Oxitropium Bromide, a New Anticholinergic Drug, in a Dose-Response and Placebo Comparison in Obstructive Airway Diseases

Flohr, E; Bischoff, K.

doi:10.1159/000194065

Cited by 17 publications

(5 citation statements)

References 2 publications

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“…In contradiction with our results ob tained with the flow interruption method, Wiessman [5] and Floher and Bischoff [1] demonstrated a decrease of the airway re sistance, measured by plethysmography re spectively 1 and 5 min after inhalation of oxitropium. This discrepancy could be ex plained by a greater sensitivity of the pleth ysmography in comparison with the flow in terruption method.…”

Section: Discussioncontrasting

confidence: 99%

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Early Bronchodilating Effect of Oxitropium Bromide in Comparison with Ipratropium Bromide

Lulling¹,

Delwiche²,

Prignot³

1981

Respiration

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The bronchodilating effects of a metered aerosol dose of 40 μg ipratropium bromide and of 200 μg oxitropium bromide are similar 15 min after administration. The bronchodilating activity of ipratropium bromide appears earlier (i.e. 75–90 s after administration) than that of oxitropium bromide but later than that of ibuterol, a β₂-agonist. Ipratropium bromide administered at the dose of 80 μg provokes a bronchodilation about double of that obtained with 40 μg. An adaptation of the usual dosage should be considered.

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Section: Discussioncontrasting

confidence: 99%

“…According to the presently available phar macological and clinical data, a scopolam ine-like derivate, oxitropium bromide, when administered as a metered aerosol seems to have a good therapeutic index [1,3,5]. On the other hand, the bronchodilating effect of anticholinergic drugs seems to appear some what later than that of ^-agonists.…”

Section: Introductionmentioning

confidence: 99%

Early Bronchodilating Effect of Oxitropium Bromide in Comparison with Ipratropium Bromide

Lulling¹,

Delwiche²,

Prignot³

1981

Respiration

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“…According to preclinical pharmacolo gical studies, this compound possesses a greater potency and a longer duration of action than IPR. These findings were con firmed in earlier clinical trials on its bronchodilator effect [10][11][12], Using bronchial allergen provocation tests our studies were designed to evaluate the potency of OTB in extrinsic bronchial asthma.…”

mentioning

confidence: 56%

Anticholinergic versus <i>β</i><sub>2</sub>-Adrenergic Therapy in Allergic Airways Obstruction

Schultze‐Werninghaus¹

1981

Respiration

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Two double-blind studies were performed in allergic subjects with bronchial asthma to evaluate the bronchodilator effect and antiallergic protection of oxitropium bromide (OTB), a new antiallergic drug. Study 1, bronchodilator trial: 2 puffs of OTB or Fenoterol (FEN) were administered by metered dose aerosol after bronchial allergen provocation tests in 12 subjects each. The bronchodilator effect of FEN was significantly better (between 0 and 30 min after drug administration). At the same time there was an improvement of PaO₂ after FEN (before: 62.4 Torr; after: 70.1 Torr), but not after OTB. Study 2, antiallergic protection: OTB or FEN were administered 30 min before bronchial allergen provocation tests in 12 subjects each, complemented by open DSCG controls. All 3 drugs provided significant protection compared with nonmedicated control tests, but only inhibition by FEN was complete. In conclusion, β_2-adrenergic drugs seem to be superior to anticholinergic drugs in allergic asthma, not only as bronchodilators, but also as prophylactic agents.

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“…In the course of developing it for utilization as a pharmaceutically active ingredient in the treatment of asthma and other bronchial disorders, − oxitropium bromide, first synthesized in the 1950s, was found to undergo a dimorphic single-crystal-to-single-crystal phase transition . Initial hot-stage microscopic experiments to investigate the nature of this phase transition immediately indicated that the transition is an example of the thermosalient phenomenon , occasionally colloquially referred to as “jumping crystals”. − …”

Section: Introductionmentioning

confidence: 99%

The Thermosalient Phenomenon. “Jumping Crystals” and Crystal Chemistry of the Anticholinergic Agent Oxitropium Bromide

et al. 2010

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The anticholinergic agent oxitropium bromide possesses rich crystal chemistry, most remarkably exhibiting a strong thermosalient effect ("jumping crystal" effect), a mechanical property with potential applications in organic-based actuators. The thermosalient effect, manifested in forceful jumps of up to several centimeters, was investigated by a combination of structural, microscopic, spectroscopic, and thermoanalytical techniques, providing data on which to base a proposed mechanism for the phenomenon. Direct observation of the effect in a single crystal and structure determination of both phases revealed that the jumping of the crystals is a macroscopic manifestation of a highly anisotropic change in the cell volume. The cell distortion is accompanied by a conformational change of the oxitropium cation, which triggers increased separation between the ion pairs in the lattice at nearly identical separation between the cation and the anion within each ion pair. At the molecular level, the cation acts as a molecular shuttle composed of two rigid parts (epoxy-aza-tricyclic-nonyl portion and phenyl ring) that are bridged by a flexible ester linkage. The structure of the rigid, inert aza-tricyclic portion remains practically unaffected by the temperature, suggesting a mechanism in which the large, thermally accumulated strain is transferred over the ester bridge to the phenyl ring, which rotates to trigger the phase transition. Mechanistic details of the higher temperature solid-state phenomena are also presented. The high-temperature phase can also be obtained by grinding or UV irradiation of the room-temperature phase. In addition, if it is irradiated with UV light in the presence of KBr, the high-temperature phase undergoes intramolecular photochemical rearrangement. Heating the high-temperature phase to slightly below the melting temperature results in an additional solid-state reaction that results in the conversion of the salt to a mixture of neutral compounds.

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Oxitropium Bromide, a New Anticholinergic Drug, in a Dose-Response and Placebo Comparison in Obstructive Airway Diseases

Cited by 17 publications

References 2 publications

Early Bronchodilating Effect of Oxitropium Bromide in Comparison with Ipratropium Bromide

Early Bronchodilating Effect of Oxitropium Bromide in Comparison with Ipratropium Bromide

Anticholinergic versus <i>β</i><sub>2</sub>-Adrenergic Therapy in Allergic Airways Obstruction

The Thermosalient Phenomenon. “Jumping Crystals” and Crystal Chemistry of the Anticholinergic Agent Oxitropium Bromide

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