[Symposium of lung doctors. 9. Value of combinations of parasympatholytic and sympathomimetic drugs].
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Aerosols↗
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[Bronchodilation action of a benzimidazole derivative (parasympatholytic mechamism?) (proceedings)].
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Asthma↗
The parasympatholytic effects of atropine sulfate and glycopyrrolate in rats and rabbits.
Nine groups of rats (n = 5 per group) received an intramuscular (IM) injection of one of the following drugs or drug combinations: saline, atropine (0.05 mg/kg), glycopyrrolate (0.5 mg/kg), ketamine:xylazine (85:15 mg/kg), ketamine:detomidine (60:10 mg/kg), atropine:ketamine:xylazine (0.05: 85:15 mg/kg), glycopyrrolate: ketamine:xylazine (0.5:85:15 mg/kg), atropine:ketamine:detomidine (0.05: 60:10 mg/kg) or glycopyrrolate: ketamine:detomidine (0.5:60:10). Similarly six groups of rabbits (n = 5) received an IM injection of either saline, atropine (0.2 mg/kg), atropine (2 mg/kg), glycopyrrolate (0.1 mg/kg), ketamine:xylazine (35:10 mg/kg) or glycopyrrolate:ketamine:xylazine (0.1:35:10 mg/kg). In rats, atropine sulfate (0.05 mg/kg) and glycopyrrolate (0.5 mg/kg) produced an increase in heart rate for 30 and 240 min, respectively. In rabbits atropine sulfate at either 0.2 or 2.0 mg/kg did not induce a significant increase in heart rate, but glycopyrrolate (0.1 mg/kg) elevated the heart rate above saline treated animals for over 50 min. Both atropine and glycopyrrolate provided protection against a decrease in heart rate in rats anesthetized with ketamine: xylazine (85:15 mg/kg) or ketamine: detomidine (60:10 mg/kg); however, glycopyrrolate was significantly more effective in maintaining the heart rate within the normal range. Glycopprrolate also prevented a decrease in heart rate in rabbits anesthetized with ketamine:xylazine (35:5 mg/kg). Neither glycopyrrolate nor atropine influenced respiration rate, core body temperature or systolic blood pressure when used alone or when combined with the injectable anesthetic. Glycopyrrolate is an effective anticholinergic agent in rabbits and rodents and more useful as a preanesthetic agent than atropine sulfate in these animals.
Animals↗
A new parasympatholytic bronchodilator: a study of its onset of effect after inhalation.
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Adolescent↗
The effects on pupil size and accommodation of sympathetic and parasympatholytic agents.
The time-response effect of two currently used mydriatics, phenylephrine and tropicamide, were evaluated in 524 eyes. Four different types of dilating regimens were used: 2.5% phenylephrine, 10% phenylephrine, 0.5% tropicamide, and the combination of 2.5% phenylephrine and 0.5% tropicamide. The analysis indicated that the recovery from mydriasis occurs between 5.5 and 7.0 hours with 2.5% phenylephrine and at more than 7 hours with 10% phenylephrine. The 0.5% tropicamide induced rapid dilation, whereas the combined treatment, 2.5% phenylephrine plus 0.5% tropicamide, produced the largest maximum pupillary diameter. Tropicamide, alone or in combination, also produced a longer mydriatic effect, lasting more than 7.0 hours. The recovery from the cycloplegic effect of the mydriatics occurred between five and seven hours in the majority of patients, with tropicamide alone or in combination with phenylephrine requiring the most time to revert to normal ranges of accommodation. The findings in this study indicate that, in normal subjects, the recovery from the effect of mydriatic agents is longer than what is generally reported in the literature.
Accommodation, Ocular↗
Effect of tetraalkylammonium derivative of 6-methyluracil on amplitude and temporal parameters of miniature endplate potentials in frog neuromuscular junction.
