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Buspirone
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| Systematic (IUPAC) name | |
| 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]- 8-azaspiro[4. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general 5]decane-7,9-dione |
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| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C21H31N5O2 |
| Mol. mass | 385. CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component 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 a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 50314 g/mol |
| Pharmacokinetic data | |
| Bioavailability | low and variable (approx. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of 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) |
| Legal status |
Rx-only, not a controlled substance |
| 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. A drug's efficiency 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 it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials 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 The United States of America —commonly referred to as the The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route 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. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam in treating generalized anxiety disorder. The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic Diazepam (daɪˈæzɨpæm 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 that [1][2]
It shows no potential for addiction compared to other drugs commonly prescribed for anxiety, especially benzodiazepine medications. The term " addiction " is used in many contexts to describe an obsession compulsion or excessive Physical dependence or psychological dependence such as Anxiety is a physiological and psychological state characterized by Cognitive, Somatic, Emotional and Behavioral components The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic The development of tolerance has not been noticed. Cross-tolerance to benzodiazepines, barbiturates and alcohol does not exist. Cross-tolerance refers to a Pharmacological phenomenon in which a patient being treated with a drug exhibits a physiological resistance to that medication as a result of tolerance 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 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. See Chemical synapse for an introduction to concepts and terminology used in this article Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons In the field of Neurochemistry, 5-HT receptors are receptors for the Neurotransmitter and peripheral signal mediator Serotonin, also An agonist is a term used to describe a type of ligand or drug that binds and alters the activity of a receptor. Additionally, it acts as a mixed agonist/antagonist on postsynaptic dopamine receptors. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates GABA-mediated effects are lacking. Gamma-aminobutyric acid (GABA is the chief inhibitory Neurotransmitter in the Mammalian Central nervous system. 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. Selective serotonin reuptake inhibitors ( SSRIs) are a class of Antidepressants used in the treatment of depression, Anxiety disorders
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. Bristol-Myers Squibb ( colloquially referred to as BMS, is a Pharmaceutical Corporation, formed by a 1989 merger between pharmaceutical companies The drug went generic in 2001.
Contents |
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
Contraindications
- 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. Generalized anxiety disorder ( GAD) is an Anxiety disorder that is characterized by excessive uncontrollable and often irrational worry about everyday things that Obsessive-compulsive disorder (OCD is a Chronic Anxiety disorder most commonly characterized by obsessive Distressing Intrusive thoughts Agoraphobia is an Anxiety disorder, often precipitated by the fear of having a Panic attack in a setting from which there is no easy means of escape Selective serotonin reuptake inhibitors ( SSRIs) are a class of Antidepressants used in the treatment of depression, Anxiety disorders Major depressive disorder, also known as major depression, unipolar depression, unipolar disorder, clinical depression, or simply depression Myasthenia gravis (literally "serious muscle-weakness" from Greek μύς "muscle" "weakness" and Latin gravis Glaucoma is a group of diseases of the Optic nerve involving loss of retinal ganglion cells in a characteristic pattern of optic neuropathy. The liver is a vital organ in the human body and is present in Vertebrates and some other animals The kidneys are complicated organs that have numerous biological roles Monoamine oxidase inhibitors ( MAOIs) are a class of powerful antidepressant drugs prescribed for the treatment of depression. Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated g. myocardial infarction)
Side-effects
Rarely, side-effects have a dangerous nature or intensity. Myocardial infarction ( MI or AMI for acute myocardial infarction) also known as a heart attack, occurs when the blood supply An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences Some tend to disappear with continued therapy, or are less frequent if the initial dose is low and increased gradually (vertigo, agitation, insomnia). Vertigo (from the Latin vertere, to turn and the suffix -igo, a condition i Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity
- 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. Vertigo (from the Latin vertere, to turn and the suffix -igo, a condition i Nausea ( Latin: Nausea, Greek:, " Sea-sickness " also called wamble) is the sensation of unease and discomfort Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity Confusion, of a Pathological degree usually refers to loss of orientation (ability to place oneself correctly in the world by time location and personal identity and Major depressive disorder, also known as major depression, unipolar depression, unipolar disorder, clinical depression, or simply depression Paresthesia (pron /ˌpɛɹɪsˈθiʒə/ paraesthesia in British English, pron Tremor is an unintentional somewhat rhythmic muscle movement involving to-and-from movements (oscillations of one or more parts of the body Tinnitus (tɪˈnaɪtəs or /ˈtɪnɪtəs/ from the Latin word for " Ringing " is the perception of sound within the human ear in the absence of corresponding Angina pectoris, commonly known as angina, is severe Chest pain due to Ischemia (a lack of blood and hence Oxygen supply of the heart A palpitation (medical term ectopic heart beat) is an abnormal awareness of the beating of the Heart, whether it is too slow too fast irregular Allergy is a disorder of the Immune system often also referred to as Atopy. 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 A hallucination, in the broadest sense is a Perception in the absence of a stimulus. Psychosis (from the Greek ψυχή "psyche" for mind or soul and -οσις "-osis" for abnormal condition with adjective psychotic Ataxia (from Greek α- as a negative prefix + -τάξις, meaning "lack of order" is a neurological sign and symptom consisting An epileptic seizure is caused by excessive and/or hypersynchronous electrical Neuronal activity and is usually self-limiting Hyperosmia is an increased ability to smell - for example being able to identify the perfume of the previous occupant of a chair Alopecia or hair loss is the medical description of the loss of hair from the head or body sometimes to the extent of Baldness. Itch ( Latin: pruritus) is an unpleasant Sensation that evokes the desire or Reflex to scratch
There are no dyscognitive side-effects like those seen in benzodiazepines. An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic
Other side-effects have been seen, but are not more frequent than those encountered with placebo. Placebo is a substance or procedure a patient accepts as medicine or therapy but which has no specific therapeutic activity An unusual side effect reported by patients has been an enhanced sense of smell.
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. Haloperidol is a Typical antipsychotic. It is in the Butyrophenone class of Antipsychotic medications and has pharmacological effects similar Rifampicin ( INN) (rɪˈfæmpəsɪn or rifampin ( USAN) is a Bactericidal Antibiotic drug of the Rifamycin group Monoamine oxidase inhibitors ( MAOIs) are a class of powerful antidepressant drugs prescribed for the treatment of depression.
- 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. The grapefruit is a subtropical Citrus Tree grown for its Fruit which was originally named the "forbidden fruit " of Barbados
References
- ^ 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.
- ^ 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.
- ^ Lydiurd, R. Bruce (2000). "An Overview of Generalized Anxiety Disorder: Disease State-Appropriate Therapy". Clinical Therapeutics 22 (Supplement A): A3-A24.
- ^ 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.
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