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At least 721 records · Page 40Linked to original sources
PubMed1987

Responses of horses to acepromazine maleate administered orally in a paste.

The effects of acepromazine maleate (ACP), given orally in a paste form, were examined in six standard-bred geldings over a 12 hour period. Three dose rates, zero (placebo paste), 0.13 mg kg-1 and 0.26 mg kg-1, given before or after feeding, were investigated. The data were divided into two sampling periods for analysis, one from zero to 120 minutes and the other from four to 12 hours. Sedation was assessed by a score (TS score) based on general appearance, anal sphincter relaxation and penile protrusion. This TS score was significantly elevated 40 minutes after dosing with ACP, irrespective of whether the horses had been fed or not. Dose rate had no significant effect on TS in the zero to 120 minute sampling period, but the TS score was significantly (P less than 0.01) higher at the higher dose rate in the four to 12 hour period. At both dose rates, the TS scores were still significantly higher than their pretreatment values 12 hours after dosing. Systolic blood pressure (SBP), measured indirectly from the coccygeal artery, haematocrit (PCV) and total plasma protein concentration (TPP) were also examined. ACP caused significant falls in SBP and PCV, but the effect was complicated by feeding. ACP given after feeding had a reduced effect on SBP and PCV. Feeding appeared to cause a rise then a fall in PCV and TPP which was superimposed upon the fall caused by ACP. There was no difference between the two dose rates of ACP on SBP and PCV.(ABSTRACT TRUNCATED AT 250 WORDS)

Acepromazine↗
PubMed1978

[Cirrhogenic hepatitis due to perhexiline maleate: general review based upon one new case with ultrastructural study (author's transl)].

The authors describe a case of cirrhogenic hepatitis due to Pexid which was given for 8 months at 400 mg/day for a severe angina pectoris. We find here the anatomo-clinical profile of perhexiline maleate hepatiits already described in approximately 20 cases. There was a cirrhogenic evolution in our case as in 5 others : but here cirrhosis was revealing and seems stabilized since the treatment was stopped. The cirrhogenic evolution could be due to a cumulative effect of the drug and/or to an immuno-allergic mechanism as in alcoholic cirrhosis which is very similar, especially from an anatomical point of view. However cirrhogenic hepatitis differs by a characteristic lysosomal overload : brown pigment under microscopic observation and lipolysosomes with in some cases a lamellar structure under electron microscopic observation. The prescription of such a drug should be limited to cases of refractory angina pectoris and needed a regular clinical and biological survey.

Aged↗
PubMed1986

Absorption, distribution and excretion of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate in rats, dogs and monkeys.

Absorption, distribution and excretion of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) were studied in rats, dogs and monkeys after administration of [14C]-MN-1695. MN-1695 was found to be well absorbed from the small intestine after oral administration in all species examined. Plasma level of unchanged MN-1695 reached a maximum at 1 to 4 h after oral administration of [14C]-MN-1695 in rats, dogs and monkeys. The mean elimination half-life of unchanged MN-1695 from plasma was about 3, 4 and 50 h in rats, dogs and monkeys, respectively. Tissue levels of radioactivity after oral administration of [14C]-MN-1695 in rats indicated that [14C]-MN-1695 was distributed throughout the body and the radioactivity in tissues disappeared with a rate similar to that in plasma. A stomach autoradiogram after intravenous administration of [14C]-MN-1695 in the rat revealed the radioactivity localized in the gastric mucosa where MN-1695 was assumed to exert its pharmacological activity. In pregnant rats, [14C]-MN-1695 was distributed to the fetus with levels similar to maternal blood levels. After oral administration of [14C]-MN-1695 in rats, 39 to 46% of the dose was excreted into the urine and 50 to 63% of the dose into the feces, within 96 h. In dogs, about 40% of the dose was excreted into the urine and about 50% of the dose into the feces, within 6 days after oral administration. In monkeys, within 14 days after oral administration, about 60 and 30% of the dose were excreted into the urine and feces, respectively, and the main excretion route was the urine.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1986

Metabolism of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate in rats, guinea pigs, dogs and monkeys.

