Diuretics chlorothiazide

Electroneutral NaCl transport in the distal convoluted tubule is inhibited by the class of thiazide diuretics (chlorothiazide, hydrochlorothiazide, metolazone, chlorthalidone, and others). Thiazides interfere with the Cl binding site of NCC, and cause a relatively small... 

May have synergistic activity with a loop diuretic ° Chlorothiazide... 

Changing the substitution pattern on the carbo-cyclic ring of the benzothiadiazine diuretics is well known to have a marked effect on the qualitative biological activity. Thus, the direct analogue of the diuretic chlorothiazide (199) in which chlorine replaces one sulfonamide group, diazoxide (200), shows negligible diuretic activity instead the compound is a potent antihypertensive vasodilator. 

The need to characterise and define light sources in photodegradation studies was outlined by investigators from the FDA [73]. They reported on UV-A-induced photolytic decomposition products of the anti-diuretics, chlorothiazide and hydrochlorothiazide. Both drugs are reported to be potent photosensitisers however, their photodegradation had previously been reported only under very specific conditions [74,75]. 

Diuretics are therapeutic agents used in certain pathological conditions to eliminate bodily fluids. Furosemide and the thiazide diuretics, chlorothiazide, hydrochlorothiazide, and trichlormethiazide are approved for use in dairy cattle for treatment of postparturient edema of the mammary gland and associated structures. The potential misuse of these diuretic drugs in cattle could lead to unacceptable residues in meat or milk destined for human consumption. Therefore, analytical methods sufficiently sensitive to monitor residue concentration levels in foods are valuable in preventing unapproved use of diuretics. 

The nurse is discussing the thiazide diuretic chlorothiazide (Diuril) with the client diagnosed with essential hypertension. Which discharge instruction should the nurse discuss with the client ... 

TABLE 25.1 Some Older Drues lOver 50 Diuretic Chlorothiazide 1958... 

In a study with 3427 male and female patients having DBP of 95—109 mm Hg (12—15 Pa), and no clinical evidence of cardiovascular diseases, half of the patients were placebo-treated and half were SC antihypertensive dmg-treated, ie, step 1, chlorothiazide step 2, methyldopa, propranolol [525-66-6], or pindolol [13523-86-9], and step 3, hydralazine, or clonidine [4205-90-7] (86). Overall, when the DBP was reduced below 100 mm Hg (13 Pa), there were more deaths in the dmg-treated group than in the placebo group. The data suggest reduction of blood pressure by antihypertensive dmg treatment that includes a diuretic is accompanied by increased cardiovascular risks. 

Thiazide diuretics such as chlorothiazide act on the distal tubule, a portion of the tubule that is permeable to sodium. The mechanism of action of these diuretics involves inhibition of NaCl reabsorption by blocking the Na+, CL symporter in the luminal membrane. The thiazide diuretics are only moderately effective due to the location of their site of action. Approximately 90% of the filtered Na+ ions have already been reabsorbed when the filtrate reaches the distal tubule. These drugs may be used for treatment of edema associated with heart, liver, and renal disease. Thiazide diuretics are also widely used for the treatment of hypertension. 

A few important drugs, namely thiazide diuretics (e.g., chlorothiazide, hydroflumethiazide, bendroflumethiazide, benzthiazide, cyclothiazide etc.), neomycin, tetracyclines, methyldopa etc., help in enhancing the BUN levels perhaps due to interference with normal renal function,... 

Diazoxide (II) has been known since the early 1960 s (9.) and must be considered as a well known lead. It bears a structural resemblance to the diuretic agent, chlorothiazide (XIX) but, unlike chlorothiazide, it is non-diuretic. Analogs have been prepared by scientists at Schering (10) and by a group in Italy (11). The Italian group reported that compound XX lowers blood pressure and heart rate intravenously in rats but causes... 

Chlorothiazide Chlorothiazide, 1,1-dioxide 6-chloro-2//-l,2,4-benzothiadiazin-7-sulfon-amide (21.3.3) is synthesized in the exact same manner, is aU thiazide diuretics. 3-Chloroanihne (or 3-trifluoromethylaniline) undergoes sulfoylchlorination by chlorosulfonic acid, forming 4,6-sntfonochloride-3-chloroanihne (21.3.1), the reaction of which with ammonia gives 4,6-sutfonylamido-3-chloroaniline (21.3.2). Heating this with formamide leads to formation of chlorothiazide (21.3.3) [9-11]. 

The diuretic action of chlorothiazide, like other drugs of this series, is caused by reduced absorption of sodium and chloride ions by the kidneys during their simultaneous, intense excretion from the organism. 

When diuretic therapy is indicated for the treatment of primary hypertension, the thiazide-type compounds (e.g., chlorothiazide, hydrochlorothiazide) are generally the drugs of choice. They can be used alone or in combination with other antihypertensive agents Approximately 30% of patients with mild hypertension may be treated effectively with thiazide therapy alone. 

Thiazide diuretics consist of two distinct groups those containing a benzothiadiazine ring, such as hydrochlorothiazide and chlorothiazide, referred to as thiazide diuretics, and those that lack this heterocyclic structure but contain an unsubstituted sulfonamide group. The latter are called thiazidelike diuretics they include metolazone, xipamide, and indapamide. The major thiazide and thiazidelike drugs available in the United States are bendrofiumethiazide, benzthiazide, chlorothiazide, hydrochlorothiazide, hydroflumethiazide, methyclothiazide, polythiazide, and trichlormethiazide and chlorthalidone, indapamide, metolazone, and quinethazone, respectively. 

Furosemide (Lasix), torsemide (Demadex), and bumetanide (Bumex) possess some carbonic anhydrase inhibiting activity (about one-tenth that of chlorothiazide). This property may account for the increased bicarbonate and phosphate excretion seen after large doses of these diuretics. The elevated HCOj" loss probably indicates some proximal tubular effects for furosemide and bumetanide. 

The development of sulfonamide carbonic anhydrase inhibitors was based on the observation that antibacterial sulfanilamides produce alkaline urine. This discovery led to the development of acetazolamide (8.29), a thiadiazole derivative. It is not an ideal drug because it promotes K+ excretion and causes a very high urine pH. Since chloride ions are not excreted simultaneously, systemic acidosis also results. Much more useful are the chlorothiazide (8.30) derivatives, which are widely used as oral diuretic drugs. These compounds differ from one another mainly in the nature of the substituent on C3 ... 

Abnormalities in fluid volume and electrolyte composition are common and important clinical disorders. Drugs that block specific transport functions of the renal tubules are valuable clinical tools in the treatment of these disorders. Although various agents that increase urine volume (diuretics) have been described since antiquity, it was not until 1957 that a practical and powerful diuretic agent (chlorothiazide) became available for widespread use. 

All thiazides can be administered orally, but there are differences in their metabolism. Chlorothiazide, the parent of the group, is not very lipid-soluble and must be given in relatively large doses. It is the only thiazide available for parenteral administration. Chlorthalidone is slowly absorbed and has a longer duration of action. Although indapamide is excreted primarily by the biliary system, enough of the active form is cleared by the kidney to exert its diuretic effect in the DCT. 

Chlorothiazide Synthetic Diuretic C7H6CIN3O4S2 296 225, 280 8-10 H2O, EtOH, MeOH Hexane,... 

---