DESLORATADINE AND PSEUDOEPHEDRINE SULFATE 24 HOUR
Clinical safety rating: safe
MAOIs can cause hypertensive crisis Can cause insomnia and tachycardia.
Desloratadine is a long-acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity. Pseudoephedrine sulfate is an alpha-adrenergic receptor agonist causing vasoconstriction.
| Metabolism | Desloratadine is metabolized to 3-hydroxydesloratadine via CYP2C8 and CYP3A4. Pseudoephedrine is partially metabolized in the liver by N-demethylation. |
| Excretion | Desloratadine: 41% urine (metabolites), 47% feces (metabolites); pseudoephedrine sulfate: 70-90% renal (unchanged), 1% biliary. |
| Half-life | Desloratadine: 27 hours (terminal); pseudoephedrine sulfate: 5-8 hours (terminal, dependent on urine pH). |
| Protein binding | Desloratadine: 83-87% bound (primarily albumin); pseudoephedrine sulfate: minimal binding, ~20% bound. |
| Volume of Distribution | Desloratadine: ~16.8 L/kg (high Vd, extensive tissue distribution); pseudoephedrine sulfate: ~2.6-3.5 L/kg (moderate Vd). |
| Bioavailability | Desloratadine: 76% (oral); pseudoephedrine sulfate: ~100% (extended-release formulation). |
| Onset of Action | Desloratadine: 1 hour (oral); pseudoephedrine sulfate: 30-60 minutes (oral). |
| Duration of Action | Desloratadine: 24 hours (once-daily dosing); pseudoephedrine sulfate: 24 hours (extended-release formulation). |
One tablet (desloratadine 5 mg/pseudoephedrine sulfate 240 mg) orally once daily.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | Contraindicated in GFR < 30 mL/min. For GFR 30-59 mL/min: not recommended due to lack of data. For GFR ≥ 60 mL/min: no adjustment needed. |
| Liver impairment | No specific Child-Pugh based recommendations. Use with caution in severe hepatic impairment; desloratadine clearance reduced. |
| Pediatric use | Not approved for pediatric patients; safety and efficacy not established in children <12 years. For ≥12 years: same as adult. |
| Geriatric use | Use with caution due to increased sensitivity, risk of CNS effects, and potential renal impairment. Consider starting at lower doses; avoid in patients with severe renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
MAOIs can cause hypertensive crisis Can cause insomnia and tachycardia.
| FDA category | Animal |
| Breastfeeding | Desloratadine: low excretion into breast milk; M/P ratio not established. Pseudoephedrine: small amounts in milk; peak milk concentration at 2-4 hours; M/P ratio 1.7-3.5. May cause irritability or sleep disturbance in infants; reduce breast milk production. Not recommended during breastfeeding. |
| Teratogenic Risk | Desloratadine: no human data, animal studies show no evidence of harm; risk cannot be excluded. Pseudoephedrine: associated with increased risk of gastroschisis in first trimester; possible uterine vasoconstriction in second/third trimester. Overall, avoid in first trimester; use only if benefit outweighs risk in second/third trimester. |
■ FDA Black Box Warning
None.
| Common Effects | Insomnia |
| Serious Effects |
["Hypersensitivity to desloratadine, pseudoephedrine, or any component","Severe hypertension","Coronary artery disease","Use of MAO inhibitors within 14 days","Narrow-angle glaucoma","Urinary retention","Severe renal impairment (CrCl <30 mL/min)"]
| Precautions | ["Severe hypertension and/or tachycardia","Cardiovascular disease including ischemic heart disease and arrhythmias","Increased intraocular pressure","Diabetes mellitus","Thyroid dysfunction","Prostatic hypertrophy/urinary retention","Renal impairment","Seizure disorders","Use in elderly patients"] |
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| Fetal Monitoring | Monitor fetal heart rate and uterine activity with prolonged use due to potential vasoconstriction. Assess blood pressure and heart rate in mother. Fetal ultrasound if used in first trimester to detect gastroschisis. No specific monitoring for desloratadine. |
| Fertility Effects | No known effect on fertility from desloratadine. Pseudoephedrine may temporarily decrease uterine blood flow, but no evidence of lasting fertility impact. |