Buspirone
Systematic (IUPAC) name
8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]- 8-azaspiro[4.5]decane-7,9-dione
Identifiers
CAS number	36505-84-7
ATC code	N05BE01
PubChem	2477
DrugBank	APRD00222
Chemical data
Formula	C21H31N5O2
Mol. mass	385.50314 g/mol
Pharmacokinetic data
Bioavailability	low and variable (approx. 5%), due to high first pass metabolism
Protein binding	95% bound to plasma proteins
Metabolism	mainly hepatic, active metabolite 1-Pyrimidylpiperazin (1-PP)
Half life	2-3hr
Excretion	urine (29-63%) and feces (18-38%) in the form of metabolites
Therapeutic considerations
Pregnancy cat.	B(US) Image File history File links Formula is drawn in bkchem and GIMP. File history Legend: (cur) = this is the current file, (del) = delete this old version, (rev) = revert to this old version. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is an easy way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... This article is about the chemistry of hydrogen. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... This article is about the chemical element and its most stable form, or dioxygen. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The biological half-life of a substance is the time required for half of that substance to be removed from an organism by either a physical or a chemical process. ... The kidneys are important excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... For other uses of terms redirecting here, see US (disambiguation), USA (disambiguation), and United States (disambiguation) Motto In God We Trust(since 1956) (From Many, One; Latin, traditional) Anthem The Star-Spangled Banner Capital Washington, D.C. Largest city New York City National language English (de facto)1 Demonym American...
Legal status	Rx-only, not a controlled substance The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...
Routes	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] In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... An anxiolytic is a drug prescribed for the treatment of symptoms of anxiety. ... A serotonin receptor agonist is a compound that activates serotonin receptors, mimicking the effect of the neurotransmitter serotonin. ... Azaspirodecanediones are a class of drugs with anxiolytic effects used in the treatment of anxiety. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ... Diazepam (IPA: ), first marketed as Valium by Hoffmann-La Roche) is a benzodiazepine derivative drug. ... Generalized anxiety disorder (GAD) is an anxiety disorder that is characterized by excessive, uncontrollable and often irrational worry about everyday things, which is disproportionate to the actual source of worry. ...

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, barbiturates and alcohol does not exist. Furthermore, it is non-sedating. This article is about the concept of addiction. ... This article is about state anxiety. ... Alprazolam 2 mg tablets The benzodiazepines (pronounced , often abbreviated to benzos) are a class of sedative hypnotic psychoactive drugs with varying hypnotic, sedative, anxiolytic, anticonvulsant, muscle relaxant and amnesic properties, which are mediated by slowing down the central nervous system. ... Dendritic cells can take up self antigens from other cells and cross-present them to autoreactive T cells. ... Barbituric acid, the basic structure of all barbiturates Barbiturates are drugs that act as central nervous system depressants, and by virtue of this they produce a wide spectrum of effects, from mild sedation to anesthesia. ... Grain alcohol redirects here. ...

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. Chemical structure of D-aspartic acid, a common amino acid neurotransmitter. ... For the professional wrestling stable, see Ravens Nest#Serotonin. ... In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT. 5-HT receptors are located on the cell membrane of nerve cells and other cell types in animals and mediate the effects of serotonin... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... For other uses, see Dopamine (disambiguation). ... Gaba may refer to: Gabâ or gabaa (Philippines), the concept of negative karma of the Cebuano people GABA, the gamma-amino-butyric acid neurotransmitter GABA receptor, in biology, receptors with GABA as their endogenous ligand Gaba 1 to 1, an English conversational school in Japan Marianne Gaba, a US model...

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. SSRI redirects here; for other uses, see SSRI (disambiguation). ...

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 (NYSE: BMY), colloquially referred to as BMS, is a pharmaceutical corporation, formed by a 1989 merger between pharmaceutical companies Bristol-Myers Company, founded in 1887 by William McLaren Bristol and John Ripley Myers in Clinton, NY (both were graduates of Hamilton College), and Squibb Corporation. ...

Indications

• 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 depression

Bold text== Contraindications == Generalized anxiety disorder (GAD) is an anxiety disorder that is characterized by excessive, uncontrollable and often irrational worry about everyday things, which is disproportionate to the actual source of worry. ... SSRI is an acronym that stands for several things: It is a class of antidepressants called selective serotonin reuptake inhibitor SSRI also is used as the stock symbol for Silver Standard Resources Inc. ... On the Threshold of Eternity. ...

• Myasthenia gravis
• Acute closed angle glaucoma
• Severely compromised liver- and renal-function
• Concomitant treatment with a MAO-Inhibitor (severe hypertensive crises have been seen)
• Preexisting heart conditions (e.g. myocardial infarction)

buspirone also used for cessation of smoking Myasthenia gravis (sometimes abbreviated MG; from the Greek myastheneia, lit. ... The liver is the largest internal organ in the human body, and is an organ present in vertebrates and some other animals. ... Kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ... Monoamine oxidase inhibitors (MAOIs) are a class of antidepressant drugs prescribed for the treatment of depression. ... In medicine, hypertension refers to the problem of abnormally high blood pressure. ... Heart attack redirects here. ...

