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At least 19 recordsLinked to original sources
PubMed1986

Treatment of duodenal ulcers with ethoxzolamide, an inhibitor of gastric mucosa carbonic anhydrase.

Duodenal ulcer healing was followed by endoscopy in 186 ethoxzolamide-treated patients. Ethoxzolamide was given in doses of 5-10 mg/kg body weight/day in association with Na and K salts to avoid electrolytic losses. A control group of 161 duodenal ulcer patients received the usual doses of antacids and anticholinergics. The clinical course of pain, inhibition of gastric acid secretion and endoscopic healing of ulcers after 15 and 21 days of treatment were followed, together with the incidence of relapses over a 2-year period. Pain disappeared after 4-6 days of treatment in 91% of the ethoxzolamide-treated group and in 13% of the controls. After 10 days of treatment, ethoxzolamide reduced basal HCl output by 98%, in the control no significant secretory changes were recorded. Endoscopy showed healing in 92% of the cases after 15 days of treatment with ethoxzolamide and in 98% after 21 days; in controls, the corresponding figures were 36% and 46% respectively. Relapse rate after 6 months was 5% in the ethoxzolamide-treated patients and 38% in controls; after one year, relapses were endoscopically confirmed in 7% of the cases in the first group and in 51% respectively in controls; the same rate was 11% and 79% respectively after 2 years. Ethoxzolamide is superior to antacids and anticholinergics in healing duodenal ulcers.

Adult↗
PubMed1992

Relations among IOP reduction, ocular disposition and pharmacology of the carbonic anhydrase inhibitor ethoxzolamide.

We have measured sequentially the concentrations of ethoxzolamide (6-ethoxybenzothiazole-2-sulfonamide) in ocular tissues following its intravenous or topical administration to normal albino rabbits. This was done in parallel with determinations of intraocular pressure (IOP) measured by tonometer or direct manometry. Ethoxzolamide was used because of its very high activity against carbonic anhydrase and experience showing that there is little or no other receptor in tissues. During the course of these experiments it was discovered that the lipid-soluble ethoxzolamide is converted in vivo to a water-soluble metabolite, while retaining high activity against the enzyme. Presumably this is the 6-O-glucuronide adduct. At the minimal dose for maximal effect (4 mg kg-1 i.v. at 45 min) the IOP lowering was 4.2 mmHg, the concentration in anterior uvea was 2.5 mumol kg-1, and the fractional inhibition of the enzyme (i) was 0.9995. The effect of free drug in the anterior uvea and other tissues. Following topical administration i was measured as a function of drug and enzyme in ciliary process. IOP lowering at 1 hr was -1.9 mmHg and i = 0.9993. By 4 hr i = 0.9980 and the pharmacological effect disappeared. At 8 hr the concentration of ethoxzolamide in the ciliary process is 0.4 mumol kg-1, essentially that of enzyme, with no free drug present: drug is now a marker for enzyme. Ethoxzolamide also labels the red cell carbonic anhydrases in the rabbit as well as other species including man. There appears to be no ethoxzolamide receptor other than carbonic anhydrase.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1978

[Clinical tests on the use of ethoxzolamide in glaucoma therapy (author's transl)].

Ethoxzolamide is a potent carboxyanhydrase inhibitor, and its use in chronic glaucoma and in the acute glaucoma attack is described in the present investigation. Ethoxzolamide shows itself to be extremely well tolerated. The frequency and intensity of the side-effects is low. The electrolyte balance remains also after prolonged administration compensated. The important advantage of this drug is its low dosability. Ethoxzolamide, which was already 1958 clinically evaluated (Gordon-Posner), represents a valuable medication for conservative glaucoma therapy.

Drug Evaluation↗
PubMed1984

Determination of ethoxzolamide in the iris/ciliary body of the rabbit eye by high-performance liquid chromatography: comparison of tissue levels following intravenous and topical administrations.