The metabolism of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) was studied in rats, guinea pigs, dogs and monkeys. MN-1695 was metabolized to more than 8 metabolites after oral administration in a dose of 3.1 mg/kg in rats. These metabolites were isolated from the urine and characterized by cochromatography with reference compounds, mass spectrometry and other instrumental analysis. The main metabolite in the urine was MN-1695 X m-OH, which was excreted as a conjugate, in rats and guinea pigs, and MN-1695 X N-oxide in dogs. In monkeys, MN-1695 X m-OH (free and conjugate) and MN-1695 X N-oxide predominated in the urine, although MN-1695 was not extensively metabolized. In rats, over 90% of the radioactivity excreted into the bile consisted of the polar metabolites. The major metabolic pathways of MN-1695 found in various animal species involved the hydroxylation at the positions of 3 and 4 of the aromatic ring and the N-oxidation at the position of 3 of the s-triazine ring. In addition, the sulfur-containing metabolites were detected in all species examined.

Animals↗
PubMed1986

[Value of esophageal manometry with the methylergometrin maleate test in angina with normal coronarography. The concept of esophageal angina].

22 patients presenting an "angina with normal coronarography" and 5 control subjects were subjected to a manometric exploration of the oesophagus in the basal state and under methylergometrine maleate (MEM) treatment. The MEM test is shown to be a good one for the induction of painful oesophageal dyskinesias, particularly in patients who had suffered in an inexplicable manner when that substance was administered for coronarography.

Adult↗
PubMed1986

Clinical experience with timolol maleate monotherapy of hypertension.

Beta-adrenergic blocking drugs are gaining acceptance as initial therapy for patients with mild to moderate hypertension. In a postmarketing surveillance study, 5,190 hypertensive patients received timolol maleate monotherapy and were evaluated by 1,355 physicians. A total of 1,057 patients did not complete the study: 28% of these patients experienced an adverse event. Mean systolic and diastolic blood pressure readings were reduced 20 and 13 mm Hg, respectively. Mean diastolic blood pressure was reduced 11% for patients with mild hypertension; larger mean reductions were noted for patients with moderate (17%) and severe hypertension (22%). The effect in black and elderly patients was less than in other groups. Although 22% of all patients experienced an adverse event, less than 2.2% of all patients experienced events related to beta-adrenergic blockade, ie, respiratory difficulty, heart failure, bradycardia, and cold extremities. Fatigue, dizziness, and nausea were the most frequently reported adverse events requiring discontinuation of therapy. Timolol monotherapy is a well-tolerated and effective treatment for a broad range of hypertensive patients.

Adult↗
PubMed1985

The effect of an aerosolized antihistamine, chlorpheniramine maleate, on exercise-induced bronchospasm.

We studied the effect on airway function of chlorpheniramine maleate (C), an H1 antagonist, delivered as an aerosol to 12 asthmatic subjects, 40 minutes before submaximal exercise. The study consisted of three protocol days. A first day established that the asthmatic subjects had exercise-induced bronchospasm (EIB). On the remaining two protocol days, 10 mg of C or a saline placebo (P) were administered by aerosol nebulizer in a double-blind randomized fashion over a 5-minute period. Pulmonary function was measured immediately after the aerosol inhalation as well as 10 and 30 minutes later. A 5-7-minute period of exercise was then performed by each subject on a cycloergometer, and lung function was again measured immediately and 5 minutes after exercise. Thirty minutes after the inhalation of C there was a significant increase in lung function parameters (1.80 +/- 0.23 to 2.32 +/- 0.34/sec for MEF40%(P); Mean +/- 1 SE, P less than .05) but not for placebo. MEF40%(P) remained significantly higher on the C day than on the P day following exercise; however, this difference was no greater than the difference seen immediately before exercise. We suggest that C promotes mild bronchodilation of asthmatic airways, and that this effect in EIB may be interpreted as the result of an alteration of baseline airway caliber.

Adult↗
PubMed1985

Potential systemic and ocular side effects associated with topical administration of timolol maleate.

A review of current literary sources disclosed a host of adverse reactions which may potentially be associated with the topical administration of timolol maleate. Systemic complications included a variety of cardiovascular, respiratory, central nervous system, gastrointestinal, and dermatologic reactions. Numerous ocular side effects were also reported including superficial punctate keratitis, ocular pain or discomfort, corneal anesthesia, and vague visual disturbances.

Eye↗
PubMed1985

[The anti-inflammatory effect of a combination of dimethindene maleate and betamethasone in topical formulations].

The antiinflammatory activity of three preparations (cream, ointment, jelly) of Fenistil Plus (betamethasone + dimethindene maleate) was shown by means of reflection densitometry, a new pharmacodynamic model. The three preparations led to restitution of the Tesafilm-stripped skin within 4 h. There was no significant difference in the efficacy of the preparations. After application of 10 g of the ointment the plasma levels of betamethasone remained within the limits of identification of the analytical method. An influence of the drug on the endogenous plasma hydrocortisone (cortisol) levels could not be found.

Administration, Topical↗
PubMed1985

Attempted suicide with acepromazine maleate: a case report.

1.25 g acepromazine maleate was consumed by a young woman in an unsuccessful suicide attempt. The drug is used extensively as an anesthetic premedication in veterinary practice. The woman had worked as a lay veterinary assistant. The clinical signs of toxicity were in part consistent with phenothiazine over-dosage in the human and were inconsistent with signs usually observed in animals.

Acepromazine↗
PubMed1985

[Evaluation of the systemic effects of timolol maleate in eye drops].

The systemic effects of timolol eye drops were investigated in 35 patients divided into three groups: 1. (15 asthmatics); 2. (10 non-asthmatic patients suffering from glaucoma); 3. (10 elderly control subjects). A placebo eye drops was given at time 0, the timolol maleate drops were given at time 30 mn. The control parameters were checked every 15 minutes. They did not show variations under placebo. After administration of timolol, systolic and diastolic blood pressures as well as vital capacity remained unchanged. Heart rate decreased in 91% of subjects by a mean: 18.5% and, extreme 38%: Bradycardia was always sino-atrial and there was a dose effect relationship. Also F.E.V., decreased in 13 of the 15 asthmatics and in 2 patients with chronic bronchitis: in 4 patients the decrease in flow exceeded 20%. The importance of timolol in the treatment of open-angle chronic glaucoma is well-established, but the results reported here and else where emphazing frequent risks should induce prescribers to comply with the rules of good use: analysis of previous history, and compliance with general contra-indications to beta blockers. Routine E.C.G. and strict adjustment of dosage is recommended.

Asthma↗
PubMed1979

The effects of perhexiline maleate (Pexid) and alcohol on rat liver.

Perhexiline maleate is an anti-anginal drug believed to cause liver damage. The possibility that this effect could be potentiated by alcohol has been investigated. Rats fed both the drug and alcohol did not show more severe liver damage than those fed alcohol alone. Livers from rats fed perhexiline alone did not differ from controls. There is no evidence from this study that alcohol potentiates the effect of perhexiline in rat liver. These results may have a bearing in perhexiline-induced liver damage in humans, but clinical studies are required.

Animals↗
PubMed1979

Semautomated method for the analysis of chlorpheniramine maleate tablets: collaborative study.

A semautomated method for the analysis of chlorpheniramine maleate tablets, which is based on the USP XIX general assay for salts of organic nitrogenous bases, was collaboratively studied by 6 laboratories. Collaborators were supplied with 4 composites from 4 manufacturers. In the method, the active ingredient is dissolved in dilute HCl, sampled, made basic with dilute NaOH, and extracted with isooctane. The isooctane phase is resampled and the drug is re-extracted into dilute HCl. The absorbance of the acidic aqueous solution is measured at 265 nm. The Associate Referee assayed the collaborative samples to compare the semiautomated and USP XIX methods, and found close agreement in the results from the 2 methods. In the collaborative study of the semiautomated method, there was excellent agreement of the results obtained by the collaborators. The coefficients of variation ranged from 0.46 to 2.24%. The method has been adopted as official first action.

