Kenzamide Mechanism of Action

Pharmacology: Injection: Action: Furosemide (Kenzamide) is a potent diuretic with a rapid action. It inhibits the reabsorption of electrolytes in the ascending limb of the loop of Henle and also in the distal renal tubules. It may also have a direct effect in the proximal tubules. Excretion of sodium, potassium and chloride ions is increased and water excretion enhanced. It has no clinically significant effect on carbonic anhydrase. Used similarly to chlorothiazide and may be effective in patients unresponsive to thiazide diuretic. It is also used in the treatment of renal insufficiency unlike the thiazide diuretics were owing to their flat dose-response curve, very little is gained by increasing the dose, Furosemide (Kenzamide) has a steep dose-response curve, which gives it a wide therapeutic range.
Pharmacokinetics: Tablet: Furosemide is fairly rapidly absorbed from the gastrointestinal tract; bioavailability has been reported to be about 60 to 70% but absorption is variable and erratic. The half-life of Furosemide is up to about 2 hours although it is prolonged in neonates and in patients with renal and hepatic insufficiency. It is up to 99% bound to plasma albumin, and is mainly excreted in the urine, largely unchanged. There is also some excretion via the bile and non-renal elimination is considerably increased in renal impairment. Furosemide crosses the placental barrier and is distributed into breast milk. The clearance of Furosemide is not increased by haemodialysis.
Injection: Absorption: Furosemide (Kenzamide) is readily absorbed from injection site. The onset of diuresis following intravenous administration is within 5 minutes and somewhat later intramuscular administration.
Blood concentration: The peak effect occurs within the first half hour. The duration of diuretic effect is approximately 2 hours.
Half-life: Peak plasma concentrations increase with increasing dose but times-to-peak do not differ among doses. The terminal half-life of is approximately 2 hours.
Protein binding: Plasma concentrations ranging from 1 to 400 mcg/ml are 91 to 99% bound in healthy individuals. The unbound fraction averages 2.3 to 4.1% at therapeutic concentration.
Excretion: It is mainly excreted in the urine; largely unchanged variable amounts are also excreted in the bile, non-renal elimination being considerably increased in renal failure.