Cilastatin Sodium

(BANM, USAN, rINNM)
Synonyms: Cilastatin sodná sůl; Cilastatina sódica; Cilastatine sodique; Cilastatinnatrium; Cilastatino natrio druska; Cilastatinum natricum; Cilasztatin-nátrium; L-642957; MK-791; Natrii Cilastatinas; Natrii Cilastatinum; Natriumsilastatinaatti; Natriumsilastatinat; Silastatiininatrium; Silastatin Sodyum. (Z)-(S)-6-Carboxy-6-[(S)-2,2dimethylcyclopropanecarboxamido]hex-5-enylmonosodium salt.
Cyrillic synonym: Натрий Циластатин.

💊 Chemical information

Chemical formula: C16H25N2NaO5S = 380.4.
CAS — 82009-34-5 (cilastatin); 81129-83-1 (cilastatin sodium).

Pharmacopoeias.

In Eur., Jpn, and US.

Ph. Eur. 6.2

(Cilastatin Sodium). A white or light yellow, hygroscopic, amorphous powder. Very soluble in water and in methyl alcohol; slightly soluble in dehydrated alcohol; practically insoluble in acetone and in dichloromethane; very slightly soluble in dimethyl sulfoxide. A 1% solution in water has a pH of 6.5 to 7.5. Store at a temperature not exceeding 8° in airtight containers.

USP 31

(Cilastatin Sodium). A white to tan-coloured powder. Soluble in water and in methyl alcohol. pH of a 1% solution in water is between 6.5 and 7.5. Store at a temperature less than 8°.

💊 Profile

Cilastatin is an inhibitor of dehydropeptidase I, an enzyme found in the brush border of the renal tubules. It is given as the sodium salt with the antibacterial imipenem to prevent its renal metabolism to microbiologically inactive and potentially nephrotoxic products. This increases the concentrations of imipenem achieved in the urine and protects against any nephrotoxic effects, which were seen with high doses of imipenem given experimentally to animals. Cilastatin has no antibacterial activity itself, and does not affect the antibacterial activity of imipenem.

💊 Preparations

USP 31: Imipenem and Cilastatin for Injectable Suspension; Imipenem and Cilastatin for Injection.

Proprietary Preparations

Pol.: Tienam. Multi-ingredient: Arg.: Dixabiox; Imipecil; Imistatin; Klonam†; Zienam; Austral.: Primaxin; Austria: Zienam; Belg.: Tienam; Braz.: Penexil†; Tienam; Canad.: Primaxin; Chile: Inem; Tienam; Cz.: Tienam; Denm.: Tienam; Fin.: Tienam; Fr.: Tienam; Ger.: Zienam; Gr.: Primaxin; Hong Kong: Prepenem; Tienam; Hung.: Tienam; India: Cilanem; Indon.: Pelastin; Tienam; Israel: Tienam; Ital.: Imipem; Tenacid; Tienam; Malaysia: Bacqure; Tienam; Mex.: Arzomeba; Iminen; Tienam; Neth.: Tienam; Norw.: Tienam; NZ: Primaxin; Philipp.: Anipen; Tienam; Port.: Tienam; Rus.: Tienam (Тиенам); S.Afr.: Tienam; Singapore: Tienam; Spain: Tienam; Swed.: Tienam; Switz.: Tienam; Thai.: Tienam; Turk.: Tienam; UK: Primaxin; USA: Primaxin; Venez.: Zienam.
Published January 21, 2019.