Drug Guide
Gepirone Hydrochloride
Classification
Therapeutic: Antidepressant, Anxiolytic
Pharmacological: Serotonin Receptor Modulator
FDA Approved Indications
- Generalized Anxiety Disorder (GAD)
Mechanism of Action
Gepirone is a selective partial agonist at the 5-HT1A serotonin receptors, which modulates serotonergic activity in the brain, leading to anxiolytic and antidepressant effects.
Dosage and Administration
Adult: Typically, 10 mg twice daily, titrated up based on response and tolerability. Always follow prescribing guidelines.
Pediatric: Not approved for pediatric use.
Geriatric: Start at the lower end of dosing; monitor closely due to increased sensitivity and comorbidities.
Renal Impairment: Use with caution; consider dose adjustments based on renal function.
Hepatic Impairment: Use with caution; hepatic impairment may increase plasma concentrations.
Pharmacokinetics
Absorption: Well absorbed with oral administration.
Distribution: Widely distributed; crosses the blood-brain barrier.
Metabolism: Hepatically metabolized via CYP450 enzymes; specific pathways not fully characterized.
Excretion: Primarily in urine as metabolites.
Half Life: Approximately 6-8 hours.
Contraindications
- Hypersensitivity to gepirone or related compounds
Precautions
- Use cautiously in patients with hepatic impairment, history of seizure disorders, or concurrent MAOI use. Avoid in pregnancy and lactation unless benefits outweigh risks.
Adverse Reactions - Common
- Nausea (Common)
- Dizziness (Common)
- Headache (Common)
Adverse Reactions - Serious
- Serotonin syndrome (Rare)
- Seizures (Rare)
- Hepatotoxicity (Rare)
Drug-Drug Interactions
- CYP450 inhibitors or inducers may alter gepirone levels.
- Concurrent use with other serotonergic agents may increase the risk of serotonin syndrome.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for efficacy and adverse effects, including liver function tests and signs of serotonin syndrome.
Diagnoses:
- Risk for injury related to dizziness or hypotension
Implementation: Administer as prescribed; educate patient about adherence and side effects.
Evaluation: Assess symptom improvement and adverse reactions.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report any signs of serotonin syndrome (confusion, hallucinations, seizures).
- Avoid alcohol and CNS depressants.
- Notify provider of any worsening symptoms or adverse effects.
Special Considerations
Black Box Warnings:
- Serotonin syndrome risk if combined with other serotonergic drugs.
- Potential for hepatic impairment.
Genetic Factors: No specific pharmacogenomic data available.
Lab Test Interference: May slightly alter liver function test results.
Overdose Management
Signs/Symptoms: Dizziness, nausea, vomiting, somnolence, seizures in severe cases.
Treatment: Supportive care; monitor vital signs; hemodialysis if necessary for severe overdose.
Storage and Handling
Storage: Store at room temperature, 15-30°C (59-86°F).
Stability: Stable when stored properly; check expiration date.