Source: Marketing Authorisation Holder Revision Year: 2021 Publisher: Alphapharm Pty Ltd, Level 1, The Bond, 30-34 Hickson Road, Millers Point NSW 2000, www.mylan.com.au
Furosemide (frusemide) is an anthranilic acid derivative. Furosemide (frusemide) is a potent diuretic. It inhibits sodium and chloride absorption in the ascending Limb of Henle’s Loop and in both the proximal and distal tubules. The high degree of efficacy is due to this unique site of action. The action on the distal tubule is independent of any inhibitory effect on carbonic anhydrase or aldosterone. Furosemide (frusemide) may promote diuresis in cases which have previously proved resistant to other diuretics.
Furosemide (frusemide) has no significant pharmacological effects other than on renal function.
No data available.
Furosemide (frusemide) is rapidly absorbed from the gastrointestinal tract. Absorption rates in healthy subjects have been reported from 60 to 69%, and from 43 to 46% in patients with end stage renal failure.
The onset of diuresis following oral administration is within 1 hour. The peak effect occurs within the first or second hour. The duration of diuretic effect is 6 to 8 hours. Peak plasma concentrations of frusemide increase with increasing dose, but times to peak do not differ among doses.
Furosemide (frusemide) is extensively bound to plasma proteins, mainly to albumin. Plasma concentrations ranging from 1 to 400 µg/mL are 91 to 99% bound in healthy individuals. The unbound fraction averages 2.3 to 4.1% at therapeutic concentrations.
Recent evidence suggests that furosemide (frusemide) glucuronide is the only, or at least the major, biotransformation product of furosemide (frusemide) in man.
In patients with normal renal function, approximately 80% of an intravenous or intramuscular dose is excreted in the urine within 24 hours. Urinary excretion is accomplished both by glomerular filtration and proximal tubular secretion, which accounts for roughly 66% of the ingested dose, the remainder being excreted in the faeces. A small fraction is metabolised by cleavage of the side chain.
Furosemide (frusemide) has a biphasic half life in the plasma with t1/2 ranging up to 100 minutes; t1/2 is prolonged by renal and hepatic insufficiency and in newborn infants.
No data available.
No data available.
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