Buspar
Buy BusparBuspar Information
Generic Name: Buspirone HCl
Buspar (Buspirone) is used for the treatment of nervousness and anxiety. Optimum results are usually seen after three to four weeks of treatment.
Indications:
Buspar (Buspirone HCl) is indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.
The efficacy of Buspar (buspirone HCl) has been demonstrated in controlled clinical trials of outpatients whose diagnosis roughly corresponds to Generalized Anxiety Disorder (GAD). Many of the patients enrolled in these studies also had coexisting depressive symptoms and buspirone HCl relieved anxiety in the presence of these coexisting depressive symptoms. The patients evaluated in these studies had experienced symptoms for periods of 1 month to over 1 year prior to the study, with an average symptom duration of 6 months. Generalized Anxiety Disorder (300.02) is described in the American Psychiatric Association's Diagnostic and Statistical Manual, III1 as follows:
Generalized, persistent anxiety (of at least one month continual duration), manifested by symptoms from three of the four following categories:
- Motor tension: Shakiness, jitteriness, jumpiness, trembling, tension, muscle aches, fatigability, inability to relax, eyelid twitch, furrowed brow, strained face, fidgeting, restlessness, easy startle.
- Autonomic hyperactivity: Sweating, heart pounding or racing, cold, clammy hands, dry mouth, dizziness, lightheadedness, paresthesias (tingling in hands or feet), upset stomach, hot or cold spells, frequent urination, diarrhea, discomfort in the pit of the stomach, lump in the throat, flushing, pallor, high resting pulse and respiration rate.
- Apprehensive expectation: Anxiety, worry, fear, rumination, and anticipation of misfortune to self or others.
- Vigilance and scanning: Hyperattentiveness resulting in distractibility, difficulty in concentrating, insomnia, feeling "on edge", irritability, impatience.
The above symptoms would not be due to another mental disorder, such as a depressive disorder or schizophrenia. However, mild depressive symptoms are common in GAD.
The effectiveness of Buspar (buspirone HCl) in long-term use, that is, for more than 3 to 4 weeks, has not been demonstrated in controlled trials. There is no body of evidence available that systematically addresses the appropriate duration of treatment for GAD. However, in a study of long-term use, 264 patients were treated with buspirone HCl for 1 year without ill effect. Therefore, the physician who elects to use Buspar (buspirone HCl) for extended periods should periodically reassess the usefulness of the drug for the individual patient.
Buspar Ingredients and Composition
How Does Buspar Work?
The mechanism of action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models.
Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.
How To Take Buspar and Buspar Dosage and Administration
The recommended initial Buspar dose is 15 mg daily (5 mg 3 times a day). To achieve an optimal therapeutic response, at intervals of 2 to 3 days the dosage may be increased 5 mg per day, as needed. The maximum daily Buspar dosage should not exceed 60 mg per day. In clinical trials allowing dose titration, divided doses of 20 to 30 mg per day were commonly employed.
If you suspect a Buspar Overdose
Signs and Symptoms: In clinical pharmacology trials, Buspar doses as high as 375 mg/day were administered to healthy male volunteers. As this dose was approached, the following symptoms were observed: nausea, vomiting, dizziness, drowsiness, miosis, and gastric distress. No deaths have been reported in humans either with deliberate or accidental overdosage of buspirone HCl. Toxicology studies of buspirone yielded the following LD50 values: mice, 655 mg/kg; rats, 196 mg/kg; dogs, 586 mg/kg; and monkeys, 356 mg/kg. These dosages are 160 to 550 times the recommended human daily dose.
Recommended Buspar Overdose Treatment: General symptomatic and supportive measures should be used along with immediate gastric lavage. Respiration, pulse, and blood pressure should be monitored as in all cases of drug overdosage. No specific antidote is known to buspirone, and dialyzability of buspirone has not been determined.
Buspar Side Effects
Buspar Precautions and Contraindications
General
Interference with cognitive and motor performance: Studies indicate that Buspar (buspirone HCl) is less sedating than other anxiolytics and that it does not produce significant functional impairment. However, its CNS effects in any individual patient may not be predictable. Therefore, patients should be cautioned about operating an automobile or using complex machinery until they are reasonably certain that buspirone treatment does not affect them adversely.
While formal studies of the interaction of Buspar (buspirone HCl) with alcohol indicate that buspirone does not increase alcohol-induced impairment in motor and mental performance, it is prudent to avoid concomitant use of alcohol and buspirone.
Potential for withdrawal reactions in sedative/hypnotic/anxiolytic drug-dependent patients: Because Buspar (buspirone HCl) does not exhibit cross-tolerance with benzodiazepines and other common sedative/hypnotic drugs, it will not block the withdrawal syndrome often seen with cessation of therapy with these drugs. Therefore, before starting therapy with buspirone HCl, it is advisable to withdraw patients gradually, especially patients who have been using a CNS-depressant drug chronically, from their prior treatment. Rebound or withdrawal symptoms may occur over varying time periods, depending in party on the type of drug, and its effective half-life of elimination.
The syndrome of withdrawal from sedative/hypnotic/anxiolytic drugs can appear as any combination of irritability, anxiety, agitation, insomnia, tremor, abdominal cramps, muscle cramps, vomiting, sweating, flu-like symptoms without fever, and occasionally, even as seizures.
Possible concerns related to Buspar (buspirone's) binding to dopamine receptors: Because buspirone can bind to central dopamine receptors, a question has been raised about its potential to cause acute and chronic changes in dopamine-mediated neurological function (e.g., dystonia, pseudo-parkinsonism, akathisia, and tardive dyskinesia). Clinical experience in controlled trials has failed to identify any significant neuroleptic-like activity; however, a syndrome of restlessness, appearing shortly after initiation of treatment, has been reported in some small fraction of buspirone-treated patients. The syndrome may be explained in several ways. For example, Buspar (buspirone) may increase central noradrenergic activity; alternatively, the effect may be attributable to dopaminergic effects (i.e., represent akathisia). Obviously, the question cannot be totally resolved at this point in time. Generally, long-term sequelae of any drug's use can be identified only after several years of marketing.
Contraindications to Buspar
Buspar (Buspirone HCl) is contraindicated in patients hypersensitive to buspirone hydrochloride.
Buspar Drug Interactions
It is recommended that Buspar (buspirone hydrochloride) not be used concomitantly with MAO inhibitors. Because the effects of concomitant administration of buspirone HCl with most other psychotropic drugs have not been studied, the concomitant use of buspirone HCl with other CNS-active drugs should be approached with caution.
There is one report suggesting that the concomitant use of trazodone hydrochloride (Desyrel) and Buspar (buspirone HCl) may have caused 3- to 6-fold elevations on SGPT (ALT) in a few patients. In a similar study, attempting to replicate this finding, no interactive effect on hepatic transaminases was identified.
In a study in normal volunteers, concomitant administration of Buspar (buspirone HCl) and haloperidol resulted in increased serum haloperidol concentrations. The clinical significance of this finding is not clear.
Buspar and Alcohol Interaction
Do not take any other sedating drugs or drink alcohol while taking Buspar.
Storing Buspar
Store at Room Temperature. Protect from temperatures greater than 86°F (30°C).
