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Buspirone (/ˈbjuːspᵻroʊn/ BEW-spi-rohn), trade name Buspar, is an anxiolytic psychotropic drug of the azapirone chemical class.^[3] It is primarily used to treat generalized anxiety disorder (GAD). Unlike most drugs predominantly used to treat anxiety, buspirone's pharmacology is not related to benzodiazepines or barbiturates, and so does not carry the risk of physical dependence and withdrawal symptoms for which those drug classes are known.

Buspirone was first identified by a team at Mead Johnson in 1972, but was not patented until 1975.^[4]^[5]

In 1986, Bristol-Myers Squibb gained Food and Drug Administration (FDA) approval for buspirone in the treatment of GAD. The patent placed on buspirone expired in 2001 and buspirone is now available as a generic drug.

Medical uses

Buspirone is approved in the United States by the FDA for the treatment of anxiety disorders and the short-term relief of the symptoms of anxiety.^[6] Likewise in Australia, buspirone is licensed for the treatment of anxiety disorders.^[7]^[8] In the United Kingdom, buspirone is indicated only for the short-term treatment of anxiety.^[9]^[10]

Although not approved for this indication, studies such as STAR*D have shown buspirone to be an effective augmentation agent alongside treatment with selective serotonin reuptake inhibitors (SSRIs) for clinical depression and is also used to counter the sexual side effects (anorgasmy and impotence) of the SSRI.^[11]^[12]^[13]^[14]

Several clinical trials, most randomised double-blind trials (and in one buspirone was used as an adjunct to atomoxetine) and one open-label, have been conducted to evaluate the utility of buspirone in the treatment of attention deficit hyperactivity disorder with mostly positive results.^[15]^[16]^[17]^[18]

Buspirone is also used in the treatment of mild to moderate cerebellar ataxia.^[19]

Dosage

For generalized anxiety disorder (GAD): 15–60 mg. Starting dose is 5 mg, 3 times daily, average dosage being 20–30 mg a day. If symptoms still persist after several weeks then the dose may be titrated up to 60 mg. Due to Buspar's short half-life and linear pharmacokinetics,^[20] dosage can be increased by 5 mg every two to three days.^[21]^[22]^[23]^[24]^[25]^[26]^[27]

Adverse effects

Buspar (buspirone) 10-mg tablets.

Adverse effects by incidence^[1]^[6]^[7]^[9] include:

Very common (>10% incidence)

Dizziness/light-headedness
Headache
Somnolence (sleepiness)
Premature ejaculation^{[not in citation given]}

Common (1-10% incidence)

Nervousness
Insomnia
Sleep disorder
Disturbance in attention
Depression
Confusional state
Anger
Tachycardia (fast heart rate)
Chest pain
Sinusitis (nasal congestion)
Pharyngolaryngeal pain
Paraesthesia (tingling skin)
Blurred vision
Abnormal coordination
Tremor
Cold sweat
Rash
Nausea
Abdominal pain
Dry mouth
Diarrhea
Constipation
Vomiting
Fatigue
Musculoskeletal pain

Uncommon (0.1-1%)

Syncope
Hypotension
Hypertension
Redness and itching of the eyes
Altered taste
Conjunctivitis
Flatulence
Anorexia
Increased appetite
Salivation
Rectal bleeding
Urinary frequency
Urinary hesitancy
Menstrual irregularity or spotting
Dysuria
Muscle cramps
Muscle spasms
Muscle rigidity/stiffness
Involuntary movements
Shortness of breath
Chest congestion
Changes in libido
Oedema
Pruritus
Flushing
Easy bruising
Dry skin
Facial oedema
Mild increases in hepatic aminotransferases (AST, ALT)
Weight gain
Fever
Roaring sensation in the head
Weight loss
Malaise
Depersonalisation
Noise intolerance
Euphoria
Akathisia
Fearfulness
Loss of interest
Dissociative reaction

Rare (<0.1% incidence)

Cerebrovascular accident (stroke)
Myocardial infarction (heart attack)
Cardiomyopathy
Congestive heart failure
Bradycardia
Dysphoria
Hallucinations
Feelings of claustrophobia
Cold intolerance
Stupor
Seizures
Slurred speech
Extrapyramidal symptoms including dyskinesias (acute & delayed)
Dystonic reactions
Cogwheel rigidity
Emotional lability
Psychosis
Suicidal ideation
Ataxias
Transient difficulty with recall
Serotonin syndrome
Parkinsonism
Restless leg syndrome
Restlessness
Eye pain
Altered sense of smell
Photophobia
Pressure on eyes
Inner ear abnormality
Tunnel vision
Galactorrhoea
Irritable colon
Burning of the tongue
Arthralgias
Amenorrhoea (cessation of menstrual cycles)
Enuresis
Nocturia
Pelvic inflammatory disease
Urinary retention
Hyperventilation
Epistaxis
Delayed ejaculation
Impotence
Acne
Hair loss
Blisters
Thinning of nails
Allergic reactions including urticaria, ecchymosis, angioedema
Eosinophilia
Leucopenia
Thrombocytopaenia
Alcohol abuse
Bleeding disturbance
Loss of voice
Hiccoughs
Thyroid abnormality