Side-effects

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). An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted, negative consequences associated with the use of given medications. ... For other uses, see Vertigo. ... Agitation may have the following special meanings Agitation, an emotional state Agitation, putting into motion (by shaking or stirring) Agitation, a term from the lexicon of Communists: political activities aimed at urging people to do something This is a disambiguation page — a navigational aid which lists other pages that might... This article is about the sleeping disorder. ...

• Most frequent: vertigo, headaches, nervousness, agitation, light-headedness, nausea;
• Often (>1%) : drowsiness, insomnia, concentration disorders, confusion, depression, agitation, intestinal disorders, paresthesia, coordination disorders, tremors, disturbed vision, tinnitus, fatigue, weakness, Angina pectoris, sore throat, tachycardias, palpitations, dry mouth, pain in muscles and joints;
• Seldom: allergic reactions, subdermal bleeding, extrapyramidal symptoms, hallucinations, psychosis, ataxia, epileptic seizures, syncope, tunnel vision, urine retention, hyperosmia, alopecia, pruritus, hot flashes.

There are no dyscognitive side-effects like those seen in benzodiazepines. For other uses, see Vertigo. ... For other uses, see Nausea (disambiguation). ... This article is about the sleeping disorder. ... Look up Confusion in Wiktionary, the free dictionary Confusion can have the following meanings: Unclarity or puzzlement, e. ... On the Threshold of Eternity. ... Paresthesia or paraesthesia (in British English) is a sensation of tingling, pricking, or numbness of a persons skin with no apparent long-term physical effect, more generally known as the feeling of pins and needles or of a limb being asleep (but not directly related to the phenomenon of... For the film, see Tremors (film). ... Tinnitus (pronounced or ,[1] from the Latin word for ringing[2]) is the perception of sound in the human ear in the absence of corresponding external sound(s). ... The word fatigue is used in everyday living to describe a range of afflictions, varying from a general state of lethargy to a specific work induced burning sensation within muscle. ... This article or section does not cite any references or sources. ... This article does not cite any references or sources. ... This article needs cleanup. ... In human anatomy, the extrapyramidal system is a neural network located in the brain that is part of the motor system involved in the coordination of movement. ... A hallucination is a false sensory perception in the absence of an external stimulus, as distinct from an illusion, which is a misperception of an external stimulus. ... For other uses, see Psychosis (disambiguation). ... For other uses, see Ataxia (disambiguation). ... Epilepsy (often referred to as a seizure disorder) is a chronic neurological condition characterized by recurrent unprovoked seizures. ... This article or section does not cite its references or sources. ... Hyperosmia is an abnormally heightened sense of smell. ... Alopecia is a set of disorders ranging from male and female pattern alopecia (alopecia androgenetica), to alopecia areata, which involves the loss of some of the hair from the head, alopecia totalis, which involves the loss of all head hair, to the most extreme form, alopecia universalis, which involves the... An itch (Latin: pruritus) is a sensation felt on an area of skin that makes a person or animal want to scratch it. ... An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted, negative consequences associated with the use of given medications. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ...

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. For other uses, see Placebo (disambiguation). ...

Drug abuse and dependence

Buspirone has no known potential for abuse, psychological or physical dependence^[3].

Interactions

• Haloperidol : increased plasma-levels of haloperidol
• Rifampicin : decreased plasma-levels of buspirone
• MAO-Inhibitors : severe hypertensive crises are possible.
• Alcohol : The sedative properties of alcohol are increased slightly.
• Grapefruit, Grapefruit juice, Grapefruit extract : drastically increased plasma-levels of Buspirone ^[4] Do not mix the pills in grapefruit juice.

Haloperidol (sold under the tradenames Aloperidin, Bioperidolo, Brotopon, Dozic, Duraperidol (Germany), Einalon S, Eukystol, Haldol, Halosten, Keselan, Linton, Peluces, Serenace, Serenase, Sigaperidol) is a conventional, or typical, butyrophenone antipsychotic drug. ... Rifampicin (INN) (IPA: ) or rifampin (USAN) is a bacteriocidal antibiotic drug of the rifamycin group. ... Monoamine oxidase inhibitors (MAOIs) are a class of antidepressant drugs prescribed for the treatment of depression. ... Grain alcohol redirects here. ... Binomial name Macfad. ...

References

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. ^ Lydiurd, R. Bruce (2000). "An Overview of Generalized Anxiety Disorder: Disease State-Appropriate Therapy". Clinical Therapeutics 22 (Supplement A): A3-A24. 
4. ^ Lilja, JJ; Kivisto KT, Backman JT, Lamberg TS, Neuvonen PJ (December 1998). "Grapefruit juice substantially increases plasma concentrations of buspirone". Clinical Pharmacology & Therapeutics 64 (6): 655-660.