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At least 19 recordsLinked to original sources
PubMed1976

[Toxicological studies on ipratropiumbromide (author's transl)].

The acute, subacute and chronic toxicity of (8r)-3alpha-hydroxy-8-isopropyl-1alphaH,5alphaH-tropaniumbromide (ipratropiumbromide, Sch 1000, Atrovent) was studied on mice, rats, dogs and monkeys following oral, s.c., i.v. administration and inhalation. With toxic doses all typical symptoms of atropine or atropine derivatives were present, like mydriasis, dryness of the mucosa and meteorism with coprostasis. It was not possible to determine the LC50 of the substance due to its low toxicity.

Administration, Oral↗
PubMed1978

[Broncholytic therapy--beta 2 stimulation and vagolysis from an animal experimental viewpoint].

Continuous recordings of heart rate, respiration rate, minute volume and bronchial resistance were made over a period of altogether 3 h in spontaneously breathing dogs anesthetized with chloralose. At hourly intervals, before and 1 and 2 h after the administration of bronchodilators, bronchial spasm was induced by inhalation of an acetylcholine solution. Terbutaline, a beta-stimulant, was administered by inhalation in doses of 0.5, 0.16 and 0.05 mg/kg. For comparison, an atropine derivative, ipratrapium bromide, was given in doses of 0.04 and 0.01 mg/kg. Controls received normal saline. Terbutaline caused an increase in heart rate, respiration rate and minute volume. Acetylcholine-induced bronchial spasm was inhibited to the extent of 10-70% for 2 h after the administration of terbutaline. The acetylcholine antagonist ipratropium bromide caused only transient changes in heart rate, respiration rate and minute volume. Acetylcholine-induced bronchial spasm was inhibited by 95% and 80% for 2 h after doses of 0.04 and 0.01 mg/kg respectively. Terbutaline had a slight stimulant effect; ipratropium bromide displayed no stimulant activity.

Acetylcholine↗
PubMed1978

Bronchial spasmolytic action of terbutaline and fenoterol compared with that of ipratropium bromide in the anaesthetized dog.

Continuous recordings of heart rate, respiration rate, minute volume and bronchial resistance were made over a period of altogether three hours in spontaneously breathing dogs anaesthetized with chloralose. At hourly intervals, before and 1 and 2 hr after the administration of bronchodilators, bronchial spasm was induced by inhalation of an acetylcholine solution. Two beta2-stimulants, terbutaline and fenoterol, were administered by inhalation in doses of 0.5, 0.16 and 0.05 mg/kg and 0.1, 0.3 and 0.01 mg/kg respectively. For comparison, an atropine derivative, ipratropium bromide, was also given by the same route in doses of 0.04 and 0.01 mg/kg. Controls received normal saline. Terbutaline and fenoterol caused an increase in heart rate, respiration rate and minute volume. Acetylcholine-induced bronchial spasm was inhibited to the extent of 10--70% for 2 hr after the administration of terbutaline, and by 15--70% after fenoterol. The acetylcholine antagonist ipratropium bromide caused only transient changes in heart rate, respiration rate and minute volume. Acetylcholine-induced bronchial spasm was inhibited by 95% and 80% for 2 hr after doses of 0.04 and 0.01 mg/kg, respectively. Fenoterol had a slightly greater central stimulant effect than terbutaline; ipratropium bromide displayed no stimulant activity.

Acetylcholine↗
PubMed1979

Inhaled atropine in asthma.

Ten adult asthmatics inhaled atropine and isoproterenol to determine the site of action in the airways and relative effectiveness of the two drugs. The two agents were equal in their effect on lung volumes and airway resistance but isoproterenol produced significantly better flows. Atropine was shown to be an effective bronchodilator with a predominant site of action in large airways. The authors believe atropine and atropine derivatives deserve ongoing investigation, especially regarding potential side effects of retarding mucociliary clearance and the clinical significance of apparent failure to dilate small airways.

Administration, Intranasal↗
PubMed1975

Sch 1000: a new anticholinergic bronchodilator.

Sch 1000 is a derivative of atropine with equivalent bronchodilator activity. A double blind controlled study of Sch 1000 administered to asthmatic subjects by inhalation in 4 doses from 10 mug to 80 mug was conducted. The onset of action was between 15 and 30 min, compared to 5 min for isoproterenol, but persisted for 4 hours compared to 1 hour for isoproterenol. The maximal level of bronchodilatation produced by Sch 1000 was comparable to but not as great as that after isoproterenol. Dose-response data suggested that maximal bronchodilatation may be achieved by 10 to 20 mug of Sch 1000; larger doses did not result in significantly greater increases in forced expiratory volume in 1 sec or maximal mid-expiratory flow. The Sch 1000-mediated increase in maximal mid-expiratory flow was significantly greater than that of forced expiratory volume in 1 sec. Fewer side effects were encountered after Sch 1000 than after isoproterenol and no atropine-like effects could be attributed to Sch 1000 in the doses studied.

Administration, Intranasal↗
PubMed1976

[Ipratropium Bromide, an Anticholinergic Bronchodilator/Behavior of airways resistance in patients with reversible respiratory obstruction following inhalation of various doses of ipratropium bromide].

