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PubMed1982

Timolol maleate in the treatment of glaucoma simplex and glaucoma capsulare. A three-year follow up study.

180 eyes of 97 patients with primary open angle glaucoma and IOP greater than 22 mm were treated for more than 3 years with timolol-maleate. 130 eyes had glaucoma simplex, and 50 eyes had glaucoma capsulare. With timolol maleate as the only medication after 3 years, the IOP was controlled in 33% of the glaucoma simplex group, and in 8% of the glaucoma capsulare group. No serious local or systemic side-effects were observed.

Aged↗

PubMed1985

A study of the efficacy of two commercial preparations of timolol maleate with special reference to side effects.

The intraocular pressure lowering effect of 2 commercial preparations of timolol maleate was studied in 57 adult outpatients suffering from open angle glaucoma or ocular hypertension. Special attention was paid to side effects of topical treatment with timolol, while comparing the efficacy of the 2 preparations. The intraocular pressure lowering effect with each strength (0.25% and 0.5%) of both preparations (Blocanol and Oftan-Timolol) was identical. No clearcut effect on lacrimal gland function, accommodation, or pupil size was seen. The adverse effects of timolol maleate during 6 months of treatment were of transient nature and generally mild. The only serious adverse effect was respiratory distress which occurred with 0.25% timolol in one patient. The respiratory distress developed slowly and the trial had to be discontinued for this patient after 2 months of treatment. There was a tendency toward a decrease in blood pressure and heart rate with both commercial preparations.

Clinical Trials as Topic↗

PubMed1989

Effects of trimebutine maleate on electrical activities of isolated mammalian cardiac preparations.

The effects of trimebutine maleate on electrical activity in guinea-pig isolated papillary muscles and rabbit sino-atrial nodes have been studied by means of a standard microelectrode method. In papillary muscles, trimebutine (above 10 microM) decreased the maximum rate of rise (Vmax) and the action potential duration at 90% repolarization (APD90), whereas the resting potential was not significantly altered. As to a decrease in Vmax, trimebutine produced a negative shift of the curve relating Vmax to the resting potential along the voltage axis. Trimebutine also depressed the slow action potentials of papillary muscles produced by 27 mM K and 0.2 mM Ba. In spontaneously beating sino-atrial node preparations, trimebutine (above 10 microM) decreased the heart rate, Vmax and the rate of diastolic depolarization. These results indicate that trimebutine maleate possesses a depressant action on the electrical activities of the fast- and slow-response fibres of the heart mainly due to inhibitions of both fast Na+ and slow Ca2+ channels.

Action Potentials↗

PubMed1984

Severe ocular side effects of perhexilene maleate: case report.

We report a case of perhexilene maleate (PEXID) toxicity in which the presenting feature was loss of vision secondary to chronic papilloedema. Vortex keratopathy similar to that seen in amiodarone keratopathy was present, and corneal and conjunctival biopsy findings are presented. To our knowledge this is the first case report of a keratopathy occurring in perhexilene toxicity. After withdrawal of the drug the papilloedema and keratopathy subsided, but some visual deficit remains. The properties of perhexilene maleate and other amphiphilic drugs are described, and the possible aetiology of vortex keratopathy is discussed.

Conjunctiva↗

PubMed1980

Perhexiline maleate toxicity on human liver cell lines.

When added to the culture medium of human liver cell lines, perhexiline maleate induced formation of numerous myeloid bodies containing unicentric or multicentric smooth membranes within a few days. The nine lysosomal enzyme activities studied, except for beta-galactosidase which decreased, remained unchanged. These results indicate that on cultured human liver cells perhexiline maleate has an effect similar to that described on hepatocytes of some patients treated with this drug and suggest that myeloid body formation is not due to impairment of lysosomal enzyme activities.

Adult↗

PubMed1984

Polymorphic hydroxylation of perhexiline maleate in man.

Long term perhexiline maleate therapy causes peripheral neuropathy and hepatic damage in certain subjects. An association between these adverse reactions and a genetically determined relative inability to hydroxylate debrisoquine has been described. This association could indicate either that the effects of perhexiline impair debrisoquine oxidation thus producing a phenocopy, or that perhexiline is polymorphically hydroxylated and that the polymorphism is controlled by the same alleles as control the debrisoquine polymorphism. To test the second possibility, a study investigating the hydroxylation status of a population of healthy volunteer subjects has been performed using perhexiline maleate. Hydroxylation phenotyping was performed on 50 normal volunteers. A standard oral dose was given and plasma and urinary perhexiline, 4-monohydroxyperhexiline (MI metabolite), and 4'monohydroxyperhexiline (MIII metabolite) was measured. The 24-hour plasma perhexiline concentration, the 24-hour plasma MI metabolite concentration, and 12 to 24-hour urinary MI metabolite excretion were clearly bimodal, suggesting the existence of a polymorphism for perhexiline hydroxylation. Poor metabolisers represent 6% of the population studied. Known poor metabolisers of debrisoquine are also poor metabolisers of perhexiline, while known extensive metabolisers of debrisoquine are also extensive metabolisers of perhexiline, indicating that in white British subjects the hydroxylation polymorphism is under identical genetic control for both compounds. The poor metaboliser sub-group exhibited the highest plasma perhexiline levels. Perhexiline phenotyping separates the poor and extensive metaboliser phenotypes much more clearly than other tests and defines a sub-group at risk from perhexiline toxicity. Pretreatment phenotyping using this test, followed by exclusion of poor metabolisers from perhexiline therapy, should substantially reduce the incidence of major adverse effects.

Adult↗

PubMed2002

The diagnosis of lichen-planus-like contact dermatitis to chlorpheniramine maleate.

In spite of the common use of the diagnostic category of lichen-planus-like contact dermatitis, we were unable to find established criteria for such a condition. An atypical distribution of otherwise typical lichen planus lesions is usually considered as a feature of a lichenoid eruption. When facing unusual or unexpected clinical features, it is always advisable to consider an adverse reaction to a medical intervention as a potential option. We report a lichen-planus-like eruption occurring after contact with a topical agent containing chlorpheniramine maleate. To our knowledge, this is the first reported case of lichen-planus-like contact dermatitis associated with chlorpheniramine maleate.

Aged↗

PubMed1986

Terfenadine and brompheniramine maleate in urticaria and dermographism.

The effects of brompheniramine maleate (12 mg twice daily in sustained release form) and terfenadine (60 mg twice daily) on the symptoms and well-being of 16 adults with urticaria with or without dermographism were assessed by symptom questionnaire. Following an initial 2-week period without therapy, each drug was taken for 2 weeks in a randomised double-blind cross-over study. Both drugs produced significant relief of itch and rash but only brompheniramine produced significant drowsiness. Brompheniramine maleate was more effective than terfenadine in the patients with dermographism.

Adult↗

PubMed1978

Evaluation of the local antihistaminic activity of dimetindene maleate by a quantitative method.

The topical application of a 0.1% dimetindene maleate gel on the forearms of 11 subjects reduces the areas of both erythema and wheal produced by the intradermal injection of 0.025 mg of histamine hydrochloride to a statistically greater degree than 1% d-chlorpheniramine maleate cream (p less than 0.005 and p less than 0.0005, respectively). The quantitative method employed in this study has proved to be an excellent means for the evaluation of the antihistaminic activity of topical preparations.

Administration, Topical↗

PubMed1978

Reduction of coronary blood flow during coronary artery spasm occurring spontaneously and after provocation by ergonovine maleate.

