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At least 937 records · Page 52Linked to original sources
PubMed1978

Influence of cicloxilic acid on the intracellular transport of 3H-palmitic acid during acute ethanol fatty liver.

cis-2-Hydroxy-2-phenyl-cyclohexanecarboxilic acid (cicloxilic acid) modifies the rat's hepatocyte intracellular movements of 3H-palmitic acid in the course of fatty liver by acute ethanol intoxication. It counteracts the impairment of radioactive lipid uptake due to ethanol treatment and promotes the early and complete release of the radioisotope inhibited by ethanol. The relevance of these results to the role of changes in the intracellular transport systems in the pathogenesis of ethanol steatosis is discussed. This and previous studies show that cicloxilic acid acts by stimulating the intracellular lipoprotein transport probably preventing by this mechanism the ethanol induced liver injury.

Animals↗
PubMed1987

Distribution of tranexamic acid to plasma and saliva after oral administration and mouth rinsing: a pharmacokinetic study.

The objective of the study was to investigate the content of tranexamic acid in plasma and in mixed, unstimulated whole saliva after oral administration and mouth rinsing. Ten healthy volunteers each received 1 g of tranexamic acid orally, whereas 20 healthy volunteers rinsed their mouths with 10 mL of a 5% aqueous tranexamic acid solution for two minutes. Blood and saliva were collected 30, 60, 120, 240, 360, and 480 minutes after administration of tranexamic acid. Samples of blood and saliva were analyzed for tranexamic acid content by electron capture gas chromatography. After oral administration, the mean plasma concentration of tranexamic acid reached its maximum after 120 minutes at approximately 7 micrograms/mL, whereas none of the saliva samples contained tranexamic acid at detectable levels. After mouth rinse, the plasma concentrations remained below 2 micrograms/mL, whereas the concentrations found in saliva initially were very high (after 30 minutes mean concentration above 200 micrograms/mL) and remained at a therapeutic level for more than two hours. These findings indicate, that fibrinolysis in the oral cavity can be inhibited only by local administration of tranexamic acid. This finding may be of significance when the drug is used for prevention and treatment of bleeding in the oral cavity in patients with coagulation defects.

Administration, Oral↗
PubMed1978

The anaerobic decomposition of benzoic acid during methane fermentation. IV. Dearomatization of the ring and volatile fatty acids formed on ring rupture.

A possible pathway for the anaerobic utilization of benzoic acid by a methanogenic consortium is suggested. Cyclohexane carboxylic acid and 1-cyclohexene-1-carboxylic acid have been identified as intermediates before ring rupture. Suprisingly, 3-cyclohexene-1-carboxylic acid interferes with utilization of other cyclic acids. In addition, isobutyric acid or short chain acids containing carbon-carbon double bonds could not be used without induction periods of a week or longer. A number of volatile fatty acids (heptanoic, valeric, butyric, propanoic, and acetic) have been identified and are suggested intermediates.

Anaerobiosis↗
PubMed2003

Asymmetric synthesis of the putative structure of (-)-oryzoxymycin.

[reaction: see text] A short asymmetric synthesis of (2'S,5R,6R)-2'-[6-amino-5-hydroxy-1,3-cyclohexadiene-1-carbonyloxy]propionic acid, the enantiomer of the reported structure of (+)-oryzoxymycin is described. The reported spectral data does not match that obtained for synthetic "oryzoxymycin".

Cyclohexanecarboxylic Acids↗
PubMed1991

2-amino-4-phosphonobutyric acid exerts a light-dependent effect on post-gabaculine levels of retinal gamma-aminobutyric acid (GABA): evidence that ON synaptic pathways regulate retinal GABAergic transmission.

The effects of light, 2-amino-4-phosphonobutyric acid (APB), and kainic acid on rat retinal gamma-aminobutyric acid (GABA)-ergic transmission were studied by measuring levels of retinal GABA following subcutaneous injection of gabaculine, an irreversible inhibitor of GABA-transaminase. Post-gabaculine levels of retinal GABA in light-exposed rats were significantly greater than those in rats held in darkness. The synaptic mechanism of this effect of light was examined by measuring post-gabaculine levels of retinal GABA in rats placed into either lighted or darkened conditions after receiving unilateral intravitreal injections of APB, a glutamate analogue that selectively decreases the activity of ON synaptic pathways in the retina. APB attenuated the post-gabaculine accumulation of GABA in rats held in the light, but not in those placed into darkness. Furthermore, the light-dependent increment in post-gabaculine accumulation of retinal GABA was entirely APB sensitive, and the effect of APB was entirely light dependent. In contrast to APB, kainic acid stimulated the post-gabaculine accumulation of retinal GABA in vivo. Our findings suggest that APB and kainic acid influence GABAergic transmission at different sites in the retina and that some retinal GABAergic neurons are either ON or ON-OFF amacrine cells.

Aminobutyrates↗
PubMed1999

The clinical pharmacokinetics of the new antiepileptic drugs.

Because pharmacokinetics is a major determinant of the magnitude and duration of pharmacologic response, understanding the kinetic properties of the new antiepileptic drugs (AEDs) is essential for the correct use of these compounds in clinical practice. After oral administration, absorption is rapid and relatively efficient for the new AEDs, the most notable exception being gabapentin, whose bioavailability decreases with increasing dosage. None of the new AEDs is extensively bound to plasma proteins except for tiagabine, which is over 95% protein-bound. The route of elimination differs to an important extent from one compound to another, and elimination half-lives range from over 30 h for zonisamide to 5-7 h for gabapentin. For all drugs that are metabolized, half-life is shortened and clearance is increased when patients receive concomitant enzyme-inducing agents such as barbiturates, phenytoin, and carbamazepine. Lamotrigine metabolism is markedly inhibited by valproic acid, and felbamate may increase the serum levels of most other AEDs. Felbamate, topiramate, and oxcarbazepine may also reduce the efficacy of the contraceptive pill by stimulating its metabolism.

Acetates↗
PubMed1977

Traumatic hyphaema treated with the antifibrinolytic drug tranexamic acid II.

During the year 1976 (January 1st to December 31st) 75 patients, consecutively admitted to the eye department of Arhus Kommunehospital with traumatic hyphaema, were treated with the antifibrinolytic drug tranexamic acid. No secondary haemorrhage occurred. The patients were not confined to bed. The eyes were not patched and the activities of the patients were not restricted. In a previous series from 1975 where the patients were confined to bed but otherwise treated identically with tranexamic acid one out of 72 patients had a secondary haemorrhage. When the two materials are combined one out of 147 patients had a secondary haemorrhage corresponding to 0.68%.

Adolescent↗
PubMed1978

A double-blind study on the influence of tranexamic acid on the intraocular pressure and the central corneal thickness after trabeculectomy for glaucoma simplex.

The influence of tranexamic acid on the intraocular pressure and central corneal thickness has been examined by means of a double-blind trial in patients with glaucoma simplex. The material comprised 28 patients (14 pairs) who had all been operated on for glaucoma in one eye by trabeculectomy. Tranexamic acid was found not to influence the intraocular pressure, neither in the operated eye nor in the opposite eye. The possible antifibrinolytic effect on the outflow of the aqueous humour is discussed. As in previous studies an effect of tranexamic acid on the central corneal thickness was found in both the operated and in the non-operated eye. A possible mechanism behind this is discussed.

Aged↗
PubMed1983

Effect of cicloxilic acid on bile lipid composition in patients with gallstones: a multicenter trial.

24 gallstone patients were treated with cicloxilic acid, an agent endowed with choleretic activity, at the dose of 240 mg/day for 1 month. 24 comparable patients on placebo treatment acted as controls. Bile lipid composition was determined and the saturation index calculated before and after treatment, on samples collected by duodenal siphonage after caerulein stimulation, in both groups. In the cicloxilic group there was little or no change in bile salts and phospholipids, whereas biliary cholesterol concentration was significantly reduced (p less than 0.05) and consequently the lithogenic index lowered (from 1.5 to 1.2, p less than 0.01). Cicloxilic acid can have a place in gallstone disease therapy in association with the litholytic bile acids or in the prevention of gallstone formation in high-risk populations.

Adult↗
PubMed1996

Clinical pharmacokinetics of newer antiepileptic drugs. Lamotrigine, vigabatrin, gabapentin and oxcarbazepine.

The clinical pharmacokinetics of the 4 antiepileptic drugs lamotrigine, vigabatrin, gabapentin and oxcarbazepine have been reviewed in this paper. All the drugs have linear kinetics and reliable absorption, although the saturation of transport across the gut may occur at high doses with gabapentin. All the drugs can be conveniently given as a twice daily dosage apart from gabapentin, which has a short half-life and a midday dose is needed. Unlike many of the older drugs, lamotrigine, vigabatrin and gabapentin have a predominantly renal excretion and are not metabolised through the cytochrome P450 system. They do not induce their own metabolism or that of other commonly used anticonvulsants. Similarly, clinically important interactions with other major classes of drugs metabolised this way, such as anticoagulants or steroid hormones, do not occur. Oxcarbazepine, however, can cause oral contraceptive pill failure. Oxcarbazepine is immediately metabolised to a hydroxy metabolite and could be considered a prodrug. It appears to have fewer pharmacokinetic interactions than carbamazepine. Valproic acid (sodium valproate) inhibits the glucuronidation of lamotrigine and increases its half-life; when used together, dosage modification of lamotrigine is needed to avoid toxicity.

Acetates↗
PubMed1988

An objective evaluation of flurbiprofen and tranexamic acid in the treatment of idiopathic menorrhagia.

The effect of flurbiprofen (100 mg x 2 for 5 days) was compared with tranexamic acid (1.5 g x 3 for 3 days, 1 g x 2 days 4 and 5) in the treatment of 15 women with idiopathic menorrhagia. The mean blood loss during two medication-free periods was 295 +/- 52 ml. A significant (p less than 0.01) reduction in menstrual blood loss was recorded during treatment with both flurbiprofen and tranexamic acid. The menstrual blood loss was significantly (p less than 0.01) lower during treatment with tranexamic acid (155 +/- 33 ml) than with flurbiprofen (223 +/- 44 ml). Various side effects were recorded by 7 of 15 women during treatment with tranexamic acid and by 4 women of 15 during treatment with flurbiprofen. Many women with menorrhagia suffer simultaneously from dysmenorrhea. Thus although tranexamic acid was generally more effective in reducing menstrual blood loss, flurbiprofen provides an important therapeutic alternative to antifibrinolytic agents, especially in patients with concomitant dysmenorrhea.

Adult↗
PubMed1979

New approach to protein-losing gastroenteropathy.

Fibrinolytic activity in the biopsied gastrointestinal mucosa was investigated in patients with protein-losing gastroenteropathy, and the increased activity was observed in patients associated with erosive gastritis, Menetrier's disease, atrophic gastritis, or Crohn's disease. However, patients with intestinal lymphangiectasia showed normal mucosal fibrinolysis. Antifibrinolytic therapy with tranexamic acid revealed significant therapeutic effect in the group with increased mucosal fibrinolysis. It is concluded that tranexamic acid appeared to be successful in blocking the vicious circle of "membrane disorder","increased tissue fibrinolysis", "increased vascular permeability", and "hypoproteinemia" in protein-losing gastroenteropathy.

Antifibrinolytic Agents↗
PubMed2000

New antiepileptic drugs and preparations.

Epilepsy affects 1.2% to 4.4% of the general population. Given the clinical profile of the newer antiepileptic agents, it is likely their usage will increase in the coming years, thus increasing the emergency physician's exposure to these medications and their side effects. Several of these side effects can have high morbidity, such as the aplastic anemia and hepatotoxicity caused by felbamate, and the Stevens-Johnson syndrome associated with lamotrigine. Overdoses of these medications also could increase, as will our knowledge of recognizing and managing them. The clinical spectrum of the newer medications is the treatment of partial seizures. None of the newer medications can be orally loaded nor are they available in an i.v. preparation. Serum drug levels are not available in most institutions and are not routinely measured in the ED. The new preparations of phenytoin, diazepam, and valporic acid add increased efficiency in drug administration, providing a new method for prehospital treatment of seizures and a more tolerable means of administration in the ED.

Acetates↗
PubMed1972

In vitro synthesis of procollagen on polysomes.

The major collagenous products synthesized in a cell-free polysome preparation are pro-alpha1 and pro-alpha2, formed in a ratio of 2:1. They are the precursor forms of alpha1 and alpha2 chains of normal connective-tissue collagen that are also formed in small amounts. A procollagen peptidase activity has been demonstrated in the supernatant fraction that can account for the formation of alpha1 and alpha2 chains from their precursors. The polysomal system is activated by a salt extract of reticulocyte ribosomes and is inhibited by aurintricarboxylic acid, suggesting that the polysomes are able to initiate protein synthesis.

Animals↗
PubMed1996

Gabapentin for the treatment of hemifacial spasm.

