CLARINEX-D 12 HOUR desloratadine and pseudoephedrine sulfate 2.5 mg; 120 mg Tablet, Extended Release, 100-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Histamine-1 Receptor Antagonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Desloratadine is used to treat allergy symptoms: sneezing runny nose itching of the nose or throat red, itchy, or watery eyes. It is also used to treat urticaria (hives) to reduce itching and the number and size of the hives. Desloratadine is in a class of medications called antihistamines. It works by blocking histamine, a substance in the body that causes allergic symptoms.
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII LMI26O6933
Alumina is a white powder form of aluminum oxide. It's used as a filler to add bulk to tablets and capsules, and sometimes as a thickening or anti-caking agent in powdered formulations.
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UNII XF417D3PSL
Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
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UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
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UNII L06K8R7DQK
A synthetic blue dye approved by the FDA for use in medications and foods. It serves as a colorant to make pills and liquids visually distinct and easier to identify.
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UNII 3NXW29V3WO
Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII FZ989GH94E
Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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UNII O8232NY3SJ
A plant-based carbohydrate derived from corn kernels. It acts as a filler to add bulk, a binder to hold ingredients together, and a disintegrant to help the tablet break apart in your stomach for absorption.
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UNII 4ELV7Z65AP
Stearic acid is a fatty acid derived from plant or animal sources. It acts as a binder and lubricant in tablets and capsules, helping them hold together and flow smoothly during manufacturing.
11 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $6.073 | $607.28 / 100 tablets |
| Medicaid paysCMS SDUD · 12 mo | $6.04 | $604.37 / 100 tablets |
| Medicare drug plans payPart D · Q2 2026 | $6.04 | $604.38 / 100 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Clarinex-D 12 Hour 2.5 mg/1; 120 mgthis 78206-0120-01 | Organon | 100 tablets | $6.073 | — | Availability likely | — |
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⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route.
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🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 78206-0120-01 You're viewing this | 100 TABLET, EXTENDED RELEASE in 1 BOTTLE, PLASTIC (78206-120-01) | 2021-06-01 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE CLARINEX-D 12 HOUR is a combination product containing a histamine-1 (H1) receptor antagonist and an alpha adrenergic agonist indicated for: Relief of nasal and non-nasal symptoms of seasonal allergic rhinitis, including nasal congestion, in adults and adolescents 12 years of age and older. ( 1.1 )
1.1Seasonal Allergic Rhinitis CLARINEX-D ® 12 HOUR Extended Release Tablets is indicated for the relief of the nasal and non-nasal symptoms of seasonal allergic rhinitis, including nasal congestion, in adults and adolescents 12 years of age and older. CLARINEX-D 12 HOUR Extended Release Tablets should be administered when the antihistaminic properties of desloratadine and the nasal decongestant properties of pseudoephedrine are desired [see Clinical Pharmacology (12) ].
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Administer CLARINEX-D 12 HOUR Extended Release Tablet by the oral route only. Do not break, chew, or crush the tablet. Swallow the tablet whole. For oral use only ( 2 ) Adults and adolescents 12 years of age and over: The recommended dose of CLARINEX-D 12 HOUR Extended Release Tablets is one tablet twice a day. ( 2.1 )
2.1Adults and Adolescents 12 years of Age and Over The recommended dose of CLARINEX-D 12 HOUR Extended Release Tablets is 1 tablet twice a day, administered approximately 12 hours apart and with or without a meal. Higher doses or increased dosing frequency of CLARINEX-D 12 HOUR Extended Release Tablets have not demonstrated increased effectiveness. Do not exceed the recommended dose as desloratadine and pseudoephedrine, the active components of CLARINEX-D 12 HOUR Extended Release Tablets have been associated with adverse effects at higher doses [see Overdosage (10.1) and (10.2) ].
