Meperidine analog

Langston, J. W., Ballard, P., Tetrud, J. W. and Irwin, I. Chronic Parkinsonism in humans due to a product of meperidine-analog synthesis. Science 219 979-980,1983. 

Alexander Sasha" Shulgin (1925- ) Meperidine Analogs Phencyclidine Analogs GHB and Rohypnol Guesses and Risks... 

Diphenoxylate is a synthetic meperidine analog with little or no analgesic activity. However in high doses it shows opioid activity such as euphoria and a morphine-like physical dependence after chronic administration. Its insolubility however, in aqueous solution prevents parenteral abuse. Nevertheless, diphenoxylate has in most countries been replaced by loperamide. 

Brand Namefs) Lomocot, Lomotil, Lonox, Vi-Atro Chemical Class Meperidine analog... 

Reports in the early 1980s of a rapidly progressive form of parkinsonism in young persons opened a new area of research in the etiology and treatment of parkinsonism. The initial report described apparently healthy young people who attempted to support their opioid habit with a meperidine analog synthesized by an amateur chemist. 

Davis GC, Williams AC, Mai key SP, Ebert MH, Caine ED, Reichert CM, Kopin IJ (1979) Clri onic pai kinsonism secondar-y to inti ave-nous mjection of meperidine analogs. Psychiatiy Res 1 249—254. 

The considerable number of meperidine analogs prepared and tested showed that other than ester reversal, changes at position 4 usually abolished or decreased activity. An exception, wherein the ester function was altered to ketone and meta hydroxyl added to the phenyl ring, was ketobemidone (Fig. 5-10D), whose potency over meperidine increased five- to sixfold. However, as with molecular improvements of other opiatelike compounds, addiction liability increased as well. 

It has been possible to produce a balanced type of anesthesia wherein low-potency N20 is combined with an opioid analgesic, usually the meperidine analog fentanyl (Fig. 5-10), or the more recent analogs sufentanil and alfentanil. When a butyrophenone-type neuroleptic (see later), particularly droperidol, is added, a state of neuroleptoanesthesia is produced where, without loss of consciousness, analgesia sufficient for surgery is achieved during which the patient still responds to commands.6... 

E. Antidiarrbeal Agents The most effective antidiarrheal drugs are the opioids and derivatives of opioids that have been selected for maximal antidiarrheal and minimal CNS effect. Of the latter group, the most important are diphenoxylate and loperamide, meperidine analogs with very weak analgesic effects. Difenoxin, the active metabolite of diphenoxylate, is also available as a prescription medication. Diphenoxylate is formulated with antimuscarinic alkaloids to reduce the already minimal likelihood of abuse loperamide is formulated alone and sold over the counter as such. 

The benzomorphan-prodine hybrid IXa was more like prodine than a typical benzomorphan It would support morphine dependence in the monkey, in contrast to a previous benzomorphan-meperidine hybrid (IX-b). The stereoisomers of the phenylmorphan X behaved like benzomorphans rather than meperidine analogs. ... 

J. Meperidine Analogs - WY-22811 (VI) and both of its optical Isomers were some diat more potent analgesics than pentazocine, and both antagonized morphine, the (-) isomer being the more potent. Side effects were minimal. 

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