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At least 19 recordsLinked to original sources
PubMed1984

Topical ocular hypotensive activity and ocular penetration of dichlorphenamide sodium in rabbits.

A single topical instillation (50 microliter) of the water soluble sodium salt of dichlorphenamide (10%) produced a pronounced and prolonged lowering of intraocular pressure (IOP), compared to suspensions of its free acid, in rabbits with alpha-chymotrypsin-induced ocular hypertension. In normal rabbits, instillation of dichlorphenamide sodium also produced a markedly elevated drug aqueous humor level relative to instillation of its free acid, indicating enhanced penetration into the eye. The IOP response after ocular instillation of dichlorphenamide sodium was equivalent to that produced by oral administration of 6 or 18 mg/kg dichlorphenamide sodium. Serum drug levels were lower and aqueous humor and iris-ciliary body levels were higher after instillation of dichlorphenamide sodium (10%) than after oral administration of 2 or 6 mg/kg. The data indicate that topically instilled dichlorphenamide sodium is capable of lowering IOP by a local action in the eye and provides a rationale for the potential utility of topical carbonic anhydrase inhibitors as a therapy for glaucoma in man.

Administration, Topical↗
PubMed1976

[Dichlorphenamide treatment in acute glaucoma (author's transl)].

Dichlorphenamide as well as Diamox lowers intraocular pressure. For adequate treatment of acute glaucoma only 20% of commonly used Diamoxdosis is requested to reach comparable pressure release two hours later. After one hour control intraocular pressure of 60% from patients with Dichlorphenamide treatment was found below 40 mm Hg since in Diamoxgroup there were only 30% below 40 mm Hg. Different effects of Dichlorphenamide and Diamox after one hour use is demonstrated in respect of serum electrolytes and base excess as well. Essential side effects after a single dosis of 200 mg Dichlorphenamide or in combination with Diamox for acute glaucoma treatment could not be observed.

Acetazolamide↗
PubMed1966

Effect of dichlorphenamide on gas exchange and CSF acid-base state in chronic respiratory failure.

Dichlorphenamide was administered to 13 patients with chronic respiratory failure, and the effects on gas exchange at rest and during exercise and on the acid-base state of CSF were observed. The ventilation for a given level of CO(2) production was increased both at rest and during exercise, resulting in an increased arterial Po(2) and decreased Pco(2).The ventilatory stimulation paralleled the development of a metabolic acidosis but was not associated with tissue CO(2) accumulation. Indeed, CSF Pco(2) and the oxygenated mixed venous (rebreathing) Pco(2) fell by the same amount as arterial Pco(2). The level of CO(2) elimination after two minutes of exercise was as great for a given work load after dichlorphenamide as before. These findings do not support the view that the drug impairs CO(2) transport from tissues either at rest or during exercise. They are most consistent with the view that the primary locus of action of dichlorphenamide in therapeutic doses is the kidney. The metabolic acidosis which results is likely the basis of the respiratory stimulatin, perhaps by its effects on the CSF H(2)CO(3)-HCO(3) - system. Inhibition of carbonic anhydrase in the red cell and choroid plexus are probably unimportant effects.

Acidosis↗
PubMed1979

Electron-capture GLC assay of dichlorphenamide.

GLC with electron-caputre detection was applied to the assay of the carbonic anhydrase inhibitor dichlorphenamide and demonstrated a sensitivity of 10 ng in 0.5 ml of rabbit serum or whole aqueous humor (congruent to 0.25 ml) from one rabbit eye. After extraction of the drug and internal standard (monochlorphenamide) from the biological fluid, these compounds were converted to their tetramethyl derivatives by a nucleophilic alkylation method. Dichlorphenamide contents of aqueous humor and serum of rabbits treated with this drug are reported.

Animals↗
PubMed1978

Patient tolerance to carbonic anhydrase inhibitors.

We evaluated carbonic anhydrase inhibitors in a crossover study with a placebo and random allocation of treatment administration. Drugs evaluated included acetazolamide tablets and Sequels, dichlorphenamide, ethoxzolamide, methazolamide, and an ascorbic acid placebo. The best tolerated drug was acetazolamide Sequels. Methazolamide was next. The least tolerated drugs were ethoxzolamide, acetazolamide tablets, and dichlorphenamide.

Acetazolamide↗
PubMed1979

Ocular hypotensive effects of carbonic anhydrase inhibitors in normotensive and glaucomatous Beagles.

Four carbonic anhydrase inhibitors (acetazolamide, dichlorphenamide, ethoxzolamide, and methazolamide) cause ocular hypotony in normotensive and glaucomatous Beagles. Four dosages of acetazolamide and methazolamide and three dosages of dichlorphenamide and ethoxzolamide were evaluated. The extent of ocular hypotony after these carbonic anhydrase inhibitors was usually greater in glaucomatous Beagles than it was in normotensive Beagles.

Acetazolamide↗
PubMed1975

Teratogenesis of acetazolamide in the CBA/J and SWV strains of mice. I. Teratology.

SWV mice were totally resistant to the teratogenic and embryolethal actions of acetazolamide. The time of maximal sensitivity to acetazolamide-induced ectrodactyly in the CBA/J strain was the middle of day 10; the dose response at this time was studied. Comparison of the responses of the two strains and reciprocal hybrids indicated that sensitivity is a property of the embryo and is not maternally mediated. SWV mice were also resistant to dichlorphenamide which suggests they may be resistant to many or even all teratogenic carbonic anhydrase inhibitors.

Abnormalities, Drug-Induced↗
PubMed1985

Delayed protein digestion in the alligator following carbonic anhydrase inhibition.