A 50-year-old man suffering from recurrent chest pain accompanied by transient ST-segment elevation developed spasm of the left anterior descending coronary artery after receiving ergonovine maleate. During spontaneous chest pain, thermodilution coronary sinus blood flow fell from 96 ml/min to 46 ml/min, while the coronary sinsu arteriovenous oxygen difference widened from 9.82 volumes percent to 11.3 volumes percent. During spontaneous relief of pain, coincident with resolution of the ST-segment changes, coronary sinus blood flow gradually rose to 135 ml/min, while coronary sinus arteriovenous oxygen difference narrowed to 6.82 volumes percent. Similar aterations in coronoary sinus blood flow accompanied chest pain provoked by ergonovine maleate. A thallium-201 scan confirmed a perfusion defect in the distribution the left anterior descending coronary artery. Thus, coronary artery spasm can produce a marked deficity in coronary blood flow that is associated with increased myocardial oxygen extraction; release of spasm creates a hyperemic response.

Coronary Angiography↗

PubMedDate not supplied

Analgesic activity of flupirtine maleate: a controlled double-blind study with diclofenac sodium in orthopaedics.

A controlled, parallel group study of the analgesic efficacy of flupirtine maleate, was compared against diclofenac sodium in 40 orthopaedic patients with post-operative pain. Clinically, both drugs were of equal analgesic efficacy. A mathematical model has been developed, however, to evaluate the speed, intensity and duration of the analgesic effect and provides data which significantly favour flupirtine maleate in the treatment of these patients.

Adult↗

PubMed2000

Effects of trimebutine maleate on delayed rectifier K+ currents in guinea-pig ventricular myocytes.

The effects of trimebutine maleate, a drug commonly used to regulate motility in the gastrointestinal tract, on the delayed rectifier K+ current (I(K)) were evaluated in guinea-pig ventricular myocytes to determine whether the drug has a proarrhythmic effect through blockade of I(K). Trimebutine decreased I(K) in a concentration-dependent manner. To investigate the effects of trimebutine on two components of I(K) (I(Kr) and I(Ks); rapidly activated and slowly activated components, respectively), we performed the envelope-of-tails test. Trimebutine-sensitive I(K) was determined by digital subtraction of I(K) during exposure to trimebutine from control I(K) for each duration of the test pulse over the range 50 ms-2 s. The ratio of deltaI(K,tail)/deltaI(K) plotted against pulse duration for trimebutine-sensitive I(K) gradually decreased to a steady-state value as the duration of the test pulse was lengthened. This finding suggested a weak inhibitory effect of trimebutine on both I(Kr) and I(Ks). The effects of trimebutine on the inward rectifier K+ current (I(K1)) responsible for the resting potential and final repolarization phase of the action potential were investigated by applying voltage clamp ramps over a broad range of potentials. No significant effects were observed at 10 or 100 microM. We next investigated the effects of the drug on the L-type Ca2+ current (I(Ca)). Significant inhibition of I(Ca) was observed at trimebutine concentrations greater than 10 microM. These results suggested that trimebutine maleate has weak inhibitory effects on I(Kr), I(Ks) and I(Ca) at concentrations much higher than those in clinical use.

Animals↗

PubMed1989

[Behavior of chlorpheniramine in vivo after administration of d- and l-chlorpheniramine maleate].

A high performance liquid chromatographic (HPLC) method was developed for the determination of chlorpheniramine (I) in the plasma. By this method, 1 ng of I could be measured. Plasma levels of I were determined by the HPLC method after oral administration of d-chlorpheniramine maleate (II) or l-chlorpheniramine maleate (III) to healthy subjects and dogs. Plasma levels of I brought about by oral administration of II were evidently higher than those by III both in humans and dogs. On the other hand, there was no difference in plasma levels of I when II or III was injected intravenously into dogs. Therefore, it was considered that the discrepancy in plasma levels of I after oral administration of II and III to dogs was neither due to a difference in elimination rate nor a distribution volume but rather in first-pass effect in absorption process. The result observed in the human study could be also explained in the same way as that in dogs.

Administration, Oral↗

PubMed1986

Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug (4). Mode of action on anti-inflammatory activity.

