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At least 289 records · Page 16Linked to original sources
PubMed1991

Anti-arrhythmic activities of six indole derivatives of changrolin.

The indole-derived compounds, which possessed side chains resembling those of changrolin (4-[3',5'-bis[(N-pyrrolidinyl)methyl]-4'-hydroxyaniline]-quinazoline) showed potent anti-arrhythmic activity by restoration of sinus rhythm from ouabain-induced tachycardia in guinea pigs. The potency was assessed by comparison of the maintenance time of sinus rhythm recovered from tachyarrhythmias induced by ouabain. The promising compound was MI2 with piperidyl residue on position 3 & 5 of phenol moiety. There was no difference in anti-arrhythmic activities resulting from substitutions between a benzene ring and methyl residue at position 2 of indole, but the latter had weaker parasympatholytic activity. The anti-arrhythmic activity of MI2 (greater than 60 min) was 2.4 times more potent then changrolin (25 min), but its anti-cholinergic activity was only half of the latter. To compare the suppressive effect on reperfusion-induced arrhythmias by iv MI2 at different time in relation to the ligation-reperfusion protocol, it was the most effective when administered either 30 min prior to coronary occlusion or at the moment of reperfusion. The compound MI might belong to the Ic group shown by the slowing impulse conduction within the heart.

Animals↗
PubMed1990

Effects of benzoyltropine and tropacocaine on several cholinergic processes in the rat brain.

Benzoyltropine and tropacocaine are two contaminants of street-cocaine reported to have parasympatholytic activity. Because the mechanism underlying this activity is obscure, we investigated the effects of these compounds on several cholinergic processes: sodium-dependent choline uptake, sodium-independent choline uptake, acetylcholine synthesis, acetylcholine release (spontaneous and veratridine-induced) and binding of [3H]quinuclidinyl benzylate to muscarinic receptors. These studies used rat cerebral cortical synaptosomes, except for the receptor-binding studies, which used whole brain plasma membranes. Benzoyltropine and tropacocaine each inhibited sodium-dependent choline uptake and acetylcholine synthesis in a dose-related manner that was competitive with extracellular choline. Benzoyltropine was 4 to 5 times more potent in both actions than tropacocaine. Sodium-independent choline uptake was not affected by either compound. Benzoyltropine (30 microM) had no effect on the sodium-dependent uptake of norepinephrine, gamma-amino-butyric acid, glutamate or serotonin; tropacocaine (30 microM) inhibited only norepinephrine uptake at this concentration. Benzoyltropine and tropacocaine each inhibited the spontaneous and veratridine-induced release of newly synthesized acetylcholine, but not via activation of presynaptic muscarinic receptors. Instead, each compound was able to attenuate the oxotremorine-induced inhibition of the release of acetylcholine, suggesting antimuscarinic activity. Binding experiments showed that benzoyltropine and tropacocaine were, respectively, about 1,000- and 10,000-fold less potent than scopolamine as receptor antagonists. Finally, we demonstrated that benzoyltropine accumulates in the rat brain after its peripheral injection (10 mg/kg i.p.) and remains there with a half-life similar to that of cocaine.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetylcholine↗
PubMed1990

[The atropine test in patients with stress incontinence and their treatment with a combination of diltiazem and oxyphenonium].

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.

Atropine↗
PubMed1990

Circadian rhythms of specific airway conductance and bronchial reactivity to histamine: the effects of parasympathetic blockade.

In ten healthy, nonsmoking, non-atopic, young volunteers, specific airway conductance and bronchial response to aerosolized histamine were measured plethysmographically at intervals of 4.8 h during two periods of 24 h, i.e. one day without, the other with, a parasympatholytic aerosol (0.20-0.24 mg ipratropium bromide) inhaled 1 h before each measurement, in order to determine the role of the parasympathetic innervation in the circadian rhythms of the airways. Specific airway conductance and bronchial reactivity showed clear circadian variations with corresponding peak times (16.11 and 04.41 h, respectively). Topical vagal blockade markedly increased specific conductance and resulted in a significant reduction of its rhythm amplitude, whereby the strong correlation between specific conductance and heart rate was significantly diminished. On the other hand, bronchial reactivity to histamine was lowered without flattening of its circadian rhythm. It is concluded that central parasympathetic outflow is an essential factor for the circadian rhythm of bronchial tone and, thus, for the increase in bronchial resistance at night.

