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Glutethimide

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Glutethimide chemical structure
Glutethimide

3-ethyl-3-phenyl-piperidine-2,6-dione
IUPAC name
CAS number
77-21-4
ATC code

N05CE01

PubChem
3487
DrugBank
N/A
Chemical formula {{{chemical_formula}}}
Molecular weight 217.264 g/mol
Bioavailability Variable
Metabolism Hepatic
Elimination half-life 10-12 hours
Excretion Renal:2%
Fecal:2%
Lactic (in lactiferous females)
Pregnancy category C: (USA)
Legal status Schedule II
Routes of administration Oral


Glutethimide is one of the carbamates, a central nervous system depressant.

Introduced in 1954 it was used as a hypnotic sedative that was as a safe alternative to barbiturates to treat anxiety and insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similarly severe withdrawal symptoms. Doriden is the brand-name version of the drug; both the generic and brand-name forms are rarely prescribed today.

File:Glutethimide DOJ.jpg

EtymologyEdit

The name Glutethimide is derived from its chemical name glut(aryl) + eth(yl) +imide.

Legal statusEdit

Glutethimide is a Schedule II drug under the Convention on Psychotropic Substances.[1] It was originally a Schedule III drug in the United States under the Controlled Substances Act, but in 1991 it was upgraded to Schedule II, more than a decade after recreational abusers discovered that combining the drug with codeine produced a euphoria which closely resembles that obtained from heroin.

A question has appeared on the DABT examination (www.abtox.org) on Glutethimide.

Recreational drug useEdit

Glutethimide is a CYP2D6 enzyme inducer. When taken with codeine, it enables the body to convert higher amounts of the codeine (higher than the average 5 - 10%) to morphine. The general sedative effect also adds to the power of the combination. In these respects, glutethimide is a stronger booster of codeine and related opioids than is promethazine (Phenergan®, Phenergan VC With Codeine® cough syrup, Atosil® and many others), an antihistamine used clinically and to some extent non-clinically for the very same purpose. These two drugs are alone amongst known opioid potentiators as having the CYP2D6 enzyme inducer effect. Somewhat more common are drugs which reduce the enzyme levels, including cimetidine and white grapefruit juice, which intensifies and prolongs the effects of most opioids with codeine and ethylmorphine being the most-commonly encountered exceptions. The remainder of the potientiators in common use, including hydroxyzine, carisoprodol, and diazepam (metabolism of which is also impacted by tbe CYP2D6 enzyme system) work in the second way mentioned, by increasing the effects of the drugs on the central nervous system. Combining this with a possible third mode of action is tripelennamine, which is also used with codeine, morphine, and pentazocine for its unique effects -- especially in the latter case, known as "T's and Blues" amongst other names.

The street name for a combination of Doriden and Codeine #4 pills is a "load", a "pack", or "doors and fours". Combined with certain cough medicines, they are "D's", as in A/C and D's, referencing a Robotussin product with codeine, and "Pancakes", as in Pancakes and Syrup (Glutethimide and codeine based cough syrup).[How to reference and link to summary or text]

See alsoEdit


Sedatives edit

(Methaqualone) (Ethchlorvynol) (Chloral Hydrate) (Meprobamate) (Glutethimide) (Methyprylon) (Gamma-hydroxybutyrate) (Gamma-butyrolactone) (Propofol)





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