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Pronunciation

Generic Name: Desloratadine
Class: Second Generation Antihistamines
ATC Class: R06AX27
VA Class: AH109
Chemical Name: 8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Molecular Formula: C19H19ClN2
CAS Number: 100643-71-8

Introduction

Second generation antihistamine; active descarboethoxy metabolite of loratadine.1 2 3 9

Uses for Clarinex

Allergic Rhinitis

Symptomatic relief of nasal and nonnasal symptoms of perennial allergic rhinitis.1

Symptomatic relief (alone or in fixed combination with pseudoephedrine sulfate) of nasal and nonnasal symptoms of seasonal (e.g., hay fever) allergic rhinitis.1 9 18 19 Use fixed-combination preparation only when both antihistamine and nasal decongestant activity are desired.18

Slideshow: 2014 Update: First Time Brand-to-Generic Switches

Improves nasal and nonnasal symptoms in patients with seasonal allergic rhinitis and concomitant mild to moderate asthma without impairing pulmonary function.1 2 6 9

Chronic Idiopathic Urticaria

Symptomatic treatment of pruritus and urticaria associated with chronic idiopathic urticaria.1

Clarinex Dosage and Administration

Administration

Oral Administration

Administer conventional tablets, oral solution, orally disintegrating tablets, and fixed-combination extended-release tablets orally once daily without regard to meals.1 9 18

Orally disintegrating tablets: Remove tablet from blister just prior to administration.1 Place tablet on the tongue, allow it to disintegrate, then swallow with or without water.1

Oral solution: To measure and administer dose, use a dropper or syringe calibrated to deliver 2 or 2.5 mL.1

Fixed-combination desloratadine/pseudoephedrine sulfate extended-release tablets: Swallow whole; do not chew, break, or crush.18

Dosage

Fixed-combination preparation contains 5 mg of desloratadine in an immediate-release outer shell and 240 mg of pseudoephedrine sulfate in an extended-release matrix core that slowly releases the drug.18

Pediatric Patients

Allergic Rhinitis
Seasonal
Oral

Children 2–5 years of age: 1.25 mg once daily (as oral solution).1

Children 6–11 years of age: 2.5 mg once daily (as oral solution or orally disintegrating tablets).1

Children ≥12 years of age: 5 mg once daily (as conventional tablets, oral solution, orally disintegrating tablets, or fixed-combination extended-release tablets with 240 mg pseudoephedrine sulfate).1 18

Perennial
Oral

Children 6–11 months of age: 1 mg once daily (as oral solution).1

Children 1–5 years of age: 1.25 mg once daily (as oral solution).1

Children 6–11 years of age: 2.5 mg once daily (as oral solution or orally disintegrating tablets).1

Children ≥12 years of age: 5 mg once daily (as conventional tablets, oral solution, or orally disintegrating tablets).1

Chronic Idiopathic Urticaria
Oral

Children 6–11 months of age: 1 mg once daily (as oral solution).1

Children 1–5 years of age: 1.25 mg once daily (as oral solution).1

Children 6–11 years of age: 2.5 mg once daily (as oral solution or orally disintegrating tablets).1

Children ≥12 years of age: 5 mg once daily (as conventional tablets, oral solution, or orally disintegrating tablets).1

Adults

Allergic Rhinitis
Seasonal
Oral

5 mg once daily (as conventional tablets, oral solution, orally disintegrating tablets, or fixed-combination extended-release tablets with pseudoephedrine sulfate).1 18

Perennial
Oral

5 mg once daily (as conventional tablets, oral solution, or orally disintegrating tablets).1

Chronic Idiopathic Urticaria
Oral

5 mg once daily (as conventional tablets, oral solution, or orally disintegrating tablets).1 9

Prescribing Limits

Pediatric Patients

Allergic Rhinitis
Oral

Children ≥12 years of age: Dosages >5 mg provide no additional benefit but may increase risk of adverse effects (e.g., somnolence).1 9

Adults

Allergic Rhinitis
Oral

Dosages >5 mg provide no additional benefit but may increase risk of adverse effects (e.g., somnolence).1 9

Special Populations

Dosage adjustment based on gender, race, or age generally not necessary.1 3

Hepatic Impairment

Pediatric patients: No specific dosage recommendations at this time because of lack of data.1

Adults: 5 mg every other day (as conventional tablets, oral solution, or orally disintegrating tablets).1 Avoid fixed-combination preparation.18

Renal Impairment

Pediatric patients: No specific dosage recommendations at this time because of lack of data.1

