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Pronunciation
(des lor AT a deen)
Generic Available (U.S.)
No
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
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 Considerations
Adverse events have been observed in animal reproduction studies; therefore, the manufacturer classifies desloratadine as pregnancy category C. The use of antihistamines for the treatment of rhinitis during pregnancy is generally considered to be safe at recommended doses. Information related to the use of desloratadine during pregnancy is limited; therefore, other agents may be preferred. Desloratadine is the primary metabolite of loratadine; refer to the Loratadine monograph for additional information.
Lactation
Enters breast milk/not recommended
Breast-Feeding Considerations
Desloratadine is excreted into breast milk. According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother.
Contraindications
Hypersensitivity to desloratadine, loratadine, or any component of the formulation
Warnings/Precautions
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment needed.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment needed.
Special populations:
• Pediatrics: Safety and efficacy have not been established for children <6 months of age.
• Slow metabolizers: Use with caution in patients known to be slow metabolizers of desloratadine (incidence of side effects may be increased).
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
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, hepatitis, hypersensitivity reactions, palpitation, pruritus, psychomotor hyperactivity, rash, seizure, tachycardia, transaminases increased, urticaria
Metabolism/Transport Effects
Substrate of P-glycoprotein
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Food: Does not affect bioavailability.
Storage
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
Onset of action: Within 1 hour
Duration: 24 hours
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: Oral
May be taken with or without food.
RediTabs® 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.
Test Interactions
May suppress the wheal and flare reactions to skin test antigens
Dietary Considerations
May be taken with or without food. Some products may contain phenylalanine.
Patient Education
Avoid use of alcohol. You may experience headache, drowsiness, dizziness, dry mouth, dry throat, or nausea. Report rapid heartbeat, shortness of breath, or skin rash.
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
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Syrup, oral:
Clarinex®: 0.5 mg/mL (480 mL) [contains propylene glycol, sodium benzoate; bubblegum flavor]
Tablet, oral:
Clarinex®: 5 mg
Tablet, orally disintegrating, oral:
Clarinex®: 2.5 mg [contains phenylalanine 1.4 mg/tablet; tutti frutti flavor]
Clarinex®: 5 mg [contains phenylalanine 2.9 mg/tablet; tutti frutti flavor]
Pricing: U.S. (www.drugstore.com)
Syrup (Clarinex)
0.5 mg/mL (473): $238.58
Tablet, orally-disintegrating (Clarinex Reditabs)
2.5 mg (30): $164.99
5 mg (30): $162.99
Tablets (Clarinex)
5 mg (30): $152.99
References
McClellan K and Jarvis B, “Desloratadine,” Drugs, 2001, 61(6):789-96.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
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