Cromolyn

468.37

468.37

240-279-8

Y0TK0FS77W

DTXSID4022860

C61691

Colorless crystals from ethanol + ether

S01GX01|A - Alimentary tract and metabolism|D - Dermatologicals|R - Respiratory system|S - Sensory organs

2922499990

166

1.6

Hygroscopic white powder

1.623

241-242 °C (decomp)

752.3±60.0 °C(Predicted)

263.9ºC

1.681

3.58e-02 g/L

Oral cromolyn sodium capsules should be stored in tight containers at 15 to 30 deg C. Capsules containing cromolyn sodium powder for oral inhalation should be stored at room temperature in tight, light-resistant containers; exposure to excessive moisture and to temperatures greater than 40 deg C should be avoided. Cromolyn sodium aerosol for oral inhalation should be stored at 2 to 30 deg C. /Cromolyn sodium/

1.08E-23mmHg at 25°C

1.1|pKa= 1.10

HIGHLY POLAR; LIPID-SOLUBLE @ PKA= 1.9 /CROMOLYN DISODIUM/

Water soluble.

Acids, Carboxylic

Carboxylic acids donate hydrogen ions if a base is present to accept them. They react in this way with all bases, both organic (for example, the amines) and inorganic. Their reactions with bases, called "neutralizations", are accompanied by the evolution of substantial amounts of heat. Neutralization between an acid and a base produces water plus a salt. Carboxylic acids in aqueous solution and liquid or molten carboxylic acids can react with active metals to form gaseous hydrogen and a metal salt. Such reactions occur in principle for solid carboxylic acids as well, but are slow if the solid acid remains dry. Even "insoluble" carboxylic acids may absorb enough water from the air and dissolve sufficiently in it to corrode or dissolve iron, steel, and aluminum parts and containers. Carboxylic acids, especially in aqueous solution, also react with sulfites, nitrites, thiosulfates (to give H2S and SO3), dithionites (SO2), to generate flammable and/or toxic gases and heat.

2

36/37/38

26-36

DJ2380000

Xi

VERY STABLE WITH NO DEGRADATION UNDER NORMAL STORAGE CONDITIONS EXCEPT FOR MOISTURE GAIN /DISODIUM/

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

Lourwood DL; Am Pharm 35 (6): 16-24 (1995). Treatment of chronic diseases during pregnancy.|Zsamboki G; East Pharm 38: 41-4 (1995). Pharmacology of sodium cromoglycate.|Sly RM; Ann Allergy 73 (5): 439-43 (1994). Changing asthma mortality and sales of inhaled bronchodilators and anti-asthmatic drugs.|Boulet LP; Rev Mal Respir 9 (1): 99-101 (1992). Review of North American studies on nedocromil sodium.

Flash point data for this chemical are not available. It is probably combustible. (NTP, 1992)

Fires involving this material can be controlled with a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)

STORAGE PRECAUTIONS: You should store this material in a refrigerator. (NTP, 1992)

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

Symptoms of overdose include cough, nasal congestion, nausea, sneezing and wheezing.

