Buspirone
Buspirone
is non-benzodiazepine anxiolytic which is the most selective anxiolytic
currently
Mechanism of Action
-anxiety
associated with altered serotonin transporters
-partial
agonist at 5-HT 1A receptor presynaptic
-inhibit
serotoin release
-dose
not involve GABA receptors
-delayed
onset (~ 1-2 week)
-pregnancy
category: B
-oral
administration
Advantages
-lack
CNS depressant effect
-no
sedation
-no
impairment of performance
-no
tolerance or withdrawal
-no
cross-tolerance with BDZ
-no
abuse/addiction potential
-minimal
effect on psychomotor functions
Binding
of a partial agonist to the 5-HT1A receptor causes the dissociation of
inhibitory G-proteins. The G-protein alpha sub-unit binds to and inhibits
adenylate cyclase. This prevents the conversion of ATP to cAMP and the
initiation of other secondary messenger signaling mechanisms, hence cell
depolarisation is inhibited.
Pharmacokinetics
-rapidly
absorbed and undergo extensive first pass metabolism
-oxidised
by CYP3A4 to active metabolite
-excretion
through urine (30-60%) and feces (20-40%)
-t1/2
2-11 hours
Side effects
-dizziness,
drowsiness, headache, nervousness
-tachycardia/
palpitations
-parethesia
-GI
distress, N/D
-pupillary
constrition (dose-dependent)
Drug-drug
interactions
+fluoxetine
= reduce buspirone effect
+haloperidol
= increase p [haloperidol]
+CYP3A4
inducer (carbamazepine, barbiturates, phenyton) = reduce p [buspirone]
+CYP3A4
inhibitor (erythromycin, azole, protease, inh) = increase p [buspirone]
+MAOIs
= risk of elevated BP
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