Krokodil—Morphine’s Deadly Derivative

Abstract

Graphically publicized in the media, the use of Krokodil, a heroin-like morphine derivative, has grown in Eastern Europe the last decade. The popularity of the injectable drug has grown in part due to its inexpensive and simple manufacturing process through the use of codeine tablets. Krokodil has a similar mechanism of action to morphine, although it is said to be as much as 10 times more potent and is notorious for plaguing its victims with rotting, scale-like skin lesions. The drug was originally synthesized in hopes of creating a safer, less addictive alternative to morphine, however its impure manufacturing process, toxicity and addiction profile led to abuse and infection among its users. The use of Krokodil is seen most commonly in the Ukraine and Russia, particularly in Siberia, however use has been recorded in Moscow and 27 other Russian cities, Kiev and 24 other Ukrainian cities, Kazakhstan, and other Kazakh regions bordering Russia. Use has not yet been confirmed in the United States despite several reports due to the difficulty in isolating and discerning various metabolites in test samples. Various attempts have been made in Eastern Europe in recent years to halt its production by restricting access to codeine, however without concrete legislation and increased public awareness, it is unclear if the growing Krokodil epidemic will be contained.

Lethal endomyocarditis caused by chronic “Krokodil” intoxication

“…"Krokodil" or "Russian Magic" is the street name of a home-made injectable drug used as a cheap substitute for heroin, which was introduced in Russia, Ukraine and the other former Soviet countries in the first years of the 21 st century [1,2]. Its name refers to the scaly rotten appearance of users' skins after multiple injections, as well as untreated skin and soft tissue infections, that causes them to resemble a crocodile skin [3,4]. Krokodil use spread because of the easy availability of the materials, which can be purchased in supermarkets, chemist's shops and hardware stores [2].…”

DARK Classics in Chemical Neuroscience: Krokodil

“…Desomorphine binds primarily to μ-opioid receptors and to a lesser extent to the κ- and δ-opioid receptors. , Desomorphine presents opioid-like pharmacological properties as an analgesic and sedative. Its sedative activity is 15 times more potent than that of morphine. ,, …”

“…Nevertheless, the absence of the hydroxyl group in desomorphine makes it more toxic and more of a convulsant . Desomorphine is known to be 3 times more toxic than morphine. ,, For subcutaneous inoculation, the LD 50 of desomorphine in mice is 27 mg/kg, compared with 400 mg/kg for morphine. , …”

“…Its sedative activity is 15 times more potent than that of morphine. 7,34,46 Eddy and Howes were the first to describe the pharmacological properties of desomorphine in studies aiming to find a suitable substitute for morphine in the treatment of moderate to severe pain. 34 Desomorphine was found to be 10 times more potent than morphine (1 mg of desomorphine caused similar effects as 10 mg of morphine) and apparently was entirely devoid of emetic effect and exhibited very little convulsant action.…”

“…36 Desomorphine is known to be 3 times more toxic than morphine. 7,36,46 For subcutaneous inoculation, the LD 50 of desomorphine in mice is 27 mg/kg, compared with 400 mg/kg for morphine. 2,7 ■ METABOLISM OF DESOMORPHINE Desomorphine is not a new substance and was in the market for more than 10 years.…”