AZDONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AZDONE (AZDONE).
AZDONE is a selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity in the central nervous system by inhibiting the reuptake of serotonin at the presynaptic neuronal membrane.
| Metabolism | Primarily hepatic via CYP2D6 and CYP3A4; metabolites include norAZDONE and didesmethylAZDONE. |
| Excretion | Renal: 60% unchanged; fecal: 30% as metabolites; biliary: 10% as conjugates |
| Half-life | Terminal elimination half-life: 18 hours; clinically relevant for once-daily dosing |
| Protein binding | 95% bound to albumin |
| Volume of Distribution | Vd: 0.5 L/kg; indicates moderate tissue distribution |
| Bioavailability | Oral: 75% |
| Onset of Action | Oral: 30-60 minutes; IV: 5-10 minutes |
| Duration of Action | 12-24 hours; sustained due to high protein binding and slow elimination |
10 mg orally once daily
| Dosage form | TABLET |
| Renal impairment | GFR ≥60 mL/min: no adjustment; GFR 30-59 mL/min: 5 mg once daily; GFR <30 mL/min: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 5 mg once daily; Child-Pugh C: not recommended |
| Pediatric use | Not approved for patients <18 years: safety and efficacy not established |
| Geriatric use | Initiate at 5 mg once daily; titrate cautiously due to increased sensitivity and renal function decline |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AZDONE (AZDONE).
| Breastfeeding | AZDONE is excreted into human breast milk with an M/P ratio of 0.8. It is contraindicated during breastfeeding due to potential for serious adverse effects in the infant, including respiratory depression and sedation. |
| Teratogenic Risk | AZDONE is classified as FDA Pregnancy Category X. First trimester: High risk of major congenital malformations, including neural tube defects and cardiac anomalies. Second trimester: Continued risk of structural abnormalities, potential for fetal growth restriction. Third trimester: Risk of neonatal complications such as respiratory depression and withdrawal syndrome. |
■ FDA Black Box Warning
AZDONE may increase the risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders. Patients should be closely monitored for clinical worsening, suicidality, or unusual changes in behavior.
| Serious Effects |
Concomitant use with MAOIs or within 14 days of MAOI therapy; hypersensitivity to AZDONE or any excipients; concurrent use of pimozide or thioridazine.
| Precautions | Serotonin syndrome; discontinuation syndrome; activation of mania/hypomania; seizures; angle-closure glaucoma; hyponatremia; increased bleeding risk; QT prolongation. |
| Food/Dietary | Avoid high-fat meals that may delay absorption; take with a light meal or snack to reduce gastrointestinal upset. Grapefruit juice may increase serum levels of AZDONE; avoid concurrent consumption. Alcohol should be avoided due to potential hepatotoxicity and CNS depression. High-fiber foods may bind to the drug in the gut, reducing efficacy; separate intake by at least 2 hours. |
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| Fetal Monitoring | Monitor maternal vital signs, respiratory function, and level of consciousness. Assess fetal growth and well-being via serial ultrasounds and fetal heart rate monitoring. Monitor for signs of fetal distress or withdrawal after delivery. |
| Fertility Effects | AZDONE may impair female fertility by inhibiting gonadotropin release, leading to anovulation and menstrual irregularities. In males, it can reduce sperm count and motility. Effects are generally reversible upon discontinuation. |
| Clinical Pearls | Monitor renal function at baseline and periodically; adjust dose in moderate to severe renal impairment (CrCl <60 mL/min). Avoid use in patients with severe hepatic impairment (Child-Pugh C). Titrate dose gradually over 4 weeks to minimize gastrointestinal side effects. May cause somnolence; advise caution with driving or operating machinery. Administer with food to reduce dyspepsia. |
| Patient Advice | Take this medication exactly as prescribed by your doctor. Do not change your dose or stop taking without consulting your healthcare provider. · Swallow the tablet whole with a glass of water; do not crush, chew, or break it. · This drug may cause dizziness or drowsiness; avoid driving or operating heavy machinery until you know how it affects you. · It may take several weeks to feel the full effect of this medication. Do not stop taking it abruptly. · Avoid alcohol while taking this medication as it may increase the risk of liver problems or worsen side effects. · If you experience symptoms of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing), seek immediate medical attention. · Inform your doctor about all other medications, supplements, or herbal products you are taking to avoid potential interactions. · Store at room temperature away from moisture, heat, and light. Keep out of reach of children. |