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Rhinocort Aqua eent

Generic Name: Budesonide eent
Class: Corticosteroids
ATC Class: R01AD05
VA Class: NT200
Chemical Name: [11β,16α(R)]-16,17-Butylidene-bis(oxy)-11,21-dihydroxy-pregna-1,4-diene-3,20-dione and 16α,17-[(S)-butylidinebis(oxy)]-11β,21-dihydroxypregna-1,4-diene-3,20-dione
Molecular Formula: C25H34O6
CAS Number: 51333-22-3

Warning(s)

REMS:

FDA approved a REMS for budesonide to ensure that the benefits of a drug outweigh the risks. The REMS may apply to one or more preparations of budesonide and consists of the following: communication plan. See the FDA REMS page () or the ASHP REMS Resource Center ().

Introduction

Synthetic, non-halogenated corticosteroid.1 16

Uses for Rhinocort Aqua

Allergic Rhinitis

Symptomatic treatment of seasonal or perennial allergic rhinitis.1 7 8 9 12 13 14 15 16 17 18 19

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

Rhinocort Aqua Dosage and Administration

General

  • For therapeutic effectiveness, use at regular intervals.1

Administration

Intranasal Inhalation

Administer by nasal inhalation using a metered-dose pump spray.1

Shake inhaler gently immediately prior to use.1 17

Prior to initial use, the metered-dose pump spray must be primed with 8 actuations.1 10

If spray pump is not used for 2 consecutive days, partially prime (1 actuation or until a fine spray is observed).1 17 If the spray pump is not used for more than 14 days, rinse the applicator and reprime with 2 sprays or until a fine spray appears.1 Rinse the applicator when not used for more than 14 days.1 17

Clear nasal passages prior to administration.a

Tilt the head slightly forward, insert the spray tip into one nostril, and point the tip toward the back of the nose.a Pump the drug into one nostril while holding the other nostril closed and concurrently inspire through the nose.a Repeat this procedure for the other nostril.a

Dosage

After priming, nasal spray pump delivers about 32 mcg of budesonide per metered spray and about 120 metered doses per 8.6-g container.1 10

Pediatric Patients

Titrate dosage to the lowest possible effective level.1 (See Pediatric Use under Cautions.)

Seasonal Allergic Rhinitis
Intranasal Inhalation

Children 6–11 years of age: initially, 32 mcg (1 spray) in each nostril once daily (64 mcg total).1 17 May be increased to 64 mcg (2 sprays) in each nostril once daily (128 mcg total).1

Children ≥12 years of age: initially, 32 mcg (1 spray) in each nostril once daily (64 mcg total).1 17 May be increased to 128 mcg (4 sprays) in each nostril once daily (256 mcg total).1

Perennial Allergic Rhinitis
Intranasal Inhalation

Children 6–11 years of age: initially, 32 mcg (1 spray) in each nostril once daily (64 mcg total).1 17 May be increased to 64 mcg (2 sprays) in each nostril once daily (128 mcg total).1

Children ≥12 years of age: initially, 32 mcg (1 spray) in each nostril once daily (64 mcg total).1 17 May be increased to 128 mcg (4 sprays) in each nostril once daily (256 mcg total).1

Adults

Seasonal Allergic Rhinitis
Intranasal Inhalation

Initially, 32 mcg (1 spray) in each nostril once daily (64 mcg total).1 17 May be increased to 128 mcg (4 sprays) in each nostril once daily (256 mcg total).1

Perennial Allergic Rhinitis
Intranasal Inhalation

Initially, 32 mcg (1 spray) in each nostril once daily (64 mcg total).1 17 May be increased to 128 mcg (4 sprays) in each nostril once daily (256 mcg total).1

Prescribing Limits

Pediatric Patients

Seasonal Allergic Rhinitis
Intranasal Inhalation

Children 6–11 years of age: maximum 128 mcg (2 sprays in each nostril) once daily.1

Children ≥12 years of age: maximum 256 mcg (4 sprays in each nostril) once daily.1

Perennial Allergic Rhinitis
Intranasal Inhalation

Children 6–11 years of age: maximum 128 mcg (2 sprays in each nostril) once daily.1

Children ≥12 years of age: maximum 256 mcg (4 sprays in each nostril) once daily.1

