69049-74-7 Usage
Description
Nedocromil sodium is an antiallergic agent with mast cell stabilizing properties, which is more effective than cromolyn sodium. It is administered as an aerosol and is useful in the treatment of bronchial asthma and related diseases.
Uses
Used in Pharmaceutical Industry:
Nedocromil sodium is used as a medication for preventing wheezing, shortness of breath, and other breathing problems caused by asthma.
Used in Allergy Treatment:
Nedocromil sodium is used as an anti-allergic agent for prophylactic treatment of allergic reactions.
Used in Mast Cell Stabilization:
Nedocromil sodium is used as a mast cell stabilizer to inhibit IgE-induced histamine release from rat peritoneal mast cells cocultured with 3T3 cells (MC/3T3) and preincubated with IL-2.
Used in Asthma Treatment:
Nedocromil sodium is used to prevent earlyand late-phase bronchoconstriction in a guinea pig model of asthma induced by ovalbumin.
Used in Conjunctivitis Treatment:
Nedocromil sodium is used to prevent conjunctival edema and erythema and reduce mast cell degranulation in a rat model of conjunctivitis when administered intravenously. Formulations containing nedocromil have been used in the treatment of allergic conjunctivitis.
Originator
Fisons (United Kingdom)
Indications
nedocromil sodium(Tilade) is chemically related drugs called chromones that is used for the prophylaxis of mild or moderate
asthma. It is administered by inhalation and has very good safety profiles, making them particularly useful
in treating children.
Therapeutic Function
Antiallergic, Anti-asthmatic
Pharmacokinetics
Nedocromil sodium was developed by changing the furan ring of khellin to a piperidinone ring. In vitro, nedocromil sodium inhibits the release of inflammatory response mediators from a variety of cells, including neutrophils, mast cells, macrophages, and platelets. Inhaled nedocromil sodium is poorly absorbed into the systemic circulation, with approximately 3% of an inhaled dose excreted in the urine during the first 6 hours after administration. Only 2% of orally dosed nedocromil sodium is bioavailable, 89% of which is protein bound. When administered IV, nedocromil sodium is not metabolized and is excreted unchanged in the bile and the urine. Nedocromil sodium is available in aerosol canisters for oral inhalation via a mouthpiece.
Clinical Use
nedocromil sodium is used almost
exclusively for the prophylactic treatment of mild
to moderate asthma and should not be used for the control
of acute bronchospasm. This agent is effective
in about 60 to 70% of children and adolescents with
asthma. Unfortunately, there is no reliable means to
predict which patients will respond.It is less effective
in older patients and in patients with severe
asthma. It may take up to 4 to 6 weeks of treatment for
cromolyn sodium to be effective in chronic asthma, but
it is effective after a single dose in exercise-induced
asthma. With respect to clinical efficacy, cromolyn
sodium and nedocromil sodium do not differ in a substantial
way.
Side effects
nedocromil sodium is the least
toxic of available therapies for asthma. Adverse reactions
are rare and generally minor. Those occurring in
fewer than 1 in 10,000 patients include transient bronchospasm,
cough or wheezing, dryness of throat, laryngeal
edema, swollen parotid gland, angioedema, joint
swelling and pain, dizziness, dysuria, nausea, headache,
nasal congestion, rash, and urticaria.
Check Digit Verification of cas no
The CAS Registry Mumber 69049-74-7 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,9,0,4 and 9 respectively; the second part has 2 digits, 7 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 69049-74:
(7*6)+(6*9)+(5*0)+(4*4)+(3*9)+(2*7)+(1*4)=157
157 % 10 = 7
So 69049-74-7 is a valid CAS Registry Number.
InChI:InChI=1/C19H17NO7.2Na/c1-3-5-9-16-10(13(21)7-12(18(23)24)20(16)4-2)6-11-14(22)8-15(19(25)26)27-17(9)11;;/h6-8H,3-5H2,1-2H3,(H,23,24)(H,25,26);;/q;2*+1/p-2
69049-74-7Relevant articles and documents
New Antiallergic Pyranoquinoline-2,8-dicarboxylic Acids with Potential for the Topical Treatment of Asthma
Cairns, Hugh,Cox, David,Gould, Ken J.,Ingall, Anthony H.,Suschitzky, John L.
, p. 1832 - 1842 (2007/10/02)
A nimber of antiallergic pyranoquinolinedicarboxylic acid derivatives with potential for the topical treatment of asthma have been synthesized.All the compounds have been evaluated against rat passive cutaneous anaphylaxis and in a dog hypotension screen.This is the first detailed description of the application of the latter screen for the identification of antiallergic agents.Two compounds, disodium 9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyranoquinoline-2,8-dicarboxylate (86) and disodium 6-(methylamino)-4-oxo-10-propyl-4H-pyranoquinoline-2,8-dicarboxylate (72), were selected and further evaluated for their ability to induce phosphorylation of a 78000 molecular weight protein associated with the rat peritoneal mast cell.Their ability to inhibit histamine release from these cells and from a mucosal mast cell preparation has also been evaluated.These compounds, nedocromil sodium (TILADE 86) and minocromil (the free acid of 72), are at present undergoing therapeutic evaluation.The rationale for the screening procedure and the relevance of the second carboxylic acid function of these dibasic acids to receptor binding are discussed.