The effect of C-547, a tetraalkylammonium derivative of 6-methyluracil, a novel highly selective acetylcholinesterase inhibitor, on frog neuromuscular junction was studied. In concentrations 10(-9)-10(-7)M the preparation increased the amplitude and temporal parameters of miniature endplate potentials. In contrast to the effect of C-574 on purified acetylcholinesterase from mammals, the effect of this agent on frog neuromuscular junction was reversible. In a concentration of 10(-6)M the preparation apart from anticholinesterase activity produced a parasympatholytic effect manifested in a decrease in amplitude and decay time constant of miniature endplate potentials accompanied by a decrease in spontaneous transmitter secretion. After washout, the parasympatholytic effect recovered more slowly, but disappeared more rapidly compared to anticholinesterase activity. These findings suggest that parasympatholytic effect of C-547 results from direct action on receptor-channel complexes in the endplate membrane.
Acetylcholinesterase↗
Possible antidotes in severe intoxication with fenitrothion in rats.
We investigated antidotal effects of nine drugs against acute fenitrothion poisoning in rats. The antidotal effects were evaluated by a relief from toxic signs, an increased survival ratio and a prolonged surviving time. In the poisoning with approximate LD50 fenitrothion (500 mg/kg), oximes such as 2-PAM (2-pyridine aldoxime methiodide) and TPMM (1-(methyl morphorinium)-3-(4-hydroxyiminomethylpyridinium) propane dibromide), diphenhydramine and parasympatholytics such as atropine, scopolamine and biperiden significantly increased survival ratio and/or prolonged surviving time. These effective drugs did not sufficiently depress the toxic signs, except that the parasympatholytics markedly blocked salivation, miosis and motor ataxia. In contrast, reduced glutathione and central depressants such as diazepam and phenobarbital made the poisoning serious. In the poisoning with 100% lethal dose of fenitrothion (800 mg/kg), the parasympatholytics were more effective than 2-PAM and diphenhydramine, and they elevated the survival ratio up to 20-40%. The best therapy against the severe poisoning with 100% lethal dose of fenitrothion was confirmed to be the repeated and combined treatment with atropine and 2-PAM as established in parathion poisoning, resulting in 90% survival ratio and considerable alleviation from the toxic signs.
Animals↗
Characterization of chronotropic and dysrhythmogenic effects of atropine in dogs with bradycardia.
OBJECTIVE: To characterize the magnitude, character, and time course of chronotropic and dysrhythmogenic responses of dogs with vagally mediated bradycardia to atropine sulfate. DESIGN: Latin square design. ANIMALS: Seven clinically normal adult mixed-breed dogs. PROCEDURE: Vagally mediated bradycardia was induced with morphine and fentanyl citrate. Atropine (0.02 mg/kg of body weight) was administered i.v., s.c., or i.m.. Electrocardiograms were recorded continuously for 5 minutes before and for 35 minutes after atropine administration or until a sustained parasympatholytic response was observed. Data were digitized, analyzed independently for changes in atrial and ventricular rate, and compared between different routes of administration. RESULTS: All dogs developed second-degree atrioventricular (AV) block after i.v. administration of atropine, and 71% of dogs developed AV block after s.c. or i.m. administration. The AV block arose and resolved more rapidly with i.v. administration than with s.c. or i.m. administration. The AV block was principally attributable to an increase in the atrial rate prior to increases in the ventricular rate. Atropine, regardless of route of administration, potentiated baseline ventricular bradycardia in 62% of the experiments (mean heart rate decrease of 16 beats/min; decreased to < 20 beats/min in 2 dogs for < or = 10 seconds). Duration of the bradycardic potentiation was longer with s.c. administration (9.1 minutes, s.c., vs 1.4 minutes, i.v., and 4.6 minutes, i.m.). Parasympatholytic rate was higher for i.v. than s.c. or i.m. administration (128 beats/min vs 92 beats/min and 101 beats/min). Two dogs given atropine s.c. failed to resolve the AV block and attain sinus rhythm. CONCLUSIONS: Administration of 0.02 mg of atropine/kg by i.v., i.m., and s.c. routes for vagally mediated bradycardia in dogs consistently induces AV block and occasional brief potentiation of ventricular bradycardia. CLINICAL RELEVANCE: Parasympathomimetic effects occur and resolve most rapidly and consistently, and the stable parasympatholytic effect is of greatest magnitude after i.v. administration. Thus, vagally mediated bradycardia in clinically normal dogs appears to be best abolished by i.v. administration of atropine.
