NEDOCROMIL SODIUM Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Nedocromil sodium is an antiallergic agent with broader mast cell stabilizing
properties than related cromolyn sodium. Administered as an aerosol, it is useful in
the treatment of bronchial asthma and related diseases.
Verwenden
Nedocromil Sodium (Technical Grade) is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma.
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.
Allgemeine Beschreibung
Nedocromil sodium, disodium9-ethyl-6, 9-dihydro-4,6-dioxo-10-propyl-4H-pyrano[3, 2-g]quinoline-2,8-dicarboxylate (Tilade), is structurally relatedto cromolyn and displays similar, but broader, pharmacologicalactions. It was available as an aerosol in ametered-dose inhaler for asthma treatment, and currently remainsavailable as ophthalmic solution for the treatmentof itching associated with allergic conjunctivitis. The inhalationformulation was marketed for maintenance therapyin the management of patients with mild-to-moderatebronchial asthma, but since has been withdrawn.
Pharmakokinetik
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.
Nebenwirkungen
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.
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