Professional Drug Information > Opticrom

Cromolyn (Ophthalmic)

INN:
Cromoglicic acid. ^{14}

BAN:
Cromoglycic acid. ^{14}

VA CLASSIFICATION
Primary: OP801

Commonly used brand name(s): Crolom; Opticrom; Vistacrom.

Another commonly used name is
sodium cromoglycate .
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Mast cell stabilizer (ophthalmic)—

antiallergic (ophthalmic)—

Indications

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

Accepted

[Conjunctivitis, seasonal allergic (treatment)]^{{08}{09}{10}{11}}
Conjunctivitis, vernal (treatment)^1{12}{25}
Keratitis, vernal (treatment)¹ or^{12}{25}
Keratoconjunctivitis, vernal (treatment)^{{08}{09}{10}{11}{12}{25}}—Cromolyn ophthalmic solution is indicated in the treatment of certain allergic ocular disorders, specifically, seasonal allergic conjunctivitis, vernal conjunctivitis, vernal keratitis, and vernal keratoconjunctivitis. ^{{08} {09} {10} {11} {12} {16} {17} {18} {19} {20} {23} {25}}

¹ Not included in Canadian product labeling.

Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    512.34 ^{14}


pH
    4.0 to 7.0. ^{{12} {13}}

Mechanism of action/Effect:

Cromolyn is a mast cell stabilizer that inhibits the Type I immediate hypersensitivity reaction by preventing the antigen-stimulated release of histamine. Cromolyn also prevents the release of leukotrienes and inhibits eosinophil chemotaxis. ^{{07} {08} {12} {16} {23} {24}}

In vitroand in vivo animal studies have shown that cromolyn inhibits the degranulation of sensitized mast cells that occurs after exposure to specific antigens. ^{{12} {16} {20}} Some in vitro studies have shown that cromolyn inhibits the degranulation of nonsensitized rat mast cells by phospholipase A and the subsequent release of chemical mediators. ^{12} One study has shown that cromolyn does not inhibit the enzymatic action of released phospholipase A on its specific substrate. ^{{02} {04} {12}}

Absorption:

Poorly absorbed. ^{{12} {23}}

In normal individuals, approximately 0.03% of cromolyn is absorbed systemically following ophthalmic administration. ^{{02} {04} {12} {16}}

Studies in rabbits have shown that less than 0.07% of the administered dose is absorbed systemically following multiple doses. ^{{12} {16}} Also, trace amounts (less than 0.01%) ^{{12} {16}} of the administered dose penetrate into the aqueous humor, and clearance from this chamber is almost complete within 24 hours following discontinuation of treatment. ^{{02} {04} {12} {16}}

Onset of therapeutic effect

Usually within a few days. ^{{01} {02} {04} {05} {07} {12}}


Precautions to Consider

Carcinogenicity

Long-term studies in mice (12 months of intraperitoneal treatment followed by 6 months of observation), hamsters (12 months of intraperitoneal treatment followed by 12 months of observation), and rats (18 months of subcutaneous treatment) did not show any neoplastic effect associated with administration of cromolyn. ^{{02} {04} {12}}

Mutagenicity

In various mutagenicity studies, there was no evidence of chromosomal damage or cytotoxicity. ^{{02} {04} {12}}

Pregnancy/Reproduction
Fertility—
In animal reproduction studies with cromolyn, there was no evidence of impaired fertility. ^{{02} {04} {12}}

Pregnancy—
Adequate and well-controlled studies in humans have not been done. ^{{02} {04} {12} {25}}

Reproduction studies in mice, rats, and rabbits with cromolyn administered parenterally in doses up to 338 times the human clinical doses showed no evidence of fetal malformations. ^{{12} {25}} Adverse fetal effects (increased resorptions and decreased fetal weight) were noted only at very high parenteral doses that produced maternal toxicity. ^{{02} {03} {04} {12} {25}}

FDA Pregnancy Category B. ^{{02} {03} {04} {12} {25}}

Breast-feeding

It is not known whether cromolyn is distributed into breast milk. ^{{12} {25}} However, problems in humans have not been documented. Since cromolyn reaches very low concentrations in maternal serum, it would be expected to reach even lower and probably undetectable concentrations in breast milk. ^{{02} {04}}

Pediatrics

Appropriate studies on the relationship of age to the effects of ophthalmic cromolyn have not been performed in children up to 4 years of age. Safety and efficacy have not been established. ^{{12} {25}} In older children, no pediatrics-specific problems have been documented to date.


Geriatrics


Appropriate studies on the relationship of age to the effects of cromolyn have not been performed in the geriatric population. However, geriatrics-specific problems that would limit the usefulness of this medication in the elderly are not expected.

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problem exists
Sensitivity to cromolyn^{12}{22}




Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence rare
    
Chemosis^{15}{20} (swelling of the membrane covering the white part of the eye), conjunctival injection^{{12}{15}{16}{20}} (redness of the white part of the eye), styes,^{12}{16} or other signs of eye irritation not present before therapy
    
contact dermatitis^{21} (rash or redness around the eyes)



Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Burning or stinging of eye, mild, temporary^{04}{12}{18}

Incidence less frequent or rare
    
Dryness or puffiness around the eye
    
watering or itching of eye, increased
^{{12}{15}{16}{20}}




Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Cromolyn (Ophthalmic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to cromolyn





Use in children—Safety and efficacy have not been established in children up to 4 years of age ^{12}


Proper use of this medication
Proper administration technique; not touching applicator tip to any surface; keeping container tightly closed

» Importance of not using more medication than the amount prescribed

» Compliance with therapy; symptomatic response usually occurs within a few days

» Proper dosing
Missed dose: Using as soon as possible

» Proper storage

Precautions while using this medication
» Checking with physician if symptoms do not improve or if condition becomes worse


Side/adverse effects
Signs of potential side effects, especially chemosis, conjunctival injection, styes, or other signs of eye irritation not present before therapy; or contact dermatitis


General Dosing Information
Symptomatic response to therapy (decreased itching, redness, watering, and discharge) usually occurs within a few days; however, treatment may be required for up to 6 weeks. ^{{02} {04} {07} {12} {16}}

Corticosteroids may be used concurrently with cromolyn, if required. ^{{02} {04} {12}}

Although the manufacturer recommends that patients not wear soft contact lenses during treatment with cromolyn ophthalmic solution, ^{{02} {04} {05} {07} {12}} medical experts do not believe this precaution is necessary unless the patient has corneal epithelial problems and the medication is to be used more often than once every 1 to 2 hours. No significant problems have been documented with ophthalmic solutions containing 0.03% or less of benzalkonium chloride as a preservative, and used as eyedrops in patients with no significant corneal surface problems.


Ophthalmic Dosage Forms

Note: Bracketed uses in the Dosage Forms section refer to categories of use and/or indications that are not included in U.S. product labeling.

CROMOLYN SODIUM OPHTHALMIC SOLUTION USP

Usual adult and adolescent dose
[Conjunctivitis, seasonal allergic]
Conjunctivitis, vernal¹
Keratitis, vernal or¹
Keratoconjunctivitis, vernal
Topical, to the conjunctiva, 1 drop four to six times a day at regular intervals. ^{{01} {02} {03} {04} {05} {07} {08} {09} {10} {11} {12} {25}}


Usual adult prescribing limits
Up to 12.8 mg. ^{{08} {09} {10} {11}}

Usual pediatric dose
[Conjunctivitis, seasonal allergic]
Conjunctivitis, vernal¹
Keratitis, vernal¹ or
Keratoconjunctivitis, vernal
Children up to 4 years of age: Safety and efficacy have not been established. ^{{12} {25}}

Children 4 years of age and older: See Usual adult and adolescent dose . ^{12}


Usual geriatric dose
See Usual adult and adolescent dose .