Analysis of Variance↗
Effectiveness of bronchodilators in cystic fibrosis.
Bronchodilators (xanthines, adrenergics, and parasympatholytics) have been used for years in the treatment of airway obstruction associated with cystic fibrosis. Their effectiveness in bringing about consistent and significant reversal of airway obstruction remains a topic for debate. A review of the literature suggests that the majority of patients with cystic fibrosis have hyperresponsive and hyperactive airways and will respond favorably to bronchodilators, at least some of the time. Bronchial hyperresponsiveness tends to be greater in patients with advanced disease than in mildly affected ones. Responses to bronchodilators appear to be greatest when airway disease is mild-to-moderate, when there is a documented excessive bronchial hyperresponsiveness to nonspecific bronchoconstrictors (methacholine, histamine), and when the patients are young. The response to intravenous xanthine and terbutaline is best when patients experience an acute pulmonary exacerbation and when aerosolized bronchodilators are relatively ineffective. Patients with advanced airway destruction and obstruction have a high degree of airway wall instability, which may be worsened by inhaled bronchodilators. Adrenergic and parasympatholytic aerosols are equally effective; combining them in optimal doses may be more beneficial than using either alone. Atropine and ipratropium bromide may be more effective in adults than children, but this remains to be further evaluated. Some of the apparently poor responses to inhaled bronchodilators are likely due to inadequate dosing. In conclusion, most patients with cystic fibrosis are likely to benefit from bronchodilator therapy when given in adequate doses, appropriate combinations, and by the appropriate route.
Adrenergic beta-Agonists↗
Supersensitivity of the submaxillary gland following exclusion of the postganglionic parasympathetic neurone.
The repeated subcutaneous injection of four different parasympatholytic agents into cats has been found to cause a supersensitivity of the submaxillary glands to adrenaline. The fact that the level of sensitivity reached is the same with all four drugs is taken as evidence that the supersensitivity is due to the absence of an action of acetylcholine on the gland cells. This acetylcholine can only in part be that released by the secretory impulse, for the supersensitivity produced is more marked than that caused by preganglionic parasympathetic denervation. It is assumed that the postganglionic cholinergic neurone exerts some action of its own on the gland cell. Sensitization above the level reached after decentralization ensues when such an action is abolished by parasympatholytic agents. Degenerative section of the postganglionic fibres would also exclude this action, but for anatomical reasons this cannot be made complete. The supersensitivity which follows this operation is greater than after decentralization but less than that produced by treatment with atropine-like drugs.
Acetylcholine↗
[Therapy changes and cost development in bronchial asthma. A 10-year retrospective study at the medical outpatient clinic of the Zurich University Hospital].
The changes that have taken place in asthma therapy during the past ten years and their consequences regarding costs were studied analyzing retrospectively 285 clinical histories of asthmatics treated at the University Hospital Zurich in 1977, 1982 and 1987. The following changes in the use of the five basic antiasthmatic drugs i.e. beta-adrenoceptor agonists, anticholinergic drugs, xanthines, glucocorticosteroids and antiallergic drugs were observed: In 1977 80% of asthmatics received beta-agonists, in 1987 90%. Conversely, parasympatholytics were rarely used: In 1977 in only 2%, in 1982 in 16% and in 1987 in 27% of patients. In 1987 xanthines were prescribed in only 50% of asthmatics whereas in 1982 after the introduction of retarded preparations, these drugs were given to 86% of patients. In 1977 only one-third of asthmatics received glucocorticosteroids; in 1987, however, three-quarters of them. Antiallergic drugs were prescribed in 1977 and 1987 in about 25% of the asthmatics, in 1982 in only 13%. Considering the form of application there was a significant trend towards metered aerosols. This was true for betamimetics, parasympatholytics and glucocorticosteroids. Fixed combinations and rectal applications of xanthines were substituted for retarded formulations. In 1977 one or two antiasthmatic drugs accounted for 75% of asthma therapy. In contrast, in 1987 60% of asthmatics received more than two antiasthmatic drugs. The dosages of salbutamol and beclomethasone increased significantly from 1977 to 1987. Other changes in dosages were not significant. The change in costs of antiasthmatic therapy revealed significant savings in regard of xanthines and antiallergic drugs. During the past ten years the overall costs of antiasthmatic drugs therapy remained the same despite more complex therapy.
