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Buspirone: Anxiolytic Insights

Buspirone is a partial agonist of the 5-HT1A receptor that is used to treat generalized anxiety disorder. It was originally developed as an antipsychotic but failed for that indication. However, it displayed anxiolytic effects in animals. Unlike benzodiazepines, buspirone does not impair functioning, lacks abuse potential, and does not cause withdrawal symptoms upon discontinuation. Its anxiolytic effects are believed to be mediated by actions at pre- and postsynaptic 5-HT1A receptors. It has a half-life of 3-4 hours and is generally well tolerated, though side effects like dizziness and drowsiness may occur.

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513 views10 pages

Buspirone: Anxiolytic Insights

Buspirone is a partial agonist of the 5-HT1A receptor that is used to treat generalized anxiety disorder. It was originally developed as an antipsychotic but failed for that indication. However, it displayed anxiolytic effects in animals. Unlike benzodiazepines, buspirone does not impair functioning, lacks abuse potential, and does not cause withdrawal symptoms upon discontinuation. Its anxiolytic effects are believed to be mediated by actions at pre- and postsynaptic 5-HT1A receptors. It has a half-life of 3-4 hours and is generally well tolerated, though side effects like dizziness and drowsiness may occur.

Uploaded by

leeperlhan2000
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPT, PDF, TXT or read online on Scribd

Chapter 14

Buspirone

Introduction
Partial agonist of the 5-HT1A receptor
There is high regional density of 5-HT1A
receptors in midbrain, hippocampus, and limbic
region.
Consistent with the notion that 5-HT
neurotransmission modulates mood and anxiety.
Therefore, drugs targeting this receptor hold
interest for the treatment of mood disorders.

History
Buspirone was synthesized in 1968 in
Mead Johnsons lab.
Originally studied as antipsychotic, but
failed clinically.
However, it had a marked taming effect in
aggressive monkeys.
Anti-anxiety agent.

Pharmacological Profile
Inactive in receptor binding at
noradrenergic, cholinergic and
histaminergic sites.
Dopmine receptor binding is believed to
play no role in therapeutic or side effects.
The antianxiety properties of buspirone
appear to be its actions at both pre- and
postsynaptic 5-HT1A receptors.

Pharmacokinetics and Mechanism


of Action
Oral administration
Half-life of 3-4 hours
prolonged by food ingestion and hepatic/renal
impairment

Metabolites
5-OH-Bu, 8-OH-Bu, 1-PP(1-2-pyrimidinyl piperazine),
6-OH-Bu

1-PP has noradrenergic effects


6-OH-Bu
High affinity & partial agonist activity for the 5-HT1A R
Contributes significantly to the therapeutic effect of
buspirone

Buspirone increases plasma cortisol, prolaction


and growth hormone.

Buspirone VS benzodiazepine

Does not impair psychomotor performance


Lacks abuse potential
Shows anti-depressant like activity
Non-sedating
Spares cognitive and memory functions
But slow in action
But has serotonin syndrome

Somatic anxiety and psychic anxiety


Ongoing treatment found similar therapeutic
response.
Stopping abruptly after 6 months revealed
BZDs: Relapsed in 4 weeks (withdrawal syndrome)
Buspirone: No symptom changes

Longterm follow up at 40 months after 6 months


medication (Rickels and Schweizer 1990)
BZDs: 50% of patients still required BZDs
Buspirone: None required anxiolytics

Indications and Efficacy


FDA: Generalized Anxiety Disorder
Initial15-20mg/day
Maximum60mg/day

Nonapproved Clinical Indications

PTSD
Other anxiety disorders
Smoking cessation
Depression, adjunctive therapy usually with SSRIs
and SNRIs
May required higher dosage for MDD treatment
(90mg/day)

Side Effects and Toxicology

Dizziness(12%)
Drowsiness(10%)
Nausea(8%)
Headache(6%)
Nervousness(5%)
Fatigue(4%)
Insomnia,light-headedness,dry mouth(3%)
Excitement(2%)
No death yet. Unusually safe, except for
potential serotonin syndrome.

Conclusion
Partial agonist of the 5-HT1A receptor.
Indication: GAD (start with 15-20mg/day,
maximum 30mg/day).
Better than BZDs because of no
dependence or withdrawal effects.
However, no sedation and slower onset.

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