[The clinical use of tranexamic acid in acute inflammation of the upper respiratory tract].
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Adolescent↗
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Convulsant and anticonvulsant actions in DBA/2 mice of compounds blocking the reuptake of GABA.
Compounds blocking the uptake of GABA into neurons or glia have been injected intracerebroventricularly (icv) or intraperitoneally (ip) in DBA/2 mice, age 21-28 days. Protection against audiogenic seizures was seen 30 min after the icv injection of (+)-2,4-diaminobutyric acid (0.5-2.0 mumoles), (+/-)-nipecotic acid (1.6-3.2 mumoles), (+)-ethyl nipecotate (0.4-0.8 mumoles), (-)-piperazic acid (4 mumoles) and putrescine (2 mumoles) or the ip injection of (+)-2,4-diaminobutyric acid (4-8 mmoles/kg and (+)-ethyl nipecotate (0.24-0.32 mmoles/kg). Of these ethyl nipecotate and nipecotic acid were the most effective anticonvulsants icv, but nipecotic acid was ineffective ip. Limb myoclonus and other epileptic manifestations (rearing, wild running, tonic clonic seizures) occurred in the absence of auditory stimulation after (+)-2,4-diaminobutyric acid (0.5-2.0 mumoles), (+/-)-cis-3-aminocyclohexane carboxylic acid (3.2-6.4 mumoles) and putrescine (2 mumoles). beta-Alanine (2-4 mumoles, icv) depressed respiration but did not protect against audiogenic seizures or induce myoclonus.
Alanine↗
Antifibrinolytic treatment in subarachnoid hemorrhage.
We enrolled 479 patients with subarachnoid hemorrhage in a multicenter, randomized, double-blind, placebo-controlled trial to determine whether treatment with the antifibrinolytic agent tranexamic acid improves outcome by preventing rebleeding. At three months there was no statistical difference between the outcomes in the tranexamic acid group and the control group. Of the 173 patients who died, 84 had received tranexamic acid and 89 placebo (95 per cent confidence interval for the difference in mortality rate, -6 to 11 per cent). Similarly, when analysis was restricted to patients with an angiographically demonstrated aneurysm, there was no significant difference between the groups. This absence of effect was not due to a lack of antifibrinolytic action, since the rate of rebleeding was reduced from 24 per cent in the control group to 9 per cent in the tranexamic acid-treated group (chi-square = 18.07, P less than 0.001), but resulted from a concurrent increase in the incidence of ischemic complications (15 per cent in the control group and 24 per cent in the tranexamic acid group; chi-square = 8.07, P less than 0.01). We conclude that until some method can be found to minimize ischemic complications, tranexamic acid is of no benefit in patients with subarachnoid hemorrhage.
Cerebral Angiography↗
The effect of tranexamic acid on secondary haemorrhage after traumatic hyphaema.
During the period from March 1978 to November 1979, 232 consecutive patients with traumatic hyphaema were allocated by admission-date to conservative treatment and to treatment with the antifibrinolytic drug tranexamic acid. Secondary haemorrhage occurred in only two of 102 tranexamic acid treated patients, while secondary haemorrhage occurred in 12 out of 130 conservatively treated patients. This difference was statistically significant. Some clinical aspects of the rebleeding cases are presented and briefly discussed.
Adolescent↗
[Effect of naphthenic acids on the permeability of ascitic tumor cells to potassium ions].
Ascite cells were treated with naphthenic acid preparation, containing a mixture of naphthenic acids with average molecular weight equal to 240, and with a fraction of this preparation differing in the boiling temperature. A 5-10(-7)M and higher concentrations of the preparation and its fraction brought about an increased permeability in ascite cells for K-ions. The effectiveness of naphthenic acids is associated with their hydrophobic properties, which was characterized in the present communication by the value of hydrophilic-lipophilic balance calculated according to the Davies formula.
Animals↗
Establishment of a human ovarian cancer cell line capable of forming ascites in nude mice and effects of tranexamic acid on cell proliferation and ascites formation.
The present study was designed to obtain an experimental tumor model as similar as possible to human ovarian cancer which often had a large amount of ascites and to assess the therapeutic value of tranexamic acid. Human tumor cell lines which form ascites in nude mice were established from ascites of patient with serous cystadenocarcinoma of the ovary. Two cloned cell lines designated HRA and HR-1 were obtained from the parent cell line designated HR. All of these cultured cell lines had about 2.5-3.5 times higher lactate dehydrogenase activities than the original tumor. The original tumor and the tumor grown in nude mice had all 5 bands of lactate dehydrogenase isoenzymes, while all cultured cell lines had only a marked lactate dehydrogenase-3 in addition to a faint lactate dehydrogenase-2. Modal chromosome numbers of HR cells ranged from 50-76, while that of HRA cells ranged widely from 40-140. The DNA histograms of HR and HRA cells were similar to each other, showing predominant G1 and S phases. Although these cell lines had ability to produce ascites in the nude mice when the cells were inoculated i.p., the HRA cell inoculation made ascites most rapidly and brought about the shortest median survival (39 days). The proliferations of all three cell lines were dose-dependently inhibited by tranexamic acid. However, the concentration of this drug required for 50% inhibition of the proliferation of HRA cells was about one-half of that of HR and HR-1 cells. In addition, i.p. injections of tranexamic acid to nude mice treated with cisplatin resulted in a significant inhibition of the ascites formation and prolongation of 50% survival.
Animals↗
[The effect of gabapentin and gabapentin-lactam on retinal ganglion cell survival. Situation after acute retinal ischemia in animal models].
BACKGROUND: Reduction in the excitatory and potentially toxic neurotransmitter glutamate can protect retinal ganglion cells. What are the effects of the antiepileptic drug gabapentin, for which antiglutamatergic effects have been described, and the new substance gabapentin-lactam (GBP-L) on retinal ganglion cell survival after retinal ischemia? METHODS: In 3 groups of 10 rats each, ischemia was induced by elevating the intraocular pressure of the left eye to 120 mmHg for 1 h. Saline, gabapentin (2 x 50 mg/kg intraperitoneally) and GBP-L (2 x 50 mg/kg intraperitoneally) were injected before and 5 h after ischemia. Two weeks later ischemic damage was quantified histologically by counting the number of neurons in the ganglion cell layer. In vitro transmitter release experiments were performed to obtain information on the effect of gabapentin and GBP-L on ischemia-induced glutamate release and the mechanism of action of GBP-L. RESULTS: In the control group 17% of the retinal ganglion cells survived ischemia. GBP-L doubled the number of the surviving cells while gabapentin was not effective in these experiments. In vitro gabapentin and GBP-L reduced ischemia-induced glutamate release by 35.7% and 42.5%, respectively. The blockade of ATP-sensitive potassium channels antagonized the effect of GBP-L completely. CONCLUSION: GBP-L is neuroprotective in retinal ischemia and diminishes the release of the excitatory neurotoxic amino acid glutamate. The effect of GBP-L might be mediated by ATP-sensitive potassium channels. Also gabapentin reduced glutamate release but was not neuroprotective in vivo.
Acetates↗
Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex.
