Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0012833 (dizziness)
 9,689 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Buspirone (Buspar) is a azaspirodecanedione anxiolytic agent. Its mechanism of action is extremely complex, but current investigations indicate that its main neuropharmacologic effects are mediated by the 5-HT1A receptors. Other neuroreceptor systems could be involved, as buspirone displays some affinity for DA2 autoreceptors and 5-HT2 receptors. It has been proposed that inhibition of synthesis and release of serotonin result through the combined interactions of neuroreceptors and secondary messenger systems. This action leads to inhibition of the firing rate of 5-HT-containing neurons in the dorsal raphe. From this novel profile, that differs from that of the benzodiazepines, buspirone lacks anticonvulsant and muscle-relaxant properties, and causes only minimal sedation. The drug is rapidly absorbed after oral administration, with a mean bioavailability of 3.9%. After a single oral dose, the mean elimination half-life is 2.1 hours. Buspirone is mainly bound to albumin and alpha 1-acid glycoprotein. It is metabolized to an active metabolite 1-(2-pyrimidinyl) piperazine (1-PP). The mean elimination half-life of 1-PP is 6.1 hours. Buspirone is indicated in the treatment of generalized anxiety disorders. Its efficacy is comparable to the benzodiazepines. Its use in depression and panic disorders requires further investigation. When combined with alcohol or given alone, psychomotor impairment was not detected. Abuse, dependence, and withdrawal symptoms have not been reported. The frequency of adverse effects is low, and the most common effects are headaches, dizziness, nervousness, and lightheadness. Buspirone should be added to drug formularies and could represent a significant addition in psychopharmacology.
 ...
PMID:Buspirone: an update on a unique anxiolytic agent. 304 84

The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, dosage, administration, and availability of buspirone hydrochloride, a novel nonbenzodiazepine anxiolytic, are reviewed. Buspirone hydrochloride is an azaspirodecanedione anxiolytic. The exact mechanism of its anxiolytic action is unknown. It does not appear to influence the benzodiazepine-gamma-aminobutyric acid-chloride ionophore complex as the benzodiazepines do. It antagonizes striatal-dopamine autoreceptors, and it may act as a midbrain modulator exerting selective anxiolytic activity. Buspirone is rapidly absorbed after oral administration. Administration with food appears to slow the rate of drug absorption and increase the amount of unchanged drug reaching the systemic circulation. Buspirone's elimination half-life is 2.5-3 hours. It is extensively metabolized, with less than 1% of an administered dose excreted as unchanged drug. The contribution of its metabolites to its anxiolytic effects is unknown. Buspirone has been shown to be as effective as diazepam and clorazepate and more effective than placebo in the treatment of generalized anxiety. Buspirone lacks the sedative, muscle relaxant, and anticonvulsive effects of the benzodiazepines. Its adverse effects are minimal, with dizziness, nervousness, and headaches as the most common side effects. Buspirone does not impair driving skills, interact with alcohol or concomitant medications, or produce physiologic dependence. It appears to have little potential for abuse. The average daily adult dose is 15-20 mg. Buspirone hydrochloride is an effective drug in the treatment of generalized anxiety disorder that is comparable with the conventional benzodiazepine anxiolytics.
 ...
PMID:Buspirone, a novel nonbenzodiazepine anxiolytic. 615 Jul 81