gepirone

Action and Spectrum

Actions and Spectrum: 

gepirone is a partial agonist at the 5-HT1A (serotonin 1A) receptors. By binding to these receptors, gepirone increases the release and availability of serotonin, a neurotransmitter in regulating mood and anxiety.

The net effect enhances serotonergic transmission in specific brain regions, contributing to its therapeutic effects. The spectrum of activity of gepirone is primarily focused on its antidepressant and anxiolytic properties.  

Drug Interaction

Adverse Reaction

N/A 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

N/A 

Caution: 

N/A 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

gepirone primarily targets the 5-HT1A receptors, widely distributed throughout the CNS. Activation of 5-HT1A receptors modulates the release of various neurotransmitters, including serotonin, dopamine, and norepinephrine, and influences neuronal activity related to mood and anxiety regulation. 

Pharmacodynamics: 

• 5-HT1A Receptor Partial Agonism: gepirone acts as a partial agonist at the 5-HT1A receptors in the brain. By stimulating the 5-HT1A receptors, gepirone increases the release and availability of serotonin (5-HT) in specific brain regions. 
• Serotonergic Transmission Modulation: Activation of 5-HT1A receptors by gepirone modulates serotonergic transmission in the brain.  
• Enhanced Serotonin Signaling: gepirone’s partial agonist activity at the 5-HT1A receptors enhances serotonergic signaling in specific brain areas.  

Pharmacokinetics: 

Absorption 

gepirone is rapidly absorbed from the gastrointestinal tract, and peak plasma concentrations are typically reached within 2 to 4 hours following oral dosing.  

Distribution 

gepirone has moderate to high protein binding (approximately 90%) to plasma proteins, primarily to albumin. It has a relatively large volume of distribution, indicating extensive distribution into body tissues.  

Metabolism 

gepirone undergoes extensive metabolism in the liver. The primary metabolic pathway involves oxidation via the cytochrome P450 enzyme CYP3A4. The major metabolite formed is hydroxygepirone. Subsequently, hydroxygepirone undergoes further metabolism, leading to the formation of several inactive metabolites. These metabolites are primarily conjugated with glucuronic acid before being eliminated. 

Elimination and Excretion 

The elimination half-life of gepirone is relatively short, averaging around 3 to 5 hours. Most gepirone and its metabolites are excreted in the urine, primarily as glucuronide conjugates. Only a tiny portion of the drug is excreted unchanged in the urine. Renal clearance is the predominant route of elimination. 

Adminstartion

Administration: 

gepirone can be taken with or without food. However, taking it with food may help reduce stomach discomfort if a gastrointestinal upset occurs. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: gepirone 

Why do we use gepirone? 

gepirone is primarily used to treat major depressive disorder and generalized anxiety disorder.  

• Major Depressive Disorder: gepirone is prescribed as an antidepressant medication to help alleviate symptoms of major depressive disorder.  
• Generalized Anxiety Disorder (GAD): gepirone is also indicated for treating generalized anxiety disorder, characterized by excessive and uncontrollable worry and anxiety.