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'''Buspirone''' (brand-names '''Ansial'''®, '''Ansiced'''®, '''Anxiron'''®, '''Axoren'''®, '''Bespar'''®, '''BuSpar'''®, '''Buspimen'''®, '''Buspinol'''®, '''Buspisal'''®, '''Narol'''®) is an [[anxiolytic]] agent and a [[serotonin]] [[receptor]] [[agonist]] belonging to the [[azaspirodecanedione]] class of compounds. Its structure is unrelated to those of the [[benzodiazepines]], but it has an efficacy comparable to [[diazepam]]{{fact}}.
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'''Buspirone''' (brand-names '''Ansial''', '''Ansiced''', '''Anxiron''', '''Axoren''', '''Bespar''', '''BuSpar''', '''Buspimen''', '''Buspinol''', '''Buspisal''', '''Narol''', '''Spitomin''', '''Sorbon''') is an [[anxiolytic]] agent and a [[serotonin receptor agonist]] belonging to the [[azaspirodecanedione]] class of compounds. Its structure is unrelated to those of the [[benzodiazepines]], but it has an efficacy comparable to [[diazepam]] in treating [[generalized anxiety disorder]].<ref>{{cite journal |last=Cohn |first=JB |coauthors=Rickels K |year=1989 |title=A pooled, double-blind comparison of the effects of buspirone, diazepam and placebo in women with chronic anxiety |journal=Curr Med Res Opin. |volume=11 |issue=5 |pages=304-320 }}</ref><ref>{{cite journal |last=Goldberg |first=HL |coauthors=Finnerty RJ |year=1979 |month=September |title=The comparative efficacy of buspirone and diazepam in the treatment of anxiety |journal=Am J Psychiatry |volume=136 |issue=9 |pages=1184-1187 }}</ref>
   
It shows no potential for [[addiction]] compared to other drugs commonly prescribed for [[anxiety]], especially [[benzodiazepine]] medications. The development of tolerance has not been noticed. Cross-tolerance to benzodiazepines, [[barbiturate]]s and [[ethanol|alcohol]] does not exist. Furthermore, it is non-sedating.
+
It shows no potential for [[addiction]] compared to other drugs commonly prescribed for [[anxiety]], especially [[benzodiazepine]] medications {{Fact|date=January 2008}}. The development of tolerance has not been noticed. Cross-tolerance to benzodiazepines, [[barbiturate]]s and [[ethanol|alcohol]] does not exist. Furthermore, it is non-sedating.
   
It is thought to act by interfering with the function of the neurotransmitter [[serotonin]] in the brain, particularly by serving as a [[5-HT receptor|5-HT1A receptor]] partial [[agonist]]. Additionally, it acts as a mixed agonist/antagonist on postsynaptic [[dopamine]] receptors. [[GABA]]-mediated effects are lacking. Buspirone may also have indirect effects on other neurotransmitters in the brain.
+
It is thought to act by interfering with the function of the neurotransmitter [[serotonin]] in the brain, particularly by serving as a [[5-HT receptor|5-HT1A presynaptic receptor]] partial [[agonist]]. Additionally, it acts as a mixed agonist/antagonist on postsynaptic [[dopamine]] receptors. [[GABA]]-mediated effects are lacking. Buspirone may also have indirect effects on other neurotransmitters in the brain.
   
The action of a single dose is much longer than the short halflife of 2-3 hours indicates.
+
The action of a single dose is much longer than the short halflife of 2-3 hours indicates. The bioavailability of buspirone is very low and variable due to extensive first pass metabolism. The drug is quickly resorbed. Taking the drug together with food may increase the bioavailability. The drug is highly (95%) plasma-bound. The active metabolite 1-PP is also a 5-HT1A partial agonist with anxiolytic properties, but weaker so than the mother-drug.
The bioavailability of Buspirone is very low and variable due to extensive first pass metabolism. The drug is quickly resorbed. Taking the drug together with food may increase the bioavailabilty. The drug is highly (95%) plasma-bound. The active metabolite 1-PP is also a 5-HT1A partial agonist with anxiolytic properties, but weaker so than the mother-drug.
 
   
It is also useful as an augmenting agent, for the treatment of depression, when added to [[selective serotonin reuptake inhibitor|SSRI]]s (selective serotonin reuptake inhibitors).
+
It is also useful as an augmenting agent, for the treatment of depression, when added to [[selective serotonin reuptake inhibitor|SSRI]]s.
   
