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Medication Safety Issues
Sound-alike/look-alike issues:
Clarinex® may be confused with Celebrex®
Pronunciation
(des lor AT a deen)
U.S. Brand Names
Generic Available
No
Canadian Brand Names
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
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
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
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: Paliperidone. Risk C: Monitor therapy
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. Risk C: Monitor therapy
P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein 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 Inhibitors: May increase the serum concentration of P-Glycoprotein 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
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase risk of sedation).
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
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.
Dietary Considerations
May be taken with or without food. Orally-disintegrating tablets contain phenylalanine.
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
Nursing: Physical Assessment/Monitoring
Assess effectiveness and interactions of other medications patient may be taking. Monitor effectiveness of therapy and adverse reactions at beginning of therapy and periodically with long-term use. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Syrup:
Clarinex®: 0.5 mg/mL (480 mL) [contains propylene glycol, sodium benzoate; bubble gum flavor]
Tablet:
Clarinex®: 5 mg
Tablet, orally disintegrating:
Clarinex® RediTabs®: 2.5 mg [contains phenylalanine 1.4 mg/tablet; tutti-frutti flavor]; 5 mg [contains phenylalanine 2.9 mg/tablet; tutti-frutti flavor]
Pricing: U.S. (www.drugstore.com)
Syrup (Clarinex)
0.5 mg/mL (473): $198.05
Tablet, orally-disintegrating (Clarinex Reditabs)
2.5 mg (30): $138.94
5 mg (30): $127.67
Tablets (Clarinex)
5 mg (30): $125.74
References
McClellan K and Jarvis B, “Desloratadine,” Drugs, 2001, 61(6):789-96.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2009
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