Contraindications

Buspirone has these contraindications:^[28]^[29]

Hypersensitivity to buspirone
Metabolic acidosis, as in diabetes
Should not be used with MAO inhibitors
Severely compromised liver and/or renal function

Interactions

Buspirone has been shown in vitro to be metabolized by CYP3A4. This finding is consistent with the in vivo interactions observed between buspirone and these inhibitors or inducers of cytochrome P450 3A4 (CYP3A4), among others:^[28]

Itraconazole: Increased plasma level of buspirone
Rifampicin: Decreased plasma levels of buspirone
Nefazodone: Increased plasma levels of buspirone
Haloperidol: Increased plasma levels of haloperidol
Carbamazepine: Decreased plasma levels of buspirone
Grapefruit: Significantly increases the plasma levels of buspirone.^[30] See Grapefruit–drug interactions.

The occurrence of elevated blood pressure has been reported when buspirone hydrochloride has been added to a regimen including a monoamine oxidase inhibitor (MAOI).^[28]

Overdose

Activated charcoal is believed to be an effective treatment for overdose, provided the patient is treated promptly. Expected symptoms (based on symptoms in male healthy volunteers treated with 375 mg/day — compared to the maximum daily licensed dosage in Australia, the UK, and the US):^[6]^[7]^[9]

Nausea
Vomiting
Dizziness
Drowsiness
Miosis
Gastric distress

Buspirone appears to be relatively benign in cases of single-drug overdose, although no definitive data on this subject appear to be available.^[31]

Pharmacology and mechanism

Buspirone functions as a serotonin 5-HT_1A receptor partial agonist (IA = 0.465).^[28]^[32]^[33] It is this action that is thought to mediate its anxiolytic and antidepressant effects.^[34] Additionally, it functions as a presynaptic dopamine antagonist at the D₂, D₃ and D₄ receptors.^[28]^[35]^[36] Buspirone is also a partial α₁ receptor agonist.^[37]^[38]^[39] Buspirone also appears to produce some oxytocin stimulation via 5-HT1A receptor-induced action. Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus reducing the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced. ^[40]^{[not in citation given]}^[41]

Binding Profile of Buspirone (towards cloned human receptors)^[42]

Receptor	Binding Affinity (K_i [nM])	Action
5-HT_1A	28.62	Agonist
5-HT_2A	138.03	Agonist
5-HT_2B	213.79	Agonist
5-HT_2C	489.77	Agonist
D₂	484	Antagonist
D₃	98	Antagonist
D₄	29	Antagonist
α₁		Agonist
α_1D		Agonist

Comparison to benzodiazepines

Buspirone's efficacy is comparable to that of members of the benzodiazepine family in treating GAD, although it tends to have a delayed onset of action.^[43]^[44]

Abrupt discontinuation of diazepam after six weeks of continuous administration resulted in withdrawal symptoms. This was not the case when administration of buspirone was ceased after six weeks.^[45] It may take several weeks before buspirone's anxiolytic effects become noticeable, and many patients may also need a higher dosage to adequately respond to treatment.^[28]

Buspirone's chemical structure and mechanism of action are completely unrelated to those of benzodiazepines and is not effective as a treatment for benzodiazepine withdrawal.^[46] Unlike benzodiazepines, buspirone is not a drug of abuse.^[7]

Synthesis

Buspirone synthesis:^[47] DE 2057845 U.S. Patent 3,717,634 U.S. Patent 3,907,801 U.S. Patent 3,976,776

Alkylation of 1-(2-pyrimidyl)piperazine (1) with 3-chloro-1-cyanopropane (2, 4-chlorobutyronitrile) gives 3, which is reduced either by hydrogenation over Raney nickel catalyst, or with LAH. The resulting 1° amine (4) from the previous step is then reacted with 3,3-Tetramethyleneglutaric anhydride (5, 8-Oxaspiro[4.5]decane-7,9-dione) in order to yield buspirone (6).

analogues

Gepirone, Tandospirone, Zalospirone, Tiospirone.

