Lodoxamide tromethamine

Contraindications Wearing soft contact lenses (product contains benzalkonium chloride), hypersensitivity to lodoxamide tromethamine or any component of the formulation... 

Mast cell stabilizers include cromolyn sodium 4% (Opticrom, Crolom) and lodoxamide tromethamine 0.1% (Alomide), which are currently approved by the U.S. Food and Drug Administration for VKC but offer off-label relief for allergic conjunctivitis. Other mast cell stabilizers include pemirolast (Alamast) and nedocromil sodium 2% (Alocril), with both approved for treatment of itching in allergic conjunctivitis. Perennial allergic conjunctivitis may be treated with mast cell stabilizers year round. 

The anti-allergy drugs, cromolyn sodium and lodoxamide tromethamine show in vitro dose responses which are bell-shaped or biphasic in mast cells. The nature of the biphasic dose response is poorly understood however, through the use of specific antagonists it has been possible to show that at the high concentrations of these drugs leading to enhanced histamine release or... 

The Effect of Muscarinic Blockers on the DSCXS and Lodoxamide Tromethamine Dose Response in Rat Mast Cell... 

The cholinergic stimulation by lodoxamide tromethamine was time and dose-related. Both inhibition of mediator release (5 yg/ml) and high-dose enhancement of release (500 yg/ml) were near maximal at 4 to 10 min (Fig. 2). The high dose also caused the accumulation of cGMP in P815 mastocytoma cells and the time of maximal stimulation was 6 to 12 min after < rug was added (27). 

The Effect of Pretreatment of Rats with the Muscarinic Blockers Atropine and QuinuclicHnyl Benzilate (QNB) on Multiple Dose DS and Lodoxamide Tromethamine Tachyphylaxis... 

Rats dosed twice with inhibiting doses of either DSCG or lodoxamide tromethamine show tachyphylaxis to an inhibition of the subsequent passive cutaneous anaphylaxis assay (10.11,13 16,17). Atropine (25 mg/kg) or QNB (0.01 mg/kg) given ip 20 min prior to the first iv dose of DSCG or lodoxamide, partially blocked this multiple dose tachyphylaxis (13,16,17,27). Atropine or QNB by themselves at these concentrations had no inhibitory effect on the PCA reaction, but markedlv reduced (or almost totally eliminated) the tachyphylaxis (Fig. 3,4) to DSCG and to a lesser... 

These data indicate that DSCG and lodoxamide tromethamine exhibit biphasic dose responses for inhibition of mediator release and that both a portion of the bell-shaped curve and a part of the multiple dose tachyphylaxis can be blocked by prior treatment with atropine. 

Comparison Be en Cromolyn Sodium and Lodoxamide Tromethamine in imates Against Aerosolized Ascaris suum Antigen. 

We have reported studies on the effect of drugs on various lung parameters induced by Ascaris sensitivity (17.22). We quantitated these parameters and adapted the syston to test cromolyn Na by aerosol and intravenous administration as well as lodoxamide tromethamine. Lodoxamide tromethamine in this assay showed quantitative advantages to cromolyn Na (DSCX3) because it was significantly more active and was orally adsorbed. 

When lodoxamide tromethamine was administered orally to reactor Ascaris monkeys, excellent inhibition of both lung function parameters was seen Indicating a reversal of antigen challenge induced changes. Table 11 summarizes the activity of lodoxamide tromethamine and its duration of effect vAien dosed orally. This table also shows that when the optimal time (30 min.) is used to assay a dose response, inhibition can be seen as low as 5.0 mg/kg. Table 12 shows that when lodoxamide tromethamine was administered i.v. 5 min. before ascaris aerosolization (0.16 ml aerosolized in 50 respirations), protection was seen even at 0.001 mg total dose per animal (Table 13). 

Multiple doses of DSCG and other similar conpounds have been shown to develop a time and dose related period of tachyphylaxis in rats and primates, (12. 17. 23). Lodoxamide tromethamine also showed a similar phenomenon when multiple oral doses of 50 mg/kg were given (Table 14). Tachyphylaxis was evident if a hi dose (50 mg/kg) preceded a similar hi dose. Several low doses (0.1 mg/kg) appeared to give good inhibition in this assay. 

D. Hunan Clinical Studies With Lodoxamide Tromethamine. 

The promising animal studies with lodoxamide tromethamine led to its investigation in hunan subjects. TVio independent broncho-provocation studies in patients with extrinsic bronchial asthma have been reported. Moreno and LeZotte (24) studied 12 j tients, who had been pretreated randomly with inhaled lodoxamide tromethamine (1.0 mg, 0.1 mg, 0.01 mg) or placebo in a double blind manner, in a standard bronchial challenge. Each of the j tients was treated with each drug dose and placebo in separate settings... 

In a similar study, Townley and co-workers (25.26) challenged 10 extrinsic asthmatics with increasing amounts of allergen after pretreatment with inhaled placebo or lodoxamide tromethamine (1.0 mg, 0.1 mg, and 0.01 mg) in a randomized double blind fashion. Statistical analysis of the results demonstrated that the cumulative log dose of allergen which produced a 15% drop in FEVi (PD15) was 2-65 greater for all three drug doses than for placebo. 

Studies are being undertaken to determine the efficacy of lodoxamide tromethamine in exercise induced bronchospasm, allergic rhinitis and various skin allergies. 

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