Pharmacologic therapy for hemifacial spasm is often limited by the paucity of effective medications and problems with side effects. Gabapentin is a novel antiepileptic drug that is generally well tolerated. Its anticonvulsant effect is independent of gamma-aminobenzoic acid (GABA) receptor mechanisms. We report a patient with hemifacial spasm who responded well to gabapentin therapy. Gabapentin may be a useful alternative medical therapy to currently used drugs.

Acetates↗
PubMed1978

Prolonged antifibrinolysis: an effective non-surgical treatment for ruptured intracranial aneurysms?

The outcome of treatment with an antifibrinolytic agent (tranexamic acid) for six weeks after rupture of an intracranial aneurysm was assessed in a randomised controlled trial. Twenty-two out of 25 (88%) treated patients survived at follow-up of three to 33 months compared with 14 out of 25 (56%) control patients. Among the patients who did not undergo operation the survival rate was 81% (13 out of 16) in treated patients and 42% (8 out of 19) in controls. Antifibrinolytic treatment has so far been assumed merely to postpone rebleeding and has been used to enable surgery to be deferred. These findings suggest that tranexamic acid may actually prevent rebleeding without operation. Prolonged antifibrinolysis may therefore prove useful in those patients in good condition whose aneurysms do not lend themselves to surgical obliteration.

Clinical Trials as Topic↗
PubMed1989

Enhancement of the activation of Glu-plasminogen by urokinase in the simultaneous presence of tranexamic acid or fibrin.

The activation rate of Glu-plasminogen (Glu-plg) by urokinase (UK) was enhanced in the presence of either tranexamic acid or fibrin with an increase in the catalytic rate constant (kcat). The maximum increase in kcat was obtained at 0.5 mM of tranexamic acid and 0.1 microM of fibrin. Km did not change. The addition of fibrin to 1 mM tranexamic acid resulted in a further increase in kcat of the UK activation of Glu-plg. On the other hand, the addition of tranexamic acid to 0.1 microM fibrin further increased kcat of the UK activation of Glu-plg. Thus, stimulatory effects were observed on the activation of Glu-plg by UK in the simultaneous presence of tranexamic acid and fibrin. Fibrin-binding sites on the kringle 5 of Glu-plg may be involved in the further increase in the activation rate of Glu-plg by UK in the presence of both fibrin and tranexamic acid in comparison to that in the presence of tranexamic acid alone. Possibly, the Glu-plg binding with both tranexamic acid and fibrin (at kringle 5) may be most effectively activated by UK. It is also suggested that two molecules of Glu-plg bind to one molecule of fibrin monomer.

Cyclohexanecarboxylic Acids↗
PubMed1993

Effects of synthetic trypsin inhibitors on the cell cycle of synchronized HeLa cells.

HeLa cells were synchronized by a double-thymidine block. After removal of thymidine, the cells immediately caused the uptake of [3H]thymidine into DNA and reached a half-maximum. The duration of the cell cycle was 23 h, and definite changes in cell density were observed between 12 and 13 h and between 35 and 36 h after removal of thymidine. Thus, the initiation time of S phase could be fixed. A trypsin-like proteinase appearing at around 17 h 17 min after removal of thymidine and correlated with the onset of the second S phase, tryptase 17:17 [cf., M. Muramatu et al., Biochim. Biophys. Acta, 1087, 87 (1990)], was obtained. 4-tert-Butylphenyl and 4-biphenyl esters of trans-4-guanidinomethylcyclohexanecarboxylic acid (GMCHA) and amidinopiperidine-4-alkanoic acids, trypsin inhibitors, strongly inhibited the tryptase activity, and these esters exert different effects on the cell cycle of HeLa cells at concentrations showing complete inhibition or maximal inhibitory effect on the tryptase. Both esters of GMCHA elongated the onset of the second S phase for 3 h. Esters of amidinopiperidine-4-acetic and 4-propionic acids showed a similar effect at lower concentrations than GMCHA esters. 4-tert-Butylphenyl esters of amidinopiperidine-4-propionic acid and butyric acids strongly suppressed the second S and M phases by probably affecting the G1 late phase, since they have no effect on the first S and M phases. The addition of amidinopiperidine-4-carboxylic acid 4-tert-butylphenyl ester 0 min after removal of thymidine into the cells completely suppressed the first S and M phases.(ABSTRACT TRUNCATED AT 250 WORDS)

Amidines↗