Adrenergic beta-Agonists↗
Inhibitory effect on gastric motility of chloroquine and mepacrine.
Measured on isolated rat-stomach fundus strips, the isolated cervical sympathetic trunk, and on the superior cervical ganglion, chloroquine and mepacrine have parasympatholytic, spasmolytic, ganglionic blocking and local anaesthetic effects. On rising the doses these manifest themselves in a given sequence. On the basis of this fact it is concluded that the inhibition of gastric motility by chloroquine and mepacrine in the rat, is based on the parasympatholytic property of the drugs in question.
Animals↗
The effects of lidocaine on cardiac parasympathetic control in normal subjects and in subjects after myocardial infarction.
It has been widely accepted that lidocaine has little or no effect on the autonomic nervous system. However, we have previously shown that in dogs with vagally induced atrial fibrillation, lidocaine has a pronounced parasympatholytic effect. To study the possible effect of lidocaine on autonomic cardiac control in humans, we performed spectral analysis of heart rate fluctuations in 19 healthy volunteers, who received an i.v. bolus of lidocaine (1.4 mg/kg), as well as in 13 patients suffering from acute inferior myocardial infarction (IMI) and 13 patients suffering from acute anterior myocardial infarction (AMI), who received therapeutic doses of i.v. lidocaine infusion (4 mg/min). Heart rate variability and respiratory pattern were monitored according to a predetermined protocol, with and without lidocaine. Computing the heart rate power spectrum and integrating over predetermined frequency bands, we focused mainly on the respiratory frequency band, known to predominantly reflect parasympathetic control. The administration of lidocaine resulted in a significant overall increase in mean heart rate: for the healthy control group an increase of 5.5 +/- 2.2% (mean +/- SE), for the IMI group an increase of 9.4 +/- 3.5%, and for the AMI group an increase of 8.1 +/- 2.9% (p < 0.01 for all). Simultaneously, following the administration of lidocaine, there was a decrease in the power of respiratory fluctuations: for the healthy control group a decrease of 38.4 +/- 12.5%, for the IMI group a decrease of 46.3 +/- 32.9%, and for the AMI group a decrease of 33.9 +/- 16.2% (p < 0.01 for all). These findings indicate that lidocaine has a consistent and significant parasympatholytic effect on the human heart, in healthy volunteers as well as in patients in the acute phase of myocardial infarction.
Adult↗
[Current conservative treatment of renal colic: value of prostaglandin synthesis inhibitors].
Prostaglandin synthesis inhibitors and parasympatholytic drugs are often used as analgetics in the case of renal colic. This paper analyzes how and whether these drug effects are important for the analgetic therapy. In an animal and in a human model with acutely obstructed kidneys we found that intravenous application of Indometacine and dipyrone significantly reduces renal pelvic pressure. The parasympatholytic drug hyoscine butylbromide did not produce any change of upper urinary tract dynamics. Inhibitors of prostaglandin synthesis thus effect pressure reduction in the renal pelvis, which is necessary for analgetic therapy. In contrast, hyoscine butylbromide does not have any influence on the acute upper urinary tract obstruction; consequently its usefulness in the treatment of renal colic is rather doubtful.
English Abstract↗
[Cardiac side-effects of oesophago-gastro-duodenoscopy in relation to premedication (author's transl)].
