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At least 1,099 records · Page 61Linked to original sources
PubMed1984

The effects of timolol maleate on subjective and physiological components of air travel phobia.

Twenty-one monophobic patients with moderately severe fear of flying were exposed to two 40 minute challenge flights after taking either Timolol 20 mg/day or placebo. Heart rate, blood pressure, subjective ratings of anxiety, fear and palpitation and Hamilton Anxiety Scale ratings were made at the predetermined assessment intervals. Post-treatment global ratings of improvement were provided by patients and the attending psychiatrist. Results showed that heart rate significantly increased from baseline with placebo while Timolol successfully inhibited tachycardia during the challenge flights. Subjective ratings of anxiety, fear and palpitations did not show any drug group differences. These variables, however, showed a non-significant decrease from outgoing to return flight assessments after an initial significant increase from baseline scores. Hamilton Anxiety Scale ratings showed a significant decrease from baseline to post-treatment assessments, irrespective of drug group. Global improvement ratings revealed no significant differences between drug groups. Overall ratings by the psychiatrist were generally more positive than patients' ratings, with the difference between the two sources of assessment reaching significance only in the placebo group. Disregarding group membership, heart rate was positively and significantly correlated with subjective ratings of fear, but not with palpitations or ratings of overall anxiety.

Adolescent↗
PubMedDate not supplied

Nomifensine maleate (Merital, Hoechst-Roussel).

Nomifensine is an isoquinoline antidepressant that inhibits the reuptake of dopamine at central synapses. It also inhibits norepinephrine reuptake but is only a weak inhibitor of 5-hydroxytryptamine. Open and controlled trials comparing nomifensine with placebo and other standard antidepressants have shown it to be an effective antidepressant in divided doses up to 200 mg/d. The full dosage range of 50-200 mg/d is well tolerated, and doses can be selected to suit patient disease, age, and therapeutic response. Minimal anticholinergic and sedative side effects and no impairment of psychomotor performance make nomifensine a suitable drug for use in a wide variety of ambulatory outpatients, including the elderly. A relative lack of cardiotoxicity and epileptogenic activity add to this profile; the safety of the drug, when taken in overdose, has been documented. However, the place of nomifensine in the treatment of depression, relative to other antidepressants, is still unclear.

Animals↗
PubMedDate not supplied

Safety and efficacy of bimatoprost 0.03% versus timolol maleate 0.5%/dorzolamide 2% fixed combination.

PURPOSE: To determine the efficacy and safety of bimatoprost given every evening versus the dorzolamide/timolol fixed combination (DTFC) given twice daily in open-angle glaucoma and ocular hypertensive patients. METHODS: A double-masked, three-center, prospective, randomized, crossover comparison with two 8-week treatment periods following a 4-week medicine free washout period. Diurnal curve intraocular pressures (IOPs) were taken at 08:00 (trough) and 10:00 and 16:00 hours. RESULTS: A total of 35 patients were enrolled and 32 completed all evaluations. The diurnal untreated baseline intraocular pressures was 24.8 +/- 2.4 mmHg. On the last day of treatment the mean diurnal intraocular pressures was 17.4 +/- 2.9 for bimatoprost and 18.1 +/- 2.8 mmHg for DTFC (p = 0.35). The individual time points for intraocular pressures were not statistically different between groups. Both groups statistically reduced the intraocular pressures from baseline for each time point and for the diurnal curve (p < 0.05). Regarding ocular safety and tolerability, there was more conjunctival hyperemia with bimatoprost (n = 15) than with DTFC (n = 7, p = 0.013) and more burning and stinging with DTFC (n = 12) than with bimatoprost (n = 0, p = 0.0005). Few systemic adverse events were recorded and there was no statistical difference between groups for any individual event (p > 0.05). CONCLUSIONS: This study indicates that the intraocular pressures are lowered to a statistically similar amount with DTFC compared to bimatoprost in open-angle glaucoma and ocular hypertensive patients.

