Category: benzothiophene

Prandota, J published the artcileEffect of tienilic acid (Diflurex) on the binding of warfarin 14C to human plasma proteins., Product Details of C13H8Cl2O4S, the main research area is .

Tienilic acid (Diflurex), a new diuretic with a chemical structure close to that of ethacrynic acid, displaces significant amounts of warfarin from 2 g/l human albumin in vitro by a competitive mechanism. When physiologic concentrations of human albumin are used, or with human plasma there is no such interaction. Because excessive hypoprothrombinaemia and haemorrhage were reported in vivo when tienilic acid was added to oral coumarin anticoagulant therapy, it is advised to use another diuretic if necessary.

International journal of clinical pharmacology, therapy, and toxicology published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Product Details of C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Ambrosioni, E published the artcileEffects of tienilic acid used alone and in association with triamterene or amiloride on urinary excretion of electrolytes., Quality Control of 40180-04-9, the main research area is .

The K-sparing effects of amiloride (A) and triamterene (T) associated with tienilic acid (C) are studied, along with their effects on diuresis and on the urinary excretion of uric acid, Mg, Na, Cl, P, and Ca. Eighteen hospitalized patients, divided into two groups of nine, received the following dosages of the drugs. The first group took 250 mg of C (equivalent to 50 mg hydrochlorothiazide), 5 mg of A and 100 mg of T; the second received double doses of both A and T but the same dose of C. Each treatment was administered on 2 not necessarily consecutive days, so as to have a total of 6 days of treatment per patient according to a balanced randomized design identical for the two groups. The data were obtained from urine collected during the first 8 h after the drug was administered, and during the following 16 h. A and T showed a significant K-sparing effect (p less than 0.01) only for the second group, and only at the higher dosages were minor effects on the urinary excretion of uric acid, Mg, and Cl noted (p less than 0.05). The association of A or T with C was well tolerated, and no important side effects were observed.

International journal of clinical pharmacology, therapy, and toxicology published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Quality Control of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Rosendorff, C published the artcileThe treatment of mild to moderate essential hypertension with tienilic acid (ticrynafen)., Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

This paper reports a clinical trial of tienilic acid, a new diuretic with uricosuric properties, in 23 patients with mild to moderate hypertension (standing diastolic blood pressure 90-120 mmHg). Tienilic acid was compared with hydrochlorothiazide in a variable-dose, double-blind cross-over study, and the duration of therapy was 8 weeks for each drug. The falls in blood pressure (systolic/diastolic) were: 11/11 mmHg supine and 17/11 mmHg standing for tienilic acid, and 8/12 mmHg supine and 9/17 mmHg standing for hydrochlorothiazide. There were no significant differences between the two drugs in their effect on blood pressure and heart rate, and regarding side-effects and laboratory results, except for serum uric levels (mean fall of 1,5 mg/dl with tienilic acid and mean increase of 1.1 mg/l with ydrochlorothiazide).

South African medical journal = Suid-Afrikaanse tydskrif vir geneeskunde published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Riegelman, R K published the artcileWhat to do until the FDA arrives., Application In Synthesis of 40180-04-9, the main research area is .

The need for clinical monitoring to assure drug safety despite reliance on Food and Drug Administration testing is illustrated. The need to temper theory with clinical experience is exemplified by the recent examples of swine flu, resistant gonorrhea, and resistant pneumococcal infection. The potential for adverse effects to escape detection in animal studies and small-scale human trials is illustrated by the examples of ticrynafen, chloramphenicol, and diethylstilbestrol. The potential for unexpected side effects when established drugs are used in new ways is demonstrated by the examples of retrolental fibroplasia and vitamin D toxicity. The responsibilities of the medical profession and the individual practitioner include a healthy skepticism of newly introduced treatments, active participation in clinical monitoring, and maintenance of a system for chart retrieval when drugs are recalled or new effects reported.

