Alprazolam


The pharmacology of alprazolam a review

12.15.2018 by Brianna Marshman
Alprazolam

Alprazolam is the product of the incorporation of the triazolo ring into the benzodiazepine structure. More than 90% of alprazolam is absorbed after an oral dose;.

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Alprazolam is the product of the incorporation of the triazolo ring into the benzodiazepine structure. More than 90% of alprazolam is absorbed after an oral dose; the absorption rate is dose independent. After a single oral dose of 0.5 to 3 mg of alprazolam, peak plasma concentrations of 7 to 40 ng/ml are reached at 0.7 to 2.1 hours after administration. Factors such as liver and kidney disease, smoking, age, sex, and obesity have minimal effects on alprazolam pharmacokinetics. A review of alprazolam-drug interactions revealed few that were clinically significant, except that cimetidine and oral contraceptives reduce alprazolam clearance and increase its half-life. The mechanisms of action of alprazolam are reviewed. Its anxiolytic effect is similar to that of other benzodiazepines, but the basis of its other effects is less clear. Like other benzodiazepines, it has a good ratio of efficacy to side effects; its most common side effect, mild sedation, occurs early in treatment. The potential of dependence to and abuse of alprazolam and its toxicity are similar to that of other benzodiazepines. Finally, alprazolam's therapeutic role as an anxiolytic and anti-depressant and its use in the management of panic attacks, agoraphobia, schizophrenia, cancer, the premenstrual syndrome, and anxiety and as a cardioprotective agent are assessed.

Clinical pharmacology, clinical efficacy, and behavioral toxicity of

11.14.2018 by Matthew Allford
Alprazolam

CNS Drug Rev. 2004 Spring;10(1):45-76. Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature. Verster JC(1).

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Since alprazolam is widely used, many clinical studies investigated its cognitive and psychomotor effects. Alprazolam has a fast onset of symptom relief (within the first week); it is unlikely to produce dependency or abuse. Therefore, alprazolam is recommended as a second line treatment option, when SSRIs are not effective or well tolerated. No tolerance to its therapeutic effect has been reported. At discontinuation of alprazolam treatment, withdrawal and rebound symptoms are common. In addition to its therapeutic effects, alprazolam produces adverse effects, such as drowsiness and sedation. Alprazolam is a benzodiazepine derivative that is currently used in the treatment of generalized anxiety, panic attacks with or without agoraphobia, and depression. An exhaustive review of the literature showed that alprazolam is significantly superior to placebo, and is at least equally effective in the relief of symptoms as tricyclic antidepressants (TCAs), such as imipramine. It is evident from these studies that alprazolam may impair performance in a variety of skills in healthy volunteers as well as in patients. Since the majority of alprazolam users are outpatients, this behavioral impairment limits the safe use of alprazolam in patients routinely engaged in potentially dangerous daily activities, such as driving a car. However, although alprazolam and imipramine are significantly more effective than placebo in the treatment of panic attacks, Selective Serotonin Reuptake Inhibitors (SSRIs) appear to be superior to either of the two drugs. Hence, alprazolam discontinuation must be tapered.

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Alprazolam and exposure alone and combined in panic disorder

8.11.2018 by Alexis Johnson
Alprazolam

Br J Psychiatry. 1993 Jun;162:776-87. Alprazolam and exposure alone and combined in panic disorder with agoraphobia. A controlled study in London and.

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A cross-national randomised trial of alprazolam for chronic panic disorder with agoraphobia was run. Compared with previous trials it had three new features: an exposure therapy contrast group, a six-month treatment-free follow-up, and a low rate of early placebo drop-outs ('non-evaluables'). The dose of alprazolam was high (5 mg/day). The 154 patients had eight weeks of: alprazolam and exposure (combined treatment); or alprazolam and relaxation (a psychological placebo); or placebo and exposure; or placebo and relaxation (double placebo). Drug taper was from weeks 8 to 16. Follow-up was to week 43. Results were similar at both sites. Treatment integrity was good. All four treatment groups, including double placebo, improved well on panic throughout. On non-panic measures, by the end of treatment, both alprazolam and exposure were effective, but exposure had twice the effect size of alprazolam. During taper and follow-up, gains after alprazolam were lost, while gains after exposure were maintained. Combining alprazolam with exposure marginally enhanced gains during treatment, but impaired improvement thereafter. The new features put previous trails in a fresh light. By the end of treatment, though gains on alprazolam were largely as in previous studies, on phobias and disability they were half those with exposure. Relapse was usual after alprazolam was stopped, whereas gains persisted to six-month follow-up after exposure ceased. Panic improved as much with placebo as with alprazolam or exposure.

Alprazolam absorption kinetics affects abuse liability. - NCBI

7.10.2018 by Matthew Allford
Alprazolam
Alprazolam absorption kinetics affects abuse liability. - NCBI

Clin Pharmacol Ther. 1995 Mar;57(3):356-65. Alprazolam absorption kinetics affects abuse liability. Mumford GK(1), Evans SM, Fleishaker JC, Griffiths RR.

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To evaluate the behavioral, subjective, and reinforcing effects of immediate-release (IR) alprazolam and extended-release (XR) alprazolam to assess the effect of release rate on laboratory measures of abuse liability.

These data indicate that extended-release alprazolam has less potential for abuse than immediate-release alprazolam.

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Alprazolam - Drugs and Lactation Database (LactMed) - NCBI

6.9.2018 by Brianna Marshman
Alprazolam
Alprazolam - Drugs and Lactation Database (LactMed) - NCBI

Because of reports of effects in infants, including sedation, alprazolam is probably not the best benzodiazepine for repeated use during nursing.

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One mother who was taking sertraline 50 mg daily, zopiclone 2.5 mg about every 3 days as needed, and also took alprazolam 0.25 mg on 2 occasions, reported sedation in her breastfed infant.