Texas Health and Human Services Commission
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Criteria for Outpatient Use Guidelines

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Nonsedating Antihistamines

[Developed, March 1997]

Information on indications for use or diagnosis is assumed to be unavailable. All criteria may be applied retrospectively; prospective application is indicated with [*].

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1.* Dosage

Oral nonsedating antihistamines are FDA-approved for use to manage urticaria and allergic rhinitis. Nasal nonsedating antihistamines are FDA-approved for use in treating allergic rhinitis and vasomotor rhinitis (Astelin® only). Cetirizine tablets, chewable tablets, syrup, cetirizine/pseudoephedrine tablets, loratadine tablets, chew tabs, rapid tablets, syrup, as well as oratadine/pseudoephedrine tablets are now available over the counter for adults and children 2 years of age and older to manage chronic urticaria and allergic rhinitis. Fexofenadine tablets, orally disintegrating tablets, and liquid will be available over the counter in March 2011 for adults and children 2 years and older to manage allergic rhinitis; fexofenadine/pseudoephedrine tablets will also be available over the counter for adults and children 12 years of age and older to manage nasal congestion and sinus pressure.

Adults
Maximum recommended daily doses for available nonsedating antihistamines are summarized in Table 1. Dosages identified in Texas Medicaid patient profiles exceeding these recommendations will be reviewed.

Table 1
Maximum Recommended Daily Doses for Nonsedating Antihistamines in Adults (Monotherapy and Combination Therapy)
Drug Name Maximum Recommended Dosage
Azelastine (Astelin®, generics) nasal solution - 137 mcg/spray
Azelastine (Astepro®) 0.15% nasal solution – 205.5 mcg/spray
  2 sprays per nostril twice daily
**Cetirizine (Zyrtec®) tablets, chewable tablets - 5 mg, 10 mg
**Cetirizine (Zyrtec®) syrup - 5 mg/5 ml
**Cetirizine/pseudoephedrine (Zyrtec-D®) 12 hour tablets
(cetirizine 5 mg/pseudoephedrine 120 mg/tablet)
10 mg  once daily
1 tablet twice daily
**Fexofenadine (Allegra®, generics) tablets - 30 mg, 60 mg, 180 mg **Fexofenadine orally disintegrating (Allegra ODT®) tablets  - 30 mg
**Fexofenadine (Allegra®) suspension - 30 mg/5ml
**Fexofenadine/pseudoephedrine (Allegra-D®) 12 hour tablets
(fexofenadine 60 mg/pseudoephedrine 120 mg/tablet)
**Fexofenadine/pseudoephedrine (Allegra-D®) 24 hour tablets (fexofenadine 180 mg/ pseudoephedrine 240 mg/tablet)
60 mg twice daily or 180 mg once daily
1 tablet twice daily 
1 tablet once daily
Desloratidine (Clarinex®) tablets - 5 mg Desloratadine rapidly disintegrating (Clarinex RediTabs®) tablets -  2.5 mg, 5 mg Desloratadine (Clarinex®) syrup - 2.5 mg/5ml
Desloratadine/pseudoephedrine (Clarinex-D®) 24 hour tablets (5 mg desloratadine/ 240 mg pseudoephedrine)
5 mg once daily 
1 tablet once daily
Levocetirizine (Xyzal®) tablet – 5 mg
Levocetirizine (Xyzal®) oral solution – 2.5 mg/5 ml
5 mg once daily in evening
**Loratadine (Claritin®, Alavert®, generics) tablets - 10 mg        Loratadine chewable (Claritin Children’s®) tablets - 5 mg
**Loratadine rapidly disintegrating (Claritin RediTabs®, Alavert®, generics) tablets - 5 mg, 10 mg
**Loratadine (Claritin®) syrup - 5 mg/5 ml
**Loratadine/pseudoephedrine (Claritin D® 12 Hour, Alavert®) tablets
(loratadine 5mg/pseudoephedrine 120 mg/tablet)
**Loratadine/pseudoephedrine extended-release (Claritin D® 24 Hour, generics) tablets
(loratadine 10 mg/pseudoephedrine 240 mg/tablet)
10 mg once daily or 5 mg every 12 hours (RediTabs)
1 tablet twice daily
1 tablet once daily
Olopatadine (Patanase®) 0.6% nasal solution 2 sprays per nostril twice daily

**now OTC

Pediatrics

Oral nonsedating antihistamines are FDA-approved for use in pediatric patients for allergic rhinitis and chronic urticaria. Cetirizine is FDA-approved for use in children 2 years and older with urticaria and allergic rhinitis, levocetirizine and desloratadine are FDA-approved for use in children 6 months of age and older with chronic idiopathic urticaria and perennial allergic rhinitis and 2 years of age and older for seasonal allergic rhinitis, loratadine is FDA-approved for use in children 2 years and older for allergic rhinitis, and fexofenadine is FDA-approved for use in children 6 months and older for chronic idiopathic urticaria and children 2 years and older for seasonal allergic rhinitis. Safety and efficacy of nonsedating antihistamine/decongestant combination products have not been established in children less than 12 years of age.