A dose- and time-response study using different doses of an inhaled derivative of atropine, (8r)-3alpha-hydroxy-8-isopropyl-1 aH, 5aH-tropaniumbromide-(+/-)-tropate (Sch 1000, ipratropium bromide, Atrovent) was performed in 12 patients with reversible chronic obstructuve airways disease. The drug was shown to be an effective bronchodilator with the typical action of reducing airways resistance with 2 puffs (0.02 mg per puff). Increasing the dose to 4 and 8 puffs did not produce any relevant difference in time response. The onset of action was rapid and reached a maximum between 30 and 60 min after inhalation. The duration of bronchodilation was maintained during the observation period of 3 h. 30 min after inhalation the results corresponded to those following the inhalation of 2 puffs of orciprenaline (0.75 mg per puff). Isolated side-effects were independent of the dosage.

Adult↗
PubMed1977

[Antiallergic asthma effect of ipatropium bromide (Sch 1000) in dogs (author's transl)].

Antiasthmatic effect of ipratropium bromide (Sch 1000) which is a quarternary ammonium derivative of atropine was investigated in comparison with atropine in anesthetized dogs. Asthmatic responses were provoked with inhalation of Ascaris suum antigen. Sch 1000 (0.1 approximately 0.3%) and atropine (0.1 approximately 0.3%) were given by inhalation for 10 min prior to or after the antigen inhalation. Pretreatment of Sch 1000 and atropine inhibited the increase in respiratory resistance (Rrs) induced by antigen by 55 approximately 75% and 25 approximately 50%, respectively. After treatment with each drug, the enhanced Rrs was reduced by 40 approximately 55% and 35 approximately 40%, respectively. The activity of Sch 1000 was three fold stronger than that of atropine. Sch 1000 and atropine also effectively inhibited the increase in airway secretion produced by antigen, while both drugs in 0.3% solution had no effect on the normal bronchial tone and secretion. The findings suggest that vagal activity is involved in allergy related asthma and inhalations of anticholinergic drugs such as Sch 1000 show promise in the treatment of bronchial asthma.

Airway Resistance↗
PubMed1975

Aerosol Sch 1000. An anticholinergic bronchodilator.

Atropine is known to be an effective bonrchodilator. We studied the effectiveness of aerosol Sch 1000, a derivative of atropine, in relieving bronchoconstriction in asthma. A single dose of drug was effective within 5 min, and the effect had a duration of 4 hours. No side effects were noted. The major effect of the drug appeared to be in large airways.

Adolescent↗
PubMed1975

[Treatment of bradycardia with an atropine ester].

In view of the unsatisfying drug treatment of bradycardias in most cases, clinical studies with new compounds seem to be urgent. A report is given on experiences with a derivative of atropine (gen. Ipratropiumpromid) in 34 cases suffering from various types of bradycardias. Comparing heart rate following intravenous injections of 0.5 to 1.0 mg, the new drug proved to be definitely more effective than atropine sulfate. Side effects were limited to diminution of salivary glands function.

Adolescent↗
PubMed1977

Newer medications to aid treatment of asthma.

The selective beta-2 adrenergic bronchodilator preparations should be considered the medications for the first line of defense in the treatment of the average asthmatic patient. Theophylline and derivatives of theophylline are the second line of defense. Cromolyn sodium, atropine and derivatives, corticosteroids and other selected agents follow, depending on the individual case and the circumstances involved.

Adrenal Cortex Hormones↗
PubMed1976

[Findings in the gastric mucosa and gastric secretion in rats treated with methyl O-(4-hydroxy-3-methoxycinnamoyl)reserpate (CD-3400) and reserpine derivatives].

CD-3400 developed by Nippon Chemiphar Co. Ltd., is a new antihypertensive agent belonging to the class of rauwolfa alkaloids. Influence of the agent on gastric mucosa, healing process of acetic acid-induced gastric ulcer and gastric juice in rats was investigated and compared with effects of reserpine and rescinnamine. CD-3400-induced gastric lesions were fewer in number than those produced with reserpine and rescinnamine in fasted rats. After a three day treatment of CD-3400 to fed rats, however, there were few gastric lesions, while reserpine- and rescinnamine-induced gastric lesions were aggravated to a greater extent that when a single administration was given to fasted rats. Influence of CD-3400, reserpine and rescinnamine on the healing process of acetic acid-induced ulcer was insignificant, but treatment with high doses of reserpine and rescinnamine resulted in death. Pretreatment with CD-3400 and reserpine produced a decrease in gastric acid and K+, and an increase in Na+. Repeated administration of reserpine for 5 days resulted in a decrease of both gastric volume and acid, while such was not seen with CD-3400. Treatment with anticholinergic agents such as atropine sulfate and atropine methylbromide inhibited CD-3400- and reserpine-induced gastric lesions. From these results, it would appear that cholinergic factors play a role in the pathogenesis of CD-3400-induced gastric lesions, as in the case with reserpine, and that the responses of these lesions to reserpine and CD-3400 correlate with changes of ionic fluxes in gastric juice.

Acetates↗