Studies demonstrating a lack of ion pair formation between sodium cromoglycate (cromolyn sodium) and alkylbenzdimethylamonium ions in rat intestine are briefly discussed. /Cromolyn sodium/|An analysis of the absorption and desorption isotherms for sodium cromoglycate (cromolyn sodium) and cromolyn sodium lactose moisture uptake is presented. Up to 15% moisture content had no effect on the tensile and shear properties of cromolyn sodium, due to adsorption into the interior of cromolyn sodium, leaving little absorbed moisture on the surface of the particles.|The mechanism of action of the mast cell stabilizers sodium cromoglycate and FPL-52694 as protective agents against ethanol induced gastric mucosal damage was investigated in the rat. Using an ex vivo gastric chamber model, various concn (l0-80 mg/ml) of the two agents were applied to the gastric mucosa prior to exposure to 40% ethanol. Both agents significantly reduced ethanol induced damage in a dose dependent manner. When given orally (80 mg/kg) both agents significantly reduced gastric damage induced by subsequent oral administration of absolute ethanol. Pretreatment with indomethacin did not significantly affect the protection afforded by FPL-52694, but did cause a partial reversal of the protective effect of sodium cromoglycate. Changes in gastric leukotriene C4 synthesis did not correlate with the protective effects of the two agents. Both mucosal and connective tissue mast cell numbers were significantly reduced following oral ethanol administration. In the groups pretreated with FPL-52694 or sodium cromoglycate, mucosal mast cell numbers were not significantly different from those in rats not treated with ethanol. Furthermore, the connective tissue mast cell numbers were significantly lower than in ethanol treated control rats, despite a greater than 95% reduction of ethanol induced hemorrhagic damage. These results therefore suggest that stimulation of gastric prostaglandin synthesis is not important in the mechanism of action of FPL-52694, and neither agent appears to reduce damage through a mechanism related to effects on gastric leukotriene C4 synthesis. The present studies further suggest that the protection afforded by pretreatment with sodium cromoglycate or FPL-52694 may be unrelated to effects of these agents on the connective tissue mast cell population in the stomach. /Sodium cromoglycate/|The effect of histamine on the absorption and clearance of inhaled cromolyn sodium (sodium cromoglycate) was examined in 7 mildly asthmatic patients with hyperresponsive airways and 8 normal subjects who inhaled either placebo or histamine followed by cromolyn. In the asthmatic group histamine inhalation led to a mean 24% reduction in the forced expiratory volume in 1 second but had no effect on the normal subjects. When compared with the inhaled placebo, histamine incr the initial pulmonary absorption of cromolyn without influencing the total amount of drug absorbed in both asthmatics and normals. These observations suggest that the pharmacokinetics of the inhaled drug may be altered significantly by inflammatory mediators present at the site of drug absorption from the airways. /Cromolyn sodium/|For more Interactions (Complete) data for CROMOLYN (9 total), please visit the HSDB record page.

For the management of patients with bronchial asthma. Also used in the treatment of vernal keratoconjunctivitis, vernal conjunctivitis, and vernal keratitis.

Anti-Asthmatic Agents|A LARGE PROPORTION OF CHILDREN WITH CHRONIC, INTRACTABLE ASTHMA (MILD OR SEVERE) EXPERIENCE EITHER PARTIAL OR COMPLETE PROTECTION AFTER ORAL INHALATION OF CROMOLYN. /CROMOLYN DISODIUM/|...EVIDENCE APPEARS TO INDICATE THAT PATIENTS WITH EXTRINSIC ASTHMA /KNOWN HYPERSENSITIVITY TO AN EXTRINSIC ALLERGEN/ ARE MORE LIKELY TO RESPOND TO CROMOLYN THAN PATIENTS WITH INTRINSIC ASTHMA /NO SUCH HYPERSENSITIVITY KNOWN/. HOWEVER, IT IS NOT CURRENTLY POSSIBLE TO PREDICT WHICH PATIENTS WILL RESPOND SATISFACTORILY TO CROMOLYN. /CROMOLYN DISODIUM/|THE INHALATION OF CROMOLYN SHORTLY BEFORE EXERCISE LESSENS BRONCHOCONSTRICTION THAT SOME ASTHMATIC PATIENTS THEN DEVELOP. THIS EFFECT MAY BE ENHANCED IF PATIENT IS RECEIVING CONTINUOUS THERAPY. /CROMOLYN DISODIUM/|For more Therapeutic Uses (Complete) data for CROMOLYN (20 total), please visit the HSDB record page.

