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. |
| Molecular Weight | 297.37 |
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 | Duloxetine is contraindicated in the first trimester due to risk of neural tube defects and other major malformations. |
| 2nd trimester | Use only if benefit outweighs risk; associated with increased risk of preterm birth and low birth weight. |
| 3rd trimester | Avoid in third trimester due to risk of persistent pulmonary hypertension of the newborn (PPHN) and neonatal adaptation syndrome (irritability, feeding difficulties, respiratory distress). |
Clinical note
Comprehensive clinical and safety monograph for DRIZALMA SPRINKLE (DRIZALMA SPRINKLE).
| Placental transfer | Duloxetine crosses the placenta; Cmax in umbilical cord plasma is approximately 50-70% of maternal plasma concentration. Animal studies show embryotoxicity and delayed ossification at doses similar to therapeutic doses. |
| Breastfeeding | Duloxetine is excreted into breast milk in low concentrations. The relative infant dose is ~1-2% of maternal weight-adjusted dose. Monitor infant for adverse effects such as sedation, poor feeding, and weight gain. Consider risk-benefit, especially in neonates and premature infants. |
■ 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 (monoamine oxidase inhibitors) within 14 daysUncontrolled narrow-angle glaucomaSevere renal impairment (CrCl <30 mL/min)Known hypersensitivity to duloxetine or any excipients
| 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. |
| Food/Dietary | DRIZALMA SPRINKLE may be taken with or without food. However, grapefruit or grapefruit juice should be avoided as they may increase duloxetine levels. Alcohol consumption is not recommended due to increased risk of hepatotoxicity and CNS depression. |
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| Lactation Rating | L2 (Probably Compatible) according to LactMed |
| 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. |
| 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. |
| Clinical Pearls | DRIZALMA SPRINKLE (duloxetine delayed-release capsules) is a serotonin-norepinephrine reuptake inhibitor (SNRI). Capsules can be opened and sprinkled on applesauce for patients with swallowing difficulties, but do not chew or crush the pellets. Avoid abrupt discontinuation to prevent withdrawal symptoms. Monitor blood pressure regularly as duloxetine can increase heart rate and blood pressure. Use cautiously in patients with hepatic impairment or chronic kidney disease (CrCl <30 mL/min). Contraindicated with MAOIs and within 14 days of MAOI therapy. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily with or without food. · Swallow capsules whole; if you have trouble swallowing, you may open the capsule and sprinkle the contents onto a spoonful of applesauce. Swallow immediately without chewing. · Do not crush, chew, or dissolve the pellets inside the capsule. · It may take 2-4 weeks to feel the full benefit of the medication. · Avoid drinking alcohol while taking this medication. · Do not stop taking this medication suddenly; your doctor will guide you on how to taper off gradually. · Contact your doctor if you experience new or worsening depression, suicidal thoughts, or unusual changes in mood. · Report any signs of serotonin syndrome (e.g., agitation, hallucinations, rapid heart rate, fever, muscle stiffness, loss of coordination). |