The association of buspirone and its metabolite 1-pyrimidinylpiperazine in the remission of comorbid anxiety with depressive features and alcohol dependency.

Recent literature has addressed a frequent comorbidity between alcoholism and anxiety/depression. These disorders have been interdigitated with the brain amines serotonin (5-HT) and norepinephrine. We investigated 51 dually diagnosed patients (generalized anxiety disorder with depressive features plus alcohol abuse/dependency) under a randomized, double-blind, placebo-controlled trial employing the 5-HT1A compound buspirone. Buspirone was superior to placebo as an anxiolytic. It was well tolerated and reduced the number of days patients desired alcohol. At the final study dose, the buspirone metabolite 1-pyrimidinylpiperazine (1-PP) was significantly related to improvement in anxiety, global depressive symptoms, and number of days not using alcohol. Analysis using the Hamilton Rating Scale for Depression and its retardation cluster revealed significant improvement secondary to anxiolysis. Thus, buspirone (especially via its 1-PP metabolite) may be an effective treatment strategy in the anxious or mixed anxious-depressive patient with comorbid alcoholism when other conventional anxiolytics may be contraindicated.

The relationship of serum anticholinergic activity to mental status performance in an elderly nursing home population.

Adverse drug reactions among elderly patients pose a significant clinical problem. The authors used a serum radioreceptor assay [RRA] to quantify drug-induced muscarinic blockade in 34 randomly selected nursing home residents. A random intervention group and the nonintervention control subjects were then retested 4 weeks later. The reduction of serum antimuscarinic activity (as determined by RRA) did relate to changes on several measures of cognitive function. A calculated "antimuscarinic index" lost significance with the RRA following intervention and may have overestimated the impact of a dosage reduction.

Buspirone: effects on prolactin and growth hormone as a function of drug level in generalized anxiety.

Certain evidence suggests that buspirone, a novel nonbenzodiazepine anxiolytic, may be a 5-HT1A serotonergic agonist and may antagonize postsynaptic dopaminergic receptors. The latter property raises questions regarding a dyskinesia- or extrapyramidal symptom-inducing potential. We monitored serum prolactin and growth hormone in 10 subjects with generalized anxiety disorder and 10 matched controls before and after 4 weeks of pharmacotherapy. A drug effect upon serotonin-modulated prolactin release or on the tubero-infundibular dopamine axis (prolactin; growth hormone) was negligible at clinically effective dosages of buspirone. Concomitant buspirone levels also failed to demonstrate any significant relationships.