ANAPHYLAXIS, VASCULITIS, OR OTHER SERIOUS ADVERSE EFFECTS HAVE NOT BEEN REPORTED IN MAN. URTICARIA & MACULOPAPULAR RASHES HAVE OCCURRED RARELY BUT HAVE CLEARED WHEN DRUG WAS WITHDRAWN. EOSINOPHILIC PNEUMONIA HAS BEEN ASSOCIATED WITH /INHALATION/ ADMIN OF CROMOLYN IN TWO PATIENTS. /DISODIUM/|DESCRIBED IS A 42 YR OLD MALE PATIENTS WHO DEVELOPED SEVERE BRONCHOCONSTRICTION AFTER INHALING SODIUM CROMOGLYCATE (CROMOLYN).|A STUDY OF THE FREQUENCY OF ADVERSE REACTIONS (DERMATITIS, MYOSITIS, GASTROENTERITIS) TO CROMOLYN SODIUM, 0.5%, IN 375 ASTHMATIC PATIENTS, IS PRESENTED. THE FREQUENCY RATES WERE FOUND TO BE 2%; REACTIONS WERE NONLIFE THREATENING & COMPLETELY REVERSIBLE.|SEVERE NASAL CONGESTION DEVELOPED IN 13 YR OLD ASTHMATIC PATIENTS AFTER 4 WK OF THERAPY WITH CROMOLYN & DISAPPEARED WITHIN 24 HR OF DISCONTINUANCE OF THERAPY. REACTION OCCURRED AGAIN WHEN REINITIATION OF CROMOLYN WAS ATTEMPTED 3 DAYS & 3 WEEKS AFTER FIRST ATTACK.|For more Drug Warnings (Complete) data for CROMOLYN (25 total), please visit the HSDB record page.

CONTROLLED & UNCONTROLLED STUDIES ON LONG-TERM USE OF CROMOLYN IN CHILDREN & ADULTS INDICATE THAT TOLERANCE USUALLY DOES NOT DEVELOP, THAT INTOLERANCE DOES NOT OCCUR, & THAT ADULTS CAN ADJUST THE DOSE IN A RESPONSIBLE MANNER. /CROMOLYN DISODIUM/

Cromoglicate or cromolyn (USAN), a synthetic compound, inhibits antigen-induced bronchospasms and, hence, is used to treat asthma and allergic rhinitis. Cromoglicate is used as an ophthalmic solution to treat conjunctivitis and is taken orally to treat systemic mastocytosis and ulcerative colitis.

Drugs that are used to treat asthma. (See all compounds classified as Anti-Asthmatic Agents.)|Compounds that prevent the release of inflammatory mediators from MAST CELLS. (See all compounds classified as Mast Cell Stabilizers.)

1%|MOST OF ABSORBED DRUG IS EXCRETED UNCHANGED BY LIVER & KIDNEYS WITHIN A FEW DAYS & NONE APPEARS TO UNDERGO METABOLIC DEGRADATION. THE UNABSORBED PORTION (APPROX 80%) IS RECOVERABLE FROM FECES. FOLLOWING INHALATION, MAX PLASMA LEVEL...REACHED WITHIN SEVERAL MIN, & PLASMA T1/2 IS ONE TO ONE-HALF HOURS. /CROMOLYN DISODIUM/|THE AMT OF CROMOLYN...ABSORBED INTO BLOODSTREAM FOLLOWING INHALATION OF A DOSE OF 20 MG DOES NOT APPEAR TO EXERT ANY GENERALIZED PHARMACOLOGIC EFFECTS. /CROMOLYN DISODIUM/|THE SMALL AMT OF CROMOLYN THAT IS ABSORBED IS EXCRETED UNCHANGED BY LIVER & KIDNEYS... APPROX 10% OF A 20% MG DOSE...MAY REMAIN IN INHALER AFTER PATIENTS /USE/ &...APPROX 8% OF DOSE IS ABSORBED INTO BLOODSTREAM (PRIMARILY BY LUNG BUT ALSO BY GI TRACT). /CROMOLYN DISODIUM/|FATE OF CROMOLYN WAS EXAMINED IN 12 ASTHMATIC PATIENTS. MAX PLASMA CONCN (MEAN 9.2 NG/ML OBTAINED WITHIN 15 MIN OF INHALING 20 MG). ABSORPTION FROM LUNG IS RAPID, MOST OF INHALED DOSE IS SWALLOWED.|For more Absorption, Distribution and Excretion (Complete) data for CROMOLYN (10 total), please visit the HSDB record page.

