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Glutethimide
Systematic (IUPAC) name
3-ethyl-3-phenyl-piperidine-2,6-dione
Identifiers
CAS number 77-21-4
ATC code N05CE01
PubChem 3487
DrugBank N/A
Chemical data
Formula C13H15NO2 
Mol. mass 217.264 g/mol
Pharmacokinetic data
Bioavailability Variable
Metabolism Hepatic
Half life 10-12 hours
Excretion Renal:2%
Fecal:2%
Lactic (in lactiferous females)
Therapeutic considerations
Pregnancy cat. C: (USA)
Legal status Schedule II
Routes Oral
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Glutethimide is a hypnotic sedative that was introduced in 1954 as a safe alternative to barbiturates to treat 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.

Glutethimide DOJ.jpg

Contents

Long term use

Long term use may cause toxic effects which resemble those seen in withdrawal in patients who are still taking a stable dose of the drug. The symptoms include delirium, hallucinosis, convulsions and fever.[1]

Recreational use

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(though these combinations produce severe constipation). 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 - a combination of Tylenol #4 - acetaminophen with 60mg of codeine - and Doriden, a trade name of glutethimide tablets, taken to achieve a similar effect to stronger opioids such as heroin, morphine, fentanyl, and oxycodone.

Glutethimide is a CYP450 inducer that increases the degree of conversion of codeine to morphine (the active metabolite of codeine - a prodrug with no intrinsic activity), in vivo, by approximately a factor of three, increasing the average degree of codeine metabolized to morphine from 10% to 30% (thus increasing the activity of codeine by roughly 300%) - while synergistically adding to the depressant effects of the codeine.

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).[citation needed]

Legal status

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.

See also

References

  1. ^ Cookson JC (September 1995). "Rebound exacerbation of anxiety during prolonged tranquilizer ingestion". J R Soc Med 88 (9): 544. PMID 7562864. 







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