Gabapentin and pregabalin (S-(+)-3-isobutylgaba) produced concentration-dependent inhibitions of the K(+)-induced [Ca(2+)](i) increase in fura-2-loaded human neocortical synaptosomes (IC(50)=17 microM for both compounds; respective maximal inhibitions of 37 and 35%). The weaker enantiomer of pregabalin, R-(-)-3-isobutylgaba, was inactive. These findings were consistent with the potency of these drugs to inhibit [(3)H]-gabapentin binding to human neocortical membranes. The inhibitory effect of gabapentin on the K(+)-induced [Ca(2+)](i) increase was prevented by the P/Q-type voltage-gated Ca(2+) channel blocker omega-agatoxin IVA. The alpha 2 delta-1, alpha 2 delta-2, and alpha 2 delta-3 subunits of voltage-gated Ca(2+) channels, presumed sites of gabapentin and pregabalin action, were detected with immunoblots of human neocortical synaptosomes. The K(+)-evoked release of [(3)H]-noradrenaline from human neocortical slices was inhibited by gabapentin (maximal inhibition of 31%); this effect was prevented by the AMPA receptor antagonist NBQX (2,3-dioxo-6-nitro-1,2,3,4-tetrahydro[f]quinoxaline-7-sulphonamide). Gabapentin and pregabalin may bind to the Ca(2+) channel alpha 2 delta subunit to selectively attenuate depolarization-induced Ca(2+) influx of presynaptic P/Q-type Ca(2+) channels; this results in decreased glutamate/aspartate release from excitatory amino acid nerve terminals leading to a reduced activation of AMPA heteroreceptors on noradrenergic nerve terminals.
Acetates↗
A novel method for purification of prephenic acid.
Prephenic acid accumulated in culture filtrates of Neuro-spora crassa has been purified in 66% yield utilizing adsorption chromatography on Sephadex G-10 in the major purification steps.
Barium↗
Influence of tranexamic acid and acetylsalicylic acid on the thickness of the normal cornea.
In a masked cross-over study ten normal subjects were treated with tranexamic acid and acetylsalicylic acid one g three times daily for seven days. The central corneal thickness. was found to increase in response to acetylsalicylic acid and to decrease in response to tranexamic acid. This finding provides evidence for the involvement of the fibrinolytic system in the regulation of the normal corneal thickness. The endothelial morphology, as seen with the specular microscope, was unchanged during treatment with either drug.
Adult↗
Tranexamic acid in the prevention of secondary haemorrhage after traumatic hyphaema.
The occurrence of secondary haemorrhage after traumatic hyphaema was studied in 239 patients treated in the Department of Ophthalmology, Tampere Central Hospital during the years 1972 to 1980. From 1972 to 1976, 126 patients with traumatic hyphaema were confined to bed and treated without antifibrinolytic agents; nine (7.1%) of these patients developed secondary haemorrhage. From 1977 to 1980, none of 58 patients with traumatic hyphema treated with tranexamic acid developed secondary haemorrhage which was seen in 3 (5.5%) of 55 patients treated without antifibrinolytic agents; the activities of these patients were not restricted and the eyes were not patched. The resorption of the hyphaema was significantly delayed in the tranexamic acid treated patients. It is concluded that tranexamic acid delays resorption of the blood-clot sealing the damaged vessel and preventing secondary haemorrhage after traumatic hyphaema without bed-rest and binocular patching.
Adolescent↗
[The effect of trisporic acids on the composition of components of the cell wall in Blakeslea trispora Thaxter].
The cell wall of Blakeslea trispora was found to contain chitin similar to crustaceaous chitin in physico-chemical properties; this was confirmed by the data of IR spectroscopy and X-ray diffraction analysis. Trisporic acids, hormonal regulators of reproduction, hardly affected the content of chitin, xylan, and other polysaccharides of the cell wall of Blakeslea trispora, but increased the content of protein.
Cell Wall↗
The effect of tranexamic acid on growth and spread of an experimental tumor model.
In the spontaneously metastasizing murine P815 mastocytoma studied, exposure of the cell cultures to Tranexamic acid increased plasminogen activator activity (PAA) in the cytosol and in the primary solid tumors. These increased PAA levels were associated with an increased rate of metastasis to the liver.
Animals↗
Simultaneous high-performance liquid chromatographic analysis of pregabalin, gabapentin and vigabatrin in human serum by precolumn derivatization with o-phtaldialdehyde and fluorescence detection.
