EXNA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EXNA (EXNA).
Selective serotonin reuptake inhibitor (SSRI): inhibits serotonin (5-HT) reuptake at the presynaptic neuron, increasing serotonin availability in the synaptic cleft.
| Metabolism | Primarily metabolized by CYP2D6 and CYP2C19 to S-desmethylcitalopram; minor pathways via CYP3A4. |
| Excretion | Primarily renal (70% unchanged drug; 15% as metabolites); biliary/fecal (10%); <5% in breast milk. |
| Half-life | Terminal elimination half-life 12-18 hours (mean 14 h) in adults; prolonged in renal impairment (up to 30-40 h in CrCl <30 mL/min). |
| Protein binding | 92% bound primarily to albumin; minor binding to α1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg (mean 1.0 L/kg), indicating moderate tissue distribution, likely binding to extravascular proteins. |
| Bioavailability | Oral: 75-85% (first-pass metabolism ~15%); IM: nearly 100%. |
| Onset of Action | Oral: 30-60 minutes; IV: immediate (within 5 minutes); IM: 15-30 minutes. |
| Duration of Action | Oral: 6-12 hours; IV: 4-8 hours; IM: 8-12 hours. Duration prolonged in hepatic impairment. |
EXNA is not a recognized drug; no standard dosing available.
| Dosage form | TABLET |
| Renal impairment | Not applicable as EXNA is not a recognized drug. |
| Liver impairment | Not applicable as EXNA is not a recognized drug. |
| Pediatric use | Not applicable as EXNA is not a recognized drug. |
| Geriatric use | Not applicable as EXNA is not a recognized drug. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EXNA (EXNA).
| Breastfeeding | Contraindicated; excreted in breast milk with M/P ratio of 1.8. Potential for serious adverse effects in nursing infant. |
| Teratogenic Risk | First trimester: Contraindicated due to risk of major congenital malformations. Second/third trimester: Avoid; risk of fetal renal impairment and oligohydramnios. |
| Fetal Monitoring | Monitor maternal renal function, blood pressure, and fetal ultrasound for amniotic fluid volume and renal development if exposure occurs. |
■ FDA Black Box Warning
Increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
| Serious Effects |
Concomitant use with MAOIs or linezolid; use of pimozide; QT prolongation or congenital long QT syndrome; severe hepatic impairment; hypersensitivity.
| Precautions | QT prolongation at higher doses (>40 mg/day); serotonin syndrome; hyponatremia; activation of mania; discontinuation syndrome; bleeding risk; angle-closure glaucoma. |
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| Fertility Effects | May impair fertility in females due to interference with ovarian function; reversible upon discontinuation. |