Sulfadiazin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R22:Gesundheitssch?dlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R42/43:Sensibilisierung durch Einatmen und Hautkontakt m?glich.
S-S?tze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Chemische Eigenschaften
White to slightly yellow crystalline pow
Verwenden
It is used in the form of silver salts (sulfadiazine silver) as an external antibacterial
agent, primarily for treating burns. It is believed that the presence of the silver ion in the
molecule facilitates increased antimicrobial and wound-healing action.
Definition
ChEBI: A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.
Antimicrobial activity
Sulfadiazine is somewhat more active than other sulphonamides.
Allgemeine Beschreibung
Sulfadiazine’s plasma half-life is 17 hours. It is a white,odorless crystalline powder soluble in water to the extentof 1:8,100 at 37°C and 1:13,000 at 25°C, in human serumto the extent of 1:620 at 37°C, and sparingly soluble in alcoholand acetone. It is readily soluble in dilute mineralacids and bases. Its pKa is 6.3.
Pharmazeutische Anwendungen
Sulfadiazine is almost insoluble in water and unstable on
exposure to light. It is administered orally or, as the sodium
salt, by intravenous injection. It is a component of several
multi-ingredient preparations. Its low solubility in urine led
to its general replacement by other compounds. The intravenous
solution is highly alkaline and should not be given by
any other route.
Pharmakokinetik
Oral absorption： Very good
C
max 3 g oral： c. 50 mg/L after 3–4 h
Plasma half-life ：7–12 h
Volume of distribution： 0.36 L/kg
Plasma protein binding： c. 40%
Absorption and distribution
Adequate blood concentrations are easily achieved and
maintained after oral administration. It is well distributed
and penetrates in therapeutic concentrations into
the CSF, but because of resistance it is no longer the
drug of choice in meningitis. It crosses the placenta and
enters breast milk to achieve concentrations around 20%
of plasma levels.
Metabolism and excretion
Sulfadiazine is subject to acetylation in the liver. The acetyl
derivative lacks antibacterial activity and is excreted more
slowly (half-life 8–18 h). Parent compound and metabolite
are both excreted mainly by glomerular filtration.
Clinical Use
Urinary tract infection
Nocardiasis
Chancroid
Toxoplasmosis (in combination with pyrimethamine)
Meningococcal infections
Prophylaxis of rheumatic fever
Nebenwirkungen
In addition to side effects common to the group, sulfadiazine
inhibits the metabolism of phenytoin. The risk of crystalluria
can be reduced by high fluid intake and alkalization of
the urine.
Sicherheitsprofil
Poison by intravenous route. Moderately toxic by ingestion and intraperitoneal routes. Human systemic
effects by ingestion: hematuria, anuria, general anesthesia, gastrointestinal effects. Experimental teratogenic and reproductive effects. When heated to decomposition it emits very toxic fumes of NOx and SOx.
Sulfadiazin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