References

^ ^a ^b ^c ^d ^e "buspirone (Rx) - BuSpar, Buspirex, more..". Medscape Reference. WebMD. Retrieved 14 November 2013.
^ http://www.rxlist.com/script/main/mobileart-rx.asp?drug=buspar&monotype=rx-cp&monopage=10
^ "Commonly Prescribed Psychotropic Medications". NAMI. Retrieved 25 June 2014.
^ Wu Y-H, Rayburn LE, Ferguson JW (1972). "Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro[4.5]decane-7,9-diones". J.Med.Chem. 15 (5): 477–479. doi:10.1021/jm00275a009. PMID 5035267.
^ US Patent 3907801 N-(8 (4-pyridyl-piperazino)-alkyl(9 -azaspiroalkanediones
^ ^a ^b ^c "BUSPIRONE HCL (buspirone hydrochloride) tablet [Watson Laboratories, Inc.]". DailyMed. Watson Laboratories, Inc. July 2013. Retrieved 14 November 2013.
^ ^a ^b ^c ^d "BUSPAR® (buspirone hydrochloride) Tablets 5 mg & 10 mg PRODUCT INFORMATION" (PDF). TGA eBusiness Services. Aspen Pharma Pty Ltd. January 2010. Retrieved 14 November 2013.
^ Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.
^ ^a ^b ^c "Buspirone 10mg Tablets". electronic Medicines Compendium. Actavis UK Ltd. 10 September 2012. Retrieved 14 November 2013.
^ Joint Formulary Committee. British National Formulary (BNF). Pharmaceutical Press. p. 224.
^ "The STAR*D Trial: First Results". Psych Central. The Carlat Psychiaty Report. Retrieved 15 September 2014.
^ National Institute Of Health. "Questions and Answers about the NIMH Sequenced Treatment Alternatives to Relieve Depression (STAR*D) Study — All Medication Levels". Retrieved 12 August 2012.
^ Trivedi MH, Fava M, Wisniewski SR, Thase ME, Quitkin F, Warden D, Ritz L, Nierenberg AA, Lebowitz BD, Biggs MM, Luther JF, Shores-Wilson K, Rush AJ (March 2006). "Medication augmentation after the failure of SSRIs for depression". The New England Journal of Medicine. 354 (12): 1243–52. doi:10.1056/NEJMoa052964. PMID 16554526.
^ Appelberg BG, Syvälahti EK, Koskinen TE, Mehtonen OP, Muhonen TT, Naukkarinen HH (June 2001). "Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors: results from a placebo-controlled, randomized, double-blind, placebo wash-in study". The Journal of Clinical Psychiatry. 62 (6): 448–52. doi:10.4088/JCP.v62n0608. PMID 11465522.
^ Malhotra S, Santosh PJ (April 1998). "An open clinical trial of buspirone in children with attention-deficit/hyperactivity disorder". Journal of the American Academy of Child and Adolescent Psychiatry. 37 (4): 364–71. doi:10.1097/00004583-199804000-00013. PMID 9549956.
^ Mohammadi MR, Hafezi P, Galeiha A, Hajiaghaee R, Akhondzadeh S (November 2012). "Buspirone versus Methylphenidate in the Treatment of Children with Attention- Deficit/ Hyperactivity Disorder: Randomized Double-Blind Study". Acta Medica Iranica. 50 (11): 723–8. PMID 23292622.
^ Sutherland SM, Adler LA, Chen C, Smith MD, Feltner DE (April 2012). "An 8-week, randomized controlled trial of atomoxetine, atomoxetine plus buspirone, or placebo in adults with ADHD". The Journal of Clinical Psychiatry. 73 (4): 445–50. doi:10.4088/JCP.10m06788. PMID 22313788.
^ Davari-Ashtiani R, Shahrbabaki ME, Razjouyan K, Amini H, Mazhabdar H (December 2010). "Buspirone versus methylphenidate in the treatment of attention deficit hyperactivity disorder: a double-blind and randomized trial" (PDF). Child Psychiatry and Human Development. 41 (6): 641–8. doi:10.1007/s10578-010-0193-2. PMID 20517641.
^ http://archneur.jamanetwork.com/article.aspx?articleid=593671
^ "The relationship between buspirone bioavailability and dose in healthy subjects". Biopharmaceutics & Drug Disposition. 6: 139–145. doi:10.1002/bdd.2510060205.
^ List, RX. "Buspar Dosage". RX List. Retrieved 25 August 2014.
^ "Clinical Effects of the 5-HT1A Partial Agonists in Depression: A Composite Analysis of Buspirone in the Treatment of Depression.". Journal of Clinical Psychopharmacology:.
^ "Buspirone, a novel nonbenzodiazepine anxiolytic.". Clinical Pharmacy.
^ "Clinical Studies of Buspirone". Psychopathology.
^ "Effects of Buspirone on Agitation Associated With Dementia". The American Journal of Geriatric Psychiatry. 1: 82–84. doi:10.1097/00019442-199300110-00011.
^ "Metabolism and disposition of buspirone". The American Journal of Medicine. 6: 139–145. doi:10.1002/bdd.2510060205.
^ "The comparative efficacy of buspirone and diazepam in the treatment of anxiety.". The American Journal of Psychiatry.
^ ^a ^b ^c ^d ^e ^f "Buspirone monograph". Drugs.com. Retrieved 2011-08-27.
^ Geddes, John; Gelder, Michael G.; Mayou, Richard (2005). Psychiatry. Oxford [Oxfordshire]: Oxford University Press. p. 237. ISBN 0-19-852863-9.