The main disadvantage is that 1 to 3 weeks elapse before the anxiolytic activity becomes evident. Often patients have to be initially cotreated with a benzodiazepine for immediate anxiolysis. Generally, Buspirone works less well than benzodiazepines. It is particularly difficult to treat patients pretreated with benzodiazepines knowing the immediate effects of these tranquilizers.
+
The main disadvantage is that 1 to 3 weeks elapse before the anxiolytic activity becomes evident. Often patients have to be initially cotreated with a benzodiazepine for immediate anxiolysis. Generally, buspirone works less well than benzodiazepines. Therefore, benzodiazepines are often the first approach in immediately treating panic attacks and social phobias. It is also particularly difficult to treat patients pretreated with benzodiazepines knowing the immediate effects of these tranquilizers.
   
 
[[Bristol-Myers Squibb]] gained FDA approval for Buspirone in 1986. The drug went generic in 2001.
 
[[Bristol-Myers Squibb]] gained FDA approval for Buspirone in 1986. The drug went generic in 2001.
 
 
== Indications ==
 
== Indications ==
* [[Generalized anxiety disorder]] of mild to moderate intensity (N.B. Buspirone is not considered effective against other types of anxiety disorders with or without agoraphobia and social phobia.)
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<!-- Deleted image removed: [[Image:BusparAd.png|thumb|300px|left|Buspar advertisement to medical professionals.]] -->
* Augmention of [[SSRI]]-Treatment against [[clinical depression|Depression]]
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* [[Generalized anxiety disorder]] of mild to moderate intensity (it is not considered effective against other types of anxiety disorders such as [[obsessive-compulsive disorder]], with or without agoraphobia and social phobia)
  +
* Augmention of [[SSRI]]-treatment against [[clinical depression|depression]]
   
 
== Contraindications ==
 
== Contraindications ==
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* Acute closed angle [[glaucoma]]
 
* Acute closed angle [[glaucoma]]
 
* Severely compromised [[liver]]- and [[renal]]-function
 
* Severely compromised [[liver]]- and [[renal]]-function
* Concomittant treatment with a [[MAOI|MAO-Inhibitor]] (severe [[hypertensive]] crises have been seen)
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* Concomitant treatment with a [[MAOI|MAO-Inhibitor]] (severe [[hypertensive]] crises have been seen)
* Caution : Preexisting heart conditions (e.g. [[myocardial infarction]])
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* Preexisting heart conditions (e.g. [[myocardial infarction]])
   
 
== Side-effects ==
 
== Side-effects ==
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* Most frequent: [[Vertigo (medical)|vertigo]], headaches, nervousness, agitation, light-headedness, [[nausea]];
 
* Most frequent: [[Vertigo (medical)|vertigo]], headaches, nervousness, agitation, light-headedness, [[nausea]];
 
* Often (>1%) : drowsiness, [[insomnia]], concentration disorders, [[confusion]], [[Clinical depression|depression]], agitation, intestinal disorders, [[paresthesia]], coordination disorders, [[tremor]]s, disturbed vision, [[tinnitus]], [[fatigue (physical)|fatigue]], weakness, [[Angina pectoris]], sore throat, [[tachycardia]]s, [[palpitation]]s, dry mouth, pain in muscles and joints;
 
* Often (>1%) : drowsiness, [[insomnia]], concentration disorders, [[confusion]], [[Clinical depression|depression]], agitation, intestinal disorders, [[paresthesia]], coordination disorders, [[tremor]]s, disturbed vision, [[tinnitus]], [[fatigue (physical)|fatigue]], weakness, [[Angina pectoris]], sore throat, [[tachycardia]]s, [[palpitation]]s, dry mouth, pain in muscles and joints;
* Seldomly: [[allergic reactions]], subdermal bleeding, [[extrapyramidal]] symptoms, [[hallucinations]], [[psychosis]], [[ataxia]], [[epileptic seizures]], [[syncope]], tunnel vision, urine retention, [[alopecia]], [[pruritus]].
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* Seldom: [[allergic reactions]], subdermal bleeding, [[extrapyramidal]] symptoms, [[hallucinations]], [[psychosis]], [[ataxia]], [[epileptic seizures]], [[syncope]], tunnel vision, urine retention, [[hyperosmia]], [[alopecia]], [[pruritus]], hot flashes.
   
The [[dyscognitive]] [[Adverse drug reaction|side-effects]] of [[benzodiazepines]] are lacking completely.
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There are no [[dyscognitive]] [[Adverse drug reaction|side-effects]] like those seen in [[benzodiazepines]].
   
 
Other side-effects have been seen, but are not more frequent than those encountered with [[placebo]]. An unusual side effect reported by patients has been an enhanced sense of smell.
 
Other side-effects have been seen, but are not more frequent than those encountered with [[placebo]]. An unusual side effect reported by patients has been an enhanced sense of smell.
   
 
== Drug abuse and dependence==
 
== Drug abuse and dependence==
Buspirone has no known potential for abuse, psychological and physical dependence.
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Buspirone has no known potential for abuse, psychological and physical dependence{{Fact|date=January 2008}}
   
 
== Interactions ==
 
== Interactions ==
* [[Haloperidol]] : increased plasma-levels of Haloperidol
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* [[Haloperidol]] : increased plasma-levels of haloperidol
* [[Rifampizin]] : decreased plasma-levels of Buspirone
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* [[Rifampicin]] : decreased plasma-levels of buspirone
 
* [[MAOI|MAO-Inhibitors]] : severe hypertensive crises are possible.
 
* [[MAOI|MAO-Inhibitors]] : severe hypertensive crises are possible.
* [[Ethanol|Alcohol]] : The sedative properties of alcohol are not increased.
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* [[Ethanol|Alcohol]] : The sedative properties of alcohol are increased slightly.
* [[grapefruit|Grapefruit, Grapefruit juice, Grapefruit extract]] : '''drastically''' increased plasma-levels of Buspirone <sup>[http://www.biologicalunhappiness.com/BuspGrpf.htm][http://www.rxlist.com/rxboard/general.pl?noframes;read=1386][http://bipolar.about.com/od/medications/f/faq_grapefruitj.htm][http://www.inhousepharmacy.co.uk/anti-depressants/buspar-information.html][http://www.google.com/search?hl=en&q=buspar+grapefruit&btnG=Google+Search ...]</sup>
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* [[grapefruit|Grapefruit, Grapefruit juice, Grapefruit extract]] : '''drastically''' increased plasma-levels of Buspirone <ref>{{cite journal |last=Lilja |first=JJ |coauthors=Kivisto KT, Backman JT, Lamberg TS, Neuvonen PJ |year=1998 |month=December |title=Grapefruit juice substantially increases plasma concentrations of buspirone Do not mix the pills in grapefruit juice. Resulting so would be in euphoria
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|journal=Clin Pharmacol Ther |volume=64 |issue=6 |pages=655-660 }}</ref>
   
 
== Dosage ==
 
== Dosage ==
Initially, 10-15mg in 2-3 single doses per day. The dose may be increased to a maximum of 60mg daily (3 times 20mg, a single dose should not exceed 20mg).
+
Initially, 10-15mg in 2-3 single doses per day. The dose may be increased to a maximum of 60mg daily (3 times 20mg, a single dose should not exceed 20mg).
   
 
== Duration of treatment ==
 
== Duration of treatment ==
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== Other remarks ==
 
== Other remarks ==
Buspirone should not be used as a substitute for [[benzodiazepines]], [[barbiturates]] or [[Ethanol|alcohol]] before withdrawing these agents properly. No residual signs of withdrawal should exist when Buspirone is started. Buspirone is not able to alleviate any [[withdrawal]] symptoms caused by these drugs.
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Buspirone should not be used as a substitute for [[benzodiazepines]], [[barbiturates]] or [[Ethanol|alcohol]] before withdrawing these agents properly. No residual signs of withdrawal should exist when Buspirone is started. Buspirone is not able to alleviate any [[withdrawal]] symptoms caused by these drugs.{{Fact|date=December 2007}}
  +
  +
  +
==See also==
  +
*[[Minor tranquillizers]]
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*[[Serotonin agonists]]
   
  +
==References==
  +
<references />
   
   
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[[Category:Anxiolytics]]
 
[[Category:Anxiolytics]]
  +
[[Category:Minor tranquillizers]]
 
[[Category:Serotonin agonists]]
 
[[Category:Serotonin agonists]]
   
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[[de:Buspiron]]
 
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[[es:Buspirona]]
 
[[zh:丁螺環酮]]
 
[[zh:丁螺環酮]]
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{{enWP|Buspirone}}
 
{{enWP|Buspirone}}

Latest revision as of 22:47, January 18, 2008

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Buspirone chemical structure
Buspirone

8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-
8-azaspiro[4.5]decane-7,9-dione
IUPAC name
CAS number
36505-84-7
ATC code

