Monograph: |
Sulphamethizole
Almost odourless, white or yellowish-white crystalline pow-
der or crystals.
Soluble I in 2000 of water, I in 38 of alcohol. I in 13 of
Acetone and I in 1900ofchloroformandofether;itdissolves
in solutions of alkali hydroxides and in dilute mineral acids.
Protect from light.
Adverse Effects, Treatment, and Precautions
As for Sulphamethoxazole.
Sulphamethizole and its acetyl derivative are rela-
tively soluble in urine, and the risk of crystalluria is
quite low, but an adequate fluid intake should gener-
ally be maintained.
Interactions
As for Sulphamethoxazole.
Antimicrobial Action
As for Sulphamethoxazole.
Pharmacokinetics
Sulphamethizole is readily absorbed from the gas-
tro-intestinal tract: about 90% has been reported to
he bound to plasma proteins, its half-life has been
reported to range from about 1.5 to 3 hours. It is only
slightly acetylated in the body and is rapidly excret-
ed. about 60% of a dose being eliminated in the
urine in 5 hours and around 90% within 10 hours.
Sulphamethizole and its acetyl derivative are readily
soluble in urine over a wide pH range. Only low
concentrations are achieved in blood and tissues be-
cause of its rapid excretion.
Uses and Administration
Sulphamethizole is a short-acting sulphonamide
that is given by mouth in the treatment of infections
of the urinary tract, sometimes in combination with
other antibacterials: it is unsuitable for the treatment
of systemic infection since only relatively low con-
centrations of drug are achieved in the blood and tis-
sues.
It is given in adult doses of 1.5 to 4 g daily in 3 to 4
divided doses. A suggested dose for children is 30 to
45 mg per kg body-weight daily in 4 divided doses.
Sulphamethizole monoethanolamine has also been
used.
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