Adults

Seasonal Allergic Rhinitis
Intranasal Inhalation

Maximum 256 mcg (4 sprays in each nostril) once daily.1

Perennial Allergic Rhinitis
Intranasal Inhalation

Maximum 256 mcg (4 sprays in each nostril) once daily.1

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.1

Renal Impairment

No specific dosage recommendations at this time.1

Geriatric Patients

No specific dosage recommendations at this time.1

Cautions for Rhinocort Aqua

Contraindications

  • Known hypersensitivity to budesonide or any ingredient of the formulation.1

Warnings/Precautions

Warnings

Withdrawal of Systemic Corticosteroid Therapy

Possible corticosteroid withdrawal symptoms (e.g., joint pain, muscular pain, lassitude, depression), acute adrenal insufficiency, or severe symptomatic exacerbation of asthma or other clinical conditions if prolonged systemic corticosteroid therapy is replaced with topical corticosteroid therapy; careful monitoring recommended.1

Use particular caution in patients with associated asthma or other conditions that may be exacerbated by too rapid a reduction in systemic corticosteroid dosage.1

Immunosuppressed Patients

Increased susceptibility to infections in patients who are taking immunosuppressant drugs.1 Certain infections (e.g., varicella [chickenpox], measles) can be serious or even fatal in such patients, particularly in children.1

Exposure to varicella and measles should be avoided in previously unexposed patients.1 If exposure to varicella (chickenpox) or measles occurs in susceptible patients, consider administering varicella zoster immune globulin (VZIG) or immune globulin (IG) respectively.1 10 Consider treatment with an antiviral agent if varicella develops.1

Sensitivity Reactions

Rarely, immediate or delayed hypersensitivity reactions may occur.1 16 Wheezing reported very rarely.1

General Precautions

Systemic Corticosteroid Effects

Possible growth suppression in children and adolescents.1 20 (See Pediatric Use under Cautions.)

Excessive intranasal dosages or use in patients who are particularly sensitive to corticosteroid effects may increase risk of systemic corticosteroid effects (e.g., hypercorticism and adrenal suppression).1

To minimize the systemic effects, titrate dosage to the lowest possible effective level;1 avoid use of higher than recommended dosages.1 If systemic effects occur, slowly reduce dosage and discontinue drug.1

Nasopharyngeal and Ocular Effects

Rarely, localized candidal infections of the nose and/or pharynx have been reported.1 Local treatment of such infections and/or discontinuance of intranasal therapy may be required.1

Rarely, nasal septum perforation and increased intraocular pressure (IOP) have been reported.1

Periodically examine nasal passages for mucosal changes during long-term therapy (several months or longer).1

Use not recommended in patients with recent nasal septal ulcers, nasal surgery, or nasal trauma until healing has occurred.1

Concomitant Infections

Use with caution, if at all, in patients with clinical or asymptomatic Mycobacterium tuberculosis infection of the respiratory tract; in untreated fungal, bacterial, or systemic viral infections; or ocular herpes simplex infections.1

Specific Populations

Pregnancy

Category B.1 a

Use during pregnancy may result in hypoadrenalism in infants;1 a monitor these infants carefully.1 a

Lactation

Not known whether budesonide is distributed into milk.1 Caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established in children <6 years of age.1

Intranasal corticosteroids may reduce growth velocity in pediatric patients.1 Routine monitoring of growth (e.g., via stadiometry) recommended.1 Titrate dosage to the lowest possible effective level.1

Geriatric Use

No overall substantial differences in safety and efficacy relative to younger patients.1 However, possible increased sensitivity to the drug.1 Frequency of epistaxis may increase with age.1

Hepatic Impairment

Possible decreased clearance and increased systemic availability.1

Renal Impairment

Pharmacokinetics not studied in patients with renal impairment.1

Common Adverse Effects

Epistaxis, pharyngitis, bronchospasm, cough, nasal irritation.1

Interactions for Rhinocort Aqua

Metabolized by CYP3A4 isoenzyme.1

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (increased plasma budesonide concentrations) with concomitant use of CYP3A4 isoenzyme inhibitors.1

Inhibitors of the CYP2C19 isoenzyme do not appear to affect the pharmacokinetics of oral budesonide.1

