Sulfamethizole

(BAN, rINN)
Sulfamethizole Chemical formula
Synonyms: Sulfaméthizol; Sulfamethizol; Sulfamethizolum; Sulfametitsoli; Sulfametizol; Sulfametizolas; Sulphamethizole; Szulfametizol. N 1 -(5Methyl-1,3,4-thiadiazol-2-yl)sulphanilamide.
Cyrillic synonym: Сульфаметизол.

💊 Chemical information

Chemical formula: C9H10N4O2S2 = 270.3.
CAS — 144-82-1.
ATC — B05CA04; D06BA04; J01EB02; S01AB01.
ATC Vet — QB05CA04; QD06BA04; QJ01EQ02; QS01AB01.

Pharmacopoeias.

In Eur., Jpn, and US.

Ph. Eur. 6.2

(Sulfamethizole). White or yellowish-white crystalline powder or crystals. Very slightly soluble in water; sparingly soluble in alcohol; soluble in acetone. It dissolves in dilute solutions of alkali hydroxides and in dilute mineral acids. Protect from light.

USP 31

(Sulfamethizole). Practically odourless, white crystals or powder. Soluble 1 in 2000 of water, 1 in 38 of alcohol, 1 in 13 of acetone, and 1 in 1900 of chloroform and of ether; freely soluble in solutions of ammonium, potassium, and sodium hydroxides; soluble in dilute mineral acids; practically insoluble in benzene. Protect from light.

💊 Adverse Effects, Treatment, and Precautions

As for Sulfamethoxazole. Sulfamethizole and its acetyl derivative are relatively soluble in urine, and the risk of crystalluria is quite low, but an adequate fluid intake should generally be maintained.

💊 Interactions

💊 Antimicrobial Action

💊 Pharmacokinetics

Sulfamethizole is readily absorbed from the gastrointestinal tract; about 90% has been reported to be 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 excreted, about 60% of a dose being eliminated in the urine in 5 hours and around 90% within 10 hours. Sulfamethizole and its acetyl derivative are readily soluble in urine over a wide pH range. Only low concentrations are achieved in blood and tissues because of its rapid excretion.

💊 Uses and Administration

Sulfamethizole is a short-acting sulfonamide that is given orally in the treatment of infections of the urinary tract, sometimes with other antibacterials; it is unsuitable for the treatment of systemic infection since only relatively low concentrations of drug are achieved in the blood and tissues. It is given in adult doses of 1.5 to 4 g daily in 3 or 4 divided doses. A usual dose for children is 30 to 45 mg/kg daily in 4 divided doses. Sulfamethizole monoethanolamine has also been used.

💊 Preparations

USP 31: Sulfamethizole Oral Suspension; Sulfamethizole Tablets.

Proprietary Preparations

Denm.: Lucosil; Fr.: Rufol; Norw.: Lucosil†; Thai.: Luco-Oph†. Multi-ingredient: Spain: Micturol Sedante; USA: Urobiotic-250; Venez.: Bacteval.
Published May 08, 2019.