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Desloratadine

U.S. Brand Names: Clarinex�(r)



Generic Available: No



Canadian Brand Names: Aerius�(r)



Use: Relief of nasal and non-nasal symptoms of seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR); treatment of chronic idiopathic urticaria (CIU)



Pregnancy Risk Factor: C



Pregnancy Implications: There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed.



Lactation: Enters breast milk/not recommended



Contraindications: Hypersensitivity to desloratadine, loratadine, or any component of the formulation



Warnings/Precautions: Dose should be adjusted in patients with liver or renal impairment. Use with caution in patients known to be slow metabolizers of desloratadine (incidence of side effects may be increased). RediTabs�(r) contain phenylalanine. Safety and efficacy have not been established for children <6 months of age.



Adverse Reactions:

>10%: Central nervous system: Headache (14%)

1% to 10%:

Central nervous system: Fatigue (2% to 5%), somnolence (2%), dizziness (4%)

Endocrine & metabolic: Dysmenorrhea (2%)

Gastrointestinal: Xerostomia (3%), nausea (5%), dyspepsia (3%)

Neuromuscular & skeletal: Myalgia (2% to 3%)

Respiratory: Pharyngitis (3% to 4%)

Postmarketing and/or case reports: Anaphylaxis, bilirubin increased, dyspnea, edema, hypersensitivity reactions, liver enzymes increased, palpitation, pruritus, rash, tachycardia, urticaria



Overdosage/Toxicology: Information is limited to doses studied during clinical trials (up to 45 mg/day). Symptoms included somnolence, and small increases in heart rate and QTc interval (not clinically significant). In the event of an overdose, treatment should be symptom-directed and supportive. Desloratadine and its metabolite are not removed by hemodialysis.



Drug Interactions:

Erythromycin: Cmax and AUC of desloratadine and its metabolite are increased; however, no clinically-significant changes in the safety profile of desloratadine were observed in clinical studies.

Ketoconazole: Cmax and AUC of desloratadine and its metabolite are increased; however, no clinically-significant changes in the safety profile of desloratadine were observed in clinical studies.



Ethanol/Nutrition/Herb Interactions: Food: Does not affect bioavailability.



Stability: Syrup, tablet, orally-disintegrating tablet: Store at 25°C (77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). Protect from moisture and excessive heat (85°F). Use orally-disintegrating tablet immediately after opening blister package. Syrup should be protected from light.



Mechanism of Action: Desloratadine, a major metabolite of loratadine, is a long-acting tricyclic antihistamine with selective peripheral histamine H1 receptor antagonistic activity and additional anti-inflammatory properties.



Pharmacodynamics/Kinetics:

Protein binding: Desloratadine: 82% to 87%; 3-hydroxydesloratadine: 85% to 89%

Metabolism: Hepatic to active metabolite, 3-hydroxydesloratadine (specific enzymes not identified); undergoes glucuronidation. Decreased in slow metabolizers of desloratadine. Not expected to affect or be affected by medications metabolized by CYP with normal doses.

Half-life elimination: 27 hours

Time to peak: 3 hours

Excretion: Urine and feces (as metabolites)



Dosage: Oral:

Children:

6-11 months: 1 mg once daily

12 months to 5 years: 1.25 mg once daily

6-11 years: 2.5 mg once daily

Children

12 years and Adults: 5 mg once daily

Dosage adjustment in renal/hepatic impairment:

Children: Not established

Adults: 5 mg every other day



Administration: May be taken with or without food.

RediTabs�(r) should be placed on the tongue; tablet will disintegrate immediately. May be taken with or without water.

Syrup: A commercially-available measuring dropper or syringe calibrated to deliver 2 mL or 2.5 mL should be used to administer age-appropriate doses in children.



Dietary Considerations: May be taken with or without food. Orally-disintegrating tablets contain phenylalanine 1.75 mg/tablet.



Patient Education: Take as directed; do not exceed recommended dose. Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. You may experience headache, drowsiness, or dizziness (use caution when driving or engaging in tasks that require alertness until response to drug is known); or dry mouth, dry throat, or nausea (small, frequent meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report rapid heartbeat, shortness of breath, skin rash, persistent flu-like symptoms, or muscle aches. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.



Dental Health: Effects on Dental Treatment: Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).



Dental Health: Vasoconstrictor/Local Anesthetic Precautions: No information available to require special precautions



Mental Health: Effects on Mental Status: May cause sedation, fatigue, or dizziness



Mental Health: Effects on Psychiatric Treatment: May cause nausea; concurrent use with SSRIs, lithium, and valproic acid may be additive



Dosage Forms:

Syrup (Clarinex�(r)): 0.5 mg/mL (480 mL) [bubble gum flavor]

Tablet (Clarinex�(r)): 5 mg

Tablet, orally-disintegrating (Clarinex�(r) RediTabs�(r)): 5 mg [contains phenylalanine 1.75 mg/tablet; tutti-frutti flavor]



References:

McClellan K and Jarvis B, "Desloratadine,"Drugs, 2001, 61(6):789-96.



International Brand Names: Aerius�(r) (AT, BE, CA, CH, CO, CR, CZ, DE, DK, DO, ES, FI, FR, GT, HN, ID, IL, IT, NO, PA, PL, PT, RO, SE, SG, SI, SV, TH, YU); Aviant�(r) (EC); Azomyr�(r) (EC, IT, PT); Claramax�(r) (NZ); Desalex�(r) (CO, SG); Deslor�(r) (IN); Lestacan�(r) (CR, DO, GT, HN, PA, SV); Neoclarityn�(r) (GB, IE)




Review Date:
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