The possible mechanism of the anti-inflammatory activity of proglumetacin maleate (PGM), a new indomethacin (IND) derivative interacting with arachidonic acid (AA) metabolism, was investigated to elucidate the contributions of PGM itself and its two major metabolites, desproglumideproglumetacin maleate (DPP) and IND. PGM caused much less inhibition of PGE2 formation by sheep seminal vesicle microsomes (IC50 = 310 microM) and TXB2 formation by a washed rabbit platelet suspension (IC50 = 6.3 microM) than IND. DPP also caused less inhibition of cyclooxygenase than IND. Moreover, PGM had less effect on sodium arachidonate (SAA)-induced rat platelet aggregation ex vivo and AA-induced sudden death in rabbits than IND. These results show that PGM has anti-inflammatory activity after its conversion to the active metabolite IND. However, the inhibitory effects of PGM and DPP were as strong as that of IND on SAA- or collagen-induced rabbit platelet aggregation in vitro. These activities are considered to be associated with platelet membrane interaction. Moreover, unlike IND, PGM (IC50 = 1.5 microM) and DPP (IC50 = 16.3 microM) strongly inhibited 5-HETE formation by the cytosol of guinea pig polymorphonuclear leukocytes. This unique activity of PGM on 5-lipoxygenase may contribute to its anti-inflammatory activity.

Animals↗

PubMed1998

Effects of KW-5617 (zaldaride maleate), a potent and selective calmodulin inhibitor, on secretory diarrhea and on gastrointestinal propulsion in rats.

KW-5617 (zaldaride maleate), 1,3-dihydro-1-[1-[(4-methyl-4H,6H-pyrrolo[1,2-a][4,1]-benzoxazepin -4-yl)methyl]-4-piperidinyl]-2H-benzimidazol-2-one maleate, is a selective calmodulin inhibitor. We studied the effects of KW-5617 on secretory diarrhea and gastrointestinal propulsion in rats, as compared with those of loperamide, a conventional anti-diarrheal drug. Diarrhea was induced in rats either by 16,16-dimethyl prostaglandin E2 (500 microg/kg, i.p.) or by castor oil (1 ml/100 g body weight, p.o.). In the 16,16-dimethyl prostaglandin E2 model, KW-5617 at the doses of 3 mg/kg (p.o.) and higher ameliorated the diarrhea. Similarly, loperamide improved the diarrhea, the activity of loperamide being equivalent to that of KW-5617. In the castor oil model, KW-5617 significantly delayed the onset of diarrhea at the doses of 3 mg/kg (p.o.) and higher, while loperamide delayed the onset of diarrhea at the doses of 0.3 mg/kg (p.o.) and higher. KW-5617 only at the high doses of 30 and 100 mg/kg (p.o.) reduced gastric emptying, small intestinal propulsion, proximal colonic propulsion and distal colonic propulsion. In contrast, loperamide at its anti-diarrheal doses inhibited gastrointestinal propulsion. Our results show that KW-5617, unlike loperamide, at its anti-diarrheal doses does not exert anti-propulsive effects in rats. KW-5617 may be a useful drug for the treatment of diarrhea in terms of less side effects such as constipation.

Animals↗

PubMed1985

[The acute effects of the new angiotensin I-converting enzyme inhibitor, enalapril maleate, on blood pressure, plasma renin, aldosterone and kinins in hypertensive patients].

The acute antihypertensive effect of a new long-acting oral angiotensin I-converting enzyme (ACE) inhibitor, enalapril maleate, was assessed in 20 hypertensive patients, of whom 14 had essential hypertension, 4 had renovascular hypertension, one had hypertension associated with chronic renal failure, and one had primary aldosteronism. Enalapril maleate significantly lowered the blood pressure in either low-renin or normal- and high-renin hypertensives. There was a significant correlation for all patients as a group between the pretreatment levels of serum ACE activity and the reduction in mean blood pressure (r = -0.454, p less than 0.05, n = 20) 2 h after drug administration. The serum ACE activity decreased maximally 3 to 4 hours after drug administration and did not return to baseline levels within 24 h. There was a significant correlation between the reduction in mean blood pressure and changes in ACE activity 90 min and 2 h after drug administration, respectively, for all patients as a group (r = 0.495, p less than 0.05, n = 20, at 90 min; r = 0.508, p less than 0.05, n = 20, at 2 h). The plasma renin activity (PRA) significantly increased in normal- and high-renin hypertensives but not in low-renin hypertensives. There was a close correlation between the reduction in mean blood pressure and the PRA 8 h after drug administration in normal- and high-renin patients (r = -0.623, p less than 0.05, n = 13), while no such relationship was observed in low-renin patients. The plasma aldosterone concentration (PAC) significantly decreased within 3 h, the lowest values occurring at 8 h after drug administration, and it returned to baseline levels within 24 h in all patients. No relationship was found between the reduction in mean blood pressure and changes in PAC after drug administration in either low-renin or normal- and high-renin hypertensives. The plasma bradykinin concentration (PBC) increased within 1 h, the highest values occurring at 3 h after drug administration, and returned to baseline levels within 24 h in low-renin hypertensives, while the PBC was significantly increased at 4 h and had not returned to baseline levels within 24 h in normal- and high-renin hypertensives. There was a significant correlation between percentage changes in mean blood pressure and those in PBC 90 min after drug administration in normal- and high-renin hypertensives (r = -0.556, p less than 0.05, n = 13), while no relationship was observed between them in low-renin hypertensives.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1982

Effects of ACTH on the zona glomerulosa of sodium-loaded timolol maleate-treated rats: stereology and plasma hormone concentrations.

The effect of chronic ACTH administration on the growth and aldosterone secretion of the zona glomerulosa of sodium-loaded timolol maleate-treated rats was investigated by stereological and radioimmunological techniques. Combined sodium loading and timolol maleate administration induced a significant atrophy of the zona glomerulosa and its cells. The plasma concentration of aldosterone was significantly decreased, while that of corticosterone did not vary. ACTH administration completely reversed zona glomerulosa atrophy, and the plasma concentration of corticosterone was noticeably enhanced, whereas that of aldosterone underwent a further decrease. This data suggests that in the absence of the other adrenoglomerulotrophic factors, ACTH stimulates the growth of the zona glomerulosa, but transforms its parenchymal elements to a functional fasciculata cell type.

Adrenal Glands↗

PubMed1985

Effects of enalapril maleate (MK-421) on renovascular hypertension.

The effects of enalapril maleate (MK-421), a new angiotensin converting enzyme inhibitor, were studied on 5 patients with renovascular hypertension (RVH) due to unilateral renal artery stenosis. The therapeutic dosage was increased when the blood pressure (BP) was not controlled for more than 3 days. Blood sampling was performed before, and 5 hr and 24 hr after the first administration, and on the 3rd day with each dosage. The BP was normalized on 5 mg/day in 1 case, 10 mg in 1 case, 20 mg in 2 cases, and 40 mg plus mefruside in 1 case. Plasma renin activity (PRA) was significantly increased after 5 hr and recovered after 24 hr with 2.5 mg of the enalapril maleate, when the BP was not affected. This indicates that the increase in PRA is likely due to the reduced negative feedback of angiotensin II. When the blood pressure was lowered, PRA was increased and plasma aldosterone concentration (PAC) was decreased significantly. This rise of PRA may depend not only on the reduced negative feedback but also on the fall of BP. It is also considered that the PAC was decreased through the decrease in plasma angiotensin II. A fall of the glomerular filtration rate in one case and also a fall of the perfusion of the kidney of the stenotic side in another case were observed by radioisotope renograms. MK-421 administration was a useful treatment for RVH, and clearly normalized the BP of all the patients studied. However, there was a risk of a fall of renal function on the stenotic side due to the decrease in perfusion pressure.

Adolescent↗