^ Lilja JJ, Kivistö KT, Backman JT, Lamberg TS, Neuvonen PJ (December 1998). "Grapefruit juice substantially increases plasma concentrations of buspirone". Clinical Pharmacology and Therapeutics. 64 (6): 655–60. doi:10.1016/S0009-9236(98)90056-X. PMID 9871430.
^ Fulton B, Brogden RN (January 1997). "Buspirone" (PDF). CNS Drugs. 7 (1): 68–88. doi:10.2165/00023210-199707010-00007.
^ Blier P, Bergeron R, de Montigny C (May 1997). "Selective activation of postsynaptic 5-HT1A receptors induces rapid antidepressant response". Neuropsychopharmacology. 16 (5): 333–8. doi:10.1016/S0893-133X(96)00242-4. PMID 9109104.
^ Zuideveld KP, Rusiç-Pavletiç J, Maas HJ, Peletier LA, Van der Graaf PH, Danhof M (December 2002). "Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats". The Journal of Pharmacology and Experimental Therapeutics. 303 (3): 1130–7. doi:10.1124/jpet.102.036798. PMID 12438536.
^ Loane C, Politis M (2012). "Buspirone: what is it all about?". Brain Research. 1461: 111–8. doi:10.1016/j.brainres.2012.04.032. PMID 22608068.
^ Shelton KL, Hendrick ES, Beardsley PM (May 2013). "Efficacy of buspirone for attenuating cocaine and methamphetamine reinstatement in rats". Drug and Alcohol Dependence. 129 (3): 210–6. doi:10.1016/j.drugalcdep.2013.01.003. PMC 3628295. PMID 23374566.
^ Bergman J, Roof RA, Furman CA, Conroy JL, Mello NK, Sibley DR, Skolnick P (March 2013). "Modification of cocaine self-administration by buspirone (buspar®): potential involvement of D3 and D4 dopamine receptors". The International Journal of Neuropsychopharmacology. 16 (2): 445–58. doi:10.1017/S1461145712000661. PMID 22827916.
^ "Role of α 1-adrenoceptors in the reduction of external carotid blood flow induced by buspirone and ipsapirone in the dog". Retrieved 17 September 2014.
^ Maximiliano Marquez. "Pharmacological evidence for interactions between 5HT1A receptor agonists and subtypes of α1-adrenoceptors on rabbit aorta". Retrieved 17 September 2014.
^ Manfrid Eltze; Helga König; Brigitte Ullrich; Thomas Grebe. "Buspirone functionally discriminates tissues endowed with α1-adrenoceptor subtypes A, B, D and L". European Journal of Pharmacology. 378: 69–83. doi:10.1016/S0014-2999(99)00426-4. Retrieved 17 September 2014.
^ Uvnäs-Moberg K, Hillegaart V, Alster P, Ahlenius S (1996). "Effects of 5-HT agonists, selective for different receptor subtypes, on oxytocin, CCK, gastrin and somatostatin plasma levels in the rat". Neuropharmacology. 35 (11): 1635–40. doi:10.1016/S0028-3908(96)00078-0. PMID 9025112.
^ Chiodera P, Volpi R, Capretti L, Caffarri G, Magotti MG, Coiro V (April 1996). "Different effects of the serotonergic agonists buspirone and sumatriptan on the posterior pituitary hormonal responses to hypoglycemia in humans". Neuropeptides. 30 (2): 187–92. doi:10.1016/S0143-4179(96)90086-4. PMID 8771561.
^ Roth BL, Driscol J (12 January 2011). "PDSP K_i Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 November 2013.
^ Cohn JB, Rickels K (1989). "A pooled, double-blind comparison of the effects of buspirone, diazepam and placebo in women with chronic anxiety". Current Medical Research and Opinion. 11 (5): 304–20. doi:10.1185/03007998909115213. PMID 2649317.
^ Goldberg HL, Finnerty RJ (September 1979). "The comparative efficacy of buspirone and diazepam in the treatment of anxiety". The American Journal of Psychiatry. 136 (9): 1184–7. doi:10.1176/ajp.136.9.1184. PMID 382878.
^ Murphy SM, Owen R, Tyrer P (April 1989). "Comparative assessment of efficacy and withdrawal symptoms after 6 and 12 weeks' treatment with diazepam or buspirone". The British Journal of Psychiatry. 154 (4): 529–34. doi:10.1192/bjp.154.4.529. PMID 2686797.
^ Sontheimer DL, Ables AZ (March 2001). "Is imipramine or buspirone treatment effective in patients wishing to discontinue long-term benzodiazepine use?". The Journal of Family Practice. 50 (3): 203. PMID 11252203.
^ Allen LE, Ferguson HC, Kissel JW (May 1972). "Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro(4.5)decane-7,9-diones". Journal of Medicinal Chemistry. 15 (5): 477–9. doi:10.1021/jm00275a009. PMID 5035267.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. Pharmacotherapy for generalized anxiety disorder in adults
2. 成人の単極性うつ病：抗不安薬による治療 unipolar depression in adults treatment with anxiolytics
3. 小児および思春期における自閉症スペクトラム障害：薬理学的介入 autism spectrum disorder in children and adolescents pharmacologic interventions
4. Approach to treating generalized anxiety disorder in adults
5. 選択的セロトニン再取り込み阻害剤（SSRI）に起因する性機能不全：マネージメント sexual dysfunction caused by selective serotonin reuptake inhibitors ssris management