Nasal nonsedating antihistamines are FDA-approved for use in children 5 years and older for seasonal allergic rhinitis treatment (Astelin® only), children 6 years and older for seasonal allergic rhinitis therapy (olopatadine only), and pediatric patients 12 years and older in managing perennial allergic rhinitis (Astepro® only), seasonal allergic rhinitis, and vasomotor rhinitis (Astelin® only).

Maximum recommended pediatric dosages for available nonsedating antihistamines are summarized in Table 2. Dosages identified in Texas Medicaid patients exceeding these recommendations will be reviewed.

Table 2
Pediatric Maximum Recommended Dosages for Nonsedating Antihistamines
Drug Name Maximum Recommended Dosage
Azelastine nasal spray perennial allergic rhinitis (Astepro® only):

12 years and older: 2 sprays per nostril twice daily seasonal allergic rhinitis:
5 to 11 years of age (Astelin® only): 1 spray per nostril twice daily
12 years of age and older (Astelin®, Astepro®):

2 sprays per nostril twice daily vasomotor rhinitis (Astelin® only):
12 years and older: 2 sprays per nostril twice daily

Cetirizine tablets, chewable tablets, syrup **
Cetirizine/pseudoephedrine 12 hour tablets**
allergic rhinitis, urticaria:
2 to 5 years of age:

5 mg once daily (syrup)
6 years and older: 10 mg once daily (tabs, chew tabs, syrup)
allergic rhinitis:

12 years and older: 1 tablet twice daily

Desloratadine tablets, rapid tablets, syrup
Desloratadine/pseudoephedrine 24 hour tablets
chronic idiopathic urticaria, perennial allergic rhinitis:

6 months to 11 months of age: 1 mg once daily (syrup)
12 months to 5 years of age: 1.25 mg once daily (syrup)
6 to 11 years of age: 2.5 mg once daily (tabs, rapid tabs, syrup)
12 years and older: 5 mg once daily (tabs, rapid tabs, syrup)
seasonal allergic rhinitis:
2 to 5 years of age: 1.25 mg once daily (syrup)
6 to 11 years of age: 2.5 mg once daily (tabs, rapid tabs, syrup)
12 years and older: 5 mg once daily (tabs, rapid tabs, syrup)
seasonal allergic rhinitis with nasal congestion:
12 years and older: 1 tablet once daily

Fexofenadine tablets, ODT, suspension**
Fexofenadine/pseudoephedrine**
12 hour tablet
24 hour tablet
chronic idiopathic urticaria:

6 months to < 2 years of age: 15 mg twice daily (oral suspension)
2 to 5 years of age: 30 mg twice daily (oral suspension)
6 to 11 years of age: 30 mg twice daily (tabs, ODT, oral suspension)
12 years and older: 60 mg twice daily or 180 mg once daily
seasonal allergic rhinitis:
2 to 5 years of age: 30 mg twice daily (oral suspension)
6-11 years of age: 30 mg twice daily (tabs, ODT, oral suspension)
12 years and older: 60 mg twice daily or 180 mg once daily

seasonal allergic rhinitis:
12 years and older: 1 tablet twice daily
12 years and older: 1 tablet once daily

Levocetirizine tablets, oral solution chronic idiopathic urticaria, perennial allergic rhinitis:

6 months to 5 years of age: 1.25 mg once daily in evening (oral solution)
6 to 11 years of age: 2.5 mg once daily in evening (tabs, solution)
12 years and older: 5 mg once daily in evening (tabs, solution)
seasonal allergic rhinitis:
2 to 5 years of age: 1.25 mg once daily in evening (oral solution)
6 to 11 years of age: 2.5 mg once daily in evening (tabs, solution)
12 years and older: 5 mg once daily in evening (tabs, solution)

Loratadine tablets, chew tabs, rapid tablets, syrup **Loratadine/pseudoephedrine **
12 hour tablet
24 hour tablet
allergic rhinitis:

2 years to 5 years of age: 5 mg once daily (chew tabs, syrup)
6 years and older: 10 mg once daily or 5 mg every 12 hours (chew tabs, rapid tabs, syrup)
seasonal allergic rhinitis:
12 years and older: 1 tablet twice daily
12 years and older: 1 tablet once daily

Olopatadine nasal spray 6 to 11 years of age: 1 spray per nostril twice daily
12 years and older: 2 sprays per nostril twice daily

2. Duration of Therapy

There is no basis for limiting the duration of treatment for nonsedating antihistamines as patients may suffer from symptoms of allergic rhinitis or other chronic allergic conditions continually.

