Anxiolytics clonazepam

Anxiolytics clonazepam, diazepam, temazepam, triazolam, alprazolam, midazolam, buspirone Anticonvulsants ethosuximide, carbamazepine Calcium channel blockers diltiazem, felodipine, nifedipine, verapamil... 

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. 

Because OCD is considered one of the anxiety disorders according to DSM-IV [American Psychiatric Association 1994] [but not according to ICD-10 [World Health Organization 1992]], it is not surprising that anxiolytics have been suggested for its treatment. Thus, alprazolam and clonazepam have been reported as efficient in several uncontrolled studies and case series [Hewlett et al. 1990 Tollefson 1985]. 

More recently, Hewlett et al. [1992a] reported in a small [N = 28], double-blind, randomized, multiple crossover study that clonazepam was as effective as CMl and superior to diphenhydramine [a control drug]. However, more studies with large samples of patients with OCD are needed in order to draw substantial conclusions on this topic. Furthermore, because OCD is a chronic disorder, the use of anxiolytics for long periods raises questions of dependency brought about by benzodiazepine use. 

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... 

It is 1,5 benzodiazepine with a chemical structure slightly different from that of diazepam and clonazepam. This change in structure results in less sedative and psychomotor retardation. Though introduced as an anxiolytic it has been found to be useful in treatment of patients with refractory epilepsy. 

Insomnia is a common comorbid condition with depression, and frequently is made worse by antidepressants, particularly the SSRIs. When insomnia persists despite adequate evaluation and attempts to reduce it by other approaches, it is often necessary to use a concomitant sedative-hypnotic, especially a short-acting nonbenzodiazepine with rapid onset such as zaleplon or zolpidem. At times a benzodiazepine sedative hypnotic such as triazolam or temazepam may be necessary. If anxiety persists during the day and cannot be otherwise managed, it may be necessary to add an anxiolytic benzodiazepine such as alprazolam or clonazepam. Use of sedative-hypnotics and anxiolytics should be short-term whenever possible. 

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)... 

Side effects. Because clobazam has been widely used as an anxiolytic, its side effects are well known and essentially similar to those of the other benzodiazepines. Thus sedation, dizziness, ataxia, blurred vision and diplopia are the most commonly reported in epileptic patients. One of the most problematic features of clobazam is its tendency to produce tolerance, an effect which may occur more frequently with clobazam than with the other widely used benzodiazepine, clonazepam. It has been estimated that at least 50% of patients develop tolerance. Tolerance to the sedative effects of the drug develop more rapidly than those to the antiepileptic effect. Clobazam should be considered as adjunctive therapy whenever treatment with a single first-line drug has proven to be ineffective. 

CARBAMAZEPINE ANXIOLYTICS AND HYPNOTICS-BZDs-clonazepam L carbamazepine levels Induction of metabolism Watch for poor response to carbamazepine... 

If clonazepam can be considered a long-acting alprazolam-like anxiolytic , then alprazolam XR can be considered an even longer-acting clonazepam-like anxiolytic with the potential of improved tolerability features in terms of less euphoria, abuse, dependence, and withdrawal problems, but this has not been proven... 

The best-known and most-used anxiolytics are the benzodiazepines, of which those in use include alprazolam, bromazepam, chlordiazepoxide, clobazam, clonazepam, diazepam, flunitrazepam, halazepam, loprazolam, lorazepam, medazepam, midazolam, oxazepam, quazepam, temazepam and triazolam. The benzodiazepines work by acting as benzodiazepine binding-SITE AGONISTS at a site of the GABA receptors. 

Although the BZs show a robust anxiolytic effect, many of the clinical trials were conducted before the currently used divisions between specific anxiety disorders became available (4). As a result, knowledge of their efficacy in discrete anxiety disorders is incomplete. In clinical practice (48) BZs are widely used for GAD and as prophylactics in situational anxiety, with diazepam (l)historically being the most popular choice. Others in common use are chlordiazepoxide (2), clorazepate (3), lorazepam (4), alprazolam (5), oxazepam (6), bromazepam (7), and clonazepam (8) Response rates are high and the onset of therapeutic effect is immediate. This is an important contrast to the MAOIs, TCAs, and SSRIs, where an anxiolytic effect is not seen for several weeks. Although not specifically approved for this disorder. BZs are also effective in social phobia, with clonazepam (49) showing a superior response rate to that of alprazolam (50). Alprazolam and clonazepam are the only BZs approved for the treatment of panic disor-... 

Cl Anticonvulsant drugs Hypnotic or anxiolytic drugs Muscle-relaxant drugs Clonazepam, phenobarbital Clonazepam, diazepam, lorazepam Diazepam... 

When compared with four marketed anxiolytics in monkeys, (92) was approximately tenfold less potent (higher ED5o) than lorazepam, alprazolam, clonazepam, and equipotent with diazepam (Table 4.9). However, (92) was superior to these reference anxiolytics, when comparing the effective anxiolytic dose (ED50) with that which causes appreciable unwanted CNS effects i.e. therapeutic index. In addition to a generally wider separation between... 

Benzodiazepines. The benzodiazepines (BZs) are well established as anxiolytics, hypnotics, and muscle relaxants as represented bydiazepam,clonazepam,midazo-1am, and triazolam (Fig. 10.9). The BZ nucleus also occurs in natural products. Asperlicin is a... 

With an understanding of the mechanisms and metabolic reactions of these drugs, newer drug design concepts were applied in later synthetic phases. It is not surprising that compounds were developed in which certain pharmacologic properties became elevated or subdued (but never eliminated). Flurazepam (No. 7, Table 12-8), nitrazepam (No. 13), and triazolam (No. 22) became widely used as hypnotics clonazepam (No. 3) is used almost exclusively as an anticonvulsant, while diazepam (No. 6), clorazepate (No. 4), lorazepate (No. 19), prazepam (No. 16), and aprazolam (No. 19) are marketed primarily as anxiolytics. 

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