Mast cell stabilizers bronchial asthma

Drugs given by this route are quickly absorbed, which takes place from the vast surface of alveoli and produce rapid action. Various bronchodilators and mast cell stabilizers are used in the treatment and prophylaxis of bronchial asthma i.e. salbutamol (ASTHALIN) and sodium cromoglycate (FINTAL) inhaler. 

Like mast cell stabilizer, corticosteroids do not relax airway smooth muscle directly but reduce bronchial reactivity, increase airway caliber, suppress inflammatory response to antigen antibody reaction or trigger stimuli and reduce the frequency of asthma exacerbations. They produce more sustained symptomatic relief than any bronchodilator and mast cell stabilizer. 

Indications Bronchial asthma, pruritus of allergic conjunctivitis Category Mast cell stabilizer Half-life 3.3 hours... 

Cromolyn sodium (inhalation 20 mg/2 mL), Intal in capsules (20 mg for inhalation only), solution (20 mg per amp for nebulizer only), and aerosol spray (delivers 800 meg), Nasalcrom (nasal solution in 40 mg/mL), and Gastrocom (100 mg capsule for oral administration) are used for prophylactic management of severe bronchial asthma. As an antiasthmatic, antiallergic, and mast cell stabilizer, cromolyn has no bronchodilating, antiinflammatory, anticholinergic, or vas-oconstricting properties. 

Mast cells release histamines, leukotrienes and other mediators of the inflammatory process. Mast cell stabilizer drugs inhibit the early asthmatic response and the late asthmatic response. They have no bronchodilator effect nor do they have any effect on any inflammatory mediators already released in the body. They are indicated for the prevention of bronchospasms and bronchial asthma attacks. They are administered by aerosol inhalation. The exact action of the drugs have not been determined. However, they are believed to have a modest effect in lowering the required dose of corticosteroids. The most common mast stabilizer dmgs are cromolyn (Intal) and nedocromil (Tilade). 

Stabilization of mast cells. Cromolyn prevents IgE-mediated release of mediators, although only after chronic treatment. Moreover, by interfering with the actions of mediator substances on inflammatory cells, it causes a more general inhibition of allergic inflammation. It is applied locally to conjunctiva, nasal mucosa, bronchial tree (inhalation), intestinal mucosa (absorption almost nil with oral intake). Indications prophylaxis of hay fever, allergic asthma, and food allergies. 

There is some evidence that children under five years of age obtain benefit from use of nedocromil sodium or sodium cromoglicate. These agents are used only in prophylaxis cromoglicate is not a bronchodilator and cannot be used to treat acute episodes of asthma. Its action is not well understood but the prophylactic effect appears to be partly due to stabilization of mast cells, which reduces release of histamine and other mediators so that hyperactive bronchial muscle is less responsive to environmental triggers. 

Nedocromil, 9-Etkyl-6,tFdihydrO-4,6 ioxo-IO-propyl-4H-pyrano[3,2-g]qu i notine-2, H-dicarboxylic acid 4,6-dioxo-1 -ethyl-10-propyl-4H,6H-pyrano[3,2-g]quinotlne-2,8-dicar boxy lie acid FPL 59002. C HpNO, mol wt 371.35. C 61.45%, H 4.61%, N 3.77%, O 30.16%. Anti-aller-gic compound with the ability to stabilize both mucosal and connective tissue mast cells. Prepn and pharmacology H. Cairns, D. Cox. Belg. pat. 866,622 eidem, U.S. pat. 4,474,-787 (1978, 1984 both to Fisons) H. Cairns et at, J. Med. Chem. 28, 1832 (1985). Prevention of histamine release from mast celts, inhibition of Monchoconstriction in monkeys R. P. Eady et at.. Bril. J. Pharmacol 85, 323 (1985). Early clinical trial in bronchial asthma S. Lai et al. Thorax 39, 809 (1984). 

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