Adult↗
PubMed1990

[Urinary incontinence and prolapse. Medical treatment and functional treatment].

Urinary continence implies that the variations of the vesical pressure does not exceed the capacities of the cervico-urethral closure system. The aim of the various methods of treatment is to have a beneficial action on those two parameters: drug therapy will mainly reduce the intra-vesical pressure (parasympatholytics...) and also improve the urethral tone (alpha-adrenergics...), or have a mixed effect on both systems (tricyclic antidepressants, oestrogens...). The side effects are often numerous due to the impact on the vegetative or neuromuscular system. The re-education is complemented by: local and general kinesitherapy, sensorial retrocontrol, associated or not to electrotherapy. Motivation and active participation of the patient are essential. The indications covers all the various pathologies (perineal insufficiency, defects in the body pattern, prolapse, sphincteral insufficiency, transmission problems, vesical instability, urethral instability) and concerns patients of all age groups.

Biofeedback, Psychology↗
PubMed1989

Intranasal ipratropium: literature abstracts and comments.

Eighty micrograms of the topically active parasympatholytic drug ipratropium were applied intranasally four times daily in 20 adults with perennial rhinitis and severe watery rhinorrhoea in a double-blind controlled cross-over trial. There was a significant reduction in nasal hypersecretion during ipratropium treatment. Fourteen patients preferred the ipratropium period, three the placebo period and three had no preference. There were no systemic or local side effects. Ipratropium was effective also in patients resistant to glucocorticoids, sodium cromoglycate and antihistamines. As the drug works immediately it can also be used before exposure to known provocating factors. It is concluded that continuous use of this new medication is of value in the management of severe rhinorrhoea in patients with perennial rhinitis, and that the occasional use is helpful in subjects with infrequent attacks of nasal hypersecretion.

Administration, Inhalation↗
PubMed1987

Nasal disorders and anticholinergic therapy.

Treatment of patients with perennial rhinitis, common cold and watery nasal hypersecretion, is still unsatisfactory. As the glands are innervated by parasympathetic nerves we examined the effect of intranasal application of a parasympatholytic drug, ipratropium bromide. In the laboratory we have studied the effect, dosage and duration of ipratropium in normal subjects. These investigations showed a strong inhibition of the secretion from the nasal glands for more than 6 hours in a dosage regimen with no local or systemic adverse effects. We continued in a placebo-controlled clinical short term study and an open long term study on patients with perennial rhinitis. Furthermore we conducted a clinical trial in patients with common cold. We found an effect on watery hypersecretion in all these patient groups. Several laboratory and clinical studies have since confirmed our results. Ipratropium inhibits the reflectory watery secretion from the nasal glands, but does not change the basal secretion rate. The onset of action is rapid and the effect is prolonged. Long term treatment is safe and may possibly have a curative effect in some patients.

Airway Resistance↗
PubMed1986

Oculocardiac reflex and the anesthesiologist.

Oculocardiac reflex is one of the trigemino-vagal reflexes, and is frequently observed during anesthesia for pediatric strabismus surgery. The reflex is greatly exaggerated in the presence of hypoventilation, hypoxemia and acidosis. The reflex is important as a cause of cardiac arrest during eye surgery. Several related reflexes are known, such as blepharocardiac reflex, oculorespiratory reflex, and the sudden infant death syndrome. Although the reflex can be prevented by a retrobulbar block or the administration of parasympatholytic drugs, well conducted anesthesia and cooperation with the surgeon is much more important.

Anesthesia, General↗
PubMed1986

Isolation, and characterization of a bioactive volatile oil from Ducrosia ismaelis Asch.

Physical characteristics, chemical constituents and biological activities of the volatile oil of Ducrosia ismaelis Asch. have been studied. It is a light yellow volatile liquid with a strong aromatic odour and a specific gravity of 0.9573. IR, NMR and GLC spectrometry studies revealed the presence of free alcohols, alkenes and highly conjugated alkenes, aromatic functions, alicyclic structures and cyclic ketones. The pharmacological studies show a highly significant and dose dependent central nervous system depressant and marked neuromuscular blocking actions. Experiments on smooth muscles and heart show a parasympatholytic activity. It also exhibits significant antimicrobial activity against Staphylococcus aureus, Bacillus subtilis and Candida albicans. Further studies are being undertaken to find out its mechanism of pharmacological actions and to identify the active principle(s) responsible for those effects.