Amides↗
PubMed1984

Left ventricular changes after chronic therapy with enalapril maleate in moderate to severe hypertensive patients.

A randomized double-blind trial was carried out to determine the relationship of the changes in blood pressure and heart rate with changes in echocardiographic left ventricular indices in moderate to severe hypertensive patients with established left ventricular hypertrophy who were being treated chronically with enalapril or hydrochlorothiazide plus propranolol for 26 weeks. After a 2-week period on placebo, drug dosages in the two groups were adjusted to individual needs until blood pressure was normalized (diastolic less than 90 mmHg). Patients in Group I received 10 to 40 mg enalapril/day; those in Group II received 50 mg hydrochlorothiazide plus 80 to 240 mg propranolol/day. Echocardiographic measurements were made at the end of the placebo and 26-week active treatment periods. Significant correlations were observed between the changes in four pairs of variables in each group. In the 8 patients receiving enalapril, there were negative correlations between interventricular septal thickness and supine systolic blood pressure, erect and supine heart rates, and a positive correlation between relative wall thickness and erect diastolic blood pressure. In the 7 patients on hydrochlorothiazide plus propranolol, there were negative correlations between relative wall thickness and erect and supine heart rate, and positive correlations between left ventricular mass and erect diastolic blood pressure, and the percentage change in internal diameter of the left ventricle and supine systolic blood pressure. Possible explanations for and implications of these regional changes are discussed.

Adult↗
PubMed1999

A comparison of the intraocular pressure-lowering effect of 0.5% timolol maleate and the docosanoid derivative of a PGF2 alpha metabolite, 0.12% unoprostone, in subjects with chronic open-angle glaucoma or ocular hypertension.

The efficacy of 0.5% timolol was compared with that of the prostaglandin derivative unoprostone in maintaining control of intraocular pressure (IOP) in subjects with chronic open angle glaucoma (COAG) or ocular hypertension (OH) already responding satisfactorily to beta-blocker monotherapy. In a two-centre, double-masked, randomised parallel group study, 40 subjects were placed on 0.5% timolol eyedrops twice daily for two weeks. They were then randomised either to continue with 0.5% timolol or to switch to 0.12% unoprostone, applied twice daily for six weeks. IOP was measured at two-weekly intervals. The status of the conjunctiva, iris, cornea and anterior chamber was kept under observation. Ocular safety was monitored by measurements of visual acuity, and any systemic adverse events were recorded. After six weeks' treatment, there were no statistically significant differences in mean change from baseline IOP within or between treatment groups. For the subjects treated with unoprostone, mean IOP increased by 0.69 mm Hg (p = 0.368) while that of the timolol-treated subjects fell by 0.47 mm Hg (p = 0.287). The difference in mean IOP between groups was 1.16 mm Hg (p = 0.211, 95% confidence interval [CI] -0.69 to 3.02). The most common complaint was a mild and transient burning sensation on instillation which occurred more frequently in the unoprostone group. In conclusion, an aqueous solution of 0.12% unoprostone isopropyl, applied topically to the eye twice daily for six weeks, was as effective as 0.5% timolol in maintaining control of IOP in subjects with chronic open angle glaucoma or ocular hypertension. Both treatments were safe and well tolerated.

Adrenergic beta-Antagonists↗
PubMed1978

Lisuride hydrogen maleate: evidence for a long lasting dopaminergic activity in humans.