N05BE01

PubChem
2477
DrugBank
APRD00222
Chemical formula {{{chemical_formula}}}
Molecular weight 385.50314 g/mol
Bioavailability low and variable (approx. 5%), due to high first pass metabolism
Metabolism mainly hepatic, active metabolite 1-Pyrimidylpiperazin (1-PP)
Elimination half-life 2-3h
Excretion urine (29-63%) and feces (18-38%) in the form of metabolites
Pregnancy category B, only use when clearly needed
Legal status Rx-only, not a controlled substance
Routes of administration oral


Buspirone (brand-names Ansial, Ansiced, Anxiron, Axoren, Bespar, BuSpar, Buspimen, Buspinol, Buspisal, Narol, Spitomin, Sorbon) is an anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam in treating generalized anxiety disorder.[1][2]

It shows no potential for addiction compared to other drugs commonly prescribed for anxiety, especially benzodiazepine medications [How to reference and link to summary or text]. The development of tolerance has not been noticed. Cross-tolerance to benzodiazepines, barbiturates and alcohol does not exist. Furthermore, it is non-sedating.

It is thought to act by interfering with the function of the neurotransmitter serotonin in the brain, particularly by serving as a 5-HT1A presynaptic receptor partial agonist. Additionally, it acts as a mixed agonist/antagonist on postsynaptic dopamine receptors. GABA-mediated effects are lacking. Buspirone may also have indirect effects on other neurotransmitters in the brain.

The action of a single dose is much longer than the short halflife of 2-3 hours indicates. The bioavailability of buspirone is very low and variable due to extensive first pass metabolism. The drug is quickly resorbed. Taking the drug together with food may increase the bioavailability. The drug is highly (95%) plasma-bound. The active metabolite 1-PP is also a 5-HT1A partial agonist with anxiolytic properties, but weaker so than the mother-drug.

It is also useful as an augmenting agent, for the treatment of depression, when added to SSRIs.

The main disadvantage is that 1 to 3 weeks elapse before the anxiolytic activity becomes evident. Often patients have to be initially cotreated with a benzodiazepine for immediate anxiolysis. Generally, buspirone works less well than benzodiazepines. Therefore, benzodiazepines are often the first approach in immediately treating panic attacks and social phobias. It is also particularly difficult to treat patients pretreated with benzodiazepines knowing the immediate effects of these tranquilizers.

Bristol-Myers Squibb gained FDA approval for Buspirone in 1986. The drug went generic in 2001.

Indications Edit

Contraindications Edit

Side-effects Edit

Rarely, side-effects have a dangerous nature or intensity. Some tend to disappear with continued therapy, or are less frequent if the initial dose is low and increased gradually (vertigo, agitation, insomnia).

There are no dyscognitive side-effects like those seen in benzodiazepines.

Other side-effects have been seen, but are not more frequent than those encountered with placebo. An unusual side effect reported by patients has been an enhanced sense of smell.

Drug abuse and dependenceEdit

Buspirone has no known potential for abuse, psychological and physical dependence[How to reference and link to summary or text]

Interactions Edit

Dosage Edit

Initially, 10-15mg in 2-3 single doses per day. The dose may be increased to a maximum of 60mg daily (3 times 20mg, a single dose should not exceed 20mg).

Duration of treatment Edit

The duration of treatment is not limited, but the prescribing physician should reassess in regular intervals, if continued treatment is still necessary.

Other remarks Edit

Buspirone should not be used as a substitute for benzodiazepines, barbiturates or alcohol before withdrawing these agents properly. No residual signs of withdrawal should exist when Buspirone is started. Buspirone is not able to alleviate any withdrawal symptoms caused by these drugs.[How to reference and link to summary or text]


See alsoEdit

ReferencesEdit

  1. Cohn, JB, Rickels K (1989). A pooled, double-blind comparison of the effects of buspirone, diazepam and placebo in women with chronic anxiety. Curr Med Res Opin. 11 (5): 304-320.
  2. Goldberg, HL, Finnerty RJ (September 1979). The comparative efficacy of buspirone and diazepam in the treatment of anxiety. Am J Psychiatry 136 (9): 1184-1187.
  3. Lilja, JJ, Kivisto KT, Backman JT, Lamberg TS, Neuvonen PJ (December 1998). Grapefruit juice substantially increases plasma concentrations of buspirone Do not mix the pills in grapefruit juice. Resulting so would be in euphoria. Clin Pharmacol Ther 64 (6): 655-660.


External linksEdit

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