NO METABOLITES WERE DETECTED IN MAN & IN NINE MAMMALIAN SPECIES AFTER ORAL & IV ADMIN. /CROMOLYN DISODIUM/

1.3 hours|FATE OF CROMOLYN WAS EXAMINED IN 12 ASTHMATIC PATIENTS. AVG PLASMA T/2 WAS 81 MIN.

Cromoglicate inhibits degranulation of mast cells, subsequently preventing the release of histamine and slow-reacting substance of anaphylaxis (SRS-A), mediators of type I allergic reactions. Cromoglicate also may reduce the release of inflammatory leukotrienes. Cromoglicate may act by inhibiting calcium influx.|One important action of cromolyn is believed to be the inhibition of pulmonary mast cell degranulation in response to a variety of stimuli, including the interaction between cell-bound IgE and specific antigen. ... The release of histamine and other granular contents, as well as the production of leukotrienes, can be shown to be markedly reduced in vitro by cromolyn. However, its efficacy and potency are highly dependent on the source of the mast cells.|... Attention has been focused on the ability of cromolyn to reverse various functional changes in leukocytes obtained from the blood of asthmatic subjects undergoing allergen challenge, such as increased expression of membrane-bound receptors.|... Low concentrations (100 nM) of cromolyn can suppress completely the activation effects of chemoattractant peptides of human neutrophils, eosinophils, or monocytes.|The mechanisms of action of cromolyn remain relatively poorly defined. Most attention has been focused on the ability of cromolyn to reduce the accumulation of intracellular Ca +2 induced by antigen in sensitized mast cells. One biochemical correlate of the reduction of histamine release from mast cells by cromolyn is the enhanced phosphorylation of a 78,000-dalton protein. Unfortunately, these observations have been made using rather high concn of cromolyn (50 to 200 uM), and their relationship to therapeutic response has yet to be established.|For more Mechanism of Action (Complete) data for CROMOLYN (6 total), please visit the HSDB record page.

SYMPTOMS: Symptoms of exposure to this compound may include irritation of the skin, eyes and mucous membranes; brochospasm, laryngeal edema, rash, and dysuria. ACUTE/CHRONIC HAZARDS: This compound is an irritant. (NTP, 1992)

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. IMMEDIATELY transport the victim after flushing eyes to a hospital even if no symptoms (such as redness or irritation) develop. SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment. INHALATION: IMMEDIATELY leave the contaminated area; take deep breaths of fresh air. If symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop, call a physician and be prepared to transport the victim to a hospital. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be used; if not available, use a level of protection greater than or equal to that advised under Protective Clothing. INGESTION: DO NOT INDUCE VOMITING. If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Be prepared to transport the victim to a hospital if advised by a physician. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

...CROMOLYN IS VIRTUALLY NONTOXIC. ACUTE OVERDOSAGE HAS NOT BEEN REPORTED &, OTHER THAN A FEW ALLERGIC REACTIONS, SERIOUS ADVERSE EFFECTS APPEAR RARE. /CROMOLYN DISODIUM/

Aarane

DSCG, SODIUM CHROMOGLYCATE /CROMOLYN DISODIUM/|CROMOLYN SODIUM SALT /CROMOLYN DISODIUM/|Cromolyn sodium, disodium cromoglycate, DSCG, FPL-670, Aarane, Alercrom, Alerion, Allergocrom, Colimune, Cromovet, Fivent, Gastrofrenal, Inostral, Intal, Introl, Irtan, Lomudal, Lomupren, Lomusol, Lomuspray, Nalcrom, Nalcron, Nasalcrom, Nasmil, Opticrom, Opticron, Rynacrom, Sofro, Vividrin /Cromolyn disodium/

US PATENT 3,419,578. /CROMOLYN DISODIUM/|Available commercially as the disodium salt.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals