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The syntesis of a number of 2-(5-substituted-2-thienylthio)benzoic acid derivatives is described. The synthesized compounds were screened for their muscle relaxant and parasympatholytic activities and the results are reported.
Two technics (chronic electrodes-electrointraperitoneography : EIG) have been used simultaneously in the conscious dog for the pharmacological study of drug effects on the electrical activity of intestine. The results show a good correlation between records obtained with the technic which needs a surgical operation (chronic electrodes) and the other which doesn't (EIG). The expected effects of the parasympathomimetic (acetylcholine-neostigmine) parasympatholytic (scopolamine) and adrenergic (epinephrine-neosynephrine) drugs used on the spiking activity are obtained with the two technics.
Contributions from various sources to the nasal fluid are a serious complicating factor for investigating the isolated role of the nasal glands in the production of this fluid. This study is an attempt to obtain a better insight in the secretory behaviour of the nasal glands and its neural regulation. Radioligand binding strongly suggests that rat nasal glands contain muscarinic receptors. Parasympathomimetic drugs mainly promote the discharge of the secretory proteins from the glandular cells. However, histological sections do not show any change in the number of secretory granules after parasympatholytic drug application. These observations refer to a complex nature of the parasympathetic regulation of the glandular secretory activity.
The authors remind the fundamental items of the bronchodilating treatments by means of pressurized aerosols using beta 2-agonists and parasympatholytics; a review of the literature on the toxicity of the different propellants used in the cartridges is presented. The problems proceeding from inequalities of deposition of the aerosols in the normal subjects and in lung diseases are stressed. Results regarding the prevalence of positive responses to aerosols of atropine methonitrate and to aerosols of a beta-agonist given to a group of patients with reversible broncho-obstruction are presented and discussed. The advantages of oxitropium bromide, a recently synthetized parasympatholitic drug which appears more interesting than ipratropium bromide, are discussed by means of the ventilatory results observed with both drugs in 19 patients with reversible broncho-obstruction. The interest of associating atropinics and beta 2-agonists in the same cartridges is discussed. The efficacy of a recently commercialized preparation associating fenoterol and ipratropium bromide is commented.
Disturbances of the bladder-urethra function may lead either to frequency, urinary incontinence, or urinary retention. A survey is given on the drugs most frequently used in the treatment of lower urinary tract dysfunction. Special attention is drawn to the use of parasympatholytics in the treatment of hyperactive detrusor function (unstable bladder), sympathomimetics in the treatment of decreased urethral resistance, parasympathomimetics in the treatment of hypoactive detrusor function and alpha-adrenergic blocking agents in the treatment of increased urethral resistance.
The change in the site of maximal flow-limitation with time in exercise-induced bronchoconstriction was studied in 16 asthmatic children by repeated measurements of maximal flow-volume curves in air and helium-oxygen (80/20). Bronchoconstriction shortly after exercise is determined by flow-limitation in the more peripheral airways in nearly all of the patients. Bronchoconstriction then fades away, while the site of maximal flow-limitation returns towards the central airways. Both variables have a significant relationship (P less than 0.05), which differs with time and among patients. The degree of protection by the beta-sympathetic agonist is more pronounced (mean 28%) than that of the parasympatholytic (mean 3%), and its action increases along with the degree of shift in the maximal flow-limitation towards the periphery. The implications for the mechanism involved and the therapy are discussed.
Ipratropium bromide is a parasympatholytic drug. After application to the nose, the nasal mucociliary transport time was measured using the method of the saccharin test. This compound did not cause any changes in the nasal mucociliary transport function.
Commonly used drugs that may cause sexual dysfunction are reviewed. The anatomy and physiology of the normal sexual response are reviewed. The influence of drugs on neurogenic, hormonal, and vascular mechanisms may result in diminished libido, impotence, ejaculatory and orgasmic difficulties, inhibited vaginal lubrication, menstrual irregularities, and gynecomastia in men or painful breast enlargement in women. Parasympatholytic agents, which interfere with cholinergic transmission, may affect erectile potency, while adrenergic inhibiting agents may interfere with ejaculatory control. Central nervous system depressants or sedating drugs, drugs producing hyperprolactinemia, and antiandrogenic drugs also may affect the normal sexual response. Drugs such as antihypertensive and antipsychotic agents may induce sexual dysfunction that can result in patient noncompliance. Usually, drug-induced side effects are reversible with discontinuation of the offending agent.
