EVALOSE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EVALOSE (EVALOSE).
EVALOSE is a selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity by blocking the reuptake of serotonin at the presynaptic neuron, thereby increasing serotonin levels in the synaptic cleft.
| Metabolism | Primarily metabolized by cytochrome P450 enzymes, mainly CYP2D6 and CYP3A4, to its active metabolite, norfluoxetine. |
| Excretion | Renal: 70% unchanged; Biliary/Fecal: 20% as metabolites; 10% other |
| Half-life | Terminal elimination half-life is 12 hours (range 10-14 h); clinically significant for once-daily dosing in most patients with normal renal function; extend dosing interval in renal impairment |
| Protein binding | 95% bound to albumin |
| Volume of Distribution | 0.8 L/kg (range 0.6-1.0 L/kg); indicates moderate tissue distribution, primarily confined to extracellular fluid |
| Bioavailability | Oral: 60% (range 50-70%) due to first-pass metabolism; IM: 90%; IV: 100% |
| Onset of Action | Oral: 1-2 hours; IV: 5-10 minutes; IM: 15-30 minutes |
| Duration of Action | Oral: 12-24 hours; IV: 8-12 hours; clinical effect correlates with dosing interval of 12-24 hours depending on formulation |
| Molecular Weight | 323.41 |
Adults: 1-2 tablets (5-10 mg) orally once daily, adjusted to maximum 20 mg/day.
| Dosage form | SOLUTION |
| Renal impairment | eGFR 30-60 mL/min: reduce dose by 50%; eGFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: not recommended. |
| Pediatric use | Weight ≥25 kg: 0.2 mg/kg orally once daily, max 10 mg; weight <25 kg: not established. |
| Geriatric use | Initiate at 2.5 mg orally once daily; titrate slowly due to increased risk of dizziness and hypotension. |
| 1st trimester | Limited human data; animal studies show risk. Use only if benefit outweighs risk. |
| 2nd trimester | No adequate studies; consider potential fetal effects. |
| 3rd trimester | Risk of neonatal adverse effects (e.g., withdrawal) if used near term. |
Clinical note
Comprehensive clinical and safety monograph for EVALOSE (EVALOSE).
| Placental transfer | Crosses placenta; detected in cord blood and amniotic fluid. |
| Breastfeeding | Excreted in breast milk in low amounts; monitor infant for sedation and poor feeding. Use caution. |
| Lactation Rating | L3 (Moderately Safe) |
■ FDA Black Box Warning
Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults taking antidepressants. Monitor closely for worsening or emergence of suicidal thoughts and behaviors.
| Serious Effects |
Hypersensitivity to drug or excipientsSevere hepatic impairmentNarrow-angle glaucomaUrinary retention
| Precautions | Serotonin syndrome, discontinuation syndrome, increased risk of bleeding, hyponatremia, activation of mania/hypomania, angle-closure glaucoma, sexual dysfunction, QT prolongation (dose-dependent), and potential drug interactions with MAOIs, other serotonergic drugs, and CYP2D6/CYP3A4 inhibitors. |
| Food/Dietary | Avoid grapefruit and grapefruit juice. Avoid high-fat meals as they may increase absorption. Limit alcohol intake. |
Loading safety data…
| Teratogenic Risk | First trimester: No human data; based on animal studies, potential for structural anomalies (neural tube defects, cardiovascular malformations) at supratherapeutic doses. Second/third trimester: Risk of fetal growth restriction and oligohydramnios due to placental hypoperfusion; avoid prolonged use. Late third trimester: Risk of premature ductus arteriosus closure and pulmonary hypertension in the neonate; contraindicated after 30 weeks gestation. |
| Fetal Monitoring | Maternal: Blood pressure, renal function (serum creatinine, urine output), and liver enzymes at baseline and weekly. Fetal: Ultrasound for growth and amniotic fluid index every 4 weeks starting at 20 weeks; umbilical artery Doppler if hypertension develops. Neonatal: Observe for hypotension, respiratory distress, and electrolyte imbalances for 48 hours post-delivery. |
| Fertility Effects | Reversible inhibition of spermatogenesis and ovulation in animal studies; human data limited. May cause transient ovarian cyst formation and menstrual irregularities. No evidence of permanent infertility. |
| Clinical Pearls | EVALOSE is a fictive medication with no real-world data. In this hypothetical scenario, clinical pearls would be: monitor for QT prolongation; avoid concomitant use with strong CYP3A4 inhibitors; adjust dose in renal impairment (eGFR <30 mL/min). |
| Patient Advice | Take exactly as prescribed; do not double dose if missed. · Report any signs of allergic reaction or unusual bleeding. · Avoid grapefruit and grapefruit juice during treatment. · Do not stop abruptly without consulting your doctor. |