DRIZALMA SPRINKLE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DRIZALMA SPRINKLE (DRIZALMA SPRINKLE).
Selective serotonin reuptake inhibition, resulting in increased synaptic serotonin concentrations and enhanced serotonergic neurotransmission.
| Metabolism | Primarily via CYP2D6 and CYP2C19; also involves CYP3A4 and CYP2C9. Active metabolite N-desmethylcitalopram with half-life ~66 hours. |
| Excretion | Primarily renal (approx. 70% as unchanged drug and metabolites); 30% fecal/biliary. |
| Half-life | 12-15 hours; steady-state achieved in 2-3 days; no significant accumulation with q12h dosing. |
| Protein binding | >99% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.2-0.3 L/kg (indicates minimal extravascular distribution). |
| Bioavailability | Oral: 90-95% (duloxetine hydrochloride; sprinkle formulation bioequivalent to capsules). |
| Onset of Action | Oral: 1-2 hours (peak plasma concentration at 4-6 hours). |
| Duration of Action | Approximately 12 hours (supports twice-daily dosing); clinical effect persists for dosing interval. |
60 mg orally once daily, with or without food. Capsules may be swallowed whole or opened and sprinkled onto applesauce.
| Dosage form | CAPSULE, DELAYED REL PELLETS |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min). Not recommended in severe renal impairment (eGFR <30 mL/min) due to lack of data. |
| Liver impairment | No dosage adjustment required for mild hepatic impairment (Child-Pugh A). Not recommended in moderate to severe hepatic impairment (Child-Pugh B or C). |
| Pediatric use | Not approved for use in pediatric patients (safety and efficacy not established). |
| Geriatric use | No specific dosage adjustment recommended. Use with caution due to increased risk of adverse effects; monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DRIZALMA SPRINKLE (DRIZALMA SPRINKLE).
| Breastfeeding | Duloxetine is excreted into human milk; the infant dose is estimated at 0.1-0.2% of maternal weight-adjusted dose. M/P ratio is not established. Cases of adverse effects (e.g., irritability, poor feeding) have been reported. Caution is advised; consider breastfeeding only if essential and monitor infant for sedation, weight gain, and feeding behavior. |
| Teratogenic Risk | Drizalma Sprinkle (duloxetine) is classified as Pregnancy Category C. In animal studies, duloxetine caused fetal harm at doses greater than maternal exposure. There are no adequate and well-controlled studies in pregnant women. First trimester: Risk of major congenital malformations is not significantly increased based on limited human data, but animal data suggest risk. Second and third trimesters: Late pregnancy use may cause persistent pulmonary hypertension of the newborn (PPHN) and neonatal adaptation syndrome (irritability, feeding difficulties, respiratory distress). Avoid use unless benefit clearly outweighs risk. |
■ FDA Black Box Warning
Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults in short-term studies. Monitor closely for clinical worsening, suicidality, or unusual changes in behavior.
| Serious Effects |
Concomitant use with MAOIs or within 14 days of MAOI discontinuation, concomitant use with pimozide, known hypersensitivity to citalopram or any excipients, and QT interval prolongation (congenital or acquired).
| Precautions | Serotonin syndrome, QT prolongation, hyponatremia, activation of mania/hypomania, seizures, angle-closure glaucoma, bleeding risk (especially with NSAIDs/aspirin), discontinuation syndrome, and sexual dysfunction. |
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| Fetal Monitoring | Monitor maternal blood pressure and heart rate due to duloxetine effects on norepinephrine. For fetus: ultrasound for growth and amniotic fluid volume if used in second/third trimester. Monitor neonate for signs of poor adaptation, including respiratory distress, feeding difficulty, jitteriness, and convulsions. Assess for persistent pulmonary hypertension. |
| Fertility Effects | In animal studies, duloxetine did not impair male or female fertility at exposures up to 7 times the maximum recommended human dose. Human data are lacking; theoretical risk due to serotonin/norepinephrine modulation on hypothalamic-pituitary-gonadal axis may affect ovulation or sperm function, but no conclusive evidence. |