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Buspirone-an anxiolytic drug that is primarily used to treat generalized anxiety disorder.

Buspirone, brand name Buspar, is an anxiolytic drug that is primarily used to treat generalized anxiety disorder. It is also commonly used to augment antidepressants in the treatment of depression. More

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Description

Buspirone, brand name Buspar, is an anxiolytic drug that is primarily used to treat generalized anxiety disorder. It is also commonly used to augment antidepressants in the treatment of depression.

Generic Name

Buspirone-an anxiolytic drug that is primarily used to treat generalized anxiety disorder.

Chemical names

Ansial; Buspironum; Buspirona

Brand names

Buscalm, Buson, Buspidac, Buspin, Supiron-B, Tamspar

IUPAC name

8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione

Pharmacokinetics

Actions

Buspirone will suppress serotonergic activity is while noradrenergic and dopaminergic cell firing is enhanced, it binds to 5-HT type 1A serotonin receptors on postsynaptic neurons and on presynaptic neurons in the dorsal raphe, in the hippocampus thus inhibiting the rate of 5-HT-containing neurons in the dorsal raphe. It also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of neither neither brain where nor are epinephrine cell bodies found in high concentration. 

Dosage/Dosage form

Initially, 5 mg bid/tid increased by 5-mg increments at intervals of 2-3 days.

Therapeutic uses

In short term management of anxiety

Adverse effects/Side effects

Dizziness, nausea, headache, nervousness, lightheadedness, paraesthesia, excitement, sleep disturbances, tinnitus, chest pain, nasal congestion, sore throat. Less sedation and lower potential for dependence compared to other anxiolytics.

Interaction

  • Elevation of BP when taken concomitantly with MAOIs.
  • Enhanced sedative effects with alcohol or CNS depressants.
  • Increases serum haloperidol. Concurrent admin with MAOIs may lead to increase in BP.

Contraindications

  • Hypersensitivity.
  • Epilepsy; severe renal or hepatic impairment; children <18 yr;
  •  Pregnancy
  •  Lactation.

Storage

Store at 15-30°C

Information

Molecular weight

385.5031

Molecular formula

C21H31N5O2

CAS number

36505-84-7

Precautions

  • Preceding co-administration of MAOIs decreased renal or hepatic function.
  • May impair ability to drive or operate machinery.
  • In patients on benzodiazepines, withdraw the drug gradually.