English Journal

Involvement of serotonin and oxytocin in neural mechanism regulating amicable social signal in male mice: Implication for impaired recognition of amicable cues in BALB/c strain.

Arakawa H.
Behavioral neuroscience.Behav Neurosci.2017 Apr;131(2):176-191. doi: 10.1037/bne0000191.
Social signals play a primary role in regulating social relationships among male mice. The present series of experiments investigated the neural mechanisms underlying an induction of amicable cues that facilitate social approach in male mice of the C57BL/6 (B6) and BALB/c (BALB) strains. Male mice e
PMID 28301190

Human motoneurone excitability is depressed by activation of serotonin 1A receptors with buspirone.

D'Amico JM1, Butler AA1,2, Héroux ME1,2, Cotel F3, Perrier JM4, Butler JE1,2, Gandevia SC1,2, Taylor JL1,2.
The Journal of physiology.J Physiol.2017 Mar 1;595(5):1763-1773. doi: 10.1113/JP273200. Epub 2016 Dec 17.
PMID 27859267

Long-Term Effects of Chronic Buspirone during Adolescence Reduce the Adverse Influences of Neonatal Inflammatory Pain and Stress on Adaptive Behavior in Adult Male Rats.

Butkevich IP1, Mikhailenko VA1, Vershinina EA2, Aloisi AM3, Barr GA4.
Frontiers in behavioral neuroscience.Front Behav Neurosci.2017 Jan 26;11:11. doi: 10.3389/fnbeh.2017.00011. eCollection 2017.
PMID 28184190

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★リンクテーブル★

「BUSPAR」

Buspirone
Systematic (IUPAC) name
	8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione
Clinical data
Trade names	Buspar
AHFS/Drugs.com	Monograph
MedlinePlus	a688005
Pregnancy; category	AU: B1; US: B (No risk in non-human studies); ;
Routes of; administration	Oral
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	~4%
Protein binding	86-95%
Metabolism	Hepatic mostly via CYP3A4
Biological half-life	2-3 hours
Excretion	Urine (29-63%), Faeces (18-38%)
Identifiers
CAS Number	36505-84-7
ATC code	N05BE01 (WHO)
PubChem	CID 2477
IUPHAR/BPS	36
DrugBank	DB00490
ChemSpider	2383
UNII	TK65WKS8HL
KEGG	D07593
ChEBI	CHEBI:3223
ChEMBL	CHEMBL49
Chemical data
Formula	C21H31N5O2
Molar mass	385.50314 g/mol
	SMILES O=C1N(CCCCN2CCN(CC2)C3=NC=CC=N3)C(CC4(CCCC4)C1)=O ;
	InChI InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2 ; Key:QWCRAEMEVRGPNT-UHFFFAOYSA-N ;
(verify)

　　[★] ブスピロン

関: buspirone

[MSR-1] "buspirone (Rx) - BuSpar, Buspirex, more..". Medscape Reference. WebMD. Retrieved 14 November 2013.

[2] ttp://www.rxlist.com/script/main/mobileart-rx.asp?drug=buspar&monotype=rx-cp&monopage=10

[3] "Commonly Prescribed Psychotropic Medications". NAMI. Retrieved 25 June 2014.

[4] Wu Y-H, Rayburn LE, Ferguson JW (1972). "Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro[4.5]decane-7,9-diones". J.Med.Chem. 15 (5): 477–479. doi:10.1021/jm00275a009. PMID 5035267.

