Tilade

Generic Name: Nedocromil Sodium
Class: Mast-cell Stabilizers
ATC Class: R01AC07
VA Class: RE101
Chemical Name: 9-Ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano(3,2-g)quinoline-2,8-dicarboxylic acid disodium salt
Molecular Formula: C19H17NO7•2Na
CAS Number: 69049-74-7

Introduction

Mast cell stabilizer; a pyranoquinoline dicarboxylic acid derivative.1 2 3 4 5 6 7 9 10 11 1 2 3 9 10 11

Uses for Tilade

Asthma

Used as an adjunct in the overall management of mild to moderate bronchial asthma.1 2 3 4 5 9 10 11 a

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For prophylaxis only; not indicated for reversal of acute bronchospasm, including status asthmaticus.a 1 9 10 (See Acute Bronchospasm under Warnings.)

Tilade Dosage and Administration

General

  • Initially, administer concurrently with patient’s existing maintenance dosages of β-adrenergic agonists, theophylline, and/or corticosteroids.a 1 2 4 5 Once clinical response is observed and asthma adequately controlled, gradual reduction in concomitant therapy may be possible.a 1 2 4 5

Administration

Oral Inhalation

Administer by oral inhalation using an oral aerosol inhaler.1

Shake inhaler well before use.1 8 Actuate aerosol inhaler 3 times prior to the initial use or if it has not been used for >7 days.a

Exhale slowly and completely, invert the inhaler, place the mouthpiece of the inhaler well into the mouth, and close the lips around it.8 Inhale slowly and deeply through the mouth while actuating the inhaler.8 Hold breath for 5–10 seconds, withdraw the mouthpiece, and exhale slowly.2 8

Avoid spraying in eyes.a

Clean inhaler twice weekly. Remove metal canister and cap and rinse plastic mouthpiece in hot running water. Allow to dry overnight in a warm place.a 8

Optimal therapeutic effect is dependent upon administration at regular intervals, even during symptom-free periods.a

Dosage

Available as nedocromil sodium, dosage expressed in terms of the salt.a 1

The dose of nedocromil sodium is expressed as the amount delivered from the actuator of the inhaler per metered spray.a

Oral inhalation aerosol delivers 2 mg from the valve and 1.75 mg from the actuator per metered spray.a Each aerosol canister delivers ≥104 metered sprays.a 1

Pediatric Patients

Asthma
Oral Inhalation

Children ≥6 years of age: 3.5 mg (2 inhalations) 4 times daily at regular intervals (14 mg/day).1

Less frequent administration may be effective if asthma is well controlled at this dose (e.g., patients only need occasional β-agonist therapy and are not experiencing serious exacerbations).a

Adults

Asthma
Oral Inhalation

3.5 mg (2 inhalations) 4 times daily at regular intervals (14 mg/day).1

Less frequent administration may be effective if asthma is well controlled at this dose (e.g., patients only need occasional β-agonist therapy and are not experiencing serious exacerbations).a

Prescribing Limits

Pediatric Patients

Asthma
Oral Inhalation

Children ≥6 years of age: Maximum 3.5 mg (2 inhalations) 4 times daily (14 mg/day).1

Adults

Asthma
Oral Inhalation

Maximum 3.5 mg (2 inhalations) 4 times daily (14 mg/day).a 1

Special Populations

No special population dosage recommendations at this time.a

Cautions for Tilade

Contraindications

Known hypersensitivity to nedocromil or any ingredient in the formulation.a

Warnings/Precautions

Warnings

Acute Bronchospasm

Nedocromil is not a bronchodilator; do not use for reversal of acute bronchospasm, especially status asthmaticus.1 9 10 a

Use should generally be continued during acute exacerbations, unless patient becomes intolerant to use of inhaled dosage forms.a

Bronchospasm, possibly life-threatening, may occur immediately after administration.a If this occurs, discontinue nedocromil and institute alternative therapy.a

General Precautions

Concomitant Corticosteroid Dosage

Role of nedocromil as a corticosteroid-sparing agent in patients receiving oral or inhaled corticosteroids not defined.a Monitor patients closely if systemic or inhaled corticosteroids are reduced.a

Specific Populations

Pregnancy

Category B.a

Lactation

Not known if nedocromil is distributed into milk.a Caution is advised if nedocromil is used.a

Pediatric Use

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

Common Adverse Effects

Unpleasant taste, coughing, pharyngitis, rhinitis, upper respiratory infection, dyspnea, bronchospasm, sinusitis, nausea, vomiting, headache, chest pain, fever, viral infection.a

Interactions for Tilade

No formal drug interaction studies to date.a

Tilade Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability is 8 and 17% for single and multiple inhaled doses, respectively.a

Onset

Full therapeutic effect may not be obtained for ≥1 week.a

Distribution

Plasma Protein Binding

89%.a

Elimination

Elimination Route

Excreted principally in urine as unchanged drug.a

Half-life

3.3 hours.a

Special Populations

Pharmacokinetics in children 6–11 years of age appear similar to those in adults.a

Stability

Storage

Oral Inhalation

Aerosol, Solution for Inhalation

2–30°C.a Do not freeze.a

Temperatures >120°F may cause aerosol canister to burst.a

Actions

  • Inhibits acute bronchoconstrictor response and delayed inflammatory response.a 1 2 6 9 10 11

  • In vitro, inhibits eosinophils, neutrophils, macrophages, mast cells, monocytes, platelets,a 1 2 3 9 10 11 histamine, leukotriene C4, and prostaglandin D2.a 1 2 3 5 6

  • Inhibits bronchoconstriction caused by sulfur dioxide, inhaled neurokinin A, various antigens, exercise, cold air, fog, and adenosine monophosphate.a

  • Exhibits no bronchodilator, antihistamine, or corticosteroid activity.a

  • Exhibits cough suppression resulting from inhibition of neuronal reflexes in airways.2 6 9 10

Advice to Patients

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

  • Importance of adequate understanding of proper storage, preparation, disposal, and inhalation technique.a

  • Importance of adherence to dosing schedules, even during symptom-free periods, and of not changing dose unless otherwise instructed by a clinician.a

  • Importance of notifying physician immediately if symptoms do not improve or condition worsens.a

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.a

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

  • Importance of informing patients of other important precautionary information.a (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Nedocromil Sodium

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral Inhalation

Aerosol

1.75 mg/metered spray (from the mouthpiece)

Tilade Inhaler (with chlorofluorohydrocarbon propellants)

Monarch

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2010, Selected Revisions May 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Aventis. Tilade (nedocromil sodium) inhalation aerosol prescribing information. Kansas City, MO; 1999 Oct.

2. Gonzalez JP, Brogden RN. Nedocromil sodium: a preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of reversible obstructive airways disease. Drugs. 1987; 34:560-77. [IDIS 236663] [PubMed 2826101]

3. Rebuck AS, Kesten S, Boulet LP et al. A 3-month evaluation of the efficacy of nedocromil sodium in asthma: a randomized, double-blind, placebo-controlled trial of nedocromil sodium conducted by a Canadian multicenter study group. J Allergy Clin Immunol. 1990; 85:612-7. [IDIS 314389] [PubMed 2155958]

4. Callaghan B, Teo NC, Clancy L. Effects of the addition of nedocromil sodium to maintenance bronchodilator therapy in the management of chronic asthma. Chest. 1992; 101:787-92. [IDIS 293018] [PubMed 1311666]

5. Cherniack RM, Wasserman SI, Ramsdell JW et al. A double-blind multicenter group comparative study of the efficacy and safety of nedocromil sodium in the management of asthma. Chest. 1990; 97:1299-1306. [IDIS 289144] [PubMed 2161328]

6. Tandon MK. Double-blind crossover study of nedocromil sodium in partially reversible chronic obstructive airways disease. Chest. 1993; 103:105-10. [IDIS 308235] [PubMed 8380266]

7. Morton AR, Ogle SL, Fitch KD. Effects of nedocromil sodium, cromolyn sodium, and a placebo in exercise-induced asthma. Ann Allergy. 1992; 68:143-8. [IDIS 292497] [PubMed 1310834]

8. Fisons. Tilade (nedocromil sodium) inhalation aerosol patient information. (undated)

9. Anon. Nedocromil for asthma. Med Lett Drugs Ther. 1993; 35:62-3. [PubMed 8390598]

10. Parish RC, Miller LJ. Nedocromil sodium. Ann Pharmacother. 1993; 27:599-606. [IDIS 314179] [PubMed 8394165]

11. Lal S, Dorow PD, Venho KK et al. Nedocromil sodium is more effective than cromolyn sodium for the treatment of chronic reversible obstructive airway disease. Chest. 1993; 104:438-47. [IDIS 319804] [PubMed 8393398]

12. Fisons Pharmaceuticals, Rochester, NY: Personal communication.

13. National Asthma Education and Prevention Program. Expert panel report II: guidelines for the diagnosis and management of asthma. 1997 Feb.

14. Kemp JP. Comprehensive asthma management: guidelines for clinicians. J Asthma. 1998; 35:601-20. [PubMed 9860081]

15. Kemp JP. Guidelines update: where do the new therapies fit in the management of asthma? Drugs. 2000; 59(Suppl 1):23-8.

a. King Pharmaceuticals. Tilade (nedocromil sodium) inhalation aerosol prescribing information. Bristol, TN; 2004 July.

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