Adults: 5 mg every other day (as conventional tablets, oral solution, orally disintegrating tablets, or fixed-combination tablets).1 18

Cautions for Clarinex

Contraindications

  • Known hypersensitivity to desloratadine, loratadine, or any ingredient in the formulation.1

Warnings/Precautions

General Precautions

Shares the toxic potentials of loratadine and other second generation antihistamines; observe usual precautions related to therapy with such drugs.1

Use of Fixed Combination

When using fixed-combination preparation containing pseudoephedrine sulfate, consider the cautions, precautions, and contraindications associated with pseudoephedrine.18

Phenylketonuria

Clarinex RediTabs contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 1.4 or 2.9 mg of phenylalanine per 2.5- or 5-mg tablet, respectively.1

Specific Populations

Pregnancy

Category C.1

Lactation

Distributed into milk.1 18 Discontinue nursing or the drug.1 18 Caution if fixed-combination preparation is used in nursing women.18

Pediatric Use

Safety and efficacy not established for seasonal allergic rhinitis in children <2 years of age.1

Safety and efficacy not established for perennial allergic rhinitis or chronic idiopathic urticaria in children <6 months of age.1

Safety and efficacy of fixed combination for seasonal allergic rhinitis not established in children <12 years of age.18

Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection.22 23 Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1 18 Select dosage with caution.1 18 (See Elimination: Special Populations, under Pharmacokinetics.)

Hepatic Impairment

Conventional tablets, oral solution, or orally disintegrating tablets: Dosage reduction recommended.1 (See Hepatic Impairment under Dosage and Administration and also see Elimination: Special Populations, under Pharmacokinetics.)

Fixed-combination desloratadine/pseudoephedrine sulfate preparation: Use not recommended.18

Renal Impairment

Conventional tablets, oral solution, or orally disintegrating tablets: Dosage reduction recommended.1 (See Renal Impairment under Dosage and Administration and also see Absorption: Special Populations, under Pharmacokinetics.)

Fixed-combination desloratadine/pseudoephedrine sulfate preparation: Dosage reduction recommended.18 (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

Children 6–11 months of age receiving oral solution: Upper respiratory tract infection, diarrhea, fever, irritability, coughing, somnolence, bronchitis, otitis media, vomiting.1

Children 12–23 months of age receiving oral solution: Fever, diarrhea, upper respiratory tract infection, coughing.1

Children 2–5 years of age receiving oral solution: Fever.1

Adults and children ≥12 years of age receiving conventional or orally disintegrating tablets for management of allergic rhinitis: Pharyngitis,1 3 4 9 dry mouth.1 3 4 9

Adults and children ≥12 years of age receiving conventional or orally disintegrating tablets for management of chronic idiopathic urticaria: Headache,1 7 9 nausea,1 fatigue.1 7

Fixed-combination desloratadine/pseudoephedrine sulfate preparation: Dry mouth, headache, insomnia.18

Interactions for Clarinex

No formal drug interaction studies conducted with fixed-combination desloratadine/pseudoephedrine sulfate preparation.18 When using this preparation, consider drug interactions associated with pseudoephedrine (e.g., MAO inhibitors).18

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (increased plasma concentrations of desloratadine and active metabolite) with drugs affecting hepatic microsomal enzymes.1 9 (See Specific Drugs and Foods under Interactions.)

Specific Drugs and Foods

Drug or Food

Interaction

Azithromycin

Increased plasma concentrations of desloratadine and active metabolite;1 9 no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects1 9

Cimetidine

Increased plasma concentrations of desloratadine and active metabolite;1 9 no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects1 9

Erythromycin

Increased plasma concentrations of desloratadine and active metabolite;1 9 no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects1 9

Fluoxetine

Increased plasma concentrations of desloratadine and active metabolite;1 9 no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects1 9

Grapefruit juice

Pharmacokinetic interaction unlikely1 3

Ketoconazole

Increased plasma concentrations of desloratadine and active metabolite;1 9 no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects1 9

Clarinex Pharmacokinetics

Absorption

Bioavailability

Conventional tablets and oral solution are bioequivalent.1 Reformulated orally disintegrating tablets are bioequivalent to the original orally disintegrating formulation (no longer commercially available);1 original formulation previously shown to be bioequivalent to conventional tablets and oral solution.20

Peak plasma concentrations occur at approximately 3 or 6–7 hours following administration of conventional tablets or fixed-combination extended-release preparation, respectively.1 18