[5] US Patent 3907801 N-(8 (4-pyridyl-piperazino)-alkyl(9 -azaspiroalkanediones

[DM-6] "BUSPIRONE HCL (buspirone hydrochloride) tablet [Watson Laboratories, Inc.]". DailyMed. Watson Laboratories, Inc. July 2013. Retrieved 14 November 2013.

[TGA-7] "BUSPAR® (buspirone hydrochloride) Tablets 5 mg & 10 mg PRODUCT INFORMATION" (PDF). TGA eBusiness Services. Aspen Pharma Pty Ltd. January 2010. Retrieved 14 November 2013.

[AMH-8] Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.

[EMC-9] "Buspirone 10mg Tablets". electronic Medicines Compendium. Actavis UK Ltd. 10 September 2012. Retrieved 14 November 2013.

[BNF-10] Joint Formulary Committee. British National Formulary (BNF). Pharmaceutical Press. p. 224.

[11] "The STAR*D Trial: First Results". Psych Central. The Carlat Psychiaty Report. Retrieved 15 September 2014.

[12] National Institute Of Health. "Questions and Answers about the NIMH Sequenced Treatment Alternatives to Relieve Depression (STAR*D) Study — All Medication Levels". Retrieved 12 August 2012.

[pmid16554526-13] Trivedi MH, Fava M, Wisniewski SR, Thase ME, Quitkin F, Warden D, Ritz L, Nierenberg AA, Lebowitz BD, Biggs MM, Luther JF, Shores-Wilson K, Rush AJ (March 2006). "Medication augmentation after the failure of SSRIs for depression". The New England Journal of Medicine. 354 (12): 1243–52. doi:10.1056/NEJMoa052964. PMID 16554526.

[pmid11465522-14] Appelberg BG, Syvälahti EK, Koskinen TE, Mehtonen OP, Muhonen TT, Naukkarinen HH (June 2001). "Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors: results from a placebo-controlled, randomized, double-blind, placebo wash-in study". The Journal of Clinical Psychiatry. 62 (6): 448–52. doi:10.4088/JCP.v62n0608. PMID 11465522.

[15] Malhotra S, Santosh PJ (April 1998). "An open clinical trial of buspirone in children with attention-deficit/hyperactivity disorder". Journal of the American Academy of Child and Adolescent Psychiatry. 37 (4): 364–71. doi:10.1097/00004583-199804000-00013. PMID 9549956.

[16] Mohammadi MR, Hafezi P, Galeiha A, Hajiaghaee R, Akhondzadeh S (November 2012). "Buspirone versus Methylphenidate in the Treatment of Children with Attention- Deficit/ Hyperactivity Disorder: Randomized Double-Blind Study". Acta Medica Iranica. 50 (11): 723–8. PMID 23292622.

[17] Sutherland SM, Adler LA, Chen C, Smith MD, Feltner DE (April 2012). "An 8-week, randomized controlled trial of atomoxetine, atomoxetine plus buspirone, or placebo in adults with ADHD". The Journal of Clinical Psychiatry. 73 (4): 445–50. doi:10.4088/JCP.10m06788. PMID 22313788.

[18] Davari-Ashtiani R, Shahrbabaki ME, Razjouyan K, Amini H, Mazhabdar H (December 2010). "Buspirone versus methylphenidate in the treatment of attention deficit hyperactivity disorder: a double-blind and randomized trial" (PDF). Child Psychiatry and Human Development. 41 (6): 641–8. doi:10.1007/s10578-010-0193-2. PMID 20517641.

[19] ttp://archneur.jamanetwork.com/article.aspx?articleid=593671

[20] "The relationship between buspirone bioavailability and dose in healthy subjects". Biopharmaceutics & Drug Disposition. 6: 139–145. doi:10.1002/bdd.2510060205.

[21] List, RX. "Buspar Dosage". RX List. Retrieved 25 August 2014.

[22] "Clinical Effects of the 5-HT1A Partial Agonists in Depression: A Composite Analysis of Buspirone in the Treatment of Depression.". Journal of Clinical Psychopharmacology:.

[23] "Buspirone, a novel nonbenzodiazepine anxiolytic.". Clinical Pharmacy.

[24] "Clinical Studies of Buspirone". Psychopathology.

[25] "Effects of Buspirone on Agitation Associated With Dementia". The American Journal of Geriatric Psychiatry. 1: 82–84. doi:10.1097/00019442-199300110-00011.

[26] "Metabolism and disposition of buspirone". The American Journal of Medicine. 6: 139–145. doi:10.1002/bdd.2510060205.

[27] "The comparative efficacy of buspirone and diazepam in the treatment of anxiety.". The American Journal of Psychiatry.

[mono-28] ^ ^a ^b ^c ^d ^e ^f "Buspirone monograph". Drugs.com. Retrieved 2011-08-27.

