Variable effects of previously untested muscarinic receptor antagonists on experimental myopia.

PURPOSE: Atropine, pirenzepine, and himbacine prevent form-deprivation myopia (FDM) when administered intravitreously. The mechanisms and sites of action of these drugs against myopia are not clear. To shed further light on whether this mechanism is muscarinic, several other muscarinic antagonists were tested. METHODS: Various concentrations of atropine, pirenzepine, dexetimide, scopolamine, tropicamide, benztropine, dicyclomine, gallamine, mepenzolate, oxyphenonium, propantheline, procyclidine, 4-diphenylacetoxy-N-methylpiperidine (4-DAMP), hexahydro-sila-difenidol (HHSiD), p-fluorohexahydro-sila-difenidol (pf-HHSiD), methoctramine, AFDX-116, and quinuclidinyl benzilate (QNB) were injected into goggled eyes of Leghorn cockerels three times at 48-hour intervals. Fellow control eyes received saline. Control animals received saline in both eyes. Twenty-four hours after final injections, refraction, eye weight, and axial length were measured, and eyes were prepared for microscopy. RESULTS: Other than atropine and pirenzepine, only oxyphenonium caused full rescue from FDM (goggled versus control; mean +/- SD; refraction differences: -9.50 +/- 0.22 D vs. 0.83 +/- 0.31 D, P < 0.001; wet weight differences: 75.67 +/- 3.84 mg vs. 2.33 +/- 6.14 mg, P < 0.001; axial length differences: 0.80 +/- 0.05 mm vs. 0.03 +/- 0.04 mm, P < 0.001). Oxyphenonium-treated retinas showed no damage. Of the other compounds, several elicited partial rescue and/or damaged the retina, whereas others had no effect. CONCLUSIONS: Oxyphenonium prevents FDM in chicks. The ineffectiveness or partial effectiveness of other compounds, coupled with the high concentrations of effective compounds required to prevent FDM, suggests that muscarinic antagonists act to prevent FDM, either at sites distant from the retina, or through a nonmuscarinic mechanism, on which only some of these drugs act.

The effect of oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux in children with vesicoureteral reflux and detrusor instability.

In a prospective study the effects of the anticholinergic drugs oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux were studied. Although anticholinergic properties are claimed of both drugs, only oxybutynin hydrochloride proved to decrease detrusor contractility and the degree of reflux, probably due to a direct spasmolytic effect on the detrusor. Therefore, in cases of reflux and detrusor instability treatment with oxybutynin hydrochloride is recommended.

[The effect of metacin on the activity of digestive enzymes participating in the hydrolysis of fats normally and in stress]. / Vliianie metatsina na aktivnost' pishchevaritel'nykh fermentov, uchastvuiushchikh v gidrolize zhirov, v norme i pri stresse.

The effect of a peripheral cholinolytic methacin on the activity of lipolytic enzymes of the pancreas and small intestine was studied on intact and stress-exposed animals. The drug was shown to induce certain changes in the activity of lipolytic enzymes. The preliminary administration of methacin attenuates the shifts in the activity of the studied enzymes observed under stress action.

[The atropine test in patients with stress incontinence and their treatment with a combination of diltiazem and oxyphenonium]. / Atropinový test u pacientek s urgentní inkontinencí a jejich lécba kombinací léku diltiazemu a oxyfenonia.

The authors applied the Atropine test in 28 patients with the motor type of urgent incontinence in an attempt to establish the prognosis of the success of treatment with parasymthatholytics. Atropine was administered in amounts of 0.01 mg/kg body weight by the i.m. route and after 30 mins. a urodynamic control examination was made. The assumption that a reduced frequency or amplitude of detrusor contractions will occur or that they will disappear in patients, where subsequent treatment with parasympatholytics will be successful, was not confirmed. The patients were subsequently treated by a combination of dilthiazem (Diacordin), 3 X 30 mg by the oral route per day and oxyphenonium (Oxyphenon dupl.) 2 X 10 mg by the oral route per day. After evaluation of the therapeutic results the group was divided into two sub-groups. The first one comprised patients where during the urodynamic check-up examination a drop of the intracystic pressure occurred after Atropine administration. The second group comprised patients where the drop of intracystic pressure did not occur. The therapeutic effect in these groups was evaluated separately. In the course of treatment there was a relatively high percentage of undesirable side-effects of the drugs in 43% of the patients. After the general evaluation of the therapeutic effect when the patients had no complaints or improved markedly in 70.4% there were no marked differences between the sub-groups.

Comparative study of the bronchodilating effects of (-)- and (+)-oxyphenonium bromide.

1. Racemic oxyphenonium bromide, its enantiomers and placebo were inhaled by eight adult patients with chronic airflow obstruction, in a four-way double-blind cross-over study. 2. Forced expiratory volume in one second (FEV1) and slow inspiratory vital capacity (VC) were measured during the first 6 h after inhalation. 3. (+)-Oxyphenonium was found to be the active enantiomer (eutomer), providing better bronchodilation than (+/-)-oxyphenonium. 4. The distomer, (-)-oxyphenonium, showed only a slight effect on FEV1 and VC as compared with placebo.

Bronchial obstructive reactions after inhalation with endotoxin and precipitinogens of Haemophilus influenzae in patients with chronic non-specific lung disease.

Bronchial obstructive reactions occur after inhalation of Haemophilus influenzae in the absence of proteolytic activity in patients with CNLSD and a lowered histamine threshold in whom specific precipitins are demonstrated. It may be presumed, that the direct bronchial reaction is caused by its content of endotoxin, whereas the late bronchial reaction is the result of a toxic action and a type III allergic reaction. When proteolytic activity is present it lowers the histamine threshold and may influence the endotoxin effect in this way.

Nocturnal gastric acid secretion in duodenal ulcer: inhibition by cimetidine.

The inhibitory effect of cimetidine 200 mg, cimetidine 400 mg, cimetidine 200 mg + oxyphenonium bromide 10 mg and placebo was studied on nocturnal gastric acid secretion in 10 patients with duodenal ulcer. Each patient was studied over a period of four nights and trial medication was given in a randomized sequence. Cimetidine in both doses significantly inhibited the nocturnal gastric acid secretion. The drug reduced both the H+ concentration and gastric juice volume but the reduction of H+ concentration was more impressive. Mean percentage inhibition of nocturnal acid output with cimetidine 400 mg (89.6 +/- 2.868) was significantly higher than cimetidine 200 mg (80.3 +/- 4.085; p less than 0.01). Combination of cimetidine 200 mg and oxyphenonium bromide 10 mg was significantly better than cimetidine 200 mg alone (p less than 0.05) and this combination produced inhibition of gastric juice volume, H+ concentration and acid output comparable to cimetidine 400 mg.

Glucagon vs anticholinergics in the treatment of acute pancreatitis. A double-blind controlled trial.

Sixty-two cases of acute pancreatitis, evaluated for severity according to uniform standards, were treated identically except that patients in one group received glucagon hydrochloride (group A) and those in the other oxyphenonium bromomethylate (group B). Each of the two homologous series comprise 31 patients, and mortality was the same for both groups (3/31, 10%). Statistical comparison of both series showed no significant differences in frequency of expected complications nor in fall of serum amylase levels. During treatment, serum calcium levels were significantly reduced in group A (P less than .005), and the duration of the abdominal pain was shortened (P less than .05). The volume of gastric aspirate was smaller in group B (P less than .005), and vesical catheterization proved necessary more frequently (P less than .005). Thus, similar results are obtained when glucagon or anticholinergics are employed in the treatment of acute pancreatitis, although secondary effects differ.