Strength(s) usually available
U.S.—


4% (Rx) [Crolom^{25} (benzalkonium chloride) (edetate disodium) (hydrochloric acid) (sodium hydroxide)]

Canada—


2% (Rx) [Opticrom^{10}{11} (benzalkonium chloride)] [Vistacrom^{08}{09} (benzalkonium chloride 0.01%) (edetate disodium)]

Note: One drop of cromolyn sodium ophthalmic solution 2% contains approximately 0.8 mg of cromolyn sodium; ^{{08} {09} {10} {11}} and one drop of cromolyn sodium ophthalmic solution 4% contains approximately 1.6 mg of cromolyn sodium. ^{{12} {25}}


Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container. Protect from freezing. ^{{13} {25}}

Auxiliary labeling:
   • For the eye.

Revised: 07/10/1995

References

1. Vistacrom package insert (Allergan—Canada), Rec 6/7/88.
   

2. Opticrom (Fisons). In: PDR Physicians' desk reference. 42nd ed. 1988. Montvale, NJ: Medical Economics Data, 1988: 953.
   

3. Opticrom (Fisons). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 23rd ed. Ottawa: Canadian Pharmaceutical Association, 1988.
   

4. Opticrom package insert (Fisons—US), Rev 11/85, Rec 6/30/89.
   

5. Opticrom (Fisons). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 24th ed. Ottawa: Canadian Pharmaceutical Association, 1989: 739.
   

6. Open.
   

7. Opticrom product monograph (Fisons—Canada), Rev 1/5/89, Rec 3/29/90.
   

8. Vistacrom package insert (Allergan—Canada), Rev 1990, Rec 11/93.
   

9. Vistacrom product monograph (Allergan—Canada), Rev 8/88, Rec 8/92.
   

10. Opticrom (Fisons). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 869.
    

11. Opticrom product monograph (Fisons—Canada), Rev 1/89, Rec 9/92.
    

12. Opticrom package insert (Fisons—US), Rev 11/91, Rec 11/93.
    

13. The United States pharmacopeia. The national formulary. USP 22nd revision (January 1, 1990). NF 17th ed (January 1, 1990). Rockville, MD: The United States Pharmacopeial Convention, Inc., 1990: 360.
    

14. Fleeger CA, editor. USAN 1993. USAN and the USP dictionary of drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1992: 174.
    

15. Ostler HB. Acute chemotic reaction to cromolyn. Arch Ophthalmol 1982 Mar; 100: 412-3.
    

16. Allansmith MR, Ross RN. Ocular allergy and mast cell stabilizers. Surv Ophthalmol 1986 Jan/Feb; 30(4): 229-44.
    

17. Foster CS, The Cromolyn Sodium Collaborative Study Group. Evaluation of topical cromolyn sodium in the treatment of vernal keratoconjunctivitis. Ophthalmol 1988 Feb; 95(2): 194-201.
    

18. Kalpaxis JG, Thayer TO. Double-blind trial of pentigetide ophthalmic solution, 0.5%, compared with cromolyn sodium, 4%, ophthalmic solution for allergic conjunctivitis. Ann Allergy 1991 May; 66: 393-8.
    

19. Ciprandi G, Cerqueti PM, Sacca S, Cilli P, Canonica GW. Levocabastine versus cromolyn sodium in the treatment of pollen-induced conjunctivitis. Ann Allergy 1990 Aug; 65: 156-8.
    

20. Caldwell DR, Verin P, Hartwich-Young R, Meyer SM, Drake MM. Efficacy and safety of lodoxamide 0.1% vs cromolyn sodium 4% in patients with vernal keratoconjunctivitis. Amer J Ophthalmol 1992 Jun; 113: 632-7.
    

21. Kudo H, Tanaka T, Miyachi Y, Imamura S. Contact dermatitis from sodium cromoglycate eyedrops. Contact Derm 1988 Oct; 19: 312-3.
    

22. Skarpaas I. An unexpected reaction towards disodium cromoglycate. Allergy 1987; 42: 318-9.
    

23. Sorkin EM, Ward A. Ocular sodium cromoglycate. An overview of its therapeutic efficacy in allergic eye disease. Drugs 1986 Feb; 31(2): 131-48.
    

24. Panel comments, 1/12/94.
    

25. Crolom package insert (Bausch & Lomb—US), Rev 12/94, Rec 6/8/95.
    

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