Complications from mydriatic and cycloplegic drugs are rare compared with their extensive use. Adverse effects are often related to dosage or other factors. The ocular complications include increased intraocular pressure, pigmentation of the conjunctiva and cornea, pigment in the anterior chamber, lacrimal duct blockage, macular edema, corneal endothelium damage, hyperemia, allergy, discomfort, and blurred vision. The systemic complications are those common to sympathomimetic and parasympatholytic drugs and include tachycardia, hypertension, headache, faintness. pallor, trembling, excessive sweating, palpitations, arrhythmias, confusion, hallucinations, drowsiness, ataxia, flushed skin, high fever, dysarthria, thirst, dry mouth, convulsions, disorientation, nervousness, coma, and death. An understanding of all possible side effects is of paramount importance to those using these drugs in the treatment of anticholinesterase poisoning. This review is intended as a ready reference to the adverse effects of mydriatic and cycloplegic drugs.
Thirty-seven subjects without eye diseases were treated with rociverine, a new direct myolytic and parasympatholytic antispasmodic: 15 by intravenous injection (20 mg) and 22 by oral administration (20 mg three times daily for four days). Intraocular pressure, pupil size, iridocorneal angle, blood pressure, and heart rate were checked before and during treatment. No clinically significant variations were observed in the parameters tested.
It has been known that chloroquine and mepacrine, through their parasympatholytic and spasmolytic effects, inhibit the gastric motility in rats. In the present study these drugs were shown to prevent by virtue of their antispasmodic property the spontaneous and induced movements in the isolated portal vein of the rat. As measured on isolated fundus strips of the stomach, chloroquine and mepacrine possessed almost the same pD'2 as had papaverine and drotaverine on the isolated portal vein. Chloroquine and mepacrine as well as the drugs used for comparison administered in vivo into the small intestine reached such concentrations in the portal vein blood which were shown to be capable of inhibiting the spontaneous and evoked movements in vitro.
OBJECTIVE: To compare, in psittacines, the mydriatic effects of several topically applied curariform, sympathomimetic, and parasympatholytic drugs with and without the addition of surface-acting penetrating agents. DESIGN: Prospective, randomized controlled trial. ANIMALS: 10 adult cockatoos (Cacatua sulphurea subspecies), 2 adult African gray parrots (Psittacus erithacus), and 3 adult Blue-fronted Amazon parrots (Amazona aestiva). PROCEDURE: Three curariform drugs (d-tubocurarine, pancuronium, and vecuronium bromide) and 2 autonomic drugs (atropine and phenylephrine hydrochloride) were evaluated. Drugs were tested with and without the addition of a surface-acting penetrating agent, either saponin or benzalkonium chloride. The agent that resulted in the most significant change in pupillary diameter with the fewest systemic side effects in the cockatoos then was evaluated for its effects in the African gray parrots and the Blue-fronted Amazon parrots. During each drug trial, 1 eye was randomly selected to receive the control drug (0.9% NaCl), and the opposite eye was selected to receive the test drug. Each pupil was videotaped 5 (cockatoos only), 15, 30, 45, 60, and 75 minutes after treatment. Pupil diameters were measured by use of a computerized image analysis system. Data for pupil size were analyzed by means of repeated measures ANOVA. RESULTS: Vecuronium without the addition of a surface-acting penetrating agent produced the most consistent and greatest pupillary dilatation in all 3 species with the fewest systemic side effects. CLINICAL IMPLICATIONS: Vecuronium is potentially a clinically useful, topical mydriatic agent for use in avian species. Documented differences in the prevalence of systemic side effects between species suggests that caution should be applied when applying this drug bilaterally.
Future advances in the pharmacotherapy of lung disease will occur mainly in the treatment of asthma, and will include the development of new long-acting beta 2-agonists, long-acting parasympatholytics, phosphodiesterase inhibitors, corticosteroids with fewer systemic side-effects, and other antiinflammatory drugs. Free radicals play an important role in most lung diseases, including asthma, emphysema, fibrosis, and adult respiratory distress syndrome. The search for free radical scavengers is now in progress. Replacement therapy with alpha 1-antitrypsin and surfactant is now possible. Progress in this area stems principally from a better understanding of the pathogenesis of lung disease.
The exact relationship between cardiac arrhythmias and sudden infant death syndrome (SIDS) is uncertain. Several reports have implicated both ventricular and supraventricular arrhythmias in isolated cases, but there have been no studies of the incidence or type of arrhythmias that occur in populations at risk for SIDS. Of 1699 infants at high risk for SIDS, 60 (4%) were found to have a primary cardiac arrhythmia (i.e., not associated with disordered respiration or apnea). The incidence of atrial and ventricular premature beats, supraventricular tachycardia, and Wolff-Parkinson-White syndrome was similar to the incidence found in normal infants. Primary bradycardia (defined as a heart rate less than 60 for greater than 10 s not associated with abnormal respiration) was the most common arrhythmia, occurring with a frequency and severity not seen in normal infants. Thirty-two infants experienced periodic bradycardia. In 19 of these latter infants, there were symptoms associated with these bradyarrhythmias that necessitated treatment. Heart rates as low as 20 beats/min were recorded. One infant presented with an episode of ventricular fibrillation and on further evaluation was noted to have recurrent bradyarrhythmias. In no infant was there abnormal prolongation of the QT interval. Primary bradyarrhythmias are seen at an increased incidence in infants at high risk for SIDS and may play a causal role in this syndrome. Most symptomatic infants can be adequately controlled with sympathomimetic or parasympatholytic therapy. Other cardiac arrhythmias occur at a rate similar to that in normal infants and are therefore unlikely to play a major role in SIDS.
The more extensive a surgical procedure in a small pelvis, the higher the risk for the lower urinary tract with its nerve supply and nerve plexus. This concerns mainly the sympathetic chains, the parasympathetic structures and, rarely, the visceral supply of the pelvic floor. Direct trauma to the bladder and its vascular supply as well as indirect injury by displacement of the bladder need to be seriously considered. Problems with micturition and impaired storage capacity of the bladder are the result. Complete urodynamic examination and follow-up can help in differentiating between temporary and persisting disturbances and in taking therapeutical decisions. The most evident postoperative complication is disturbed micturition, managed initially by suprapubic urinary diversion, followed as soon as possible by intermittent self-catheterisation. This is the only way to avoid overstretching of the bladder, recurring urinary tract infection and damage to the upper urinary tract. Restoration of spontaneous micturition can be supported by drug treatment with parasympatholytics and/or alpha-blockers if the measured bladder pressure and residual urine are within tolerable limits. For electrostimulation of micturition, intravesical therapy, although timeconsuming, is best suited because it can easily be done on an outpatient basis. More promising seems bilateral sacral neuromodulation, which, however, is a rather complicated and expensive procedure. Surgical procedures to reduce the voiding resistance of the bladder involve the risk of postoperative incontinence because the sphincter function in those patients is often disturbed too. Persisting problems with bladder storage capacity as a result of tumor surgery in the small pelvis are frequently secondary to retention of urine (overflow incontinence). In these cases, regular evacuation of the bladder by intermittent self-catheterisation can lead to social acceptance. Reduced bladder compliance and lowering of the urethral leak pressure point may result in stress and urge incontinence, which, according to the established rules, should be managed by physiotherapy and behaviour therapy as well as drug therapy and only in exceptional cases by surgical measures. Prevention of postoperative bladder dysfunction can be tried by tissue- and nerve-sparing surgical techniques, but is always determined by oncological aspects.
We describe two cases of severe colonic pseudo-obstruction (Ogilvie's Syndrome) after high dose clonidine i.v. infusions for delirium tremens. The first symptoms occurred 36 h and 5 days, respectively, after institution of therapy. The diagnosis of colonic pseudo-obstruction (CPO) was confirmed during emergency laparotomy in both cases. While other known risk factors may have been present, we propose that clonidine had a major parasympatholytic effect on the large bowel of these patients and was therefore responsible, either alone or in combination with these other factors, for the development of CPO. We conclude that the therapy of delirium tremens with high i.v. doses of clonidine carries the risk of provoking severe CPO, especially when other contributing factors are present. While therapy of the alcohol withdrawal syndrome with clonidine appears to be an attractive alternative to conventional treatment, ICU physicians should be alerted to this potentially serious complication.