[Gelder-29] Geddes, John; Gelder, Michael G.; Mayou, Richard (2005). Psychiatry. Oxford [Oxfordshire]: Oxford University Press. p. 237. ISBN 0-19-852863-9.

[30] Lilja JJ, Kivistö KT, Backman JT, Lamberg TS, Neuvonen PJ (December 1998). "Grapefruit juice substantially increases plasma concentrations of buspirone". Clinical Pharmacology and Therapeutics. 64 (6): 655–60. doi:10.1016/S0009-9236(98)90056-X. PMID 9871430.

[CNS-31] Fulton B, Brogden RN (January 1997). "Buspirone" (PDF). CNS Drugs. 7 (1): 68–88. doi:10.2165/00023210-199707010-00007.

[32] Blier P, Bergeron R, de Montigny C (May 1997). "Selective activation of postsynaptic 5-HT1A receptors induces rapid antidepressant response". Neuropsychopharmacology. 16 (5): 333–8. doi:10.1016/S0893-133X(96)00242-4. PMID 9109104.

[33] Zuideveld KP, Rusiç-Pavletiç J, Maas HJ, Peletier LA, Van der Graaf PH, Danhof M (December 2002). "Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats". The Journal of Pharmacology and Experimental Therapeutics. 303 (3): 1130–7. doi:10.1124/jpet.102.036798. PMID 12438536.

[pmid22608068-34] Loane C, Politis M (2012). "Buspirone: what is it all about?". Brain Research. 1461: 111–8. doi:10.1016/j.brainres.2012.04.032. PMID 22608068.

[pmid23374566-35] Shelton KL, Hendrick ES, Beardsley PM (May 2013). "Efficacy of buspirone for attenuating cocaine and methamphetamine reinstatement in rats". Drug and Alcohol Dependence. 129 (3): 210–6. doi:10.1016/j.drugalcdep.2013.01.003. PMC 3628295. PMID 23374566.

[36] Bergman J, Roof RA, Furman CA, Conroy JL, Mello NK, Sibley DR, Skolnick P (March 2013). "Modification of cocaine self-administration by buspirone (buspar®): potential involvement of D3 and D4 dopamine receptors". The International Journal of Neuropsychopharmacology. 16 (2): 445–58. doi:10.1017/S1461145712000661. PMID 22827916.

[37] "Role of α 1-adrenoceptors in the reduction of external carotid blood flow induced by buspirone and ipsapirone in the dog". Retrieved 17 September 2014.

[38] Maximiliano Marquez. "Pharmacological evidence for interactions between 5HT1A receptor agonists and subtypes of α1-adrenoceptors on rabbit aorta". Retrieved 17 September 2014.

[39] Manfrid Eltze; Helga König; Brigitte Ullrich; Thomas Grebe. "Buspirone functionally discriminates tissues endowed with α1-adrenoceptor subtypes A, B, D and L". European Journal of Pharmacology. 378: 69–83. doi:10.1016/S0014-2999(99)00426-4. Retrieved 17 September 2014.

[pmid9025112-40] Uvnäs-Moberg K, Hillegaart V, Alster P, Ahlenius S (1996). "Effects of 5-HT agonists, selective for different receptor subtypes, on oxytocin, CCK, gastrin and somatostatin plasma levels in the rat". Neuropharmacology. 35 (11): 1635–40. doi:10.1016/S0028-3908(96)00078-0. PMID 9025112.

[pmid8771561-41] Chiodera P, Volpi R, Capretti L, Caffarri G, Magotti MG, Coiro V (April 1996). "Different effects of the serotonergic agonists buspirone and sumatriptan on the posterior pituitary hormonal responses to hypoglycemia in humans". Neuropeptides. 30 (2): 187–92. doi:10.1016/S0143-4179(96)90086-4. PMID 8771561.

[42] Roth BL, Driscol J (12 January 2011). "PDSP K_i Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 November 2013.

[43] Cohn JB, Rickels K (1989). "A pooled, double-blind comparison of the effects of buspirone, diazepam and placebo in women with chronic anxiety". Current Medical Research and Opinion. 11 (5): 304–20. doi:10.1185/03007998909115213. PMID 2649317.

[44] Goldberg HL, Finnerty RJ (September 1979). "The comparative efficacy of buspirone and diazepam in the treatment of anxiety". The American Journal of Psychiatry. 136 (9): 1184–7. doi:10.1176/ajp.136.9.1184. PMID 382878.

[45] Murphy SM, Owen R, Tyrer P (April 1989). "Comparative assessment of efficacy and withdrawal symptoms after 6 and 12 weeks' treatment with diazepam or buspirone". The British Journal of Psychiatry. 154 (4): 529–34. doi:10.1192/bjp.154.4.529. PMID 2686797.