The electrocardiogram was monitored in 100 patients undergoing oesphago-gastro-duodenoscopy. Premedication differed: 25 patients each were given either (Group I) atropine 0.5 mg, hyoscine-N-butylbromide 20 mg, and diazepam 5 mg, or (Group II) hyoscine-N-butyl-bromide 20 mg and diazepam 5 mg, or (Group II) diazepam 5 mg and glucagon 0.2 mg, or (Group IV) only diazepam 5 mg intravenously. After injection of the parasympatholytic drugs (Groups I and II) there was a significantly higher heart rate duringthe entire length of the examination than in groups III and IV. Nine of the ten cases of ascending S-T depression were found in Groups I and II, while descending (ischaemic) S-T changes occurred equally frequently in patients of all four groups. Two of the three more serious arrhythmias were registered after atropine. Since parasympatholytic drugs fail to inhibit arrhythmias and ST-T changes, while accentuating the rise in heart rate, it is recommended that premedication for oesophago-gastro-duodenoscopy should not include such drugs.
Adolescent↗
Effect of the H1 antihistamine chlorpheniramine maleate on histamine-induced symptoms in the human conjunctiva. Indirect evidence for nervous H1 receptors.
Earlier studies have shown that intranasal chlorpheniramine (0.77%) can inhibit histamine-induced tickling, sneezing, and hypersecretion by a local effect on nerve fibres. The aim of the present study was to examine whether this solution had local anaesthetic of parasympatholytic properties. If neither of these properties are present it suggests that the anti-pruritic effects of the solution are caused by inhibition of H1 receptors, which in turn is indirect evidence for the presence of H1 receptors on nerve fibers. In a double-blind design 15 normal subjects were provoked with histamine in the eye after pretreatment with chlorpheniramine or with a local anaesthetic, oxybuprocain. Both drugs inhibited itching, but the H1 antihistamine was significantly more effective than the local anaesthetic (P less than 0.01). Corneal sensitivity was measured by an esthesiometer, and pupil difference was used as a measure for atropine activity. Chlorpheniramine had neither a local anaesthetic nor a parasympatholytic effect. This study has therefore strengthened the hypothesis that there are nervous H1 receptors in the mucous membranes of the eye and airways and has extended its application in animals to also include man.
Adult↗
On the interrelations of immune and mediator receptors of mice lymphocytes.
It was shown that the blockade of M-cholinereceptors, of B-lymphocytes in the spleen of mice of the BALB/c line immune to sheep erythrocytes, by parasympatholytics 3H-Quinuclidinyl benzilate, etc., markedly inhibits the rosette-formation with the specific antigen. The blockade of M-cholinereceptors of B-lymphocytes in the mice spleen of the given line by the anticholinereceptor rabbit serum (with removed Forsmann antibodies) induces a similar result. The specific antigen fixation on B-lymphocytes of mice immunized by egg albumin is suppressed by preliminary blockade of M-cholinereceptors by the above mentioned parasympatholytics. The number of free cholinereceptors on the surface of B-lymphocytes of mice spleen immunized with egg albumin, was reduced after the specific antigen was joined. The blockade of beta-adrenoreceptors of mice spleen evokes a similar effect but in a lesser degree. The problem of interrelation of immune and mediator lymphocyte receptors is discussed in relation with the mechanisms of nervous regulation of immune and allergic reactions.
Animals↗
Effect of mechanical stimulation on mucociliary clearance of chicken sinus.
The hypothesis that homeostatic control mechanisms control mucociliary function in ciliated mucous membranes was induced artificially by means of mechanical stimulation. The edge of right palatine cleft was stimulated mechanically by gentle touching with a dissecting needle, and sinus clearance time was recorded as soon as mechanical stimulation was initiated. Mechanical stimulation caused acceleration of mucociliary flow of the sinus; sinus clearance time was accelerated on the side adjacent to the mechanically stimulated side of the palatine cleft, but not on the opposite side. Therefore, the reflex may be effective only on the stimulated side. We investigated the effect of nerve blockers on mechanical stimulation. Mucociliary clearance in the chicken sinus was not affected by parasympatholytic agents, but was decelerated by the beta-adrenergic blocker. The effect of nerve blockers on the mechanical stimulation showed that parasympatholytic agents blocked mechanical stimulation, while sympatholytic agents did not completely block the response. These data suggest that mucociliary clearance may be regulated by the reflex of parasympathetic and partially sympathetic nerve fibers.
Adrenergic Fibers↗