RATIONALE: The time-course of the pupillary light reflex response is determined by the successive activation of the parasympathetic and sympathetic innervations of the iris, the latency and the amplitude reflecting parasympathetic and the recovery time mainly sympathetic activity. OBJECTIVE: To compare the effects of single doses of three antidepressants (venlafaxine: serotonin/noradrenaline reuptake inhibitor, paroxetine: selective serotonin reuptake inhibitor, and desipramine: tricyclic antidepressant) on resting pupil diameter and the pupillary light reflex response. METHODS: Fifteen healthy male volunteers participated in five weekly sessions, each of which was associated with one treatment (venlafaxine 75 mg or 150 mg, paroxetine 20 mg, desipramine 100 mg, or placebo) according to a double-blind, double-dummy, balanced, cross-over design. An infrared binocular television pupillometer was used for the recording of the resting pupil diameter and the pupillary light reflex in darkness, in previously dark-adapted eyes. Resting pupil diameter in darkness was recorded before and after treatment. The pupillary light reflex was elicited after treatment, with six light flashes (green, 565 nm peak wavelength) of 200 ms duration and of incremental illuminance (measured in the plane of the cornea): 3.0 x 10(-3) 8.5 x 10(-3) 2.5 x 10(-2), 7.0 x 10(-2), 0.18, 0.43 mW cm(-2). The parameters studied were: latency, amplitude and 75% recovery time. RESULTS: Analyses of variance followed by post hoc tests (least significant difference test or Dunnett's test; P < 0.05) revealed that both doses of venlafaxine produced a significant increase in resting pupil diameter, decrease in amplitude and shortening of the 75% recovery time of the light reflex response; venlafaxine 150 mg prolonged the latency, while the other treatments had no significant effects. CONCLUSIONS: The increase in resting pupil diameter could be indicative of parasympathetic inhibition and/or sympathetic activation. The shortening of the recovery time of the light reflex response is consistent with sympathetic potentiation resulting from noradrenaline uptake blockade in the iris. The prolongation of the latency and decrease of the amplitude of the light reflex response are indicative of a parasympatholytic effect of venlafaxine. However, as venlafaxine has negligible affinity for muscarinic cholinoceptors, this effect cannot be attributed to the blockade of cholinoceptors in the iris. A possible explanation for this finding is that it reflects a central rather than a peripheral effect of the drug: the blockade of noradrenaline uptake in the brain could lead to the potentiation of the noradrenergic inhibition of central parasympathetic (Edinger-Westphal) neurones. These results demonstrate the ability of therapeutically relevant single doses of venlafaxine to potentiate noradrenergic responses in man, consistent with the blockade of noradrenaline uptake.
OBJECTIVES: This study sought to determine the procedural success and the in-hospital outcome after primary coronary angioplasty in patients with acute inferior myocardial infarction and right ventricular involvement (RVI). BACKGROUND: RVI represents an easily detectable, highly prevalent subset of acute inferior infarction associated with poor outcome even in the era of thrombolysis. Primary PTCA may offer advantages in patients with inferior infarction involving the right ventricle. METHODS: Primary coronary angioplasty with optimal stenting was performed in 87 of 88 consecutive patients presenting within 24 hours after onset of acute inferior myocardial infarction. On the basis of right precordial ST segment elevations at admission, patients were classified into those without (n=61) and those with RVI (n=27). The patients were followed prospectively for angiographic success at 10 days and for in-hospital clinical outcome. RESULTS: Baseline characteristics including age, severity of coronary artery disease, proportion of stent implantation, and occurrence of cardiogenic shock were comparable. Patients with RVI had larger infarct sizes (lactate dehydrogenase level: 962 vs 580 U/l, P=0.03), developed more often complete atrioventricular block (18.5 vs. 2%, p=0.0038), needed more often parasympatholytics (48.1 vs 18.8%, p<0.001), and had a substantially higher incidence of the Bezold-Jarisch reflex (29.6 vs 6.6%, p<0.01) following reperfusion. Success of recanalization therapy acutely and at 10 days, as well as in hospital mortality were similar in patients with and without RVI (88.5 vs. 85.2%, 79.3 vs. 84.7%, 7.4 vs 9.8%). However, patients with RVI revealed a greater lumen gain acutely after PTCA (2.49 vs. 2.13 mm, p=0.025) and experienced less frequently major cardiac events (14.8 vs. 36.1%, p=0.04) which included reinfarction, re-ischemia, coronary bypass grafting, stent thrombosis, and cardiac death. In addition, procedural success was established more rapidly (fluoroscopy time: 10 vs 15 min., p=0.032) and with less contrast material (242 vs 295 ml, p=0.015) in patients with RVI. This is probably due to the more proximal location (84.6 vs 6.6%, p<0.0001) and the larger reference diameter (3.17 vs. 2.79 mm, p=0.03) of the occluded right coronary artery. CONCLUSIONS: Primary PTCA is an appropriate reperfusion strategy in patients with RVI. Further comparative studies are required to compare the effectiveness of primary PTCA with early thrombolytic therapy in this high risk setting.