In 12 acromegalics a single oral dose of 0.2 mg lisuride, an ergoline derivative, significantly reduced plasma PRL but not GH concentrations. Three-tenths milligram of the drug significantly reduced plasma levels of the two hormones. Four-tenths milligram of lisuride did not augment this inhibitory effect. Plasma PRL levels were suppressed in all patients, whereas GH levels were reduced by more than 50% of the base-line values in only seven patients who also responded to the administration of 2.5 mg bromocriptine (CB154). In the patients unresponsive to lisuride, CB154 also failed to change GH levels. The suppressive effect of lisuride started at 60 min (at 150 min for CB154) and plasma GH and PRL levels were still markedly suppressed at 300 min. Plasma GH and PRL concentrations were consistently reduced in two acromegalic patients during 2 weeks of chronic treatment with 0.3 mg lisuride four times a day. In six normal subjects, TRH-induced PRL release was significantly inhibited by pretreatment with 0.3 mg of the drug. The similarity in the effects of lisuride and CB154 suggests that the observed effects of lisuride on GH and PRL are attributable to the known dopaminergic activity of the drug. This conclusion is supported by the data showing that pimozide effectively counteracted the inhibitory action of lisuride on GH and PRL release. We suggest that lisuride may be of value in the medical treatment of acromegaly and hyperprolactinemic states.

Acromegaly↗
PubMed2000

The effect of zaldaride maleate, an antidiarrheal compound, on acetylcholine-induced intestinal electrolyte secretion.

The effect of zaldaride on acetylcholine-induced colonic electrolyte secretion was examined. The short-circuit current response to acetylcholine was partially reduced by tetrodotoxin, a neuronal blocker, and was completely inhibited by atropine, an acetylcholine M receptor antagonist, in the rat colonic preparations. The tetrodotoxin sensitive effect was significantly inhibited by zaldaride, whereas the tetrodotoxin insensitive effect was not affected. Acetylcholine release from synaptosomes of submucosal nerves of guinea-pig colon was significantly reduced by zaldaride. Zaldaride may reduce colonic electrolyte secretion by acetylcholine due to the inhibition of acetylcholine release from synaptosomes of colonic submucosal nerves.

Acetylcholine↗
PubMed1985

Serum concentration and effects of a single dose of enalapril maleate in patients with essential hypertension.

The antihypertensive effect of a non-sulfhydryl, long acting ACE (angiotensin converting enzyme) inhibitor, MK-421, was evaluated by administering a single dose of 10 mg to 13 patients with mild to moderate essential hypertension. The pharmacokinetic profile of MK-421 and its potent active metabolite, MK-422, was also assessed, together with the effect on the various components of the renin-angiotensin system. A single dose of MK-421 produced a significant fall in MBP from 2 to 24 hours post-drug. As could be expected, plasma ACE activity was suppressed up to 24 hours after MK-421. The half-life of MK-422, Cmax and [AUC]24(0) of MK-421 and MK-422 were measured. No significant change in plasma bradykinin or urinary excretion rate of kallikrein was observed, whereas a slight increase was observed in the urinary excretion rate of kinins after MK-421 in 8 patients. Significant correlations were observed between pretreatment PRA levels and the maximum fall in MBP.

Adult↗
PubMed1979

[Effect of 1-[(1-pyrrolidynylcarbonyl) methyl]-4-(3, 4, 5-trimethoxycinnamoyl)piperazine maleate (cinepazide) on cerebral and peripheral circulation in cats (author's transl)].

Effects of cinepazide, a vasoactive agent, on regional circulations in various sites of brain and other organs in curarized, artificially respirated cats were studied using a thermoelectrical method. The mechanism of the vascular effect was also investigated. Cinepazide produced a marked increase in blood flow in the cerebellar cortex and an apparent increase in blood flow in the cerebral cortex. Effects of the drug on blood flow in the thalamus, hypothalamus and amygdala were inconsistent. Cinepazide produced the most significant increase in myocardial blood flow and also an apparent increase in muscular blood flow, whereas the drug did not consistently alter hepatic blood flow, and decreased renal and dermal blood flow. Cinepazide produced a mild and sustained fall in blood pressure, however, a transient slight rise in blood pressure was noted when the drug was given into the vertebral artery. It seems possible that the action of cinepazide might involve a mild stimulation of beta adrenergic receptors and slight stimulation of alpha adrenergic receptors but not cholinergic receptors, in the cerebral and peripheral vascular systems. Increase in blood flow induced by cinepazide seems to be mainly due to the smooth muscle relaxant effect and may be mediated via a metabolic mechanism.

Amygdala↗