Animals↗
PubMed1979

[Role of premedication in the prevention of accidents during aorto-coronary bypass].

Study of the type of premedication used in aorto-coronary bypass surgery involved 60 clinical cases of patients operated upon in the department of Professor GALEY (Henri Mondor Hospital, Creteil). The choice of drugs used showed the important role of tranquilisers and anxiolytics: diazepam, dipotassium chlorazepate, to which, in the majority of cases, were added an antihistamine: promethazine and a parasympatholytic: atropine. No accidents or complications were seen during the pre-anaesthetic period, and above all during the induction of anaesthesia in these patients, more than half of whom were in major cardiovascular decompensation. This would appear to confirm the efficacy of the drugs chosen for the premedication of these patients.

Adult↗
PubMed1982

[Pharmacodynamics of alizapride (author's transl)].

Studies of alizapride (N[(allyl-1 pyrrolidinyl-2) methyl] méthoxy-2 azimido-4,5 benzamide hydrochlorate) in mice and rats demonstrated little toxicity, particularly after parenteral administration. Alizapride's main pharmacodynamic effects are on the central nervous system. It is very effective against emesis induced by apomorphine and dihydrogenated ergot alkaloids in dogs. In this respect it is three times more effective than metoclopramide. In contrast to neuroleptics, alizapride does not modify equilibrium reflexes in mice, nor does it reinforce hypnosis induced by barbiturates. Only minor central antidopaminergic effects were recorded, less marked than those seen with metoclopramide. In mice, alizapride has no anticonvulsant or analgesic effects. It has little action on the autonomic nervous system or on the cardiovascular system. Alizapride has no antihistaminic or parasympatholytic effect. In dogs, sympatholytic effects and hypotension are seen only after giving a much higher dose than that which is effective against apomorphine and dihydrogenated ergot alkaloids.

Animals↗
PubMed1978

Macromolecular secretion by isolated gastric mucosa: fundamental differences in pepsinogen and intrinsic factor secretion.

The secretion of pepsinogen and intrinsic factor (IF) in response to various known stimulators and inhibitors of gastric acid secretion was examined in isolated rabbit gastric mucosa maintained in organ culture. Acetylcholine (10(-8) M) stimulated stimulated both pepsinogen (P less than 0.01) and IF (P less than 0.01) secretion and this stimulation was blocked by atropine. Parasympatholytic agents did not alter unstimulated (basal) secretion of pepsinogen even at high concentrations (atropine, 10(-2) M or propanthelene bromide, 5 X 10(-3) M), however, at these concentrations basal IF secretion was abolished. Histamine (10(-4) and 10(-2) M) had no effect on pepsinogen secretion but stimulated IF secretion (P less than 0.001). Antagonism of H2 receptors by cimetidine reduced both basal and histamine-stimulated IF secretion, but pepsinogen secretion remained unaltered. Under the conditions of the above experiments the gastric mucosal surface was not exposed to HCl but was constantly buffered by culture medium at pH 7.4. When we applied 50 mN HCl to the mucosal surface of the biopsies, pepsinogen secretion doubled (P less than 0.001) but IF secretion was abolished. These studies have clearly documented that: (1) fundamental differences exist in the responses of pepsin and IF secreting cells; (2) H+ ions bathing the mucosal surface of the stomach may influence the results of experiments designed to examine the mechanisms of gastric mucosal macromolecular secretion.

Acetylcholine↗
PubMed1984

Treatment of motor urge incontinence with clenbuterol and flavoxate hydrochloride.

A controlled double-blind trial is reported of the parasympatholytic drug, flavoxate hydrochloride, and the new sympathomimetic drug, clenbuterol, in the treatment of 39 women with motor urge incontinence. The clinical results and the urodynamic findings of urethro-cystomanometry after therapy showed clenbuterol to be very effective with few side effects.

Clenbuterol↗
PubMed1982

The efficacy and selectivity of pirenzepine. Review and commentary.