Specific Drugs

Drug

Interaction

Cimetidine

Decreased budesonide clearance and increased oral bioavailability1

Clarithromycin

Increased plasma budesonide concentrations1

Erythromycin

Increased plasma budesonide concentrations1

Itraconazole

Increased plasma budesonide concentrations1

Ketoconazole

Increased plasma budesonide concentrations1

Omeprazole

No apparent pharmacokinetic interaction1

Rhinocort Aqua Pharmacokinetics

Absorption

Bioavailability

Relatively well absorbed following intranasal inhalation.1 Following intranasal administration, approximately 34% of a dose reaches systemic circulation.1 Mean peak plasma budesonide concentrations are attained in about 0.7 hours.1

Onset

Nasal symptoms improve within 8–12 hours following initiation of therapy.1 7 About 50–66% of the total symptomatic relief is evident within 1–2 days after treatment initiation.1 May require about 2 weeks of therapy for optimum effectiveness.1

Special Populations

Children have plasma drug concentrations approximately twice those observed in adults due to differences in weight.1

Distribution

Extent

Distributes into red blood cells.1 Not known whether the drug crosses the placenta or distributes into breast milk; however, other corticosteroids are distributed into breast milk.1

Plasma Protein Binding

85-90%.1 Little to no binding to glucocorticosteroid binding globulin.1

Elimination

Metabolism

Rapidly metabolized to metabolites of low corticosteroid potency by CYP3A4.1

Elimination Route

Excreted in urine (66%) and feces (33%) as metabolites.1

Half-life

2–3 hours.1

Special Populations

Hepatic impairment may affect elimination of corticosteroids by increasing the systemic availability of oral budesonide.1 Intranasally applied budesonide not studied in such patients.1

Stability

Storage

Intranasal Inhalation

Suspension

20–25°C; do not freeze.1 Protect from light.1

Actions

  • Potent glucocorticoid and weak mineralocorticoid activity.1

  • Decreases the nasal reactivity to allergens and decreases release of inflammatory mediators1 4 and proteolytic enzymes.4

  • Reduces the number of certain mediator cells (basophils,5 15 eosinophils,1 5 15 T-helper cells,6 mast cells,1 4 and neutrophils)1 5 in the nasal mucosa.

Advice to Patients

  • Importance of providing patient a copy of the manufacturer’s patient information.1 17

  • Importance of understanding proper storage, preparation, and administration techniques.1 Importance of shaking container gently prior to each use.1 Importance of avoiding spraying drug into the eyes.1 17

  • Advise patients that containers of budesonide nasal spray should be discarded after 120 actuations.1

  • Importance of regular use to obtain therapeutic effectiveness.1 Importance of not exceeding prescribed dosage.1

  • Advise that the drug usually will provide symptomatic relief within 2 days, but 2 weeks of continuous therapy usually are required for optimum effects.1

  • Importance of informing clinician if symptoms worsen or fail to improve within 2 weeks.1

  • Importance of advising clinician if recurrent epistaxis or nasal septum discomfort occurs.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1

  • Importance of women informing clinicians 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.

In 2002, the manufacturer decided to gradually phase out budesonide nasal aerosol (Rhinocort)2 from the US market.3 AstraZeneca will continue to manufacture budesonide nasal spray (Rhinocort Aqua) that unlike budesonide nasal aerosol does not contain fluorocarbons which have been associated with excessive drying of the nasal mucosa in some patients.11

Budesonide

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Suspension, for intranasal use only

32 mcg/metered spray

Rhinocort Aqua Nasal Spray

AstraZeneca

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.

Rhinocort Aqua 32MCG/ACT Suspension (ASTRAZENECA LP): 9/$115.99 or 26/$329.99

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions October 27, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. AstraZeneca. Rhinocort Aqua (budesonide nasal spray) prescribing information. Wilmington, DE; 2001 Oct.

2. AstraZeneca. Rhinocort (budesonide nasal inhaler) prescribing information (dated 2001 Apr). In: Physicians' desk reference. 56th ed. Montvale, NJ: Medical Economics Company Inc; 2002:640-2.

3. Anon. Dear Pharmacist letter concerning discontinuance of the manufacture of Rhinocort (budesonide nasal inhaler). Wilmington, DE: AstraZeneca; 2002 Nov 15.

