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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C21H31N5O2
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RX_link
http://www.rxlist.com/cgi/generic/buspir.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
U.S. Pat. 3,717,634 (1973)
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Molecular Weight
385.503 g/mol
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Melting Point
201.5-202.5oC
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H2O Solubility
21.4 mg/L
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State
Solid
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LogP
1.238
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Dosage Forms
Tablet (5 mg, 10 mg)
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Indication
For the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.
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Pharmacology
Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. 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.
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Absorption
Rapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism.
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side effects and Toxicity
Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.
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Patient Information
Buspirone is used for the treatment of nervousness and anxiety. Optimum results are usually seen after three to
four weeks of treatment. This medication may be taken with or without food. Inform your physican if you are pregnant
or nursing. Buspirone may cause dizziness and drowsiness; use caution while driving or operating hazardous machinery.
Do not take any other sedating drugs or drink alcohol while taking this medication. Do not take this medication with
a monoamine oxidase inhibitor. Notify physician if you develop muscle spasms, uncontrolled twitching in the face and
body, or uncontrolled tongue movements.
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Organisms Affected
Humans and other mammals