Pirenzepine is a new anticholinergic agent which selectively binds to gastric mucosal muscarinic receptors. We reviewed the double-blind, therapeutic studies on ulcer patients and the clinical pharmacology for evidence of healing and selectivity. Healing rates of ulcer at doses of 100-150 mg/day varied between 54-84% in trials with 718 duodenal ulcer patients and 630 patients with gastric ulcer. Total side effects incidence in these trials was 18.1%. At 150 mg/day, there was 13.5% incidence of dry mouth, 6.3% incidence of visual disturbance and 2.6% incidence of constipation. In clinical pharmacology trials, pirenzepine moderately inhibited gastric secretion with a slight inhibition of salivary secretion and esophageal motility at 100 mg/day. Higher doses produced the expected parasympatholytic profile, except for the absence of cardioacceleration. We conclude that pirenzepine in low doses, compared to classical antimuscarinic drugs, is relatively selective for gastric hyposecretion. It may be associated with a lower frequency of side effects in therapeutic trials at doses of 100-150 mg/day. Dry mouth and visual disturbance are the most common side effects. Selectivity is dose limited and has so far been demonstrated only at a daily dosage of 100 mg, in 2 divided doses.

Anti-Ulcer Agents↗
PubMed1980

A simple animal test system to predict the likelihood of a drug causing human physical dependence.

The test system utilizes adult, male, Sprague-Dawley rats to consume their entire daily water intake in a single 60 minute session. The results of administering various doses of more than 70 therapeutic agents 15 minutes prior to the test session permit the classification of drugs into two categories. Group I drugs cause only a dose-dependent reduction in water intake, beginning at a threshold value below which no effect is seen. Group II drugs, upon reaching a threshold value, cause first a dose-dependent increase in water intake to a maximum; additional dosage increments produce a dose-dependent decrease. Group I agents include: amphetamines, antidepressants, antihistamines, antipsychotics, narcotic antagonists, parasympathomimetics, and parasympatholytics. Group II includes agents known to induce human physical dependence, namely anxiolytics, barbiturates, sedative/hypnotics, and narcotic agonists. Double-blind testing has confirmed the value of this test system as a predictive screen for identifying drugs capable of causing physical dependence.

Animals↗
PubMed1981

Purinergic reflex activated by cathartics in the rat.

Phenlaxine and bisacodyl were shown to inhibit gastric emptying and motility by activating a reflex arising from the small intestine. This effect produced by the cathartics could not be prevented either by alpha or beta sympatholytic, or by parasympatholytic agents; further it was antagonized by quinine and quinidine, as well as by chloroquine and mepacrine in doses found to suppress gastric motility in untreated animals. The inhibition of gastric motility through cathartics does not appear to be due to an effect on adrenergic or cholinergic pathways but rather to involve a purinergic mechanism.

Animals↗
PubMed1982

Effects of cholinergic drugs and adrenergic drugs on aqueous humor formation in the rabbit eye.

The aqueous humor formation rate was determined in the anesthetized rabbit with a tracer dilution technique. The anterior chamber was cannulated with two 25-gauge needles: one was inserted into the posterior chamber through the pupil and the other was placed in the anterior chamber near the iridocorneal angle. Fluorescein-dextran solution was infused into the posterior chamber at a constant rate and the aqueous humor was collected through the anterior chamber needle. The aqueous humor formation rate and the volume of dye distribution were calculated simultaneously from the dye dilution curve. Utilizing this technique, the effects of the following substances on aqueous humor formation were studied following topical administration to the conjunctival reservoir: cholinomimetic drugs, pilocarpine and physostigmine; the parasympatholytic drug, atropine; adrenoceptor agonists, norepinephrine, epinephrine, isoproterenol and salbutamol; and beta-adrenoceptor antagonists, timolol and propranolol. Cholinomimetic drugs, i.e., pilocarpine 0.1 mg ml-1 to 10 mg ml-1 and physostigmine 1 mg ml-1, increased the aqueous humor formation rate, while atropine 1 mg ml-1 decreased the rate. The increase in aqueous humor formation by the cholinomimetics was completely antagonized with simultaneous administration of atropine. Norepinephrine 5 mg ml-1 and epinephrine 5 mg ml-1 reduced significantly both the aqueous humor formation rate and intraocular pressure (IOP). Isoproterenol 5 mg ml-1 caused a significant lowering of the blood pressure and IOP and tended to lower aqueous humor formation, although the decrease was not statistically significant. No significant effect on the blood pressure, IOP or aqueous humor formation was observed with isoproterenol 2 mg ml-1. Salbutamol 5 mg ml-1 raised the IOP while timolol 1 mg ml-1 lowered the IOP without any significant change in aqueous humor formation or blood pressure. Timolol 0.5 mg ml-1 or propranolol 5 mg ml-1 did not cause a significant effect on the blood pressure, IOP or aqueous humor formation rate.

Albuterol↗