Journal of Labelled Compounds and Radiopharmaceuticals
SEDATIVES AND HYPNOTICS |authorSTREAM
The glucuronidationof bile proceeds in two steps: first glucuronic aid (GA) issynthesized from cytosolic glucose that is complexed with uridinediphosphate (UDP)ad forms udpglucuronic acid (UDPGA). From this compound, the glucuronicacid is transferred to blirubin. The first reaction is catalyzed by a UP-glucose dehydrogenate, the second reaction is catalyzed by bilirubin- DUGAN- transferees that is synthesized by microsomes. Any deficiency ofthese two enzymes will result in defective conjugation and elimination ofbilirubin. On the other end, administration of microsomal enzyme inducers suchas phenobarbital, glutethimide and antipyrine favor bilirubin conjugation andelimination by increasing blirubin transferase activity. Conjugation occurs inthe endoplasmic reticulum and consists of forming an ester between glucuronicacid and one or both propionic side-chains of bilirubin. The result will beformation of bilirubin mono and di-glucuronides. In general, about 80% ofthe di and less than 20% of the mono are formed. Human bile cotains also smallamounts of unconjugated bilirubin. In summary:
Glutethimide (Piperidinediones) Methaquolone, Ethinazone ..
Glutethimide is a enzyme inducer. When taken with ,"hits", "cibas and codeine ", it enables the body to convert higher amounts of the codeine (higher than the average 5 - 10%) to . The general sedative effect also adds to the effect of the combination. It produces an intense euphoria similar to IV heroin use. The effect was also used clinically, including some research in the 1970s in various countries of using it under carefully monitored circumstances as a form of oral opioid agonist substitution therapy, e.g. as a that may be a useful alternative to methadone. The demand for this combination in Philadelphia, Pittsburgh, Newark, NYC, Boston, Baltimore, and surrounding areas of other states and perhaps elsewhere, has led to small-scale clandestine synthesis of glutethimide since 1984, a process that is, like methaqualone (Quaalude) synthesis, somewhat difficult and fraught with potential bad outcomes when less-than-gifted chemists are doing the deed with industrial-grade precursors without adequate quality control. The fact that the simpler clandestine synthesis of other extinct pharmaceutical depressants like , , or the oldest is not reported would seem to point to a high level of motivation surrounding a unique drug, again much like . Doriden was discontinued in the US by manufacturers in 1993. Analysis of confiscated glutethimide seems to invariably show the drug or the results of attempted synthesis, whereas purported methaqualone is in a significant minority of cases found to be inert, or contain or .