CLARINEX-D 12 HOUR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CLARINEX-D 12 HOUR (CLARINEX-D 12 HOUR).
Desloratadine is a long-acting tricyclic histamine antagonist selective for H1-receptor with additional anti-inflammatory properties. Pseudoephedrine is a sympathomimetic amine that acts as a vasoconstrictor via alpha-adrenergic receptors.
| Metabolism | Desloratadine: primarily metabolized by CYP3A4 and CYP2D6 to active metabolite 3-hydroxydesloratadine. Pseudoephedrine: partially metabolized in liver by N-demethylation via CYP450 enzymes; largely excreted unchanged in urine. |
| Excretion | Desloratadine: 40.2% renal (unchanged and metabolites), 41.7% fecal; pseudoephedrine: 70-90% renal (unchanged). |
| Half-life | Desloratadine: 27 hours (terminal), allows once-daily dosing; pseudoephedrine: 4-6 hours (prolonged in alkaline urine). |
| Protein binding | Desloratadine: 83-87% (mainly albumin); pseudoephedrine: negligible binding. |
| Volume of Distribution | Desloratadine: 49 L (approx. 0.7 L/kg), extensive tissue distribution; pseudoephedrine: 2.6-3.5 L/kg. |
| Bioavailability | Desloratadine: 100% (oral); pseudoephedrine: ~100% (oral). |
| Onset of Action | Desloratadine: 60 minutes (oral); pseudoephedrine: 30-60 minutes (oral). |
| Duration of Action | Desloratadine: 24 hours (symptom relief), pseudoephedrine: 4-6 hours (12-hour formulation). |
1 tablet (5 mg desloratadine / 120 mg pseudoephedrine) orally every 12 hours.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | Contraindicated in patients with GFR < 60 mL/min due to pseudoephedrine component. |
| Liver impairment | No specific Child-Pugh based adjustments for desloratadine; pseudoephedrine may require caution in severe hepatic impairment. |
| Pediatric use | Not recommended for use in pediatric patients under 12 years of age. |
| Geriatric use | Use with caution; initiate at lower doses due to increased sensitivity to pseudoephedrine and risk of anticholinergic effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CLARINEX-D 12 HOUR (CLARINEX-D 12 HOUR).
| Breastfeeding | Desloratadine: Excreted into breast milk; estimated infant dose <2% of maternal weight-adjusted dose. No known adverse effects in nursing infants. Pseudoephedrine: Excreted into breast milk; estimated infant dose ~2-7% of maternal dose; may cause irritability, sleep disturbance. M/P ratio: not reported for desloratadine; pseudoephedrine M/P ~3.0. Manufacturer recommends caution due to pseudoephedrine's effects. |
| Teratogenic Risk | Clarinox-D 12 Hour (desloratadine/pseudoephedrine) is classified as FDA Pregnancy Category C. Desloratadine: No adequate studies in pregnant women; animal studies show no teratogenicity at doses 210 times human exposure, but potential for adverse effects is unknown. Pseudoephedrine: Case reports suggest possible association with gastroschisis at first-trimester exposure; vasoconstriction may reduce uteroplacental blood flow, especially in third trimester. Avoid in first trimester if possible; use only if benefit outweighs risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to desloratadine, pseudoephedrine, or any component","Severe hypertension or coronary artery disease","Concurrent use with MAO inhibitors or within 14 days of stopping MAOI","Narrow-angle glaucoma","Urinary retention","Breastfeeding"]
| Precautions | ["Cardiovascular effects: Use with caution in patients with hypertension, arrhythmias, or ischemic heart disease.","CNS stimulation: May cause insomnia, dizziness, or nervousness.","Urinary retention: Use with caution in patients with prostatic hypertrophy or bladder neck obstruction.","Renal impairment: Reduce dose or avoid in severe renal impairment.","Hepatic impairment: Caution in severe hepatic disease."] |
Loading safety data…
| Fetal Monitoring | Monitor maternal blood pressure and heart rate due to pseudoephedrine's vasoconstrictive effects. Fetal heart rate monitoring via non-stress test may be considered in third trimester. Assess for signs of reduced placental perfusion (e.g., fetal growth restriction) if used chronically. |
| Fertility Effects | No specific human data on fertility effects. Pseudoephedrine may theoretically impair fertility via peripheral vasoconstriction affecting reproductive organs. Desloratadine animal studies showed no impairment. Effects in humans unknown. |