Autoanalysis↗
PubMed1975

The anti-arrhythmic effects of perhexiline maleate in patients with ischaemic heart disease.

In a preliminary study which lasted 14 weeks, an anti-anginal preparation, perhexiline maleate (Pexid), was prescribed in a dosage of 200 mg twice a day to 7 patients who were suffering from cardiac arrhythmias associated with ischaemic heart disease. There was a significant reduction in ventricular extrasystoles during the 4th and 8th weeks of the study in 6 of the patients who had multiple ventricular ectopic beats. In 4 of these patients, an effective anti-arrhythmic response was maintained until the end of the study. These findings confirm other studies regarding the efficacy of the preparation in reducing ventricular extrasystoles in patients with cardiac ischaemia.

Arrhythmias, Cardiac↗
PubMed1979

Effect of perhexiline maleate on lipid metabolism in the rat.

The effect of long-term (7-11 weeks) administration of perhexiline maleate (Pexid) on liver, lung, plasma and bile lipids was studied in adult male Sprague-Dawley rats. Maximum non-toxic doses of the drug (80 mg/kg/day) produced a fall of total cholesterol concentration in liver, lung and plasma, a fall of total lung phospholipid concentration, and an elevation of bile flow and biliary bile acid excretion. Minimum lethal doses (160 mg/kg/day) produced an increased liver concentration of total phospholipids and gangliosides and decreased lung concentration of gangliosides. Plasma transaminase activity was not significantly affected in either of the treated groups.

Animals↗
PubMed1980

Pharmacology of ocular drugs. 1. Timolol maleate.

Timolol maleate is a new, potent ocular antihypertensive that has an effect additive with other antiglaucoma medications. It does not cause miosis and is relatively free of ocular complications, although a few have been documented. Timolol does exacerbate asthma and should not be used in patients with a history of this disease. It should be used with caution in cases of significant cardiovascular disease and may produce occasional psychic disturbances. In general, timolol is a potent, effective, and relatively safe drug with few ocular side effects but should be used with appropriate care.

Adrenergic beta-Antagonists↗
PubMed1980

[Studies on the solubility and the distribution behaviour of butaperazine dihydrogen maleate (author's transl)].

The present paper deals with the study of those parameters of butaperazine dihydrogen maleate, the knowledge of which is of importance in planning dosage forms for oral use. The solubility of the free butaperazine base in artificial intestinal juice (2.03 mg / 100 ml) was determined by means of the pKa values (pKa = 3.58 and pKa = 8.14). The total solubility decreases as the pH value of the dissolving medium increases, because the concentration of the base limits the solubility of the drug. Only the base can be distributed between n-heptane and an aqueous phase. The actual distribution coefficients are very high and explain the high solubility in fat. The water-lipid transfer was also estimated quantitatively. The highest velocities of transfer were observed at a pH value somewhat less than 7.0, as it is commonly measured in the small intestine. At pH 8.0, the low solubility of butaperazine became the velocity-limiting factor of the transfer. The velocities of the back transfer suggest that it is not wise to study the distribution behaviour of butaperazine in a three-phase model if the transfer at a buffer pH 7.4 is the centre of interest.

Gastric Juice↗
PubMed1981

The effect of timolol maleate on the disruption of the blood-aqueous barrier in the rabbit eye.

A disruption of the blood-aqueous barrier in rabbit eyes was elicited by use of topical prostaglandin E2(PGE2), infrared irradiation of the iris, or by subcutaneous alpha-melanocyte-stimulating hormone (alpha-MSH). The aqueous flare provoked was measured quantitatively with a photoelectric instrument. The effect of the (topical) beta-adrenergic antagonist timolol maleate on the breakdown of the blood-aqueous barrier was tested. Timolol applied topically in very large doses had no effect on exogenously administered PGE2. However, even in a very small concentration applied topically, timolol reduced the flare response to both infrared irradiation and alpha-MSH. These results support the theory that the effect of alpha-MSH and infrared irradiation on the blood-aqueous barrier is dependent on intact beta-adrenergic receptor sites.

Administration, Topical↗