Buspirone is an anti-anxiety medicine that affects chemicals in the brain that may be unbalanced in people with anxiety. Originally the drug was being developed as an antipsychotic but found not to be effective for psychosis, but it had anxiolytic features that were useful. Buspirone has recently come back into favor , mostly due to its decreased side-effect profile compared to other anxiolytic treatments. BUSPIRONE
Buspirone is thought to work by decreasing the amount and actions of a chemical known as serotonin in certain parts of the brain . The delayed onset of action of buspirone suggests that the therapeutic effectiveness in generalized anxiety may involved more than its molecular mechanism of action at the 5-HT1A receptors , or buspirone may induce adaptations of 5-HT1A receptors. PHARMACODYNAMICS
Is an azaspirodecanedione ; high affinity for serotonin 5HT1A and weak affinity for serotonin 5HT2 receptors and acts as a weak antagonist on dopamine D2 receptors, but no effect on benzodiazepine GABA receptors. It enhances the activity of specific noradrenergic and dopaminergic pathways and reduces activity of serotonin and acetylcholine. MECHANISM OF ACTION
BUSPIRONE MECHANISM OF ACTION The anxiolytic action of buspirone is mainly thought to arise from the interaction at presynaptic 5-HT1A autoreceptors . Acting as a potent agonist in these receptors, buspirone initially causes activation of these autoreceptors and inhibition of 5-HT release. It is proposed that Buspirone induces desensitization of somatodendritic autoreceptors over time, which may explain the delayed onset of action of the drug. Desensitization of the autoreceptors ultimately results in heightened excitation of serotonergic neurons and enhanced 5-HT release.
Buspirone hydrochloride tablets are indicated for the short term management of anxiety disorders and the relief of the symptoms of anxiety with or without accompanying depression. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic . USES
More common dizziness nausea headache nervousness lightheadedness excitement Serious side effects Heart or cardiovascular effects . Trouble with coordination (controlling your movements) Outbursts of anger Serotonin syndrome. SIDE EFFECTS OF BUSPIRONE
Symptoms can include : fast heart rate palpitations (feeling like your heart is skipping a beat) chest pain low or high blood pressure fainting Heart or cardiovascular effects
Symptoms can include : confusion large pupils (the black centers of your eyes) fast heart rate high blood pressure fever excessive sweating rigid muscles nausea vomiting seizures Serotonin syndrome
Buspirone hydrochloride tablets are contraindicated in patients hypersensitive to buspirone hydrochloride . It is contraindicated in epilepsy. It is contraindicated in severe renal & hepatic disease. It is contraindicated in pregnancy & lactation. Contraindications
tell your doctor if you have or have ever had kidney or liver disease or a history of alcohol or drug abuse. if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking buspirone . you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you . Special precaution
Elevation of blood pressure in combination with MAO inhibitors Elevates blood digoxine levels. When taken with buspirone , rifampin can lower the amount of buspirone in your body . When taken with buspirone , dexamethasone can lower the amount of buspirone in your body . Taking certain drugs used to treat HIV with buspirone can increase the levels of buspirone in your body. Increases serum haloperidol. Drug Interaction