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS CLARINEX-D 12 HOUR Extended Release Tablets are oval shaped, blue and white bilayer tablets with "D12" embossed in the blue layer. Each tablet contains 2.5 mg desloratadine in the blue immediate-release layer and 120 mg of pseudoephedrine sulfate USP in the white extended-release layer. Desloratadine 2.5 mg/Pseudoephedrine sulfate 120 mg tablets. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS CLARINEX-D 12 HOUR Extended Release Tablets are contraindicated in: Patients with hypersensitivity to any of its ingredients, or to loratadine [see Warnings and Precautions (5.4) and Adverse Reactions (6.2) ] Patients with narrow-angle glaucoma Patients with urinary retention Patients receiving monoamine oxidase (MAO) inhibitor therapy or within fourteen (14) days of stopping such treatment [see Drug Interactions (7.1) ] Patients with severe hypertension or severe coronary artery disease Hypersensitivity ( 4 ) Narrow-Angle Glaucoma ( 4 ) Urinary Retention ( 4 ) Patients Receiving MAO Inhibitors or within 14 days of stopping such treatment ( 4 ) Severe hypertension or severe coronary artery disease.
( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Cardiovascular and central nervous system effects: Use with caution in patients with cardiovascular disorders. ( 5.1 ) Coexisting conditions: Use with caution in patients with increased intraocular pressure, prostatic hypertrophy, diabetes mellitus, or hyperthyroidism. ( 5.2 )
5.1Cardiovascular and Central Nervous System Effects The pseudoephedrine sulfate contained in CLARINEX-D 12 HOUR Extended Release Tablets, like other sympathomimetic amines, can produce cardiovascular and central nervous system (CNS) effects in some patients such as insomnia, dizziness, weakness, tremor, or arrhythmias. In addition, central nervous system stimulation with convulsions or cardiovascular collapse with accompanying hypotension has been reported. Therefore, CLARINEX-D 12 HOUR Extended Release Tablets should be used with caution in patients with cardiovascular disorders, and should not be used in patients with severe hypertension or severe coronary artery disease.
5.2Coexisting Conditions CLARINEX-D 12 HOUR Extended Release Tablets contain pseudoephedrine sulfate, a sympathomimetic amine, and therefore should be used with caution in patients with diabetes and hyperthyroidism. Also use with caution in patients with prostatic hypertrophy or increased intraocular pressure, as urinary retention and narrow-angle glaucoma may occur [see Contraindications (4) ].
5.3Co-Administration with Monoamine Oxidase (MAO) Inhibitors CLARINEX-D 12 HOUR Extended Release Tablets should not be used in patients receiving monoamine oxidase (MAO) inhibitor therapy or within fourteen (14) days of stopping such treatment as an increase in blood pressure or hypertensive crisis, may occur [see Contraindications (4) and Drug Interactions (7.1) ].
5.4Hypersensitivity Reactions Hypersensitivity reactions including rash, pruritus, urticaria, edema, dyspnea, and anaphylaxis have been reported after administration of desloratadine a component of CLARINEX-D 12 HOUR Extended Release Tablets. If such a reaction occurs, therapy with CLARINEX-D 12 HOUR Extended Release Tablets should be stopped and alternative treatment should be considered [see Adverse Reactions (6.2) ].
5.5Renal Impairment CLARINEX-D 12 HOUR Extended Release Tablets should generally be avoided in patients with renal impairment [see Clinical Pharmacology (12.3) ].
5.6Hepatic Impairment CLARINEX-D 12 HOUR Extended Release Tablets should generally be avoided in patients with hepatic impairment [see Clinical Pharmacology (12.3) ].
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the label: Cardiovascular and Central Nervous System effects [see Warnings and Precautions (5.1) ] Increased intraocular pressure [see Warnings and Precautions (5.2) ] Urinary retention in patients with prostatic hypertrophy [see Warnings and Precautions (5.2) ] Hypersensitivity reactions [see Warnings and Precautions (5.4) ] Severe Skin Reactions The most common adverse reactions (reported in ≥2% of patients) were insomnia, headache, mouth dry, fatigue, somnolence, pharyngitis, dizziness, nausea, and anorexia.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Organon LLC, a subsidiary of Organon & Co., at 1-844-674-3200 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The safety data described below are from 2 clinical trials with CLARINEX-D 12 HOUR Extended Release Tablets that included 1248 patients with seasonal allergic rhinitis, of which 414 patients received CLARINEX-D 12 HOUR Extended Release Tablets twice daily for up to 2 weeks.
The majority of patients were between 18 and <65 years of age with a mean age of 35.8 years and were predominantly women (64%). Patient ethnicity was 82% Caucasian, 9% Black, 6% Hispanic and 3% Asian/other ethnicity. The percentage of subjects receiving CLARINEX-D 12 HOUR Extended Release Tablets and who discontinued from the clinical trials because of an adverse event was 3.6%.
Adverse reactions that were reported by ≥2% of subjects receiving CLARINEX-D 12 HOUR Extended Release Tablets are shown in Table 1 . Table 1: Incidence of Adverse Reactions Reported by ≥2% of Subjects Receiving CLARINEX-D 12 HOUR Extended Release Tablets Adverse Reaction CLARINEX-D 12 HOUR BID (N=414) Desloratadine 5 mg QD (N=412) Pseudoephedrine 120 mg BID (N=422) Gastrointestinal Disorders Mouth Dry 8% 2% 8% Nausea 2% 1% 3% General Disorders and Administration Site Conditions Fatigue 4% 2% 2% Metabolism and Nutrition Disorders Anorexia 2% 0% 2% Nervous System Disorders Headache 8% 8% 9% Somnolence 3% 4% 2% Dizziness 3% 2% 2% Psychiatric Disorders Insomnia 10% 3% 13% Respiratory, Thoracic, and Mediastinal Disorders Pharyngitis 3% 3% 3% There were no relevant differences in adverse reactions for subgroups of patients as defined by gender, age, or race.
6.2Post-Marketing Experience In addition to the adverse reactions reported during clinical trials and listed above, adverse events have been identified during post approval use of CLARINEX-D 12 HOUR Extended Release Tablets. Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Adverse events identified from post-marketing surveillance on the use of CLARINEX-D 12 HOUR Extended Release Tablets include: Cardiac disorders: tachycardia, palpitations Respiratory, thoracic and mediastinal disorders: dyspnea Skin and subcutaneous tissue disorders: rash, pruritus In addition to these events, the following spontaneous adverse events have been reported during the marketing of desloratadine as a single ingredient product: Nervous system disorders: headache, somnolence, dizziness, psychomotor hyperactivity, movement disorders (including dystonia, tics, and extrapyramidal symptoms), seizures (reported in patients with and without a known seizure disorder) Immune system disorders: hypersensitivity reactions (such as urticaria, edema and anaphylaxis) Investigations: elevated liver enzymes including bilirubin Hepatobiliary disorders: hepatitis Metabolism and nutrition disorders: increased appetite Cases of severe skin reactions such as…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS No specific interaction studies have been conducted with CLARINEX-D 12 HOUR Extended Release Tablets. Monoamine Oxidase (MAO) Inhibitors: Do not use. May potentiate the effect of pseudoephedrine on vascular system. ( 7.1 )
7.1Monoamine Oxidase Inhibitors CLARINEX-D 12 HOUR Extended Release Tablets should not be used in patients receiving monoamine oxidase (MAO) inhibitor therapy or within fourteen (14) days of stopping such treatment because the action of pseudoephedrine a component of CLARINEX-D 12 HOUR Extended Release tablets on the vascular system may be potentiated by these agents [see Contraindications (4) and Warnings and Precautions (5.3) ].
7.2Beta-Adrenergic Blocking Agents The antihypertensive effects of beta-adrenergic blocking agents, methyldopa, and reserpine, may be reduced by sympathomimetics such as pseudoephedrine. Exercise caution when using CLARINEX-D 12 HOUR Extended Release Tablets with these agents.
7.3Digitalis Increased ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis. Exercise caution when using CLARINEX-D 12 HOUR Extended Release Tablets with these agents.
7.4Inhibitors of Cytochrome P450 3A4 In controlled clinical studies co-administration of desloratadine with ketoconazole, erythromycin, or azithromycin resulted in increased plasma concentrations of desloratadine and 3-hydroxydesloratadine but there were no clinically relevant changes in the safety profile of desloratadine [see Clinical Pharmacology (12.3) ].
7.5Fluoxetine In controlled clinical studies co-administration of desloratadine with fluoxetine, a selective serotonin reuptake inhibitor (SSRI), resulted in increased plasma concentrations of desloratadine and 3-hydroxydesloratadine but there were no clinically relevant changes in the safety profile of desloratadine [see Clinical Pharmacology (12.3) ].
7.6Cimetidine In controlled clinical studies co-administration of desloratadine with cimetidine a histamine H 2 -receptor antagonist resulted in increased plasma concentrations of desloratadine and 3-hydroxydesloratadine but there were no clinically relevant changes in the safety profile of desloratadine [see Clinical Pharmacology (12.3) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Renal impairment: Avoid in patients with renal impairment. ( 8.6 ) Hepatic impairment: Avoid in patients with hepatic impairment. ( 8.7 )
8.1Pregnancy Risk Summary The limited available data with CLARINEX-D 12 HOUR in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are no adequate and well-controlled studies of desloratadine and pseudoephedrine in combination in pregnant women. Neither are there animal reproduction studies conducted with the combination of desloratadine and pseudoephedrine or pseudoephedrine alone .
Desloratadine given during organogenesis to pregnant rats was not teratogenic at the summed area under the concentration-time curve (AUC)-based exposures of desloratadine and its metabolite approximately 320 times that at the recommended human daily oral dose (RHD) of 5 mg/day. Desloratadine given during organogenesis to pregnant rabbits was not teratogenic at the AUC-based exposures of desloratadine approximately 230 times that at the RHD. Desloratadine given to pregnant rats during organogenesis through lactation resulted in reduced body weight and slow righting reflex of F 1 pups at the summed AUC-based exposures of desloratadine and its metabolite approximately 70 times or greater than that at the RHD [see Data ].
The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Human Data Pseudoephedrine The majority of studies examining the use of pseudoephedrine in pregnancy did not find an association with an increased risk of congenital anomalies.
A few case-control studies conducted reported potential associations with isolated congenital disorders. However, several similar studies did not find statistically significant associations. Methodological limitations of these studies included small sample size, selection bias, recall bias, inadequate adjustment for risk factors, residual confounding, exposure misclassification, and lack of information regarding dose and timing of exposure.
Animal Data No animal reproduction studies were conducted with the combination of desloratadine and pseudoephedrine or pseudoephedrine alone. Desloratadine Desloratadine was given orally during organogenesis to pregnant rats at doses of 6, 24 and 48 mg/kg/day (approximately 50, 200 and 320 times the summed AUC-based exposure of desloratadine and its metabolite at the RHD). No fetal malformations were present.
Reduced fetal weights and skeletal variations noted at doses of 24 and 48 mg/kg/day were likely secondary to the maternal toxicities of reduced body weight gain and food consumption observed at the same doses. Desloratadine was also given orally during organogenesis to pregnant rabbits at doses of 15, 30 and 60 mg/kg/day (approximately 30, 70 and 230 times the AUC-based exposure of desloratadine at the RHD). No adverse effects to the fetus were noted.
Reduced maternal body weight gain was noted in rabbits at 60 mg/kg/day. In a peri- and post-natal development study, desloratadine was given to rats orally during the peri-natal (Gestation Day 6) through lactation periods (Postpartum Day 21) at doses of 3, 9 and 18 mg/kg/day. Reduced body weight and slow righting reflex were reported in F 1 pups at doses of 9 mg/kg/day or greater (approximately 70 times or greater than the summed AUC-based exposure of desloratadine and its metabolite at the RHD).
Desloratadine had no effect on F 1 pup development at 3 mg/kg/day (approximately 10 times the summed AUC-based exposure of desloratadine and its metabolite at the RHD). Maternal toxicities including reduced body weight gain and food consumption were noted at 18 mg/kg/day for F 0 dams. F 1 offspring were subsequently mated and there was no developmental toxicity for F 2…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary The limited available data with CLARINEX-D 12 HOUR in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are no adequate and well-controlled studies of desloratadine and pseudoephedrine in combination in pregnant women. Neither are there animal reproduction studies conducted with the combination of desloratadine and pseudoephedrine or pseudoephedrine alone .
Desloratadine given during organogenesis to pregnant rats was not teratogenic at the summed area under the concentration-time curve (AUC)-based exposures of desloratadine and its metabolite approximately 320 times that at the recommended human daily oral dose (RHD) of 5 mg/day. Desloratadine given during organogenesis to pregnant rabbits was not teratogenic at the AUC-based exposures of desloratadine approximately 230 times that at the RHD. Desloratadine given to pregnant rats during organogenesis through lactation resulted in reduced body weight and slow righting reflex of F 1 pups at the summed AUC-based exposures of desloratadine and its metabolite approximately 70 times or greater than that at the RHD [see Data ].
The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Human Data Pseudoephedrine The majority of studies examining the use of pseudoephedrine in pregnancy did not find an association with an increased risk of congenital anomalies.
A few case-control studies conducted reported potential associations with isolated congenital disorders. However, several similar studies did not find statistically significant associations. Methodological limitations of these studies included small sample size, selection bias, recall bias, inadequate adjustment for risk factors, residual confounding, exposure misclassification, and lack of information regarding dose and timing of exposure.
Animal Data No animal reproduction studies were conducted with the combination of desloratadine and pseudoephedrine or pseudoephedrine alone. Desloratadine Desloratadine was given orally during organogenesis to pregnant rats at doses of 6, 24 and 48 mg/kg/day (approximately 50, 200 and 320 times the summed AUC-based exposure of desloratadine and its metabolite at the RHD). No fetal malformations were present.
Reduced fetal weights and skeletal variations noted at doses of 24 and 48 mg/kg/day were likely secondary to the maternal toxicities of reduced body weight gain and food consumption observed at the same doses. Desloratadine was also given orally during organogenesis to pregnant rabbits at doses of 15, 30 and 60 mg/kg/day (approximately 30, 70 and 230 times the AUC-based exposure of desloratadine at the RHD). No adverse effects to the fetus were noted.
Reduced maternal body weight gain was noted in rabbits at 60 mg/kg/day. In a peri- and post-natal development study, desloratadine was given to rats orally during the peri-natal (Gestation Day 6) through lactation periods (Postpartum Day 21) at doses of 3, 9 and 18 mg/kg/day. Reduced body weight and slow righting reflex were reported in F 1 pups at doses of 9 mg/kg/day or greater (approximately 70 times or greater than the summed AUC-based exposure of desloratadine and its metabolite at the RHD).
Desloratadine had no effect on F 1 pup development at 3 mg/kg/day (approximately 10 times the summed AUC-based exposure of desloratadine and its metabolite at the RHD). Maternal toxicities including reduced body weight gain and food consumption were noted at 18 mg/kg/day for F 0 dams. F 1 offspring were subsequently mated and there was no developmental toxicity for F 2 pups observed.
🧒 Pediatric Use ▾
8.4Pediatric Use CLARINEX-D 12 HOUR Extended Release Tablets are not indicated for use in pediatric patients under 12 years of age.
🧓 Geriatric Use ▾
8.5Geriatric Use The number of subjects (n=10) ≥65 years old treated with CLARINEX-D 12 HOUR Extended Release Tablets was too limited to make any formal statistical comparison regarding the efficacy or safety of this drug product in this age group, or to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences between the elderly and younger patients, although the elderly are more likely to have adverse reactions to sympathomimetic amines. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy [see Clinical Pharmacology (12.3) ].
Pseudoephedrine, desloratadine, and their metabolites are known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with renal impairment. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor the patient for adverse events [see Clinical Pharmacology (12.3) ].
🆘 Overdosage ▾
10 OVERDOSAGE In the event of overdose, consider standard measures to remove any unabsorbed drug. Symptomatic and supportive treatment is recommended. Desloratadine and 3-hydroxydesloratadine are not eliminated by hemodialysis.
10.1Desloratadine Information regarding acute overdosage with desloratadine is limited to experience from post-marketing adverse event reports and from clinical trials conducted during the development of the CLARINEX product. In the reported cases of overdose, there were no significant adverse events that were attributed to desloratadine. In a dose-ranging trial, at doses of 10 mg and 20 mg/day, somnolence was reported.
In another study, no clinically relevant adverse events were reported in normal male and female volunteers who were given single daily doses of CLARINEX 45 mg for 10 days [see Clinical Pharmacology (12.2) ].
10.2Sympathomimetics In large doses, sympathomimetics such as pseudoephedrine may give rise to giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty in micturition, muscle weakness and tenseness, anxiety, restlessness, and insomnia. Many patients can present a toxic psychosis with delusions and hallucinations. Some may develop cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Desloratadine is a long acting tricyclic histamine antagonist with selective H 1 -receptor histamine antagonist activity. Receptor binding data indicate that at a concentration of 2 to 3 ng/mL (7 nanomolar), desloratadine shows significant interaction with the human histamine H 1 receptor. Desloratadine inhibited histamine release from human mast cells in vitro .
Results of a radiolabeled tissue distribution study in rats and a radioligand H 1 -receptor-binding study in guinea pigs showed that desloratadine does not readily cross the blood brain barrier. The clinical significance of this finding is unknown. Pseudoephedrine sulfate is an orally active sympathomimetic amine and exerts a decongestant action on the nasal mucosa.
Pseudoephedrine sulfate is recognized as an effective agent for the relief of nasal congestion due to allergic rhinitis. Pseudoephedrine produces peripheral effects similar to those of ephedrine and central effects similar to, but less intense than, amphetamines. It has the potential for excitatory side effects.
12.2Pharmacodynamics Wheal and Flare: Human histamine skin wheal studies following single and repeated 5 mg doses of desloratadine have shown that the drug exhibits an antihistaminic effect by 1 hour; this activity may persist for as long as 24 hours. There was no evidence of histamine-induced skin wheal tachyphylaxis within the desloratadine 5 mg group over the 28-day treatment period. The clinical relevance of histamine wheal skin testing is unknown.
Effects on QT c : In clinical trials for CLARINEX-D 12 HOUR Extended Release Tablets, ECGs were recorded at baseline and endpoint within 1 to 3 hours after the last dose. The majority of ECGs were normal at both baseline and endpoint. No clinically meaningful changes were observed following treatment with CLARINEX-D 12 HOUR Extended Release Tablets for any ECG parameter, including the QT c interval.
An increase in the ventricular rate of 7.1 and 6.4 bpm was observed in the CLARINEX-D 12 HOUR Extended Release Tablets and pseudoephedrine groups, respectively, compared to an increase of 3.2 bpm in subjects receiving desloratadine alone. Single daily doses of CLARINEX 45 mg were given to normal male and female volunteers for 10 days. All ECGs obtained in this study were manually read in a blinded fashion by a cardiologist.
In the CLARINEX-treated subjects, there was a mean increase in the maximum heart rate of 9.2 bpm relative to placebo. The QT interval was corrected for heart rate (QT c ) by both Bazett's and Fridericia methods. Using the QT c (Bazett), there was a mean increase of 8.1 msec in the CLARINEX-treated subjects relative to placebo.
Using QT c (Fridericia) there was a mean increase of 0.4 msec in CLARINEX-treated subjects relative to placebo. No clinically relevant adverse events were reported.
12.3Pharmacokinetics Absorption: In a single dose pharmacokinetic study, the mean time to maximum plasma concentrations (T max ) for desloratadine occurred at approximately 4 to 5 hours post dose and mean peak plasma concentrations (C max ) and area under the concentration-time curve (AUC) of approximately 1.09 ng/mL and 31.6 ng∙hr/mL, respectively, were observed. In another pharmacokinetic study, food and grapefruit juice had no effect on the bioavailability (C max and AUC) of desloratadine. For pseudoephedrine, the mean T max occurred at 6 to 7 hours post dose and mean peak plasma concentrations (C max ) and area under the concentration-time curve (AUC) of approximately 263 ng/mL and 4588 ng∙hr/mL, respectively, were observed.
Food had no effect on the bioavailability (C max and AUC) of pseudoephedrine. Following oral administration of CLARINEX-D 12 HOUR Extended Release Tablets twice daily for 14 days in healthy volunteers, steady-state conditions were reached on Day 10 for desloratadine, 3-hydroxydesloratadine and pseudoephedrine. For desloratadine, mean steady-state peak plasma concentrations (C…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Desloratadine is a long acting tricyclic histamine antagonist with selective H 1 -receptor histamine antagonist activity. Receptor binding data indicate that at a concentration of 2 to 3 ng/mL (7 nanomolar), desloratadine shows significant interaction with the human histamine H 1 receptor. Desloratadine inhibited histamine release from human mast cells in vitro .
Results of a radiolabeled tissue distribution study in rats and a radioligand H 1 -receptor-binding study in guinea pigs showed that desloratadine does not readily cross the blood brain barrier. The clinical significance of this finding is unknown. Pseudoephedrine sulfate is an orally active sympathomimetic amine and exerts a decongestant action on the nasal mucosa.
Pseudoephedrine sulfate is recognized as an effective agent for the relief of nasal congestion due to allergic rhinitis. Pseudoephedrine produces peripheral effects similar to those of ephedrine and central effects similar to, but less intense than, amphetamines. It has the potential for excitatory side effects.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING CLARINEX-D 12 HOUR Extended Release Tablets are oval-shaped, blue and white bilayer tablets with "D12" embossed in the blue layer, containing 2.5 mg desloratadine in the blue immediate-release layer and 120 mg of pseudoephedrine sulfate USP in the white extended-release layer. CLARINEX-D 12 HOUR Extended Release Tablets are supplied in high-density polyethylene bottles of 100 (NDC 78206-120-01). Storage: Store at 25°C (77°F); excursions permitted to 15°–30°C (59°–86°F) [see USP Controlled Room Temperature].
Avoid exposure at or above 30°C (86°F). Protect from excessive moisture. Protect from light.
📦 Storage and Handling ▾
Storage: Store at 25°C (77°F); excursions permitted to 15°–30°C (59°–86°F) [see USP Controlled Room Temperature]. Avoid exposure at or above 30°C (86°F). Protect from excessive moisture. Protect from light.
📋 Description ▾
11 DESCRIPTION CLARINEX-D 12 HOUR Extended Release Tablets are oval-shaped blue and white bilayer tablets containing 2.5 mg desloratadine in the blue immediate-release layer and 120 mg of pseudoephedrine sulfate USP in the white extended-release layer which is released slowly, allowing for twice-daily administration. The inactive ingredients contained in CLARINEX-D 12 HOUR Extended Release Tablets are hypromellose USP, microcrystalline cellulose NF, povidone USP, silicon dioxide NF, magnesium stearate NF, corn starch NF, edetate disodium USP, citric acid anhydrous USP, stearic acid NF, and FD&C Blue No.
2 aluminum lake dye. Desloratadine, 1 of the 2 active ingredients of CLARINEX-D 12 HOUR Extended Release Tablets, is a white to off-white powder that is slightly soluble in water, but very soluble in ethanol and propylene glycol. It has an empirical formula: C 19 H 19 ClN 2 and a molecular weight of 310.8.
The chemical name is 8-chloro-6,11-dihydro-11-(4-piperdinylidene)-5 H -benzo[5,6] cyclohepta [1,2- b ]pyridine and has the following structure: Pseudoephedrine sulfate, the other active ingredient of CLARINEX-D 12 HOUR Extended Release Tablets, is the synthetic salt of one of the naturally occurring dextrorotatory diastereomers of ephedrine and is classified as an indirect sympathomimetic amine. Pseudoephedrine sulfate is a colorless hygroscopic crystal or white, hygroscopic crystalline powder, practically odorless, with a bitter taste.
It is very soluble in water, freely soluble in alcohol, and sparingly soluble in ether. The empirical formula for pseudoephedrine sulfate is (C 10 H 15 NO) 2 • H 2 SO 4 ; the chemical name is benzenemethanol, α-[1-(methylamino) ethyl]-,[ S -( R *, R *)]-, sulfate (2:1)(salt); and the chemical structure is: Chemical Structure Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling ( Patient Information ).
17.1Cardiovascular and Central Nervous System Effects Patients should be informed that pseudoephedrine, one of the active ingredients in CLARINEX-D 12 HOUR Extended Release Tablets may cause cardiovascular or central nervous system effects such as insomnia, dizziness, tremor, convulsions or arrhythmia.
17.2Dosing Patients should be advised not to increase the dose or dosing frequency of CLARINEX-D 12 HOUR Extended Release Tablets.
17.3Additional Antihistamines and/or Decongestants Patients should be advised against the concurrent use of CLARINEX-D 12 HOUR Extended Release Tablets with other antihistamines and/or decongestants.
17.4Monoamine Oxidase (MAO) Inhibitors Patients should be informed that due to its pseudoephedrine component, they should not use CLARINEX-D 12 HOUR with a monoamine oxidase (MAO) inhibitor or within 14 days of stopping use of an MAO inhibitor.
17.5Coexisting Conditions Patients with severe hypertension or severe coronary artery disease, narrow-angle glaucoma, or urinary retention should be advised not to use CLARINEX-D 12 HOUR Extended Release Tablets.
17.6Instructions for Use Patients should be instructed not to break, crush, or chew the tablet; the tablet should be swallowed whole, and can be taken without regard to meals.