Small alligators were injected with a carbonic anhydrase (CA) inhibitor (dichlorphenamide) and a day later they were fed large amounts of lean beef. The rate of protein digestion was determined and compared with that in controls fed the same amount. The controls began digestion at once, while in the CA-inhibited ones, digestion was blocked for over 10 hr. The inhibitor decreased gastric HCl production to one-third that in controls and delayed activation of pancreatic and intestinal proteases. After 15 hr, digestion began in the inhibited group and proceeded to completion. Once digestion began, further injections of the inhibitor could not block it. It seems that CA inhibition blocks digestion (for a time) by reducing HCl synthesis. NaHCO3 to neutralize the acid chyme in the intestine, was derived from that in the plasma.

Acetazolamide↗
PubMed1991

Carbonic anhydrase inhibitors are antiarthritic in the rat.

Adjuvant-induced arthritis in rats was attenuated by the therapeutic administration of carbonic anhydrase inhibitors. Female Lewis rats with established disease were treated daily (day 18 through day 50) with various carbonic anhydrase inhibitors; oedema and joint integrity (X-ray) were determined post-treatment. Acetazolamide, ethoxzolamide, methazolamide, and dichlorphenamide reduced paw oedema and attenuated the deterioration of the joints of rats with adjuvant arthritis. However, no carbonic anhydrase inhibitor tested possessed significant, acute, anti-inflammatory activity in the carrageenan-paw oedema test. The activity of carbonic anhydrase inhibitors in the chronic model of inflammation may be due to their reported inhibition of bone resorption.

Acetazolamide↗
PubMed1979

[The broncholytic effect of carboanhydrase inhibitors in subjects with healthy lungs (author's transl)].

Carboanhydrase inhibitors are said to have a positive effect on respiratory insufficiency. We examined this, especially regarding the bronchial system. Actions and reactions of the human bronchial system can be followed by measurement of the anatomical dead space breath by breath. We have developed a new method which was tested by classical broncho-effective substances. Our experiments show in case of two men with healthy lungs that the three carboanhydrase inhibitors acetazolamide, methazolamide, and dichlorphenamide have a pronounced broncholytic effect. The effect is greater than that of fenoterol. In addition the bronchial peristalsis and the bronchial compliance are increased. In contrast to fenoterol carboanhydrase inhibitors have no cardiac side effect.

Acetazolamide↗
PubMedDate not supplied

[3H]acetazolamide binding to carbonic anhydrase in normal and transformed cells.

The binding of [3H]acetazolamide (AZ), a carbonic anhydrase (CA) inhibitor, to soluble and particulate forms of CA was investigated. Sources for the assays were purified CA II, adult rat cortical, oligodendrocyte and neuronal enriched preparations; cultured murine glial cells, rat C-6 glioma, rat hepatoma and human glioblastoma cells. CA enzyme activity in the same preparations was also assayed by following change in pH during incubation. A gel permeation chromatographic method was developed to assess [3H]AZ binding to soluble CA, while glass fiber filter vacuum filtration was used for particulate CA binding. Saturable specific binding of [3H]AZ to rat cortical soluble and particulate CA preparations was demonstrated. Computer-assisted data analysis estimated the binding parameters of [3H]AZ to soluble rat cortical CA to be Bmax = 0.38 +/- 0.13 pmol/mg protein and Kd = 34.7 +/- 17.5 nM. The rat cortical particulate fraction Bmax was 2.05 +/- 0.28 pmol/mg protein with a Kd of 107.1 +/- 24.2 nM. Purified bovine CA-II bound 1.15 +/- 0.19 pmol [3H]AZ/mg protein with a Kd of 54.0 +/- 3.4 nM. The pH optima for [3H]AZ binding to soluble and particulate CA was between 6.5 and 7.5. Binding was linear with respect to protein up to 1.0 mg/mL. The particulate fraction bound 3-4 times more [3H]ligand per unit protein than the soluble fraction. Interestingly, no detectable CA enzyme activity or [3H]AZ binding was observed in the soluble or particulate fractions of human glioblastoma, rat C-6 glioma or rat hepatoma cells. Binding of [3H]AZ to other soluble enzymes or proteins was negligible. In competition binding experiments, a rank order of inhibition of [3H]AZ binding to rat cortical CA by established CA inhibitors was: dichlorphenamide greater than acetazolamide greater than or equal to benzolamide greater than methazolamide greater than hydrochlorothiazide greater than or equal to sulfanilamide. [3H]AZ binding was not affected by other classes of pharmacologic characterizing agents. The binding of [3H]AZ to the CA enzyme molecule is highly specific and sensitive and may prove useful in vitro or in situ as a probe for this enzyme.

Acetazolamide↗
PubMed1992

Diuretic screening in human urine by gas chromatography-mass spectrometry: use of a macroreticular acrylic copolymer for the efficient removal of the coextracted phase-transfer reagent after derivatization by direct extractive alkylation.

A simple and efficient procedure has been developed for the derivatization of diuretic agents in human urine by direct extractive alkylation and their detection by gas chromatography-mass spectrometry. The procedure is an improvement over previous extractive alkylation methods because of the development of a simple clean-up step using a macroreticular acrylic copolymer (SM-7 resin) to remove the coextracted phase-transfer reagent from the organic phase after derivatization. With 1 ml of sample the method gives detection limits in the range 10-50 ng/ml for acetazolamide, probenecid, dichlorphenamide, hydroflumethiazide, furosemide, chlorthalidone, bumetanide, hydrochlorothiazide, quinethazone, bendroflumethiazide, metolazone and cyclopenthiazide.

Acrylic Resins↗