Postgraduate medicine published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Application In Synthesis of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Weidmann, P published the artcileDiuretic treatment and serum lipoproteins: effects of tienilic acid and indapamide., Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

Treatment with the commonly used diuretic, chlorthalidone, has previously been found to increase the serum low-density-lipoprotein cholesterol (LDL-C) fraction. Therefore, the effects of two new agents, tienilic acid (a combined diuretic-uricosuric) and indapamide on serum lipid and lipoprotein levels were assessed. Six weeks of treatment with tienilic acid, 250 mg/day, markedly decreased serum uric acid and significantly increased LDL-C and triglycerides in 16 men. In contrast, indapamide 2.5 mg/day, had no apparent influence on serum lipids or lipoproteins in 18 men.

Klinische Wochenschrift published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Liu, Zhang-Xu published the artcileImmune-mediated drug-induced liver disease., Product Details of C13H8Cl2O4S, the main research area is .

Drug-induced immune-mediated hepatic injury is an adverse immune response against the liver that results in a disease with hepatitic, cholestatic, or mixed clinical features. Drugs such as halothane, tienilic acid, dihydralazine, and anticonvulsants trigger a hepatitic reaction, and drugs such as chlorpromazine, erythromycins, amoxicillin-calvulanic acid, sulfonamides and sulindac trigger a cholestatic or mixed reaction. Unstable metabolites derived from the metabolism of the drug may bind to cellular proteins or macromolecules, leading to a direct toxic effect on hepatocytes. Protein adducts formed in the metabolism of the drug may be recognized by the immune system as neoantigens. Immunocyte activation may then generate autoantibodies and cell-mediated immune responses, which in turn damage the hepatocytes. Cytochromes 450 are the major oxidative catalysts in drug metabolism, and they can form a neoantigen by covalently binding with the drug metabolite that they produce. Autoantibodies that develop are selectively directed against the particular cytochrome isoenzyme that metabolized the parent drug. The hapten hypothesis proposes that the drug metabolite can act as a hapten and can modify the self of the individual by covalently binding to proteins. The danger hypothesis proposes that the immune system only responds to a foreign antigen if the antigen is associated with a danger signal, such as cell stress or cell death. Most clinically overt adverse hepatic events associated with drugs are unpredictable, and they have intermediate (1 to 8 weeks) or long latency (up to 12 months) periods characteristic of hypersensitivity reactions. Immune-mediated drug-induced liver disease nearly always disappears or becomes quiescent when the drug is removed. Methyldopa, minocycline, and nitrofurantoin can produce a chronic hepatitis resembling AIH if the drug is continued.

Clinics in liver disease published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Product Details of C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Zimmerman, H J published the artcileEffects of ticrynafen on hepatic excretory function in the isolated perfused rat liver., Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

Ticrynafen, a uricosuric diuretic agent which causes hepatocellular injury in man as an apparent idiosyncratic reaction, was found to impair the function of the isolated perfused rat liver. At concentrations in the perfusate equivalent to those produced in the blood of man by therapeutic doses, the drug led to a striking reduction in bile flow and sulfobromophthalein excretion and release of aspartate aminotransferase into the perfusate. These adverse effects were enhanced by treatment of rats with phenobarbital prior to removal of the liver, indicating that the adverse effect of ticrynafen is probably caused by a metabolite produced in the cytochrome P-450 system.

Hepatology (Baltimore, Md.) published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Homberg, J C published the artcileDrug-induced hepatitis associated with anticytoplasmic organelle autoantibodies., Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