4. Meltzer EO, Jalowayski AA, Field EA et al. Intranasal fluticasone propionate reduces histamine and tryptase in the mucosa of allergic rhinitis patients. J Allergy Clin Immunol. 1993; 91:298.

5. Bryson HM, Faulds D. Intranasal fluticasone propionate: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in allergic rhinitis. Drugs. 1992; 43:760-75. [IDIS 359172] [PubMed 1379151]

6. Masuyama K, Jacobson MR, Rak S et al. Topical glucocorticosteroid (fluticasone propionate) inhibits cells expressing cytokine mRNA for interleukin-4 in the nasal mucosa in allergen-induced rhinitis. Immunology. 1994; 82:192- 9. [PubMed 7927488]

7. Fokkens WJ, Cserhati E, dos Santos JM et al. Budesonide aqueous nasal spray is an effective treatment in children with perennial allergic rhinitis, with an onset of action within 12 hours. Ann Allergy Asthma Immunol. 2002; 89:279-84. [IDIS 486624] [PubMed 12269648]

8. Ciprandi G, Canonica WG, Grosclaude M et al. Effects of budesonide and fluticasone propionate in a placebo-controlled study on symptoms and quality of life in seasonal allergic rhinitis. Allergy. 2002; 57:586-91. [PubMed 12100298]

9. Bende M, Carrillo T, Vona I et al. A randomized comparison of the effects of budesonide and mometasone furoate aqueous nasal sprays on nasal peak flow rate and symptoms in perennial allergic rhinitis. Ann Allergy Asthma Immunol. 2002; 88:617-23. [IDIS 482210] [PubMed 12086370]

10. AstraZeneca, Wilmington, DE: Personal communication.

11. Mygind N, Clark TJH. Topical steroid treatment for asthma and rhinitis. London: Bailliere Tindall; 1980:89,91,152,159,172.

12. Andersson M, Svensson C, Persson C et al. Dose-dependent effects of budesonide agueous nasal spray on symptoms in a daily nasal allergen challenge model. Ann Allergy Asthma Immunol. 2000; 85:279-83. [IDIS 454624] [PubMed 11061470]

13. Day J, Carrillo T. Comparison of the efficacy of budesonide and fluticasone propionate aqueous nasal spray for once daily treatment of perennial allergic rhinitis. J Allergy Clin Immunol. 1998; 102(6 Part 1):902-8. [IDIS 424214] [PubMed 9847429]

14. Creticos P, Fireman P, Settipane G et al, for the Rhinocort Aqua Study Group. Intranasal budesonide aqueous pump spray (Rhinocort Aqua) for the treatment of seasonal allergic rhinitis. Allergy Asthma Proc. 1998;19:285-94.

15. Meltzer EO. Clinical and antiinflammatory effects of intranasal budesonide aqueous pump spray in the treatment of perennial allergic rhinitis. Ann Allergy Asthma Immunol. 1998; 81:128-34. [IDIS 412928] [PubMed 9723557]

16. Brogden RN, McTavish D. Budesonide: an updated review of its pharmacological properties, and therapeutic efficacy in asthma and rhinitis. Drugs. 1992;44:375-407.

17. AstraZeneca. How to use Rhinocort Aqua. Wilmington, DE; April 2002. From AstraZeneca website (). Accessed 2003 March 4.

18. Yanez A, Rodrigo GJ. Intranasal corticosteroids versus topical H1 receptor antagonists for the treatment of allergic rhinitis: a systematic review with meta-analysis. Ann Allergy Asthma Immunol. 2002; 89:479-84. [IDIS 490491] [PubMed 12452206]

19. Galant SP, Wilkinson R. Clinical prescribing of allergic rhinitis medication in the preschool and young school-age child: what are the options? BioDrugs. 2001; 15:453-63.

20. Pedersen S. Assessing the effect of intranasal steroids on growth. J Allergy Clin Immunol. 2001; 108(1 Suppl):S40-4. [IDIS 467845] [PubMed 11449205]

a. AstraZeneca. Rhinocort Aqua (budesonide nasal spray) prescribing information. Wilmington, DE; 2004 Aug.

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