonized by lorazepam 1. Additive effect both drugs are sedatives 2. Uncertain 1. Closely monitor vital signs during co-administration 2. Although this effect may be considered to be beneficial, risk of additive effects should be borne in mind if the combination of an opioid and BZDs is used for sedation for painful procedures... 

PROTEASE INHIBITORS ANXIOLYTICS AND HYPNOTICS - BZDs, BUSPIRONE t adverse effects, e.g. prolonged sedation Inhibition of CYP3A4-mediated metabolism of BZDs and buspirone Watch closely for t sedation i dose of sedative as necessaiy. Some recommend considering substituting long-acting for shorter-acting BZDs with less active metabolites (e.g. lorazepam for diazepam)... 

Lorazepam / Ativan / Wyeth-Ayerst/ anxiolytic, sedation... 

---