A rapid, simple and robust method is presented for the simultaneous determination of the gamma-amino-n-butyric acid (GABA) derivatives pregabalin (PGB), gabapentin (GBP) and vigabatrin (VGB) in human serum by high-performance liquid chromatography (HPLC). Serum is deproteinized with trichloroacetic acid and aliquots of the supernatant are precolumn derivatized with o-phtaldialdehyde (OPA) and 3-mercaptopropionic acid. Separation is achieved on a Alltima 3C18 column using isocratic elution; the drugs are monitored using fluorescence detection. Norvaline is used as an internal standard. Within-day precision (COV; n = 10) is 1.2% for PGB (serum concentration 10.0 mg/l), 1.1% for GBP (serum concentration 15.8 mg/l) and 0.3% for VGB (serum concentration 15.5 mg/l). The method is linear up to at least 63 mg/l for PGB, 40 mg/l for GBP and 62 mg/l for VGB. Lower limits of quantitation (LOQ) are 0.13 mg/l for PGB, 0.53 mg/l for GBP and 0.06 mg/l for VGB. No interferences were found from commonly coadministered antiepileptic drugs (AEDs) and from endogenous amino acids. Experimental design in combination with statistical evaluation (ANOVA) was used to study the robustness of chromatography and sample preparation. The method is very suitable for routine therapeutic drug monitoring and for pharmacokinetic studies.
Amines↗
Allergic contact sensitization to the glycidyl ester of hexahydrophthalic acid in a cutting oil.
Allergic contact dermatitis is reported in 5 machine operatives working with a cutting oil containing an epoxy compound used as a stabilizer. Positive patch test reactions to this compound were obtained in all 5 men and were negative in 25 controls.
Adult↗
Preferential action of gabapentin and pregabalin at P/Q-type voltage-sensitive calcium channels: inhibition of K+-evoked [3H]-norepinephrine release from rat neocortical slices.
Gabapentin (GBP; Neurontin) and pregabalin (PGB; CI-1008), efficacious drugs in several neurological and psychiatric disorders, inhibit neurotransmitter release from mammalian brain slices at therapeutically relevant concentrations. A detailed investigation, exploring the basis for this in vitro phenomenon, focused on norepinephrine (NE) and rat neocortical tissue in complementary assays of neurotransmitter release and radioligand binding. The results are consistent with the hypothesis that GBP, PGB, and related substances decrease neocortical NE release by acting at the alpha2delta subunit of presynaptic P/Q-type voltage-sensitive Ca2+ channels (VSCC) subserving Ca2+ influx in noradrenergic terminals. The inhibitory action appears competitive with [Ca2+]o and preferential to those neurons undergoing prolonged depolarization. Other results indicate that the reduction of exocytotic NE release is independent of L- and N-type VSCC, classical drug/peptide binding sites on VSCC, Na+ channels, alpha2-adrenoceptors, NE transporter, and system L amino acid transporter. These findings suggest a selective modulation of P/Q-type VSCC that are implicated in neurotransmission and several GBP-responsive pathologies.
Acetates↗
Effect of tranexamic acid on the fibrinolytic activity of human uterine fluid.
The normally occurring fibrinolytic activity of uterine fluid was used to evaluate the possibility of influencing fibrinolytic enzymes liberated in the uterine cavity in humans. Oral and intravenous administration of a synthetic fibrinolytic inhibitor, tranexamic acid, was found to significantly suppress the fibrinolytic activity of uterine fluid during the luteal phase. The significance of this observation is discussed in relation to the possible participation of fibrinolytic enzymes during the implantation process in humans as in some other species.
Body Fluids↗
Effect of tranexamic acid on choroidal melanoma.
Four cases of malignant choroidal melanoma have been treated with the antifibrinolytic agent tranexamic acid (Cyklocapron). One patient treated for six months showed no progression in tumor growth. Three eyes have been enucleated, and the histological examination revealed that the tumours were surrounded by fibrin. No side-effects of the treatment were observed.
Adult↗