Onset

Following single- and multiple-dose administration, antihistaminic effects occur within 1 hour.1 Symptomatic (nasal and nonnasal) improvement observed as early as 1 day after initiation of therapy.2 4 5 6 9

Duration

Following single- and multiple-dose administration, antihistaminic effects persist for up to 24 hours.1 No evidence of histamine-induced skin wheal tachyphylaxis over 28-day treatment period.1

Food

Food or grapefruit juice does not appear to affect bioavailability following administration as conventional tablets, oral solution,1 or fixed-combination tablets;18 water does not appear to affect bioavailability following administration as orally disintegrating tablets.1

Special Populations

In patients with renal impairment and those who require hemodialysis, peak plasma desloratadine concentrations and AUC are increased.1

Distribution

Plasma Protein Binding

Approximately 82–87% (for desloratadine) and 85–89% (for 3-hydroxydesloratadine).1

Special Populations

Protein binding not altered in patients with renal impairment.1

Elimination

Metabolism

Extensively metabolized to 3-hydroxydesloratadine (active metabolite), which subsequently undergoes glucuronidation; enzyme(s) responsible for metabolism of desloratadine not identified.1

Elimination Route

Approximately 87% excreted as metabolic products in urine and feces in equal proportions.1

Desloratadine and 3-hydroxydesloratadine are poorly removed by hemodialysis.1

Half-life

27 hours for desloratadine and 3-hydroxydesloratadine.1

Special Populations

Approximately 6% of patients are poor metabolizers (decreased ability to form 3-hydroxydesloratadine); higher frequency of poor metabolizers in blacks (17%) than in Caucasians (2%) or Hispanics (2%).1 18 Substantially (approximately 6-fold) greater drug exposure in poor metabolizers than in normal metabolizers;1 however, no overall differences in safety observed between these groups.1 18 Nevertheless, an increased risk of adverse effects in poor metabolizers cannot be ruled out.1 18

In patients ≥65 years of age, plasma desloratadine concentrations are increased and elimination half-life is prolonged.1

In patients with hepatic impairment, AUC and elimination half-life are increased and clearance is decreased.1

Stability

Storage

Oral

Tablets and Orally Disintegrating Tablets

25°C (may be exposed to 15–30°C).1

Solution

25°C (may be exposed to 15–30°C).1 Protect from light.1

Fixed-combination Tablets

25°C (may be exposed to 15–30°C).18 Protect from excessive moisture.18

Actions

  • Specific, selective peripheral H1-receptor antagonist;1 2 3 4 6 9 relatively “nonsedating” or second generation antihistamine.2 5 6 7 9

  • May suppress release of histamine from human mast cells.1 9

  • May reduce nasal congestion/stuffiness.2 3 5 9

Advice to Patients

  • Importance of adhering to prescribed dosage regimen and directions for use; increase in dosage or dosing frequency not recommended since higher dosages provide no additional benefit but may increase risk of adverse effects (e.g., somnolence).1

  • Importance of informing patients with phenylketonuria that orally disintegrating tablets contain aspartame.1

  • Importance of avoiding concomitant use of fixed-combination preparation with OTC antihistamines and/or decongestants.18

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1

  • Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Desloratadine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Solution

0.5 mg/mL

Clarinex Syrup

Schering

Tablets, film-coated

5 mg

Clarinex

Schering

Tablets, orally disintegrating

2.5 mg

Clarinex RediTabs

Schering

5 mg

Clarinex RediTabs

Schering

Desloratadine Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, extended-release core (pseudoephedrine sulfate only)

5 mg with Pseudoephedrine Sulfate 240 mg

Clarinex-D 24-Hour

Schering

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Clarinex 0.5MG/ML Syrup (SCHERING): 473/$238.58 or 1419/$683.68

Clarinex 5MG Tablets (SCHERING): 30/$152.99 or 90/$435.96

Clarinex Reditabs 2.5MG Dispersible Tablets (SCHERING): 30/$164.99 or 90/$486.99

Clarinex Reditabs 5MG Dispersible Tablets (SCHERING): 30/$162.99 or 90/$470.00

Clarinex-D 12 Hour 2.5-120MG 12-hr Tablets (SCHERING): 100/$340.99 or 300/$965.96

Clarinex-D 24 Hour 5-240MG 24-hr Tablets (SCHERING): 30/$161.98 or 90/$472.98

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions November 1, 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Schering Corporation. Clarinex (desloratadine) tablets, syrup, RediTabs tablets prescribing information. Kenilworth, NJ; 2005 Apr.

