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Product Name: Buspar

Generics: Buspirone

Common Brand Names: Bespar; Buspinol; Censpar

Pharmaceutical Category: Antidepressants / Anti Anxiety

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There is an additional general information about this medication active ingredient buspirone:

Pharmacological action

Buspar is an anxiolytic drug, a derivative azaspirodecanedione. The mechanism of action is not established. On pharmacological properties this medication does not apply to benzodiazepines or barbiturates. Buspar has a selective anxiolytic effect. This medicine has no anticonvulsant activity, it has no myorelaxant action. It has no sedative effects, especially in low doses.
Buspar has a high affinity for serotonin 5-HT1A-receptors in the neurons of the dorsal suture, and moderate affinity for dopamine D2-receptors in the brain. Buspirone has no pronounced affinity for the benzodiazepine receptors, it does not affect the binding of GABA.
Unlike benzodiazepines, the level of spontaneous excitation of noradrenergic cells in locus ceruleus (locus ceruleus) under the action of buspirone increases rather than decreases. These specific differences in the scene due to differences in the development of dependence and tolerance between benzodiazepines and buspirone.
It is believed that Buspar does not cause tolerance, physical or psychological dependence.

Pharmacokinetics

After oral administration Buspar is rapidly absorbed from the gastrointestinal tract, Cmax plasma levels achieved after 40-90 min. The bioavailability is low due to the pronounced effect in the "first pass" through the liver. When Buspar is administered together with food it may increase the bioavailability of buspirone due to violation of absorption from the gastrointestinal tract and therefore reduce the first-pass clearance.
The binding of buspirone to plasma proteins is about 95%. This medication is subjected to intensive metabolism in the liver, with the participation of isoenzyme CYP3A4. As a result of hydroxylation is produced several inactive metabolites, oxidative dealkylation leads to the formation of 1-(2-pyrimidinyl)-piperazine, which has anxiolytic activity. T1/2 of buspirone is typically 2-4 hours, but the end of T1/2 may be 11 hours. Buspar derived mainly as metabolites in the urine, as well as in feces.

Why is Buspar prescribed?

A treatment of anxiety disorders or the temporary relief of anxiety symptoms.

Dosage and administration

Buspar is taken orally, for adults at the beginning of treatment - 5 mg 3 times / day. If necessary the dose increases to 5 mg / day every 2-3 days until the desired effect.
The maximum dose is 45-60 mg / day.

Buspar side effects, adverse reactions

Possible: dizziness, headache, a syndrome of motor restlessness.
Rarely: blurred vision, decreased ability to concentrate, dry mouth, myalgia, muscle cramps, muscle cramps and stiffness, ringing in the ears, sleep disorders, nightmares, fatigue, indigestion, chest pain, depression, tachycardia, paresthesia, sore throat, fever.

Buspar contraindications

Pronounced renal dysfunction, pronounced hepatic dysfunction, hypersensitivity to buspirone.

Using during pregnancy and breastfeeding

Avoid using Buspar during pregnancy and lactation. Category of the fetus by FDA - B.

Special instructions

Buspar is not used to treat anxiety and reduce stress associated with the stresses of everyday life.
This medicine should not be used in patients with epilepsy or a history of guidance on the propensity to develop seizures.
Use Buspar with caution in patients with impaired liver and / or kidneys function.
Patients who abuse drugs or indications for a history of drug dependence, during treatment require careful monitoring to detect the development of tolerance or dependence to buspirone.
In controlled studies it was found that buspirone is not effective for long-term (more than 3-4 weeks) treatment of anxiety. However, when applying Buspar for a few months there were found no adverse effects.
If buspirone is used for a long time, its effectiveness should be checked at regular intervals.
During treatment, patients should refrain from activities associated with the need to focus and speed of psychomotor reactions.
Safety and efficacy of buspirone in children and adolescents under the age of 18 have not been identified.

Buspar drug interactions

Buspirone is metabolized in the liver, with the participation of isoenzyme CYP3A4 and, apparently, may interact with drugs that are inhibitors or inducers of this isoenzyme. In combination with MAO inhibitors it may developed a hypertensive crisis.

Buspar in case of emergency / overdose

Symptoms: nausea, vomiting, gastrointestinal and other disorders, dizziness, cramps, drowsiness.
Treatment: gastric lavage, the appointment of activated charcoal, symptomatic therapy. Dialysis is ineffective.

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