A study from five hepatology units documenting 157 cases of drug-induced hepatitis and a second study from a laboratory of immunology which tested more than 100,000 sera permitted us to establish the frequency of antiorganelle antibodies and their diagnostic value in drug-induced hepatitis. In drug-induced hepatitis caused by a heterogenous group of drugs consisting of ajmaline, aminopterine, isaxonine, isoniazid, perhexiline, phenylbutazone and troleandromycine, antiorganelle antibodies were absent or rare. In drug-induced hepatitis caused by another heterogenous group of drugs, including clometacin, fenofibrate, oxyphenisatin and papaverine, antismooth muscle, antinucleus and antimitochondria antibodies were found in isolation or in different combinations in 70% of cases. From the presence of antismooth muscle antibodies in sera, we could trace 30 cases of clometacin-induced hepatitis. The third group included drug-induced hepatitis with special antibody:iproniazid-induced hepatitis with antimitochondrial antibody 6 and tienilic acid (ticrynafen)-induced hepatitis with antiliver/kidney microsome antibody 2 (anti-LKM2). These two antibodies are rare in routine sera and were absent in patients who received the drug and had no liver damage. From the presence of corresponding antibodies, we detected six cases of iproniazid-induced hepatitis and 67 cases of tienilic acid-induced hepatitis. Antiorganelle antibodies found in high titers disappeared in 2 to 24 months following withdrawal of the offending drug. The fourth group was represented by halothane-induced hepatitis; antiliver/kidney microsome antibody 1 was weak and infrequent. Similarities between drug-induced hepatitis of the second group and lupoïd hepatitis suggest that drugs may reveal this spontaneous disorder.(ABSTRACT TRUNCATED AT 250 WORDS)

Hepatology (Baltimore, Md.) published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Zimmerman, H J published the artcileTicrynafen-associated hepatic injury: analysis of 340 cases., Related Products of benzothiophene, the main research area is .

Ticrynafen, a uricosuric diuretic, was withdrawn from clinical use in the United States in 1980 after having been implicated as the cause of a number of instances of serious hepatic injury. In this report, we analyze 340 cases of ticrynafen-associated hepatic disease reported to the manufacturer from the time of initial marketing until shortly after the drug had been recalled. Jaundice was recorded in 246 of 287 patients with sufficient clinical information, and 25 (10.2%) of these icteric patients died. The high levels of serum aminotransferase and the case fatality rate are consistent with the hepatocellular injury that was evident in all of the histologic material. In three-fourths of the cases available to us for histologic study, the lesion was that of acute hepatocellular injury. In the remaining cases there was evidence of chronic active hepatitis and/or cirrhosis. Comparison of demographic characteristics of the total population exposed to ticrynafen with the subset developing hepatic injury suggests a proportionately higher risk of injury for females over the age of 60 years. The variable and unusually prolonged latent period and lack of reported eosinophilia or rash generally suggest a mechanism other than hypersensitivity. However, the recurrence of hepatic injury in 15 of the 16 patients challenged with the drug and the prominence of eosinophils in hepatic tissue in some of the cases suggests that hypersensitivity may also play a pathogenetic role. Accordingly, there is reason to incriminate both metabolic idiosyncrasy and hypersensitivity in the mechanism of injury.

Hepatology (Baltimore, Md.) published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Related Products of benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Noble, R E published the artcileLong-term usage of tienilic acid in essential hypertension., HPLC of Formula: 40180-04-9, the main research area is .

The purpose of this double-blind study was to compare the effects on blood pressure of tienilic acid and hydrochlorothiazide in patients with essential hypertension. The biochemical effects of tienilic acid in relation to those of hydrochlorothiazide were also determined over a long-term period of therapy. Sixty-six outpatients with mild to moderate essential hypertension were treated for seven months with either 250 mg of tienilic acid or 50 mg of hydrochlorothiazide after a 3 week placebo period. When warranted, dosage was increased to a maximum of 500 mg of tienilic acid and 100 mg of hydrochlorothiazide daily. Results indicate that tienilic acid reduced blood pressure significantly and to the same extent as hydrochlorothiazide. No significant side effects were observed. The effects on potassium, blood urea nitrogen and creatinine were comparable in both groups. However, serum uric acid rose with hydrochlorothiazide but fell with tienilic acid. In view of this effect, tienilic acid may have certain advantages over thiazide therapy in the treatment of hypertension.

Postgraduate medical journal published new progress in MEDLINE about 40180-04-9, 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, HPLC of Formula: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem