Diuretics furosemide

Therapeutics. Compounds containing the furan or tetrahydrofuran ring are biologically active and are present in a number of pharmaceutical products. Eurfurjdamine [617-89-0] is an intermediate in the diuretic, furosemide. Tetrahydrofurfurylamine [4795-29-3] may also have pharmaceutical applications. 5-(E)imethyiaininomethyi)furfuryi alcohol [15433-79-17 is an intermediate in the preparation of ranitidine, which is used for treating ulcers. 2-Acet5dfuran [1192-62-7] prepared from acetic anhydride and furan is an intermediate in the synthesis of cefuroxime, a penicillin derivative. 2-Euroic acid is prepared by the oxidation of furfural. Both furoic acid [88-14-2] and furoyl chloride [527-69-5] are used as pharmaceutical intermediates. 

Examples of commercial reactive duoroaromatics are not restricted to duoronitroben2enes. The duorine-free diuretic, furosemide [54-31-9], is prepared in 85% yield from 2-duoro-4-chloro-5-sulfamoylben2oic acid and furfurjlamine at 95°C for 2 h (155). 

Diuretic activity can be retained in the face of replacement of one of the sulfonamide groups by a carboxylic acid or amide. Reaction of the dichlorobenzoic acid, 174, with chlorsulfonic acid gives the sulfonyl chloride, 175 this is then converted to the amide (176). Reaction of that compound with furfuryl ine leads to nucleophilic aromatic displacement of the highly activated chlorine at the 2 position. There is thus obtained the very potent diuretic furosemide (177). ... 

The loop diuretics, furosemide (Lasix) and ethacrynic acid (Edecrin), increase the excretion of sodium and chloride by inhibiting reabsorption of these ions in the... 

Consider combining with a thiazide diuretic ° Furosemide continuous IV infusion... 

Loop diuretics (furosemide, bumetanide, torsemide, and ethacrynic acid) are all equally effective when given in equivalent doses. Therefore, selection is based on the side-effect profile, cost, and pharmacokinetics of the agents. The incidence of ototoxicity is significantly higher with ethacrynic acid compared to the other loop diuretics therefore, its use is limited to patients who are allergic to the sulfa component in the other loop diuretics.15 While ototoxicity is a well-established side effect of furosemide, its incidence is greater when administered by the intravenous route at a rate exceeding 4 mg per minute.16 Torsemide has not been reported to cause ototoxicity. 

The answer is c. (Hardman, pp 704-706J Triamterene produces retention of the K ion by inhibiting in the collecting duct the reabsorption of Na, which is accompanied by the excretion of K ions. The loop diuretics furosemide and bumetanide cause as a possible adverse action the development of hypokalemia. In addition, thiazides (e g, hydrochlorothiazide) and the thiazide-related agents (e.g., metolazone) can cause the loss of K ions with the consequences of hypokalemia. Triamterene can be given with a loop diuretic or thiazide to prevent or correct the condition of hypokalemia. 

Foop diuretics (furosemide, bumetanide, torsemide) are usually necessary to restore and maintain euvolemia in HF. In addition to acting in the thick ascending limb of the loop of Henle, they induce a prostaglandin-mediated increase in renal blood flow that contributes to their natriuretic effect. 

Equipotent doses of loop diuretics (furosemide, bumetanide, torsemide, ethacrynic acid) have similar efficacy. Ethacrynic acid is reserved for sulfa-allergic patients. Continuous infusions of loop diuretics appear to be more effective and to have fewer adverse effects than intermittent boluses. An initial IV loading dose (equivalent to furosemide 40 to 80 mg) should be administered before starting a continuous infusion (equivalent to furosemide 10 to 20 mg/hour). 

Patients with SIADH should be treated with 3% saline plus, if the urine osmolality exceeds 300 mOsm/kg, a loop diuretic (furosemide, 40 mg IV every 6 hours). 

Patients with sodium overload should be treated with loop diuretics (furosemide, 20 to 40 mg IV every 6 hours) and 5% dextrose at a rate that decreases serum sodium by approximately 0.5 mEq/L/hour or, if hypernatremia developed rapidly, 1 mEq/L/hour. 

Gastric lavage is contraindicated because of the serious danger of aspiration and the relatively benign gastrointestinal effects. Patients with respiratory difficulties require oxygen and sometimes mechanical ventilation. Pulmonary oedema, if it occurs, should be treated with diuretics (furosemide 25-100 mg intravenously) or by mechanical ventilation. Antibiotic treatment is unnecessary unless bacterial pneumonia, a rare sequel to kerosene pneumonitis, develops. Mortality is less than 1%. 

Thiazide diuretics are not the drugs of choice in patients with renal insufficiency. In this situation, the loop diuretics furosemide and bumetanide are recommended they have greater intrinsic natriuretic potency than do the thiazides and do not depress renal blood flow. 

Sulfasalazine is contraindicated in individuals with hypersensitivity to salicylates, sulfonamides, sulfonylureas, and certain diuretics (furosemide, thiazides, and carbonic anhydrase inhibitors). Because it can cause kernicterus, sulfasalazine is contraindicated in infants and children under 2 years of age. Sulfasalazine passes into breast milk and is therefore contraindicated for nursing mothers. Similarly, pregnant women near term should not use this drug, although it appears to be the safest of the DMARDs during early pregnancy. 

Offers potential advantages over other loop diuretics, including a longer duration of action and fewer adverse electrolyte and metabolic effects available data not extensive or convincing enough at present to recommend replacement of standard loop diuretic (furosemide) considered alternative in refractory patients... 

Loop diuretics Furosemide Block Na/K/2CI transporter in renal loop of Henle Like thiazides t greater efficacy Severe hypertension, heart failure See Chapter 15... 

Depomed initiates phase II trial with once daily diuretic Furosemide GR. Business Wire Press Release, 2004. 

When ( )-A-formyl-4-fluorotryptophan methyl ester is irradiated in methanol, replacement of fluorine by methoxy takes place387. Because of the strength of the C—F bond, homolysis cannot occur under photolytic conditions. Heterolysis, however, may occur in a polar medium and the aryl cation is probably stabilized by resonance involving the lone electron pair on the indole nitrogen atom. The chlorine atom in the diuretic furosemide is... 

Ototoxicity Ototoxicity (vestibular and cochlear) is directly related to high peak plasma levels and duration of treatment. Deafness may be irreversible and has been known to affect fetuses in utero. Patients simultaneously receiving another ototoxic drug such as the loop diuretics furosemide, bumetanide, ethacrynic acid (see p. 227) or cisplatin (see p. 396), are particulary at risk. Vertigo and loss of balance may also occur because these drugs affect the vestibular apparatus. 

Figure 2.5 In addition to its antibacterial activity, sulfanilamide 11 (Figure 2.4) inhibits the enzyme carbonic anhydrase. Acetazolamide 12 is much more potent as a carbonic anhydrase inhibitor but its clinical use as diuretic was impaired by some serious side effects. Hydrochlorothiazide 13 is the prototype of orally active saluretic sulfonamide diuretics. Furosemide (frusemide) 14 and bumetanide 15 are so-called loop diuretics .

Q8 The thiazide diuretics reduce urinary excretion of calcium and can also be used to decrease the likelihood of calcium-based renal stones. On the other hand, the loop diuretic furosemide reduces reabsorption of calcium and increases calcium excretion. 

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