2. McClellan K and Jarvis B. Desloratadine. Drugs. 2001; 61:789-96. [PubMed 11398910]

3. Agrawal DK. Pharmacology and clinical efficacy of desloratadine as an anti-allergic and anti-inflammatory drug. Expert Opin Investig Drugs. 2001; 10:547-60. [PubMed 11424898]

4. Meltzer EO, Prenner BM, Nayak A for the Desloratadine Study Group. Efficacy and tolerability of once-daily 5 mg desloratadine, an H1-receptor antagonist, in patients with seasonal allergic rhinitis assessment during the spring and fall allergy seasons. Clin Drug Invest. 2001; 21:25-32.

5. Nayak AS and Schenkel E. Desloratadine reduces nasal congestion in patients with intermittent allergic rhinitis. Allergy. 2001; 56:1077-80. [PubMed 11703222]

6. Baena-Cagnani CE. Desloratadine activity in concurrent seasonal allergic rhinitis and asthma. Allergy. 2001; 56(Suppl):21-7. [PubMed 11243501]

7. Ring J, Hein R, Gauger A et al. Once-daily desloratadine improves the signs and symptoms of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study. Int J Dermatol. 2001; 40:1-5. [PubMed 11277944]

8. Gupta S, Banfield C, Kantesaria B et al. Pharmacokinetic and safety profile of desloratadine and fexofenadine when coadministered with azithromycin: a randomized, placebo-controlled, parallel-group study. Clin Ther. 2001; 23:451-66. [IDIS 465266] [PubMed 11318079]

9. Schering, Kenilworth, NJ: Personal communication.

10. Borge PA. Problems in allergic rhinitis. Arzneimittelforschung. 1982; 32:1199-201. [PubMed 6891258]

11. Anon. Treatment of seasonal and perennial rhinitis. BMJ. 1981; 283:808-10. [PubMed 6117350]

12. Food and Drug Administration. Over-the-counter drugs: establishment of a monograph for OTC cold, cough, allergy, bronchodilator and antiasthmatic products. [21 CFR 341] Fed Regist. 1976; 41:38312-424. (IDIS 66640)

13. Douglas WW. Histamine and 5-hydroxytryptamine (serotonin) and their antagonists. In: Gilman AG, Goodman LS, Rall TW et al, eds. Goodman and Gilman’s the pharmacologic basis of therapeutics. 7th ed. New York: Macmillan Publishing Company; 1985:605-38.

14. Cirillo VJ, Tempero KF. The pharmacology and therapeutic use of H1 and H2 antihistamines. In: Miller RR, Greenblatt DJ, eds. Drug therapy reviews. Vol 2. New York: Elsevier/North Holland Inc; 1979:24-47.

15. Church JA. Allergic rhinitis: diagnosis and management. Clin Pediatr (Philadelphia). 1980; 19:655-9.

16. AMA Division of Drugs. AMA drug evaluations. 5th ed. Chicago: American Medical Association; 1983:1465-79.

17. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; tentative final monograph for OTC antihistamine drug products. [21 FR Part 341] Fed Regist. 1985; 50:2200-18. (IDIS 195256)

18. Schering Corporation. Clarinex-D 24-Hour (desloratadine 5 mg and pseudoephedrine sulfate) extended-release tablets prescribing information. Kenilworth, NJ; 2005 Mar.

19. Pleskow W, Grubbe R, Weiss S, Lutsky B. Efficacy and safety of an extended-release formulation of desloratadine and pseudoephedrine vs the individual components in the treatment of seasonal allergic rhinitis. Ann Allergy Asthma Immunol. 2005; 94:348-54. [PubMed 15801245]

20. Schering Corporation. Clarinex (desloratadine) tablets, syrup, RediTabs tablets prescribing information. Kenilworth, NJ; 2004 Aug.

21. Schering-Plough. FDA approves re-formulated Clarinex (desloratadine) RediTabs tablets—orally disintegrating prescription antihistamine. Kenilworth, NJ: 2005 Jul 15. Press release. From website.

22. Srinivasan A, Budnitz D, Shehab N et al. Infant deaths associated with cough and cold medications—two states, 2005. MMWR Morb Mortal Wkly Rep. 2007; 56:1-4. [PubMed 17218934]

23. Food and Drug Administration. Cough and cold medications in children less than two years of age. Rockville, MD; 2007 Jan 12. From FDA website.

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