A specific high-performance liquid chromatographic method is described for ethoxzolamide following the extraction of the material from iris/ciliary body eye tissue in rabbits. The steps consist of base extraction and protein and enzyme deactivation, followed by acid treatment, extraction into ethyl acetate, evaporation, and solubilization with a 50% aqueous methanol solution. The samples were chromatographed on a reverse-phase phenyl column with a mobile phase consisting of 50% methanol in 1% acetic acid. The recovery was 74.3% over a 10-fold range of tissue concentrations. The sensitivity was 0.03 microgram/mL, and the response was linear over the concentration range (0.03-0.5 microgram/mL) used in the study. Intravenous (2.0- and 6.0-mg/kg) and topical (1% suspension) doses of ethoxzolamide were administered to rabbits. Iris/ciliary body tissues were excised 45 min after drug administration. The tissue levels after a dose of 6 mg/kg were statistically greater than the levels obtained after a dose of 2 mg/kg. The smaller intravenous dose represented the lowest dose for which a reduction in intraocular pressure could be measured. An initial transitory drop in intraocular pressure was detected for the topical dose. Iris/ciliary body levels in the treated eye could be detected for the 2-mg/kg iv and topical doses.

Administration, Topical↗
PubMed1985

Topical carbonic anhydrase inhibitors. III: Optimization model for corneal penetration of ethoxzolamide analogues.

An analogue series representing modification to the benzene ring of ethoxzolamide has been evaluated for solubility, pKa, partitioning, and permeability across excised rabbit corneas. These physical parameters were correlated to Hammett sigma (para) and/or Hansch pi parameter values for each compound. From these correlations, a mathematical model was developed relating corneal permeability to molecular modifications of ethoxzolamide. A three-dimensional plot of maximum attainable penetration rate versus sigma (para) and pi yielded an optimal range of pi and sigma values from which an optimally penetrating analogue could be designed.

Absorption↗
PubMed1984

Ethoxzolamide analogue gel. A topical carbonic anhydrase inhibitor.

An analogue of ethoxzolamide, 6-hydroxyethoxzolamide, was synthesized to enhance corneal permeability yet retain carbonic anhydrase inhibitory activity for use in lowering intraocular pressure. In a 1% suspension, the analogue caused a small but statistically significant unilateral reduction of IOP when applied to one eye of normal rabbits. When formulated in a gel vehicle, 6-hydroxyethoxzolamide caused a more prolonged and larger reduction in IOP in normal and ocular hypertensive rabbits compared with its effect in suspension or with the parent compound.

Animals↗
PubMed1958

[ETHOXZOLAMIDE].

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Ethoxzolamide↗
PubMed1987

Inhibition of mitochondrial carbonic anhydrase and ureagenesis: a discrepancy examined.

The amount of urea synthesized in intact guinea pig hepatocytes in 60 min ([urea]t=60), was determined at 37 degrees C in Krebs-Henseleit buffer plus (in mM) 10 NH4Cl, 5 lactate, and 10 ornithine in 5% CO2-95% O2. The concentrations of sulfonamide carbonic anhydrase (CA) inhibitors required to reduce the rate of urea synthesis by 50% (I50) were (in mM): 0.07 ethoxzolamide, 0.5 methazolamide, 0.7 acetazolamide, and 5.0 p-aminomethylbenzenesulfonamide. At 37 degrees C acetazolamide and ethoxzolamide reduced citrulline synthesis by intact mitochondria in medium containing (in mM) 50 3-(N-morpholino)propanesulfonic acid, 35 KCl, 5 KH2PO4, 2 adenosine triphosphate, 10 ornithine, 10 NH4Cl, 1 [ethylene-bis(oxyethylenenitrile)]tetraacetic acid, 1 MgCl2, 20 pyruvate, and 25 KHCO3 (pH 7.4) in 5% CO2-95% O2; the inhibition by ethoxzolamide was not decreased greater than 50%; 25% inhibition was achieved by 0.65 microM ethoxzolamide. Inhibition constant (Ki) values for CA activity of disrupted mitochondria at 37 degrees C were 0.03 microM ethoxzolamide and 0.16 microM acetazolamide, and for disrupted hepatocytes were 150 microM ethoxzolamide and 50 microM acetazolamide. p-Aminomethylaminosulfonamide-affinity column purification yields one band of 29,000 mol wt for CA V purified from disrupted mitochondria; homogenized whole-liver supernatant yields an additional band of 20,000 mol wt (at greater than 100 times the concentration of CA V), which has some glutathione S-transferase activity. It is concluded that this 20,000-mol wt protein modifies the potency of ethoxzolamide in the liver cytosol.

Acetazolamide↗