EVALOSE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EVALOSE (EVALOSE).

How it works

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.

What the body does with it

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

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EVALOSE (EVALOSE).

Breastfeeding

Excreted into human milk (M/P ratio 0.87); relative infant dose 4.2% of maternal weight-adjusted dose. Cases of neonatal hypotension and renal impairment reported with maternal use. Avoid breastfeeding during therapy and for 5 half-lives after last dose.

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.

Warnings & precautions

■ 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.

Side Effect Profile

Serious Effects

Absolute Contraindications

Concomitant use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing MAOI therapy, hypersensitivity to EVALOSE or any component of the formulation, concurrent use of pimozide or thioridazine.

Clinical Precautions

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.

Clinical Tips & Counseling

Drug interactions

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EVALOSE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EVALOSE (EVALOSE).

How it works

What the body does with it

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

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EVALOSE (EVALOSE).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ 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.