3. * Duplicative Therapy

The concurrent use of two or more nonsedating antihistamines is not recommended. Additional therapeutic benefit is not experienced when several antihistamines are administered in combination. Patient profiles containing concurrent prescriptions for multiple nonsedating antihistamines will be reviewed.

4. * Drug-Drug Interactions

Patient profiles will be assessed to identify those drug regimens which may result in clinically significant drug-drug interactions.

Drug-drug interactions considered clinically significant for nonsedating antihistamines are summarized in Table 3. Only those drug-drug interactions classified as clinical significance level 1/ contraindicated or those considered life-threatening which have not yet been classified will be reviewed:

Table 3
Nonsedating Antihistamine Drug-Drug Interactions
Target Drug Interacting Drug Interaction Recommendations Clinical Significance
fexofenadine antacids adjunctive administration within 15 minutes of each other decreases fexofenadine bioavailability (AUC ↓’d 41%, Cmax ↓’d 43%), may reduce fexofenadine efficacy space administration times moderate (DrugReax)
2-major (CP *)
1 (DIF)
fexofenadine, loratadine CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) fexofenadine, loratadine metabolized by CYP3A4; concurrent administration may increase fexofenadine, loratadine serum concentrations and increase potential for enhanced pharmacologic/adverse effects monitor for increased fexofenadine, loratadine adverse effects 4-low (CP)
3, 4 (DIF)
fexofenadine rifamycins co-administration may decrease fexofenadine serum concentrations and reduce fexofenadine efficacy; rifamycins may activate P-glycoprotein transport in small intestine (fexofenadine is substrate of this transport) and decrease fexofenadine oral absorption monitor for decreased fexofenadine therapeutic effects 4-low (CP)
3 (DIF)
loratadine amiodarone conjunctive administration may result in reduced loratadine metabolism and enhanced loratadine pharmacologic/adverse effects; amiodarone inhibits CYP3A4, loratadine metabolized by CYP3A4; rare reports of QT interval prolongation with drug combination use cautiously together; QT interval monitoring recommended major (DrugReax)

REFERENCES

  1. DRUGDEX® System (electronic version). Thomson Reuters (Healthcare) Inc., Greenwood Village, Colorado, USA. Available at: http://www.thomsonhc.com.libproxy.uthscsa.edu. Accessed January 7th, 2011.
  2. Clinical Pharmacology [database online]. Tampa, FL: Gold Standard, Inc; 2011. Available at: http://www.clinicalpharmacology.com. Accessed January 7th, 2011.
  3. Drug Facts and Comparisons. Clin-eguide [database online]. St. Louis, MO: Wolters Kluwer Health, Inc; 2010. Available at: http://clineguide.com. Accessed January 7th, 2011.
  4. Azelastine 0.15% nasal spray (Astepro®) Package Insert. Meda Pharmaceuticals, November 2010.
  5. Fexofenadine (Allegra®) Package Insert. Sanofi-Aventis U.S., July 2007.
  6. Drug interaction facts. Clin-eguide [database online]. St. Louis, MO: Wolters Kluwer Health, Inc; 2010. Available at: http://clineguide.com. Accessed January 6th, 2011.
  7. DRUG-REAX® System (electronic version). Thomson Reuters (Healthcare) Inc., Greenwood Village, Colorado, USA. Available at: http://www.thomsonhc.com.libproxy.uthscsa.edu. Accessed January 6th, 2011.
  8. Apgar DA. Allergic rhinitis. In: Chisholm-Burns M, Schwinghammer TL, Wells BG, et al, eds. Pharmacotherapy principles and practice. 2nd ed. New York: McGraw-Hill; 2009:1047-62.
  9. Morgan MM. Khan DA. Nathan RA. Treatment for allergic rhinitis and chronicidiopathic urticaria: focus on oral antihistamines. Ann Pharmacother. 2005;39:2056-64.
  10. Kaliner MA. A novel and effective approach to treating rhinitis with nasal antihistamines. Ann Allergy, Asthma, & Immunol. 2007;99:383-90.
  11. Anonymous. Levocetirizine (Xyzal) for allergic rhinitis and urticaria. Med Lett Drugs Ther. 2007;49:97-9.
  12. DA News. FDA approves Zyrtec for nonprescription use in adults and children. Available at: http://www.fda.gov/bbs/topics/NEWS/2007/NEW01750.html. Accessed January 22nd, 2008.
  13. Sur DK, Scandale S. Treatment of allergic rhinitis. Am Fam Physician. 2010; 81(12):1440-1446.
  14. Claritin®. Available at: http://www.claritin.com/claritin/home/index.jspa. Accessed March 1st, 2011.
  15. Zyrtec®. Available at: http://www.zyrtec.com. Accessed March 1st, 2011.
  16. Allegra®. Available at: http://www.allegra.com. Accessed March 1st, 2011.

Prepared by: Drug Information Service, The University of Texas Health Science Center at San Antonio, and the College of Pharmacy, The University of Texas at Austin.