[46] Sontheimer DL, Ables AZ (March 2001). "Is imipramine or buspirone treatment effective in patients wishing to discontinue long-term benzodiazepine use?". The Journal of Family Practice. 50 (3): 203. PMID 11252203.

[47] Allen LE, Ferguson HC, Kissel JW (May 1972). "Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro(4.5)decane-7,9-diones". Journal of Medicinal Chemistry. 15 (5): 477–9. doi:10.1021/jm00275a009. PMID 5035267.

v t e Anxiolytics (N05B)

5-HT_1A agonists	Buspirone Tandospirone

GABA_AR PAMs	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam Others: Alpidem^‡ Barbiturates Carbamates Chlormezanone^‡ Ethanol Etifoxine; Herbs: Kava Skullcap Valerian

α₂δ VDCC blockers	Gabapentin Gabapentin enacarbil Phenibut Pregabalin

Antidepressants	SSRIs SNRIs SARIs TCAs TeCAs MAOIs; Others: Agomelatine Bupropion Vilazodone Vortioxetine

Sympatholytics	Beta blockers (e.g., propranolol) Clonidine Dexmedetomidine Guanfacine Prazosin

Others	Benzoctamine Cannabidiol Cycloserine Fabomotizole Hydroxyzine Kanna Lavender Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum

v t e Piperazines

Simple piperazines (no additional rings)	1-Cyclohexylpiperazine Aminoethylpiperazine Diethylcarbamazine HEPPS Midafotel Piperazine PIPES

Phenylpiperazines	Acaprazine Antrafenine Aripiprazole Batoprazine Bifeprunox BRL-15,572 Ciprofloxacin CSP-2503 Dapiprazole DCPP DMPP Diphenylpiperazine Dropropizine EGIS-12,233 Elopiprazole Eltoprazine Enpiprazole Ensaculin Etoperidone Flesinoxan Flibanserin Fluprazine Itraconazole Ketoconazole Levodropropizine Lorpiprazole mCPP Mefway MeOPP Mepiprazole Naftopidil Naluzotan Naphthylpiperazine Nefazodone Niaprazine Oxypertine Pardoprunox pCPP pFPP Posaconazole S-14,506 S-14,671 S-15,535 SB-258,585 SB-271,046 SB-357,134 SB-399,885 Sonepiprazole TFMPP Tolpiprazole Trazodone Urapidil Vesnarinone Vilazodone Vortioxetine WAY-100,135 WAY-100,635

Benzylpiperazines	2C-B-BZP Befuraline Bifeprunox Buclizine BZP Chlorbenzoxamine DBZP Fipexide Imatinib MBZP MDBZP Meclozine Methoxypiperamide Piberaline Piribedil Sunifiram Trimetazidine Vesnarinone

Diphenylalkylpiperazines (benzhydrylalkylpiperazines)	Almitrine Amperozide BRL-15,572 Buclizine BW373U86 Cetirizine Chlorbenzoxamine Chlorcyclizine Cinnarizine Clocinizine Cyclizine DBL-583 Diphenylmethylpiperazine Dotarizine DPI-221 DPI-287 DPI-3290 GBR-12,783 GBR-12,935 GBR-13,069 GBR-13,098 GBR-13,119 Hydroxyzine Lidoflazine Manidipine Meclozine Oxatomide SNC-80 Vanoxerine

Pyrimidinylpiperazines	Buspirone Dasatinib Eptapirone Gepirone Ipsapirone Piribedil Prazitone Pyrimidinylpiperazine Revospirone Tandospirone Tirilazad Trimazosin Umespirone Zalospirone

Pyridinylpiperazines	Atevirdine Azaperone Delavirdine Mirtazapine Pyridinylpiperazine

Benzo(iso)thiazolylpiperazines	Lurasidone Perospirone Revospirone Tiospirone Ziprasidone

Tricyclics (piperazine attached via side chain)	Amoxapine Clopenthixol Clorotepine Clozapine Cyanothepin Doclothepin Docloxythepin Flupentixol Fluphenazine Isofloxythepin Loxapine Meperathiepin Metitepine Octomethothepin Olanzapine Opipramol Oxyclothepin Oxyprothepin Peradithiepin Perathiepin Perazine Perphenazine Pirenzepine Prochlorperazine Thiethylperazine Thiothixene Trifluoperazine Trifluthepin Zuclopenthixol

Others/Uncategorized	6-Nitroquipazine Azimilide Cinepazet Cinepazic acid Cinepazide Cyclohexylpiperazine Hexocyclium Indinavir JNJ-7777120 Lodenafil Mirodenafil PB-28 Quipazine Ranolazine SA-4503 Sildenafil Tadalafil Vardenafil VUF-6002 Zipeprol

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